UNIT 1

Introduction to
Pharmacognosy

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 Pharmacognosy is derived from two Greek words, Pharmakon & Gnosis wherein Pharmakon means “drug” and Gnosis means
“knowledge”. It is a study of drugs that originate in the plant & animal kingdoms. Pharmacognosy is a branch of pharmacy which deals
with the basic resources of medicines from nature (plant & animal) and their uses as medicaments from ancient time to present day. In
short, pharmacognosy means “knowledge of drugs”.

At present, pharmacognosy involves not only the crude drugs but also their natural derivatives (pure compounds or
constituents). For example, digitalis leaf and its isolated glycoside, digitoxin; Rauwolfia root and its purified alkaloid, reserpine; and
thyroid gland with its extracted hormone, thyroxine, are all part of the subject matter of pharmacognosy. Therefore, pharmacognosy
may be defined as an important branch of pharmacy which deals with the study of structural, physical, chemical, biochemical and
sensory characters of natural drugs of plant and animal origin. It also includes a study of their history, distribution, cultivation, collection,
identification, preparation, evaluation, preservation, use and commerce.

How do we relate Pharmacognosy to other Sciences?

1. Botany and plant chemistry are branches of science related to study of medicinal plants
2. Pharmacy administration. Methods of procurement (obtaining) and preparation of drugs affect the price. As far as economic is
concerned, pharmacognosy is associated with the phases of pharmacy administration that deals with prescription pricing.
3. Dispensing pharmacy and clinical pharmacy. Because of the pharmacist’s knowledge of drug constituents, he is able to predict
not only the chemical and physical incompatibilities encountered in compounding, now manufacture, but also the therapeutic
incompatibilities that the patient may encounter.
4. Pharmacology is an outgrowth of materia medica, the ancient science that dealt with all aspects of medicinal agents. While
pharmacognosy deals with information on the sources and constituents of natural drugs, pharmacology is focused with their
actions and effects.
5. Medicinal chemistry is the science that deals with the discovery or design of new therapeutic chemicals and their development
into useful medicines. It may involve synthesis of new compounds, investigations of their relationships between the structure of
natural or synthetic compounds and their biological activities, elucidations of their interactions with receptors of various kinds,
including enzymes and DNA, the determination of their absorption, transport, and distribution properties, and studies of the
metabolic transformations of these chemicals into other chemicals. (https://chem.libretexts.org/)

What are the fields of Pharmacognosy?

1. Medical ethnobotany is the study of medicinal plants used by a group of people.

2. Ethnopharmacology is the study of medicines (pharmacological properties) derived from naturally occurring substances like
plants and fungi that have been traditionally used by specific groups of people for medicinal purposes. (https://study.com/)
3. Phytotherapy is commonly defined as the study of the use of extracts of natural origin as medicines or health-promoting agents.
(Seed to Patient in Clinically Proven Natural Medicines; Dilip Ghosh, in Nutraceuticals, 2016)
4. Phytochemistry is the study of phytochemicals, which are chemicals derived from plants.

History of Pharmacognosy

Contributions

Theophrastus Father of Botany Historia plantarum

Dioscorides The first pharmacognosist De materia medica

Ancient Egyptian period • The ancient Egyptians 3000 B.C. were experts in using drugs for curing diseases
• Papyrus ebers: scroll containing medicinal used of plants and animals

Old Indian Medicine • The "Riveda" and Ayurveda (Acoko 2000 B.C.), contained the sacred medicinal plants.
• The collection of plant materials was done only by an innocent, pure, religious person.
• The fresh plants were considered to be the most effective.

The Old Chinese Medicine • The Pen Ts'ao Kang Moa 1000 B.C. contained an incredible number of medicinal plants
and drugs of animal origin.
• Opium is a very old Chinese drug for diarrhea and dysentery.

The Greek and the Romans • Pythagoras (560 B.C.) used drugs as Mustard and Squill, etc.

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 • Dioscorides, a Greek physican who lived in the first century A.D. wrote “De Materia
Medica” in 78 A.D. in which he described about 600 plants that were known to have
medicinal properties
• Galen (134- 200 A.C.) was a physician and to him is ascribed the use of "Galenical
preparations".

In the Philippines • The use of plants as medicine is long engrained on our culture, in particular by the
“herbolarios”, for reasons of availability and affordability

Few Natural Substances Discovered

Substances Use/s

Isolation of morphine from opium This medication is used to treat severe pain Papaver somniferum

Strychnine (1817) Strychnos nux vomica Used as a pesticide, particularly for killing small vertebrates such as birds and rodents.

Quinine and caffeine (1820) Quinine is a common treatment for malaria

Nicotine (1828) Used for smoking cessation to relieve withdrawal symptoms

Atropine (1833) Belladona A prescription medicine used to treat the symptoms of low heart rate (bradycardia),
reduce salivation and bronchial secretions before surgery

Cocaine (1855) Erythroxylum coca A powerfully addictive stimulant drug

Drugs and Technical Products

Crude drugs vegetable and animal drugs that consists of natural substances that have undergone only the
process of collection and drying
dried, unprepared material of plant, animal, or mineral origin used for medicine

Crude any product that has not been advanced in value or improved in condition by shredding,
grinding, chipping, crushing, distilling, evaporating, extracting, artificial mixing with other
substances or by any other process or treatment beyond what is essential to its proper packing
and to the prevention of its decay or deterioration pending manufacture.

Natural Substances found in nature including whole plant and herbs, their anatomical parts, extracts, secretions and
other constituents, whole animal, their parts, organs, secretions etc; does not undergo several
processes

Synthetic drug one that has been chemically altered or created in order to form the correct compound

Organic drug one that is found in nature that does not require chemical changes to have an effect on the body

Geographic source and habitat the region in which a plant and animal yielding the drug grows

1. Indigenous - expected to grow in local regions

2. Naturalized - grow in native regions other than their native homes

Preparation of Drugs for Commercial Market

A. Cultivation and Time and season affect the quality and quantity of a drug
Collection

1. Rainfall: plants containing alkaloids, glycosides and even volatile oils have low yield due to water
soluble components

2. Day light: a factor that helps determine the amount of glycosides or alkaloids such as belladonna
(Atropa belladonna) and stramonium (Datura stramonium) aka Devil’s trumpet or Devil’s weed of
Fam. Solanaceae (anticholinergic)

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 3. Altitude: coconut and sugar cane are lowland plants while tea, cocoa, coffee and cinchona
require elevation

4. We always choose the most advantageous collection time

5. We collect them on conditions with their highest content of active principles

6. The material must be dried to give the maximum quality and appearance

7. Ontogeny gives us the idea that the concentration of the active constituent varies on stage of
development

8. Morphine from Papaver somniferum is highest at 2 1/2 -3 weeks after flowering

Rules for collection 1. Roots and rhizomes are collected at the end of the vegetation period, i.e. usually in the autumn. In
most cases they must be washed free of adhering soil and sand.
❖ October to February-peak of storing food in the underground parts

2. Bark is collected in the spring; damp weather: separate easily from wood

3. Leaves and herbs are collected at the flowering stage.

4. Flowers are usually gathered when fully developed. Buds after morning dew has evaporated

5. Fruits and seeds are collected when fully ripe.

6. Leaves, flowers and fruits should not be collected when covered with dew or rain

7. Leaves and flowers are collected when fully expanded

8. Gum and resins should be collected during dry weather

B. Drying Either sun or by artificial heat and it is the most common method of preservation

Two main principles include control of temperature and regulation of air flow

It is the removal of sufficient moisture to ensure good keeping qualities and to prevent molding, the
action of enzymes, the action of bacteria and chemical or other possible changes.

Enzymes promote various chemical changes in the other cell constituents, e.g. by oxidation or hydrolysis
occurring normally in aqueous solution

It facilitates grinding and milling and converts the drug into a more convenient form for commercial
handling

Living plant material has a high-water content: leaves may contain 60-90% water, roots and rhizomes 70-
85%, and wood 40-50%. The lowest percentage, often no more than 5 to 10%, is found in seeds.

The air temperature is kept at 20-40 °C for thin materials such as leaves, but is often raised to 60-70 °C for
plant parts that are harder to dry, e.g. roots and barks.

Rapid drying helps flowers and leaves to retain their color and aromatic drugs their aroma

Curing is a special drying process to bring about changes in the constituents

C. Garbling Final step in the preparation of crude drug

Consist of removal of extraneous matter such as other parts of the plant, dirt, and added adulterants
Could be done during collection but should be done after drying

D. Packaging, Storage Wrong means of packaging, storage and preservation will lead to low quality and inactive constituents
and Preservation

The packaging must provide ample protection (insect attacks) to the drug and gives the economy of
space

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 There should be low humidity (below 10% moisture for packaging and storage), well ventilated, spacious
storage area. Dry drugs must be stored in tightly-sealed container and protected from daylight

In the fumigation of large lots of crude drugs, use methyl bromide

Drugs containing glycosides and esters are usually less stable than those containing alkaloids.

Drugs with essential oils deteriorate rather quickly through evaporation, oxidation and polymerization

Tannins on the other hand, have an almost unlimited durability.

Preservation maintains the quality unchanged during transport and storage.

Wrong means of packaging, storage and preservation will lead to low quality and inactive constituents

The packaging must provide ample protection (insect attacks) to the drug and gives the economy of
space

Other methods of Freeze drying/ Lyophilization: used for heat sensitive substances such as antibiotics and proteins; frozen
Preservation material is placed in the evacuated apparatus which has cold surface maintained as -60 °C to -80°C

Stabilization: used for substances susceptible to enzymatic degradation and for water sensitive
substances; prevention of degradation through destroying enzymes before drying by exposing samples in
ethanol vapors under pressure

- on long storage, enzymatic reactions will completely destroy the constituents because the last traces of
water can never be removed;

Fermentation: increasing enzymatic activity by increasing the temperature (30°C to 40°C) and humidity

- removes bitter and unpleasant taste to come up with more aromatic smell

- desirable enzymatic transformation of the original plant constituent

- fermented product must be dried afterwards to prevent attack by microorganism such as molds

- mainly applied to drugs which are used as spices and stimulant such as vanilla, tea and cocoa

Official VS Unofficial Drugs VS Nonofficial

Official • One which is listed and described in a book recognized by the government as the legal authority for standards
"Pharmacopoeia” such as USP, BP, JP
• Examples: Metformin as hypoglycemic agent, Celebrex as anti-inflammatory

Unofficial • A drug which has been recognized earlier in the pharmacopoeia or in national formulary or in recognized books
but not found in the current issue is designated as an ‘unofficial drug’. Those substances were excluded from the
recognized books due to their severe toxic effects on humans.
• Example: Sucralfate (hyperacidity), mercurial compounds (diuretics), benzoic acid (preservative) etc.

Nonofficial • Substance that has never been appeared in either of the official books may be called nonoffical.
• Such types of compounds may be published in current journals having proven clinical value, but we do not know
about their side effects.
• For example - Curcumin (sinusitis), etc.

How do we evaluate crude drugs?

The evaluation of a drug involves a number of methods, which may be classified as follows: 1. Organoleptic 2. Microscopic 3.
Biological 4. Chemical 5. Physical

Definition of Terms

Evaluate To identify a drug and determine its quality and purity, and detection of nature of adulteration

Quality Refers to the intrinsic value of the drug, i.e. the amount of medicinal principles or active constituents present

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 Types of Crude Drug Evaluation

1. Organoleptic/ • Means the study of a drug with the help of organs of sense
Morphological • Includes any drug’s macroscopic or external appearance, color, odor, taste, feel of drug to touch and
sounds of its snap or fracture
• The macroscopic or external characteristic of a drug may be divided into 7 headings - 1. Shape 2. Size 3.
Color 4. Fracture & internal color 5. Odor 6. Taste

2. Microscopic • Can be done in the laboratory by the use of microscopes and utilizes various microscopic characters of
the drugs, such as types and arrangement of various cells and tissues.
• Essential to study adulterants in powered drugs and in identification of pure powdered drugs
• Very fine sections are selectively subjected to staining reactions with various staining reagents for the
study of chemical nature of cellular organization

Staining techniques and reagents:

• Phloroglucinol and hydrochloric acid for lignified tissues (lignin in cell walls that makes it woody in nature)
• Chlor-zinc iodide reagent for cellulosic tissues (structural polysaccharide in cell wall)
• Tincture of alkannol for cuticularized walls (cuticle in plants-film protecting the epithelial cells)
• Ruthenium red for gums and mucilages containing cells

3. Biologic • very useful in determining the pharmacological activity of the drug.

Evaluation • Since living organism or their isolated living tissues are used, this method is also called the biological
method or bioassay.
• Many drugs, particularly the antibiotics, toxins and toxoids and also vitamins are assayed by this method.
• Involves using an intermediate in vivo or in vitro tissue or cell model under controlled conditions

Bioassay: assay of the pharmacologically active substance by using biological means yield valuable
information about the potency of the drug

4. Chemical • Involves both qualitative and quantitative determination of their active principles.
Evaluation • In this method characteristic qualitative chemical tests are employed to identify crude drugs and their
constituents:
o Checking the color reactions present leads to possible identity of the substance and
adulteration
• Involves isolation, purification and identification of active ingredients
• “Preliminary Phytochemical Screening” is a part of chemical evaluation for establishing chemical profile
of a drug

5. Physical • Accomplished by the determination of various physical characteristics using various physico-chemical
Evaluation techniques
• Example: specific gravity (of fats and volatile oils), melting points (of alkaloids), optical rotation (of
alkaloid and volatile oils) and
o ash values: to judge the identity and purity of the crude drug ¼ represent inorganic substances
o moisture content: helps prevent degradation of product

How do we classify drugs in the context of pharmacognosy?

1. Morphology • In this system, the drugs are grouped according to the part of the plants, such as roots, leaves, stems,
barks, flowers, seeds etc.
• The drugs obtained from the direct parts of the plants are called as organized drugs. They are made
up of whole plants or any parts derived from them. eg., Root – Rauwolfia, aconite, ginger; Bark –
Cinnamon, Cinchona
• The drugs which are prepared from plants by some intermediate physical process such as incision,
drying or extraction with a solvent are called unorganized drugs, eg., Dried juice (Aloe juice), Dried
extract (agar), Dried latex (Opium latex)

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 • Disadvantage: there is no co-relation of chemical constituents with the therapeutic actions.

2. Taxonomic • In this system crude drugs are arranged according to the natural groups (e.g. Families) of their source.
classification Large number of plant families share distinguishable properties.
• Example: all the drugs obtained from Solanaceae are grouped together as Solanaceous drugs.
Tropane alkaloids are the main constituents of Solanaceous drugs. Other examples are:
o Glycyrrhiza glabra (glabrous = smooth)
o Piper nigrum (= black)
o Hyoscyamus muticus (muticus = short)
o Digitalis purpurea (= purple)

3. Pharmacologic or • Drugs are grouped according to their therapeutic use.

Therapeutic • Examples:
Classification o Cardiotonic drugs: digitalis
o Purgative drugs: castor oil
o Anticholinergic agents: atropine, hyoscyamine
o Counter irritants: methyl salicylate, camphor, capsicum
o Vasodilators: reserpine and ergotamine

4. Chemical • The biological activity of a drug is due to the presence of certain chemical constituents in the drug.
classification • Plants and animals synthesize chemical compounds such as carbohydrates, protein, fat, volatile oils,
alkaloids, resin etc.
• The chemical classification of drugs is dependent upon the grouping of drugs with identical chemical
constituents.
• This is the basis of classification of drugs of the main reference of this module.
• Therefore, this module is also devoted to the following active constituents and drugs such as:
Carbohydrates and related compounds, Glycosides and tannins, Lipids, Volatile oils, Resins and resin
combinations, Steroids, and Alkaloids

Chemistry of Drugs

Chemical compounds give plant and animals their therapeutic properties. These chemicals are formed via processes (biosynthesis) in
living organisms. The pathways for generally modifying and synthesizing carbohydrates, proteins, fats, and nucleic acids are found to
be essentially the same in all organisms, apart from minor variations. These processes are collectively described as primary metabolism,
with the compounds involved in the pathways being termed primary metabolites.

What are the two general types of metabolism?

1. Primary Metabolism: comprises the chemical processes that every plant must carry out every day in order to survive and
reproduce its line.

Primary metabolites: compounds that are commonly produced by all plants that are directly used in plant growth and
development such as CHO, CHON, lipids, nucleic acids
• Duplication of genetic material
• Photosynthesis • Transamination
• Reproduction of cells (growth)
• Glycolysis • Synthesis of proteins and enzymes
• Absorption of nutrients
• Citric Acid Cycle (Krebs cycle) • Synthesis of coenzymes
• Synthesis of amino acids • Synthesis of structural materials

2. Secondary Metabolism: metabolic pathways that are not essential for growth, development or reproduction

Secondary Metabolites (SM): compounds that are not required for normal growth and development and are not made through
metabolic pathways common to all plants; they exert physiologic effects.

• Grouped into classes based on similar structures, biosynthetic pathways, or kind of plants that make them.

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 • Found in only specific organisms, or groups of organisms, and are an expression of the individuality of species (it’s what makes
each species unique).
• Largest classes of SM: alkaloids (nitrogen containing compounds), terpenoids (volatile oil) and phenolics (tannins)

What are active constituents (AC)?

Active constituents are compounds responsible for the therapeutic effect.

Sources Active Constituents

Talumpunay (Datura metel) Fam. Solanaceae Alkaloids: hyoscyamine, scopolamine, leaves used as anti-
asthma

Senna leaf (Cascara sagrada) Fam. Fabaceae Glycoside: Sennoside, used as laxative

Witch hazel nut (Hamamelis virginiana) Fam. Hamamelidacea Tannins: hamamelitannin, Gallic acid used as astringent

Two Classes of Active constituents

1. Pharmaceutically Active: cause precipitation or chemical changes in a medicinal preparation. Examples are:

Cinchotannic acid + iron salts Leads to precipitation

Rheotannic acid + Anthraquinone They have less gripping effect (intestinal cramps)
drugs (laxative drugs)

Rheotannic acid As an astringent from Rhubarb, cure diarrhea

The cathartic effect of rhubarb is succeeded by a mild astringency due to the rheo-tannic
acid, thus making the drug a calmative after a preliminary stimulating catharsis.

2. Pharmacologically active: responsible for the therapeutic activity of the drug

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 UNIT 2
Pharmacobiotechnology

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 Pharmaceutical biotechnology is a relatively new and growing field in which the principles of biotechnology are applied
to the development of drugs. A majority of therapeutic drugs in the current market are bioformulations, such as
antibodies, nucleic acid products and vaccines. Such bioformulations are developed through several stages that
include: understanding the principles underlying health and disease; the fundamental molecular mechanisms governing
the function of related biomolecules; synthesis and purification of the molecules; determining the product shelf life,
stability, toxicity and immunogenicity; drug delivery systems; patenting; and clinical trials. (Krishna Mallela, retrieved from
https://www.ncbi.nlm.nih.gov/)

At the end of this lesson, you should be able to

1. Define pharmacobiotechnology
2. Enumerate and describe the steps in the production of pharmacobiotechnology products
3. Determine the role of biotechnology in the production of drugs.

What is Biotechnology?
▪ It Is the technology that uses biological systems, living organisms or parts of this (organisms or enzymes) to develop
or create different products.
▪ Examples: wine and cheese-making, fermentation process that yields antibiotics, recombinant DNA technologies
▪ It was revolutionized by the advent of recombinant DNA techniques in 1973 (ability to clone human genes and
express encoded proteins in microorganism)
▪ Recombinant DNA: molecules of DNA from two different species that are inserted into a host organism to produce
new genetic combinations that are of value to science, medicine, agriculture, and industry.
(https://www.britannica.com/)
▪ Applications: use of microbes to produce useful products, tissue culture, isolated enzymes, genetically engineered
cows and goats producing foreign proteins, genetically engineered plants
▪ Herbert Boyer and Stanley Cohen (1973): Genetic material from one organism to another is replicated.

Watch the video “Biotechnology principles and processes

What is Pharmacobiotechnology?
▪ This refers to the wide application of “biotechnology” to the development of pharmaceuticals or pharmaceutically
active substances.
▪ An example of pharmacobiotechnology product is recombinant lnsulin Ely Lilly and company and in 1982 Humulin
was approved by the FDA.

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 What are the fields of Biotechnology?
1. Recombinant DNA–technology
▪ This technology permits the replication of a specific DNA sequence. It is possible when a genetic material from one
organism is artificially introduced into the genome (a genome is all genetic material of an organism) of another
organism and then replicated and expressed by that other organism

Watch the video “Recombinant DNA”

2. Molecular biology
▪ Chiefly concerns itself with understanding the interactions between the various systems of a cell, including the
interrelationship of DNA, RNA and protein synthesis and learning how these interactions are regulated.
(https://www.sciencedaily.com/)
▪ It deals with the macromolecules essential to life while biotechnology involves the manipulation of living organisms
to create useful products

3. DNA-alteration
▪ It can be acquired/somatic or as genetic mutation
▪ A mutation is a change that occurs in our DNA sequence, either due to mistakes when the DNA is copied or as the
result of environmental factors such as UV light and cigarette smoke. Mutations can occur during DNA replication if
errors are made and not corrected in time. Mutations can also occur as the result of exposure to environmental
factors such as smoking, sunlight and radiation. Often cells can recognize any potentially mutation-causing damage
and repair it before it becomes a fixed mutation. (https://courses.lumenlearning.com/)

Watch the video “DNA Alterations”

4. Gene-splicing
▪ Gene splicing is the process of chemically cutting DNA in order to add bases to the DNA strand. The DNA is cut using
special chemicals called restriction enzymes. Gene splicing is the removal of introns from the primary transcript of a
discontinuous gene during the process of Transcription. (https://www.longdom.org/)

Watch the video “Splicing mechanism and its importance”

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 5. Genetic engineering
▪ Genetic engineering is the process of using recombinant DNA (rDNA) technology to alter the genetic makeup of an
organism.

Watch the video “Genetic engineering”

6. Immunology
▪ It is a branch of biology that covers the study of immune systems in all organisms. Immunology charts, measures, and
contextualizes the physiological functioning of the immune system

Watch the video “Immune system”

7. Immunopharmacology
▪ A branch of pharmacology concerned with the application of immunological techniques and theory to the study
of the effects of drugs especially on the immune system

Let us have a few examples of biotechnology-based products

Actimmune® For chronic granulomatous disease

Betaseron® For relapsing, remitting multiple sclerosis where the immune system attacks the
protectivesheath (myelin) that co vers nerve fibers
Epogen® For treatment of anemia associated with chronic renal failure
KoGENate® For treatment of haemophilia A. It is genetic deficiency in clotting factor VIII, which causes
increased bleeding and usually affects males
Leukine® For autologus bone marrow transplantation (Autologous means obtained from the same
individual)
OncoScint® CR/OV For detection, staging and follow up of colorectal and ovarian cancer
Proleukin® For renal cell carcinoma.

Important means/processes in Biotechnology

1. Recombinant DNA
Steps:
1st Restriction enzymes cleave the DNA at particular sites
2nd enzymes known as ‘ligases’ will help to insert the cut piece of DNA (called the ‘insert’) directly into the Vector DNA
(i.e., viral DNA or plasmid).
3rd resulting vector DNA shall be capable of entering conveniently into a ‘host’ cell or otherwise called as microorganism.

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 4th once the foreign DNA (or vector DNA) gains an entry into the microorganism (i.e., host organism), it is known as a
“recombinant organism”

Recall the video “Recombinant DNA”

2. Restriction Enzymes
▪ It is also known as ‘restriction endonucleases’.
▪ It acts as a pair of “molecular scissors and is found to ‘digest’ DNA into corresponding short strands at very particular
sites

Watch the video “Restriction enzymes”

3. DNA–Ligase
▪ It is a DNA-joining enzyme. If two pieces of DNA have matching ends, ligase can link them to form a single, unbroken
molecule of DNA.
▪ The DNA pieces cut that were with the same enzyme shall possess ‘sticky ends’ which would anneal under the
appropriate and favorable conditions when such ‘pieces’ are pooled together.
▪ Mixed pieces are treated with an enzyme, termed as DNA – ligase, it will ultimately give rise to an intact piece of
recombinant DNA by the combination of phosphodiester bond (at the ends of the DNA strands) with the
complementary bases (adenine, cytosine, guanine and thymidine).

Watch the video “DNA ligation”

4. Cloning Vector
▪ This is a small piece of DNA that can be stably maintained in an organism, and into which a foreign DNA fragment
can be inserted for cloning purposes.
▪ May be a plasmid or a bacteriophage
▪ Gene having a close resemblance to a particular protein shall be joined together with a cloning vector so as to
enable it get transferred into a host cell.

Watch the video “Required characteristics of cloning vectors”

5. Hybridization Probes
▪ It refers to complementary sequence of DNA (either larger segments of DNA or synthetic oligonucleotides or even
whole plasmids) that is specifically labelled with anyone of the three different means namely:
o Radioactive substance
o Fluorescent material
o Chromogenic material

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 Watch the video “Nucleic acid hybridization and probes”

6. Cloning Process
▪ Cloning simply means to make identical copies. It is the process of generating a genetically identical copy of a cell
or an organism. Cloning happens often in nature—for example, when a cell replicates itself asexually without any
genetic alteration or recombination. Prokaryotic organisms (organisms lacking a cell nucleus) such as bacteria
create genetically identical duplicates of themselves using binary fission or budding. In eukaryotic organisms
(organisms possessing a cell nucleus) such as humans, all the cells that undergo mitosis, such as skin cells and cells
lining the gastrointestinal tract, are clones; the only exceptions are gametes (eggs and sperm), which undergo
meiosis and genetic recombination. (https://www.britannica.com/)

Watch the video “DNA cloning”

How do we relate biotechnology and modern pharmacy?

A host of modern drug substances available belong to the class of protein and peptides – these
drug substances essentially require consideration towards their stability, dosage forms, storage,
administration and lastly the probable side-effects as compared to the relatively much smaller
synthetic drug molecules

The proper selection of the recombinant products would heavily depend upon not only the correct
choice of the expression system but also the small differences existing in the structure which may
result from the use of various known expression systems

A wide range of new drug class have evolved as a result of the advent of more in-depth knowledge
of pathophysiology besides newer modes of therapies for such diseases that could not be
successfully treated earlier

A good number of ‘diagnostic products’, available in the form of ‘kits’, are solely based on
monoclonal antibody technology. They have been exclusively developed for the proper diagnosis
of thyroid disorders, anemia, fertility for pregnancy, allergies, cancer, and finally the management
of several hormone-related imbalances (i.e., disorders). In short, diagnostic products represent one
of the largest biotech startups

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 Applications

Human proteins

A. Hormones
▪ Human Insulin
o Humulin® (Eli Lily)
o Recombinant DNA technology in E. coli (1983)
o NOVO – A Danish company evolved a continuous process for the production of genetically engineered
human insulin from yeast cells instead of E. coli
▪ Calcitonin
o thyroid hormone which helps in the regulation of calcium retention in bones
o developed by Sandoz (Basel, Switzerland) with a view that the peptide could be useful in the treatment of
cardiovascular diseases (lowers blood pressure and cardioprotective)

B. Blood Products
▪ Tissue Plasminogen Activator (tPA)
o tPA is cloned into bacterial cells (E. coli). It is a serine protease that catalyzes the conversion of plasminogen
to plasmin (plasmin is responsible for the breakdown of unnecessary and unwanted blood clots
▪ Factor VIII: The genetically engineered Factor–VIII
o Cloned in hamster cells and used for the treatment of hemophilia
▪ Lymphokines
a. α-Interferon - for rare cancer hairy cell leukemia. The bone marrow makes too many B cells (lymphocytes), a
type of white blood cell that fights infection. These excess B cells are abnormal and look "hairy" under a
microscope.
b. Interleukin–2 - It is a protein that regulates the activities of white blood cells (leukocytes, often lymphocytes) that
are responsible for immunity.
c. Tumor Necrosis Factor (TNF) – It is used for killing tumor cells and causing a generalized wasting syndrome
(unwanted weight loss of more than 10 percent of a person's body weight. It is useful in cell survival, proliferation,
differentiation, and death.

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 Vaccines

Vaccines are suspension of infectious agents, or some part of them given for the purpose of establishing resistance to
an infectious disease

What are the differences between traditional vaccines and Recombinant vaccines?

Types of traditional vaccines

▪ containing living attenuated infectious organisms – example: vaccine for poliomyelitis
▪ containing infectious agents either by chemical or physical means – examples: vaccines for typhoid fever, rabies and whooping
cough
▪ containing soluble toxins of microorganisms (toxoids) – Example: vaccine used in the prevention of diphtheria and tetanus
▪ containing substances extracted from infectious agents – Example: capsular polysaccharides extracted from pneumococci.

Recombinant vaccines (or subunit vaccines)

▪ eliminate the potential vaccine-induced illness by separating effectively the immune activation function of pathogens from the
disease producing functions
▪ all the gene(s) solely dedicated for encoding the cell surface molecules that eventually trigger the immune activation function is
isolated
o these genes are removed from the pathogenic genome by endonuclease action and subsequently inserted into a
cloning vehicle that later on employed to transform either a bacterium (E. coli) or yeast (Saccharomyces cerevisiae) host
cell.

Monoclonal Antibodies (MABs)

Watch the video “How do Monoclonal antibodies work?”

Hybridoma technology - process whereby the fusion of an immortal cell with a lymphocyte to produce an immortal
lymphocyte. Antibody producing cells are duly fused with the respective tumor cells which results into the production of
a hybrid that could be grown in an appropriate laboratory culture and which reproduces antibodies of a single
specificity (monoclonal antibodies) with the longevity and reproductivity of the myeloma.

Watch the video “Production of Monoclonal antibodies by Hybridoma technology”

Examples: Pregnancy Dipstick Test, Ovulation Dipstick Test, AIDS Test.

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 DNA probes and RELP analysis

DNA probes - genetic probes makes it possible to establish future outset of some ailments for instance: emphysema and
Huntington’s disease.

Review the video “Nucleic acid hybridization and probes”

Restriction Fragment Length Polymorphism (RFLP) Analysis - Each and every human being born on this earth essentially
inherits one set of genes from its father and another one from its mother which in most cases have been found to be
identical. RELP analysis refers to the diagnosis of genetic defects prenatally. Because of RELP analysis, schizophrenia,
Alzheimer’s disease and complications of heart can be detected prenatally.

Watch the video “Restriction Fragment Length Polymorphism”

Enzyme Linked Immunosorbent Assay

(ELISA)

Watch the video “Principles of ELISA”

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 UNIT 3
Carbohydrates and
Related Compounds

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 Awareness of the importance of carbohydrates in living systems and medicine is growing due to the increasing
understanding of their biological and pharmacological relevance. Carbohydrates are ubiquitous and perform a wide
array of biological roles. Carbohydrate-based or -modified therapeutics are used extensively in cardiovascular and
hematological treatments ranging from inflammatory diseases and anti-thrombotic treatments to wound healing.
(Carbohydrates in therapeutics: Michelle Kilcoyne, Lokesh Joshi. Retrieved from https://pubmed.ncbi.nlm.nih.gov/)

At the end of this lesson, you should be able to:

1. Discover natural drug

substances and the general properties of
each carbohydrate and related compounds
2. Illustrate the general biosynthetic pathway of the natural substances
3. Classify drugs related to each of the natural drug substances
4. List the chief constituent and use of representative drugs with natural drug substances
5. Classify the different sources of the natural drug products

The Germans first and foremost introduced the word ‘kohlenhydrates’ which was later on coined to
carbohydrates. The name obviously suggests that these compounds are essentially the hydrates of carbon. In reality, all
carbohydrates comprise of carbon, hydrogen and oxygen; whereas, the last two elements are found to exist in the same
proportions as in water ( i.e., H2O – 2:1). However, it has been observed that there are certain compounds that do
conform to the said ‘hydrate rule’ i.e., maintain the ratio of H and O (2:1) but do not belong to the category of
carbohydrates.

▪ Compounds with same proportions as in water but are not hydrates of carbon:
o Formaldehyde [HCHO]
o Acetic Acid [CH3COOH]
o Lactic Acid [C3H6O3]
▪ Carbohydrates that do not abide in the “rule of H 2O”
o Cymarose C7H14O4
o Digitoxose C6H12O4
o Rhamnose C6H12O5
o Sarmentose C7H14O4
o Oleandrose C7H14O4
o Digitalose C7H14O5

Under this unit, carbohydrates represent not only the sugars but also those substances that are related to them
basically in structure and other characteristic features. They belong to the chemical class of the aldehydes, ketone
alcohols, and also the condensation polymers of these partially oxidized polyalcohol collectively known as
‘Polysaccharides’ or ‘Oligosaccharides’. It is important to recall the properties and classifications of carbohydrates
discussed in Pharmaceutical Biochemistry.

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 Physical Properties

Solubility – with increasing complexity of the chemical structure, the water solubility decreases. This means that
monosaccharides and disaccharides are soluble in water while polysaccharides are insoluble, hence, heat is required
to dissolve them.

Shape - monosaccharides and disaccharides (like sucrose) appear as white crystalline while polysaccharides (like starch)
are amorphous (no definite shape)

Taste – with increasing complexity of the chemical structure, the level of sweetness decreases). This means that
monosaccharides and disaccharides taste sweet while polysaccharides taste bland.

Chemical Properties

1. Can undergo hydrolysis - e.g. Starch hydrolyzes to amylodextrin → erythrodextrin → achrodextrin → maltose → 2
glucose
2. Can reduce metals – e.g. reducing sugars can reduce cupric ion from Fehling’s solution to produce cuprous ion.
3. Form osazones with phenylhydrazine
4. Can be fermented to produce ethanol and carbon dioxide:
▪ Initiated by yeast (Saccharomyces cerevisiae)
▪ Fruits and flowers are made into wine
▪ Honey is made into mead (alcoholic beverage)
▪ Malted barley is made into beer
▪ Apple is made into cider (alcoholic beverage made from the fermented juice)
▪ Molasses is made into rhum (distilled from fermented molasses)
5. Can be metabolized
a. When sugars undergo oxidation, they produce sugar acids – e.g. glucose to gluconic acid
b. When sugars undergo reduction, they produce sugar alcohols – e.g. mannose to mannitol

How is carbohydrate synthesized? (watch the video “Photosynthesis”)

The synthesis of carbohydrates takes place due to photosynthesis wherein carbon dioxide (CO2) is one of the starting
materials. This chemical process occurs abundantly both in all plants and in certain purple bacteria.

nCO2 + n H2O + Light Energy → (CH2O)n Carbohydrate + nO2

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 Biosynthesis of sucrose:

Sucrose is the first sugar produced in photosynthesis and serves as the

main transport material. It is the usual precursor for polysaccharides
synthesis.

Steps:
1. Fructose 6-phosphate is converted to glucose 1-phosphate
2. Glucose 1-phosphate reacts with UTP uridylyltransferase to form UDP-
glucose Uridine diphosphate glucose
3. UDP-glucose reacts with fructose 6-phosphate to form sucrose
phosphate then sucrose or:
4. UDP-glucose reacts with fructose to form sucrose directly
5. Sucrose may remain as sucrose or be utilized to form
monosaccharides then oligosaccharides or polysaccharides

Sugars and sugar containing drugs

1. Dextrose (aka  -D-glucopyranose, D-glucose)

Biological Source: Grapes; Starch
Uses:
▪ Nutrient (oral, enema, SC inj., IV inj.) injection of fluid into the lower bowel
▪ Ingredient in:
✓ dextrose injection
✓ alcohol and dextrose injection
✓ dextrose and sodium chloride injection
✓ Dextrose and sodium Chloride tablets
✓ Dopamine HCl and dextrose injection Vasopressor and inotropic action
✓ Lidocaine HCl and dextrose injection
✓ Potassium chloride in dextrose injection (treatment of hypokalemia)
✓ Anticoagulant citrate dextrose solution (Anticoagulant for the storage of whole blood)
✓ Anticoagulant citrate phosphate dextrose solution (Anticoagulant for the storage of whole blood)

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 *Dextrose excipients

A. Dextrose excipient (aka Dextrose monohydrate, dextrates)

Biological Source/Source: Starch
Description: Crystalline, solid

Uses:
▪ Sweetening agent (substitute for sucrose in syrup)
▪ Tablet binder
▪ Coating agent
▪ Replacement for liquid glucose as pharmaceutic aid

B. Liquid glucose

Biological Source/Source: starch

Description: Colorless/yellowish, thick, syrupy liquid; nearly odorless; sweet
Chemical Constituents: Dextrose, dextrins, maltose, water
Uses: Agent of pharmaceutic necessity

C. Calcium gluconate (aka Calcium salt of gluconic acid)

Biological Source/Source: from Gluconic acid
Description: Soluble in cold water; less irritating for parenteral use than calcium chloride
Uses:
▪ Electrolyte replenisher (accounts for the therapeutic use of calcium)
✓ Dose: 1 g orally 3x or more in a day or IV infusion 1 to 3 days intervals

D. Calcium gluceptate and calcium levulinate (aka Calcium salts of 7- and 5-carbon acids)
Biological Source/Source:
▪ Calcium gluceptate: glucose
▪ Calcium levulinate: starch and cane sugar
Description: Salts are calcemic
Uses: Electrolyte replenisher (accounts for the therapeutic effect of calcium)

E. Ferrous gluconate (aka Ferrous salt of gluconic acid)

Biological Source/Source: Gluconic acid

Uses
▪ Hematinic increase the amount of hemoglobin in the blood
✓ Prophylactic dose: 325 mg 4x a day
✓ Less gastric distress than inorganic ferrous salts
▪ Products:
o Fergon®; Feralet®; Simron®

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 2. Fructose (aka D-fructose, levulose, B-D (-)-fructopyranose, B-D (-) – fructofuranose, fruit sugar
because it is present in most sweet fruits)
Biological Source/Source: Inversion of sucrose; honey; hydrolysis of inulin; enzymatically
prepared high fructose syrup inverted sugar glucose and fructose
Description:
▪ Ketone sugar carbonyl group (CO) bonded to an R group
▪ Colorless crystals or white crystalline or granular, odorless powder that has sweet taste
▪ Freely soluble in water
▪ Half as sweet to the taste as glucose
Uses:
▪ Food for diabetic patients (particularly diabetic acidosis)
▪ Infant feeding formulas
▪ Intravenously, less urinary secretion than glucose
▪ Fluid, nutrient and electrolyte replenisher (IV or SC)
▪ Ingredient in: fructose injection; fructose and NaCl injection

* High-fructose sweetener
Biological Source/Source: prepared by controlled enzymatic isomerization of Glucose (derived from starch)

3. Xylose (aka D-Xylose, wood sugar)

Biological Source/Source: Corn cobs, straw
Description:
▪ Sweet taste; absorbed from the small intestine
▪ Not metabolized by mammalian enzymes (to significant extent)
Uses:
▪ Diagnostic agent (FDA approved) for the evaluation of intestinal absorption
✓ Relative excretion of xylose in urine is indicative of intestinal malabsorption (celiac disease,
sprue, Crohn’s disease, pellagra, radiation enteritis, surgical resection
✓ D-xylose is normally easily absorbed by the intestines
▪ Products: Xylo-Pfan®

4. Sucrose (aka Saccharum, sugar)

Biological Source
▪ Sugarcane: Saccharum officinarum Linne (Gramineae)
▪ Sugar beet: Beta vulgaris Linne (Chenopodiaceae)
▪ Sugar maple: Acer saccharum (Aceraceae)
▪ Residual dark-colored syrup is called molasses (Use: animal food
and production of ethyl alcohol)
▪ Sugar beets: Beets are dug, washed and sliced into small, limp
slivers called cossettes like thin
Uses
▪ Pharmaceutic necessity (syrups)
▪ Demulcent relieves irritation of the mucous membranes in the mouth by forming a protective film.
▪ Nutrient
▪ Bacteriostatic and preservative (sufficient concentration in aqueous solution)

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 ▪ Sweetening agent to troches and tablets
▪ Retards oxidation to some preparations

5. Lactose (aka Milk sugar)

Biological Source/Source: Cow’s milk from Bos taurus, Bovidae
Chemical Constituents: Cow’s milk (80-90 % water; 3% casein; 5% lactose;
0.1 to 1 % mineral slats; 2.5 to 5 % fat (butter); vitamins)
Description:
▪ Cow’s milk
✓ White, opaque liquid
✓ Emulsion of minute fat globules suspended in a solution of casein,
albumin, lactose, and inorganic salts
✓ Slight but pleasant odor
✓ Agreeable sweet taste
✓ Specific gravity: 1.029 – 1.034
▪ Lactose
✓ Odorless, faintly sweet taste
✓ Stable in air; readily absorbs odor
✓ Hydrolysis: yields D-glucose and D-galactose
✓ Reduces Fehling’s solution; undergoes mutarotation; forms osazone change in the optical rotation
✓ Hydrolyzed by lactase
✓ Undergoes lactic and butyric acid fermentation
Uses:
▪ Cow’s milk
✓ Nutrient: Source of lactose, yoghurt and kumyss (fermented milk)
✓ Source of casein: Sodium caseinate is employed in culture media
▪ Lactose
✓ Nutrient: Nutrient in infant food; Easily hydrolyzed than sucrose
✓ Pharmaceutic necessity: Inert diluent for other drugs; Tablet diluent
✓ Provides substrate for lactobacilli: Minor role in establishing intestinal microflora

6. Lactulose
Biological Source/Source: lactose
Description:
▪ Semisynthetic sugar
▪ Yields fructose and galactose upon hydrolysis
▪ Poorly absorbed; remains unchanged in the colon
Uses:
▪ Laxative
o Bacteria in the colon metabolizes lactulose to acetic and lactic acid
o Accumulation of these irritating acids causes laxative effect
▪ Decreases blood ammonia concentration in portal systemic encephalopathy
o Acidified stools trap ammonia (ammonium ion), reabsorption is prevented
o Blood ammonia levels may be decreased by 25 to 50 %
▪ Product: Cephulac®; Chronuac ®; Duphalac ®; Lilac ®

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 Drugs containing compounds metabolically related to sugars

Certain pharmaceutic products, such as ethanol and citric acid, are produced by the cellular respiration of
carbohydrates, especially glucose.

Pathways:
1. Embden-Meyerhof pathway: anaerobic conversion of glucose to pyruvic acid by glycolysis. In the absence of air,
pyruvic acid may be converted to lactic acid or to ethanol. Lactic acid can be converted to energy without oxygen.
Accumulation of it in the blood results to muscle cramps

2. Oxidative decarboxylation of pyruvic acid: pyruvic acid undergoes oxidative decarboxylation to yield acetyl
coenzyme A (acetyl-CoA or active acetate) which can be utilized in a variety of reactions including the acetylation of
aromatic amines and alkaloids or the biosynthesis of fatty acids or steroids.

3. Tricarboxylic acid cycle: most of the acetyl-CoA undergoes condensation with oxaloacetate to form citrate, thereby
entering the TCA cycle where it is oxidized to CO2 and water with the liberation of energy

4. Other mechanism: hexose monophosphate shunt/pentose phosphate pathway

2 Phases of Pentose Phosphate Pathway (watch the video “Pentose Phosphate Pathway”)
1. Oxidative phase: G6P is oxidized and decarboxylated to ribulose-5-Phosphate; products: 2 equivalents NADPH
2. Regenerative “sugar-shuffle” phase: Conversion of ribulose-5-phosphate to G-6-Phosphate

Products of glycolytic and oxidative metabolism

1. Plant juices

A. Cherry Juice aka Succus cerasi

L-malic acid
Biological Source/Source: Prunus cerasus Linne (Rosaceae)
Chemical Constituents: Malic acid (1%)
Uses: Preparation of cherry syrup, a flavored vehicle that disguises agent in
pharmaceutic mixtures (esp. acidulous in nature)

B. Others: Raspberry juice

2. Acids

A. Citric acid (First isolated in crystal form from lemon juice by Sheele
1784)
Biological Source/Source: Lemons, limes, pineapples; Fermentation of
sucrose
Description:
▪ Colorless, odorless, translucent crystals Citric acid
▪ Readily soluble in water and alcohol
▪ Tricarboxylic acid

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 Uses:
▪ Used in buffering systems
▪ Acidulant in effervescent formulations confer a tart, sour, or acidic flavor
▪ Ingredient in potassium citrate and citric acid solution; sodium citrate and citric acid solution; systemic alkalinizers;
anticoagulant citrate dextrose solution; anticoagulant citrate phosphate dextrose solution

B. Lactic acid
Biological Source/Source: sugar
Description:
▪ Colorless or yellowish, nearly odorless, syrupy liquid
▪ Miscible with water, alcohol, and ether
Chemical Constituents:
▪ Lactic acid (85-90 %by weight), lactic acid lactate
Uses:
▪ Acidulant: infant feeding formulas
▪ Electrolyte replenisher: sodium lactate injection
▪ Treatment of metabolic acidosis kidneys are not removing enough acid from the body
▪ Calcium replenisher: Calcium lactate (dose: 1 to 5 g 3x a day)

C. Tartaric acid
Biological Source/Source: wine Tartaric acid

Description:
▪ Dicarboxylic acid
▪ Soluble in water; freely soluble in alcohol
Uses: Used as a substitute for citric acid in buffer systems and effervescent formulations

D. Ferrous fumarate
Description: Comparable to ferrous gluconate
Uses:
▪ Hematinic agent (Dose: 200 mg 3-4x a day)
▪ Products: Feco-T®; Feostat®; Fumasorb®; Fumerin®; Hemocyte®; Ircon®; Palmiron®
E. Others: FUMARIC ACID, MALIC ACID

3. Alcohol

A. Alcohol (aka Ethanol)

Description: Liquid containing NLT 92.3 % by weight or 94.9% by volume of ethanol at 15.56⁰C
Uses
▪ 70% w/v: anti-infective
▪ Ethanol 5-10% and dextrose (5%) IV: increases caloric intake and replenish fluids

B. Diluted alcohol
Description
▪ Mixture of alcohol and water
▪ 48.4 to 49.5 % by volume at 15.56⁰ C
Uses: solvent
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 Products of Reductive metabolism

Dulcitol, mannitol, sorbitol and other sugar alcohols are widely distributed in plants but enzymes or enzyme systems
capable of reducing sugars to sugar alcohols have never been isolated from higher plant sources. Use of microbial
enzymes indicates that sugar alcohol (glycitol) phosphates may be formed by reduction of ketose phosphates (e.g.
glycitols are produced by the action of the enzyme phosphatase).

1. Mannitol (aka D-mannitol)

Biological Source/Source
▪ Manna: Fraxinus ornus Linne (Oleaceae)
▪ Fungi
Description:
▪ Hexahydric alcohol
▪ White, crystalline, odorless powder, sweet tasting
▪ Orthorhombic prisms or aggregates of fine needle
▪ Freely soluble in water and boiling alcohol; almost insoluble in cold alcohol
Uses:
▪ Manna: Laxative
▪ Diagnostic aid: mannitol is not absorbed from the gastrointestinal tract
▪ Osmotic diuretic: when administered parenterally, not metabolized and eliminated by glomerular filtration (80% of
approximately 100g dose appear in urine in 3 hours)
▪ Product: Osmitrol®

2. Sorbitol (aka D-glucitol)

Biological Source/Source:
▪ Ripe Berries of Mountain ash: Sorbus aucuparia Linne (Rosaceae)
▪ Glucose
Description:
▪ Hexitol: hexahydric alcohol
▪ Developed during World War I: Mannitol Hexanitrate used as substitute
for mercury fulminate (short supply)
▪ Crystalline and soluble
▪ Compatible with syrup, alcohol and other polyols
▪ Half as sweet as sucrose; humectant property; not absorbed on oral ingestion; not metabolized readily
Uses:
▪ Ingredients in: toothpaste; chewing gums and dietetic products
▪ Dietetic beverages: in conjunction with saccharin because it acts as osmotic laxative
▪ In combination with mannitol for urologic irrigation

3. Others: Xylitol

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 Polysaccharides and Polysaccharide-containing Drugs

Classification of polysaccharides
▪ More accurate and precise demarcation of polysaccharides
▪ This classification is based on position and configuration of the glycosidic linkage involved and type of
monosaccharide building unit.
Homoglycan
o The polysaccharide is termed as homoglycan when it contains only one type of monosaccharide unit
o Ex: Cellulose - expressed as β-1, 4 –D-glycan
Heteroglycan
o The polysaccharide is known as heteroglycan when it involves more than one kind of monosaccharide unit.
o ex: D-gluco-D-mannose is a diheteroglycan

Starch is the most widely distributed compound in plants. It is produced in large quantities in green leaves as the
temporary storage form of photosynthetic products. Starch occurs in seeds and in pith, medullary rays and cortex of the
stems and roots of perennial and other plants. It constitutes

HOMOGLYCANS

1. Honey (aka Mel or Madhu)

Biological Source: Honey is a viscid and sweet secretion stored in the honey comb by various species of bees, such as:
Apis dorsata, Apis florea, Apis indica, Apis mellifica, belonging the natural order Hymenoptera (Family: Apideae).
Description:
▪ Appearances: Pale yellow to reddish brown viscid fluid
▪ Odour: Pleasant and characteristic
▪ Taste: Sweet, Slightly acrid
▪ Specific gravity 1.35-1.36
▪ Specific rotation: +3 o to –15o Total Ash: 0.1-0.8%

▪ On prolonged storage it usually turns opaque and granular due to

the crystallization of dextrose and is termed as ‘granular honey’.
Chemical Constituents
▪ Moisture 14-24%, Dextrose 23-36%, Levulose (Fructose) 30-47%,
Sucrose 0.4-6%, Dextrin and Gums 0-7% and Ash 0.1-0.8%.
▪ small amounts of essential oil, beeswax, pollen grains, formic acid,
acetic acid, succinic acid, maltose, dextrin, colouring pigments,
vitamins and an admixture of enzymes eg; diastase, invertase and
inulase

Uses:
▪ It is used as a sweetening agent in confectionaries.
▪ Being a demulcent, it helps to relieve dryness and is, therefore, recommended for coughs, colds, sore-throats and
constipation.
▪ Because of its natural content of easily assimilable simple sugars, it is globally employed as a good source of
nutrient for infants, elderly persons and convalescing patients.

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 2. Starch
Biological Source: Zea mays (Poaceae); Triticum aestivum (Poaceae), Solanum tuberosum (Solanaceae)

Biosynthesis of Starch (watch video https://www.youtube.com/watch?v=b723qrc6VrU)

1. Amylose
▪ Effected by an enzyme known as transglycosylases – addition of single glucose residue
2. Amylopectin
▪ Formed from amylose by the action of a transglycosylase designated Q-enzyme
▪ The enzyme effects the splitting of a monosaccharide chain containing at least 40 glucose units into 2 fragments
▪ The fragment carrying the newly exposed residue end first forms an enzyme-substrate complex
▪ Fragment is then transferred to an acceptor chain forming -1,6 branch

Chemistry and property of starch: generally, a mixture of structurally different polysaccharides

1. Amylose
▪ linear molecule; composed of 250-300 D-glucopyranose units linked by -1, 4 glucosidic bonds; helix like shape
▪ more soluble in water
▪ complexed and precipitated with suitable agents (alcohols and nitroparaffins)
▪ reacts with iodine to form deep blue complex
▪ 25% in starch
▪ Hydrolyzed by -amylase or -1,4-glucan 4-glucano-hydrolase (pancreatic juice and saliva) – random splitting of
-1, 4 glucosidic bonds
▪ Products: glucose, maltose and amylopectin

2. Amylopectin

▪ consists of 1000 or more glucose units linked by -1,4 linkages and a number of -1,6 linkages at branch points
(appears to about 4% of the total linkages or 1 in every 25 glucose units)
▪ less soluble in water
▪ reacts with iodine to form blue-violet or purple color
▪ 75% in starch
▪ Hydrolyzed by B-amylase or -1,6-glucan maltohydrolase by removing maltose units
▪ Products: polysaccharide fragments known as dextrins (product of incomplete hydrolysis)

Zea mays Triticum aestivum Solanum tuberosum

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 3. Hetastarch: semisynthetic material (contains 90% amylopectin)
Uses:
▪ a 6% solution is used as plasma expander to treat shock due to hemorrhage, burns,
etc.
▪ It is employed in the management and treatment of hypovolemic shock (Shock
caused due to diminished blood volume).
▪ It is also used as a suspension medium for leukapheresis (The separation of leukocytes
from blood, which are then transfused back into the patient).
▪ It is employed as a cryoprotective (A chemical that protects cells from the effect of
cold) agent for erythrocytes.

4. Inulin
Biological sources: Inula helenium; Eupatorium cannabinum; Cynara scolymus;
Carpesium cernuum; Calendula officinalis; Aretium lappa
Uses:
▪ it is a D-fructan used in culture media as fermentative identifying agent for certain
bacteria.
▪ it is employed as a diagnostic agent for evaluation of glomerular filteration i.e., renal–
function test (or kidney function test).

5. Dextran
Description: a-1,6-linked polyglucan that is formed from sucrose by the action of an
enzyme system, transglucosylase, present in Leuconostoc mesenteroides
Uses:
▪ plasma expander (6% solution).
▪ NOTE: May interfere with some laboratory tests and significantly increase clotting
time

6. Cellulose
Biological source/source: Gossypium hirsutum (Malvaceae)

A. Purified cotton
Description: white, soft, fine, filament -like hairs that appear under microscope as
hollow, flattened and twisted bands. (see image)
Uses:
▪ Surgical dressing – mechanical protection to absorb blood, mucus or pus
▪ Source of pure cellulose in the manufacture of cellulose acetate

B. Powdered cellulose
Description: purified, mechanically disintegrated cellulose prepared by processing a-
cellulose obtained as a pulp
Uses:
▪ Self-binding tablet diluent and disintegrating agent

C. Microcrystalline cellulose
Description: purified, partially depolymerized cellulose prepared by treating a-cellulose with mineral acids
Use: tablet diluent

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 D. Cellulose derivatives

▪ Methylcellulose - obtained by the reaction of cellulose with caustic soda and methyl chloride used as bulk
laxative, suspending agent, topical protectants marketed as “artificial tears”
▪ Ethylcellulose – an ethyl ester of cellulose used tablet binder and film coating
▪ Hydroxyethylcellulose – used as thickening agent and as an ingredient in some formulations for artificial tears
▪ Hydroxypropylcellulose – used as stabilizer and thickener in liquid preparations; binder and film coating in tablet
formulations
▪ Hydroxypropylmethylcellulose – used as a suspending agent, thickening agent, a tablet excipient and topical
protectant for contact lenses
▪ Pyroxylin or soluble guncotton – obtained from the mixture of nitric and sulfuric acid on cotton. It is a mixture of
cellulose nitrates. It is used as a pharmaceutic aid in the manufacture of collodion and flexible collodion (topical
protectants)
▪ Oxidized cellulose and oxidized regenerated cellulose – usually available in the form of sterile pads, pledgets and
strips and are used as local hemostatics.
▪ Cellulose acetate phthalate – a free-flowing, white powder and is used for enteric coating of tablets.
▪ Sodium carboxymethylcellulose – used as suspending agent, thickening agent, tablet excipient and bulk laxative

HETEROGLYCANS: GUMS & MUCILAGES

These are natural plant hydrocolloids that may be classified as anionic (examples: arabic, karaya, tragacanth, gellan,
agar, algin, carrageenan, pectic acids) or non-ionic (examples: guar, locust bean, tamarind, xanthan, amylose,
arabinan, cellulose, galactomannan) polysaccharides or salts of polysaccharides.

What are hydrocolloids?

▪ Hydrocolloids forms a gel or viscous solution in the presence of water

▪ Produced in plants naturally or as a protective after injury (or unfavorable conditions like drought)
▪ Sources: Seed embryos or other plant parts (example: pectin- group of polysaccharides derived from plant cell
walls), marine algae and microorganisms
▪ Physical Characteristics: Translucent, amorphous
▪ COMMON SOURCES:
o Shrub or Tree exudates (e.g. Acacia, Karaya, Tragacanth)
o Marine Gums (e.g. Agar, Algin, Carrageenan)
o Seed gums (e.g. Guar, Locust bean, Psyllium)
o Plant extracts (e.g. pectins)
o Starch and Cellulose derivatives (e.g. Hetastarch, CMC, Ethylcellulose, Hydroxypropyl methylcellulose,
Methylcellulose)
o Microbial gums – dextrans. Xanthan

May be linear or branched

a. Linear hydrocolloids
▪ Less soluble than branched polymers (like algin, amylose, cellulose, pectin)
▪ Yields solutions with greater viscosity:
o These features are related to the increased possibility for good alignment and considerable intermolecular
hydrogen boding among linear polymers. This tendency for intermolecular associations also explains why

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 solutions of linear polysaccharides are less stable, especially with reductions in temperature that may result to
precipitation and insoluble in cold water.
o This phenomenon influences the shelf life or product formulations problem like recrystallization of these solutions.
b. Branched hydrocolloids
▪ Form gels rather than viscous solutions at higher concentrations
o Examples: xanthan, xylan, galactomannan, gum arabic, tragacanth
o They tend to be tacky (retaining a slightly sticky feel; not fully dry) when moist which is advantageous for
adhesive purposes.
o Gluemamela is an alternative for commercialized synthetic glue that is made out of gumamela mucilage.
▪ They rehydrate more readily than linear ones which is a property of importance in drug formulations that must be
reconstituted immediately before use (like suspensions).

They may be acidic, basic or neutral

a. Acidic and neutral: widely used

b. Basic: limited commercial importance

What are the chemical components of gums and mucilage?

1. Upon hydrolysis, these substances yield arabinose, galactose, glucose, mannose, xylose and various uronic acids,
class of sugar acids with both carbonyl (C=O) and carboxylic acid (COOH) functional groups
2. Because of the numerous components, this makes gums heterogenous in composition
3. The uronic acids may form salts with Calcium, Magnesium and other cations

What are the general uses of gums and mucilage?

1. Ingredient in dental and other adhesives

2. Bulk laxative - Bulk-forming laxatives are not digested but absorb liquid in the intestines and swell to form a soft,
bulky stool. The bowel is then stimulated normally by the presence of the bulky mass. (www.mayoclinic.org)
3. Pharmaceutic Use:
▪ Tablet binders (due to hydrophilic or water-loving properties)
▪ Emulsifiers
▪ Gelling agents - used to thicken & stabilize liquid solutions
▪ Suspending agents
▪ Stabilizers - ex. Seaweed gums and guar gums in ice cream and cheese
▪ Thickeners

What are the differences between gums and mucilage?

POINT OF COMPARISON GUMS MUCILAGES

Solubility in water Readily dissolves in water Forms slimy masses with water
Nature of origin Pathologic products from upon injury Physiologic products or normal
due to unfavorable conditions such products of metabolism form within
as drought, breakdown of cell walls the cells and may represent storage
material, water storage reservoir or
protection for germinating seeds

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 Sources

PLANT EXUDATES

1. Acacia Gum aka Gum Arabic

Description: gum Arabic came from a misnomer because little acacia is produced on the
Arabian Peninsula and none is exported. The name reflects the drug’s extensive use by the
early Arabian physicians
Biological source/source: Acacia senegal, Fabaceae
Constituent: Arabin (complex mixture of Calcium, Magnesium and Potassium salts of
Arabic acid)
Uses: Emulsifying agents, Suspending Agent, Demulcent, Emollient, Adhesive, binder,
Emollient

2. Indian Gum (aka Ghatti gum)

Biological source/source: Anogeissus latifolia, Combretaceae
Use/s: Used as a substitute for Acacia gum

3. Karaya Gum aka Sterculia gum, Indian tragacanth (Sterculia is from the Latin word Sterculius meaning fetid odors and
has a marked odor of acetic acid
Biological source/source: Sterculia urens, Sterculiaceae
Properties: One of the least soluble exuded plant gums. It absorbs and swells and forms a
discontinuous type of mucilage
Use/s:
▪ Bulk laxative, Agents forming emulsions and suspensions, dental adhesives
▪ Used extensively in skin lotions, textile and printing industries and food productions
▪ Found in Movicol® (Laxative)

4. Tragacanth aka Gum Tragacanth

Biological source/source: Astragalus gummifer, Fabaceae
Method of collection:
The gums exuding from natural injuries is more or wormlike and is twisted into coils (formerly known as
Vermiform tragacanth) or is shaped irregularly in a tear-shape (tragacanth sorts).
The better grade, ribbon gum and flake gum, comes from a transverse
Constituent/s: 60 to 70% bassorin (swells in water but do not dissolve) and 30% Tragacanthin (demethoxylated bassorin
and is more water soluble)
Uses:
▪ Suspending agent for insoluble powders in mixtures, emulsifying agent for oils and resins, adhesive, employed in
cosmetics as demulcent and emollient, cloth printing, confectionery (binder and emulsifier in lozenges production
to bring cohesion to the tablet and better release of the flavor)
▪ The most resistant of the hydrocolloids to acid hydrolysis and thus is preferred for use in highly acidic conditions

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 MARINE GUMS

1. Agar aka Japanese isinglas

Biological source/source: Gelidium cartilagineum, Gelidiaceae
Description: Insoluble in cold water
Constituent: Agarose and agaropectin
Uses:
▪ laxative, suspending agent, emulsifier, gelling agent for suppositories and surgical
lubricants, disintegrant, culture media

2. Algin aka Sodium alginate

Description: From Brown seaweeds extracted using a dilute alkali
Biological source/source: Macrocystis pyrifera, Lessoniaceae (Harvested from the Pacific
ocean)
Constituents: Mannuronic acid (major component), Sodium salt of alginic acid (a polymer
of L-glucoronic acid and D-mannuronic acid).
Uses: suspending agent, tablet binder and thickening agent

3. Carrageenan (aka Irish Moss, Chondrus)

Description: From red algae / seaweeds; It has higher sulfate ester content than agar
Biological source/source: Chondrus crispus, Gigartinaceae
Components:
▪ K-carrageenan (kappa) – good gelling agent*
▪ i-carrageenan (iota) - good gelling agent*
▪ λ-carrageenan (lambda) – non-gelling agent and used as thickener
*orients in stable helices in solution
Uses: Stabilizing agent for emulsions and suspensions, Toothpaste formulation (due to firm
texture and rinsability), demulcent, bulk laxative

4. Danish Agar

Biological source/source: Furcellaria fastigiata, Furcellariaceae

Description: From red algae; Similar to K-carrageenan
Uses: Gelling agent and suspending agent

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 SEED GUMS

1. Psyllium aka Plantago seed, Plantain seed

Biological source/source: Plantago psyllium, Plantaginaceae

Constituents: 10-30% hydrocolloid (localized in the outer seed coat)
Uses: Cathartic (action: swelling of the seed coat thus giving bulk and lubrication)
Dose: 7.5 g and should be taken with a considerable amount of water
Additional information: Solutions of purified psyllium gum are thixotropic

2. Cydonium / Quince Seed

Biological source/source: Cydonia vulgaris, Rosaceae
Forms viscous solutions with thixotropic properties

3. Guar gum
Biological source/source: Cyamopsis tetragonolubus,
Fabaceae Cydonia vulgaris Cyamopsis tetragonolubus Ceratonia siliqua
Uses: bulk forming laxative, thickening agent, tablet binder,
disintegrating agent
In fast dissolving tablet (The result is that it released the 99.21% drug in 15min as compared to Sodium Starch Glycolate).

4. Locust bean gum aka St. John’s bread (legendary use as the food of St. John the Baptist), Carob Pulp
Biological source/source: Ceratonia siliqua, Fabaceae
Uses: thickener, stabilizer

MICROBIAL GUMS

Xanthan Gum

Description: High molecular weight microbial gum produced from the action of Xanthamonas
campestris on suitable carbohydrates
Component: branched, partially acetylated polysaccharide (d-glucose, d-glucuronic acid, d-
mannose)
Uses: Emulsifying and suspending agent

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 PLANT EXTRACTIVES

Pectin
▪ Purified carbohydrate product obtained from the dilute acid extract of the inner portion of the rind of citrus fruits or
from apple pomace
o Citrus peel is rich in pectin with the amounts varying from the season and variety
o Pectin in fruit is found in an insoluble form known as Protopectin and is converted to the soluble form
Pectin by heating the fruit with dilute acid
▪ From Greek word meaning congealed or curdled
▪ Consists of partially methoxylated polygalacturonic acid
▪ Pharmaceutic pectin is pure pectin with no additions made

Uses: protectant and suspending agent, antidiarrheal formulations

▪ As colloidal solution it has the property to conjugate toxins (through adsorption) and enhance physiologic
functions of the digestive tract
▪ Kaopeptate is a preparation consisting of Kaolin + Pectin (antidiarrheal)

Types of pectin
▪ Protopectin – obtained from unripe sources
▪ Pectin – obtained from ripe sources
▪ Pectinic acid – obtained from over ripe sources

Sources of pectin:

Pomelo – Citrus grandis, Dalanghita – Citrus nobilis, Ponkan – Citrus sinensis, Orange – Citrus aurantium,
Rutaceae Rutaceae Rutaceae Rutaceae

Calamansi – Citrus Grapefruit – Citrus paradisi, Lemon – Citrus limon, Apple – Malus domestica,
microcarpa, Rutaceae Rutaceae Rutaceae Rosaceae

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