Welcome To Formulation: Zaher@ntu - Edu.sg
Welcome To Formulation: Zaher@ntu - Edu.sg
Welcome To Formulation: Zaher@ntu - Edu.sg
Examinations
CA Policy
Attention
The slides represent points for discussion
You must refer to the textbook for a complete account
Course Contents
Section III: Solid Dosage Forms and Solid ModifiedRelease Drug Delivery Systems
Powders and Granules
Capsules
Tablets
Solid Oral Modified-Release Dosage Forms and Drug
Delivery Systems
Section IV: Semi-Solid Dosage Forms and Transdermal
Systems
Ointments, Creams and Gels
Transdermal Drug Delivery Systems
6
Overall Goals
10
What is Pharmaceutics?
Preformulation / Pharmaceutical
Formulation
12
Dosage Form
Oral
Sublingual
Tablets, lozenges
Parenterals
Solutions, suspensions
Ocular
Transdermal
Nasal
Respiratory
Aerosols
Vaginal
Urethral
Solutions, suppositories
Rectal
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16
biotherapeutics
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Dosage
(mg)
Onset of
action
(min.)
Peak
action
(min)
Duration of
action
(min/h)
Sublingual
0.3-0.8
2-5
4-8
10-30 min
1-3
2-5
4-10
30-300 min
6.5-19.5
20-45
45-120
2-6 h
Patches
5-10
30-60
60-180
Up to 24 h
Ointment
0.5-10inc
15-60
30-120
3-8 h
Buccal
Oral
20
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Classification:
Local/topical or systemic therapy
Immediate/conventional or Modified/novel release
Local/topical therapy
Therapeutic agent applied directly to site of action
Systemic therapy
Drug administered systemically
into blood to be transported to
site of action
Oral
IV
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Dosage forms whose drug-release characteristics of timecourse and/or location are modified:
Delayed release
Extended (sustained) release
Delayed Release:
Release of a drug (or drugs) at a time other than
immediately following oral administration, e.g.
Enteric coated: Prevents release of drug in stomach;
releases after passing phyloric sphincter
Pulsatile delivery: programmable to release drug at
predetermined time or place
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25
Drug Release
26
Paracellular:
Through gaps/pores between cells
Small molecules e.g. urea, water
Transcellular: Through cells hence biological membranes
Main mechanism, diffusion: follows Ficks law
molecules must have lipid solubility, unionised form
Active transport: energy involved, against conc
gradient carrier can be saturated, eg vit B1, B2, B3 B6
Facilitated diffusion: carrier can be saturated, no
energy involved, not against conc gradient, eg B12
Pinocytosis, endocytosis molecules (large) like some
peptides, particles
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Drug Action
Blood
Oral
ingestion
Drug
Adipose
tissue
storage
Volatile drugs
in expired air
Effector tissues,
drug receptor
binding
Peripheral
tissue,
Metabolism
Drug
Drug-plasma
protein complex
Lung
Liver,
drug
metabolism
Kidney
Drugs &
metabolites in
urine
Bile
Intestinal
reabsorption
Intestines
Drugs &
metabolites in
stool
http://www.boomer.org/c/p1/Ch03/Ch0302.html
Noyes-Whitney Equation
dC
dt
DA
(Cs
=
hV
C)
dC
dissolution rate
dt
A surface area
D diffussion coefficient
V volume of medium
Cs solubility
C concentrat
ion in medium
29
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