02.ophthalmic Solutions and Suspensions

OPHTHALMIC SOLUTIONS AND SUSPENSIONS
PHARMACEUTICAL DOSAGE forms and drug delivery systems applied

topically to the eye include solutions, suspensions, gels, ointments and
drug impregnated inserts.
Pharmaceutical preparations are applied topically to the eye to treat

surface or intraocular conditions, including:
• Infections of the eye or eyelids due to bacterial, fungal and viral

pathogens; allergic or infectious conjunctivitis or inflammation;
elevated intraocular pressure and glaucoma; and, dry-eye due to an
inadequate production of fluids bathing the eye.
• In treating certain ophthalmic conditions, as glaucoma, both systemic

drug use and topical treatments may be employed.
The normal volume of tear fluid retained in the cul-de-sac of the human
eye is about 7-8µL.
An eye that is maintained in a non-blinking state can accommodate a

maximum of about 30µL of fluid but when blinked can retain only about
10µL.
Because the capacity of the eye to retain liquid and semisolid

preparations is limited, topical applications are administered in small
amounts; liquids drop-wise and ointments as a thin ribbon applied to
the margin of the eyelid.
Larger volumes of liquid preparations may be used to flush or bathe the

eye.
Excessive liquids, both normally produced and externally delivered, are

rapidly drained from the eye.
A single drop of an ophthalmic solution/suspension' measures about 50
µL (based on 20 drops/mL) and thus, much of an administered drop may
be lost.
The optimal volume to administer, based on eye capacity, would be 5 to

10µL. Since microliter-dosing eye droppers are not generally available
for self-use, loss of instilled medication using standard eye droppers is a
common occurrence.
Due to the dynamics of the lachrymal system, the retention time of an

ophthalmic solution on the eye surface is short, and the amount of drug
absorbed is usually only a small fraction of the quantity administered.
For example, following the administration of pilocarpine ophthalmic
solution, the solution is flushed from the precorneal area within 1 to 2
minutes, resulting in the ocular absorption of less than 1 percent of the
administered dose.
Decreased frequency of dosing, increased ocular retention time and

greater bioavailability are achieved by formulations which extend
corneal contact time, as gel systems, liposomes, polymeric drug carriers
and ophthalmic suspensions and ointments.
The major categories of drugs applied topically to the eye are:-
1)-Anesthetics
2)-Antibiotic/Antimicrobial Agents
3)-Antifungal Agents
4)-Anti-inflammatory Agents
5)-Antiviral Agents
6)-Astringents
7) Beta-Adrenergic Blocking Agents

8)-Miotics and other Glaucoma Agents
9)-Mydriatics and Cycloplegics
10)Protectants/Artificial Tears
11)Vasoconstrictors/Ocular Decongestants.
Pharmaceutic Requirements
The preparation of solutions and suspensions for ophthalmic use requires

special consideration with regard to sterility, preservation, isotonicity,
buffering, viscosity, ocular bioavailability and packaging.
Sterility and Preservation
Ophthalmic solutions/suspensions must be sterilized for safe patient-use.
Although it is preferable to sterilize ophthalmics in their final containers by

autoclaving at 121°C for 15 minutes, this method sometimes is precluded
by the thermal instability of the formulation's components. As an
alternative, bacterial filters may be used, although they are not as reliable
in achieving sterility as the autoclave.
However, since final product testing is used to validate the absence of

microbes, sterility may be assured by either method employed.
One advantage of filtration is the retention of all particulate matter

(microbial, dust, fiber).
To maintain sterility during patient use, antimicrobial preservatives

generally are included in ophthalmic formulations; an exception being for
preparations intended to be used during surgery or in the treatment of
traumatized eyes because of the capacity of some preservatives to cause
eye irritation. These are packaged in single use containers
Isotonicity
In practice, the isotonicity limits of an ophthalmic solution in terms of

sodium chloride, or its osmotic equivalent, may range from 0.6 to 2.0%
without marked discomfort to the eye. Sodium chloride itself does not have
to be used to establish a solution's osmotic pressure. Boric acid in a
concentration of1.9% produces the same osmotic pressure as does 0.9%
sodium chloride. All of an ophthalmic solution's solutes, including the active
and inactive ingredients, contribute to the osmotic pressure of a solution.
Buffering
The pH of an ophthalmic preparation may be adjusted and buffered for one

or more of the following purposes: 1) for greater comfort to the eye; 2) to
render the formulation more stable; 3) to enhance the aqueous solubility of
the drug; 4) to enhance the drug's bioavailability; and, 5) to maximize
preservative efficacy.
The pH of normal tears is considered to be about 7.4, but varies among

patients (e.g., more acidic in contact lens wearers). Tears have some buffer
capacity and are thereby able to prevent marked discomfort.
Viscosity and Thickening Agents
In the preparation of ophthalmic solutions, a suitable grade of

methylcellulose or other thickening agent is frequently added to increase
the viscosity and thereby aid in maintaining the drug in contact with the
tissues to enhance therapeutic effectiveness. Generally, methylcellulose of
the 4000 cps viscosity type is used in concentrations of 0.25% and the 25
cps type at 1 % concentration.
Hydroxypropyl methylcellulose and polyvinyl alcohol are also used as

thickeners in ophthalmic solutions.
Occasionally a 1 % solution of methylcellulose without medication is used

as a tear replacement.
Viscosity for ophthalmic solutions is considered optimal in the range of 15
to 25 cps.
Ocular Bioavailability
There are physiologic factors which can affect a drug's ocular bioavailability,
including protein binding, drug metabolism, and lachrymal drainage.
Protein-bound drugs are incapable of penetrating the corneal epithelium

due to the size of the protein-drug complex.
Because of the brief time in which an ophthalmic solution may remain in

the eye the protein binding of a drug substance could quickly negate its
therapeutic value by rendering it unavailable for absorption.
Normally, tears contain between 0.6 and 2.0% of protein, including albumin
and globulins, but disease states (as uveitis) can raise these protein levels
As in the case with other biological fluids, tears contain enzymes (such as
lysozyme) capable of the metabolic degradation of drug substances.
However, the extent to which drug metabolism occurs and affects
therapeutic effectiveness is not fully determined at this time.
In addition to physiologic factors affecting ocular bioavailability, other

factors, as the physicochemical characteristics of the drug substance and
product formulation are important.
Packaging Ophthalmic Solutions and Suspensions
Although a few commercial ophthalmic solutions/suspensions are packaged

in small glass bottles with separate glass or plastic droppers, the vast
majority are packaged in soft plastic containers having a fixed, built-in
dropper.
The latter type of packaging is preferred both to facilitate administration

and to protect the product from external contamination.
Ophthalmic solutions and suspensions are commonly packaged in
containers holding 2,2.5,5,10, 15, and 30 mL of product.
Patients must exercise care in protecting an ophthalmic

solution/suspension from external contamination.
Packaging Ophthalmic Solutions and Suspensions
Although a few commercial ophthalmic solutions/suspensions are packaged

in small glass bottles with separate glass or plastic droppers, the vast
majority are packaged in soft plastic containers having a fixed, built-in
dropper.
The latter type of packaging is preferred both to facilitate administration

and to protect the product from external contamination.
Ophthalmic solutions and suspensions are commonly packaged in

containers holding 2,2.5,5,10, 15, and 30 mL of product.
Patients must exercise care in protecting an ophthalmic

solution/suspension from external contamination.
Proper Administration of Ophthalmic Solutions and Suspensions
Prior to the administration of an ophthalmic solution or suspension, the

patient or caregiver should be advised to wash his/her hands thoroughly. If
the ophthalmic drops are supplied with a separate dropper, the patient
should inspect the dropper to make sure it has no chips or cracks.
Ophthalmic solutions should be inspected for color and clarity. Out of date
or darkened solutions should be discarded.
Ophthalmic suspensions should be shaken thoroughly prior to

administration to evenly distribute the suspensoid.
The cap of an eye-drop container should be removed immediately prior to

use and returned immediately after use.
To instill eye drops, the patient should tilt his/her head back and with the
index finger of the free hand gently pull downward the lower eyelid of the
affected eye to form a pocket or cup.
While looking up, and without touching the dropper to the eye, the
prescribed number of drops should be instilled into the formed pocket.
The lower eyelid should be released and the eye closed to allow the
medication to spread over the eye. The eye should be held closed
preferably for a full minute without blinking, rubbing, or wiping.
While the eye is closed, gentle pressure should be applied just under the
inner corner of the eye by the nose to compress the nasolacrimal duct to
prevent drainage and enhance corneal contact time. Then, any excess liquid
may be wiped away with a tissue.

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OPHTHALMIC SOLUTIONS AND SUSPENSIONS

PHARMACEUTICAL DOSAGE forms and drug delivery systems applied

Pharmaceutical preparations are applied topically to the eye to treat

• Infections of the eye or eyelids due to bacterial, fungal and viral

• In treating certain ophthalmic conditions, as glaucoma, both systemic

An eye that is maintained in a non-blinking state can accommodate a

Because the capacity of the eye to retain liquid and semisolid

Larger volumes of liquid preparations may be used to flush or bathe the

Excessive liquids, both normally produced and externally delivered, are

The optimal volume to administer, based on eye capacity, would be 5 to

Due to the dynamics of the lachrymal system, the retention time of an

Decreased frequency of dosing, increased ocular retention time and

The major categories of drugs applied topically to the eye are:-

7) Beta-Adrenergic Blocking Agents

9)-Mydriatics and Cycloplegics

The preparation of solutions and suspensions for ophthalmic use requires

Sterility and Preservation

Ophthalmic solutions/suspensions must be sterilized for safe patient-use.

Although it is preferable to sterilize ophthalmics in their final containers by

However, since final product testing is used to validate the absence of

One advantage of filtration is the retention of all particulate matter

To maintain sterility during patient use, antimicrobial preservatives

In practice, the isotonicity limits of an ophthalmic solution in terms of

The pH of an ophthalmic preparation may be adjusted and buffered for one

The pH of normal tears is considered to be about 7.4, but varies among

Viscosity and Thickening Agents

In the preparation of ophthalmic solutions, a suitable grade of

Hydroxypropyl methylcellulose and polyvinyl alcohol are also used as

Occasionally a 1 % solution of methylcellulose without medication is used

Protein-bound drugs are incapable of penetrating the corneal epithelium

Because of the brief time in which an ophthalmic solution may remain in

In addition to physiologic factors affecting ocular bioavailability, other

Packaging Ophthalmic Solutions and Suspensions

Although a few commercial ophthalmic solutions/suspensions are packaged

The latter type of packaging is preferred both to facilitate administration

Patients must exercise care in protecting an ophthalmic

Packaging Ophthalmic Solutions and Suspensions

Although a few commercial ophthalmic solutions/suspensions are packaged

The latter type of packaging is preferred both to facilitate administration

Ophthalmic solutions and suspensions are commonly packaged in

Patients must exercise care in protecting an ophthalmic

Proper Administration of Ophthalmic Solutions and Suspensions

Prior to the administration of an ophthalmic solution or suspension, the

Ophthalmic suspensions should be shaken thoroughly prior to

The cap of an eye-drop container should be removed immediately prior to

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