2. .

3. Overall Aims of Course
Upon successful completion of this course the student should be able to;
Formulate, compound, sterilize, dispense, label, store, distribute,
manufacture and quality control of different sterile drug products
(parenteral, ophthalmic preparations, vaccines and blood products)
 Apply different methods of manufacturing different sterile drug products.
 Determine the factors affecting the stability of sterile drug products.
 Identify different quality control testing of sterile drug products.
Perform packing, labelling and dispensing of sterile products accurately
and safely.

5. Ophthalmic Preparations
 Ophthalmic preparations are sterile products
essentially free from foreign particles, suitably
compounded and packaged for installation into the
eye.
 They may be in the form of Solutions, Suspensions,
Ointments or solid dosage forms.

6. Pharmacologic Categories of Ophthalmic Drugs
• Topical anesthetics: as tetracaine, are employed to provide
pain relief preoperatively, postoperatively, for ophthalmic
trauma, and during ophthalmic examination.
• Antibiotic / Antimicrobial Agents: as gentamicin, are used
systemically and locally to combat ophthalmic infection.
• Antifungal Agents: as amphotericin B, are used topically
against fungal endophthalmitis and fungal keratitis.
• Steroidal anti-inflammatory Agents: as dexamethasone, are
used to treat inflammation of the eye, as allergic
conjunctivitis.
• Non-steroidal anti-inflammatory agents: as diclofenac, are
used to relief ocular inflammation.

7. • Antiviral Agents: as vidarabine, are used against viral
infections, as that caused by herpes simplex virus.
• Astringents: as Zinc sulfate, are used in the treatment
of conjunctivitis.
• Beta-Adrenergic Blocking Agents : as timolol maleate,
are used topically in the treatment of elevated
intraocular pressure (lOP) and chronic open angle
glaucoma.
• Miotics: as pilocarpine, are used in the treatment of
glaucoma.
• Mydriatics: allow examination of the fundus through
the dilation of the pupil (atropine).

8. • Protectants / Artificial Tears: as carboxymethyl cellulose
solutions employed as artificial tears or as a contact
lens fluids to lubricate the surface of the eye.
• Vasoconstrictors I Decongestants: as oxymetazoline
When applied topically to the mucous membranes of
the eye cause transient constriction of the conjunctival
blood vessels. They are intended to soothe, refresh, and
remove redness due to minor eye irritation.
• Anti-histamines: as pheniramine maleate, are included
in some products to provide relief of itching due to
pollen and ragweed.

9. Types of ophthalmic products
1- Ophthalmic Solutions
• It is the most common means of administering drugs to the eye.
• All ingredients are completely soluble and there is little physical
interference with vision.
• The main disadvantage of solutions is the short contact time
with the absorbing surface.
2- Ophthalmic suspensions:
• If the drug is not sufficiently soluble, it can be formulated as a
suspension.
• A suspension may also be desired to improve stability,
bioavailability, or efficacy.
• The major topical ophthalmic suspensions are the steroid anti-
inflammatory agents.

10. 3- Powders for reconstitution:
Several ophthalmic drugs are prepared as sterile powders for
reconstitution before dispensing to the patient. These include
Chloramphenicol, Epinephrine and Tetracycline hydrochloride.
The sterile powder is usually manufactured by lyophilization and
is packaged separately from the diluent, and a sterile dropper is
provided.
In powder form, these drugs are more stable (longer shelf-life)
than solution form. Each product has an expiration date for the
reconstituted solution which should be explained to the patient
with the proper storage conditions and method of usage.

11. 4- Ophthalmic Ointments:
• The ointment vehicle is usually a mixture of mineral oil and
white petrolatum. The main advantages of the petrolatum-
based ointments are:
1- Their inertness and anhydrous nature which make them
suitable vehicles for moisture-sensitive drugs.
2- They offer longer contact time and greater drug
bioavailability.
The main disadvantages of ophthalmic ointments are:
1- Greater dosage variability than solution.
2- Blurring of vision ( therefore used at nighttime ).

12. 5- Ocular Inserts (Ocuserts) :
• They are drug-containing devices that deliver one
or more drugs at a programmed rate, for a
prescribed period of time to provide continuous
control of drug therapy. Pilocarpine ocusert is an
example of this type of solid dosage form.
• The ocusert system provides a nearly steady zero-
order delivery rate of pilocarpine from the unit for
7 days when placed in the aqueous tear
environment of the eye.

13. • Advantages:
1- The ocusert exposes the patient to only one- fourth to one-eighth the amount of
pilocarpine compared to drop therapy. This could lead to reduced local side effects
and toxicity.
2- It provides a continuous around-the-clock control of intraocular pressure (lOP).
3- It provides more patient convenience and improved compliance, as the dose is
administered only once per week.
4- It is a good alternative for patients sensitive to preservatives.
• Disadvantage:
The patient must check periodically to see that the unit is still in place.
Replacement of contaminated unit with fresh one is very expensive.
5- Ocular Inserts (Ocuserts) :

14. Formulation and production of ophthalmic products
• Ophthalmic solutions are formulated to be sterile
isotonic and buffered for stability and comfort.
 Buffering and pH adjustment:
Ideally, an ophthalmic product should have a pH of 7.4 ( physiological pH of tear fluid ).
 Tonicity adjustment:
An ophthalmic solution is considered isotonic when it has an osmotic pressure equal to
that of tear fluid (equal to that of 0.9 % sod. chloride solution).
 Viscosity - imparting agents:
The USP permits the use of viscosity increasing agent to prolong the contact time in the
eye and thus enhance drug absorption and bioavailability. The major commercial viscous
polymers used are Polyvinyl alcohol (PVA) and hydroxvpropylmethylcellulose (HPMC).

15.  Preservatives and their choice
The limited choice of preservative agents is narrowed when the
requirements of chemical and physical stability and compatibility
are considered for a particular formulation and package.
a- Benzalkonium chloride:
It is the most widely used preservative .
b- Organic mercurials :
When benzalkonium chloride cannot be used.
c- Chlorobutanol :
It has relatively slower activity, but acceptable stability at room temperature
Methyl and Propylparabens:
They are used mainly to prevent mold growth, but in higher concentrations.

16. Contact Lenses
Contact lenses are classified according to chemical composition & physical
properties into:
I. Hard contact lenses:
a. They are termed hard because they are made of a rigid plastic resin,
poly- methyl-methacrylate (PMMA).
b. They are 7-10 mm in diameter.
c. They only cover a part of the cornea
d. They float on the tear layer overlying the cornea.
Advantages:
1. Durable.
2. Provide dear, crisp vision for the patient.

17. Disadvantages:
1. They require a long adoption period as long as a week for wearing
comfort.
2. Some patients find them difficult to wear. because of their
rigidity.
3. Are practically impermeable to O2 and moisture , impair corneal
epithelial respiration.
4. May cause physical damage to epithelial tissue If placed directly
on the corneal surface.
To prevent direct contact, solutions are used that wet the surface of
the lens and provide a cushioning layer between the corneal
epithelium and the inner surface of the lens.

18. II. Soft contact lenses
1. They are made of a hydrophilic transparent plastic hydroxy-
ethyl-methacrylate (HEMA), with small amounts of cross-linking
agents that provide a hydrogel network.
2. They are 13 to 15 mm in diameter.
3. They cover the entire cornea.
Advantages:
1. They contain 30 - 80% water, enable enhanced permeability to
oxygen , offer greater comfort to patient than hard lenses.
2. Because of their size and coverage, they are less likely than
hard lenses to dislodge spontaneously.
3. They are less likely to permit irritating foreign particles (e.g.
dust or pollen) to lodge beneath them.

19. Disadvantages:
1. Do not provide the same high level of visual acuity as hard lenses.
2. Are less durable than hard lenses.
There are 2 types of soft contact lens:
Daily-wear lenses must be removed at night before the wearer goes to Sleep.
Extended-wear lenses are designed to be worn >24 hrs with some approved for
up to 30 days of continuous wear.
However, lenses should not be retained in eye > 4 - 7 days without removal for
cleaning & disinfection , eye infection.
Disposable soft lenses do not require cleaning and disinfection for the
recommended period of use . They are discarded and replaced with a new pair.

20. III, Rigid gas permeable (RGP) lenses
They are constructed of materials that are O2 permeable but hydrophobic.
There are 2 types of RGP contact lens: daily-wear and super permeable
extended-wear.
Advantages
They take advantages of both soft and hard lenses.
Compared to hard lenses, RGP lenses:
1. Permit greater movement of O2 through the lens.
2. Retain the durability and ease of handling.
3. Provide greater wearing comfort.

21. Compared to soft lenses, RGP lenses:
1. Provide strength, durability longer life span", and
relatively easy care regimens.
2. Are easy to handle during insertion and removal.
3. Are more resistant to absorption of environmental
contaminants.
4. Provide superior visual acuity.