The document discusses ophthalmic preparations, which are specialized dosage forms designed for administration to or around the eye. It covers ideal characteristics, types of formulations including solutions, suspensions, ointments and inserts. General considerations for safety, formulation, drugs used, evaluation tests and packaging are described. The key types are solutions, suspensions and ointments as the most commonly used ophthalmic dosage forms, with newer forms including gels, inserts and intraocular injections. Safety must ensure sterility, lack of toxicity and appropriate tonicity, pH and viscosity. Evaluation includes sterility testing, clarity assessment and checking for leaks or particles.

1. OPHTHALMIC PREPARATIONS
Subject- Pharmaceutical Product Development
DEPARTMENT OF PHARMACEUTICAL SCIENCES
Dr. Hari Singh Gour Vishwavidyalaya
Sagar(M.P)-470003, India
(A Central University)
Submitted By:
DEBASIS SEN
M.PHARM 1st SEMESTER
(Y22254008)
Submitted To:
Prof. SANJAY K JAIN
(Professor, DOPS)
Dr. DHARMENDRA JAIN
(Assistant Professor, DOPS)

2. CONTENT
• INTRODUCTION
• IDEAL CHARACTERISTICS
• TYPES
• GENERAL CONSIDERATIONS
• FORMULATION CONSIDERATIONS
• DRUGS USED IN OPHTHALMIC PREPARATION
• DIFFERENT FORMULATIONS
• EVALUATION TESTS
• DRUG PRODUCT QUALITY TESTS
• PACKAGING
• CONCLUSION
• REFERENCES

3. INTRODUCTION
• Ophthalmic preparations are specialized dosage forms designed to be instilled onto the
external surface of the eye (topical), administered inside (intraocular) or adjacent
(periocular) to the eye or used in conjunction with an ophthalmic device.
• The most commonly employed ophthalmic dosage forms are solutions, suspensions and
ointments.
• The newest dosage forms for ophthalmic drug delivery includes gel, gel forming
solutions, ocular inserts, intravitreal injections and implants.

4. IDEAL CHARACTERISTICS
Following characteristics are required to optimize ocular drug delivery systems-
• Good corneal penetration.
• Prolong contact time with corneal tissue.
• Non irritative and comfortable form.
• Appropriate rheological properties.
• The buffer system must be considered with tonicity and comfort in mind.
• pH must be optimum.
• Must be free from foreign particles.

5. TYPES OF OPHTHALMIC DOSAGE FORMS
Liquid
Solutions
Suspensions
Powders for
reconstitution
Sol to gel
system
Semisolid
Ointments
Gels
Solid
Ocular inserts
Intraocular
Injections
Implants
Irrigating
solutions

6. GENERAL SAFETY CONSIDERATIONS
A. Sterility
Every ophthalmic product must be manufactured under conditions validated to render it
sterile in its final container.
USP recognizes six methods of achieving a sterile product:
• Steam sterilization
• Dry heat sterilization
• Gas Sterilization
• Sterilization by ionizing radiation
• Sterilization by filtration
• Aseptic processing

7. B. Ocular toxicity and Irritation
• Albino rabbits are used to test the ocular toxicity and irritation of ophthalmic
formulations.
The procedure based on the examination of the conjunctiva, cornea or the iris.
• USP procedure for plastic containers-
i. Containers are cleaned and sterilized as in the final packaged product.
ii. Extracted by submersion in saline and cottonseed oil.
iii. Topical ocular instillation of the extracts and blanks in rabbits is completed and ocular
changes examined.

8. C. Preservation and Preservatives
• Preservatives are included in multiple dose eye solutions for maintaining the product
sterility during use.
• The use of preservatives is prohibited in ophthalmic products that are used at eye surgery
because, if the sufficient amount of preservative is contacted with the corneal
endothelium, the cells can become damage and possible loss of vision.
• The most common organism is Pseudomonas aeruginosa that grow in the cornea and
cause loss of vision.
D. Drug and Excipient interaction
• The formulator should predetermine the extent and nature of the interactions between the
drug and excipients and conduct sufficient testing to develop an effective formulation.

9. FORMULATION CONSIDERATIONS
1. Foreign Particles
All the ophthalmic products should be clear and free from foreign particles, fibres and
filaments.
Ophthalmic solutions should be clarified very carefully by passing through bacteria proof
filters such as membrane filters, sintered glass filters.
The particle size of the eye suspension should be in an ultrafine state to minimize irritation.
2. pH
pH plays an important role in therapeutic activity, solubility, stability and comfort to the
patient.

10. 3. Viscosity
In order to prolong the contact time of the drug in the eye, various thickening agents are
added in the ophthalmic preparations.
Polyvinyl alcohol (1-4%), polyethylene glycol, methyl cellulose, carboxy methyl cellulose
are some of the commonly used thickening agents.
An ideal thickening agent should possess the following properties-
• It should be easy to filter
• It should be easy to sterilize
• It should be compatible with the other ingredients

11. 4. Sterility
Ophthalmic preparations must be sterile when prepared.
Pseudomonas aeruginosa is a very common gram –ve bacteria which is generally found to
be present in ophthalmic products. It can cause complete loss of eye sight in 24-48 hrs.
To maintain sterility in multidose containers, preservatives are added-
• Non-toxic
• Non-irritant
• Should be compatible with medicaments.

12. 5. Tonicity
• Ophthalmic products should be isotonic with lachrymal secretions to avoid discomfort and
irritation.
• A range of 0.2-2% NaCl equivalency does not cause any noticeable pain and a range of
about 0.2-0.7% should be acceptable for most persons. e.g.- NaCl, KCl, Buffer salt,
propylene glycol and mannitol.
6. Surface Activity
Vehicles used in the ophthalmic preparations must have good wetting ability to penetrate
cornea and other tissues.
It should not cause any damage to the tissue of eye.
e.g.- Benzalkonium chloride, polysorbate 20, polysorbate 80 are some surfactants which are
commonly used.

13. THERAPEUTIC CLASSES OF DRUGS CURRENTLY USED IN
OCULAR DISEASES
Drugs Class Clinical Use Dosage Form
Acyclovir
Trifluridine
Antiviral Against viral
infection
Eye ointment
Eye drop solution
Oxybuprocaine
Procaine
Local Anaesthetic Tonometry
Contact lens fitting
Eye drop solution
Dexamethasone
Hydrocortisone
Anti-inflammatory Inflammation Eye drop solution
Chloramphenicol
Tetracycline
Antibacterial Eye infection Eye ointment
Eye drop solution
Betaxolol
Timolol
Beta-Adrenergic
blocker
Treatment of
glaucoma
Eye ointment
Eye suspension
Eye drop solution
Tropicamide
Ephedrine
Mydriatics Examination Eye drop solution
Eye Ointment

14. DIFFERENT FORMULATIONS
A. TOPICAL EYE DROPS:
1. Ophthalmic solutions
Sterile solutions, essentially free from foreign particles, suitable compounded and packaged for
instillation into the eye.
The selection of appropriate salt depend on-
• Solubility
• Ocular toxicity
• The effect of pH, tonicity and buffer capacity.
Disadvantages
• The solution stays at the eye surface for very short time.
• Its poor bioavailability.

15. 2. Ophthalmic Suspensions
• Contain solid particles dispersed in a liquid vehicle, they must be homogeneous when
shaken gently and remain sufficiently dispersed to enable the correct dose to be removed
from container.
• An ophthalmic suspension should use the drug in a microfine form, usually 95% or more
of the particles a diameter of 10μm or less.
• The major topical ophthalmic suspensions are the steroid anti-inflammatory agents.
Example- Prednisolone acetate suspension.
3. Gel forming Solutions
Solutions that are liquid in the container and thus can be instilled as eye drops but forms gel
on contact with the tear fluid and provide increased contact time with the possibility of
improved drug absorption and duration of therapeutic effect.

16. B. SEMI SOLID DOSAGE FORMS:
Ophthalmic ointment
• Must be sterile.
• The ointment base selected for an ophthalmic ointment must be non-irritating to the eye
and must permit the diffusion of active ingredients throughout the eye.
• e.g.- Tetracycline ointment.
Disadvantage
• They are greasy in nature.
• Make blurring of vision.

17. C. SOLID DOSAGE FORMS:
Ocular Inserts
These are the sterile solid or semisolid preparations, with a thin flexible and multi-layered
structure, for insertion in the conjunctival sac.
Advantages
• Increasing contact time and improving bioavailability.
• Providing a prolong drug release.
• Reduction of adverse effects.
• Reduction in the number of administration and thus better patient compliance.
Types
Insoluble Inserts
Soluble Inserts

18. CONTACT LENS:
• Are small visual devices made with curved pieces of plastic.
• Shaped in a way to confirm directly to the wearing eye.
Hard Contact Lens
•Hard hydrophobic
Polymethylmethacrylate
i. Difficult to get used to
ii. Uncomfortable to wear
iii. Does not allow oxygen
to pass
Rigid Gas Permeable
i. Rigid and flexible
(silicon)
ii. More permeable to
oxygen than soft lens
iii. Better vision, durable
iv. Easier to clean
Soft Contact Lens
i. Most common lens
ii. Hydrophilic
iii. Immediate comfort
iv. More permeable to
oxygen

19. EVALUATION OF OPHTHALMIC PREPARATIONS
QUALITY CONTROL TESTS:
A. STERILITY TEST:
Two basic methods for sterility testing-
• Direct Inoculation Method
It involves the direct introduction of product test samples into the culture media.
• Membrane filtration Method
It involves filtering test sample through membrane filter, washing the filter with fluid to remove
inhibitory property and transferring the membrane aseptically to appropriate culture media.
Detection of contamination used to two culture media-
A. Soyabean-casein digest medium- Incubated at 20-25°C
B. Fluid thioglycolate medium- Incubated at 30-35°C on 7 days

20. B. CLARITY TEST:
This is done by two methods-
• Visual Inspection
Under a good light, baffled against reflection into the eye and viewed against a black and
white background.
• Instrumental Method
It is based on the principle of light scattering, light absorption and electrical resistance to
obtain particle count and size distribution- destruction of product units for quality control
testing.
Instrumental method utilizing video image projection detects moving particles without
destruction of product units.

21. C. LEAKER TEST:
• Select 10 tubes of the ointment with seals applied when specified.
• Thoroughly clean and dry the exterior surface of each tube with an absorbent cloth.
• Place the tubes in horizontal position on a sheet of absorbent blotting paper in an oven
maintained at temperature of 60± 3°C for 8 hours.
• If leakage is observed from one, but more than one of the tubes repeat the test with 20
additional tubes of the ointment.
• The requirement is met if no leakage is observed from the first 10 tubes tested or if
leakage is observed from not more than one of 30 tubes tested.

22. D. METAL PARTICLES IN OPHTHALMIC OINTMENT:
• Extrude as completely as practicable the content of 10 tubes individually into separate,
clear, flat-bottom, 60mm petri dishes that are free from scratches.
• Cover the dishes and heat at 85°C for 2 hours, increasing the temperature slightly if
necessary to ensure that a fully fluid state is obtained.
• Taking precautions against disturbing the melted sample, allow each to cool to room
temperature and to solidify.
• Remove the cover and examine the bottom of petri dish for metal particles with
microscope with 30 time magnification equipped with an eye piece micrometer disk.
• Count the number of metal particles that are 50μm or large.
• The requirements are met if the total number of metal particles in all 10 tubes does not
exceed 50 and if not more than 1 tube is found to contain more than 8 particles.

23. Drug Product Quality Tests- Universal Tests
For the identification of drugs present in the ophthalmic
preparation
Identification
For determination of drug content in the ophthalmic
preparation
Assay
Determine the stability of the Ophthalmic preparation
pH
In practice, tonicity limits may range from 0.2-2% NaCl
Osmolarity
To minimize the bacterial endotoxin
Bacterial Endotoxin
Content uniformity or weight uniformity
Uniformity of Dosage
Form

24. PACKAGING
Eye Drops ( Single-dose containers)
•Plastics bottles (LDPE) are widely used.
Eye Drops (Multi-dose containers)
•Glass bottles with rubber teat dropper
•Now a days plastic bottles (LDPE) are widely used
Eye Ointment
•Flexible plastic or collapsible metal tubes are used
•Caps or closures are made of polypropylene

25. Plastic Containers
• Thermoplastic polymers are used
Ampoules
•A parenteral product container made entirely of glass
Vials
•A glass or plastic container closed with a rubber stopper and sealed
with an aluminium crimp.

26. CONCLUSION
There has been considerable progress in ophthalmic pharmaceutics during the last
decade. Ophthalmic preparations come in various preparations to suit different patient
needs. The choice of preparation depends on the specific condition being treated, patient
preference and healthcare provider’s recommendations. Ophthalmic preparations can
effectively treat a range of eye conditions when used as directed.

27. REFERENCES
1. Maulvi FA, Ranch KM, Desai AR, Desai DT, Shukla MR. Ophthalmic preparations.
InRemington 2021 Jan 1 (pp. 565-575). Academic Press.
2. Chowhan M, Lang JC, Missel P. Ophthalmic preparations. Remington. 2012:541.
3. Aldrich DS, Bach CM, Brown W, Chambers W, Fleitman J, Hunt D, Marques M, Mille
Y, Mitra AK, Platzer SM. Ophthalmic preparations. US Pharmacopeia. 2013
Sep;39(5):1-21.

28. THANK YOU