opthalmic preparations, Classification,factors affecting for the drug given to eye, manufacturing

ophthalmic preparations are medications designed for ocular use, typically in the form of eye drops or ointments. these formulations aim to treat various eye conditions . requirements of the ophthalmic preparations includes sterility, buffers, tonicity etc. proper application is crucial for effectiveness, ensuring the medication reaches the eye surface while minimizing systemic absorption. packaging of ophthalmic preparations . labeling the ophthalmic pharmaceutical products. storage conditions.

1. OPHTHALMICPREPARATIONS

2. INTRODUCTION
•Ophthalmic preparations are sterile, liquid, semi-solid, or solid preparations that
may contain one or more active pharmaceutical ingredients or drugs used for
application to the conjunctival sac or conjunctiva and the eyelids.

3. CLASSIFICATION
LIQUIDS
solutions
Suspensions
Powders for
reconstitution
Solutions to
gel systems
SOLID
Ocular inserts
SEMI
SOLID
Ointments
Gels
INTRAOCULAR
Injections
Implants
Irrigation
solutions

4. CRITERIA FOR SELECTION OF A DRUG FOR OPHTHALMIC USE
❖The drug must be bio-chemically and pharmacologically potent.
❖The drug must be non toxic to both ocular and systemic tissues.
❖The drug must be sufficiently stable that neither significant loss in potency from admonished
availability nor little increase in toxicity from byproducts of degradation arises.
❖The drug can be either targetable to tissues and location of primary disease state etiology or to
sites responsible for symptomatic response.
❖The drug must be sufficiently compatible with the dosage form, and with the tissues exposed to it
, to achieve an effective pharmacokinetic tissue profile.

5. FACTORS AFFECTING ABSORPTION OF THE DRUG IN THE EYE
❖Loss of drug due to spillage
❖Drainage
❖Superficial Absorption
❖Transcorneal Absorption

6. LOSS OF DRUG DUE TO SPILLAGE
❖This takes place by spillage of drug from the eye & its removal by the
nasolacrimal drainage.
❖The normal volume of tears in the human eye is approximately 7-10 ul (if
blinking occurs).
❖The human eye can accommodate a volume of up to 30 ul without spillage from
the palpebral fissure.
❖With an estimated drop volume of 50 ul ,70% of the administered volume of 2
drops can be seen to be expelled from the eye by overflow.
❖If blinking occurs, the residual volume of 10 ul indicates that 90% of the
administered volume of 2 drops will be expelled within a few minutes.

7. DRAINAGE
❖Drainage of the drop through the nasolacrimal system into the
gastrointestinal tract begins immediately on instillation.
❖This takes place when either reflex tearing or the dosage form causes the
volume of fluid in the palpebral tissue to exceed the normal lacrimal volume
of 7-10 ul.
❖The excess fluid volume enters the superior and inferior lacrimal puncta,
moves down the canalicula into the lacrimal sac, and continues into the
gastrointestinal tract.
❖This also is the mechanism by which a patient may often sense a bitter or
salty taste, for example ammonium salts.

8. SUPERFICIAL ABSORPTION
❖Superficial absorption of drug into the palpebral and bulbar conjunctiva , with
generally concomitant rapid removal from ocular tissues by the peripheral blood
flow also is an influencing factor.

9. TRANSCORNEAL ABSORPTION
❖This route is most effective in bringing drug due to the anterior portion of the
eye.
❖Although transport of hydrophilic and macromolecular drugs has been reported
to occur by limbal or scleral routes, often this is at rates significantly reduced
from those expected for trans-corneal transport of conventional, modestly
lipophilic agents of low molecular weight.
❖Even here, transmembrane transport is a significant requirement for availability.

10. REQUIREMENTS OF OPHTHALMIC PREPARATIONS
1. Sterility
2. Tonicity
3. Ph / Buffering
4. Surface activity
5. Clarity / foreign particles
6. Viscosity / thickening agents (15 cps to 25 cps)

11. STERILITY
❖Ophthalmic solutions should be sterile when prepared, & care must be taken
to prevent contamination during use.
❖Even though ophthalmic preparations are sterile, they must contain an
effective, topically non-irritating anti-bacterial agent or a mixture of such
agents.
❖Examples:
Benzalkonium chloride – 0.01% or 0.013%
Chlorobutanol – 0.5%
Phenyl mercuric acetate – 0.004%
Phenyl mercuric nitrate – 0.004%
Thiomersal – 0.01%

12. Ophthalmic preparations are sterilized by any of the following techniques:
1. Autoclaving – this method can be preferred if the ingredients of the preparation are thermostable.
2. Filtration – this method involves transfer of solution into final containers after passage through the filter.
Filtration uses positive or negative pressures.
3. chemical sterilization – this method involves, all solutions should be made with sterile distilled water
and solution should be dispensed in a sterile container.

13. TONICITY
❖Ophthalmic preparations must be isotonic.
❖If hypertonic solution – the solution could cause the drawing of water toward the
site of the topical application.
❖If hypotonic solution – the solution might induce the hemolysis of red blood
cells, or the passage of water from the site of an ophthalmic application through
the tissues of the eye.

14. pH & BUFFERS
❖The pH values of ophthalmic solutions are adjusted to range at which an
acceptable shelf life stability of at least 2 years can be achieved.
❖The buffer system of an ophthalmic solution contributes to stability in another
way by preventing an increase in the pH of the solution due to the normal
leaching by the solution of alkali from the glass container.
❖Buffers are used in an ophthalmic solution for the following reasons:
1. To reduce discomfort to the patient.
2. To ensure drug stability and safety.
3. To control the therapeutic activity of the drug substance.

15. SURFACE ACTIVITY
❖ The vehicles used in ophthalmic preparations must have good wetting
property.
❖Examples – Benzalkonium chloride
polysorbate 80
polysorbate 20
Dioctyl sodium sulfosuccinate
❖These agents must be suitable for ophthalmic use and should not interact with
any of the ingredients of the ophthalmic preparation.

16. CLARITY / FOREIGN PARTICLES
❖The ophthalmic solutions must be clear and free from foreign particles such as fibres
and filaments.
❖The ophthalmic solutions are subjected to filtration to obtain desired clarity.

17. VISCOSITY
❖Viscosity can be increased by using thickening agents.
❖To increase the time of contact of the drug with the eye, the viscosity of the
preparation is increased.
❖Examples: PVA, PEG, MC, CMC etc.
❖These should posses the following ideal properties:
1. These should be easy to filter.
2. These should be easy to sterilize.
3. These should be compatible with other ingredients
4. These should possess requisite refractive index and clarity.

18. MANUFACTURING FACILITIES
❖Environment: Environmentally controlled areas are used for the manufacture.

❖Class 100 space is the area where not more than 100 particles are present per
cubic foot of air of a diameter of 0.5 micrometer or larger.
❖Class 1,00,000 space is required for the storage of raw materials, finished
products.
❖Raw materials: highest quality pharmaceutical products used to the
manufacturing process.
❖Equipments : all tanks, valves, pumps and piping must be of the best available
grade of corrosion-resistant stainless steel.

19. TYPES OF MANUFACTURING
❖Ophthalmic drops
❖Ophthalmic suspensions
❖Ophthalmic lotions
❖Ophthalmic ointments
❖Ophthalmic inserts

21. PACKAGING OF OPHTHALMIC PREPARATIONS
Ophthalmic solutions, lotions and suspensions have been packed almost entirely in
plastic bottles since the introduction of droptainer plastic dispenser. A few products still
remain in glass dropper bottles because of special stability considerations.
❖Plastic droptainer bottles
❖Glass dropper bottles
❖Metal collapsible tubes
❖Plastic collapsible tubes

22. Ophthalmic ointments are packaged in:
❖Aluminium tubes have been used because of their lower cost and as an alternative
should the supply of tin.
❖Plastic tubes made from flexible LDPE resins
❖Small collapsible tin tube usually holding 3.5g of product, the pure tin tube is
compatible with a wide range of drugs in petrolatum based ointments.

23. LABELING
❖The name of the pharmaceutical product.
❖The names of the active ingredients.
❖The batch number assigned by the manufacturer.
❖The concentrations of the active ingredients and the amount or the volume of
preparation in the container.
❖The expiry date, the utilization period and when required, the date of
manufacture.
❖Any special storage conditions or handling precautions that may be necessary.

24. ❖If applicable, the period of use after opening the container.
❖Directions for use, warnings and precautions that may be necessary.
❖The name and address of the manufacturer or the person responsible for placing
the product on the market.
❖The statement “This preparation is sterile”.

25. STORAGE
❖Ophthalmic preparations should maintain their integrity throughout their shelf – life
when stored at the temperature indicated on the label.
❖Special storage recommendations or limitations are indicated in individual
monographs.

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