BP 704 T Noval Drug Delivery System Hr.

no: 57

OCCULAR FORMULATIONS

Formulation Consideration:

Physicochemical Drug Properties : It includes the factors that affcect the corneal
permeability of the drug.

• Lipophilicity of the drug as reflected by its n - octanol – water partition

coefficient
• Molecular size and shape .

Buffer Capacity and p H:

Normal Tear fluid pH 7.4 ,posses some buffering capacity.

• pH should be chosen to optimize drug stability.

• When pH deviates from 7.4.it is important to be aware of buffer capacity to
minimize
lacrimation and irritation.

Instillation Volume : Upon application of Eye droppers the excess

volume removed by Spillage (conjunctival sac ) & Nasolacrimal drainage
system.

• Formulation target is to , keeping the applied dose constant while

decreasing the instilled volume.
Formulation Consideration

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Tonicity Adjustment :

• Tonicity needs to be adjusted so that it exerts an osmotic pressure equal to

that of

tear fluids (equivalent to 0.9% NaCl ideally) .

• Ophthalmic solutions are hypotonic to enhance absorption and provide

concentration of active ingredient sufficient to achieve efficacy.

• Common tonicity adjusting agents are NaCl , Cl, buffer salt, d-mannitol,
propylene glycol etc.

Anti-oxidants:

• They are commonly added to mitigate oxidation issues.

• Example : Sodium bisulfite or metabisulfite is used in concentrations up to

0.3% in epinephrine hydrochloride and bitartrate solutions.

Surfactants:

• Several nonionic surfactants are used in relatively low concentrations to

achieve drug solubility. Eg: Polysorbate, tyloxapol, polyoxyl 40 stearate etc.

• The order of surfactant toxicity is: Anionic > cationic > nonionic

• Nonionic surfactants preferred for ophthalmic use .

Preservatives :

• Help to prevent contamination of the bottle contents over the course of multiple
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 uses.

• By preventing contamination, preservatives may help ensure product stability.

• Benzalkonium chloride is the most commonly used ophthalmic preservative and

is used

in 72% of ophthalmic solutions

CLASSIFICATION OF OCULAR DRUG DELIVERY SYSTEMS

A multitude of ocular dosage forms are available for delivery of drugs to the eye.
These can be classified on the basis of their physical forms as follows:
1. Liquids: - Solutions, Suspensions, Sol to gel systems, Sprays
2. Solids: - Ocular inserts, Contact lenses, Corneal shield, Artificial tear inserts, Filter
paper strips
3. Semi-solids: Ointments, Gels
4. Miscellaneous: Ocular iontophoresis, Vesicular systems, Muco-adhesive dosage
forms, Particulates.