By :Dr.safia A. Alrezami

Ophthalmic Preparations

by Dr.safia alrezami.

1.Definiation.2.Dosage form. 3. Principle of ocular drug absorption.4.Ophthalmic solution.5. Ophthalmic suspension.6. Ophthalmic ointment.7.Ocuserts (Ophthalmic inserts).7.Example of drugs used to treat eye disease .

Content

1.Definitionare sterile, liquid, semi-solid, or solid preparations that may contain one or more active pharmaceutical ingredient intended for application to the conjunctiva, the conjunctiva sac or the eyelids.2.Classification Of Ocular Drug Delivery Systems:

by Dr.safia alrezami.

Ophthalmic Preparations

Liquid Topical eye

drops:Solutions

Suspensions Sol to gel systems

Semi-solid

Ointments

lotion

Gels

SolidOcular inserts

Insoluble insert

soluble insert

by Dr.safia alrezami.

3.drug absorption The sclera: The protective outer

layer of the eye, referred to as the “white of the eye” and it maintains the shape of the eye. The cornea: The front portion of the sclera, is transparent and allows light to enter the eye.

Ophthalmic Preparations

Non- corneal absorption:Penetration across sclera & conjunctiva

into intra ocular tissues.Corneal absorption:Outer epithelium: rate limiting barrier, with

pore size 60a, only access to small ionic and lipophilic molecules.

by Dr.safia alrezami.

1- Ophthalmic Solutions: are sterile solutions, essentially free from foreign particles, suitably compounded and packaged for instillation into the eye. Nearly all the major ophthalmic therapeutic agents are water soluble salts

The selection of the appropriate salt depend on : solubility - ocular toxicityThe effect of pH, tonicity, and buffer capacityExamples of topical eye drops :Atropine sulphate eye drops.Disadvantages of eye solutions:1-The very short time the solution stays at the eye surface.2- Its poor bioavailability.

A. Topical Eye drops:Ophthalmic

Preparations

by Dr.safia alrezami.

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 the container.

If the drug is not sufficiently soluble, it can be formulated as a suspension.

A suspension may also be desired to improve stability, Bioavailability ,and efficacy.

The major topical ophthalmic suspensions are the steroid anti-inflammatory agents. Examples :Prednisolone acetate suspension.

An ophthalmic suspension should use the drug in a microfine form; usually 95% or more of the particles have a Diameter of 10µm or less.

Ophthalmic Preparations

by Dr.safia alrezami.

3- Gel-Forming SolutionsSolution 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.

Ophthalmic Preparations

by Dr.safia alrezami.

B. Semisolid Dosage Forms:Ophthalmic ointment : must be sterile. The ointment base selected for an ophthalmic ointment must be nonirritating to the eye and must permit the diffusion of the active ingredient throughout the secretions bathing the eye. a longer ocular contact time E.g. Tetracycline ointment.Disadvantage:

Their are greasy nature ,blurring of vision.

Ophthalmic Preparations

by Dr.safia alrezami.

C. Solid Dosage Forms(Ocular Inserts)Ophthalmic inserts are defined as sterile solid or semisolid preparations, with a thin, flexible and multilayered structure, for insertion in the conjunctival

sac. Advantages:

1.Increasing contact time and improving bioavailability.

2.Providing a prolong drug release.3.Reduction of adverse effects.

4.Reduction of the number administrations and thus better patient compliance.

Ophthalmic Preparations

by Dr.safia alrezami.

1.Insoluble insert is a multilayered structure consisting of a drug containing core surrounded on each side by a layer of copolymer membranes through which the drug diffuses at a constant rate

2.Soluble insert consists of all monolytic polymeric devices that at the end of their release, the device dissolve.

Ophthalmic Preparations

by Dr.safia alrezami.

Contact Lenses & Care SolutionsTypes of contact lenses: 1- Hard contact lenses. 2- Soft contact lenses. 3- Rigid gas permeable (RGP). Products for soft contact lenses:Products for soft contact lenses:Cleaners(To remove lipid and protein debris)- formulation:1- viscolizing surface-active agent: to enable gentle friction with fingertips2- antibacterial-fast acting: benzalkonium chlorideRinsing and storage solutions of Soft contact lenses- Facilitate lens hydration, Inactivation of microbial contamination

and prevent the lens from drying out.

Ophthalmic Preparations

by Dr.safia alrezami.

Contact Lenses & Care Solutions

Rinsing and storage solutions of Hard contact lensesFor cleaning, microbial inactivation and hydrationFormulation:osurface-active agentoAntimicrobial:(0.01% benzalkonium chloride + 0.1% sodium

edetate )Wetting solutionsoTo achieve rapid wetting by the lachrymal fluid and promote

comfort Facilitate insertion of the lenso Provide lubricationBuffering solutions : Hypromellose eye drops B.P.C.

Ophthalmic Preparations

by Dr.safia alrezami.

Manufacturing 1.A.P.I2.Vehicle3.Buffer4.Ph5.Isotonisity 6.Antioxidant& Stabilizers 7. Surfactants

Ophthalmic Preparations

by Dr.safia alrezami.

Quality control oSterility Tests oLeakage tests

oParticle size test .oClarity test oAssay test

Ophthalmic Preparations

by Dr.safia alrezami.

Package 1. Eye drops a. plastic dropper bottles the cap is made of harder resin than the bottle.b. The glass bottle.

2.Ophthalmic ointment are packaged in :1.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.2.Aluminum tubes have been used because of their lower cost and as an

alternative should the supply of tin.3.Plastic tubes made from flexible LDPE resins

Ophthalmic Preparations

by Dr.safia alrezami.

Labeling *  the name of the pharmaceutical product.* the name(s) of the active ingredient(s).* the concentration(s) of the active ingredient(s) and the amount or the

volume of preparation in the container.* the batch number assigned by the manufacturer.* the expiry date, the utilization period, and, when required, the date of

manufacture.* any special storage conditions or handling precautions that may be

necessary.* 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".

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.

Ophthalmic Preparations

by Dr.safia alrezami.

7.Example of drugs used to treat eye disease

1.Anti-glucoma drugs e.g. pilocarpine.

2.Diagnostic drugs e.g. sodium fluorescein.

3.Topical Anesthetics e.g. Tetracaine.

4.Miotics e.g. pilocarpine.

5.Mydriatics e.g. Atropine.

6.Cycloplegics e.g. Atropine.

7.Anti-inflammatories e.g. corticosteroids.

8.Anti-infectives (antibiotics, antivirals and antifungal).

9.Protects.

Ophthalmic Preparations

by Dr.safia alrezami.

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