Special solution-and-suspension

Pharmaceutical Dosage FormPharmaceutical Dosage Form

Special Solutionsand

Suspensions

Ophthalmic Drug DeliveryOphthalmic Drug Delivery

Pharmaceutical preparations are applied topically to the eye to treat surface or intraocular conditions.

Ophthalmic Drug Delivery Ophthalmic Drug Delivery SystemSystem

EYE DROP• Eye drop is common• Volume of tear fluid in cul-

de-sac is about 7 to 8 μL7 to 8 μL• An eye that does not not

blink blink can accommodate a maximum of about 30 μL30 μL of fluid

• Microliter-dosing Microliter-dosing medication droppers medication droppers are not generally available

• When eye blinked, blinked, can retain only about 10 μ10 μLL

• One drop One drop is 5050μμLL• The optimal volume optimal volume

to administer, based on eye capacity, is 5 5 to 10 μLto 10 μL

• Average dropperAverage dropper delivers about 25 to 25 to

50 μL/drop.50 μL/drop.

Pharmacologic Categories ofOphthalmic Drugs

1. Anesthetics: 1. Anesthetics: provide pain relief preoperatively, stoperatively , for ophthalmic

trauma, and during ophthalmic examination.

2. Antibiotic and antimicrobial agents: 2. Antibiotic and antimicrobial agents: Used systemically and locally to combat ophthalmic infection.

3. Antifungal agents: 3. Antifungal agents: Among the agents used topically against fungal endophthalmitis and fungal keratitis.

4. Anti-inflammatory agents: 4. Anti-inflammatory agents: Used to treat

inflammation of the eye, as allergic conjunctivitis.

-Steroidal anti-inflammatory agents

-Non steroidal anti-inflammatory agents

5. Antiviral agents: 5. Antiviral agents: Used against viral infections, as that caused by herpes simplex virus.

6. Astringents: 6. Astringents: Used in the treatment of conjunctivitis.

7. Beta-adrenergic blocking agents: 7. Beta-adrenergic blocking agents: used topically in the treatment of intraocular pressure and chronic open-angle glaucoma.

8. Miotics and other glaucoma agents: 8. Miotics and other glaucoma agents: Miotics are used in the treatment of glaucoma, accommodative esotropia, and convergent strabismus and for local treatment of myasthenia gravis.

9. Mydriatics and cycloplegics: 9. Mydriatics and cycloplegics: Mydriatics - allow examination of the fundus by dilating the pupil. Cycloplegics - Cycloplegics - Mydriatics having a long duration of action.

10. Protectants and artificial tears: 10. Protectants and artificial tears: Solutions employed as artificial tears or as contact lens fluids to lubricate the eye contain agents.

11. Vasoconstrictors and ocular 11. Vasoconstrictors and ocular decongestants: Vasoconstrictors applied topically to the mucous membranes of the eye cause transient constriction of the conjunctival blood vessels.

Pharmaceutical RequirementsPharmaceutical Requirements

1. Sterility and Preservation

2. Isotonicity Value

3. Buffering

4. Viscosity and Thickening Agents

5. Ocular Bioavailability

• It is preferable to sterilize ophthalmics in their final containers by autoclaving at 121°C (250°F) for 15 minutes

• Bacterial filters work with a high degree of efficiency, they are not as reliable as the autoclave.

Ophthalmic Drug Delivery SystemOphthalmic Drug Delivery System


• The isotonicity limits of an ophthalmic solution in terms of sodium chloride or its osmotic equivalent may range from 0.6% to 2% without marked discomfort to the eye.

• Ophthalmic solution's solutes, including the active and inactive ingredients, contribute to the osmotic pressure of a solution.


• For maximum comfort, an ophthalmic solution should have the same pH as the

tears.

• The pH of normal tears is considered to

be about 7.4

• ViscosityViscosity is a property of liquids related to the resistance to flow. The reciprocal of viscosity is fluidityfluidity..

• In the preparation of ophthalmic solutions, a suitable grade of methylcellulose or other thickening agent is frequently added to increase the viscosity and thereby aid in maintaining the drug in contact with the tissues to enhance therapeutic effectiveness. Hydroxypropyl Hydroxypropyl methylcellulose and polyvinyl alcohomethylcellulose and polyvinyl alcohol are also used as thickeners in ophthalmic solutions.



• Ocular bioavailability is an important factor

in the effectiveness of an applied medication.

• Physiologic factors that can affect a drug's ocular bioavailability include protein binding, drug metabolism, and lacrimal drainage.


• Ophthalmic solutions must be sparkling clear and free of all particulate matter for

• Drug particles in an ophthalmic suspension must be finely subdivided, usually micronized.

• Must be easily and uniformly redistributed by gentle shaking of the container prior to use.

Packaging OphthalmicPackaging OphthalmicSolutions and SuspensionsSolutions and Suspensions

• Packaged in small glass bottles with separate glass or plastic droppers

• Packaged in soft plastic containers with a fixed built-in dropper.

• Ophthalmic solutions used as eyewashes are generally packaged with an eye cup, which should be cleaned and dried thoroughly before and after each use.

Proper Administration of Proper Administration of Ophthalmic Solutions and Ophthalmic Solutions and

SuspensionsSuspensions• Should be advised to wash the hands

thoroughly.

• Should inspect the dropper to make sure it has no chips or cracks.

• Ophthalmic solutions should be inspected for color and clarity.

• Should be shaken thoroughly prior to administration to distribute the suspensoid evenly.

• The cap of an eye drop container shouldbe removed immediately and returned

immediately after use.IMPORTANT: The dropper or administration

tip should be held as near as possible to the lid without actually touching the eye. DO NOT allow the dropper or administration tip to touch any surface.

IMPORTANT: Be very careful when applying this ointment. DO NOT allow the tip of the ointment tube to touch the eyelid, the eyeball, your finger, or any surface.

Contact Lenses and Care andContact Lenses and Care andUse SolutionsUse Solutions

Types of Contact Lenses1. Hard contact lenses 1. Hard contact lenses - provide durability and clear, crisp vision.

2. Soft contact lenses - 2. Soft contact lenses - are more popular than hard lenses because of their greater comfort. soft lenses do not provide the same high level of visual acuity as hard lenses.

Two general types of soft contact lens

1. Daily wear - 1. Daily wear - must be removed at bedtime

2. Extended wear - 2. Extended wear - designed to be worn for more than 24 hours, with some approved for up to 30 days of continuous wear.

- Disposable Disposable soft lenses soft lenses do not require cleaning and disinfection for the recommended period of use.

3. 3. Rigid gas permeable (RGP)contact Rigid gas permeable (RGP)contact lenses - lenses - They are oxygen permeable but hydrophobic.

Color Additives to Contact Lenses

Color additives that come into direct contact with the body for a significant period must be demonstrated to be safe for consumer use.

Care of Contact LensesContact lenses receive appropriate care

to retain their shape and optical characteristics and for safe use.

Types of solutions are used to achieve the care needs of contact lenses:

•Cleaning solutions Cleaning solutions

•Soaking solutions Soaking solutions

• Wetting solutionsWetting solutions

• Mixed-purpose solutionsMixed-purpose solutions

Products for Soft Contact Lenses

Products for Soft Contact LensesProducts for Soft Contact Lenses

Soft lenses tend to accumulate proteinaceous material that forms a film on the lens, decreasing clarity and serving as a potential medium for microbial growth.

Two main categories of cleaners:

-Surfactants - which emulsify accumulated oils, lipids, and inorganic compounds

-Enzymatic cleaners - which break down and remove protein deposits.


Storage and rinsing the lenses, saline saline solutions solutions are used, because saline maintains their curvature, diameter, and optical characteristics.


Two methods of Disinfection: Thermal (heat) Thermal (heat) – the lenses are

placed in a specially designed heating unitwith saline solution.

Chemical (no heat) Chemical (no heat) - hydrogenperoxide systems for chemical disinfectionhas become more popular

To prevent eye irritation from residual peroxide disinfection, it is necessary that the lenses be exposed to one

Types of neutralizing agents:

1. Catalytic type Catalytic type (an enzyme catalase or a platinum disk),

2. RReactive type eactive type (such as sodium pyruvate or sodium thiosulfate),

3. DiDilution–elution lution–elution typetype employing dilution techniques

Products for Hard Contact Lenses

Products for Hard Contact Products for Hard Contact LensesLenses

A surfactant cleaner surfactant cleaner is used by applying the solution or gel to both surfaces of the lens and then rubbing the lens in the palm of the hand with the index finger for about 20 seconds.

Products for Hard Contact Products for Hard Contact LensesLenses

Soaking solutions contain a sufficient concentration of disinfecting agent, usually 0.01% benzalkonium chloride and 0.01% edetate sodium, to kill surface bacteria.


Wetting solutions contain surfactants to facilitate hydration of the hydrophobic lens surface.


Combination solutions mix effects, such as cleaning and soaking, wetting and soaking, or cleaning, soaking, and wetting.

Products for RGP Contact Lenses

• One of two cleaning methods, either hand washing or mechanical washing, may be used.Hand washing Hand washing - the lens may be cleaned by holding the concave side up in the palm of the hand.Mechanical washing Mechanical washing -is advantageous because the possibility of the lens turning inside out or warping during cleaning is minimized.

Products for RGP Contact LensesProducts for RGP Contact Lenses

Nasal PreparationsNasal Preparations

Intranasal use contain adrenergic agents and are employed for their decongestant activity on the nasal mucosa.

Nasal Decongestant Solutions

Nasal decongestant solutions are employed in the treatment of rhinitis of the common cold, for vasomotor and allergic rhinitis including hay fever, and for sinusitis. Nasal decongestants are in the form of inhalants.

Inhalation Solutions

Inhalations are sterile drugs or sterile solutions of drugs administered by the nasal or oral respiratory route.

Proper Administration and Use ofNasal Drops

• Before using the drops, the patient should be advised to blow the nose gently and wash the hands thoroughly with soap and water.

• Patient should lie down on a flat surface, such as a bed, hanging the head over the edge and tilting the head back as far as comfortable.

• The dropper should be replaced in the bottle and tightened.

Proper Administration and Use ofNasal Sprays

• The patient should gently blow the nose to clear the nostrils and wash the hands thoroughly with soap and water.

• The patient should insert the nose piece into the nostril, pointing it slightly backward, and close the other nostril with one finger.

• Patients should not share their medicated spray with another person to prevent the possibility of cross contamination between individuals.

OTIC PREPARATIONOTIC PREPARATION

Otic preparations are sometimes referred to as ear or aural preparations. Solutions are most frequently used in the ear, with suspensions and ointments also finding some application

Ear preparations are usually placed in the ear canal by drops in small amounts for removal of excessive cerumen (earwax) or for treatment of ear infections, inflammation, or pain.

Cerumen-Removing Solutions

Cerumen is a combination of the secretions of the sweat and sebaceous glands of the external auditory canal.

Commercial product uses carbamide peroxide in glycerin and propylene glycol (Debrox drops, GSK)

Anti-Infective, Anti-Inflammatory,and Analgesic Ear Preparations• Drugs used topically in the ear for their

anti-infective activity include such agents as ciprofloxacin, colistin sulfate, neomycin, ofloxacin, polymyxin B sulfate, and nystatin, the latter agent used to combat fungal infections.

• These agents are formulated into eardrops (solutions or suspensions) in a vehicle of anhydrous glycerin or propylene glycol.

Proper Administration and Use ofOtic Drops

• Earwax removal drops should be instilled and then removed with an ear syringe.

• If the product is a suspension, shaken prior to withdrawal into the dropper.

• When instilled into the ear, to allow the drops to run in deeper, the earlobe should be held up and back.

Health & Medicine

Special solution-and-suspension