allergies, bacterial & viral infections, glaucoma and other
eye conditions Q2:Which application is most often used to deliver a drug to the eye? solution- have a short duration action but spread easily over the globe of the eye Q3:What base is primarily used for Ophthalmic ointment preparations white petrolatum Powders incorporated in the preparation must be micronized and sterilized to ensure that the final preparation is not gritty and thus is nonirritating The size of the particles in an Ophthalmic suspension must be small enough that they do not irritate or scratch the cornea. The micronized form is required. Ophthalmic suspensions must be free from agglomeration or caking. When preparing Ophthalmic solutions you must consider these physiochemical parameters: Clarity tonicity pH/buffers sterility This is usually used to remove particles and achieve clarity of the solution Filtration The ideal tonicity is 300 mOsm/L however a range of 200 to 600 mOsl/L is acceptable A sodium chloride equivalent is defined as the amount of sodium chloride that is osmotically equivalent to 1g of the drug Agents used to adjust tonicity Boric acid Dextrose Glycerin Mannitol Potassium Chloride Sodium Chloride Ophthalmic solutions must be... sterile Sterility of an Ophthalmic solution is best achieved by... sterile filtration which involves a 0.45 or 0.2 micron and filtering into a container Other methods of sterilizing or components of Ophthalmics include... dry heat steam under pressure (autoclaving) gas sterilization with ethylene oxide Because most Ophthalmic solutions and suspensions are prepared in multidose containers, they must be... preserved with a preservative A preservative must be... compatible with the active active drug and other excipients Q4:DO unit dose preparations need to be preserved? no they can be preservative free Examples of antioxidants used for Ophthalmics EDTA sodium bisulfite sodium metabisulfite thiourea Viscosity enhancers allow the preparation to remain longer in the eye to allow for more time for the drug absorption and effect. The most common viscosity enhancer used in Ophthalmics is... methylcellulose With a viscosity enhancer (actually all enhancers) it is important for this to be maintained clarity Storage of Ophthalmic solutions should be stored at room temp or refrigerated (refrigeration decreases microbial growth) Ophthalmic preparations should be labeled with For the eye Do not touch the eye or eyelid Store as directed Dispose after (appropriate date) BUD for Ophthalmics ... follows USP 797 because it is a sterile preparation Patient counseling... -cautioned not to allow the tip of dropper to touch eye or any part of the eye -allow the drug to freely fall into the eye an not to allow the drug to touch the eye How many drops should be administered to the eye at once.. 1 drop For more than one drop or more than one drug is to be administered the patient should wait how long between doses to allow the drug to be distributed and absorbed wait about 5 minutes an advantage of an Ophthalmic suspension is... they dissolve slowly and remain in the cul-de-sac longer Ophthalmic ointments provide maximum contact between the drug and the eye because they are cleared quite slowly (0.5% per minute) from the eye T/F: the size of the drop delivered can vary with the angle of the dropper and the size of the dropper orifice true Otic suspensions can be used when a long duration of drug effect is desired or when the drug is not soluble in the vehicles commonly used in otic preparations Categories of medications commonly use in the ear are: Local anesthetics Cleaning agents- peroxides Anti-infectives Antifungals Liquids for cleaning, warming, or drying the external ear and for removing any fluids that can be entrapped by local ear wax build up Vehicles most often used in otic suspensions are glycerin propylene glycol PEGs such as PEG 300 agents are primarily used for otic irrigation water and alcohol good oil vehicles Vegetable and olive oil -Mineral oil is the vehicle used for some antibiotics Otic ointments primarily use this vehicle petrolatum physiochemical considerations when developing otic preparations Solubility Viscosity Tonicity Surfactant properties Preservatives Although sterility is not generally a consideration the preparations need to be ... clean Why is the viscosity of an otic preparation important keeps the medication in the ear canal; if the medication is too thin it will drain out of the ear If the otic preparation is hypertonic some fluid can be withdrawn from the ear and thereby releasing some pressure Many otic preparations are self preserving because of the high concentration of glycerin, propylene glycol Packaging of otic preparations Otic preparations should be packaged in dropper containers, or tubes appropriate and method of administration Storage of otic preparations -should be stored at room temp or in refrigerated temps -they should not be frozen Labeling for otics labeled "for the ear" "discard after appropriate date" "use only as directed" Stability for otics These preparations do not generally have to be sterile but do need to be "clean" so the BUD is 30 days for topical; and water-containing formulations. patient counseling for otics instructed how to apply drops to the ear from dropper bottles and they should be told to place a cotton or gauze pad in the ear to keep the liquid from escaping. Nasal solution Preparations: nasal solutions are prepared for administration either as sprays or drops. Nasal suspensions: are liquid preparations containing insoluble materials Nasal gels and ointments are... semisolid preparations for nasal application that can be used either local or systemic effects Gels have what type of solubility water soluble what is collunaria is the term for early nasal preparations that contained various oils as the vehicles...this shifted to aqueous vehicles because the oil could harmful to the nose In addition to the active drugs nasal preparations contain a number of excipients which include: vehicles buffers preservatives tonicity adjusting agents gelling agents antioxidants ( if required) Ingredients used in nasal preparations must be non irritating and compatible with the nose Physiochemical considerations: A vehicle for a nasal solution should have a pH in the range of 5.5-7.5 and have a mild buffer capacity Physiochemical considerations: A nasal solution should be isotonic, stable, preserved and compatible with normal ciliary motion. -and it should not modify the normal mucous viscosity Physiochemical considerations pH & buffering: Nasal preparations are ordinarily buffered at a pH of maximum stability for the drugs they contain The buffer system of nasal preparation should be designed to maintain the pH... throughout the expected shelf life of the preparation but with a low buffer capacity Generally pH range is considered to be optimum is 4-8 buffering systems are usually compatible with most nasal medications... phosphate buffer system The preferred agents for adjusting of nasal solutions are: sodium chloride and dextrose tonicity isotonic equivalent to 0.9% NaCl If tonicity is BEYOND range what happens to the ciliary movement slows down or even stops Tonicity values ranging ___ NaCl equivalency are generally acceptable 0.6 to 1.8% If a solution is hypotonic you can add this to the substance to attain the proper tonicity NaCl, boric acid, dextrose What tonicity is ideal for nasal otics 300 mOsm/L or a range of 200-600 Are nasal preparations required to be sterile no preservations: yes because they are prepared in multiuse containers The preservative must be compatible with... ACTIVE DRUG & EXCIPIENTS