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Opthalmic drug delivery


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Examples of drug types on opthalmic drug delivery and its requirements. Based on the Hansel's Pharmaceutical Dosage Forms book.

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Opthalmic drug delivery

  1. 1.  Have additional requirements
  2. 2.  Anesthetics – employed to provide pain relief preoperatively, postoperatively, for ophthalmic trauma and during ophthalmic examinations.  Examples: tetracaine, cocaine, proparacaine
  3. 3.  Antibiotic and anti-microbial agents – used systematically and locally to combat ophthalmic infection.  Examples: azithromycin, gentamicin sulfate, sodium sulfacetamide, ciprofloxacin, hydrochloride, ofloxacin, polymyxin Bbacitracin and tobramycin
  4. 4.  Antifungal agents – agents used topically on the eye against fungal endophtalmitis and fungal keratitis  Examples: amphotericin B, natamycin, flucytosine
  5. 5.  Anti-inflammatory agents – used to treat inflammation of the eye, as allergic conjunctivites.  Examples: fluoromethalone, prednisolone, and dexamathasone salts.  Examples of non-steroidal: dicolfenac, flurbiprofen, keterolac and suprofen.
  6. 6.  Anti-viral agents – used against viral infections that are caised by herpes simplex virus.  Examples: trifluridine, ganciclovir, vidarabine
  7. 7.  Astringents – used in treatment of conjunctivitis  Examples: Zinc sulfate
  8. 8.  Beta adrenergic blocking agents – used topically on the eye in the treatment of intraocular pressure and chronic open-angle glaucoma  Examples: betaloxolol HCl, levobunolol HCl, metipranolol HCl, timolol maleate
  9. 9.  Miotic and other glaucoma agents – used in the treatment fo glaucoma, accomodative esotropia, convergent strabismus, and for local treatment of myasthenia gravis.  Examples: pilocarpine, ecothiophate
  10. 10.  Mydriatics and cycloplegics – allow the examination of the fundus by dilating the pupil. Mydriatics that have a long term of dilating are called cycloplegics  Examples: atropine, scopalamin, phenylephrine, hydrox yamphetamine, and tropicamide
  11. 11.  Protectants and artificial tears – solutions employed as artificial tears or as contact lens fluids lubricate the eye  Examples: carboxy methyl cellulose, polivinyl alcohol
  12. 12.  Vasoconstrictors and ocular decongestants – applied topically to the mucuos membranes of the eye cause transient constriction of the conjunctival blood vessels. They are intended to soothe, refresh, and remove redness due to minor eye irritation.  Examples: naphazoline, oxymetazoline and tetrahydrazoline hydrochlorides.
  13. 13.  -must be sterilized for safe use Autoclaving(in final containers) at 121 Celsius for 15 minutes is preferable but may cause thermal instability. So Bacterial Filters may be used. To keep the steriliy during use, antimicrobial preservatives are generally included in opthalmic operations.
  14. 14.  Opthalmic solutions should be isosmotic at 0.9% NaCl solution because 0.9% NaCl is the corresponding osmotic pressure of the body fluids including blood and tears.  Hypertonic solutions may draw water from the body tissues toward the solution and may cause crenation(shrinking) of blood cells  Hypotonic solutions may cause hemolysis of blood cells or passage of water from the site of an ophthalmic application throught the tissues of the eye
  15. 15. For greater comfort to the eye  Render the formulation more stable  To enhance the aqueous solubility of the drug  To enhance the bioavailability  To maximize preservative efficacy   pH of normal tears are 7.4, but tears of contact lens wearers are more acidic.  Desired solution is prepared from two stock solutions, one containing 8g of monobasic sodium phosphate per liter and the other containing 9.47g of dibasic sodium phosphate per liter.
  16. 16.  Viscosity is a property of liquids related to resistance to flow. Fluidity is the reciprocal of viscosity.  Thickening agents – methycellulose  Used to increase ophthalmic solutions’ therapeutic effectiveness
  17. 17.  Ophthlamic solutions must be sparkling clear and free of all particulate matter for comfort and safety.  Drug particles in an ophthalmic suspension must be finely subdivided, usually micronized to minimize eye irritation and/or scratching of the cornea. The suspended particles must not associate into large particles upon storage and must be easily and uniformly redistributed by gentle shaking prior to use.  If large particles/crystals form and is placed on the eye, it may hurt like hell. Lol 
  18. 18.  Small glass bottles with seperate glass or plastic dropepers.  Most are packaged in soft plastic containers w/ a fixed built in dropper. This is preferred both to facilitate administration and to protect the product from external contamination.  Patients must be careful to protect ophthalmic solutions or suspensions from external contamination
  19. 19. - wash hands thoroughly  - inspect dropper to make sure it has no chips or cracks (if applicable)  - ophthalmic solutions should be inspected for color and clarity. Suspensions should be shakened prior to administration
  20. 20. To instill eyedrops:  - patient should tilt head back with index finger of the free hand gently pull downward the lower eyelid of the affected eye to form a pocket or cup.  - while looking up and w/out touching the dropper, prescribed number of the drops should be instilled into the formed pocket.  - lower eyelid should be released and the eye closed to allow the medication to spread over the eye. Eye should be held closed for 1 min. w/out blinking rubbing or wiping.  While eye is closed, gentle pressure should be applied just under the inner corner of the eye to compress the nasolacrimal duct to prevent drainage.  -excess liquid may be wiped with a tissue 