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The Importance of Optimizing Corneal Penetration

  • Conference paper
Ophthalmic Drug Delivery

Part of the book series: FIDIA Research Series ((FIDIA,volume 11))

Abstract

The extent of absorption occurring from the instillation of drugs topically to the eye is severely limited by physiological constraints. Consequently, it is important to consider optimizing corneal penetration in the development of a new ophthalmic drug. For some drugs an increase in the penetration rate results in a dramatic increase in effect. However, for certain drugs other pharmacokinetic processes, i.e. distribution, may be more critical to increased effectiveness. Examples are presented.

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References

  • Anderson JA, Davis JL and Wei CP (1980) Site of Ocular Hydrolysis of a Prodrug and a Comparison of Its Ocular Metabolism with That of the Parent Compound, Epinephrine. Invest Ophthalmol Vis Sci 19: 817–823.

    Google Scholar 

  • Bundgaard H, Falch E, Larsen C, Mosher GL and Mikkelson TJ (1985) Pilocarpic Acid Esters as Novel Sequentially Labile Pilocarpine Prodrugs for Improved Ocular Delivery. J Med Chem 28: 979–981.

    Article  PubMed  CAS  Google Scholar 

  • Chiang CH, Schoenwald RD (1986) Ocular Pharmacokinetic Models of Clonidine-3H Hydrochloride. J Pharmacokin Biopharm 14: 175–211.

    Article  CAS  Google Scholar 

  • DeSantis L, Sallee V, Barnes G, Schoenwald R, Barfknecht C, Duffel M and Lewis R (1986) The Effect of Topically Applied Analogs of the Carvonic Anhydrase Inhibitor, Ethoxzolamide, on Intraocular Pressure in Alert Laser-Induced Ocular Hypertensive Cynomolgus Monkeys. Suppl to Invest Ophthalmol Vis Sci 16: 179.

    Google Scholar 

  • Doane MG, Jensen AD and Dohlman CH (1978) Penetration Routes of Topically Applied Eye Medications. Am J Ophthalmol 85: 383–386.

    PubMed  CAS  Google Scholar 

  • Duzman E, Anderson J, Vita JB, Lue JC, Chen CC and Leopold IH (1983) Topically Applied Oxymetazoline. Ocular Vasoconstrictive Activity, Pharmacokinetics, and Metabolism. Arch Ophthalmol 101: 1122–1127.

    Google Scholar 

  • Ethoxzolamide Analogs. University of Iowa, Iowa City, IA.; pp. 163–176.

    Google Scholar 

  • Eller MG, Schoenwald RD, Dixson JA, Segarra T and Barfknecht T (1985a) Topical Carbonic Anhydrase Inhibitors III: Optimization Model for Corneal Penetration of Ethoxzolamide Analogues. J Pharm Sci 74: 155–160.

    Google Scholar 

  • Eller MG, Schoenwald RD, Dixson JA, Segarra T and Barfknecht CF (1985b) Topical Carbonic Anhydrase Inhibitors IV: Relationship Between Excised Corneal Permeability and Pharmacokinetic Factors. J Pharm Sci 74: 525–529.

    Google Scholar 

  • Fatt I (1978) Physiology of the Eye, Butterworth, Woburn Mass; pp. 114–121.

    Google Scholar 

  • Huang HS, Schoenwald RD and Lach LL (1983) Corneal Penetration Behavior of Beta-Blocking Agents II: Assessment of Barrier Contributions. J Pharm Sci 72: 1272–1278.

    Google Scholar 

  • Hansch C and Leo A (1983) Log P and Parameter Database. Comtex Scientific Corp., New York.

    Google Scholar 

  • Lee VHL and Robinson JR (1986) Review: Topical Ocular Drug Delivery: Recent Developments and Future Challenges. J Ocular Pharmacol 2: 67–108.

    Article  CAS  Google Scholar 

  • Lewis RA, Schoenwald RD, Barfknecht CF and Phelps CD (1986) Aminozolamide Gel A Trial of a Topical Carbonic Anhydrase Inhibitor in Ocular Hypertension. Arch Ophthalmol 104: 842–844.

    Article  PubMed  CAS  Google Scholar 

  • Mosher GL and Mikkelson TJ (1979) Permeability of the n-alkyl-p-aminobenzoate Esters Across the Isolated Corneal Membrane of the Rabbit. Int J Pharm 2: 239–243.

    Article  CAS  Google Scholar 

  • Notari RE (1976) Alteration of Pharmacokinetics Through Structural Modification. In: Roche EB (ed): Design of Biopharmaceutical Properties through Prodrugs and Analogs. Am Pharm Assoc Academy of Pharm Sci, Washington D.C.; 68–97.

    Google Scholar 

  • Patton TF (1980) Ocular Drug Disposition and Pharmacokinetics. Am Pharm Assoc Academy of Pharm Sci, Abstracts 15: 47.

    Google Scholar 

  • Putnam ML, Schoenwald RD, Duffel MW, Barfknecht CF, Segarra TM and Campbell DA (1986) Ocular Disposition of Aminozolamide in the Rabbit Eye. Invest Ophthalmol Vis Sci, in press.

    Google Scholar 

  • Schoenwald RD (1985) The Control of Drug Bioavailability from Ophthalmic Dosage Forms. In: Smolen VF and Ball LA (eds): Controlled Drug Bioavailability Volume 3: Bioavailability Control by Drug Delivery System Design. John Wiley d Sons, New York; pp. 257–306.

    Google Scholar 

  • Schoenwald RD and Huang HS (1983) Corneal Penetration Behavior of Beta-Blocking Agents I: Physicochemical Factors. J Pharm Sci 72: 1266–1272.

    Article  PubMed  CAS  Google Scholar 

  • Schoenwald RD and Ward RL (1981) Relationship Between Steroid Permeability Across Excised Rabbit Cornea and Octanol Water Partition Coefficients. J Pharm Sci 67: 786–788.

    Article  Google Scholar 

  • Sendelbeck L, Moore D, Urquhart J (1975) Comparative Distribution of Pilocarpine in Ocular Tissues of the Rabbit During Administration by Eye Drop or by Membrane Controlled Delivery System. Am J Ophthalmol 80: 274–283.

    PubMed  CAS  Google Scholar 

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© 1987 Springer Science+Business Media New York

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Schoenwald, R.D. (1987). The Importance of Optimizing Corneal Penetration. In: Saettone, M.F., Bucci, M., Speiser, P. (eds) Ophthalmic Drug Delivery. FIDIA Research Series, vol 11. Springer, New York, NY. https://doi.org/10.1007/978-1-4757-4175-9_15

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  • DOI: https://doi.org/10.1007/978-1-4757-4175-9_15

  • Publisher Name: Springer, New York, NY

  • Print ISBN: 978-1-4757-4177-3

  • Online ISBN: 978-1-4757-4175-9

  • eBook Packages: Springer Book Archive

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