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Corneal Absorption of Fluorometholone in Rabbits: A Comparative Evaluation of Corneal Drug Transport Characteristics in Anesthetized and Unanesthetized Rabbits

Corneal Absorption of Fluorometholone in Rabbits: A Comparative Evaluation of Corneal Drug... Abstract A single drop of tritium-labeled 0.1% fluorometholone suspension was administered topically to intact eyes of anesthetized and unanesthetized rabbits. Aqueous humor levels of steroid were monitored as a function of time. The aqueous humor drug concentration-time profile for anesthetized rabbits is considerably different from that for unanesthetized animals. Anesthetized animals show a shift in the time to achieve a maximum aqueous humor steroid concentration, which is ascribed to a change in rate-limiting step from corneal absorption control to dissolution control. In addition, aqueous humor drug levels in the anesthetized rabbits were dependent on position of the animals and level of anesthesia. References 1. Hamashige S, Potts AM: The penetration of cortisone and hydrocortisone into ocular structures . Am J Ophthalmol 40:211-215, 1955. 2. Janes RG, Stiles JF: The penetration of cortisol into normal and pathologic rabbit eyes . Am J Ophthalmol 56:84-90, 1963. 3. Short C, et al: Ocular penetration studies: I. Topical administration of dexamethasone . Arch Ophthalmol 75:689-692, 1966.Crossref 4. Murdick PW, et al: Ocular penetration studies: II. Topical administration of prednisolone . Arch Ophthalmol 76:602-603, 1966.Crossref 5. Cox WV, Kupferman A, Leibowitz HM: Topically applied steroids in corneal disease: I. The role of inflammation in stromal absorption of dexamethasone . Arch Ophthalmol 88:308-313, 1972.Crossref 6. Cox WV, Kupferman A, Leibowitz HM: Topically applied steroids in corneal disease: II. The role of drug vehicle in stromal absorption of dexamethasone . Arch Ophthalmol 88:549-552, 1972.Crossref 7. Chrai SS, et al: Lacrimal and instilled fluid dynamics in rabbit eyes . J Pharm Sci 62:1112, 1973.Crossref 8. Higuchi WI, Rowe EL, Hiestand EN: Dissolution rates of finely divided drug powders: II. Micronized methylprednisolone . J Pharm Sci 52:162-164, 1963.Crossref 9. Hussain A: Prediction of dissolution rates of slightly water-soluble powders from simple mathematical relationships . J Pharm Sci 61:811-813, 1972.Crossref http://www.deepdyve.com/assets/images/DeepDyve-Logo-lg.png Archives of Ophthalmology American Medical Association

Corneal Absorption of Fluorometholone in Rabbits: A Comparative Evaluation of Corneal Drug Transport Characteristics in Anesthetized and Unanesthetized Rabbits

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Publisher
American Medical Association
Copyright
Copyright © 1974 American Medical Association. All Rights Reserved.
ISSN
0003-9950
eISSN
1538-3687
DOI
10.1001/archopht.1974.01010010248016
Publisher site
See Article on Publisher Site

Abstract

Abstract A single drop of tritium-labeled 0.1% fluorometholone suspension was administered topically to intact eyes of anesthetized and unanesthetized rabbits. Aqueous humor levels of steroid were monitored as a function of time. The aqueous humor drug concentration-time profile for anesthetized rabbits is considerably different from that for unanesthetized animals. Anesthetized animals show a shift in the time to achieve a maximum aqueous humor steroid concentration, which is ascribed to a change in rate-limiting step from corneal absorption control to dissolution control. In addition, aqueous humor drug levels in the anesthetized rabbits were dependent on position of the animals and level of anesthesia. References 1. Hamashige S, Potts AM: The penetration of cortisone and hydrocortisone into ocular structures . Am J Ophthalmol 40:211-215, 1955. 2. Janes RG, Stiles JF: The penetration of cortisol into normal and pathologic rabbit eyes . Am J Ophthalmol 56:84-90, 1963. 3. Short C, et al: Ocular penetration studies: I. Topical administration of dexamethasone . Arch Ophthalmol 75:689-692, 1966.Crossref 4. Murdick PW, et al: Ocular penetration studies: II. Topical administration of prednisolone . Arch Ophthalmol 76:602-603, 1966.Crossref 5. Cox WV, Kupferman A, Leibowitz HM: Topically applied steroids in corneal disease: I. The role of inflammation in stromal absorption of dexamethasone . Arch Ophthalmol 88:308-313, 1972.Crossref 6. Cox WV, Kupferman A, Leibowitz HM: Topically applied steroids in corneal disease: II. The role of drug vehicle in stromal absorption of dexamethasone . Arch Ophthalmol 88:549-552, 1972.Crossref 7. Chrai SS, et al: Lacrimal and instilled fluid dynamics in rabbit eyes . J Pharm Sci 62:1112, 1973.Crossref 8. Higuchi WI, Rowe EL, Hiestand EN: Dissolution rates of finely divided drug powders: II. Micronized methylprednisolone . J Pharm Sci 52:162-164, 1963.Crossref 9. Hussain A: Prediction of dissolution rates of slightly water-soluble powders from simple mathematical relationships . J Pharm Sci 61:811-813, 1972.Crossref

Journal

Archives of OphthalmologyAmerican Medical Association

Published: Sep 1, 1974

References

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