| Evaluation of soluble Bioadhesive Ophthalmic Drug Inserts (BODI) for prolonged release of gentamicin: lachrymal pharmacokinetics and ocular tolerance. | |
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MedLine Citation:
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PMID: 9671434 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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The purpose of this investigation was the evaluation of Bioadhesive Ophthalmic Drug Inserts (BODI) for prolonged release of gentamicin sulfate (GS) in tears. The BODIs (length 5.0 mm, diameter 2.0 mm, weight 20.5 mg, average GS content 5.0 mg) were prepared by extrusion of a mixture based on hydroxypropylcellulose (HPC), ethylcellulose (EC) and carbomer. Two methods were tested to prolong the release of GS in tears: (1) preliminary treatment of GS and (2) use of a less hydrophilic polymer than HPC, hydroxypropylmethylcellulose (HPMC), as a vehicle constituent. The preliminary treatment consisted of the formation of a GS/cellulose acetate phthalate (CAP) solid dispersion (ratio GS/CAP: 10/6) made in acetonic medium, and in the coating of GS/EC granules (GS/EC ratio: 10/0.5) with an aqueous dispersion of CAP, to form a GS/EC/CAP coprecipitate (GS/EC/CAP ratio: 10/0.5/6). Inserts containing GS/CAP solid dispersion, GS/EC/CAP coprecipitate and HPMC resulted in improved time of efficacy (t(eff)) (43.8, 23.3, and 33.1 h, respectively), when compared to inserts containing GS without preliminary treatment (t(eff) = 11.9 h). A high irritation level was observed for inserts containing the GS/EC/CAP and HPMC. A relation between t(eff) and irritation score was established, emphasizing the importance of irritability as a factor during the evaluation of the potential of these systems. |
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Authors:
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V Baeyens; V Kaltsatos; B Boisrame; M Fathi; R Gurny |
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Publication Detail:
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Type: Journal Article |
Journal Detail:
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Title: Journal of ocular pharmacology and therapeutics : the official journal of the Association for Ocular Pharmacology and Therapeutics Volume: 14 ISSN: 1080-7683 ISO Abbreviation: J Ocul Pharmacol Ther Publication Date: 1998 Jun |
Date Detail:
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Created Date: 1998-09-25 Completed Date: 1998-09-25 Revised Date: 2007-11-15 |
Medline Journal Info:
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Nlm Unique ID: 9511091 Medline TA: J Ocul Pharmacol Ther Country: UNITED STATES |
Other Details:
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Languages: eng Pagination: 263-72 Citation Subset: IM |
Affiliation:
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School of Pharmacy, University of Geneva, Switzerland. |
Export Citation:
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APA/MLA Format Download EndNote Download BibTex |
| MeSH Terms | |
Descriptor/Qualifier:
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Animals Anti-Bacterial Agents / administration & dosage, pharmacokinetics*, pharmacology Area Under Curve Biological Availability Drug Implants Evaluation Studies as Topic Eye / metabolism* Fluorescence Polarization Immunoassay Gentamicins / administration & dosage, pharmacokinetics*, pharmacology Half-Life Ophthalmic Solutions Rabbits Tears / metabolism Tissue Adhesives |
| Chemical | |
Reg. No./Substance:
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0/Anti-Bacterial Agents; 0/Drug Implants; 0/Gentamicins; 0/Ophthalmic Solutions; 0/Tissue Adhesives |
From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine
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