Study of ocular pharmacokinetics of in situ gel system for S(-)-satropane evaluated by microdialysis.

Abstract

S(-)-Satropane is currently being developed to in situ forming ophthalmic gel, a new ophthalmic delivery system, for the treatment of glaucoma. To evaluate the pharmacokinetic profiles of S(-)-satropane, the microdialysis method was employed. The concentration of S(-)-satropane in dialysates was measured by using liquid chromatography/tandem mass spectrometry (LC-MS/MS). Unlike the common solution prepared in normal saline, in which the level of S(-)-satropane in aqueous humor increased rapidly after instillation and reached the maximal level (C(max) of 1.508+/-0.297 microg ml(-1)) within 1h, S(-)-satropane exhibited 3.2-fold greater C(max) and 2.2-fold greater AUC(0-3h) (p<0.05) in the in situ forming gel. The results showed that the in situ forming gel system could improve the ocular bioavailability of S(-)-satropane.

• Authors: Jun Fu, Xuemei Feng, Haihong Yuan, Liming Yan, Xiaodong Kuang, Zheng Xia, Xiaoling Gao, Cheng Yu, Yang Lu, Hong-Zhuan Chen
• Journal: Journal of pharmaceutical and biomedical analysis (J Pharm Biomed Anal) Vol. 48 Issue 3 Pg. 840-3 (Nov 04 2008) ISSN: 0731-7085 [Print] England
• PMID: 18632240 (Publication Type: Journal Article, Research Support, Non-U.S. Gov't)

Chemical References

• Gels
• Ophthalmic Solutions
• Tropanes
• satropane

Topics

• Aqueous Humor (metabolism)
• Area Under Curve
• Biological Availability
• Chromatography, Liquid (methods)
• Drug Delivery Systems
• Gels (pharmacokinetics)
• Microdialysis (methods)
• Molecular Structure
• Ophthalmic Solutions (administration & dosage, chemistry, pharmacokinetics)
• Stereoisomerism
• Tandem Mass Spectrometry (methods)
• Tropanes