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

• Published in: Journal of pharmaceutical and biomedical analysis Vol. 48; no. 3; pp. 840 - 843
• Main Authors: Fu, Jun, Feng, Xuemei, Yuan, Haihong, Yan, Liming, Kuang, Xiaodong, Xia, Zheng, Gao, Xiaoling, Yu, Cheng, Lu, Yang, Chen, Hong-Zhuan
• Format: Journal Article
• Language: English
• Published: Amsterdam Elsevier B.V 04.11.2008; Elsevier
• Subjects: Analysis; Analytical, structural and metabolic biochemistry; Aqueous Humor - metabolism; Area Under Curve; Biological and medical sciences; Biological Availability; Chromatography, Liquid - methods; Drug Delivery Systems; Fundamental and applied biological sciences. Psychology; Gels - pharmacokinetics; General pharmacology; Glaucoma; In situ forming gel; Medical sciences; Microdialysis; Microdialysis - methods; Molecular Structure; Ophthalmic Solutions - administration & dosage; Ophthalmic Solutions - chemistry; Ophthalmic Solutions - pharmacokinetics; Pharmacokinetic; Pharmacology. Drug treatments; S(−)-satropane; Stereoisomerism; Tandem Mass Spectrometry - methods; Tropanes; S(−)-satropane; Glaucoma; Microdialysis; In situ forming gel; Pharmacokinetic; Colloidal gel; Eye disease; Glaucoma (eye); In situ; Dosage form; Pharmacokinetics; S(-)-satropane
• ISSN: 0731-7085; 1873-264X
• DOI: 10.1016/j.jpba.2008.06.001

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 μg ml −1) within 1 h, 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.