Study of ocular pharmacokinetics of in situ gel system for S(-)-satropane evaluated by microdialysis.
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.
Fu
Jun
J
Department of Pharmacology, College of Basic Medical Sciences, Shanghai JiaoTong University School of Medicine, South Chongqing Road 280, Shanghai 200025, PR China.
Feng
Xuemei
X
Yuan
Haihong
H
Yan
Liming
L
Kuang
Xiaodong
X
Xia
Zheng
Z
Gao
Xiaoling
X
Yu
Cheng
C
Lu
Yang
Y
Chen
Hong-Zhuan
HZ
D001082:Aqueous Humor / Q000378:metabolism; D019540:Area Under Curve; D001682:Biological Availability; D002853:Chromatography, Liquid / Q000379:methods; D016503:Drug Delivery Systems; D005782:Gels / Q000493:pharmacokinetics*; D017551:Microdialysis / Q000379:methods*; D015394:Molecular Structure; D009883:Ophthalmic Solutions / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D013237:Stereoisomerism; D053719:Tandem Mass Spectrometry / Q000379:methods; D014326:Tropanes
D005782:Gels; D009883:Ophthalmic Solutions; D014326:Tropanes; C535253:satropane