Desai S D, Blanchard J
Department of Pharmaceutical Sciences, College of Pharmacy, University of Arizona, Tucson 85721, USA.
J Pharm Sci. 1998 Feb;87(2):226-30. doi: 10.1021/js970090e.
The overall objective of this study was to develop pluronic F127 (PF127)-containing formulations of pilocarpine hydrochloride (PHCL) suitable for controlled-release ocular delivery of PHCL. Various aqueous formulations were evaluated containing 1% w/v PHCL and 25% w/v PF127 alone or with one of the following additives present: poly(ethylene glycol) 4600 (PEG), poly(vinylpyrrolidone) 10,000 (PVP), poly(vinyl alcohol) 10,000 (PVA), methylcellulose 15 cP (MC), and hydroxypropyl methylcellulose 80-120 cP (HPMC). The in vitro dissolution of the PF127 formulations and the pilocarpine release profiles from them were obtained simultaneously at 34 degrees C and room temperature using a membraneless in vitro model. It was observed that the PEG- and PVP-containing PF127 formulations of PHCL dissolved the quickest and released the drug at a significantly faster rate than the control PF127 formulation, which had no additive present. The PF127 formulations of PHCL containing MC or HPMC exhibited the slowest dissolution rates and released the drug the slowest. The same rank order was observed at each temperature for the dissolution and PHCL release profiles of each formulation. On the basis of the in vitro results, the PF127 formulations of PHCL containing MC or HPMC as an additive showed potential for use as controlled-release ocular delivery systems for PHCL.
本研究的总体目标是开发含泊洛沙姆F127（PF127）的盐酸毛果芸香碱（PHCL）制剂，适用于PHCL的控释眼部给药。评估了各种水性制剂，其单独含有1%w/v的PHCL和25%w/v的PF127，或含有以下添加剂之一：聚乙二醇4600（PEG）、聚乙烯吡咯烷酮10000（PVP）、聚乙烯醇10000（PVA）、15厘泊的甲基纤维素（MC）和80 - 120厘泊的羟丙基甲基纤维素（HPMC）。使用无膜体外模型，在34℃和室温下同时获得PF127制剂的体外溶出度及其毛果芸香碱释放曲线。观察到含PEG和PVP的PHCL的PF127制剂溶解最快，且药物释放速率明显快于不含添加剂的对照PF127制剂。含MC或HPMC的PHCL的PF127制剂表现出最慢的溶解速率和最慢的药物释放。在每个温度下，每种制剂的溶出度和PHCL释放曲线均观察到相同的排序。基于体外结果，含MC或HPMC作为添加剂的PHCL的PF127制剂显示出作为PHCL控释眼部给药系统的应用潜力。
