Pepić I, Jalsenjak N, Jalsenjak I
Department of Pharmaceutics, Faculty of Pharmacy and Biochemistry, University of Zagreb, A. Kovac?ića 1, Zagreb 10000, Croatia.
Int J Pharm. 2004 Mar 19;272(1-2):57-64. doi: 10.1016/j.ijpharm.2003.11.032.
Solutions of surface active triblock copolymer Pluronic F127 in the vicinity of the critical micellar concentration (cmc) were prepared with or without pilocarpine (either as the hydrochloride salt or the free base) in water and phosphate buffer. The characteristics parameters of the surface activity (cmc, Gamma and a) were determined for F127 solutions. Additionally, it was found that the pilocarpine solutions without F127 in water exhibits a certain surface activity. The solutions containing F127 (2 wt.%) well above the cmc and pilocarpine (2 wt.% for the salt, or equimolar 1.7 wt.% for the base) were further tested in vivo (miotic response) on rabbit eye. Though the entrapment efficiency of the drug in the micelles was rather low (maximal 1.9%) the pharmacokinetic parameters (duration of miotic response and the area under miotic curve) were improved when compared to the standard pilocarpine solutions. The best results were obtained for the micellar pilocarpine base solution which exhibits significant prolongation of miotic activity and an increase of AUC for 64%.
在水和磷酸盐缓冲液中，制备了临界胶束浓度（cmc）附近含有或不含有毛果芸香碱（盐酸盐或游离碱）的表面活性三嵌段共聚物普朗尼克F127溶液。测定了F127溶液的表面活性特征参数（cmc、γ和a）。此外，还发现水中不含F127的毛果芸香碱溶液具有一定的表面活性。将cmc以上的含F127（2 wt.%）和毛果芸香碱（盐为2 wt.%，碱为等摩尔1.7 wt.%）的溶液进一步在兔眼上进行体内测试（缩瞳反应）。尽管药物在胶束中的包封效率相当低（最大1.9%），但与标准毛果芸香碱溶液相比，药代动力学参数（缩瞳反应持续时间和缩瞳曲线下面积）有所改善。胶束毛果芸香碱碱溶液获得了最佳结果，其缩瞳活性显著延长，AUC增加了64%。
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