去氢骆驼蓬碱注射用乳剂中药物的相分布和体外释放研究  

Study on Phase Distribution and Release in Vitro of Harmine Emulsion for Intravenous Injection

作　　者：高晓黎[1] 孙殿甲[1] 程利勇 毕殿州[2] 

机构地区：[1]新疆医科大学,新疆乌鲁木齐830054 [2]沈阳药科大学,辽宁沈阳110015

出　　处：《中成药》2000年第2期111-115,共5页Chinese Traditional Patent Medicine

基　　金：国家科委医药技术创新博士项目! (编号 :96 90 1 0 6 0 2 1 )

摘　　要：目的 :探讨具有不同分配系数的药物在乳剂中的相分布和体外释药性能。方法 :经测定去氢骆驼蓬碱 (Har.)和去氢骆驼蓬碱盐酸盐 (Har .HCl)具有不同的辛醇 /水分配系数 ,分别制成O/W型注射用乳剂后 ,采用超速离心和微孔滤膜过滤的方法分离水相和油相 ,分别测定药物在乳剂的水相、油相和中间相的分布。采用反向透析技术分别测定两种乳剂的体外释药性能。结果 :相分布与分配系数有关 ,用Har.制成的乳剂药物主要分布在油相和中间相 ,水相较少 ;而用Har.HCl制成乳剂药物则主要分布在水相。结论 :两者的最大释药量和释药速度均存在相应的差异。相分布与分配系数有关 ;Objective: To study the distribution phose and in vitro release of the emulsions for intravenous injection containing havmine (Ⅰ) and harmine hydrochloride (Ⅱ) that have different partition coefficients. Method: After harmine (Ⅰ) and harmine hydrochloride (Ⅱ) were prepared into O/W type of emulsion for injection according to their different distribution coefficients, respectively, the aqueous and oil phases of emulsions were separated by the methods of ultracentrifugation and millipore filter membrane, then the distributions of drugs in aqueous and oil phase and O/W interface of emulsions were determined. Results: The phase distribution related to distribution coefficients. The drug in emulsion prepared by Har mainly distributed in oil phase and O/W interface, but when prepared by Har. HCl. the drug mainly distributed in aqueous phase. Conclusions: There were differences between two kinds of emulsions in maxium release amount and rate. The distribution phase and in vitro release of drug in an emulsion are interrelated with the partition coefficients of drug.

关 键 词：去氢骆驼蓬碱 乳剂 相分布 体外释放 

分 类 号：R979.1[医药卫生—药品]