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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 ;乳剂中药物的释放过程为被动扩散机制
OBJECTIVE: To investigate the phase distribution and drug release in vitro of drugs with different partition coefficients. Methods: Different octanol / water partition coefficients were determined for Harmine and Harmine HC1, respectively, and were separately formulated as O / W for injection. The method of ultracentrifugation and microfiltration was used to separate the aqueous and oil phases, and the distributions of the drug in the aqueous, oil and mesophase phases of the emulsion were determined. In vitro dialysis was used to determine the in vitro drug release of the two emulsions. Results: The phase distribution was related to partition coefficients. The emulsions made with Har were mainly distributed in the oil phase and the mesophase with less aqueous phase. The emulsions made with Har.HCl were mainly distributed in the aqueous phase. Conclusion: There is a corresponding difference between the maximum release rate and the drug release rate. Phase distribution and distribution coefficient; emulsion drug release process for the passive diffusion mechanism