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机构地区:[1]哈尔滨商业大学药物研究所,哈尔滨150076 [2]沈阳药科大学药剂教研室,沈阳110016
出 处:《中国新药杂志》2005年第9期1147-1150,共4页Chinese Journal of New Drugs
摘 要:目的:研究齐酞酸钠(OAHDPS)在大鼠肠道内的吸收特性。方法:采用大鼠在体小肠吸收实验方法,测定OAHDPS在不同剂量(100,50,25μg·mL-1)下结扎和不结扎胆管条件下的小肠吸收量和吸收速率常数(Ke),并比较各个肠段的吸收。结果:研究表明,OAHDPS在肠道内的吸收机制是被动扩散方式,且在小肠的吸收不受胆汁等分泌物的影响;在肠道正常pH值情况下,平均Ke为(0·162±0·012)h-1;各个肠段对OAHDPS均有吸收且Ke无显著差异。结论:在OAHDPS口服剂型设计时应首先考虑肠溶缓释制剂。Objective: To characterize the intestinal absorption of oleanolic acid hemidiphthalate sodium (OAHDPS) in rats .Methods: A rat intestine loop in situ technique was used to investigate the uptake rate Ke of OAHDPS in a series of concentration (25,50 and 100μg·mL^-1) at the intestine with or without ligation of bile ducts, respectively. The absorption coefficients at various intestinal segments were compared. Results:The kinetic analyses showed that the intestinal absorption of OADHPS obeyed with passive transport mechanism and first order kinetics with an absorption rate of (0.162±0.012) h^-1 under the normal pH environment. OADHPS could be absorbed at various segments of intestinal wall without significant differences of absorption coefficients. Conclusion: An enteric-coated sustained-release formulation might benefit the bioavailability of OAHDPS.
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