穿琥宁体外稳定性研究  

Study on the Stability of Potassium Dehydroandrographolide Succinate in Vitro

作　　者：王鹏[1,2] 江云鸥[1,2] 张志勇[2] 

机构地区：[1]四川大学华西药学院,成都市610041 [2]四川大学华西医院药剂科,成都市610041

出　　处：《中国药房》2010年第39期3664-3666,共3页China Pharmacy

摘　　要：目的:研究穿琥宁的体外酸碱及酶稳定性。方法:将穿琥宁溶解于不同pH值(2.0～9.0)的磷酸缓冲液、人工肠液和不同浓度的肝组织匀浆液中,37℃恒温水浴,于不同时间取样,高效液相色谱法测定穿琥宁的浓度,考察其降解情况或降解动力学。结果:穿琥宁在酸性(pH2.0～5.0)条件下迅速降解(温孵1h后残余量低于10%);在pH7.0磷酸溶液、人工肠液中相对稳定,2h内各取样点的穿琥宁含量均高于95%;37℃下,在50%肝匀浆液中温孵24h后,降解23%;在25%肝匀浆液中温孵24h后,降解15%,且随肝匀浆液浓度的增大而降解加快。结论:穿琥宁在pH<5.0的环境下极不稳定;而胰酶对其几无影响;在肝匀浆液(pH7.0)中不稳定,肝微粒体酶对其有一定影响。OBJECTIVE：To investigate the stability of Potassium Dehydroandrographolide Succinate（PDS） in vitro in different pH and enzymatic solutions.METHODS：PDS was dissolved in different phosphate buffer solutions with pH of 2.0～9.0,stimulated intestinal fluid and liver homogenate of SD rats,thermostatically maintained at 37 ℃.The concentrations of PDS were determined by HPLC to investigate the degradation kinetics and stability of PDS.RESULTS：PDS was degraded in acid solution（pH 2.0～5.0） immediately（more than 90% PDS was degraded after 1 h of incubation）,stable in phosphoric solution（pH 7.0） and stimulated intestinal fluid.The contents of PDS at different sampling points were more than 95% in 2 h.After 24 h of incubation at 37 ℃,23% PDS was degraded in 50% liver homogenate and 15% in 25% liver homogenate.The degradation speed up as the concentration of liver homogenate increased.CONCLUSION：PDS is instable in solution with pH〈5.0 and liver homogenate（pH 7.0）.The hepatomicrosome enzyme possesses effect on the stability of PDS while pancreatic enzymes is not.

关 键 词：穿琥宁 肝匀浆 酸碱稳定性 酶稳定性 

分 类 号：R285[医药卫生—中药学] R97[医药卫生—中医学]