摘要
目的测定芎冰喷雾剂(A)和川芎喷雾剂(B,经鼻腔给药)、芎冰灌胃剂(C,与A的组成相同,灌胃)的主要成分川芎嗪在大鼠脑中的药代动力学参数。方法以气相色谱法测定鼻腔给药及灌服给药后一系列时间点采集血样作药动学分析。结果给药后川芎嗪在脑内的药时过程可以开放二室模型来描述;A药后脑组织药时曲线与静脉给药的药时曲线十分相似,吸收、分布、消除迅速,在给药后1min即在脑组织达到最大浓度,仅需要1.5h(约一个半衰期)即从脑内清除掉95.7%川芎嗪。结论芎冰喷雾剂经鼻给药适用于缺血性脑血管机能不全急性期的应急处理,并可在短时间多次重复给药;冰片使川芎嗪迅速进入脑组织,并使其在脑内的时间稍延长,提高了川芎嗪在脑内的生物利用度。
SAbstact:Objective To establish a method for detecting t he pharmacokinetic parameters of te tramethylpyragine(TMPz ),the main active component in Xiongbing nasal spray(A),Chuanxiong nasal spray(B)and Xiongbing decoction(C),in the rat brain .Methods Gas chromatography was applied for pharmacokinetic analysis of TMPz in v arious time after nasal administration or gastr ic infusion.Results The concentration -time process of A can be described in an open two -department model,which is simi lar to the process of intravenous adm inistration.As compared with B and C,A has its characteristics:quick absorpt ion,quick distribution and quick excretion of TMPz.TMPz passed through blood -brain barrier almost right after administration,and reach the peak concentra tion 1minute after the administrati on.95.7%of TMPz was cleared from brain within 1.5h.Conclusion The application of Borneolum makes T MPz of A enter into the rebral tissue easily.Therefore Xiongbing nasal spray is a quick -effective pre paration for acute ischemic stoke an d can be medicated repeatedly.
出处
《中药新药与临床药理》
CAS
CSCD
2003年第3期177-179,共3页
Traditional Chinese Drug Research and Clinical Pharmacology
基金
国家中医药管理局资助项目(编号00-01KL06)。
关键词
芎冰喷雾剂/药代动力学
川芎嗪/药代动力学
鼻腔给药
大鼠
气相色谱法
Xiongbing nasal spray /pharmacokinetics
Tetramethylpyragine /pharmacokin etics
Adninistration,in-tranasal
rats
Gas chromatography
