Tissue distribution and pharmacokinetics of brucine niosomal gels in rats after topical and oral application  

外用及口服马钱子碱囊泡凝胶在大鼠体内的组织分布和药物动力学研究（英文）

作　　者：Zhenzhen Wu Hengchun Ren Yanying Li Jiajia Fu Xiaojun Liu Jie Hu 吴珍珍;任恒春;李艳英;付佳佳;刘晓俊;胡杰(北京盈科瑞创新医药股份有限公司,北京102200)

机构地区：Beijing Increase innovative pharmaceutical Co., Ltd., Beijing 102200, China

出　　处：《Journal of Chinese Pharmaceutical Sciences》2018年第2期92-98,共7页中国药学（英文版）

基　　金：National Science and Technology Major Projects for"Major New Drugs Innovation and Development"(Grant No.2017ZX09301016)

摘　　要：Brucine has anti-inflammatory and analgesic effects and is the main active compound of the seeds of Strychnos nux-vomica L. To study brucine niosomal gels, a reliable and rapid LC-MS/MS method was established to quantify brucine levels in rats. Tissue distribution and pharmacokinetics of brucine were investigated after topical and oral application of brucine niosomal gels to rats. The plasma concentration versus time profiles suggested that systemic exposure of brucine for oral administration of brucine niosomal gels was higher than that for topical administration, and topical administration showed a relatively sustained release. There was a considerable amount of brucine distributed in the knee joint. These results provided a strong basis for the follow-up study of this preparation.马钱子碱是中药马钱子的主要活性物质,具有抗炎镇痛的作用。为了开发马钱子碱囊泡凝胶制剂,我们首次建立可靠快速的液相质谱联用检测方法,用于测定大鼠血浆及组织中马钱子碱的含量,并对口服及局部给药的药物动力学及组织分布进行研究。结果表明,口服给药后血浆中马钱子碱的含量明显高于局部给药,但局部给药显示出一定的缓释效果,并且发现在膝骨关节中有相当数量的马钱子碱。本研究结果为该制剂的后续开发提供了强有力的依据。

关 键 词：Brucine niosomal gels PHARMACOKINETICS Tissue distribution LC-MS/MS 

分 类 号：R969.1[医药卫生—药理学]