黄藤素的生物药剂学分类系统分类属性研究  

BCS classification attributes of palmatine

作　　者：温艳艳 马一丹 黄山 刘艳 方玲[4] 彭灿 WEN Yan-yan;MA Yi-dan;HUANG Shan;LIU Yan;FANG Ling;PENG Can(School of Pharmacy,Anhui University of Traditional Chinese Medicine,Hefei 230012;Anhui Key Laboratory of Chinese Medicinal Formula,Hefei 230012;Anhui Province Key Laboratory of Pharmaceutical Technology and Application,Hefei 230012;Department of Pharmacy,the First Affiliated Hospital of Anhui Medical University,Hefei 230022)

机构地区：[1]安徽中医药大学药学院,合肥230012 [2]中药复方安徽省重点实验室,合肥230012 [3]药物制剂技术与应用安徽省重点实验室,合肥230012 [4]安徽医科大学第一附属医院药剂科,合肥230022

出　　处：《中南药学》2022年第4期845-849,共5页Central South Pharmacy

基　　金：国家科技重大专项-重大新药创制(No.2017ZX09101001)。

摘　　要：目的通过溶解度和渗透性研究确定黄藤素的生物药剂学分类系统(BCS)分类属性。方法根据美国FDA 2015版工业指导原则,测定在37℃,pH 1~7.5内药物的溶解性;采用在体单向原位肠灌流模型测定黄藤素在大鼠不同肠段的渗透性;结合溶解性和渗透性结果确定黄藤素的BCS分类属性。结果考察黄藤素在不同pH值介质中的溶解度发现黄藤素属于低溶解性药物,通过渗透性实验发现黄藤素在大鼠不同肠段的渗透系数P_(eff(rat))均小于5.0×10^(-5) cm·s^(-1),转换成人体吸收百分率F_(a(human))均小于85%,故黄藤素属于低渗透性药物。结论结合溶解度和渗透性结果,判定黄藤素属于BCSⅣ类药物。Objective To determine the solubility and permeability of palmatine,and its the biopharmaceutical classification system(BCS)classification.Methods The solubility of palmatine drugs(at 37℃and pH 1~7.5)was determined according to the US FDA 2015 industrial guidelines.The permeability of palmatine in different intestinal segments of rats was measured by in situ single-pass intestinal perfusion model.The BCS classification properties were determined by combining the results of solubility and permeability.Results The solubility of palmatine in different pH media showed that palmatine belonged to low solubility drugs.The permeability experiment showed that the permeability coefficient P_(eff(rat)) in different intestinal segments was less than 5.0×10^(-5) cm·s^(-1) in rats,converting into human absorption percentage F_(a(human))was less than 85%.Conclusion Palmatine is BCSⅣdrug based on the result of its solubility and permeability.

关 键 词：黄藤素 生物药剂学分类系统 溶解度 渗透性 

分 类 号：R285[医药卫生—中药学]