文献类型：期刊文献

中文题名：灵芝酸单体T片剂的制备及其兔体内药动学研究

英文题名：Preparation of Ganoderic Acid T Tablets and Pharmacokinetics in Rabbits

作者：陈香[1];姚芳[1];陈水娟[1];方源[1];高峰[1,2,3];钟建江[4]

机构：[1]华东理工大学药学院药剂教研组,上海200237;[2]上海市功能性材料化学重点实验室,华东理工大学,上海200237;[3]上海市新药设计重点实验室,华东理工大学,上海200237;[4]上海交通大学生命科学技术学院,上海200240

年份：2013

卷号：48

期号：12

起止页码：976

中文期刊名：中国药学杂志

外文期刊名：Chinese Pharmaceutical Journal

收录：CSTPCD;;Scopus;北大核心:【北大核心2011】；CSCD:【CSCD2013_2014】；PubMed;

基金：上海市科学技术委员会项目资助(11DZ2260600和10DZ2220500);上海市中药现代化专项项目(08DZ1971900);华东理工大学交叉学科与重大项目培育基金(WY1213013ECUST)

语种：中文

中文关键词：灵芝酸单体T;粉末直接压片;药动学;高效液相色谱法

外文关键词：ganoderic acid T; direct powder compression; pharmacokinetics; HPLC

摘要：目的研制灵芝酸单体T(GA-T)片剂,并评价其在兔体内的药动学特性。方法 采用单因素法考察药用辅料的种类与用量,优化处方和制备工艺,经粉末直接压片制得GA-T片剂。高效液相色谱法测定GA-T在兔体内的血药浓度,采用药动学软件kinetica 5.0计算药动学参数,研究GA-T片剂在兔体内药动学特性。结果 GA-T片剂优化处方中,选用微晶纤维素与喷雾干燥乳糖1∶1为填充剂,1%微粉硅胶和0.5%硬脂酸镁分别作为助流剂与润滑剂。制得片剂的外观、硬度、崩解时间和溶出度等各项评价指标均符合《中国药典》2010年版的要求。兔口服GA-T片剂的绝对生物利用度为33.03%。结论粉末直接压片法工艺简单可靠,GA-T片剂兔体内生物利用度良好。本实验为GA-T的临床前研究提供了实验数据。
OBJECTIVE To prepare the ganoderic acid T （GA-T） tablets and evaluate the pharmacokinetics and bioavailability in rabbits. METHODS GA-T tablets were prepared by direct powder compression. After investigating the type and amount of exeipients by single-factor method, the formulation of GA-T tablets was optimized and prepared by direct powder compression. An HPLC method was used for the determination of plasma concentration in rabbits after administration of GA-T. The main pharmacokinetic parameters were analyzed by pharmacokinetic software kinetica 5.0. The pharalacokinetic characteristics of GA-T tablets were studied. RESULTS In optimization of formulation, microcrystalline cellulose and spray-dried lactose （ 1 ： 1 ） were selected as bulking agent. In addition, 1% of the silica powder and 0. 5% magnesium stearate were used as glidant and lubricant, respectively. The prepared tablets were consistent with the requirements of the 2010 edition of Chinese Pharmacopoeia standards, including appearance, hardness, disaggregation and dissolution of the tablets. The absolute bioavailability of oral GA-T tablets was 33.03%. CONCLUSION The direct powder compression is simple and reliable, and the bioavailability of oral GA-T tablets in rabbits is well. This article provided experimental data for preclinical study of GA-T.