5 包衣工艺研究 - 中药新药与临床药理.doc

Box-Behnken响应面法优化中药调脂片薄膜包衣处方 林伟鑫1，姚 曦，朱秀辉，李 勇，何 伟（广东药/广东省代谢实验室/广东省药物新剂型重点实验室，广州510006） doi：10.3969/j.issn.1003-9783.2016.02 The optimization of film coating formulation of Traditional Chinese Medicine (TCM) tiaozhi tablet by Box-Behnken design and response surface methodology LIN Weixin1， YAO Xi， ZHU Xiuhui， LI Yong， HE Wei(Guangdong Pharmaceutical University/Guangdong TCM Key Laboratory for Metabolic Diseases/Guangdong Key Laboratory of Advanced Drug Delivery，Guangzhou 510006，China) Abstract: Objective To optimize the film coating technology of Traditional Chinese Medicine (TCM) tiaozhi tablet by box-behnken design and response surface methodology. Methods The dosage of HPMC and PEG 400 and talc powder were selected as key factors of influencing coating qualified rate. The film coating qualified rate was taken as the response value through box-behnken design.Design Expert software was used to fit quadratic multinomial models for experimental data．Response surface and contour overlay plot were delineated to campare the interactions of the key factors with each other to draw and validated the optimum formulation. Results The optimization of film coating formulation consists of 6.6% HPMC and 0.9% PEG 400 and 3.3% talc powder and 89.2% water， the calculated coating qualified rate is 99.4%， and the measured value basically agrees well with calculated value， and the disintegration and release were qualified.Conclusion The model established by box-behnken design and response surface methodology is better to predict and could be used to optimize the formulations of film coating Traditional Chinese Medicine (TCM) tiaozhi tablet. Keywords: Box-Behnken design and response surface methodology; film coating technology; prescription 中药调脂片以临床经验方“复方贞术调脂方”为开发基础，由原方中三七、黄连药材提取物配伍组成，具有健脾化浊、祛瘀降脂的功效，用于治疗疏泄失常、瘀浊内阻等病因所致的高脂血症[1]。现代药理研究表明，三七总皂苷（TSPN）能明显降低大鼠动脉粥样硬化（AS）模型体内低密度脂蛋白[2]，同时增高脂肪酸合成酶（FAS）mRNA的表达[3]，提示TSPN对FAS的表达调节可能是其降脂的主要机制之一；黄连总生物碱对高脂血症及动脉粥样硬化也有显著降血脂和抑制动脉粥样硬化作用[4]。Box-Be