绵马贯众有效部位微丸的处方工艺优化及溶出特性研究  

Optimization of the formulation process and dissolution characteristics of pellets from effective parts of Dryopteris crassirhizoma Nakai

作　　者：杨锦 高增平[1] 尹兴斌[1] 曲昌海[1] 倪健[1] YANG Jin;GAO Zeng-ping;YIN Xing-bin;QU Chang-hai;NI Jian(School of Chinese Materia Medica,Beijing University of Traditional Chinese Medicine,Beijing 102488)

机构地区：[1]北京中医药大学中药学院,北京102488

出　　处：《中南药学》2021年第6期1080-1085,共6页Central South Pharmacy

基　　金：医药创新品种研发培育及产业支撑平台能力建设(No.Z19110200760000)。

摘　　要：目的制备绵马贯众有效部位微丸,并对其进行处方优化。方法采用单因素法考察挤出速度、滚圆速度、滚圆时间等制备工艺因素,黏合剂浓度、崩解剂种类及用量、填充剂中MCC的比例、羟丙基-β-环糊精与药物比例等处方因素对微丸成型和溶出的影响;并在此基础上,采用Box-Behnken效应面法,以5 min和30 min时的累积溶出度为评价指标,对微丸处方进行优化;建立UPLC法测定溶出介质中药物含量,并对微丸溶出度及溶出曲线进行考察。结果制备工艺参数为挤出速度60 r·min^(-1),滚圆速度1500 r·min^(-1),滚圆时间5 min;溶出介质选择含5%吐温80和5 mg·mL^(-1) D-异抗坏血酸钠的PBS溶液(pH 6.8),所选定的较优处方在5 min和30 min时的累积溶出度符合要求。结论采用单因素结合Box-Behnken效应面法成功优化得到具有较快释药特征的绵马贯众有效部位微丸。Objective To prepare the pellets from the effective parts of Dryopteris crassirhizoma Nakai and to optimize the formulation.Methods Single factor method was used to determine the effect of technical parameters of extrusion speed,rounding speed and rounding time on the pellets formation and dissolution,as well as the concentration of adhesive,the type and concentration of disintegrating agent,the proportion of MCC in the filler and the proportion of hydroxypropyl-β-cyclodextrin to drug.Then Box-Behnken effect surface method was used to optimize the formulation of pellets,with the cumulative dissolution rate at 5 min and 30 min as the evaluation indexes.UPLC method was established to determine the drug content in the dissolution medium.The dissolution degree and dissolution curve of the pellets were measured.Results The process parameters of the effective parts were as follows:extrusion speed 60 r·min^(-1),rounding speed 1500 r·min^(-1),and rounding time 5 min.PBS solution contained 5%Tween 80 and 5 mg·mL^(-1) D-isoascorbate was selected as the dissolution medium(pH 6.8).The optimal prescription range was obtained by BBDeffect surface optimization.The cumulative dissolution at 5 min and 30 min met the requirements.Conclusion Single factor combined with Box-Behnken effect surface method helps optimize the pellets with rapid drug release.

关 键 词：绵马贯众 微丸 挤出滚圆法 BOX-BEHNKEN效应面法 溶出 

分 类 号：R284[医药卫生—中药学]