环维黄杨星D包合物微孔渗透泵控释片的制备及处方优化  

Preparation and formulation optimization for microporous osmotic pump controlled release tablets of cyclovirobuxine D inclusion complex

作　　者：王玉华 杨海燕[2] 郝海军 WANG Yu-hua;YANG Hai-yan;HAO Hai-jun(Zhengzhou Health Vocational College,Zhengzhou 450199,China;The First Hospital Affiliated to Henan University of Chinese Medicine,Zhengzhou 450100,China;Shanghai Leiyunshang Pharmaceutical Co.,Ltd.,Shanghai 201401,China)

机构地区：[1]郑州卫生健康职业学院,河南郑州450199 [2]河南中医药大学第一附属医院,河南郑州450100 [3]上海雷允上药业有限公司,上海201401

出　　处：《中成药》2020年第10期2555-2560,共6页Chinese Traditional Patent Medicine

摘　　要：目的制备环维黄杨星D包合物微孔渗透泵控释片,并优化处方。方法将环维黄杨星D制成包合物以提高溶解度后,进一步制备微孔渗透泵控释片。在单因素试验基础上,以聚氧乙烯(PEO)用量、聚乙二醇400(PEG 400)用量、增塑剂(邻苯二甲酸二乙酯)用量、包衣增重为影响因素,累积释放度为评价指标,正交试验优化处方。结果最佳处方为PEO用量8 mg/片,PEG 400用量25%,增塑剂用量18%,包衣增重3%,12 h内累积释放度为90.82%。所得微孔渗透泵控释片的体外释药符合零级方程(R^2=0.9924),并且不受释放介质pH值的影响。结论微孔渗透泵控释片可使环维黄杨星D包合物缓慢恒速释药,从而抑制血药浓度波动,减少不良反应。AIM To prepare the microporous osmotic pump controlled release tablets of cyclovirobuxine D inclusion complex and to optimize the formulation.METHODS Cyclovirobuxine D was prepared into inclusion complex to enhance dissolution rate,after which the microporous osmotic pump controlled release tablets was further prepared.With polyethylene oxide(PEO)consumption,polyethylene glycol 400(PEG 400)consumption,plasticizer(diethyl phthalate)consumption and coating weight gain as influencing factors,accumulative release rate as an evaluation index,the formulation was optimized by orthogonal test on the basis of single factor test.RESULTS The optimal formulation was determined to be 8 mg/tablet for PEO consumption,25%for PEG 400 consumption,18%for plasticizer consumption,and 3%for coating weight gain,the accumulative release rate within 12 h was 90.82%.The in vitro drug release of obtained microporous osmotic pump controlled release tablets accorded with zero-order equation(R^2=0.9924),which was not affected by the pH value of release medium.CONCLUSION Microporous osmotic pump controlled release tablets can make the slow and constant-speed drug release of cyclovirobuxine D inclusion complex,thus inhibit the fluctuation of plasma concentration and reduce adverse reactions.

关 键 词：环维黄杨星D 包合物 微孔渗透泵控释片 制备 处方 正交试验 

分 类 号：R944[医药卫生—药剂学]