米格列奈钙缓释片制备工艺与体外释放度研究

Studies on the Preparation Technology and in vitro Release Rate of Mitiglinide Calcium Hydrate Sustained-release Tablets

目的:确定米格列奈钙缓释片最佳制备工艺并对其体外释放度进行考察。方法:采用单因素考察、正交试验设计,确定米格列奈钙缓释片最佳制备工艺,并照《中国药典》2010年版(二部)释放度测定法测定其体外释放度。结果:米格列奈钙缓释片处方:米格列奈钙5.0g,羟丙基甲基纤维素(HPMC,K15M)30.0g,乳糖80.0g,3%聚维酮(PVP)水溶液适量,硬脂酸镁2.0g;最佳制备工艺:将上述原辅料过120目筛,充分干燥,按处方量称量、混匀,用3%PVP水溶液作为黏合剂制成软材,40目筛制粒,50℃干燥;40目筛整粒,加润滑剂混匀,测含量;用φ7.0mm圆形浅弧冲压片(8kg/cm2),每片重120mg;米格列奈钙缓释片体外释放度符合良好的Higuchi方程(r=0.9983)。结论:本研究制备的米格列奈钙缓释片具有良好的缓释效果。

Objective：To determine the optimum preparation technology of mitiglinide calcium hydrate sustained-re- lease tablets and investigate the release rate in vitro. Methods ：Using the single factor investigation and orthogonal test de- sign to determine the optimum preparation technology of mitiglinide calcium hydrate sustained-release tablets, and deter- mine the release rate in vitro according to the Chinese Pharmacopoeia of 2010 edition. （volume 1I ）. Results ： The formulation of mitiglinide calcium hydrate sustained-release tablets included mitiglinide calcium （5.0 g）, HPMC （ K 15M, 30.0 g）, lactose （80.0 g）, 3% PVP water solution （appropriate amount） and magnesium stearate （2.0 g）. The optimum preparation technology was as follows： puting the above-mentioned raw materials through 120 mesh sieve, fully drying, weighing ac- cording to the formulation and mixing, making a soft material as a binder using 3% PVP water solution, granulating with 40 mesh sieve and drying at 50 ℃ ,processing granule with 40 mesh sieve, adding lubricant and blending, and determining the content, stamping with shallow circular arc （q~ 7 ram）at a pressure 8 kg/cm2 to make each piece at a weight of 120 mg. The release profile in vitro ofmitiglinide calcium hydrate sustained-release tablets conformed to Hignchi equation （r = 0.998 3 ）. Conclusion：The release rate of mitiglinide calcium hydrate sustained-release tablets prepared in this study has a good sus- tained release effect.