帕博西尼胶囊的制备及体外溶出评价

Preparation and in-vitro dissolution evaluation of palbociclib capsules

目的筛选帕博西尼胶囊处方。方法以帕博西尼胶囊的体外溶出曲线为考察指标,调节帕博西尼胶囊的填充剂比例、崩解剂用量及厂家、原料药粒度,确定帕博西尼胶囊最优处方。结果最终确定帕博西尼胶囊内容物:微晶纤维素PH102/无水直压乳糖为1∶4,台湾永日化学的羧甲淀粉钠为6.00%,原料药粒度D_(90)为12.00～18.00μm。单剂量处方:帕博西尼125.00 mg,无水直压乳糖231.20 mg,微晶纤维素PH102 57.80 mg,羧甲淀粉钠27.00 mg,二氧化硅4.50 mg,硬脂酸镁4.50 mg。自制制剂和参比制剂在四种溶出介质中的溶出曲线均一致。结论筛选的帕博西尼胶囊处方可行。

Objective To formulate Palbociclib capsules.Methods The optimal prescription of the palbociclib capsules were fixed according to the in vitro dissolution curves of palbociclib capsules as evaluation index,through adjusting the proportion of the filler,the amount and manufacturer of the disintegrant,the particle size of Palbociclib.Results Finally,the fixed contents of Palbociclib capsules were as follows:the ratio of microcrystalline cellulose PH102 to anhydrous direct pressure lactose was 1∶4,the percent of Taiwan Yongri Chemical sodium carboxymethyl was 6.00%,the particle size D 90 of Palbociclib was 12.00-18.00μm.Single-dose prescription contain Palbociclib 125.00 mg,anhydrous direct pressure lactose 231.20 mg,microcrystalline cellulose PH102 57.80 mg,sodium carboxymethyl starch 27.00 mg,silica 4.50 mg,magnesium stearate 4.50 mg.The dissolution curve of homemade formulation and reference formulation were similar in all four dissolution media.Conclusion The screening prescription of Palbociclib capsules were feasible.