摘要
参考原研的帕博昔布胶囊(Ibrance)说明书中所述辅料,通过正交试验筛选确定了仿制胶囊的最佳处方,即每100粒含:帕博昔布7.5 g,微晶纤维素11 g,一水乳糖5.6 g,羧甲淀粉钠1.59 g,胶态二氧化硅0.265 g,硬脂酸镁0.545 g。以3%羧甲淀粉钠溶液为黏合剂湿法制粒后,60℃干燥整粒,填充胶囊。同时建立了一种新的高效液相色谱法分离和测定帕博昔布中的5种有关物质。采用InertSustain C_(18)柱,以pH 5.7乙酸铵缓冲液∶乙腈为流动相,梯度洗脱,在225 nm下检测。经方法学验证表明,本法专属性强、灵敏度高、耐用性好,可用于帕博昔布产品有关物质的检测和质量控制。
Palbociclib is an inhibitor of CDK4/6 which studied by Pfizer. It is used in the treatment of female patients with ER positive breast cancer clinically. Because of its outstanding effect in clinical trials, the FDA approved its listing only in United States. There are no relevant reports of its preparation yet. Based on the excipients of palbociclib capsules （Ibrance） from Pfizer, the formulation of generic palbociclib capsules was screened by orthogonal test, finally the optimal formulation was as follows： palbociclib 7.5 g, microcrystalline cellulose 11 g, lactose monohydrate 5.6 g,sodium carboxymethyl starch 1.59 g, colloidal silica 0.265 g, magnesium stearate 0.545 g for 100 capsules. During the preparation, 3% sodium carboxymethyl starch solution was used as adhesive for wet granulation, then the granules were dried at 60 ℃ and filled into the capsules. Meanwhile, a novel HPLC method for isolating and detecting five related
substances of palbociclib was established. An InertSustain C18 column was used with ammonium acetate buffer （pH 5.7）∶acetonitrile as mobile phase by gradient elution. The detective wavelength was 225 nm. The method was validated with specificity, sensitivity, and durability. The results indicated that the novel HPLC method could be used for its related substances＇ analysis and quality control.
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2018年第2期205-212,共8页
Chinese Journal of Pharmaceuticals
