Study On Quality Standard Of Palbociclib Capsules

Palbociclib,an oral selective cyclin-dependent kinases(CDK)4/6 inhibitor,in combination with letrozole,is approved for the first-line treatment of postmenopausal women with estrogen receptor(ER)-positive,human epidermal growth factor receptor 2(HER2)-negative advanced breast cancer as an initial endocrine-based therapy for their metastatic disease.The original manufacturer is Pfizer Inc.with brand name Ibrance(?),and the 125mg specification is approved as reference preparation by FDA.The main purpose of this paper is to establish the quality standard of palbociclib capsule,and compare the quality of self-produced capsule with Ibrance(?).The main researches are as follow:1.Palbociclib capsules prescription researchIn this paper,orthogonal test was designed to screen the formulation of palbociclib capsule using the dissolution curve as main index.The optimal formulation was as follows:palbociclib 27.78%(w/w),microcrystalline cellulose 45.72%(w/w),lactose 20%(w/w),sodium starch glycolate 3%(w/w),silicon dioxide 2%(w/w),and magnesium stearate 1.5%(w/w).2.Palbociclib capsules quality standard researchIn this paper,the quality standard of palbociclib capsule was mainly investigated,including appearance,identification,related substances,dissolution rate and content.Identification was performed by UV and HPLC,and the other items were investigated by HPLC.Systematic methodological verification of the established analysis method was also conducted.Results indicated that the established analysis method was specific,accurate and reproducible.3.The self-produced products and the reference preparations quality consistency studyBased on the established quality standard of palbociclib capsule,the quality consistency of self-produced products and reference preparations were evaluated,including related substances,dissolution curves and content.The dissolution curves in four kinds of dissolution medium showed that the dissolution characteristics between self-produced products and reference preparations were similar.There was no significant difference in impurities and contents.The results demonstrated that the quality of self-produced products was similar with the reference preparations.