枸橼酸他莫昔芬片的制备及质量评价

Preparation and Quality Evaluation of Tamoxifen Citrate Tablets

关键词:  枸橼酸他莫昔芬片  制备工艺  质量评价  溶出曲线

Key words:  tamoxifen citrate tablets  preparation process  quality evaluation  dissolution curve

摘要:

目的 探索枸橼酸他莫昔芬片的处方和制备工艺，并对其进行质量评价。方法 通过考察填充剂比例、黏合剂浓度、崩解剂用量、润滑剂用量、颗粒大小和水分含量等，筛选最优处方比例及制备工艺。制备若干批枸橼酸他莫昔芬片（1 000片/批），对颗粒休止角、药物晶型、片质量差异、硬度、崩解时限、含量等进行质量评价；同时，建立多条溶出曲线利用相似因子法评价自制片与参比制剂的相似性。结果 选用本处方和工艺条件制备的枸橼酸他莫昔芬片质量符合中国药典2015年版中的相关质量要求；4种溶出介质中溶出曲线的相似因子f₂值均>50。结论 枸橼酸他莫昔芬自制片与参比制剂具有体外溶出一致性。

Abstract:

OBJECTIVE To explore the preparation and process of tamoxifen citrate tablets and to evaluate the quality. METHODS The optimum formulation ratio and preparation process were screened by investigating the proportion of filler, binder concentration, amount of disintegrant, amount of lubricant, particle size and moisture content. Several batches of tamoxifen citrate tablets (1 000 tablets/batch) were prepared for quality evaluation of particle angle of repose, drug crystal form, tablet weight difference, hardness, disintegration time limit, content, etc. And multiple dissolution curves were established to evaluate the similarity of self-madness and reference formulation by similarity factor method. RESULTS The quality of tamoxifen citrate tablets prepared by using this prescription and process conditions was in accordance with the relevant quality requirements in the 2015 edition of the Chinese Pharmacopoeia; the similarity factor f₂ of the dissolution profiles in the four dissolution media was >50. CONCLUSION The homemade tablets of tamoxifen citrate and the reference preparation have in vitro dissolution consistency.