摘要
目的采用冷冻干燥法制备片型平整饱满、崩解性良好的奥氮平口腔崩解片,并比较自研制剂与参比制剂在4种溶出介质中的溶出行为,对自研制剂的质量做出评价。方法以外观、崩解时限、口感、水分及再分散性为指标,通过单因素分析对奥氮平口腔崩解片中的辅料用量及冻干工艺进行考察及优化,同时对其质量进行初步评价;参照美国药典USP 40中奥氮平口腔崩解片溶出方法,采用HPLC法测定并比较自研制剂与参比制剂在4种不同溶出介质中的溶出曲线。结果优化后的处方为奥氮平10 mg/片,甘露醇、明胶均为8 mg/片,阿司帕坦1 mg/片,对羟基苯甲酸甲酯钠0.15 mg/片,对羟基苯甲酸丙酯钠0.05 mg/片,所得片剂外观平整饱满、崩解较快、口感良好。自研制剂与参比制剂在4种介质中15 min时的溶出度均>85%。结论奥氮平口腔崩解片自研制剂与参比制剂的体外溶出行为相似,且批间差异小,提示其处方工艺稳定合理,为后期试验研究奠定了基础。
Objective To prepare the olanzapine orally disintegrating tablets with full shape and good disintegration by freeze-drying method,compare the dissolution behavior of self-developed preparation and reference preparation in 4 dissolution media,and evaluate the quality of self-developed preparation.Methods The appearance,disintegration time,taste,moisture and redispersibility were taken as indicators,the dosage of auxiliary materials and freeze-drying technology in the olanzapine orally disintegrating tablets were investigated and optimized by single factor analysis,and the quality of olanzapine orally disintegrating tablets was evaluated.The dissolution method of olanzapine orally disintegrating tablets in USP 40 was referred to.The dissolution curves of the self-developed preparation and the reference preparation in 4 dissolution media were determined and compared by HPLC.Results The optimized formulation of olanzapine orally disintegrating tablets was as follows:olanzapine 10 mg,mannitol 8 mg,gelatin 8 mg,aspartame 1 mg,sodium methyl parahydroxybenzoate 0.15 mg,and sodium propyl parahydroxybenzoate 0.05 mg.Its appearance was smooth and plump,with quick disintegration and good taste.The dissolution of self-developed preparation and reference preparation in the 4 media for 15 min was more than 85%.Conclusion The dissolution behavior of olanzapine orally disintegrating tablets in vitro is similar to that of the reference preparation,with small difference between batches,suggesting that the formulation process is stable and reasonable.
作者
李聘
郭杏梅
孙腾跃
闵蕊
吴茜
李红鑫
蔡程科
王洪飞
LI Pin;GUO Xing-mei;SUN Teng-yue;MIN Rui;WU Qian;LI Hong-xin;CAI Cheng-ke;WANG Hong-fei(School of Chinese Meteria Medica,Beijing University of Chinese Medicine,Beijing 102488;Beijinguantum Hi-tech Pharmaceutical Technical Co.,Ltd,Beijing 102200)
出处
《中南药学》
CAS
2020年第11期1831-1837,共7页
Central South Pharmacy
基金
北京市科技计划专项研发项目(No.Z16010101390)。
关键词
奥氮平
口腔崩解片
冷冻干燥法
溶出方法
溶出行为
olanzapine
orally disintegrating tablet
freeze-drying method
dissolution method
dissolution behavior
