阿司匹林肠溶片的制备及体内外评价  

Preparation and in Vitro-in Vivo Evaluation of Aspirin Enteric-coated Tablets

作　　者：段丽萍 陈晓雪 杨志 吴银双 刘峻宇 金笛 Liping DUAN;Xiaoxue CHEN;Zhi YANG;Yinshuang WU;Junyu LIU;Di JIN(Yunnan Institute of Medicine,Kunming Yunnan 650100;Yunnan Province Company Key Laboratory for TCM and Ethnic Drug of New Drug Creation,Kunming Yunnan 650100,China)

机构地区：[1]云南省药物研究所,云南昆明650100 [2]云南省中药和民族药新药创制企业重点实验室,云南昆明650100

出　　处：《昆明医科大学学报》2024年第6期69-74,共6页Journal of Kunming Medical University

基　　金：云南省创新引导与科技型企业培育计划基金资助项目(202004AR040019)。

摘　　要：目的 制备阿司匹林肠溶片并考察它的体内外释药特性。方法 采用粉末直压法压片,以肠溶材料L30D-55水分散体、滑石粉和枸橼酸三乙酯(1∶1∶0.1)制备阿司匹林肠溶片包衣液固含量为20%,进行肠溶包衣,阿司匹林肠溶片包衣增重范围为15%~20%,制得0.1 g阿司匹林肠溶片,即自制制剂(T)。以0.1 g拜阿司匹林肠溶片(Bayaspirin^(R))为参比制剂(R),考察2种制剂的体外释放和体内餐后药动学行为。结果 阿司匹林肠溶片T与R的体外释放曲线f_(2)相似因子均大于50;检测物乙酰水杨酸的C_(max)、AUC_(0-t)和AUC_(0-∞)均满足相应的RSABE或ABE生物等效性评价标准。结论 T与R的体外释放和体内餐后药动学行为具有较好的一致性。Objective To prepare aspirin enteric-coated tablets and investigate its in vitro-in vivo release characteristics.Methods The powder was directly pressed into tablets,and a coating solution with a solid content of 20% was prepared with the aqueous dispersion of enteric-coated material L30D-55,talcum powder and triethyl citrate(1∶1∶0.1) for enteric coating,and the weight gain ranged from 15% to 20%,so that 0.1 g aspirin entericcoated tablets were prepared,that is,the self-made preparation(T).Taking 0.1 g(Bayaspirin^(R)) enteric-coated tablets( R) as reference preparation,the in vitro release and in vivo postprandial pharmacokinetics of the two preparations were investigated.Results The f_(2) factor of the in vitro release curves of T and R was greater than 50;C_(max),AUC_(0-t) and AUC_(0-∞) of acetylsalicylic acid all meet the corresponding RSABE or ABE bioequivalence evaluation criteria.Conclusion There is a good consistency between the in vitro release of T and R and the postprandial pharmacokinetics in vivo.

关 键 词：阿司匹林肠溶片 体内外评价 生物等效性 高变异药物 

分 类 号：R541.4[医药卫生—心血管疾病]