多潘立酮口崩片在中国健康受试者中的药代动力学和生物等效性研究  

Pharmacokinetics and bioequivalence of domperidone orally disintegrating tablets in healthy Chinese volunteers

作　　者：陈朝霞 曾洁萍[1] 南峰 丁红[1] 阎博华[1] 唐诗韵[1] CHEN Zhao-xia;ZENG Jie-ping;NAN Feng;DING Hong;YAN Bo-hua;TANG Shi-yun(Drug Clinical Trial Institution,Hospital of Chengdu University of Traditional Chinese Medicine,Chengdu 610072,Sichuan Province,China)

机构地区：[1]成都中医药大学附属医院国家药物临床试验机构,四川成都610072

出　　处：《中国临床药理学杂志》2020年第23期3880-3883,共4页The Chinese Journal of Clinical Pharmacology

摘　　要：目的研究多潘立酮口崩片在中国健康受试者中的药代动力学特征,并评价其生物等效性。方法空腹入组24例健康受试者,采用随机、开放、双交叉试验设计,单次口服受试制剂(多潘立酮口崩片)和参比制剂(多潘立酮普通片) 10 mg,用HPLC-MS/MS法测定血浆中多潘立酮浓度,用WinNonlin软件计算药代动力学参数,并评价两种制剂的生物等效性。结果单次口服试验制剂和参比制剂的主要药代动力学参数:Cmax分别为(17.05±6.93)和(13.86±6.74)μg·L^-1;tmax分别为(0.61±0.35)和(1.12±1.00) h;t1/2分别为(11.50±2.94)和(12.23±6.19) h;AUC0-t分别为(55.96±16.61)和(55.35±14.81)μg·L^-1·h;AUC0-∞分别为(57.66±16.89)和(56.69±14.87)μg·L^-1·h。单次口服试验制剂和参比制剂后的Cmax、AUC0-t和AUC0-∞的几何均值比90%置信区间分别为112.5%~135.5%,96.6%~110.7%,97.2%~111.3%。结论空腹状态下,多潘立酮口崩片与普通片的AUC0-t、AUC0-∞生物等效,但口崩片的tmax显著快于普通片,Cmax显著高于普通片,显示出口崩片起效快、吸收快的剂型特征。Objective To study the pharmacokinetic characteristics of domperidone orally disintegrating tablets in healthy Chinese subjects and evaluate its bioequivalence. Methods This was a random, open, cross design, 24 healthy Chinese subjects were enrolled under fasting condition. Each subject received single oral test preparation(T) and reference preparation(R) 10 mg. The plasma concentration of domperidone were measured by LC-MS/MS and calculated by WinNonlin software to evaluate the bioequivalence. Results The main pharmacokinetic parameters of tested and referenced preparations were as follows: the Cmax were(17.05±6.93) and(13.86±6.74) μg·L^-1;tmax were(0.61±0.35) and(1.12±1.00) h;t1/2 were(11.50±2.94) and(12.23±6.19) h;AUC0-twere(55.96±16.61) and(55.35±14.81) μg·L^-1·h;AUC0-∞ were(57.66±16.89) and(56.69±14.87) μg·L^-1·h. The 90% confidence interval of Cmax, AUC0-t and AUC0-∞ of test preparation in fasting condition were 112.5%-135.5%, 96.6%-110.7%, 97.2%-111.3%. Conclusion The AUC0-t and AUC0-∞ of the two formulations were bioequivalent. However,the tmaxof test preparation was significantly faster than that of reference preparation and the Cmaxwas significantly higher than that of reference preparation. The results displayed the faster absorption of domperidone orally disintegrating tablets.

关 键 词：多潘立酮 口腔崩解片 液质联用 药代动力学 生物等效性 

分 类 号：R97[医药卫生—药品]