茶苯海明口腔崩解片及其普通片在恒河猴体内的药代动力学比较(英文)  

In vivo evaluation of dimenhydrinate orally disintegrating tablets:Comparison of the pharmacokinetics with conventional tablets in rhesus

作　　者：贺建昌[1] 刘迪[1] 冯恩富[1] 张青[1] 董丽春[1] 徐贵丽[1] 

机构地区：[1]成都军区昆明总医院药剂科

出　　处：《中国临床药理学与治疗学》2010年第4期416-421,共6页Chinese Journal of Clinical Pharmacology and Therapeutics

基　　金：supported by Yunnan Natural Science Foundation of China(No: 2003C0016R)

摘　　要：目的:比较茶苯海明口腔崩解片及其普通片在恒河猴体内的药代动力学特征。方法:采用随机、自身对照方法考察两制剂在恒河猴体内的药代动力学特点;采用HPLC-UV法测定分别口服给予相应剂量的药物(均为茶苯海明50 mg)后恒河猴体内血药浓度;并采用DAS2.0对药代动力学参数进行统计分析。结果:茶苯海明口腔崩解片相对生物利用度(F_(0-12h),F_(0-∞))分别为(154±42)%和(150±53)%。两制剂间的血药浓度时间-曲线下面积(AUC_(0-∞))差异无统计学意义(P>0.05),而C_(max)和AUC_(0-12)差异有统计学意义(P<0.05)。此外,茶苯海明口腔崩解片t_(max)与普通片比较明显缩短,但差异无统计学意义(P>0.05)。茶苯海明在恒河猴空白血浆中10～2000 ng/mL浓度范围内线性良好(r=0.99995),最低检测限(LLOQ)10 ng/mL。其他确证数据如准确度、精密度等均在要求范围内。结论:茶苯海明口腔崩解片在体内吸收比普通片快。AIM：To compare the pharmacokinetics characteristics of dimenhydrinate orally disintegrating tablets（ODTs） and conventional tablets in rhesus plasma.METHODS：A randomized two-period,self-control crossover study with regard to the pharmacokinetic characteristics of dimenhydrinate ODTs and conventional tablets was executed in rhesus.The plasma concentrations of dimenhydrinate after oral administration of two formulations（both doses were 50 mg dimenhydrinate） were estimated by a simple, sensitive and specific HPLC-UV method.The pharmacokinetic parameters were computed by software DAS 2.0 and compared by statistic analysis. RESULTS：The relative bioavailability of dimenhydrinate ODTs（F0-12 h,F0-∞ were （154±42）%and（150±53）%,respectively, compared with conventional tablets.There was no significant difference in area under the plasma concentration（AUC0-∞ ）（P〈0.05 ） between the two formulations.Interestingly,there had statistically significant difference between the dimenhydrinate ODTs and conventional tablets in Cmax,area under the plasma concentration （AUC0-12 h）（P〈0.05）.Moreover,dimenhydrinate ODTs showed a markedly,but not significantly shorter tmax compared with conventional tablets（P〈0.05）.The method was sensitive with a lower limit of quantitation（LLOQ） of 10 ng/mL and good linearity in the range 10-2000 ng/mL for dimenhydrinate（r = 0.99995）.All the validation data,such as accuracy,precision, intra-day and inter-day repeatability,were with-in the required limits.CONCLUSION：Dimenhydrinate ODTs have a faster absorption compared with conventional tablets.

关 键 词：茶苯海明 口腔崩解片 药代动力学 

分 类 号：R969.1[医药卫生—药理学]