愈美软胶囊人体相对生物利用度和生物等效性  

Study on the bioavailability and bioequivalence of Yu-Mei soft capsules in healthy volunteers

作　　者：邓俊刚[1] 李茜[1] 张营[1] 乔健[1] 黎维勇[1] 

机构地区：[1]华中科技大学同济医学院附属协和医院,湖北武汉430022

出　　处：《中国医院药学杂志》2010年第13期1107-1111,共5页Chinese Journal of Hospital Pharmacy

摘　　要：目的:用研制的愈美软胶囊与上市产品愈美片进行比较,研究两制剂间的人体相对生物利用度,并做出生物等效性评价,以考察试验制剂的药品质量。方法:按照两制剂两周期随机交叉设计,20名男性健康志愿者单剂量口服试验软胶囊4粒或参比片4片。采用高效液相色谱-荧光法同时测定血浆氧去甲右美沙芬和愈创木酚甘油醚的浓度。运用DAS2.0软件处理血药浓度数据和计算药动学参数,并进行两制剂的生物等效性评价。结果:单剂量口服愈美软胶囊4粒或参比愈美片4片,测得氧去甲右美沙芬AUC0→14分别为(4848.2±1747.7)μg.h.L-1、(5008.0±1217.8)μg.h.L-1,AUC0→∞分别(5765.3±2490.5)μg.h.L-1、(5981.4±2428.3)μg.h.L-1;Cmax分别为(917.7±395.5)μg.L-1、(902.3±295.6)μg.L-1;tmax分别为(2.1±0.7)h、(2.6±0.9)h;愈创木酚甘油醚AUC0→14分别为(3320.6±1180.8)μg.h.L-1、(3541.1±1544.7)μg.h.L-1,AUC0→∞分别(3435.7±1187.2)μg.h.L-1、(3674.6±1599.7)μg.h.L-1;Cmax分别为(2193.9±957.8)μg.L-1、(1845.6±888.9)μg.L-1;tmax分别为(0.64±0.38)h、(0.79±0.39)h。结论:统计学结果显示,试验软胶囊与参比片剂具生物等效性。OBJECTIVE To objective of the present study was to evaluate the bioequivalence of two formulations of Yu-Mei in healthy human volunteers. METHODS A single oral dose of Yu-Mei soft capsules or tablets were given to 20 healthy male volunteers in an open randomized crossover design. Concentrations of dextrophan and guaifenesin were determined by HPLC with fluorescence detector. The pharmacokinetic parameters and relative bioavailability were calculated by DAS 2. 0 program to eqvaluate the bioequivalence of the two formulations. RESULTS The main pharmacokinetic parameters of the two formulations were as follows： （1） dextrophan ：AUC0→14 were （4 848. 2± 1 747.7）μg·h·L^-1 and （5 008. 0± 1 217. 8） μg·h·L^-1 ,AUG0→8 were （5 765.3±2 491）μg·h·L^-1 and （5 981.4 ± 2 428.3）μg·h·L^-1; Cmax were （917. 7 ± 395.5） μg·L^-1 and （902. 3 ± 295.6） ng·L^-1;tmax were （2. 1 ±0. 7） h and （2. 6 ± 0. 9） h; （2） guaifenesin： AUC8→14were （3 320. 6 ± 1 180. 8） μg·h·L^-1 . （3 541.1 ± 1 544. 7）μg·h·L^-1, AUG0→∞ were （3 435. 7 ± 1 187.2） μg·h·L^-1. （3 674. 6 ±1 599.7） μg·h·L^-1; Cmax were （2 193.9 ± 957. 8）μg·L^-1. （1 845.6 ± 888.9）μg·L^-1;tmax were （0.64 ± 0. 38） h and （0. 79 ± 0. 39） h. The relative bioavailability of dextromethorphan hydrobromide soft capsule to dextromethorphan hydrobromide tablets were as follows： dextrophan was （97. 8 ± 28. 3） % and guaifenesin was （ 100. 9 ± 38. 6） %. CONCLUSION The results of the statistical analysis showed that the two formulations are bioequivalent.

关 键 词：愈美软胶囊 氧去甲右美沙芬 愈创木酚甘油醚 β-葡糖苷酸酶 生物等效性 高效液相色谱法 

分 类 号：R969.1[医药卫生—药理学]