布洛伪麻那敏片和干混悬剂在健康人体内的生物等效性

Bioequivalence of ibuprofen,pseudoephedrine and chlorphenamine for tablet and suspension in healthy volunteers

目的研究布洛伪麻那敏片和干混悬剂在健康人体内的生物等效性。方法20名健康男性志愿者随机交叉口服单剂量布洛伪麻那敏片(受试制剂)和布洛伪麻那敏干混悬剂(参比制剂)。用高效液相色谱-紫外法测定血浆中布洛芬浓度,高效液相色谱-串联质谱法同时测定血浆中伪麻黄碱和氯苯那敏浓度。采用DAS2.0软件计算药动学参数,并进行生物等效性评价。结果参比制剂和受试制剂中布洛芬的ρmax分别为(13.6±s2.4)和(14±5)mg·L-1,tmax分别为(1.6±0.6)和(2.0±0.8)h,AUC0～t分别为(52±11)和(52±13)mg.h.L-1,t1/2分别为(2.3±0.5)和(2.3±0.5)h;伪麻黄碱的ρmax分别为(150±40)和(150±50)μg·L-1,tmax分别为(1.0±0.5)和(1.7±1.7)h,AUC0～t分别为(1200±500)和(1200±600)μg.h.L-1,t1/2分别为(7.5±1.9)和(7.7±2.1)h;氯苯那敏的ρmax分别为(2.5±0.8)和(2.5±0.4)μg·L-1,tmax分别为(3.0±1.6)和(2.8±1.6)h;AUC0～t分别为(40±19)和(34±15)μg.h.L-1,t1/2分别为(20±8)和(22±8)h。受试制剂中布洛芬、伪麻黄碱和氯苯那敏的相对生物利用度分别为(100±14)%、(100±25)%和(87±18)%。结论2种制剂具有生物等效性。

AIM To study the relative bioequivalence of ibuprofen, pseudoephedrine and chlorphenamine for tablet and suspension in healthy volunteers. METHODS A total of 20 subjects were administered with single dose of tablet （test） and suspension （reference） preparations of ibuprofen, pseudoe-phedrine and chlorphenamine by across-over way. The blood concentration of ibuprofen was determined by HPLC-UV. The blood concentration of pseudoephedrine and chlorphenamine were determined by LC-MS/MS. The pharmacokinetic parameters and the bioequivalence were computed using DAS 2.0 program. RESULTS The main pharmacokinetic parameters of the reference and test preparation of ibuprofen were as follows： ρmax were （13.6 ± s 2.4） vs. （14 ± 5） mg·L^-1, tmax were （1.6 ± 0.6） vs. （2.0 ± 0.8） h, AUC0-t were （52 ± 11） vs. （52 ± 13） mg·h·L^-1, t1/2 were （2.3 ± 0.5） vs. （2.3 ± 0.5） h; pseudoephedrine as follows： ρmax were （150± 40） vs. （150±50）μg·L^-1, tmax were （1.0±0.5） vs. （1.7± 1.7） h, AUC0-t were （1 200±500） vs. （1200± 600） μg·h·L^-1, t1/2 were （7.5 ± 1.9） vs. （7.7± 2.1） h; chlorphenamine as follows： ρmax were （2.5 ±0.8） vs. （2.5 ± 0.4） μg·L^-1, tmax were （3.0 ± 1.6） vs. （2.8 ± 1.6） h, AUC0-t were （40 ± 19） vs. （34 ± 5） μg·h·L^-1, t1/z were （20 ± 8） vs. （22 ± 8） h. The bioequivalence of ibuprofen, pseudoephedrine, and chlorphenamine were （100 ± 14）%, （100 ± 25）%, and （87 ± 18）%, respectively. CONCLUSION The two preparations are bioequivalent.