复方磺胺甲噁唑片在正常人体内的药动学及相对生物利用度

Pharmacokinetics and relative bioavailability of co trimexazole in healthy volunteers

目的 :研究了 10名志愿受试者自身交叉 po单剂量Co SMZ片和Co SMZ分散片 80 0mg的药动学及相对生物利用度。方法 :按照随机交叉试验设计 ,采集服药后 0 .2 5 ,0 .5 ,0 .75 ,1,2 ,3,4,6 ,8,10 ,12 ,2 4,36 ,48h的血样本 ,用HPLC测定SMZ和TMP的血药浓度。结果 :Co SMZ分散片及Co SMZ片中SMZ和TMP的主要药动学参数分别为 :cmax为 (46 .6 9± 7.6 6 ) ,(44 .6 1± 6 .37) μg·ml-1和 (1.82± 0 .49) ,(1.6 3± 0 .43) μg·ml-1;tmax为 (3.41± 1.5 9) ,(3.4± 0 .84)h和 (1.48± 0 .83) ,(1.5 0± 0 .81)h ;AUC =(76 1± 12 9.37) ,(76 1.79± 145 .6 ) μg·h·ml-1和 (2 6 .91± 3.89) ,(2 6 .96± 4.71) μg·h·ml-1。两种制剂的药动学参数除TMP的Ka值P <0 .0 5外 ,其他参数均无显著性差异 (P >0 .0 5 )。结论 :受试制剂相对于参比制剂的相对生物利用度分别为 (10 1.2 8± 14.35 ) % ,(10 1.2 6± 15 .76 ) %。受试制剂与参比制剂生物等效。

OBJECTIVE:The pharmacokinetics and relative bioavailability of dispersible tablet of co trimexazole were studied in 10 healthy male volunteers.METHODS:A single oral dose of 800 mg co trimexazole of the two formations(test and reference preparations) was given in a randomized 2 way cross over design.Blood samples were withdrawn up to 48 hours post administration.Plasma concentrations of SMZ and TMP were assayed by HPLC.RESULTS:The main pharmacokinetic parameters of SMZ and TMP in the test preparation and the reference preparation were as following.c max :(46.69±7.66),(44.61±6.37) μg·ml -1 and (1.82±0.49),(1.63±0.43) μg·ml -1 ;t max :(3.41±1.59),(3.4±0.84) h and (1.48±0.83),(1.50±0.81) h;AUC (761±129.37),( 761.79 ±145.6) μg·h·ml -1 and (26.91±3.89),(26.96±4.71) μg·h·ml -1 ,respectively.CONCLUSION:The relative bioavailability of the test preparation was (101.28±14.35)%(SMZ) and (101.26±15.76)% (TMP) to the reference preparation,indicating that both preparations were bioequivalent.