中国临床药学杂志

目的 :通过对布洛芬混悬液人体内药物动力学及生物利用度研究 ,评价该制剂与片剂的生物等效性。方法 :采用高效液相色谱法测定 18名健康男性志愿者自身交叉单剂量口服布洛芬混悬液和布洛芬片剂 4 0 0mg的经时血药浓度。药 时曲线数据经 3P87药物动力学计算程序处理 ,计算主要药物动力学参数以及受试制剂的生物利用度 ,同时评价 2种制剂的生物等效性。结果 :受试制剂和参比制剂的吸收速率常数 (Ka)分别为 (1 6 5± 1 4 6 )h-1和 (0 70± 0 2 5 )h-1;消除半衰期 (T1/ 2 )分别为 (1 89± 0 32 )h和 (1 92± 0 38)h ;峰浓度 (cmax)分别为 (5 2 6 2± 14 2 1) μg·mL-1和 (42 4 3± 10 6 2 ) μg·mL-1;达峰时间 (tmax)分别为 (1 5 5± 0 70 )h和 (2 6 8± 0 86 )h ;药 时曲线下面积 (AUC0→∞)分别为 (2 4 2 0 3± 35 70 ) μg·h·mL-1和 (2 37 0 4± 39 6 3) μg·h·mL-1;受试制剂的生物利用度 (F)为 (10 2 81± 11 4 5 ) %。经统计学处理 ,2种制剂的Ka ,cmax,tmax有显著性差异 (P <0 0 5 ) ;布洛芬混悬液吸收迅速 ,T1/ 2 ,AUC0→∞ 无显著性差异 (P >0 0 5 )。结论 :布洛芬混悬液与片剂具有生物等效性

AIM: To compare the bioavailability of ibuprofen suspension and tablets in healthy volunteers. METHODS: A high performance liquid chromatography method was used to determine the time serum ibuprofen concentrations after oral administration of 400 mg ibuprofen suspension and tablets in a cross over test. Pharmacokinetic parameters were calculated and evaluated. RESULTS: The K a, T 1/2 , c max , T peak and AUC of suspension were (1 65±1 46) h -1 , (1 89±0 32) h, (52 62±14 21) μg·mL -1 , (1 55±0 70) h, (242 03±35 70) μg·h·mL -1 , and those of tablets were (0 70±0 25) h -1 , (1 92±0 38) h, (42 43±10 62) μg·mL -1 , (2 68±0 86) h and (237 04±39 63) μg·h·mL -1 respectively. The relative bioavailability of ibuprofen suspension versus tablets is (102 8±11 45) %. CONCLUSION: The ibuprofen suspension and tablets are bioequivalent.