布洛芬缓释片的人体生物等效性研究

目的:研究布洛芬缓释片在健康人体内的药动学及其相对生物利用度,以评价其与布洛芬缓释胶囊的生物等效性。方法:18名男性志愿者,随机分为2组,分别口服布洛芬缓释片(受试制剂)与布洛芬缓释胶囊(参比制剂)后,采用高效液相色谱法测定血药浓度,用3p97药动学程序拟合,计算药动学参数。结果:受试制剂与参比制剂Cmax分别为(25.43±0.78)、(26.87±0.66)μg·mL-1,tmax分别为(3.67±0.52)、(3.83±0.75)h,AUC0~24分别为(181.20±5.12)、(187.58±5.29)μg·h·mL-1,AUC0~∞分别为(184.34±5.35)、(191.19±4.87)μg·h·mL-1,MRT分别为(6.51±0.73)、(6.80±0.48)h;受试制剂的相对生物利用度为103.7%。结论:与参比制剂比,布洛芬缓释片有较好的缓释效果。

Bioavailability of Ibuprofen Sustained Release Tablets in Human Body

OBJECTIVE： To study the pharmacokinetics and bioavailability of Ibuprofen Sustained Release Tablets in healthy volunteers. METHODS： A total of 18 male healthy volunteers were randomly divided into two groups. They were assigned to receive lbuprofen Sustained Release Tablets （trial preparation） and Ibuprofen Sustained Release Capsules （reference preparation） respectively. The concentrations of ibuprofen in plasma were determined by RP- HPLC. The main pharmacokinetic parameters were obtained using 3p97 program. RESULTS： The C of the two preparations were （25.43± 0.78）μg · mL^-1 and （26.87 ± 0.66）μg · mL^-1 respectively; tmax were （3.67 ± 0.52） h and （3.83 ±0.75） h ; AUC0-24 were （181.20±5.12）μg· h· mL^-1and（187.58±5.29）μg· h· mL^-1;AUC0-∞were（184.34±5.35）,（191.19±4.87）μg· h·mL^-1; MRT were （6.51± 0.73）h and （6.80±0.48） h, respectively. The relative bioavailability of the sustained-release tablets was 103.7%. CONCLUSION： The ibuprofen sustained release tablets have remarkable sustained release efficacy.