布洛芬混悬液人体生物利用度和药物动力学研究

Relative bioavailability and pharmacokinetics of ibuprofen suspension

用反相高效液相色谱法，血样甲醇沉淀蛋白后直接进样测定。１０名受试者随机分组自身交叉对照试验，单剂量口服布洛芬片或混悬液３００ｍｇ，布洛芬药时数据经３Ｐ８７程序拟合为一房室模型，其主要药动学参数，片剂和混悬液分别为：Ｋａ０．７２±０．１８ｈ－１，２．５０±０．８ｈ－１；Ｔ１／２ｋｅ２．０４±０．３２ｈ，２．２±０．５ｈ；ＡＵＣ０－∞１１１±２５ｍｇ·ｌ·ｈ－１，１１９±２８ｍｇ·ｌ·ｈ；Ｔｍａｘ２．８±０．６ｈ，０．９８±０．２３ｈ；Ｃｍａｘ１９．９±３．４μｇ·ｍｌ－１，２７．３±３．３μｇ·ｍｌ；相对生物利用度１０７．１６±８．１２％。

Ibuprofen in human serum was determined using Shimadzu 10 A HPLC. A single 300mg oral administration of ibuprofen tablets and ibuprofen suspension was given to 10 healthy male volunteers in randomized selfcrossover study. The concentration time profiles of ibuprofen in the two dosage forms fitted to the manifestation of the one compartment model. Pharmacokinetic parameters for ibuprofen tablets and suspension were: Ka 0.72 ± 0.18 h -1 and 2.5 ± 0.8 h -1 ; t 1/2 2.04 ± 0.32 h and 2.2 ± 0.5 h; T max 2.8 ± 0.6 h and 0.98 ± 0.23 h; C max 19.9 ± 3.4 mg·L -1 and 27.2 ± 3.3 mg·L -1 , AUC 111 ± 25 mg·h·L -1 and 111 ± 28 mg·h·L -1 , respectively relative bioavailabity of ibuprofensuspension was 107.16 ± 8.12% .