布洛芬缓释胶囊的生物利用度和药代动力学

Bioavailability and pharmacokinetics of sustained release capsule ofibuprofen

本文比较研究了布洛芬缓释胶囊（Ｆｅｎｂｉｄ）和普通市售片的药代动力学和生物利用度，并分析了生物利用度与体外溶出度的相关性。在５位受试者一次口服９００ｍｇ药物后，Ｆｅｎｂｉｄ的半衰期比市售片长，前者为４．８７５ｈ，后者为２．２３６ｈ，Ｆｅｎｂｉｄ的相对生物利用度（Ｆ）为１５０％。在１０位受试者连续给药，测定谷浓度，Ｆｅｎｂｉｄ的谷浓度变化范围小（９．３～１３．５μｇ／ｍｌ），而市售片的变化范围大（２．７～１７．３μｇ／ｍｌ）。结果表明Ｆｅｎｂｉｄ具有较理想的缓释特性。体外溶出度与体内生物利用度相关性分析证明Ｆｅｎ－ｂｉｄ的ＡＵＣ与溶出度显示良好的相关性（ｒ＝０．９９６４）。

A crossover study in 10 subjects was couducted to compare bioavailability and phar-macokinetics of Fenbid, a sustained release capsule of ibuprofen,with common ibuprofen tabletsafter single dose and continuous administration. The results of single dose showed that the peakconcentration of Fenbid was lower and achieved later than that of the common tablets. The half-life was 4.875h for Fenhd and 2.236h for the common tablets,and the relative bioavailability ofFenbid to the common tablets was 150%. The results of continuous administration of the twoibuprofen preparations indicated that the trough concentrations of Fenbid were higher and thevariation of mean trough concentrations was much less in subjects recieving Fenbid.It is suggest-ed that the sustained release capsule possesses better sustained release property.The relationstips between in vitro dissolution and in vivo bioavailability of the two prepara-tions indicated that there were good correlations between the in vitro test and in vivo test.Thecorrelation coefficients of percent dissolution vs AUC were 0.9964 for Fenbid and 0.9271 for thecommon tablets. We couclude that the in vitro dissolution may be used as a control device to en-sure process and batch-to-batch consistency for the ibuprofen preparations.