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目的 制备化合物4-邻甲基苯磺酰氧基苯并唑酮(MBB)固体分散体,以提高其溶出度;建立高效液相色谱法(HPLC)法测定MBB固体分散体在大鼠血浆的浓度,并进行初步的药代动力学研究.方法 以聚乙烯吡咯烷酮PVPk30,PEG6000,PEG4000和泊洛沙姆188为载体,按照MBB与载体质量比为1:5、1:8、1:10制备固体分散体,并测定其溶出度,绘制溶出曲线,以确定最佳固体分散体的制备处方;SD大鼠灌胃给予MBB固体分散体,采用HPLC法测定不同时间MBB在血浆中的浓度,绘制血药浓度曲线,利用计算机程序3p87进行房室模型拟合,计算药代动力学参数.结果 当MBB与PVPk30的质量比为1:8时,溶出度最高,为该固体分散体的最优处方;该分散体在大鼠体内的药代动力学符合一室模型,其AUC为123.39(μg·ml-1)×min,cl为0.41μg·ml·h(mg/kg),t1/2(ka)为8.48 min,t1/2(ke)为8.86 min.结论 将MBB制成固体分散体,可显著提高其溶出度,且当MBB与PVPk30的质量比为1:8时为最优处方;该固体分散体可显著提高MBB的血药浓度.“,”Objective To prepare the solid dispersion of 4-o-methyl-benzenesulfonyl benzoxazolone (MBB) for enhancing its dissolution rate, and to establish HPLC method for the measurement of plasma concentration of MBB solid dispersion in rats and for preliminary pharmacokinetic study. Methods The solid dispersions of MBB were prepared with PVPk30, PEG6000, PEG4000 and poloxamer 188 as carriers at the mass ratios of 1:5, 1:8 and 1:10, and the dissolution rates were measured to determine the optimal preparation formulation. The SD rats were given in-tragastric administration of MBB solid dispersions, and the concentration of MBB in plasma was determined by HPLC at different time points. The plasma concentration curve was drawn and compartment model was fitted by the computer program 3p87 to calculate the pharmacokinetic parameters. Results When the mass ratio of MBB to PVPk30 was 1:8, the dissolution rate was the highest, which was the optimal prescription for the solid dispersion. The pharmacoki-netics of MBB solid dispersion conformed to the one-compartment model with the AUC of (μg·mL-1)×min, cl of 0.41μg/mL/h/(mg/kg), t1/2 (ka) of 8.48 min and t1/2 (ke) of 8.86 min. Conclusion The MBB-prepared solid dispersion can significantly improve the dissolution rate when the mass ratio of MBB to PVPk30 is 1:8, which is the optimal pre-scription. The solid dispersion can significantly increase the plasma concentration of MBB.