普罗布考固体分散体的制备及体内评价

Preparation and in vivo Evaluation of Probucol Solid Dispersion

普罗布考分别以PEG6000、PEG12000和PVP为载体,以不同配比、采用溶剂-熔融法或溶剂法制备固体分散体。结果表明,以PVP为载体制备的固体分散体(药物-PVP,1∶5)体外溶出效果较好,并进行了家兔体内生物利用度试验和大鼠在体肠回流试验。计算得固体分散体对原药的相对生物利用度约558%,其肠吸收与原药有显著差异(P<0.05)。

Probucol solid dispersion was prepared by the solvent-melting method and the solvent method with PEG 6000, PEG 12000 and PVP as carriers in different ratios, respectively. The results showed that the in vitro dissolution of the solid dispersion with PVP as carrier （drug-PVP, 1：5） was satisfactory. The bioavailability in rabbits and in situ recirculating of intestinal segments of rats were determined. The relative bioavailability of solid dispersion to bulk drug was 558 %, and intestinal absorption of probucol solid disoersion had a significant difference with the hulk drue （P 〈 0.05）.