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以Soluplus为载体,采用热熔挤出技术制备普罗布考固体分散体,并评价其平衡溶解度、溶出度及大鼠体内药动学行为。结果表明,普罗布考-Soluplus比例为1:3(w/w)的固体分散体,在30 min时的体外累积溶出率为97%。差示扫描量热和粉末X-射线衍射分析表明药物主要以分子状态分散于固体分散体中。大鼠体内药动学研究表明,普罗布考固体分散体的c_(max)和口服生物利用度是原药的3.26倍和3.02倍。
With Soluplus as carrier, hot-melt extrusion technology was used to prepare probucol solid dispersion, and its equilibrium solubility, dissolution and pharmacokinetic behavior in rats were evaluated. The results showed that the solid dispersion with probucol-Soluplus ratio of 1: 3 (w / w) had an in vitro cumulative dissolution rate of 97% at 30 min. Differential scanning calorimetry and powder X-ray diffraction analysis showed that the drug was mainly dispersed in the solid dispersion in a molecular state. Pharmacokinetics studies in rats showed that the cmax and oral bioavailability of probucol solid dispersions were 3.26 and 3.02 times that of the original drug.