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为提高元胡止痛方中2个有效组分延胡索乙素(1)和欧前胡素(2)的口服生物利用度,采用溶剂挥发法制备其固体分散体。优化结果表明,载体材料宜选用聚乙烯吡咯烷酮(PVP K30),药物(1∶2=1∶1)与PVP K30的比例为1∶1。差示扫描量热和X-射线衍射分析结果表明,1和2均以无定形状态存在于制剂中。与原料药相比,1和2的溶解度和溶出度均显著增加。大鼠药动学试验结果显示,与单独灌胃给予1和2原料药相比,固体分散体组大鼠血浆中1和2的AUC得到显著提高(P<0.05)。以AUC_(0→t)计算,1和2的相对生物利用度分别为155%和187%。可见,固体分散体可同时提高这2种有效成分的溶解度、溶出度和口服吸收。
In order to improve the oral bioavailability of two effective components of Yuanhu Zhitong Fang, tetrahydropalmatine (1) and imperatorin (2), the solid dispersion was prepared by solvent evaporation method. The optimization results showed that polyvinylpyrrolidone (PVP K30) should be used as the carrier material, and the ratio of drug (1: 2 = 1: 1) to PVP K30 should be 1: 1. Differential scanning calorimetry and X-ray diffraction analysis showed that both 1 and 2 were present in the formulation in an amorphous state. Compared with API, the solubility and dissolution of 1 and 2 are significantly increased. The results of pharmacokinetics in rats showed that the AUCs of 1 and 2 in the plasma of rats in the solid dispersion group were significantly increased (P <0.05) compared with those of the 1 and 2 bulk drugs administered orally. The relative bioavailability of 1 and 2, calculated as AUC_ (0 → t), was 155% and 187%, respectively. Visible, solid dispersion can improve the solubility of these two active ingredients, dissolution and oral absorption.