【摘要】 目的:比较4种不同载体制备的熊果酸(UA)固体分散体的溶解度和体外溶出度。方法:分别以泊洛沙姆188(F68)、聚维酮PVP(S630)、硬脂酸聚烃氧(40)酯(S40)和羟丙甲纤维素(HPMC)为载体,采用溶剂法制备熊果酸固体分散体。测定溶解度,进行体外溶出试验,并采用差示扫描量热法(DSC)、X-射线衍射法(XRD)法鉴别药物在固体分散体中的存在状态。结果:以4种载体制备的固体分散体均能大大增加熊果酸(UA)的溶解度,加快其体外溶出。UA在固体分散体中以无定型态或分子状态存在。结论:各种载体对提高UA溶解度大小影响的顺序为S40>F68>HPMC>S630,对溶出度大小影响的顺序为HPMC>S40>F68>S630。更多还原

【Abstract】 OBJECTIVE To compare the solubility and in vitro dissolution of ursolic acid(UA) solid dispersions(SD) with 4 different carriers.METHODS UA solid dispersions were prepared with solvent method by using poloxamer 188(F68),polyvinylpyrrolidone(S630),polyoxyethylene(40) stearate(S40),and hydroxypropyl methylcellulose(HPMC) as carriers,respectively.The solubility and in vitro dissolution of the pure drug and solid dispersions were determined.The existing forms of UA in solid dispersions were investigated by differential scanning calorimetry(DSC) and X-ray diffraction(XRD).RESULTS The solubility and dissolution of UA solid dispersions were significantly higher than those of the pure drug and physical mixtures.It was found that UA existed as amorphous or molecular state in solid dispersions.CONCLUSION The effects of HPMC and S40 as carriers of solid dispersions on enhancing the dissolution of UA in solid dispersions are better than F68 and S630.更多还原