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Fusion as an Approach to Enhance Dissolution Rate of a Poorly Water-soluble Drug (Curcurmin)

机译:融合作为提高水溶性差的药物(姜黄素)溶解速率的方法

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It's well known that curcumin is practically insoluble in water.Therefore,to improve the drug dissolution rate,fusion approach was employed to prepare curcumin solid dispersions (SDs) in the carrier Pluronic F68 with three different drug loads.The dissolution rate of curcumin from the SDs was measured at simulated gastric fluid.The concentration of the dissolved drug in the medium was determined by HPLC.The dissolution rates of the formulations were dependent on the drug loading in SDs.92.2% CUR was dissolved in 10 min from the SDs with 8.97% drug load,whereas the amounts of drug released were 65.8% and 84.2% within 120 min from the SDs with 18.9% and 29.0% drug loads,respectively.The Fourier transform infrared spectra indicated hydrogen bond between the drug and carrier.Furthermore,their physicochemical properties were well investigated using differential scanning calorimetry and X-ray diffraction.In the dispersions containing 8.97% CUR,the drug was in the molecular state.At a composition of approximately 18.9%,CUR was dispersed as micro-fine crystals.These interesting results indicate that the physical states of the drug in the carrier,which are governed by the drug loading,can affect the dissolution rate improvement.
机译:众所周知,姜黄素实际上不溶于水。因此,为了提高药物溶解速率,采用融合方法在载体Pluronic F68中制备具有三种不同的药物载荷的姜黄素固体分散体(SDS)。姜黄素的溶解速率在模拟胃液中测量SDS。通过HPLC测定介质中溶解药的浓度。制剂的溶解速率取决于SDS.92.2%的药物载量在10分钟内从SDS溶解于8.97 %药物载荷,而药物释放的药物量分别在18.9%和29.0%的药物载荷的40分钟内为65.8%和84.2%。傅里叶变换红外光谱指出药物和载体之间的氢键。繁殖,它们使用差示扫描量热法和X射线衍射进行良好研究了物理化学性质。含有8.97%Cur的分散体,药物处于分子状态。伴有Composi大约18.9%,Cur分散为微细晶体。有趣的结果表明,受药物载荷管辖的载体中药物的物理状态可以影响溶出速率改善。

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