Cyclodextrins possess the ability to increase the apparent solubility and dissolution rate of poorly water soluble drugs. The objectives of the study were to investigate the effect of β-cyclodextrin, hydroxypropyl-β-cyclodextrin and sulfobutyl ether7 β-cyclodextrin on solubility and dissolution rate of docetaxel. Four different methods (physical mixture, kneading, freeze drying and solvent evaporation) were employed for inclusion complexation, at varying drug to cyclodextrin ratios 1:1, 1:2 and 1:4. The inclusion complexes of docetaxel with β-cyclodextrin, hydroxypropyl-β-cyclodextrin and sulfobutyl ether7 β-cyclodextrin at molar ratios 1:1 were characterized by fourier transform infrared spectroscopy (FTIR), X-ray diffractometry (XRD), differential scanning calorimetry (DSC), thermogravimetric analysis (TGA) and proton nuclear magnetic resonance (1H NMR). The dissolution profiles of inclusion complexes were compared with pure drug. The results revealed formation of inclusion complexes between drug and β-cyclodextrin, hydroxypropyl-β-cyclodextrin and sulfobutyl ether7 β-cyclodextrin as confirmed by FTIR. 1H NMR revealed inclusion of drug within cyclodextrin cavity with appearance of proton shifts. Drug crystallinity was reduced with physical mixing and kneading method while amorphous form was attained by freeze drying and solvent evaporation method as revealed by XRD. The DSC and TGA confirmed the formation of inclusion complexes with the absence of melting peak of drug. The effect on solubility and dissolution rate of docetaxel was greater with sulfobutyl ether7 β-cyclodextrin than hydroxypropyl-β-cyclodextrin and β-cyclodextrin when prepared with similar methods. Drug to cyclodextrin ratio 1:1 was the optimum ratio to increase the solubility and dissolution of docetaxel irrespective of the method. It is concluded that sulfobutyl ether7 β-cyclodextrin had greater effect on solubility and dissolution rate of docetaxel than β-cyclodextrin and hydroxypropyl-β-cyclodextrin at molar ratios 1:1.

中文翻译：

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β-环糊精、HP-β-环糊精和SBE7-β-环糊精通过包合络合对多西紫杉醇溶解度和溶出度的影响比较

环糊精具有增加难溶于水药物的表观溶解度和溶出度的能力。该研究的目的是研究β-环糊精、羟丙基-β-环糊精和磺丁基醚7 β-环糊精对多西紫杉醇的溶解度和溶出度的影响。四种不同的方法（物理混合、捏合、冷冻干燥和溶剂蒸发）用于包合络合，药物与环糊精的比例不同，分别为 1:1、1:2 和 1:4。多西紫杉醇与β-环糊精、羟丙基-β-环糊精和磺丁基醚7 β-环糊精的摩尔比为1:1的包合物通过傅里叶变换红外光谱（FTIR）、X射线衍射（XRD）、差示扫描量热法（ DSC), 热重分析 (TGA) 和质子核磁共振 (1H NMR)。将包合物的溶出曲线与纯药物进行比较。结果表明，FTIR 证实了药物与 β-环糊精、羟丙基-β-环糊精和磺丁基醚 7 β-环糊精之间形成了包合物。1H NMR 显示药物包含在环糊精腔内，并出现质子位移。XRD 显示，通过物理混合和捏合方法降低了药物结晶度，而通过冷冻干燥和溶剂蒸发方法获得了无定形形式。DSC 和 TGA 证实了包合物的形成，没有药物的熔化峰。当用类似方法制备时，磺丁基醚7 β-环糊精对多西紫杉醇的溶解度和溶出速率的影响大于羟丙基-β-环糊精和β-环糊精。无论采用何种方法，药物与环糊精的比例 1:1 是增加多西紫杉醇溶解度和溶出度的最佳比例。结论是磺丁基醚7 β-环糊精对多西紫杉醇的溶解度和溶出速率的影响大于摩尔比为1:1的β-环糊精和羟丙基-β-环糊精。