依普黄酮固体分散体的制备和溶出特性(英文)

目的:制备和鉴定依普黄酮固体分散体,测定它的体外溶出度。方法:用溶剂法制备依普黄酮固体分散体,用DSC,X衍射和红外光谱鉴定固体分散体,浆法测定它的溶出度。结果:由依普黄酮和聚维酮(1:8)组成的固体分散体,其体外溶出度是依普黄酮的6.15倍,DSC曲线,X衍射图谱和红外光谱均产生了明显变化。结论:依普黄酮被制成固体分散体能明显增加依普黄酮的体外溶出度。     

槲皮素PVP固体分散体的制备及物相鉴定

目的用溶剂法制备槲皮素-PVP固体分散体并考察其溶出特性并对物相进行鉴定。方法采用溶剂法制备槲皮素-PVP固体分散体,通过溶出实验对槲皮素溶出率的测定研究固体分散体的溶出性质,利用差热分析（Differentialscanning calorimetry,DSC）、红外光谱分析（Infrared spectroscopy,IR）、粉末X衍射（X-ray powder diffractometry,PXRD）、扫描电镜（Scanning electron microscopy,SEM）等方法对其进行物相鉴定。结果槲皮素-PVP固体分散体的溶出速率相对其物理混合物有了明显的改善; 溶解实验显示固体分散体中槲皮素的溶解度有了显著的提高;热差分析及粉末X衍射结果表明固体分散体中槲皮素呈非结晶形式;扫描电镜下固体分散体中无槲皮素晶体。结论采用溶剂法制备槲皮素-PVP固体分散体可显著提高槲皮素的溶解度及溶出速度。     

Enhanced release of solid dispersions of etodolac in polyethylene glycol

This work examines the release of etodolac from various molecular weight fractions of polyethylene glycol (PEG) solid dispersions. Solid dispersions of etodolac were prepared in different molar ratios of drug/carrier by using solvent and melting methods. The release rate of etodolac from the resulting complexes was determined from dissolution studies by use of USP dissolution apparatus 2 (paddle method). The physical state and drug:PEG interaction of solid dispersions and physical mixtures were characterized by X-ray diffraction (XRD), infrared spectroscopy (IR) and differential scanning calorimetry (DSC). The dissolution rate of etodolac is increased in all of the solid dispersion systems compared to that of the pure drug and physical mixtures. The solid dispersion compound prepared in the molar ratio of 1:5 by the solvent method was found to have the fastest dissolution profile. The physical properties did not change after 9 months storage in normal conditions.     

熔融法制备卡马西平-烟酰胺共结晶固体分散体

目的联用共结晶和固体分散技术,提高卡马西平的体外溶出度。方法以PVP VA64为载体,采用熔融法制备卡马西平-烟酰胺共结晶固体分散体。进行体外溶出实验,并采用粉末X射线衍射和差示扫描量热法鉴别卡马西平和烟酰胺在载体中的分散状态。结果卡马西平和烟酰胺结合形成共结晶后以无定形态或分子态分散在载体中,而在卡马西平固体分散体中,药物和载体形成低共融物,以微晶状态分散。卡马西平-烟酰胺共结晶固体分散体的体外溶出结果优于卡马西平固体分散体。结论共结晶固体分散体显著提高了药物的体外溶出度。     

米非司酮固体分散体的制备及性质研究

目的:增加米非司酮的溶解度和体外溶出速率,为阴道环的成功制备奠定基础。方法:以PVPK30为载体,采用溶剂法制备米非司酮固体分散体。考察其体外溶出特性,并采用差示扫描量热法、红外光谱法和粉末X-射线衍射法鉴别药物在固体分散体中的存在状态。结果:固体分散体大大提高了米非司酮的溶出速率,最佳比例为1∶3。药物在分散体中以无定型状态存在。结论:溶剂法制备的固体分散体可显著提高药物的溶出速率,从而提高了阴道环中药物的释放量。     

穿心莲内酯聚丙烯酸树脂Ⅱ固体分散体的制备及表征

目的：研究无定形聚合物聚丙烯酸树脂Ⅱ（Eudragit Ⅱ）制备的穿心莲内酯固体分散体的优良性质,为固体分散体的载体选择提供参考依据。方法：以无定形聚合物Eudragit Ⅱ为载体材料,按穿心莲内酯-载体质量比为1：3,采用喷雾干燥法制备穿心莲内酯固体分散体,并用傅里叶变换红外光谱（FTIR）、热重分析（TG）、X-射线衍射（XRD）、差示扫描量热（DSC）、扫描电镜（SEM）、比表面积、粒径和溶出度测定穿心莲内酯固体分散体的理化性质及溶出行为。结果：FTIR光谱和TG分析说明在穿心莲内酯固体分散体和物理混合物中穿心莲内酯与Eudragit Ⅱ之间都存在分子间相互作用,其中穿心莲固体分散体具有更好的热稳定性;DSC和XRD分析说明无定形载体Eudragit Ⅱ制备的固体分散体中穿心莲内酯主要以无定形形式存在;SEM显示,固体分散体中穿心莲内酯由块状晶体形态变为了不规则的圆形形态;同时与物理混合物相比,穿心莲内酯固体分散体具有更大的比表面积、更大的孔体积和更小的粒径等粉体学性质;溶出实验表明穿心莲内酯固体分散体具有增大溶出的优势,效果明显。结论：以无定形载体Eudragit Ⅱ制备的穿心莲内酯固体分散体具有优良的理化性质,同时比表面积大,孔体积大的特征更有利于水分子的进入,从而有效地增大穿心莲内酯的溶出速率。     

复合载体齐墩果酸固体分散体的制备及评价

目的：制备复合载体齐墩果酸固体分散体,提高齐墩果酸的溶出度。方法：采用溶剂法,以聚乙烯吡咯烷酮（PVP VA64）和聚乙烯己内酰胺-聚乙酸乙烯酯-聚乙二醇接枝共聚物（Soluplus）为复合载体,制备齐墩果酸固体分散体,以累积溶出度为评价指标,考察不同载体比例,药物与载体比例,筛选最佳工艺。通过差式扫描量热法（DSC）、扫描电镜（SEM）、傅里叶红外光谱（FTIR）、粉末X 射线衍射（XRPD）等技术手段对其表征,并考察其溶出度。结果：Soluplus和PVP VA64复合载体比例为3∶2,药物与载体比例为1∶7,制备固体分散体,在45 min时累积溶出度为92.43%,DSC、SEM、XRPD、FTIR等表征结果显示药物以无定形状态存在于固体分散体中,且药物与载体之间存在氢键相互作用。结论：Soluplus和PVP VA64作为复合载体材料,联合应用可显著提高齐墩果酸的体外溶出度。     

托伐普坦固体分散体的制备及体外溶出特性考察

目的 采用固体分散技术提高难溶性药物托伐普坦的体外溶出度。方法 选用聚维酮K_29/32为载体材料,以溶剂蒸发法制备托伐普坦固体分散体。采用差示扫描量热法(DSC)、X-射线粉末衍射法(XRPD)对所得固体分散体进行鉴定, 并进行溶解度、体外溶出实验。结果 固体分散体的DSC 图谱及X-射线粉末衍射确定了托伐普坦以无定形态分散在载体中, 体外溶解实验表明其溶出较原料药、物理混合物均有明显提高。结论 将托伐普坦与PVP K_29/32制成固体分散体,其分散状态发生了改变,溶出性能明显提高。     

卡维地洛-PVPVA64固体分散体的制备与表征

目地：制备卡维地洛的固体分散体,提高其在水中的溶解度和溶出度。方法：以乙烯基吡咯烷酮／醋酸乙烯共聚物（PVPVA64）为载体,无水乙醇为溶剂,制备卡维地洛固体分散体,并通过差示扫描量热法、x-射线粉末衍射法、红外分光光度法、原子力显微镜扫描、溶解度测定、溶出度实验及稳定性试验对固体分散体进行表征。结果：差示扫描量热法、x-射线粉末衍射法以及原子力显微镜扫描的谱图和图像分析表明卡维地洛以无定形状态存在于制得的固体分散体中,而傅里叶变换红外光谱分析则表明在固体分散体中卡维地洛与PVPVA64间可能以氢键结合形式存在。与卡维地洛原料药相比,该固体分散体的溶解度提高了80倍,且1h溶出百分率也从10％以下提高到95．5％。经差示扫描量热法、x-射线粉末衍射法及溶出度实验考察发现,在温度为40℃、相对湿度为75％的环境条件下,于90d内,该固体分散体稳定性良好。结论：卡维地洛与PVPVA64形成固体分散体后可显著提高其溶解度和溶出度,且热力学稳定,可进一步用于制备生物利用度更高的口服固体剂型。     

Physicochemical characterization of solid dispersions of three antiepileptic drugs prepared by solvent evaporation method

We have investigated the solid dispersion and dissolution profiles of three antiepileptic drugs (carbamazepine (CBZ), oxcarbazepine (OXC) and rufinamide (RFN)) with different aqueous solubilities, prepared by the solvent evaporation method. Solid dispersions of the three drugs in hydroxy-propylmethylcellulose (HPMC), with drug:polymer ratios of 1:4, were prepared and characterized by differential scanning calorimetry (DSC), Fourier transformation infrared (FTIR) spectroscopy, X-ray diffraction (XRD) and scanning electron microscopy. The release mechanism was also investigated and the kinetic order of the solid dispersions was evaluated. It appeared that the dissolution behaviour depended on the physicochemical properties of the drug and drug-polymer interactions. DSC thermographs showed amorphous forms for all drugs confirmed by XRD patterns. The FTIR spectra of CBZ and OXC demonstrated drug interactions with HPMC through hydrogen polymer bonds. Thus, solid dispersions of these drugs had an improved dissolution profile. In contrast, solid dispersions of RUF showed modest enhancement of dissolution, suggesting negligible drug-polymer interactions. The different dissolution behaviour is attributed to the extent of interactions between the polymer hydroxyl group and the drug amide groups.