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首页> 外文期刊>Journal of drug research. >Formulation and Evaluation of Albendazole Solid-Dispersion
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Formulation and Evaluation of Albendazole Solid-Dispersion

机译：阿苯达唑固体分散体的配制与评价

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A solid-dispersion of the drug can be formulated using a polymer carrier to improve its solubility. Solid dispersions were prepared using different polymers {polyethylene glycol (PEG) 4000, 6000, 8000, polyvinylpyrrolidone K30 (PVP K30), hydroxypropylmethylcellulose (HPMC), hydroxypropyl-(3-cyclodextrm (HP(3CD), poloxamer (PXR) 188 and 407), with drug: polymer ratios (1:1, 1:2, 1:4) by the solvent evaporation as well as the spray drying techniques to improve dissolution rate of albendazole (ABZ). It was found that the dissolution rate of the drug was affected by both the polymer type and the ratio of ABZ to polymer. Spray drying technique showed enhanced dissolution compared to the solvent evaporation method. The highest dissolution of ABZ was obtained with HPfSCD followed by HPMC and PVP K30 in drug: polymer ratio 1:4, 1:4 and 1:2 respectively, prepared by the spray drying technique. Morphology and characteristics of albendazole alone as well as its microparticles from the spray drying technique with the highest dissolution results were studied and photographed. Smooth surface and spherical microparticles of ABZ were detected that indicates the possible coating of the drug crystals by the polymers. Physicochemical properties of the drug alone and its spray dried microparticles were investigated using Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and X-ray powder diffraction (PXRD). These investigations showed that ABZ transformed from the crystalline state to amorphous state by the spray drying using the polymers mentioned as confirmed by disappearance of its melting peak and the characteristic crystalline peaks. The transformation of ABZ from the crystalline to the amorphous state by the spray drying and the hydrophilic coating of drug particles by the polymers are considered among the factors that enhance the improvement of ABZ dissolution.
机译：可以使用聚合物载体配制药物的固体分散体以改善其溶解性。使用不同的聚合物{聚乙二醇（PEG）4000、6000、8000，聚乙烯吡咯烷酮K30（PVP K30），羟丙基甲基纤维素（HPMC），羟丙基-（3-环糊精（HP（3CD）），泊洛沙姆（PXR）188和407''制备固体分散体），通过溶剂蒸发以及喷雾干燥技术提高药物与聚合物的比例（1：1、1：2、1：4），以提高阿苯达唑（ABZ）的溶出度。药物受聚合物类型和ABZ与聚合物的比率的影响，喷雾干燥技术显示出比溶剂蒸发法更强的溶出度，HPfSCD，HPMC和PVP K30的ABZ溶出度最高：药物：聚合物比1分别用喷雾干燥技术制备了：4、1：4和1：2，研究并拍摄了阿苯达唑单独的形态和特性，以及用喷雾干燥技术获得的最高溶出度的微粒，并对其表面进行了照相。检测到ABZ的球形微粒，表明聚合物可能覆盖了药物晶体。使用傅里叶变换红外光谱（FTIR），差示扫描量热法（DSC）和X射线粉末衍射（PXRD）研究了药物本身及其喷雾干燥微粒的理化性质。这些研究表明，通过使用所述聚合物的喷雾干燥，ABZ从结晶态转变为非晶态，这由其熔融峰和特征结晶峰的消失证实。在增强ABZ溶解性改善的因素中，考虑了通过喷雾干燥使ABZ从结晶态转变为非晶态以及通过聚合物对药物颗粒进行亲水涂层。

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