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Formulation of immediate release pellets containing famotidine solid dispersions

机译:配制含有法莫替丁固体分散体的速释小丸

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Famotidine (FM) is a potent H2-receptor antagonist used for the treatment of peptic ulcer. It has a low and variable bioavailability which is attributed to its low water solubility. In this study, the dissolution of the drug was enhanced by a preparation of solid dispersion using two hydrophilic carriers, namely Gelucire 50/13 and Pluronic F-127. The prepared solid dispersions were characterized by differential scanning calorimetry (DSC), which indicated that there were no signs of interaction of the drug with the carriers used in the case of solid dispersions containing higher polymeric contents (1:3 and 1:5). FM solid dispersions in the matrices of Gelucire 50/13 and Pluronic F-127 (1:3) were used to prepare pellets. The scanning electron microscope (SEM) images of pellets showed that the pellets have spherical shape and their size depends on the carrier used. The dissolution of the drug from either solid dispersion or pellets was performed. The dissolution study depicted that, the presence of the drug in solid dispersion enhanced its dissolution in comparison with the drug itself. Also, the drug release from the manufactured pellets was found to be improved in the case of solid dispersions (drug:carrier 1:3). A complete drug release occurred after 30min from pellets containing solid dispersions, while only about 30% of the loaded FM was released from pellets containing untreated drug after 2h.
机译:法莫替丁(FM)是一种有效的H2受体拮抗剂,用于治疗消化性溃疡。它具有低而可变的生物利用度,这归因于其低水溶性。在这项研究中,通过使用两种亲水性载体(即Gelucire 50/13和Pluronic F-127)制备固体分散体,可以提高药物的溶解度。通过差示扫描量热法(DSC)对制得的固体分散体进行表征,这表明在含有较高聚合物含量(1:3和1:5)的固体分散体的情况下,药物与所用载体没有相互作用的迹象。使用Gelucire 50/13和Pluronic F-127(1:3)基质中的FM固体分散体制备颗粒。粒料的扫描电子显微镜(SEM)图像显示粒料为球形,其大小取决于所用载体。从固体分散体或小丸中溶解药物。溶出度研究表明,药物在固体分散体中的存在与药物本身相比提高了其溶出度。另外,在固体分散体的情况下(药物:载体1∶3),发现从制造的丸粒中释放的药物得到改善。 30分钟后,从含有固体分散体的药丸中完全释放出药物,而2小时后,只有约30%的负载FM从未经处理的药丸中释放出来。

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