高载药三元固体分散体对阿苯达唑溶出度的改善:配方及表征

S. Halder, M. Azad, Hrishik Iqbal, Madhabi Lata Shuma, E. Kabir
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引用次数: 0

摘要

水溶性差的药物,如广泛使用的驱虫药阿苯达唑(ABZ)的生物利用度很低,因此,为了获得最佳的治疗效果,需要提高这类药物的水溶性。本研究的目的是通过两种生物相容性的药物载体(Soluplus®和Ludiflash®),开发一种有效的ABZ高载药固体分散体(SD),以改善其物理化学特性。通过平衡溶解度研究选择了最佳配比,结果表明,与结晶ABZ相比,ABZ在水中的溶解度提高了50倍。SD-ABZ的x射线粉末衍射(XRPD)和差示扫描量热法(DSC)研究表明,SD中ABZ的结晶度降低。聚合物载体,特别是Soluplus®,被认为在降低ABZ的结晶度和分子多分散性中起关键作用。溶解研究表明,与结晶ABZ相比,SD-ABZ在水中的溶解改善,药物快速释放,随后逐渐溶解。然而,由于样品中ABZ晶体的高载药量和保留,其溶出行为不符合预期,可能需要进一步研究以优化SD-ABZ的处方。达卡大学药学院。科学通报20(2):149- 158,2021(12月)
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Improved Dissolution of Albendazole from High Drug Loaded Ternary Solid Dispersion: Formulation and Characterization
Bioavailability of a poorly water-soluble drug, e.g., widely used anthelmintic drug Albendazole (ABZ), is very low and thus, to obtain an optimized therapeutic efficacy, the aqueous solubility of such drugs needs to be enhanced. The objective of this study was to develop an effective high drug-loaded solid dispersion (SD) of ABZ with two biocompatible drug carriers, namely Soluplus® and Ludiflash® to improve its physicochemical characteristics. Equilibrium solubility study was performed to choose the optimum polymer ratio among the formulations and it showed up to 50-fold enhanced solubility compared to crystalline ABZ in water. X-Ray Powder Diffraction (XRPD) and Differential Scanning Calorimetry (DSC) studies of SD-ABZ showed reduced crystallinity of ABZ in the SD. The polymeric carriers, notably Soluplus®, are thought to play a key role in the reduction of crystallinity and molecular polydispersity of ABZ. The dissolution studies in water showed improved dissolution of SD-ABZ compared to crystalline ABZ, with a quick onset of drug release followed by gradual dissolution. However, due to high drug-loading and retention of crystalline ABZ in the sample, the dissolution behavior was not as expected, and may require further studies to optimize the SD-ABZ formulation. Dhaka Univ. J. Pharm. Sci. 20(2): 149-158, 2021 (December)
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