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首页> 美国卫生研究院文献>International Journal of Pharmaceutics: X >Physical stability and release properties of lumefantrine amorphous solid dispersion granules prepared by a simple solvent evaporation approach
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Physical stability and release properties of lumefantrine amorphous solid dispersion granules prepared by a simple solvent evaporation approach

机译：通过简单的溶剂蒸发方法制备Lumefantrine非晶固体分散颗粒的物理稳定性和释放性能

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摘要

Amorphous solid dispersions (ASDs) of lumefantrine, which has low aqueous solubility, have been shown to improve bioavailability relative to crystalline formulations. Herein, the crystallization tendency and release properties of a variety of lumefantrine ASD granules, formed on a blend of microcrystalline cellulose and anhydrous lactose, prepared using a simple solvent evaporation method, were evaluated. Several polymers, a majority of which contained acidic moieties, and different drug loadings were assessed. Crystallinity as a function of time following exposure to stress storage conditions of 40 °C and 75% relative humidity was monitored for the various dispersions. Release testing was performed and ASD characteristics were further evaluated using infrared and X-ray photoelectron spectroscopy (XPS). A large difference in stability to crystallization was observed between the various ASDs, most notably depending on polymer chemistry. This could be largely rationalized based on the extent of drug-polymer interactions, specifically the degree of lumefantrine-polymer salt formation, which could be readily assessed with XPS spectroscopy. Lumefantrine release from the ASDs also varied considerably, whereby the best polymer for promoting physical stability did not lead to the highest extent of drug release. Several formulations led to concentrations above the amorphous solubility of lumefantrine, with the formation of nano-sized drug-rich aggregates. A balance between the ability of a given polymer to promote physical stability and drug release may need to be sought.
机译：已经显示出具有低水溶性的Lumefantrine的无定形固体分散体（ASDS），以改善相对于结晶制剂的生物利用度。在此，评估了使用简单溶剂蒸发方法制备的微晶纤维素和无水乳糖的混合物上形成的各种Lumefantrine ASD颗粒的结晶趋势和脱模性。几种聚合物，其中大部分含有酸性部分和不同的药物载体。对于暴露于40℃和75％相对湿度的暴露后的时间后，结晶度被监测到各种分散体。进行释放测试，并使用红外和X射线光电子光谱（XPS）进一步评估ASD特性。在各种ASD之间观察到稳定性的稳定性差异，最值得注意的是，根据聚合物化学。这可以基于药物 - 聚合物相互作用的程度，特别是Lumefantrine - 聚合物盐形成的程度来大大合理地，可以用XPS光谱分辨地评估。从ASDS的Lumefantrine释放也很大差异，从而最佳用于促进物理稳定性的聚合物不会导致药物释放的最高程度。几种制剂导致Lumefantrine的无定形溶解度高于Lumefantrine的浓度，形成纳米尺寸的富含药物的聚集体。可能需要寻求给定聚合物的能力之间的平衡。可能需要寻求促进物理稳定性和药物释放的能力。

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