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首页> 外文期刊>Journal of drug delivery science and technology >Preparation and characterization of pyrimethamine solid dispersions and an evaluation of the physical nature of pyrimethamine in solid dispersions
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Preparation and characterization of pyrimethamine solid dispersions and an evaluation of the physical nature of pyrimethamine in solid dispersions

机译：吡米甲胺固体分散体的制备与表征及嘧啶嘧啶物理性质的评价

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摘要

The objective of this investigation was to prepare, characterize pyrimethamine solid dispersions formulated with different carriers and to evaluate the physical nature of pyrimethamine in solid dispersion. Pyrimethamine solid dispersions were prepared by solvent evaporation technique using a rotary evaporator and characterized using intrinsic dissolution studies, differential scanning calorimetry (DSC), x-ray diffractometry (XRD), fourier transform infrared spectroscopy (FTIR), dissolution studies, and stability studies of selected solid dispersion. To further investigate the nature of drug, nuclear magnetic resonance was also performed. Intrinsic dissolution studies demonstrate that the dissolution rate of pyrimethamine could be markedly improved via solid dispersion technique. DSC studies show that PEG 6000 and poloxamer 188 could dissolve pyrimethamine up to 50% (w/w) in molten state. Results of XRD and FTIR suggest the presence of a different polymorphic form of pyrimethamine which might be due to the disruption of the supramolecular ribbon (synthon) formation of the original pyrimethamine polymorph. Significant improvement in dissolution rate from pyrimethamine solid dispersion using poloxamer 188 was achieved and pyrimethamine/poloxamer 188 ratio at 1:3 showing maximum dissolution rate enhancement of pyrimethamine. Furthermore, stability studies indicate no significant change in the physical nature of pyrimethamine in selected solid dispersion up to 5-month.
机译：本研究的目的是制备、表征用不同载体配制的乙胺嘧啶固体分散体，并评估乙胺嘧啶在固体分散体中的物理性质。使用旋转蒸发器通过溶剂蒸发技术制备乙胺嘧啶固体分散体，并使用固有溶解研究、差示扫描量热法（DSC）、x射线衍射法（XRD）、傅里叶变换红外光谱（FTIR）、溶解研究和所选固体分散体的稳定性研究对其进行表征。为了进一步研究药物的性质，还进行了核磁共振。本征溶出度研究表明，通过固体分散技术可以显著提高乙胺嘧啶的溶出速率。DSC研究表明，PEG 6000和泊洛沙姆188在熔融状态下可溶解高达50%（w/w）的乙胺嘧啶。XRD和FTIR结果表明，乙胺嘧啶存在不同的多晶型，这可能是由于破坏了最初乙胺嘧啶多晶型的超分子带（合成子）形成。使用泊洛沙姆188可显著提高乙胺嘧啶固体分散体的溶解速率，且在1:3的比例下，乙胺嘧啶/泊洛沙姆188的溶解速率最大。此外，稳定性研究表明，在选定的固体分散体中，乙胺嘧啶的物理性质在5个月内没有显著变化。

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