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首页> 外文期刊>International Journal of Pharmaceutics >Aspartame as a co-former in co-amorphous systems
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Aspartame as a co-former in co-amorphous systems

机译：阿斯巴甜作为共创公司的共创公司

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摘要

Co-amorphous drug delivery systems are a promising approach to improve the dissolution rate and therefore potentially the oral bioavailability of poorly-water soluble drugs. Several low molecular weight excipients, for instance amino acids, have previously been shown to stabilize the amorphous form and increase the dissolution rate of drugs. In this study, the feasibility of aspartame, a methyl ester of the aspartic acid-phenylalanine dipeptide, as a co-former was investigated and compared with the respective single amino acids, both alone and in combination. The poorly water-soluble compounds mebendazole, tadalafil and piroxicam were chosen as model drugs. In contrast to the single amino acids or the physical mixture of both, all drug-aspartame mixtures became amorphous upon 90?min of ball milling. Only a single glass transition temperature (Tg) was detected by modulated differential scanning calorimetry, which indicates that a homogeneous single-phase co-amorphous system was obtained. Powder dissolution tests showed that the dissolution rates of the drugs from drug-aspartame co-amorphous samples were increased compared to crystalline drugs. Furthermore, supersaturation was observed for the mebendazole-aspartame and tadalafil-aspartame co-amorphous systems. In conclusion, aspartame has been shown to be a promising co-former in co-amorphous systems, superior to the single amino acids or their mixtures.
机译：钴基非晶药物输送系统是提高溶出速率有前途的方法，因此可能难溶水溶性药物口服生物利用度。几个低分子量的赋形剂，例如氨基酸，先前已被证明以稳定无定形形式和增加药物的溶出速率。在这项研究中，阿司帕坦的可行性，天冬氨酸 - 苯丙氨酸二肽的甲酯，作为助前进行了研究，并与相应的单个氨基酸，无论是单独和组合进行比较。该水难溶性化合物甲苯达唑，他达拉非和吡罗昔康被选为模型药物。与此相反的单个氨基酸或这两者的物理混合物，所有药物阿司帕坦的混合物在90成为无定形的？球磨分钟。只有单一的玻璃化转变温度（Tg）是通过调制式差示扫描量热，这表明得到均匀的单相共 - 无定形系统检测。粉溶解试验表明，药物阿斯巴甜钴基非晶样品药物的溶出速率相比晶毒品总量增加了。此外，观察到的甲苯咪唑，阿斯巴甜和他达拉非，阿司帕坦共 - 无定形系统过饱和。总之，天冬甜素已被证明是有前途的共同前在共 - 无定形的系统，优于单一氨基酸或它们的混合物。

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