首页> 外文期刊>Journal of Pharmaceutical and Biomedical Analysis: An International Journal on All Drug-Related Topics in Pharmaceutical, Biomedical and Clinical Analysis >Analytical and physicochemical characterisation of the senile cataract drug dipeptide beta-alanyl-L-histidine (carnosine)
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Analytical and physicochemical characterisation of the senile cataract drug dipeptide beta-alanyl-L-histidine (carnosine)

机译:老年性白内障药物二肽β-丙氨酰-L-组氨酸(肌肽)的分析和理化特性

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摘要

This study presents a simple but sensitive HPLC chromatographic method with a stability-indicating assay for determination and physicochemical characterisation of L-carnosine, a promising senile cataract prophylactic agent. Chromatographic analysis was conducted using a reverse phase (RP)-HPLC system and an isocratic mobile phase of 98% v/v trifluoroacetic acid (0.1% v/v) and 2% v/v acetonitrile with detection at 220 nm. L-carnosine was subjected to stress conditions to force its degradation using chemical and thermal agents and was subsequently detected from its degradation products using ESI-MS. The lipophilicity of the drug and 1:1 drug to phospholipid complex (PC) mol/mol was determined by estimating the partition coefficient (P). Lipophilicity was greatly enhanced when L-carnosine was formulated as a phospholipid complex using the solvent evaporation method. L-carnosine-phospholipid complex could be a promising approach for effective delivery to the human lens as offers a potential novel treatment for senile cataract. (C) 2015 Elsevier B.V. All rights reserved.
机译:这项研究提出了一种简单而灵敏的HPLC色谱方法,并带有用于指示L-肌肽(一种有望的老年性白内障预防剂)的理化特性的稳定性指示测定法。使用反相(RP)-HPLC系统和98%v / v三氟乙酸(0.1%v / v)和2%v / v乙腈的等度流动相进行色谱分析,检测波长为220 nm。 L-肌肽在压力条件下使用化学和热试剂使其降解,随后使用ESI-MS从其降解产物中检测出来。通过估计分配系数(P),确定药物和1:1药物对磷脂复合物(PC)mol / mol的亲脂性。当使用溶剂蒸发法将L-肌肽配制成磷脂络合物时,亲脂性大大提高。 L-肌肽-磷脂复合物可能是一种有希望的有效递送至人晶状体的方法,因为它为老年性白内障提供了一种潜在的新型治疗方法。 (C)2015 Elsevier B.V.保留所有权利。

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