Synthesis of cocrystals of sulfonyl urea class drug using suitable coformers for enhancement of aqueous solubility  

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作  者:Santosh S. Chhajed Yatish R. Rajderkar Anjali B. Tajanpure Jayprakash B. Ugale Sanjay J. Kshirsagar 

机构地区:[1]Department Of Pharmaceutical Chemistry, Bhujbal Knowledge City, Met’s Institute Of Pharmacy, Nashik, Maharashtra, India [2]Department Of Pharmacology, Bhujbal Knowledge City, Met’s Institute Of Pharmacy, Nashik, Maharashtra, India [3]Department Of Pharmaceutics, Bhujbal Knowledge City, Met’s Institute Of Pharmacy, Nashik, Maharashtra, India

出  处:《Journal of Pharmaceutical and Biopharmaceutical Research》2019年第2期61-69,共9页制药与生物制药研究杂志(英文)

摘  要:The pharmaceutical cocrystals and its engineering is widely accepted phenomenon regarding to the enhancement of aqueous solubility of poorly soluble drugs. The pharmaceutical cocrystals have the great ability to improve the physicochemical properties of drug substance. Cocrystals are formed by the stoichiometric combination of drug substance and the coformer. The drug glimepiride is a third generation oral hypoglycemic sulfonylurea class. Glimepiride is a drug which is get classified as biopharmaceutical classification system (BCS) class II which indicates the glimepiride having low aqueous solubility and high permeability. Cocrystal engineering is a perfect way to increases glimepiride solubility without changing its therapeutic property. The cocrystals were synthesized by the solvent drop grinding as a green chemistry approach. The coformers used to form the cocrystals are succinic acid (SA), Theobromine (TB), caffeine (CF). The synthesized cocrystals are get characterized by vibrational spectroscopy, thermal analysis, molecular crystallography, and optical microscopy. The obtained results shows the formation of cocrystal phase between the drug glimepiride and its coformers.

关 键 词:COCRYSTALS COCRYSTAL engineering BIOPHARMACEUTICAL classification system green CHEMISTRY 

分 类 号:R[医药卫生]

 

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