Solubility Enhancement of Ritonavir: Co-Crystallization

N. Sagar, A. Rahul, N. Rajani
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引用次数: 2

Abstract

The main objective of this work is to explore co-crystallization approach for increasing solubility of an antiretroviral drug, Ritonavir (RTN). In this study, different co-formers with different functional groups like carboxylic acid andacid amidewere tried in ratio of 1:1, 1:2 and 1:3 (RTN:Co-former) using neat grinding method. Co-formers used were citric acid (CIT) and adipic acid (ADP). The co-crystals formed were characterized by melting point determination, Fourier-transform infrared (FTIR), differential scanning calorimetry (DSC), X-ray diffraction (XRD) and solubility studies. Co-crystals of drug with CIT and ADP showed the improved dissolution profile when compared to the pure RTN. Melting point, DSC, FTIR spectra of co-crystals were different than pure drug and co-formers indicating their interaction. XRD patterns of co-crystals were not completely amorphous but less intense compared to drug alone.
利托那韦的溶解度增强:共结晶
这项工作的主要目的是探索提高抗逆转录病毒药物利托那韦(RTN)溶解度的共结晶方法。本研究采用精磨法,分别以1:1、1:2、1:3的比例(RTN:共成物)对羧酸、酸酰胺等不同官能团的不同共成物进行了实验。共成体为柠檬酸(CIT)和己二酸(ADP)。通过熔点测定、傅里叶变换红外(FTIR)、差示扫描量热法(DSC)、x射线衍射(XRD)和溶解度研究对所形成的共晶进行了表征。与纯RTN相比,与CIT和ADP共晶的药物溶出曲线有所改善。共晶的熔点、DSC和FTIR光谱与纯药物和共晶不同,表明它们之间存在相互作用。共晶的XRD模式并非完全无定形,但与单独药物相比强度较小。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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