{"title":"利托那韦的溶解度增强:共结晶","authors":"N. Sagar, A. Rahul, N. Rajani","doi":"10.35248/2153-2435.20.11.621","DOIUrl":null,"url":null,"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.","PeriodicalId":19833,"journal":{"name":"Pharmaceutica Analytica Acta","volume":"29 1","pages":"1-7"},"PeriodicalIF":0.0000,"publicationDate":"2020-01-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"2","resultStr":"{\"title\":\"Solubility Enhancement of Ritonavir: Co-Crystallization\",\"authors\":\"N. Sagar, A. Rahul, N. Rajani\",\"doi\":\"10.35248/2153-2435.20.11.621\",\"DOIUrl\":null,\"url\":null,\"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.\",\"PeriodicalId\":19833,\"journal\":{\"name\":\"Pharmaceutica Analytica Acta\",\"volume\":\"29 1\",\"pages\":\"1-7\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2020-01-01\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"2\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pharmaceutica Analytica Acta\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.35248/2153-2435.20.11.621\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmaceutica Analytica Acta","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.35248/2153-2435.20.11.621","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Solubility Enhancement of Ritonavir: Co-Crystallization
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.
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