{"title":"Oxaliplatin-flavone pharmaceutical co-crystal-CN111205332A: patent spotlight.","authors":"Ritu Rathi, Renu Kushwaha, Ayushi Goyal, Inderbir Singh","doi":"10.4155/ppa-2022-0011","DOIUrl":null,"url":null,"abstract":"<p><p>Co-crystallization is a technique for modifying physicochemical properties of pharmaceutical ingredients with an aim to enhance the therapeutic efficacy and subsequent reduction in toxicity. The patent describes the development of oxaliplatin co-crystals using flavonoids (baicalein and naringenin) via solvent volatilization technique with an objective to improve solubility and stability in GI tract and reduced side/toxic effects. The co-crystals were characterized via differential scanning calorimetry, thermogravimetric analysis, x-ray diffraction analysis. The co-crystals exhibited slow drug release, delayed hydrolysis, low cytotoxicity and enhanced therapeutic activity on human gastric adenocarcinoma cells. However, suitable solvent for co-crystal production, large scale production and regulatory challenges for continuous manufacturing of co-crystals must be addressed.</p>","PeriodicalId":20011,"journal":{"name":"Pharmaceutical patent analyst","volume":null,"pages":null},"PeriodicalIF":1.8000,"publicationDate":"2022-09-01","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":null,"platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmaceutical patent analyst","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.4155/ppa-2022-0011","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"2022/9/2 0:00:00","PubModel":"Epub","JCR":"Q3","JCRName":"PHARMACOLOGY & PHARMACY","Score":null,"Total":0}
引用次数: 0
Abstract
Co-crystallization is a technique for modifying physicochemical properties of pharmaceutical ingredients with an aim to enhance the therapeutic efficacy and subsequent reduction in toxicity. The patent describes the development of oxaliplatin co-crystals using flavonoids (baicalein and naringenin) via solvent volatilization technique with an objective to improve solubility and stability in GI tract and reduced side/toxic effects. The co-crystals were characterized via differential scanning calorimetry, thermogravimetric analysis, x-ray diffraction analysis. The co-crystals exhibited slow drug release, delayed hydrolysis, low cytotoxicity and enhanced therapeutic activity on human gastric adenocarcinoma cells. However, suitable solvent for co-crystal production, large scale production and regulatory challenges for continuous manufacturing of co-crystals must be addressed.