Santosh Girani, Shidallingapa Zalki, Mahantesh G. Kavatekar, Ajay S. Shahapur, Vitthal K. Vijapure
{"title":"二代COX-II抑制剂溶解度增强三元体系的开发与表征","authors":"Santosh Girani, Shidallingapa Zalki, Mahantesh G. Kavatekar, Ajay S. Shahapur, Vitthal K. Vijapure","doi":"10.21746/IJBIO.2016.12.0010","DOIUrl":null,"url":null,"abstract":"Etoricoxib is a highly selective COX-II inhibitor, used to treat pains of different etiologies. Etoricoxib has low aqueous solubility (201 µ g/ml) and high permeability and therefore classified as BCS class II drug. By formulating these drugs with cyclodextrins as inclusion complexes have shown to increase the bioavailability. Cyclodextrins when used as complexing agents, enhance the solubility of poor water soluble lipophilic drugs. The objective of the present work is to formulate Etoricoxib cyclodextrin complexes by using ternary systems as Citric acid, Tartaric acid and PVP K-30 in order to enhance solubility and evaluate the enhanced solubility by in-vitro dissolution.","PeriodicalId":13765,"journal":{"name":"International Journal of Bioassays","volume":"107 1","pages":"5163-5173"},"PeriodicalIF":0.0000,"publicationDate":"2016-11-30","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"3","resultStr":"{\"title\":\"Development and characterization of ternary system for solubility enhancement of a second-generation COX-II inhibitor\",\"authors\":\"Santosh Girani, Shidallingapa Zalki, Mahantesh G. Kavatekar, Ajay S. Shahapur, Vitthal K. Vijapure\",\"doi\":\"10.21746/IJBIO.2016.12.0010\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Etoricoxib is a highly selective COX-II inhibitor, used to treat pains of different etiologies. Etoricoxib has low aqueous solubility (201 µ g/ml) and high permeability and therefore classified as BCS class II drug. By formulating these drugs with cyclodextrins as inclusion complexes have shown to increase the bioavailability. Cyclodextrins when used as complexing agents, enhance the solubility of poor water soluble lipophilic drugs. The objective of the present work is to formulate Etoricoxib cyclodextrin complexes by using ternary systems as Citric acid, Tartaric acid and PVP K-30 in order to enhance solubility and evaluate the enhanced solubility by in-vitro dissolution.\",\"PeriodicalId\":13765,\"journal\":{\"name\":\"International Journal of Bioassays\",\"volume\":\"107 1\",\"pages\":\"5163-5173\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2016-11-30\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"3\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"International Journal of Bioassays\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.21746/IJBIO.2016.12.0010\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"International Journal of Bioassays","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.21746/IJBIO.2016.12.0010","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Development and characterization of ternary system for solubility enhancement of a second-generation COX-II inhibitor
Etoricoxib is a highly selective COX-II inhibitor, used to treat pains of different etiologies. Etoricoxib has low aqueous solubility (201 µ g/ml) and high permeability and therefore classified as BCS class II drug. By formulating these drugs with cyclodextrins as inclusion complexes have shown to increase the bioavailability. Cyclodextrins when used as complexing agents, enhance the solubility of poor water soluble lipophilic drugs. The objective of the present work is to formulate Etoricoxib cyclodextrin complexes by using ternary systems as Citric acid, Tartaric acid and PVP K-30 in order to enhance solubility and evaluate the enhanced solubility by in-vitro dissolution.