{"title":"阿托伐他汀分散自微乳化片的研制","authors":"K. Midha, M. Nagpal, G. Aggarwal, T. G. Singh","doi":"10.5530/PHM.2015.6.2","DOIUrl":null,"url":null,"abstract":"Aim: The aim of this study was to develop dispersible self-microemulsifying (SMEDDS) tablet of atorvastatin for promoting its solubility and thus its oral bioavailability. Materials and Methods: The liquid SMEDDS were prepared by water titration method using oil, surfactant and co-surfactant and converted into solid- SMEDDS (S-SMEDDS) by adsorption on solid carriers (Neusilin US2). The S-SMEDDS were blended with sodium starch glycolate (disintegrant) and tablet excipients and compressed into tablets that were dispersible and self-microemulsifying in nature. All these formulations were assessed for various physicochemical parameters viz. weight variation, hardness, friability, disintegration test. In vitro studies of pure drug, SMEDDS, S-SMEDDS and dispersible SME-tablets were carried out. Results: Pure drug released only 29.84 ± 0.16% upto 60 minutes and all the SMEDDS formulations (i.e. SMEDDS. S-SMEDDS and dispersible SME-tablets) released 100% of drug in comparatively lesser time. Formulations containing atorvastatin, 30% oleic acid, 65% tween 80 and 5% co-surfactant came out to show the best results in in vitro studies. But, FB1 (tablet) was considered to be the best since it released 100% drug in 35 min and also has advantages over SMEDDS and S-SMEDDS in terms of stability and patient compliance. Conclusion: The study revealed the potential use of dispersible SMEDDS tablet for the oral delivery of hydrophobic drugs, such as atorvastatin. Key words: Atorvastatin, Bioavailability, Phase diagram, SMEDDS.","PeriodicalId":19960,"journal":{"name":"Pharmaceutical Methods","volume":"635 1","pages":"9"},"PeriodicalIF":0.0000,"publicationDate":"2015-10-20","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"6","resultStr":"{\"title\":\"Development of Dispersible Self-microemulsifying Tablet of Atorvastatin\",\"authors\":\"K. Midha, M. Nagpal, G. Aggarwal, T. G. Singh\",\"doi\":\"10.5530/PHM.2015.6.2\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Aim: The aim of this study was to develop dispersible self-microemulsifying (SMEDDS) tablet of atorvastatin for promoting its solubility and thus its oral bioavailability. Materials and Methods: The liquid SMEDDS were prepared by water titration method using oil, surfactant and co-surfactant and converted into solid- SMEDDS (S-SMEDDS) by adsorption on solid carriers (Neusilin US2). The S-SMEDDS were blended with sodium starch glycolate (disintegrant) and tablet excipients and compressed into tablets that were dispersible and self-microemulsifying in nature. All these formulations were assessed for various physicochemical parameters viz. weight variation, hardness, friability, disintegration test. In vitro studies of pure drug, SMEDDS, S-SMEDDS and dispersible SME-tablets were carried out. Results: Pure drug released only 29.84 ± 0.16% upto 60 minutes and all the SMEDDS formulations (i.e. SMEDDS. S-SMEDDS and dispersible SME-tablets) released 100% of drug in comparatively lesser time. Formulations containing atorvastatin, 30% oleic acid, 65% tween 80 and 5% co-surfactant came out to show the best results in in vitro studies. But, FB1 (tablet) was considered to be the best since it released 100% drug in 35 min and also has advantages over SMEDDS and S-SMEDDS in terms of stability and patient compliance. Conclusion: The study revealed the potential use of dispersible SMEDDS tablet for the oral delivery of hydrophobic drugs, such as atorvastatin. Key words: Atorvastatin, Bioavailability, Phase diagram, SMEDDS.\",\"PeriodicalId\":19960,\"journal\":{\"name\":\"Pharmaceutical Methods\",\"volume\":\"635 1\",\"pages\":\"9\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2015-10-20\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"6\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Pharmaceutical Methods\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.5530/PHM.2015.6.2\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Pharmaceutical Methods","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.5530/PHM.2015.6.2","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
Development of Dispersible Self-microemulsifying Tablet of Atorvastatin
Aim: The aim of this study was to develop dispersible self-microemulsifying (SMEDDS) tablet of atorvastatin for promoting its solubility and thus its oral bioavailability. Materials and Methods: The liquid SMEDDS were prepared by water titration method using oil, surfactant and co-surfactant and converted into solid- SMEDDS (S-SMEDDS) by adsorption on solid carriers (Neusilin US2). The S-SMEDDS were blended with sodium starch glycolate (disintegrant) and tablet excipients and compressed into tablets that were dispersible and self-microemulsifying in nature. All these formulations were assessed for various physicochemical parameters viz. weight variation, hardness, friability, disintegration test. In vitro studies of pure drug, SMEDDS, S-SMEDDS and dispersible SME-tablets were carried out. Results: Pure drug released only 29.84 ± 0.16% upto 60 minutes and all the SMEDDS formulations (i.e. SMEDDS. S-SMEDDS and dispersible SME-tablets) released 100% of drug in comparatively lesser time. Formulations containing atorvastatin, 30% oleic acid, 65% tween 80 and 5% co-surfactant came out to show the best results in in vitro studies. But, FB1 (tablet) was considered to be the best since it released 100% drug in 35 min and also has advantages over SMEDDS and S-SMEDDS in terms of stability and patient compliance. Conclusion: The study revealed the potential use of dispersible SMEDDS tablet for the oral delivery of hydrophobic drugs, such as atorvastatin. Key words: Atorvastatin, Bioavailability, Phase diagram, SMEDDS.