{"title":"替米沙坦快溶片的制备及评价","authors":"A. Shatla, M. Osman","doi":"10.21608/APRH.2018.2848.1050","DOIUrl":null,"url":null,"abstract":"Objective: The aim of this work was to enhance the dissolution rate of telmisartan with the goal of developing fast disintegrating tablets (FDTs) with subsequent rapid dissolution for sublingual administration. Methods: Binary solid dispersion systems (SDS) were prepared by solvent evaporation technique for the drug with Gelucire 44/14 (formula A), polyethylene glycol 4000 (PEG4000) (formula B), Pluronic F68 (formula C), hydroxypropyl methylcellulose E5 (HPMC E5) (formula D), and finally by using sodium bicarbonate with the drug in (0.5: 1) ratio (formula E), and (1:1) ratio (formula F). These systems were evaluated for drug dissolution in addition to the physicochemical changes of the drug utilizing FTIR spectroscopy, thermal analysis, and X-ray diffraction. Results: The prepared formulations using sodium bicarbonate significantly enhanced the dissolution rate of the drug compared with those prepared using different types of polymers. The order of enhanced dissolution of the drug in the first 5 min Q5 (%) was: formula E > F > D5, where the % drug dissolved was 88.94 ± 1.31, 84.77 ± 1.1 and72.6 ± 0.81 (mean + SD) for each formula, respectively. Formula E was selected for the formulation of the rapidly dissolving tablet of telmisartan since it showed enhanced dissolution of the drug, more palatable taste in the buccal cavity, relatively inexpensive material and ease of processing compared with a solid dispersion prepared using polymer. Conclusion: Sodium bicarbonate can be utilized in the preparation of telmisartan FDT with fast dissolution rate. Conclusion: sodium bicarbonate can be utilized in the preparation of telmisartan FDT with fast dissolution rate.","PeriodicalId":15017,"journal":{"name":"Journal of Advanced Pharmacy Research","volume":"86 1","pages":""},"PeriodicalIF":0.0000,"publicationDate":"2018-06-12","publicationTypes":"Journal Article","fieldsOfStudy":null,"isOpenAccess":false,"openAccessPdf":"","citationCount":"0","resultStr":"{\"title\":\"PREPARATION AND EVALUATION OF RAPIDLY DISSOLVING TABLET OF TELMISARTAN\",\"authors\":\"A. Shatla, M. Osman\",\"doi\":\"10.21608/APRH.2018.2848.1050\",\"DOIUrl\":null,\"url\":null,\"abstract\":\"Objective: The aim of this work was to enhance the dissolution rate of telmisartan with the goal of developing fast disintegrating tablets (FDTs) with subsequent rapid dissolution for sublingual administration. Methods: Binary solid dispersion systems (SDS) were prepared by solvent evaporation technique for the drug with Gelucire 44/14 (formula A), polyethylene glycol 4000 (PEG4000) (formula B), Pluronic F68 (formula C), hydroxypropyl methylcellulose E5 (HPMC E5) (formula D), and finally by using sodium bicarbonate with the drug in (0.5: 1) ratio (formula E), and (1:1) ratio (formula F). These systems were evaluated for drug dissolution in addition to the physicochemical changes of the drug utilizing FTIR spectroscopy, thermal analysis, and X-ray diffraction. Results: The prepared formulations using sodium bicarbonate significantly enhanced the dissolution rate of the drug compared with those prepared using different types of polymers. The order of enhanced dissolution of the drug in the first 5 min Q5 (%) was: formula E > F > D5, where the % drug dissolved was 88.94 ± 1.31, 84.77 ± 1.1 and72.6 ± 0.81 (mean + SD) for each formula, respectively. Formula E was selected for the formulation of the rapidly dissolving tablet of telmisartan since it showed enhanced dissolution of the drug, more palatable taste in the buccal cavity, relatively inexpensive material and ease of processing compared with a solid dispersion prepared using polymer. Conclusion: Sodium bicarbonate can be utilized in the preparation of telmisartan FDT with fast dissolution rate. Conclusion: sodium bicarbonate can be utilized in the preparation of telmisartan FDT with fast dissolution rate.\",\"PeriodicalId\":15017,\"journal\":{\"name\":\"Journal of Advanced Pharmacy Research\",\"volume\":\"86 1\",\"pages\":\"\"},\"PeriodicalIF\":0.0000,\"publicationDate\":\"2018-06-12\",\"publicationTypes\":\"Journal Article\",\"fieldsOfStudy\":null,\"isOpenAccess\":false,\"openAccessPdf\":\"\",\"citationCount\":\"0\",\"resultStr\":null,\"platform\":\"Semanticscholar\",\"paperid\":null,\"PeriodicalName\":\"Journal of Advanced Pharmacy Research\",\"FirstCategoryId\":\"1085\",\"ListUrlMain\":\"https://doi.org/10.21608/APRH.2018.2848.1050\",\"RegionNum\":0,\"RegionCategory\":null,\"ArticlePicture\":[],\"TitleCN\":null,\"AbstractTextCN\":null,\"PMCID\":null,\"EPubDate\":\"\",\"PubModel\":\"\",\"JCR\":\"\",\"JCRName\":\"\",\"Score\":null,\"Total\":0}","platform":"Semanticscholar","paperid":null,"PeriodicalName":"Journal of Advanced Pharmacy Research","FirstCategoryId":"1085","ListUrlMain":"https://doi.org/10.21608/APRH.2018.2848.1050","RegionNum":0,"RegionCategory":null,"ArticlePicture":[],"TitleCN":null,"AbstractTextCN":null,"PMCID":null,"EPubDate":"","PubModel":"","JCR":"","JCRName":"","Score":null,"Total":0}
PREPARATION AND EVALUATION OF RAPIDLY DISSOLVING TABLET OF TELMISARTAN
Objective: The aim of this work was to enhance the dissolution rate of telmisartan with the goal of developing fast disintegrating tablets (FDTs) with subsequent rapid dissolution for sublingual administration. Methods: Binary solid dispersion systems (SDS) were prepared by solvent evaporation technique for the drug with Gelucire 44/14 (formula A), polyethylene glycol 4000 (PEG4000) (formula B), Pluronic F68 (formula C), hydroxypropyl methylcellulose E5 (HPMC E5) (formula D), and finally by using sodium bicarbonate with the drug in (0.5: 1) ratio (formula E), and (1:1) ratio (formula F). These systems were evaluated for drug dissolution in addition to the physicochemical changes of the drug utilizing FTIR spectroscopy, thermal analysis, and X-ray diffraction. Results: The prepared formulations using sodium bicarbonate significantly enhanced the dissolution rate of the drug compared with those prepared using different types of polymers. The order of enhanced dissolution of the drug in the first 5 min Q5 (%) was: formula E > F > D5, where the % drug dissolved was 88.94 ± 1.31, 84.77 ± 1.1 and72.6 ± 0.81 (mean + SD) for each formula, respectively. Formula E was selected for the formulation of the rapidly dissolving tablet of telmisartan since it showed enhanced dissolution of the drug, more palatable taste in the buccal cavity, relatively inexpensive material and ease of processing compared with a solid dispersion prepared using polymer. Conclusion: Sodium bicarbonate can be utilized in the preparation of telmisartan FDT with fast dissolution rate. Conclusion: sodium bicarbonate can be utilized in the preparation of telmisartan FDT with fast dissolution rate.