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https://hdl.handle.net/10316/105341
Título: | Multiparticulate Systems of Ezetimibe Micellar System and Atorvastatin Solid Dispersion Efficacy of Low-Dose Ezetimibe/Atorvastatin on High-Fat Diet-Induced Hyperlipidemia and Hepatic Steatosis in Diabetic Rats | Autor: | Torrado-Salmerón, Carlos Guarnizo-Herrero, Víctor Henriques, Joana Seiça, Raquel Sena, Cristina M. Torrado-Santiago, Santiago |
Palavras-chave: | ezetimibe; atorvastatin; solid dispersion; micellar system; hyperlipidemia; liver steatosis | Data: | 20-Mar-2021 | Editora: | MDPI | Projeto: | PTDC/BIM-MET/4447/2014 POCI-01-0145-FEDER-016784 Ministerio de Ciencia e Innovación [MICINU, ref. RTI2018-093940-B-100] UCM [Research Group 910939] Rafael Folch Foundation |
Título da revista, periódico, livro ou evento: | Pharmaceutics | Volume: | 13 | Número: | 3 | Resumo: | The aim of this study was to develop multiparticulate systems with a combination of ezetimibe micellar systems and atorvastatin solid dispersions using croscarmellose as a hydrophilic vehicle and Kolliphor RH40 as a surfactant. The presence of a surfactant with low hydrophilic polymer ratios produces the rapid dissolution of ezetimibe through a drug-polymer interaction that reduces its crystallinity. The solid dispersion of atorvastatin with low proportions of croscarmellose showed drug-polymer interactions sufficient to produce the fast dissolution of atorvastatin. Efficacy studies were performed in diabetic Goto-Kakizaki rats with induced hyperlipidemia. The administration of multiparticulate systems of ezetimibe and atorvastatin at low (2 and 6.7 mg/kg) and high (3 and 10 mg/kg) doses showed similar improvements in levels of cholesterol, triglycerides, lipoproteins, alanine transaminase, and aspartate transaminase compared to the high-fat diet group. Multiparticulate systems at low doses (2 and 6.7 mg/kg of ezetimibe and atorvastatin) had a similar improvement in hepatic steatosis compared to the administration of ezetimibe and atorvastatin raw materials at high doses (3 and 10 mg/kg). These results confirm the effectiveness of solid dispersions with low doses of ezetimibe and atorvastatin to reduce high lipid levels and hepatic steatosis in diabetic rats fed a high-fat diet. | URI: | https://hdl.handle.net/10316/105341 | ISSN: | 1999-4923 | DOI: | 10.3390/pharmaceutics13030421 | Direitos: | openAccess |
Aparece nas coleções: | FMUC Medicina - Artigos em Revistas Internacionais I&D ICBR - Artigos em Revistas Internacionais |
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