Sodium alginate as a potential carrier in solid dispersion formulations to enhance dissolution rate and apparent water solubility of BCS II drugs.

Autor: Borba PAA; Programa de Pós-Graduação em Farmácia, Universidade Federal de Santa Catarina, Campus Trindade, 88040-970 Florianópolis, SC, Brazil., Pinotti M; Programa de Pós-Graduação em Farmácia, Universidade Federal de Santa Catarina, Campus Trindade, 88040-970 Florianópolis, SC, Brazil., de Campos CEM; Departamento de Física, Universidade Federal de Santa Catarina, Campus Trindade, 88040-970 Florianópolis, SC, Brazil., Pezzini BR; Departamento de Farmácia, Universidade da Região de Joinville, 89219-710 Joinville, SC, Brazil., Stulzer HK; Programa de Pós-Graduação em Farmácia, Universidade Federal de Santa Catarina, Campus Trindade, 88040-970 Florianópolis, SC, Brazil. Electronic address: hellen.stulzer@gmail.com.
Jazyk: angličtina
Zdroj: Carbohydrate polymers [Carbohydr Polym] 2016 Feb 10; Vol. 137, pp. 350-359. Date of Electronic Publication: 2015 Oct 23.
DOI: 10.1016/j.carbpol.2015.10.070
Abstrakt: The solid dispersion technique is the most effective method for improving the dissolution rate of poorly water-soluble drugs, however it depends on a suitable carrier selection. The work explored the use of the biopolymer sodium alginate (SA) as a potential carrier in solid dispersions (SD). The data demonstrated that SA was able to improve the biopharmaceutical properties of the BCS II drug telmisartan (TEL) of low solubility even using relative small drug:polymer ratio. A solid state grinding process was used to prepare the solid dispersions (SD) during 45 min. The SD were prepared in different proportions of drug and carrier of 1:1, 1:3, 1:5, 1:7 and 1:9 (mass/mass). DSC, XRPD, FTIR and Raman confirmed the presence of molecular interactions between TEL and the carrier. FTIR supports the presence of hydrogen bonds between TEL and the carrier. SD_1:5, SD_1:7 and SD_1:9 enhanced the dissolution rate of the drug releasing more than 80% of the drug in just 30 min (83%, 84% and 87%). The the t-test results demonstrated equal dissolution efficiency values for SD_1:7 and Micardis(®), however the similarity (f2) and difference (f1) fit factors showed that the SD and Micardis(®) are statistically different. The physical stability studies demonstrated that SD using sodium alginate as a carrier remained unchanged during the period of 90 days at room temperature, showing that the sodium alginate acts as a good anti plasticizer agent, preventing the drug recrystallization.
(Copyright © 2015 Elsevier Ltd. All rights reserved.)
Databáze: MEDLINE
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