title: Sodium alginate as a potential carrier in solid dispersion formulations to enhance dissolution rate and apparent water solubility of BCS II drugs.
abstract: 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.
authors.affiliation: Programa de Pós-Graduação em Farmácia, Universidade Federal de Santa Catarina, Campus Trindade, 88040-970 Florianópolis, SC, Brazil.
authors.forename: Paola Aline Amarante
authors.initials: PAA
authors.lastname: Borba
authors.affiliation: Programa de Pós-Graduação em Farmácia, Universidade Federal de Santa Catarina, Campus Trindade, 88040-970 Florianópolis, SC, Brazil.
authors.forename: Marihá
authors.initials: M
authors.lastname: Pinotti
authors.affiliation: Departamento de Física, Universidade Federal de Santa Catarina, Campus Trindade, 88040-970 Florianópolis, SC, Brazil.
authors.forename: Carlos Eduardo Maduro
authors.initials: CEM
authors.lastname: de Campos
authors.affiliation: Departamento de Farmácia, Universidade da Região de Joinville, 89219-710 Joinville, SC, Brazil.
authors.forename: Bianca Ramos
authors.initials: BR
authors.lastname: Pezzini
authors.affiliation: Programa de Pós-Graduação em Farmácia, Universidade Federal de Santa Catarina, Campus Trindade, 88040-970 Florianópolis, SC, Brazil. Electronic address: hellen.stulzer@gmail.com.
authors.forename: Hellen Karine
authors.initials: HK
authors.lastname: Stulzer
mesh_terms: D000464:Alginates / Q000737:chemistry*; D001562:Benzimidazoles / Q000737:chemistry*; D001565:Benzoates / Q000737:chemistry*; D002152:Calorimetry, Differential Scanning; D004337:Drug Carriers / Q000737:chemistry*; D020723:Glucuronic Acid / Q000737:chemistry; D006603:Hexuronic Acids / Q000737:chemistry; D010316:Particle Size; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D000077333:Telmisartan
chemical_list: D000464:Alginates; D001562:Benzimidazoles; D001565:Benzoates; D004337:Drug Carriers; D006603:Hexuronic Acids; D020723:Glucuronic Acid; D000077333:Telmisartan
keywords: Mechanical grinding process; Sodium alginate; Solid dispersions; Telmisartan