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Correlation of Solubility Thermodynamics of Glibenclamide with Recrystallization and In Vitro Release Profile.
Maharjan, Ravi; Jeong, Junoh; Bhujel, Ripesh; Kim, Min-Soo; Han, Hyo-Kyung; Kim, Nam Ah; Jeong, Seong Hoon.
Afiliação
  • Maharjan R; BK21 FOUR Team, Integrated Research Institute for Drug Development, College of Pharmacy, Dongguk University, Gyeonggi 10326, Korea.
  • Jeong J; BK21 FOUR Team, Integrated Research Institute for Drug Development, College of Pharmacy, Dongguk University, Gyeonggi 10326, Korea.
  • Bhujel R; BK21 FOUR Team, Integrated Research Institute for Drug Development, College of Pharmacy, Dongguk University, Gyeonggi 10326, Korea.
  • Kim MS; College of Pharmacy, Research Institute for Drug Development, Pusan National University, Busan 46241, Korea.
  • Han HK; BK21 FOUR Team, Integrated Research Institute for Drug Development, College of Pharmacy, Dongguk University, Gyeonggi 10326, Korea.
  • Kim NA; BK21 FOUR Team, Integrated Research Institute for Drug Development, College of Pharmacy, Dongguk University, Gyeonggi 10326, Korea.
  • Jeong SH; BK21 FOUR Team, Integrated Research Institute for Drug Development, College of Pharmacy, Dongguk University, Gyeonggi 10326, Korea.
Molecules ; 27(4)2022 Feb 18.
Article em En | MEDLINE | ID: mdl-35209181
The solubility of glibenclamide was evaluated in DMSO, NMP, 1,4-dioxane, PEG 400, Transcutol® HP, water, and aqueous mixtures (T = 293.15~323.15 K). It was then recrystallized to solvate and compressed into tablets, of which 30-day stability and dissolution was studied. It had a higher solubility in 1,4-dioxane, DMSO, NMP (Xexp = 2.30 × 103, 3.08 × 104, 2.90 × 104) at 323.15 K, its mixture (Xexp = 1.93 × 103, 1.89 × 104, 1.58 × 104) at 298.15 K, and 1,4-dioxane (w) + water (1-w) mixture ratio of w = 0.8 (Xexp = 3.74 × 103) at 323.15 K. Modified Apelblat (RMSD ≤ 0.519) and CNIBS/R-K model (RMSD ≤ 0.358) suggested good comparability with the experimental solubility. The minimum value of ΔG° vs ΔH° at 0.70 < x2 < 0.80 suggested higher solubility at that molar concentration. Based on the solubility, it was recrystallized into the solvate, which was granulated and compressed into tablets. Among the studied solvates, the tablets of glibenclamide dioxane solvate had a higher initial (95.51%) and 30-day (93.74%) dissolution compared to glibenclamide reference (28.93%). There was no stability issue even after granulation, drying, or at pH 7.4. Thus, glibenclamide dioxane solvate could be an alternative form to improve the molecule's properties.
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Texto completo: 1 Base de dados: MEDLINE Assunto principal: Termodinâmica / Glibureto / Liberação Controlada de Fármacos Idioma: En Ano de publicação: 2022 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Termodinâmica / Glibureto / Liberação Controlada de Fármacos Idioma: En Ano de publicação: 2022 Tipo de documento: Article