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Binary polymeric amorphous carvedilol solid dispersions: In vitro and in vivo characterization.
Krstic, Marko; Manic, Luka; Martic, Nikola; Vasiljevic, Dragana; Mracevic, Svetlana Dogo; Vukmirovic, Sasa; Raskovic, Aleksandar.
Afiliación
  • Krstic M; University of Belgrade - Faculty of Pharmacy, Department of Analytical Chemistry, Vojvode Stepe 450, 11221 Belgrade, Serbia. Electronic address: marko.krstic@pharmacy.bg.ac.rs.
  • Manic L; University of Belgrade - Faculty of Pharmacy, PhD student, Vojvode Stepe 450, 11221 Belgrade, Serbia.
  • Martic N; University of Novi Sad, Faculty of Medicine, Department of Pharmacology, Toxicology and Clinical Pharmacology, Hajduk Veljkova 3, 21000 Novi Sad, Serbia. Electronic address: nikola.martic@mf.uns.ac.rs.
  • Vasiljevic D; University of Belgrade - Faculty of Pharmacy, Department of Pharmaceutical Technology and Cosmetology, Vojvode Stepe 450, 11221 Belgrade, Serbia. Electronic address: vasilj@pharmacy.bg.ac.rs.
  • Mracevic SD; University of Belgrade - Faculty of Pharmacy, Department of Analytical Chemistry, Vojvode Stepe 450, 11221 Belgrade, Serbia. Electronic address: sdjogo@pharmacy.bg.ac.rs.
  • Vukmirovic S; University of Novi Sad, Faculty of Medicine, Department of Pharmacology, Toxicology and Clinical Pharmacology, Hajduk Veljkova 3, 21000 Novi Sad, Serbia. Electronic address: sasa.vukmirovic@mf.uns.ac.rs.
  • Raskovic A; University of Novi Sad, Faculty of Medicine, Department of Pharmacology, Toxicology and Clinical Pharmacology, Hajduk Veljkova 3, 21000 Novi Sad, Serbia. Electronic address: aleksandar.raskovic@mf.uns.ac.rs.
Eur J Pharm Sci ; 150: 105343, 2020 Jul 01.
Article en En | MEDLINE | ID: mdl-32376386
Binary polymeric amorphous carvedilol solid dispersions were prepared using solvent method by varying solvent type, polymer type and carvedilol to polymer ratio in order to assess the influence of these factors and maximize carvedilol dissolution rate. Low and high molecular weight polyvinylpyrrolidone, polyvinylpyrrolidone-vinyl acetate copolymer and polyvinyl caprolactam-polyvinyl acetate-polyethylene glycol graft copolymer were used as polymeric carriers in carvedilol to polymer ratios 1:1, 1:2 or 1:4, while absolute ethanol or acetone were used as solvents. Hard gelatin capsules were prepared with carvedilol solid dispersion and lactose monohydrate, mannitol or microcrystalline cellulose. FTIR and PXRD were used to detect carvedilol crystallinity and identify carvedilol-polymer interactions and carvedilol polymorphs. These techniques confirmed carvedilol transition to amorphous state and suggested that hydrogen bonds were formed between carvedilol and polymer molecules. Carvedilol dissolution rate was significantly higher from solid dispersions with higher carvedilol to polymer ratio and solid dispersions prepared using the solvent in which the polymer was more soluble. Solid dispersion with polyvinylpyrrolidone-vinyl acetate copolymer in 1:4 ratio in absolute ethanol displayed the highest carvedilol dissolution rate with 91.78% carvedilol dissolved in the first 30 min. Capsules prepared with the selected solid dispersion and microcrystalline cellulose as diluent displayed the highest carvedilol dissolution rate, with 93.43% carvedilol dissolved within the first 30 min. Carvedilol bioavailability was significantly increased by formulating solid dispersions, while the analysis of serum biochemical parameters excluded damage on liver and kidney function and the lipid profile of animals exposed to investigated drug delivery system.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Polímeros / Portadores de Fármacos / Excipientes / Carvedilol / Antihipertensivos Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Revista: Eur J Pharm Sci Asunto de la revista: FARMACIA / FARMACOLOGIA / QUIMICA Año: 2020 Tipo del documento: Article Pais de publicación: Países Bajos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Polímeros / Portadores de Fármacos / Excipientes / Carvedilol / Antihipertensivos Tipo de estudio: Prognostic_studies Límite: Animals Idioma: En Revista: Eur J Pharm Sci Asunto de la revista: FARMACIA / FARMACOLOGIA / QUIMICA Año: 2020 Tipo del documento: Article Pais de publicación: Países Bajos