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1.
J Pharm Sci ; 104(5): 1767-76, 2015 May.
Artigo em Inglês | MEDLINE | ID: mdl-25761776

RESUMO

Melt blowing (MB) was investigated to prepare a fast dissolving fibrous drug-loaded solid dispersion and compared with solvent-based electrospinning (SES) and melt electrospinning (MES). As a conventional solvent-free technique coupled with melt extrusion and using a high-speed gas stream, MB can provide high-quality micro- and nanofibers at industrial throughput levels. Carvedilol, a weak-base model drug with poor water solubility, was processed using a common composition optimized for the fiber spinning and blowing methods based on a hydrophilic vinylpyrrolidone-vinyl acetate copolymer (PVPVA64) and PEG 3000 plasticizer. Scanning electron microscopy combined with fiber diameter analysis showed diameter distributions characteristic to each prepared fibrous fabrics (the mean value increased toward SES

Assuntos
Química Farmacêutica/métodos , Portadores de Fármacos/síntese química , Preparações Farmacêuticas/síntese química , Polímeros/síntese química , Portadores de Fármacos/farmacocinética , Preparações Farmacêuticas/metabolismo , Polímeros/farmacocinética , Solubilidade
2.
J Pharm Sci ; 103(4): 1278-87, 2014 Apr.
Artigo em Inglês | MEDLINE | ID: mdl-24549788

RESUMO

Melt electrospinning (MES) was used to prepare fast dissolving fibrous drug delivery systems in the presence of plasticizers. This new method was found promising in the field of pharmaceutical formulation because it combines the advantages of melt extrusion and solvent-based electrospinning. Lowering of the process temperature was performed using plasticizers in order to avoid undesired thermal degradation. Carvedilol (CAR), a poorly water-soluble and thermal-sensitive model drug, was introduced into an amorphous methacrylate terpolymer matrix, Eudragit® E, suitable for fiber formation. Three plasticizers (triacetin, Tween® 80, and polyethylene glycol 1500) were tested, all of which lowered the process temperature effectively. Scanning electron microscopy, X-ray diffraction, differential scanning calorimetry, and Raman microspectrometry investigations showed that crystalline CAR turned into an amorphous form during processing and preserved it for longer time. In vitro dissolution studies revealed ultrafast drug dissolution of the fibrous samples. According to the HPLC impurity tests, the reduced stability of CAR under conditions applied without plasticizer could be avoided using plasticizers, whereas storage tests also indicated the importance of optimizing the process parameters during MES.


Assuntos
Anti-Hipertensivos/administração & dosagem , Carbazóis/administração & dosagem , Plastificantes/química , Ácidos Polimetacrílicos/química , Propanolaminas/administração & dosagem , Anti-Hipertensivos/química , Carbazóis/química , Carvedilol , Sistemas de Liberação de Medicamentos , Estabilidade de Medicamentos , Propanolaminas/química , Solubilidade , Temperatura
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