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1.
Invest Clin ; 53(3): 223-36, 2012 Sep.
Artigo em Inglês | MEDLINE | ID: mdl-23248967

RESUMO

The aim of the present investigation was to formulate thermally sintered floating tablets of propranolol HCl, and to study the effect of sintering conditions on drug release, as well as their in vitro buoyancy properties. A hydrophilic polymer, polyethylene oxide, was selected as a sintered polymer to retard the drug release. The formulations were prepared by a direct compression method and were evaluated by in vitro dissolution studies. The results showed that sintering temperature and time of exposure greatly influenced the buoyancy, as well as the dissolution properties. As the sintering temperature and time of exposure increased, floating lag time was found to be decreased, total floating time was increased and drug release was retarded. An optimized sintered formulation (sintering temperature 50 degrees C and time of exposure 4 h) was selected, based on their drug retarding properties. The optimized formulation was characterized with FTIR and DSC studies and no interaction was found between the drug and the polymer used.


Assuntos
Química Farmacêutica/métodos , Propranolol , Comprimidos , Sistemas de Liberação de Medicamentos , Temperatura Alta , Fenômenos Físicos , Estômago
2.
Invest Clin ; 53(1): 60-70, 2012 Mar.
Artigo em Inglês | MEDLINE | ID: mdl-22524109

RESUMO

Abstract. The purpose of this research was to develop and evaluate effervescent gastric floating tablets of propranolol HCl. The oral delivery of antihypertensive propranolol HCl was facilitated by preparing an effervescent floating dosage form which could increase its absorption in the stomach by increasing the drug's gastric residence time. In the present work, effervescent floating tablets were prepared with a hydrophilic carrier such as polyethylene oxide (PEO WSR N 60K and PEO WSR 303) as a release retarding agent and sodium bicarbonate as a gas generating agent. The prepared tablets were evaluated for all their physicochemical properties, in vitro buoyancy, drug release and rate order kinetics. From the results, P9 was selected as an optimized formulation based on their 12 h drug release, minimal floating lag time and maximum total floating time. The optimized formulation followed first order rate kinetics with erosion mechanism. The optimized formulation was characterized with FTIR studies and no interaction between the drug and the polymers were observed.


Assuntos
Propranolol/administração & dosagem , Absorção , Administração Oral , Celulose/administração & dosagem , Fenômenos Químicos , Química Farmacêutica , Portadores de Fármacos , Sistemas de Liberação de Medicamentos , Desenho de Fármacos , Avaliação Pré-Clínica de Medicamentos , Estrutura Molecular , Polietilenoglicóis/administração & dosagem , Propranolol/farmacocinética , Bicarbonato de Sódio/administração & dosagem , Solubilidade , Espectroscopia de Infravermelho com Transformada de Fourier , Ácidos Esteáricos/administração & dosagem , Estômago , Comprimidos
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