RESUMO
Peanut oil and Tween 80 blends devoid of any cosurfactant were employed in the formulation of different batches of liquid self-microemulsifying drug delivery systems (LSMEDDS) and their suitability as vehicles for the delivery of a typical lipophilic drug-griseofulvin-was investigated. The LSMEDDS were evaluated using the following parameters: phase separation, globule size, viscosity, solubility of griseofulvin, and partition coefficient. The release profile of griseofulvin from the optimized LSMEDDS was evaluated in citrate/phosphate buffer solutions of pH 2.0, pH 6.5, and pH 7.4. The results obtained indicated that there was significantly higher (alpha = 0.05) percentage cumulative amounts of griseofulvin released from the LSMEDDS in comparison with that released from peanut oil alone. The release of griseofulvin from the LSMEDDS into aqueous media of pH 6.5 and pH 7.4 showed enhanced and controlled dissolution of the drug from the formulation. Incorporation of griseofulvin into this proposed formulation is suggested as a strategy to overcome the irregular dissolution and absorption behaviors often associated with conventional griseofulvin tablets.
Assuntos
Antifúngicos/administração & dosagem , Antifúngicos/farmacocinética , Sistemas de Liberação de Medicamentos/métodos , Emulsificantes/química , Griseofulvina/administração & dosagem , Griseofulvina/farmacocinética , Antifúngicos/química , Disponibilidade Biológica , Composição de Medicamentos/métodos , Desenho de Fármacos , Emulsões , Griseofulvina/química , Óleo de Amendoim , Permeabilidade , Transição de Fase , Óleos de Plantas/química , Polissorbatos/química , SolubilidadeRESUMO
The effectiveness of a polysaccharide gum obtained from the cormels of Colocassia esculenta was evaluated comparatively with acacia and methylcellulose as binders in the formulation of poorly compressible drugs. The granules of these drugs produced by wet massing method using colocassia and acacia gums as binders have high compressibility index indicating poor flow. Based on this parameter, the granules produced with methylcellulose as binder seem to flow better. The properties of tablets evaluated include breaking strength, friability, disintegration time and dissolution rate. The new polysaccharide gum showed better concentration-strength profile than acacia while methylcellulose yielded mechanically more stable tablets than the two binders. The resistance of tablets to abrasion was poor in metronidazole tablets formulated with colocassia gum. The in vitro availability characteristics showed that tablets produced with the new gum show acceptable disintegration time and release profile within a certain range of its concentration in tablets. At 4% w/w nominal concentration of colocassia gum in metronidazole tablets and 6% w/w in paracetamol, tablets show very long disintegration time and prolonged release profile. The binders used for comparison yielded tablets that show better in vitro release characteristics.