RESUMO
Azapropazone was encapsulated with pectin-rutin mixture using the fluidized bed technique. The encapsulated particles showed higher dissolution rate and bioavailability but lower ulcerogenic activity as compared with the drug alone.
Assuntos
Apazona/farmacocinética , Composição de Medicamentos/métodos , Pectinas/química , Rutina/química , Animais , Apazona/administração & dosagem , Apazona/toxicidade , Disponibilidade Biológica , Masculino , Tamanho da Partícula , Ratos , Úlcera Gástrica/induzido quimicamenteRESUMO
Acidic and basic nonsteroidal anti-inflammatory drugs were encapsulated with cellulose derivatives having different functional groups, acidic (carboxymethyl cellulose), basic (chitosan), and neutral (hydroxypropylmethyl cellulose). The properties of the microcapsules were studied and the interaction of the drugs with chitosan was assessed.
Assuntos
Anti-Inflamatórios não Esteroides , Composição de Medicamentos/métodos , Carboximetilcelulose Sódica , Fenômenos Químicos , Química , Quitina/análogos & derivados , Quitosana , Glafenina , Derivados da Hipromelose , Metilcelulose/análogos & derivados , OxifenilbutazonaRESUMO
The bioavailability and gastric ulcerogenic activity of oxyphenbutazone and glafenine (acidic and basic nonsteroidal anti-inflammatory drugs), coated with different cellulose derivatives were assessed in albino rats. The cellulose derivatives chosen have different functional groups, acidic (carboxymethyl cellulose), basic (chitosan) and neutral (hydroxypropylmethyl cellulose). The bioavailability was dependent on the drug and polymers. Generally, all the cellulose derivatives chosen decreased the gastric ulcerogenic activity of the drugs studied.
Assuntos
Glafenina/administração & dosagem , Oxifenilbutazona/administração & dosagem , Úlcera Gástrica/induzido quimicamente , ortoaminobenzoatos/administração & dosagem , Animais , Disponibilidade Biológica , Cápsulas/efeitos adversos , Carboximetilcelulose Sódica , Quitina/análogos & derivados , Quitosana , Glafenina/efeitos adversos , Glafenina/farmacocinética , Derivados da Hipromelose , Masculino , Metilcelulose/análogos & derivados , Oxifenilbutazona/efeitos adversos , Oxifenilbutazona/farmacocinética , Ratos , Fatores de TempoRESUMO
Different classes of nonsteroidal anti-inflammatory drugs, NSAIDs, were separately coated with cationic (E) and anionic (L) Eudragit using the fluidized bed technique. The bioavailability and ulcerogenic activity of coated and uncoated drugs were assessed in rats. The cationic coat decreased the ulcerogenic activity in all classes of NSAIDs and increased the bioavailability only in acidic and enolic ones. The anionic coat, however, increased the bioavailability in basic NSAIDs.
Assuntos
Anti-Inflamatórios não Esteroides/administração & dosagem , Úlcera Gástrica/induzido quimicamente , Animais , Anti-Inflamatórios não Esteroides/efeitos adversos , Anti-Inflamatórios não Esteroides/farmacocinética , Disponibilidade Biológica , Cápsulas , Masculino , RatosRESUMO
Nonsteroidal anti-inflammatory drugs, NSAIDs, were encapsulated with cationic and anionic Eudragit polymers. The properties of the microcapsules were studied. The interactions, if any, between the polymers and NSAIDs were also investigated.
