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Curr Drug Deliv ; 15(4): 520-531, 2018.
Artigo em Inglês | MEDLINE | ID: mdl-29165075

RESUMO

BACKGROUND: Asenapine is an anti-psychotic agent approved by the US-FDA for treatment of acute schizophrenia and manic or bipolar I disorder in adults. It is poorly absorbed when administered orally, hence exhibits poor oral bioavailability, which limits its use in clinical practice. OBJECTIVE: Enhancement in solubility of asenapine through complexation with three different cyclodextrins, viz. ßCD, HPßCD and sulphobutylether-ßCD (Captisol®) was attempted and compared due to its poor bioavailability. METHOD: Kneading method was used for preparation of inclusion complexes which were characterized by FTIR, DSC, and XRD methods. Extent of binding and stability of the 1:1 inclusion complexes were evaluated by molecular modelling and phase solubility studies. Pharmacokinetic studies were also carried out of these inclusion complexes. RESULTS: Captisol® complex was the most stable amongst all complexes showing 4.9 times solubility enhancement of asenapine and 96% drug release at the end of 60 min, whereas asenapine maleate (uncomplexed drug) was released completely at the end of 120min. The Cmax and AUC values of Captisol® asenapine complex (AS-Captisol complex) were 2.8 and 2.3 times higher than the uncomplexed drug. CONCLUSION: This study thus demonstrated that Captisol® inclusion complex is an effective strategy for solubility and bioavailability enhancement of asenapine.


Assuntos
Antipsicóticos/administração & dosagem , Antipsicóticos/farmacocinética , Composição de Medicamentos/métodos , Compostos Heterocíclicos de 4 ou mais Anéis/administração & dosagem , Compostos Heterocíclicos de 4 ou mais Anéis/farmacocinética , beta-Ciclodextrinas/administração & dosagem , beta-Ciclodextrinas/farmacocinética , Animais , Antipsicóticos/química , Dibenzocicloeptenos , Liberação Controlada de Fármacos , Estabilidade de Medicamentos , Compostos Heterocíclicos de 4 ou mais Anéis/química , Masculino , Modelos Moleculares , Simulação de Dinâmica Molecular , Ratos , Solubilidade , beta-Ciclodextrinas/química
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