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Acta Pharmaceutica Sinica ; (12): 1678-1686, 2012.
Artigo em Inglês | WPRIM | ID: wpr-274604

RESUMO

Total paeony glycoside (TPG) is extracted and purified from a traditional Chinese herbal medicine. It has many biological and pharmacological activities. However, there are few dosage forms of TPG in the market because of its low bioavailability. Self-microemulsifying drug delivery system (SMEDDS) is a vital tool in solving low bioavailability of poor absorption drugs. So the objective of this study is to develop a new TPG-SMEDDS for the oral delivery of poorly soluble TPG. Through the construction of pseudo-ternary phase diagrams, the optimum prescription was obtained, which consisted of 18.70% TPG, 16.27% ethyl oleate as oil, 43.34% Cremophor RH40 as surfactant and 21.73% Transcutol P as cosurfactant. The characterizations of TPG-SMEDDS including morphological characterization, droplet size, zeta-potential, emulsification time, and dissolution study of TPG-SMEDDS were evaluated. The results showed that TPG-SMEDDS is stable and its release rate is high in four different media (0.1 mol x L(-1) HCl, pH 6.8 PBS, pH 7.4 PBS, and water). The relative bioavailability of SMEDDS was dramatically enhanced in an average of 1.52-fold that of TPG-suspension. It is concluded that the bioavailability of TPG is enhanced greatly by SMEDDS.


Assuntos
Animais , Ratos , Administração Oral , Disponibilidade Biológica , Sistemas de Liberação de Medicamentos , Estabilidade de Medicamentos , Emulsões , Etilenoglicóis , Química , Glicosídeos , Química , Farmacocinética , Ácidos Oleicos , Química , Paeonia , Química , Tamanho da Partícula , Veículos Farmacêuticos , Química , Plantas Medicinais , Química , Polietilenoglicóis , Química , Solubilidade
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