| 論文名 |
Modulated dissolution rate from the inclusion complex of antichagasic benznidazole and cyclodextrin using hydrophilic polymer. |
| 著者 |
L?via C L S?-Barreto
Pricila C Gustmann
Felipe S Garcia
Fl?via P Maximiano
K?tia M Novack
Marc?lio S S Cunha-Filho
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| キーワード |
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| 出版年月 |
1970年1月 |
| 発表先 |
Pharm Dev Technol. Sep-Oct 2013;18(5):1035-41. |
| WEBサイト |
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| 論文概要（和文） |
親水性ポリマーを使用した、抗炭酸ベンズニダゾールとシクロデキストリンの包接複合体からの溶解速度の調整。 |
| 論文概要（英文） |
Benznidazole (BNZ) is the primary chemotherapeutic agent for treating Chagas' disease; however, its poor water solubility and irregular oral absorption lead to the treatment failure in the chronic phase. The aim of this work was to investigate the utility of the polymer hydroxypropyl methylcellulose (HPMC) in controlling the release of BNZ from solid inclusion complexes with cyclodextrin to overcome the problem of its bioavailability. Preliminary studies of solubility were conducted in solution using selected β-cyclodextrin derivatives according to an experimental mixture design. The best cyclodextrin composition was used to produce solid-state systems by kneading in the presence or absence of HPMC. The formulations were characterized by different physico-chemical techniques, including the dissolution rate. Hydroxypropyl-β-cyclodextrin (HPβCD) produced the greatest improvement in drug solubility and was selected for the development of solid systems. Assays confirmed the production of true inclusion complexes between BNZ and HPβCD. The dissolution rate of the BNZ-HPβCD system was markedly increased, while the presence of HPMC retarded drug release. An optimal formulation obtained by the combination of kneading systems developed in appropriate ratios could be a promising drug delivery system with a prolonged therapeutic effect coupled with more balanced bioavailability. The produced systems present interesting perspectives for Chagas' therapy. |
