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首页> 外文期刊>Journal of Young Pharmacists >Preparation and Characterization of Pioglitazone Cyclodextrin Inclusion Complexes
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Preparation and Characterization of Pioglitazone Cyclodextrin Inclusion Complexes

机译：吡格列酮环糊精包合物的制备与表征

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Pioglitazone, a class II Biopharmaceutical Classification System drug having poor water solubility and slow dissolution rate may have a negative impact on its subtherapeutic plasma drug levels leading to therapeutic failure. In order to improve its water solubility and thus dissolution, cyclodextrin complexation technique was followed. The phase solubility studies were carried using three different types of cyclodextrins viz., β, methyl-β and γ-cyclodextrins. The Gibbs free energy was calculated in order to determine ease of the complexation. Binary systems of pioglitazone with cyclodextrins were prepared by kneading method and spray drying method. The phase solubility profiles with all the three cyclodextrins were classified as A L -type, indicating the formation of 1:1 stoichiometric inclusion complexes. The complexation capability of cyclodextrins with pioglitazone increased in the order of methyl-β > β > γ-cyclodextrin. The Gibbs free energy was found to be in the order γ > methyl-β > β cyclodextrin. Characterization of inclusion complexes was done by solubility studies, in vitro dissolution studies, Fourier transformation-infrared spectroscopy, scanning electron microscopy, differential scanning calorimetry and X-ray powder diffractometry studies. Inclusion complexes exhibited higher rates of dissolution than the corresponding physical mixtures and pure drug. Greater solubility was observed with spray-dried methyl-β cyclodextrin complexes (2.29 ± 0.001 mg/ml) in comparison to the kneaded methyl-β cyclodextrin complexes (1.584 ± 0.053 mg/ml) and pure drug (0.0714 ± 0.0018 mg/ml).
机译：吡格列酮是一种水溶性差且溶解速度慢的II类生物制药分类系统药物，可能对其亚治疗性血浆药物水平产生负面影响，从而导致治疗失败。为了改善其水溶性并因此提高其溶解度，采用了环糊精络合技术。使用三种不同类型的环糊精，即β，甲基-β和γ-环糊精进行相溶解度研究。计算吉布斯自由能，以确定络合的难易程度。通过捏合法和喷雾干燥法制备吡格列酮与环糊精的二元体系。所有三种环糊精的相溶解度曲线均归为A L 型，表明形成了1：1化学计量的包合物。环糊精与吡格列酮的络合能力按甲基-β>β>γ-环糊精的顺序增加。发现吉布斯自由能为γ>甲基-β>β环糊精。包合物的表征通过溶解度研究，体外溶解研究，傅立叶变换红外光谱，扫描电子显微镜，差示扫描量热法和X射线粉末衍射法研究完成。包合物具有比相应的物理混合物和纯药物更高的溶出速率。与捏合的甲基-β-环糊精复合物（1.584±0.053mg / ml）和纯药物（0.0714±0.0018mg / ml）相比，喷雾干燥的甲基-β-环糊精复合物（2.29±0.001mg / ml）观察到更高的溶解度。 。

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