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制备方法对酮洛芬-环糊精-磷脂酰胆碱三元体系物理化学性质的影响。

Influence of the preparation method on the physical-chemical properties of ketoprofen-cyclodextrin-phosphatidylcholine ternary systems.

机构信息

Department of Pharmaceutical Sciences, University of Florence, via Schiff 6 Sesto Fiorentino 50019, Florence, Italy.

出版信息

J Pharm Biomed Anal. 2009 Dec 5;50(5):690-4. doi: 10.1016/j.jpba.2008.11.002. Epub 2008 Nov 13.

Abstract

The aim of this work was to assess the effectiveness and actual advantages of the microwave (MW) technology for preparing ternary complexes of ketoprofen (Keto) with beta-cyclodextrin (beta-Cd) or methylated-beta-cyclodextrin (Mebeta-Cd) and phosphatidylcholine (EPC3) with respect to conventional preparation methods, such as co-grinding and sealed-heating. The products obtained with the different techniques were characterized by differential scanning calorimetry (DSC), X-ray powder diffractometry, FT-IR spectroscopy and dissolution studies. For each method, the influence of different experimental conditions on the physical-chemical properties of the final products has been also investigated. DSC analysis was used to monitor physical stability of ternary complexes during 2 years storage under ambient conditions. MW irradiation resulted to be a rapid and very convenient preparation technique. In fact, it was more effective than the considered conventional methods, enabling obtainment in shorter times of products with better performance. In particular, the Keto-Mebeta-Cd-EPC3 product prepared by MW treatment at 750 W for 10 min allowed achievement of about 80% of drug dissolution after 60 min, in comparison with the 50% and 63% values obtained for the corresponding products prepared by 30-min co-grinding or 60-min sealed-heating. Moreover, such ternary products were more effective in improving drug dissolution than the corresponding Keto-Mebeta-Cd systems. Furthermore, the MW treatment at such irradiation energy enabled obtainment of totally dehydrated samples, which maintained unchanged solid-state characteristics and showed no susceptibility to ambient humidity after 2 years storage at ambient temperature. Therefore, MW-treated Keto-Mebeta-Cd-EPC3 systems can be successfully used for formulation of tablets with enhanced drug dissolution behaviour.

摘要

本工作旨在评估微波(MW)技术相对于传统制备方法(如共研磨和密封加热)在制备酮洛芬(Keto)与β-环糊精(β-Cd)或甲基-β-环糊精(Mebeta-Cd)以及磷脂酰胆碱(EPC3)的三元配合物方面的有效性和实际优势。采用差示扫描量热法(DSC)、X 射线粉末衍射、FT-IR 光谱和溶解研究对用不同技术获得的产物进行了表征。对于每种方法,还研究了不同实验条件对最终产物物理化学性质的影响。DSC 分析用于监测在环境条件下储存 2 年期间三元配合物的物理稳定性。MW 辐射是一种快速且非常方便的制备技术。事实上,它比所考虑的常规方法更有效,能够在更短的时间内获得性能更好的产品。特别是,通过 MW 处理在 750 W 下处理 10 分钟制备的 Keto-Mebeta-Cd-EPC3 产品在 60 分钟后允许达到约 80%的药物溶解,而通过 30 分钟共研磨或 60 分钟密封加热制备的相应产品的药物溶解度分别为 50%和 63%。此外,与相应的 Keto-Mebeta-Cd 系统相比,这些三元产物在提高药物溶解度方面更有效。此外,在这种辐照能量下进行 MW 处理可获得完全脱水的样品,这些样品在环境温度下储存 2 年后保持不变的固态特征,并且对环境湿度没有敏感性。因此,MW 处理的 Keto-Mebeta-Cd-EPC3 系统可成功用于制备具有增强药物溶解行为的片剂。

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