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美洛昔康- Gelucire 50/13二元体系的物理化学表征及溶解性质

Physicochemical characterization and dissolution properties of meloxicam-gelucire 50/13 binary systems.

作者信息

El-Badry Mahmoud

机构信息

Department of Pharmaceutics, College of Pharmacy, King Saud University, P.O. BOX 2457, Riyadh 11451, Saudi Arabia.

出版信息

Sci Pharm. 2011 Apr-Jun;79(2):375-86. doi: 10.3797/scipharm.1101-22. Epub 2011 Apr 10.

DOI:10.3797/scipharm.1101-22
PMID:21773073
原文链接:https://pmc.ncbi.nlm.nih.gov/articles/PMC3134858/
Abstract

A solid dispersion of Meloxicam (MX), a poorly soluble, non steroidal anti-inflammatory drug, and Gelucire 50/13 was prepared by spray drying. Spherical microparticles were yielded with smooth surfaces as observed by scanning electron microscopy. According to differential scanning calorimetry and powder X-ray diffractometry analysis, MX was transformed from the crystalline state to the amorphous state as confirmed by the disappearance of its melting peak and the crystalline peaks. The dissolution tests at pH 7.4 revealed that the dissolution rate of encapsulated MX was 2.5-fold higher than that of the corresponding physical mixture and fourfold higher than the drug alone, respectively. The microparticles prepared at a ratio of 1:4 (drug/Gelucire) exhibited a 4-fold higher anti-inflammatory activity on the paw edema of rats in comparison to the drug alone. All in all, this work reveals that spray drying is a suitable technique for preparation of solid dispersions with improved biopharmaceutical and pharmacological characteristics of MX.

摘要

通过喷雾干燥法制备了难溶性非甾体抗炎药美洛昔康（MX）与Gelucire 50/13的固体分散体。扫描电子显微镜观察显示，得到了表面光滑的球形微粒。根据差示扫描量热法和粉末X射线衍射分析，MX的熔点峰和结晶峰消失，证实其从结晶态转变为无定形态。在pH 7.4条件下的溶出试验表明，包封的MX的溶出速率分别比相应的物理混合物高2.5倍，比单独的药物高4倍。以1:4（药物/Gelucire）比例制备的微粒对大鼠爪肿胀的抗炎活性比单独的药物高4倍。总而言之，这项研究表明喷雾干燥是制备具有改善的美洛昔康生物药剂学和药理学特性的固体分散体的合适技术。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1187/3134858/72ecc72a9de8/scipharm-2011-79-375f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1187/3134858/14726697788c/scipharm-2011-79-375f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1187/3134858/fc4ab851ae67/scipharm-2011-79-375f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1187/3134858/d676149d748e/scipharm-2011-79-375f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1187/3134858/0e613f8eb841/scipharm-2011-79-375f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1187/3134858/76169b9bc7b8/scipharm-2011-79-375f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1187/3134858/72ecc72a9de8/scipharm-2011-79-375f6.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1187/3134858/14726697788c/scipharm-2011-79-375f1.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1187/3134858/fc4ab851ae67/scipharm-2011-79-375f2.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1187/3134858/d676149d748e/scipharm-2011-79-375f3.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1187/3134858/0e613f8eb841/scipharm-2011-79-375f4.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1187/3134858/76169b9bc7b8/scipharm-2011-79-375f5.jpg
https://cdn.ncbi.nlm.nih.gov/pmc/blobs/1187/3134858/72ecc72a9de8/scipharm-2011-79-375f6.jpg

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