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吲哚美辛喷雾干燥微球的制备及包衣对溶解速率影响的研究

Preparation of spray-dried microspheres of indomethacin and examination of the effects of coating on dissolution rates.

作者信息

Ermiş D, Yüksel A

机构信息

Department of Pharmaceutical Technology, Faculty of Pharmacy, Ankara University, Tandogan-Ankara, Turkey.

出版信息

J Microencapsul. 1999 May-Jun;16(3):315-24. doi: 10.1080/026520499289040.

Abstract

In this study, microspheres were prepared by the spray drying technique using suspensions of indomethacin (IM) as active substance and coated by three different polymers in order to increase the dissolution rate of IM. Water solutions (0.1, 0.2 and 0.5%) of hydroxypropylmethyl cellulose (HPMC), polyvinyl alcohol (PVA) and hydroxypropyl cellulose (HPC) were used as coating materials. Polyethylene glycol 400 (PEG 400) was added to all formulations as plasticizer. Changes of particles size and surface characteristics of the coated products were examined using optical microscopy and scanning electron microscopy (SEM), respectively. The effects of coatings on the dissolution rates of IM were examined using USP XXIII Method II in water and phosphate buffer pH 7.4. It was observed that coating the IM particles with HPMC, PVA and HPC polymers using the Spray-Drying Technique increased the dissolution rate of IM significantly.

摘要

在本研究中,以吲哚美辛(IM)悬浮液作为活性物质,采用喷雾干燥技术制备微球,并使用三种不同的聚合物进行包衣,以提高IM的溶解速率。羟丙基甲基纤维素(HPMC)、聚乙烯醇(PVA)和羟丙基纤维素(HPC)的水溶液(0.1%、0.2%和0.5%)用作包衣材料。向所有制剂中添加聚乙二醇400(PEG 400)作为增塑剂。分别使用光学显微镜和扫描电子显微镜(SEM)检查包衣产品的粒径和表面特性变化。使用美国药典XXIII方法II在水和pH 7.4的磷酸盐缓冲液中检查包衣对IM溶解速率的影响。观察到,采用喷雾干燥技术用HPMC、PVA和HPC聚合物对IM颗粒进行包衣可显著提高IM的溶解速率。

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