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采用喷雾干燥技术制备依托考昔脂质载体固体分散体及其表征

Preparation and characterization of etoricoxib solid dispersions using lipid carriers by spray drying technique.

作者信息

Chauhan Bhaskar, Shimpi Shyam, Paradkar Anant

机构信息

Department of Pharmaceutics, Bharati Vidyapeeth Deemed University, Poona College of Pharmacy, Erandwane, Pune-411038, Maharashtra, India.

出版信息

AAPS PharmSciTech. 2005 Oct 19;6(3):E405-12. doi: 10.1208/pt060350.

Abstract

The basic objectives of this study were to prepare and characterize solid dispersions of poorly water-soluble drug etoricoxib using lipid carriers by spray drying technique. The properties of solid dispersions were studied by diffuse reflectance infrared Fourier transform spectroscopy (DRIFTS), differential scanning calorimetry (DSC), hot-stage microscopy (HSM), radiograph powder diffraction (XRPD), and dissolution studies. The absence of etoricoxib peaks in XRPD profiles of solid dispersions suggests the transformation of crystalline etoricoxib into an amorphous form. In the HSM examination of solid dispersions, the dissolution of drug in the lipid carriers was observed, which was also confirmed by the absence of etoricoxib peak in DSC curves of solid dispersions. The DRIFTS spectra revealed the presence of hydrogen bonding in solid dispersions. The in vitro dissolution test showed a significant increase in the dissolution rate of solid dispersions as compared with pure etoricoxib, spray-dried etoricoxib, and physical mixtures of drug with lipid carriers. Therefore, the dissolution rate of poorly water-soluble drug etoricoxib can be significantly enhanced by the preparation of solid dispersions using lipid carriers by spray drying technique.

摘要

本研究的基本目标是通过喷雾干燥技术,使用脂质载体来制备难溶性药物依托考昔的固体分散体并对其进行表征。通过漫反射红外傅里叶变换光谱(DRIFTS)、差示扫描量热法(DSC)、热台显微镜(HSM)、X射线粉末衍射(XRPD)和溶出度研究来考察固体分散体的性质。固体分散体的XRPD图谱中没有依托考昔峰,这表明结晶态的依托考昔转变为了无定形形式。在对固体分散体的HSM检查中,观察到药物在脂质载体中的溶解情况,这也通过固体分散体DSC曲线中依托考昔峰的缺失得到了证实。DRIFTS光谱显示固体分散体中存在氢键。体外溶出试验表明,与纯依托考昔、喷雾干燥的依托考昔以及药物与脂质载体的物理混合物相比,固体分散体的溶出速率显著提高。因此,通过喷雾干燥技术使用脂质载体制备固体分散体,可以显著提高难溶性药物依托考昔的溶出速率。

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