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采用溶剂法研究格列齐特与聚乙烯吡咯烷酮K-30和聚乙二醇6000的固体分散体系统

Study of Gliclazide Solid Dispersion Systems Using PVP K-30 and PEG 6000 by Solvent Method.

作者信息

Febriyenti Febriyenti, Rahmi Suraiya, Halim Auzal

机构信息

Faculty of Pharmacy, Universitas Andalas, Padang, Indonesia.

出版信息

J Pharm Bioallied Sci. 2019 Jul-Sep;11(3):262-267. doi: 10.4103/jpbs.JPBS_87_18.

Abstract

Gliclazide is a second-generation hypoglycemic sulfonylurea, which is useful in the treatment of non-insulin-dependent diabetes mellitus. It has low bioavailability because of its limited water solubility and slow dissolution rate. In this study, solid dispersions of gliclazide were prepared by solvent method. Drug and carriers weight ratio were 1:9; 2:8; 3:7; 4:6; and 5:5. The weight ratio of carriers (polyvinyl pyrrolidone K-30 and polyethylene glycol 6000) was 1:1. The properties of solid dispersions were evaluated using scanning electron microscopy (SEM), Fourier-transform infra red (FTIR) spectroscopy, differential scanning calorimetry (DSC), X-ray diffraction (XRD), and solubility and dissolution studies. SEM result showed that gliclazide was highly dispersed and was present as amorphous state in the solid dispersions. The FTIR spectroscopy showed no chemical interaction between gliclazide and carriers. DSC studies indicated melting point of gliclazide was decreased. The XRD studies indicated that crystallinity degree of gliclazide was decreased. Rate of dissolution and solubility of solid dispersions was increased than pure gliclazide ( < 0.05).

摘要

格列齐特是第二代降血糖磺脲类药物,可用于治疗非胰岛素依赖型糖尿病。由于其水溶性有限且溶解速率缓慢,其生物利用度较低。在本研究中,采用溶剂法制备了格列齐特固体分散体。药物与载体的重量比为1:9、2:8、3:7、4:6和5:5。载体(聚乙烯吡咯烷酮K-30和聚乙二醇6000)的重量比为1:1。采用扫描电子显微镜(SEM)、傅里叶变换红外光谱(FTIR)、差示扫描量热法(DSC)、X射线衍射(XRD)以及溶解度和溶出度研究对固体分散体的性质进行了评估。SEM结果表明,格列齐特高度分散,在固体分散体中以无定形状态存在。FTIR光谱显示格列齐特与载体之间不存在化学相互作用。DSC研究表明格列齐特的熔点降低。XRD研究表明格列齐特的结晶度降低。固体分散体的溶出速率和溶解度比纯格列齐特有所提高(P<0.05)。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/31d8/6662042/61d89ac28fec/JPBS-11-262-g001.jpg

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