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格列齐特-聚乙二醇4000固体分散体的制备与表征

Preparation and characterization of gliclazide-polyethylene glycol 4000 solid dispersions.

作者信息

Patil Moreshwar P, Gaikwad Naresh J

机构信息

Department of Pharmaceutical Sciences, Rashtrasant Tukadoji Maharaj Nagpur University Mahatma Jyotiba Fuley Shaikshanik Parisar, Amravati Road, Nagpur-440033, India.

出版信息

Acta Pharm. 2009 Mar;59(1):57-65. doi: 10.2478/v10007-009-0001-3.

DOI:10.2478/v10007-009-0001-3
PMID:19304558
Abstract

The objective of the present investigation was to study the effect of polyethylene glycol 4000 (PEG 4000) on in vitro dissolution of gliclazide from solid dispersions. Initial studies were carried out using physical mixtures of the drug and carrier. Solid dispersions were prepared by the melting or fusion method.Phase and saturation solubility study, in vitro dissolution of pure drug, physical mixtures and solid dispersions were carried out. PEG was found to be effective in increasing the dissolution of gliclazide in solid dispersions when compared to pure drug. FT-IR spectroscopy, differential scanning calorimetry and X-ray diffractometry studies were carried out in order to characterize the drug in the physical mixtures and solid dispersions. Dissolution enhancement was attributed to decreased crystallinity of the drug and to the wetting and solubilizing effect of the carrier from the solid dispersions of gliclazide. In conclusion, dissolution of gliclazide can be enhanced by the use of hydrophilic carrier.

摘要

本研究的目的是考察聚乙二醇4000(PEG 4000)对格列齐特固体分散体体外溶出度的影响。最初的研究使用药物与载体的物理混合物进行。通过熔融法制备固体分散体。进行了相溶解度和饱和溶解度研究、纯药物、物理混合物和固体分散体的体外溶出度研究。与纯药物相比,发现PEG在提高格列齐特在固体分散体中的溶出度方面是有效的。进行了傅里叶变换红外光谱(FT-IR)、差示扫描量热法(DSC)和X射线衍射(XRD)研究,以表征物理混合物和固体分散体中的药物。溶出度提高归因于药物结晶度的降低以及载体对格列齐特固体分散体的润湿性和增溶作用。总之,使用亲水性载体可提高格列齐特的溶出度。

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