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The impact of polymer blends and solid dispersion technologies on drug release rates.

机译:聚合物共混物和固体分散技术对药物释放速率的影响。

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摘要

The objective of this research was to investigate the impact of polymer blends and solid dispersion formulation technologies on drug forms and release rates. An hydrophobic carrier, poly(methyl methacrylate PMMA), an hydrophilic carrier Eudragit EPO, together with an hydrophobic drug indomethacin (INDO), were used to produce various dispersion formulations through hot melt mixing (HMM) and solvent evaporation methods. Characterization of the various solid dispersion formulations was performed using standard analytical methods such as differential scanning calorimetry (DSC), polarized light microscopy (PLM), environmental scanning electron microscopy (ESEM), powder X-ray diffraction (PXRD), and Fourier transform infrared spectroscopy (FTIR). The results obtained from the various characterizations suggest that the drug was molecularly dispersed in the polymer matrices. In-vitro dissolution studies were carried out in simple model gastric fluid (pH 1.2) and also in phosphate buffer dissolution medium (pH 7.2). Approximately, 19.79 % of the INDO contained in the HMM formulation comprising PMMA 70 EPO 10 INDO 20 by weight percent was released in approximately 30 minutes while about 54% of the solvent evaporation formulation (PMMA 70 EPO 10 INDO 20) was released after 22 hours. Dissolution results demonstrated that a combination of hydrophobic and hydrophilic polymers will effectively sustain the drug release for a prolonged period of time depending on the formulation composition and the solid dispersion technology employed to produce it.
机译:这项研究的目的是研究聚合物共混物和固体分散体配制技术对药物形式和释放速率的影响。疏水性载体聚(甲基丙烯酸甲酯PMMA),亲水性载体Eudragit EPO和疏水性药物消炎痛(INDO)一起用于通过热熔混合(HMM)和溶剂蒸发法生产各种分散体配方。使用标准分析方法(例如差示扫描量热法(DSC),偏振光显微镜(PLM),环境扫描电子显微镜(ESEM),粉末X射线衍射(PXRD)和傅里叶变换红外光谱)对各种固体分散体配方进行表征光谱(FTIR)。从各种特征获得的结果表明该药物分子分散在聚合物基质中。在简单模型胃液(pH 1.2)和磷酸盐缓冲液溶解介质(pH 7.2)中进行了体外溶出研究。在约30分钟内释放约19.79%的按重量计包含PMMA 70 EPO 10 INDO 20的HMM配方中所含的INDO,而在22小时后释放约54%的溶剂蒸发配方(PMMA 70 EPO 10 INDO 20) 。溶解结果表明,疏水性和亲水性聚合物的组合将有效地延长药物释放的时间,具体取决于制剂的组成和用于生产药物的固体分散技术。

著录项

  • 作者

    Adegoke, Adeyinka A.;

  • 作者单位

    University of Rhode Island.;

  • 授予单位 University of Rhode Island.;
  • 学科 Engineering Chemical.;Health Sciences Pharmacy.
  • 学位 M.S.
  • 年度 2012
  • 页码 81 p.
  • 总页数 81
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

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