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首页> 外文学位 >Controlled release solid dispersion of metoprolol succinate for direct use in the preparation of multiple strengths solid dosage forms.
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Controlled release solid dispersion of metoprolol succinate for direct use in the preparation of multiple strengths solid dosage forms.

机译：琥珀酸美托洛尔的控释固体分散体，可直接用于制备多种强度的固体剂型。

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摘要

Solid dispersions are an established solubilisation technique for water insoluble drugs. These are essentially drug-polymer systems that are able to improve the dissolution and bioavailability profiles of water insoluble drugs owing to greater drug-polymer interactions. The purpose of this study was to exploit these drug-polymer interactions in solid dispersions to develop sustained release dosage forms of a water soluble drug, Metoprolol Succinate.;The solid dispersions were prepared by solvent evaporation method, using formulations containing various ratios of drug and rate controlling polymer and a lipid excipient. Drug release profiles were determined by the USP Apparatus 1 (Basket Apparatus) in phosphate buffer solution (pH 6.8). The solid dispersion formulations were characterised by analytical methods like powder XRD, FT-IR, DSC and UV spectroscopy to check for amorphous nature and hydrogen bonding interactions between drug and polymers.;Among all the formulations studied, the dispersion sample containing Drug/ Methocel RTM K 100 Premium LV/Compritol RTM 888 ATO in a weight ratio of 1: 1.5:0.5 gave the desired sustained Among all the formulations studied, the dispersion sample containing Drug/ Methocel K100 Premium LV/Compritol RTM 888 ATO in a weight ratio of 1: 1.5: 0.5 gave the desired sustained release profile for the 24 hr period. When compared against the pure drug and the physical mixture of the same formulation, the results showed that the drug release was sustained due to the formation of the solid dispersion and not merely due to the presence of the rate controlling polymers and lipid excipient.;To evaluate the feasibility of developing multiple strength dosage forms of this particular drug formulation, the dispersion powder equivalent to 25 mg, 50 mg, 100 mg, and 200 mg were tested for the drug-release profiles. The data revealed that the drug release was proportionate to the amount of drug present in the dispersion formulation. Further, a graph of % drug released vs time was found to be almost over lapping. This strengthens the proposition that multiple dosage strengths can be conveniently formulated using this particular method and formula.;The pXRD and DSC data confirmed the amorphous nature of the drug in the formulation. The FT-IR data was inconclusive for hydrogen bonding interactions because of overlapping of the IR absorption peaks in the formulation sample. Furthermore, the stability studies performed for a duration of 1 month at 45 °C by pXRD and DSC suggested no change in the amorphous nature of the formulation sample.
机译：固体分散体是用于水不溶性药物的成熟的增溶技术。这些基本上是药物-聚合物系统，由于药物-聚合物之间的相互作用更大，因此能够改善水不溶性药物的溶解度和生物利用度。这项研究的目的是利用固体分散体中的这些药物与聚合物的相互作用来开发水溶性药物琥珀酸美托洛尔的缓释剂型。固体分散体是通过溶剂蒸发法制备的，使用了不同比例的药物和速率控制聚合物和脂质赋形剂。药物释放曲线由磷酸盐缓冲溶液（pH 6.8）中的USP仪器1（Basket仪器）确定。通过粉末XRD，FT-IR，DSC和UV光谱等分析方法对固体分散体制剂进行了表征，以检查药物和聚合物之间的无定形性质和氢键相互作用。;在所有研究的制剂中，包含药物/ Methocel RTM的分散体样品重量比为1：1.5：0.5的K 100 Premium LV / Compritol RTM 888 ATO可以提供所需的持续性在所有研究的配方中，分散体样品中含有重量比为1的Drug / Methocel K100 Premium LV / Compritol RTM 888 ATO :: 1.5：0.5在24小时内可提供所需的持续释放曲线。当与纯药物和相同制剂的物理混合物进行比较时，结果表明药物释放得以持续是由于形成了固体分散体，而不仅仅是由于存在速率控制聚合物和脂质赋形剂。为了评估开发这种特定药物制剂的多种强度剂型的可行性，对相当于25 mg，50 mg，100 mg和200 mg的分散粉进行了药物释放曲线测试。数据显示药物释放与分散体制剂中存在的药物量成比例。此外，发现药物释放百分比与时间的关系图几乎重叠。这加强了使用该特定方法和配方可以方便地配制多种剂量强度的主张。pXRD和DSC数据证实了该药物在配方中的无定形性质。 FT-IR数据对于氢键相互作用尚无定论，因为配方样品中的IR吸收峰重叠。此外，pXRD和DSC在45°C下进行了1个月的稳定性研究，结果表明制剂样品的无定形性质没有变化。

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  • 作者

    Renawala, Harshil Kaushik Raksha.;

  • 作者单位

    Long Island University, The Brooklyn Center.;

  • 授予单位 Long Island University, The Brooklyn Center.;
  • 学科 Pharmaceutical sciences.
  • 学位 M.S.
  • 年度 2016
  • 页码 97 p.
  • 总页数 97
  • 原文格式 PDF
  • 正文语种 eng
  • 中图分类
  • 关键词

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