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Formulation and evaluation of controlled release ethylcellulose and polyethylene glycol microspheres containing metoprolol tartrate

机译:酒石酸美托洛尔的控释乙基纤维素和聚乙二醇微球的配制与评价

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摘要

Metoprolol tartrate is rapidly absorbed from both gastric and intestinal regions, after oral administration. To retard the release rate of the metoprolol tartrate, microspheres were prepared with varying concentrations of a mixture containing ethylcellulose and polyethylene glycol-6000. The prepared microspheres were evaluated for various physicochemical characteristics and drug release. The percent yield of microspheres was in the range of 75.2-87.3%. The particle size of microspheres was found to be in the range of 73.2-85.5 µm. Fourier transform-infrared spectral analysis and differential scanning calorimetry concluded the absence of any interaction between the drug and the carriers. The release time profile of metoprolol tartrate from microspheres in 0.1 N hydrochloric acid solution was to the extent of 33.4-60.2%. The complete release of metoprolol tartrate occurred from MPT-3 and MPT-4 in phosphate buffer solution (pH 7.4) within 8 and 7 h, respectively, whereas the incomplete release (72.3%) occurred from MPT-1. Nearly, the complete release (98.5%) of metoprolol occurred from MPT-2 in 10 h. Formulation MPT-2 would be a preferred formulation. The release of metoprolol involves diffusion rate limited (R² = 0.9865) as a mechanism from drug release. The prepared microspheres of metoprolol tartrate eliminate the need for multiple dosing and provide patient compliance.
机译:口服后酒石酸美托洛尔从胃和肠区域迅速吸收。为了延迟酒石酸美托洛尔的释放速率,用不同浓度的含有乙基纤维素和聚乙二醇-6000的混合物制备了微球。评价所制备的微球的各种理化特性和药物释放。微球的产率百分比在75.2-87.3%的范围内。发现微球的粒径为73.2-85.5μm。傅立叶变换红外光谱分析和差示扫描量热法得出结论,药物与载体之间不存在任何相互作用。酒石酸美托洛尔在0.1 N盐酸溶液中从微球中的释放时间分布为33.4-60.2%。酒石酸美托洛尔的完全释放分别在磷酸盐缓冲溶液(pH 7.4)中的MPT-3和MPT-4在8 h内发生,而MPT-1的释放不完全(72.3%)。在10小时内,美托洛尔几乎完全从MPT-2中释放出来(98.5%)。制剂MPT-2将是优选的制剂。美托洛尔的释放涉及扩散速率受限(R 2 = 0.9865),这是药物释放的机制。制备的酒石酸美托洛尔微球消除了多次给药的需要,并为患者提供了依从性。

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