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首页> 外文期刊>International Journal of Pharmaceutical and Life Sciences >Dissolution enhancement of poorly soluble drug by solvent evaporation method using hydrophilic polymer: a solid dispersion technique
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Dissolution enhancement of poorly soluble drug by solvent evaporation method using hydrophilic polymer: a solid dispersion technique

机译:使用亲水性聚合物的溶剂蒸发法提高难溶性药物的溶出度:固体分散技术

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In order to investigate the effect of polymers on release mechanism of poorly soluble drugs from solid dispersions, Clonazepam was used as a model drug for these purposes. Five types of solid dispersions were prepared using polyethylene glycol 6000 (PEG- 6000), Kollicoat IR, Kollidon VA 64 and Poloxomer in different drug-tocarrier ratios (1:2, 1:4, 1:6, 1:8, 1:10). The solvent evaporation method was used for preparation of solid dispersions. The in-vitro dissolution study with temperature of 37° C and a paddle method, 100 rpm was used in 1000 ml of distilled water as dissolution medium in each dissolution basket for the pure drug and solid dispersions. For pure Clonazepam showed very slow dissolution rate and the solid dispersion considerably enhanced the dissolution rate. Decreased crystalline and increased amorphous fraction of the drug was probably done by wettability and dispersibility. The highest improvement in wettability and dissolution rate of Clonazepam was observed in PEG-6000, Poloxomer and Kollidon VA 64 (1:10 ratio). Solid dispersions containing polymer (1:10 ratio) prepared by solvent method showed significant improvement in the release profile as compared to pure drug, Clonazepam. DOI: http://dx.doi.org/10.3329/ijpls.v1i2.12952 International Journal of Pharmaceutical and Life Sciences Vol.1(2) 2012
机译:为了研究聚合物对难溶性药物从固体分散体中释放的机理的影响,氯硝西am被用作这些目的的模型药物。使用聚乙二醇6000(PEG-6000),Kollicoat IR,Kollidon VA 64和Poloxomer以不同的药物-载体比率(1:2、1:4、1:6、1:8、1:1)制备五种类型的固体分散体10)。溶剂蒸发法用于制备固体分散体。在37°C温度和桨式方法的体外溶出研究中,将100 rpm的溶液用于1000 ml蒸馏水中,作为每个溶出篮中纯药物和固体分散体的溶出介质。对于纯氯硝西am显示出非常慢的溶解速率,并且固体分散体显着提高了溶解速率。药物的结晶度降低和无定形含量增加可能是通过润湿性和分散性来实现的。在PEG-6000,Poloxomer和Kollidon VA 64(比例为1:10)中观察到了氯硝西wet在润湿性和溶出度方面的最高改善。与纯药物氯硝西compared相比,通过溶剂法制备的含聚合物的固体分散体(比例为1:10)显示出释放特性的显着改善。 DOI:http://dx.doi.org/10.3329/ijpls.v1i2.12952国际药学与生命科学杂志Vol.1(2)2012

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