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ENHANCEMENT OF ORAL BIOAVAILABILITY AND DISSOLUTION RATE OF ACECLOFENAC USING SOLID DISPERSIONS BY DROPPING METHOD

机译:滴加固体分散剂增强口服苯环戊酸的生物利用度和溶出率

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In the present study, the aim was to enhance the oral bioavailability and dissolution rate of aceclofenac by solid dispersions using polyethylene glycol (PEG-6000) as a carrier and to study the effect of carrier on dissolution rate. Initial studies were carried out using physical mixtures of the drug and carrier. Solid dispersions were prepared by fusion technique using dropping method. Aceclofenac was formulated as physical mixtures and solid dispersions (dropping method) using 1:2, 1:4,1:6 and 1:8 ratios of drug and carrier (PEG 6000). Saturation solubility study for pure drug, physical mixtures and solid dispersions were carried out in water and pH 6.8 phosphate buffer solutions (PBS). The In vitro dissolution studies were carried in pH 6.8, higher in vitro dissolution of solid dispersions was recorded compared to their corresponding physical mixtures and the pure drug. The prepared solid dispersions were observed that increased in the saturation solubility and dissolution rate of aceclofenac than that of pure drug. PEG 6000 in 1: 8 drug to carrier ratio exhibited the highest drug release (98.69%) formulated as solid dispersions using dropping method. The FT-IR study shows that drug was stable in solid dispersions and there were no interactions. It is concluded that dissolution rate was improved by solid dispersion of aceclofenac: PEG 6000 prepared as 1:8 ratio by dropping method showed excellent physicochemicai characteristics and was found to be described by dissolution release kinetics and was selected as the best formulation.
机译:在本研究中,目的是通过以聚乙二醇(PEG-6000)为载体的固体分散体提高醋氯芬酸的口服生物利用度和溶解速率,并研究载体对溶解速率的影响。使用药物和载体的物理混合物进行了初步研究。使用滴注法通过熔融技术制备固体分散体。使用药物和载体(PEG 6000)的1:2、1:4、1:6和1:8比例将醋氯芬酸配制成物理混合物和固体分散体(滴加法)。在水和pH 6.8磷酸盐缓冲溶液(PBS)中进行了纯药物,物理混合物和固体分散体的饱和溶解度研究。在pH 6.8下进行了体外溶出度研究,与相应的物理混合物和纯药物相比,固体分散体的溶出度更高。观察到制备的固体分散体与纯药物相比,醋氯芬酸的饱和溶解度和溶解速率增加。以滴加法配制为固体分散体的药物与载体的比例为1:8的PEG 6000表现出最高的药物释放(98.69%)。 FT-IR研究表明药物在固体分散体中是稳定的,没有相互作用。结论是通过滴加法以1:8的比例制备醋氯芬酸:PEG 6000固体分散体可提高溶出速率,显示出优异的理化特性,并被溶出释放动力学描述,被选为最佳制剂。

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