液体固体粉剂提高吡罗昔康溶出率

Y. Javadzadeh , M.R. Siahi-Shadbad , M. Barzegar-Jalali , A. Nokhodchi
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引用次数: 189

摘要

吡罗昔康是一种难溶性、高渗透性的药物,其口服吸收率通常受其在胃肠道中的溶出率控制。水不溶性药物溶出率差仍然是制药行业面临的主要问题。有几种技术可以提高难溶性药物的溶出度。其中,液相压实技术是实现这一新目标的一种很有前途的技术。在这项研究中,研究了吡罗昔康在模拟胃液(SGF, pH 1.2)和模拟肠液(SIF, pH 7.2)中的溶出行为。为此,制备了几种含有不同比例药物Tween 80(范围为10%至50% w/w)的液体固体片剂配方。在所有配方中,微晶纤维素(载体)与二氧化硅(涂层粉末材料)的比例保持恒定。结果表明,液体固体制剂的释药速度明显高于常规制剂(微颗粒吡罗昔康胶囊和直接压缩片剂)。这是由于润湿性能和药物表面可溶性的增加。
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Enhancement of dissolution rate of piroxicam using liquisolid compacts

Piroxicam is a poorly soluble, highly permeable drug and the rate of its oral absorption is often controlled by the dissolution rate in the gastrointestinal. The poor dissolution rate of water-insoluble drugs is still a major problem confronting the pharmaceutical industry. There are several techniques to enhance the dissolution of poorly soluble drugs. Among them, the technique of liquisolid compacts is a promising technique towards such a novel aim. In this study, the dissolution behaviour of piroxicam from liquisolid compacts was investigated in simulated gastric fluid (SGF, pH 1.2) and simulated intestinal fluid (SIF, pH 7.2). To this end, several liquisolid tablets formulations containing various ratios of drug:Tween 80 (ranging from 10% to 50% w/w) were prepared. The ratio of microcrystalline cellulose (carrier) to silica (coating powder material) was kept constant in all formulations. The results showed that liquisolid compacts demonstrated significantly higher drug release rates than those of conventionally made (capsules and directly compressed tablets containing micronized piroxicam). This was due to an increase in wetting properties and surface of drug available for dissolution.

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