Javadzadeh Yousef, Siahi Mohammad Reza, Asnaashari Solmaz, Nokhodchi Ali
Department of Pharmaceutics, Faculty of Pharmacy, Tabriz University of Medical Sciences, Iran.
Pharm Dev Technol. 2007;12(3):337-43. doi: 10.1080/10837450701247574.
The potential of liquisolid systems to improve the dissolution properties of a water-insoluble agent (piroxicam) was investigated. In this study, physicochemical properties of piroxicam liquisolid tablets, effect of aging, and type of the carrier were also investigated. To this end, several liquisolid tablets formulations containing various ratios of drug: solvent and different carriers were prepared. X-ray crystallography, differential scanning calorimetry (DSC), and contact angle measurement were used for evaluation of physicochemical properties of piroxicam. Liquisolid compacts exhibited significantly higher drug dissolution rates, in different dissolution media, than compacts prepared by the direct compression technique. The results showed that enhanced dissolution rate of piroxicam liquisolid tablets was due to an increase in wetting properties and surface area of drug available for dissolution. To investigate the effect of aging on the hardness and dissolution rate of liquisolid compacts, the formulations were stored at 25 degrees C/75% relative humidity for 9 months. The results showed that aging had no significant effect on hardness or dissolution profile of liquisolid tablets. It was shown that Avicel had more liquid retention potential than other carriers, but there were no significant differences in the dissolution profiles between formulations. The results of DSC and X-ray crystallography did not show any changes in crystallinity of the drug and interaction between piroxicam and exipients (Avicel and silica) during the process.
研究了液固系统改善水不溶性药物（吡罗昔康）溶出性能的潜力。在本研究中，还考察了吡罗昔康液固片的物理化学性质、老化的影响以及载体类型。为此，制备了几种含有不同药物:溶剂比例和不同载体的液固片制剂。采用X射线晶体学、差示扫描量热法（DSC）和接触角测量法来评估吡罗昔康的物理化学性质。在不同的溶出介质中，液固型片剂的药物溶出速率显著高于直接压片法制备的片剂。结果表明，吡罗昔康液固片溶出速率的提高归因于润湿性的增加和可用于溶出的药物表面积的增加。为了研究老化对液固型片剂硬度和溶出速率的影响，将制剂在25℃/75%相对湿度下储存9个月。结果表明，老化对液固片的硬度或溶出曲线没有显著影响。结果表明，微晶纤维素比其他载体具有更强的液体保留能力，但不同制剂之间的溶出曲线没有显著差异。DSC和X射线晶体学结果未显示该过程中药物的结晶度以及吡罗昔康与辅料（微晶纤维素和二氧化硅）之间的相互作用有任何变化。
