Spireas S, Wang T, Grover R
Division of Pharmaceutics and Industrial Pharmacy, Arnold and Marie Schwartz College of Pharmacy and Health Sciences, Long Island University, Brooklyn, New York 11201, USA.
Drug Dev Ind Pharm. 1999 Feb;25(2):163-8. doi: 10.1081/ddc-100102156.
The effects of powder substrate composition on the in vitro release properties of methyclothiazide liquisolid compacts were evaluated. The dissolution patterns of this water-insoluble drug formulated in liquisolid tablets were also compared to those of commercial products. According to the new liquisolid technique, liquid medications such as solutions or suspensions of water-insoluble drugs in suitable nonvolatile liquid vehicles can be converted into acceptably flowing and readily compressible powders by a simple admixture with certain powder substrates, which are selected powders referred to as the carrier and coating materials. Enhanced release profiles may be exhibited by such systems due to the increased wetting properties and surface of drug available for dissolution. Liquisolid tablets of methyclothiazide containing a 5% w/w drug solution in polyethylene glycol 400 were prepared using powder substrates of different excipient ratios. The release rates of such products were assessed using the USP dissolution test and were compared to those of their commercial counterparts. It was observed that maximum drug dissolution rates can be exhibited by systems that have powder substrates with optimum carrier-to-coating ratios. In addition, liquisolid tablets displayed significantly enhanced dissolution profiles compared to those of marketed products.
评估了粉末基质组成对甲氯噻嗪液固型制剂体外释放特性的影响。还将这种以液固型片剂形式配制的水不溶性药物的溶出模式与市售产品的溶出模式进行了比较。根据新的液固技术，通过与某些粉末基质简单混合，水不溶性药物在合适的非挥发性液体载体中的溶液或悬浮液等液体药物可以转化为具有可接受流动性且易于压缩的粉末，这些粉末基质是被称为载体和包衣材料的精选粉末。由于润湿性增加以及可用于溶解的药物表面积增大，此类系统可能会呈现出增强的释放曲线。使用不同辅料比例的粉末基质制备了含有5%w/w药物溶液（聚乙二醇400中）的甲氯噻嗪液固型片剂。使用美国药典溶出度试验评估此类产品的释放速率，并将其与市售同类产品的释放速率进行比较。观察到具有最佳载体与包衣比例的粉末基质系统可呈现出最大药物溶出速率。此外，与市售产品相比，液固型片剂的溶出曲线显著增强。
