喷雾干燥氯诺昔康自微乳化制剂的制备及理化性质

测定氯诺昔康在含有不同量氨丁三醇的自微乳化释药系统(SMEDDS)中的溶解度,在乳糖、蔗糖和甘露醇中筛选喷雾干燥用载体及其适宜用量,制备喷雾干燥氯诺昔康自微乳化制剂,对其粒径、形态、溶出、流变性及再分散性质进行考察。结果表明:氨丁三醇的适宜用量为10 mg/g时,可将氯诺昔康载药量从7.2 mg/g提高至23.8 mg/g。适宜的载体为甘露醇,与液体SMEDDS的质量比为1∶1。喷雾干燥自微乳化粉末为近球形,具有良好的自微乳化特性,再分散后得到塑性非牛顿流体,粒径约为120 nm。固体自微乳化粉末的溶出速度在3种介质中的溶出度均极显著高于氯诺昔康片(P<0.01),具有非pH依赖性的快速溶出行为。

Preparation and physicochemical characterization of a spray-dried lornoxicam self-microemulsifying system

The solubility of lornoxicam in liquid self-microemulsifying drug delivery system(SMEDDS) containing different amounts of tromethamine was determined.The carrier for spray drying was selected from lactose,sucrose and mannitol and its appropriate amount was optimized.The obtained spray-dried lornoxicam self-microemulsifying powder was characterized by particle size,morphology,dissolution and rheological behavior.The appropriate amount of tromethamine was 10 mg/g and the solubility of lornoxicam was enhanced to be 23.8 mg/g.The suitable carrier for achieving the spray drying process was mannitol with the weight ratio of 1 ∶1 to liquid SMEDDS.The spray dried SMEDDS powder was nearly spherical powder with good self-microemulsifying properties.The reconstituted emulsion was determined to be a plastic non-Newtonian fluid with the particle size of about 120 nm.The solid spray-dried lornoxicam self-microemulsifying system had significantly higher dissolution than lornoxicam tablets in three media and its dissolution profile was demonstrated to be rapid and pH-independent.