Prodduturi Suneela, Manek Rahul V, Kolling William M, Stodghill Steven P, Repka Michael A
Department of Pharmaceutics, School of Pharmacy, The University of Mississippi, University, Mississippi 38677, USA.
J Pharm Sci. 2004 Dec;93(12):3047-56. doi: 10.1002/jps.20222.
Hot-melt extrusion technology was used to prepare thin polymer films containing hydroxypropyl cellulose and clotrimazole (CT). Films containing hydroxypropyl celluloses of different molecular weight and the drug were investigated for moisture-sorption, mechanical properties, and release characteristics. Stability of the films was also studied at 25 degrees C/60% relative humidity (RH) and 40 degrees C/75% RH for up to 3 months. To study the moisture-sorption of the hot-melt extruded films, a rapid dynamic vapor sorption technique was used. Mechanical properties were evaluated using the Texture Analyzer. The molecular weight of the polymer had a significant effect on the mechanical and release characteristics of the films but did not influence the equilibrium moisture content in the films stored at RHs ranging from 0 to 90%. However, the time to reach equilibrium was longer for the higher molecular weight polymers. The drug release rate was dependent on the rate of erosion, which in turn depended on the molecular weight of the polymer. The films were stable at 25 degrees C/60% RH for up to 3 months with no significant degradation or recrystallization of CT. However, recrystallization of the drug was observed within the films stored in accelerated stability conditions at the end of 3 months in which only 92.9% (+/-1.9) CT remained.
采用热熔挤出技术制备了含羟丙基纤维素和克霉唑（CT）的聚合物薄膜。研究了含不同分子量羟丙基纤维素和药物的薄膜的吸湿性能、力学性能及释放特性。还在25℃/60%相对湿度（RH）和40℃/75%RH条件下对薄膜稳定性进行了长达3个月的研究。为研究热熔挤出薄膜的吸湿性能，采用了快速动态蒸汽吸附技术。使用质构分析仪评估力学性能。聚合物的分子量对薄膜的力学和释放特性有显著影响，但对在0至90%RH范围内储存的薄膜的平衡水分含量没有影响。然而，较高分子量聚合物达到平衡的时间更长。药物释放速率取决于侵蚀速率，而侵蚀速率又取决于聚合物的分子量。薄膜在25℃/60%RH条件下稳定长达3个月，CT没有明显降解或重结晶。然而，在加速稳定性条件下储存3个月结束时，薄膜内观察到药物重结晶，此时仅剩余92.9%（±1.9）的CT。
