Repka Michael A, Prodduturi Suneela, Stodghill Steven P
Department of Pharmaceutics, School of Pharmacy, The University of Mississippi, University, Mississippi 38677-1848, USA.
Drug Dev Ind Pharm. 2003 Aug;29(7):757-65. doi: 10.1081/ddc-120021775.
Hot-melt extrusion technology (HME) was used to prepare muco-adhesive matrix films containing 10% w/w clotrimazole (CT) intended for local drug delivery applications for the oral cavity. This study was aimed at the production and characterization of these drug delivery systems for the prophylaxis and treatment of oral candidiasis. The film system's formulation contained hydroxypropyl cellulose and poly(ethylene oxide) as polymeric carriers, the bioadhesive polycarbophil, and other excipients. The CT formulation was processed at a temperature range of 125-130 degrees C utilizing a Killion extruder (Model KLB-100) equipped with a 6-inch flex-lip die. The films were evaluated for postextrusion drug content, physical and chemical content uniformity, drug release, thermal and crystalline behavior, and bioadhesive strength. The extruded films demonstrated excellent content uniformity and a postprocessing drug content of 93.3% (+/- 1.0). The degradation product, (o-chlorophenyl)diphenyl methanol, was also identified and quantitated using high performance liquid chromatography. The films were determined to exhibit desirable and consistent release properties and bioadhesive strength (p < 0.05). The results of this study indicate that HME is a viable technique for the preparation of muco-adhesive films containing clotrimazole for oral candidiasis.
热熔挤出技术（HME）被用于制备含10%（w/w）克霉唑（CT）的粘膜粘附基质膜，旨在用于口腔局部给药。本研究旨在生产和表征这些用于预防和治疗口腔念珠菌病的药物递送系统。该膜系统配方包含羟丙基纤维素和聚环氧乙烷作为聚合物载体、生物粘附性聚卡波非以及其他辅料。利用配备6英寸挠性唇模的Killion挤出机（型号KLB - 100）在125 - 130摄氏度的温度范围内对CT配方进行加工。对这些膜进行了挤出后药物含量、物理和化学含量均匀性、药物释放、热行为和结晶行为以及生物粘附强度的评估。挤出的膜显示出优异的含量均匀性，后处理药物含量为93.3%（±1.0）。还使用高效液相色谱法对降解产物（邻氯苯基）二苯基甲醇进行了鉴定和定量。这些膜被确定具有理想且一致的释放特性和生物粘附强度（p < 0.05）。本研究结果表明，热熔挤出技术是制备含克霉唑的粘膜粘附膜用于口腔念珠菌病的可行技术。
