达托霉素透皮制剂的制备及效果评价  

Preparation and quality analysis of daptomycin transdermal delivery system

作　　者：张晓林[1] 黄兴亮[1] 邓丽[1] 李翀[1] 廖国建[1] 陈章宝[1] 

机构地区：[1]西南大学药学院,重庆400715

出　　处：《中国抗生素杂志》2013年第2期130-134,共5页Chinese Journal of Antibiotics

基　　金："重大新药创制"科技重大专项(2010ZX09401-306-1-4)

摘　　要：目的制备达托霉素软膏,并对其进行制剂学和药效学初步评价。方法采用乳化法制备O/W型和W/O型两种达托霉素软膏。通过考察物理性状、体外透皮渗透率、体内外药效学及抗细菌生物被膜,确定较优处方并初步建立达托霉素软膏剂透皮实验方法。结果 O/W型达托霉素软膏的累积渗透率在8h时达53.35%,透皮渗透量为78.30μg/cm2。与W/O型达托霉素软膏相比具有更强的抑菌作用。结论 O/W型达托霉素软膏制备工艺简单,制剂稳定性好,抑菌快速强效。Objective To investigate the preparation and quality analysis of daptomycin ointment with good bacteriostasis efficacy. Methods Two types of daptomycin ointment were prepare by O/W and W/O emulsion process. The optimized prescription of daptomycin ointment was obtained and evaluated by a series of factors including physical behaviors, transdermal experiments in vitro, transdermal antibacterial experiments in vitro, antibiofilm in vitro and pharmacodynamics experiment. Result The cumulative release rate of O/W daptomycin ointment was 53.35% after 8 hours. The O/W ointment of daptomycin has shown priority over the W/O formulation in antibacterial effect. Conclusion The results demonstrated the advantages of the O/W daptomycin ointment： simple preparation process, good stability, fast and potent antibacterial activity.

关 键 词：达托霉素 软膏剂 透皮制剂 生物被膜 

分 类 号：R978.1[医药卫生—药品]