用于被动肺靶向的异烟肼明胶微球的制备及表征.PDFVIP

·药 剂 · 用于被动肺靶向的异烟肼明胶微球的制备及表征 常江 1,2 ，韩美华 1 ， 阎雪莹 2 ，王向涛 1*(1.中国医学科学院药用植物研究所，北京 100193 ；2.黑龙江中医药大学，哈尔滨 150040) 摘要：目的 用生物可降解材料明胶制备肺靶向异烟肼明胶微球。方法 用乳化法制备异烟肼明胶微球，正交试验优化 其制备的因素；用差示扫描量热法(DSC)和红外光谱法(IR)确证微球的形成；用正置荧光显微镜观察微球的形态；并对异 烟肼明胶微球的粒径及其分布、载药量、包封率和稳定性等进行研究。结果 最佳工艺条件，重现性好，微球形态圆整， 药物确己存于微球中；粒径在 5.0~25.0 μm 的微球占总数的 90% 以上，平均粒径为 15.63 μm ，达到肺靶向要求；载药量 和包封率分别为 14.93%和 73.30% 。常温放置 6 个月，其外观形态、大小及含量基本不变。结论 制备异烟肼明胶微球的 工艺简单稳定，可用于肺靶向注射剂的研究。 关键词：异烟肼；明胶微球；乳化法；肺靶向；差示扫描量热法；红外光谱法 中图分类号：R943.42 文献标志码：A 文章编号：1007-7693(2010)09-0809-05 Preparation and Characterization of Isoniazid Gelatin Microspheres for Passive Lung Targeting CHANG Jiang 1,2 1 2 1* , HAN Meihua , YAN Xueying , WANG Xiangtao (1.Chinese Academy of Medical Sciences Peking Union Medical College Institute of Medicinal Plant Development, Beijing 100193, China; 2.Heilongjiang University of Chinese Medicine, Harbin 150040, China) ABSTRACT: OBJECTIVE Lung targeting gelatin microspheres of isoniazid (INH-GMS) were prepared using the biodegradable materials-gelatin. METHODS INH-GMS were prepared using the emulsifying method and the effect of some factors on the technology was analyzed with the orthogonal test design. The morphology of the microspheres was observed by upright fluorescence microscope. The formation of INH-GMS was confirmed by differential scanning calorimetry (DSC) and infrared spectrometry (IR). The mean diameter and the size distribution, drug-loading rate, entrapment efficiency and stability of INH-GMS were examined. RESULTS INH was developed in microspheres and INH-GMS were regular in morphology. The mean diameter of INH-GMS was 15.63 μm, more than 90% of the INH-GMS ranging from 5.0 μm to 25.0 μm. The drug-loading