用于被动肺靶向的异烟肼明胶微球的制备及表征

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5.0~25.0μm的微球占总数的90%以上,平均粒径为15.63μm,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。

Preparation and Characterization of Isoniazid Gelatin Microspheres for Passive Lung Targeting

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 rate and entrapment efficiency were 14.93% and 73.30% respectively.The repeatability of the technology was good.The content,shape and size of the INH-GMS showed no remarkable change after storage at room temperature for 6 months.CONCLUSION The technology of preparation was successful and the INH-GMS can be used for study of passive lung target.