肺靶向硫酸链霉素明胶微球的制备

The preparation of streptomycin sulfate gelatin microspheres for lung targeting

目的:用生物可降解材料明胶制备肺靶向硫酸链霉素明胶微球。方法:用乳化法制备微球,正交试验设计考察影响制备工艺的因素,用扫描电子显微镜观察微球表面形态,用红外光谱分析确证含药微球的形成。并对所制备的硫酸链霉素明胶微球的粒径及其分布、载药量、包封率、稳定性等进行了研究。结果:微球形态圆整,药物确己存于微球中。微球的平均粒径为12.269μm,粒径在5.0～25.0μm的微球占总数的91.5%,达到肺靶向要求。载药量为42.6%,包封率为53.8%。最佳工艺条件重现性好。经37℃、RH75%放置3个月,其含量、外观形态及大小基本不变。结论:该微球制备工艺稳定,可用于肺靶向注射剂的研究。

OBJECTIVE The purpose is to optimize the preparation of lung targeting microspheres of streptomycin sulfate using the biodegradable materials-gelatin. METHODS The gelatin microspheres of streptomycin sulfate （SMS-GMS） were prepared with the emulsifying method and some factors effecting the technology were analyzed with the orthogonal test design. The surface morphology of the microspheres was observed by SEM. The formation of the drug microspheres was confirmed by FTIR The mean diameter and the size distribution of microspheres, the drug-loading rate, the entrapment rate and stability were examined. RESULTS The SMS-GMS were regular in their morphology, drug was enveloped in microspheres. The data showed that the mean diameter of SMS-GMS was 12. 269μm,with 91.5% of the microspheres ranging from 5. 0μm to 25. 0μm. The drug-loading rate and the entrapment rate were 42. 6% and 53. 8%. The repeatability of the technology was good. The content, shape and size of the microspheres showed no remarkable change after storage at 37 ℃ ,RH 75 % for 3 months. CONCLUSION The technology of preparation was successful and the SMS-GMS can be used for study of lung target.