用于肺部靶向的红霉素微球的制备及特性。

Preparation and characteristics of erythromycin microspheres for lung targeting.

机构信息

Department of Pharmacy, Guangdong Pharmaceutical University, Guangzhou, PR China.

出版信息

Drug Dev Ind Pharm. 2009 Jun;35(6):639-45. doi: 10.1080/03639040802512243.

DOI:10.1080/03639040802512243

PMID:19259878

Abstract

BACKGROUND

If erythromycin is micronized into microspheres with suitable particle size, it can improve pulmonary drug concentration to maximize its effectiveness and minimize the adverse side effects.

AIM

In this study, erythromycin gelatin microspheres (EM-GMS) were prepared and some characteristics of EM-GMS were investigated. The drug-targeting index (DTI) of EM-GMS was evaluated to predict their potential as a targeted delivery system.

METHOD

Erythromycin was microencapsulated with gelatin by a double emulsion solvent evaporation method. Some characteristics of EM-GMS, including morphology, particle size, in vitro release, and safety were researched.

RESULTS

EM-GMS had a spherical shape and smooth surface morphology. The drug loading and encapsulation efficiency of EM-GMS were 13.56 +/- 0.25% and 55.82 +/- 2.23%, respectively. The release of erythromycin from EM-GMS showed an initial burst and following a sustained release, with an accumulate release of 80% at 4 hours. The EM-GMS was safe since there was no vein irritation and no hemolysis on the erythrocyte of rabbit at 3.5 mg/mL and a LD50 of 173.07 mg/kg. After administering EM-GMS to rabbits, the concentration of erythromycin in lung was 15.92 times higher than that in plasma and the DTI of EM-GMS in lung was 6.65 as compared with erythromycin lactobionate.

CONCLUSIONS

The preparation technology of EM-GMS for lung targeting was successful and the quality of microspheres was good.

摘要

背景

如果将红霉素制成具有合适粒径的微球，可以提高肺部的药物浓度，最大限度地发挥其疗效，最大限度地减少不良反应。

目的

本研究制备红霉素明胶微球（EM-GMS），并考察 EM-GMS 的部分特性，评估其作为靶向给药系统的药物靶向指数（DTI），预测其潜在应用价值。

方法

采用复乳溶剂蒸发法，以明胶为囊材，包封红霉素。考察 EM-GMS 的形态、粒径、体外释放和安全性等特性。

结果

EM-GMS 呈球形，表面光滑。EM-GMS 的载药量和包封率分别为 13.56%±0.25%和 55.82%±2.23%。EM-GMS 中红霉素的释放呈现初期突释和后期持续释放的特点，4 小时累积释放 80%。EM-GMS 安全性良好，兔静脉注射 3.5mg/mL 时无静脉刺激性，对兔红细胞无溶血作用，LD50 为 173.07mg/kg。兔肺部给予 EM-GMS 后，肺组织中红霉素浓度是血浆中的 15.92 倍，肺组织中的 DTI 为 6.65，均显著高于红霉素乳糖酸盐。