阿奇霉素口服微球的制备及其评价

Preparation and evaluation of azithromycin-loaded microspheres for oral administration

为改善阿奇霉素(AZI)苦味与服药顺应性,以乙基纤维素(EC)为载体,采用O/W乳化溶剂挥发法制备载阿奇霉素口服微球(AZI-EC MS),对其释放与掩味效果进行初步考察,并通过差式扫描量热法、红外光谱和扫描电镜表征。通过联合应用不同相对分子质量EC解决了微球突释问题,当药载质量比1∶1、混合EC(N22/T10,7∶3)为载体时,微球0.5 h累积释放量小于40%,8 h累积释放量可达90%;该微球载药量为(48.95±0.86)%,形态圆整,表面光滑。AZI味道极苦,苦味阈值浓度为9.93μg/mL,所制备的AZI-EC MS掩味效果良好。结果表明,混合EC为载体的AZI-EC MS能够改善AZI苦味,提高患者顺应性,为AZI新制剂的研究开发奠定基础。

To mask the bitterness of azithromycin(AZI)and improve patient compliance,an AZI-loaded micro⁃sphere(AZI-EC MS)for oral administration was prepared by O/W emulsion solvent evaporation with ethylcellu⁃lose(EC)as carrier.The release profiles and taste-masking effect of AZI-EC MS were preliminarily assessed.Its physical properties and morphology were then investigated by differential scanning calorimetry(DSC),Fouriertransform infrared spectroscopy(FTIR)and scanning electron microscope(SEM).The results indicated that the polymer weight of EC could influence the drug release behavior.With a drug polymer ratio of 1∶1 and mixed EC(N22/T10,7∶3)as carrier,the cumulative release of AZI-EC MS at 0.5 h was less than 40%and reached 90%at 8 h;the drug loading efficiency of microspheres was(48.95±0.86)%with smooth spherical morphology.The AZI bitterness threshold is 9.93μg/mL with a strong bitter taste,which indicated a better taste masking effect.Therefore,AZI-EC MS prepared in this study can mask AZI bitterness and improve patient compliance,setting the stage for the research of new AZI preparations.