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
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摘要: 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9.93 μg/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。Abstract: To mask the bitterness of azithromycin（AZI） and improve patient compliance, an AZI-loaded microsphere (AZI-EC MS) for oral administration was prepared by O/W emulsion solvent evaporation with ethylcellulose (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), Fourier-transform 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 9.93 μg/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.
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Keywords:
- azithromycin /
- microspheres /
- preparation /
- bitter taste threshold /
- ethylcellulose
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