黄日, 王涛, 杨茜, 全东琴, 王阳. 阿奇霉素掩味干乳的表征及体内外评价J. 药学学报, 2017,52(5): 795-801. doi: 10.16438/j.0513-4870.2016-1214
引用本文: 黄日, 王涛, 杨茜, 全东琴, 王阳. 阿奇霉素掩味干乳的表征及体内外评价J. 药学学报, 2017,52(5): 795-801. doi: 10.16438/j.0513-4870.2016-1214
HUANG Ri, WANG Tao, YANG Xi, QUAN Dong-qin, WANG Yang. Characterization of taste-masking dry emulsion of azithromycin by in vitro and in vivo evaluationJ. Acta Pharmaceutica Sinica, 2017,52(5): 795-801. doi: 10.16438/j.0513-4870.2016-1214
Citation: HUANG Ri, WANG Tao, YANG Xi, QUAN Dong-qin, WANG Yang. Characterization of taste-masking dry emulsion of azithromycin by in vitro and in vivo evaluationJ. Acta Pharmaceutica Sinica, 2017,52(5): 795-801. doi: 10.16438/j.0513-4870.2016-1214

阿奇霉素掩味干乳的表征及体内外评价

Characterization of taste-masking dry emulsion of azithromycin by in vitro and in vivo evaluation

  • 摘要: 研制阿奇霉素儿科用掩味口服制剂,采用脂质纳米反胶束技术掩蔽药物的苦味,再以胶态二氧化硅固化含药油溶液制备掩味干乳。通过染色实验证明了干乳处方中油相均匀分散,进一步结合扫描电镜对其进行评价。采用X-射线粉末衍射及扫描电镜测定固体粉末中药物的结晶状态,激光粒度测定仪和透射电镜考察再分散乳滴的粒径大小及其形态特征。通过口腔模拟释放实验和志愿者口尝对制剂掩味效果进行评价,并对制剂进行肠黏膜刺激性评价。结果表明,制备的掩味干乳再分散乳滴平均粒径为530.1nm,混悬后再分散性良好,混悬液外观均一。与上市制剂希舒美相比,相同剂量下掩味效果相近且肠黏膜刺激性较小,具有很好的发展前景。

     

    Abstract: To develop a taste-masking oral preparation of azithromycin for pediatrics, the reversed lipid nano-micelle techniques were used to mask the bitterness of azithromycin. Dry emulsion (DE) for taste-masking was prepared by solidifying the reversed-micelle oil solution containing azithromycin. Colloidal silicon dioxide was used as absorbent and solid carrier. Solidification was confirmed through dying test and observed by scanning electron microscope (SEM). The DE formulation was characterized by X-ray powder diffraction and SEM in order to investigate the crystal state of drug. Reconstitution emulsion droplet size and morphology were also determined using Nano ZS90 Zetasizer and transmission electron microscopy (TEM). The taste testing was performed in two different ways, namely, human taste panel test and the measurement of the amount of drug released in simulated oral cavity condition. The intestinal mucosal irritation test of DE formulation was also investigated in rats in comparison with commercial product (Zithromax). The optimal taste-masking formulation of azithromycin can be re-dispersed immediately with mean diameter of 530.1 nm after agitation in water. The results of taste testing showed that the bitterness of azithromycin was successfully masked by DE formulation similar with Zithromax at the same dose, moreover reduced intestinal irritation compared to Zithromax. These results indicate that the DE formulation for taste-masking of azithromycin is promising and valuable in the future development of azithromycin for pediatrics.

     

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