β-环糊精及其衍生物对阿奇霉素的溶解度及溶出度的影响

发布时间：2018-05-28 04:40

  本文选题：阿奇霉素 + β-环糊精及其衍生物　； 参考：《中国医药工业杂志》2015年08期

【摘要】：为提高阿奇霉素(1)的溶解度和溶出度,采用饱和溶液法制备1的β-环糊精(β-CD)或其衍生物(羟丙基-β-环糊精、甲基-β-环糊精和2,6-二甲基-β-环糊精)包合物,并以正交设计优化了包合工艺。熔点法、红外光谱、扫描电镜分析结果证实1被β-CD及其衍生物包合。考察了优化所得4种包合物的包合率、溶解度和溶出度。结果表明,包合物的溶解度和溶出度均显著高于1原药及物理混合物,但包合率偏低(55.6%~60.5%)。其中,2,6-二甲基-β-环糊精对增大1的溶解度和溶出度的效果最显著。25℃时1的2,6-二甲基-β-环糊精包合物的溶解度为1 016.5mg/ml,是原药(34.2mg/ml)的29.7倍;在pH 6.8磷酸盐缓冲液中180 min的溶出率约为90%。
[Abstract]:In order to improve the solubility and dissolution of azithromycin 1, the inclusion complexes of 尾 -cyclodextrin (尾 -CD1) or its derivatives (hydroxypropyl- 尾 -cyclodextrin, methyl- 尾 -cyclodextrin and 2-dimethyl- 尾 -cyclodextrin) were prepared by saturated solution method. The inclusion process was optimized by orthogonal design. Melting point method, IR spectrum and SEM analysis confirmed that 1 was encapsulated by 尾 -CD and its derivatives. The inclusion rate, solubility and dissolution of the four optimized inclusion complexes were investigated. The results showed that the solubility and dissolution of the inclusion compound were significantly higher than that of the original drug and physical mixture, but the inclusion rate was lower than 55.6% and 60.5%. The solubility of the inclusion compound of 1 was 1016.5 mg / ml, 29.7 times as much as that of the original drug 34.2 mg / ml, and the solubility of the inclusion complex was 1016.5 mg / ml and 29.7 times as much as that of the original drug (34.2 mg / ml). The solubility of the inclusion complex of 1 was significantly higher than that of the original drug (34.2 mg / ml) at the temperature of .25 鈩，

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