本文選題：阿奇霉素 + β-環(huán)糊精及其衍生物�。� 參考：《中國醫(yī)藥工業(yè)雜志》2015年08期

【摘要】：為提高阿奇霉素(1)的溶解度和溶出度,采用飽和溶液法制備1的β-環(huán)糊精(β-CD)或其衍生物(羥丙基-β-環(huán)糊精、甲基-β-環(huán)糊精和2,6-二甲基-β-環(huán)糊精)包合物,并以正交設(shè)計優(yōu)化了包合工藝。熔點法、紅外光譜、掃描電鏡分析結(jié)果證實1被β-CD及其衍生物包合�？疾炝藘�(yōu)化所得4種包合物的包合率、溶解度和溶出度。結(jié)果表明,包合物的溶解度和溶出度均顯著高于1原藥及物理混合物,但包合率偏低(55.6%~60.5%)。其中,2,6-二甲基-β-環(huán)糊精對增大1的溶解度和溶出度的效果最顯著。25℃時1的2,6-二甲基-β-環(huán)糊精包合物的溶解度為1 016.5mg/ml,是原藥(34.2mg/ml)的29.7倍;在pH 6.8磷酸鹽緩沖液中180 min的溶出率約為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，

本文編號：1945346