Dangi J S, Vyas S P, Dixit V K
Department of Pharmaceutical Sciences, Doctor Harisingh Gour Vishwavidyalaya, Sagar, India.
Drug Dev Ind Pharm. 1998 Jul;24(7):631-5. doi: 10.3109/03639049809082364.
Amphotericin-B (AmB), a lipophilic polyene antibiotic, is the drug of choice in the treatment of many serious mycotic diseases. The solubility and gastrointestinal membrane permeability (Papp) of AmB in mixed micellar systems were examined. Membrane permeability was determined using a rat gut perfusion method. The mixed micellar systems studied contained the bile salt in association with fatty acid. All mixed micellar systems enhanced the absorption of AmB relative to the simple micelle. These results have shown that mixed micelles can enhance the absorption of AmB to a greater extent relative to nonmicellar and simple micellar systems. Maximum enhancement (> 20-fold) in the rate of AmB absorption was obtained with the sodium desoxycholate/soya lecithin 40:40 mM system. These results offer a possible explanation for the reported enhancement in gastrointestinal absorption of AmB when coadministered with lipid-bile salt mixed micelles, and these systems can be used as a vehicle for designing novel drug delivery systems for poorly absorbable drug(s).
两性霉素B（AmB）是一种亲脂性多烯抗生素，是治疗许多严重真菌病的首选药物。研究了AmB在混合胶束体系中的溶解度和胃肠膜通透性（表观渗透系数）。采用大鼠肠道灌注法测定膜通透性。所研究的混合胶束体系含有与脂肪酸结合的胆盐。相对于简单胶束，所有混合胶束体系均增强了AmB的吸收。这些结果表明，相对于非胶束和简单胶束体系，混合胶束能更大程度地增强AmB的吸收。在脱氧胆酸钠/大豆卵磷脂40:40 mM体系中，AmB吸收速率得到最大增强（>20倍）。这些结果为报道的AmB与脂质-胆盐混合胶束共同给药时胃肠吸收增强提供了一种可能的解释，并且这些体系可作为设计难吸收药物新型给药系统载体。
