Sznitowska Malgorzata, Dabrowska Ewa A, Janicki Stanislaw
Department of Pharmaceutical Technology, Medical University of Gdansk, ul.Hallera 107, Poland.
Int J Pharm. 2002 Oct 10;246(1-2):203-6. doi: 10.1016/s0378-5173(02)00395-2.
Aqueous lecithin dispersions (WLD, water-lecithin-dispersion) were obtained by dispersing egg lecithin (1.2 or 2.4% w/w) in an isotonic mixture of glycerol and water. The solubilization potential of the pure phospholipid structures was investigated and compared with that of submicron emulsions containing the same amounts of lecithin and 10 or 20% (w/w) of soya-bean oil. The increase in solubility of the investigated lipophilic drugs in WLD was proportional to the lecithin concentration. Concentration of lecithin in the emulsion was the main factor determining solubility of drugs moderately lipophilic (logP below 2.5), while for more lipophilic compounds the presence of oil was a determinant and for such drugs solubility in submicron emulsion was better than in WLD. WLD obtained in a simple technological process may be considered as a carrier particularly for highly lipophilic drugs: solubility of estradiol in this system was 100-fold higher than in water.
通过将卵磷脂(1.2%或2.4% w/w)分散在甘油和水的等渗混合物中,获得水相卵磷脂分散体(WLD,水-卵磷脂分散体)。研究了纯磷脂结构的增溶潜力,并将其与含有相同量卵磷脂和10%或20%(w/w)大豆油的亚微米乳液的增溶潜力进行比较。所研究的亲脂性药物在WLD中的溶解度增加与卵磷脂浓度成正比。乳液中卵磷脂的浓度是决定中等亲脂性药物(logP低于2.5)溶解度的主要因素,而对于亲脂性更强的化合物,油的存在是一个决定因素,对于此类药物,其在亚微米乳液中的溶解度优于在WLD中的溶解度。通过简单工艺过程获得的WLD可被视为一种载体,特别是对于高亲脂性药物:雌二醇在该体系中的溶解度比在水中高100倍。