| abstract |
PURPOSE:To obtain the titled composite, by dissolving a hardly water-soluble drug and a phospholipid in an organic solvent, distilling off the solvent to form a thin film of phospholipid containing the drug, treating the film with ultrasonic wave, centrifuging the treated product, and recovering the bottom precipitate. CONSTITUTION:A hardly water-soluble drug having a water-solubility of <=0.1mg/ml (e.g. spadicomycin, anthramycin, fluorouracil, etc.) and a phospholipid (e.g. phosphatidylcholine, phosphatidylserine, soybean phospholipid, yolk phospholipid, etc.) are dissolved in an organic solvent such as chloroform. The amount of the hardly water-soluble drug is preferably 0.01-10pts.wt. per 1pt.wt. of the phospholipid. A phospholipid thin film containing the drug is formed by distilling off the solvent, the suspension of the thin film is treated with ultrasonic wave and centrifuged, and the obtained bottom precipitate is recovered to obtain the objective composite of the hardly water-soluble drug and the phospholipid. The activity of the drug increases several times - several tens times by the solubilization effect, and a unusually effective drug preparation can be prepared. |