| 摘要 |
1. A method for preparing lipid complexes or liposomes of a water-insoluble platinum diaminocyclohexanedicarboxylate by adding to aqueous solution of platinum diaminocyclohexanenitrate a phospholipid solution in a non-aqueous solvent and a dicarboxylic acid; with further removing said non-aqueous solvent. 2. The method of Claim 1 wherein said platinum diaminocyclohexanedicarboxylate is a compound of the formula: where R<1> and R<2> are the same or different and represent hydrogen atom, C1-C10 alkyl, C6-C10 aryl, C7-C18 alkaryl, C7-C10 aralkyl, or R<1> and R<2> may form a substituted or unsubstituted, saturated or unsaturated, 4, 5 or 6-member ring; or R<1> or R<2> may combine with R<1> or R<2> on an adjacent carbon atom to form a substituted or unsubstituted, saturated or unsaturated, 4, 5 or 6-member ring, and n is 0-10. 3. The method of Claim 2 wherein said Pt dicarboxylate is selected from the group consisting of diaminocyclohexaneoxalate-Pt, diaminocyclohexanemalonate-Pt, diaminocyclohexanesuccinate-Pt, diaminocyclohexaneglutarate-Pt, diaminocyclohexaneadipate-Pt, diaminocyclohexanepimelate-Pt, diaminocyclohexanemaleate-Pt, diaminocyclohexanefumarate-Pt, diaminocyclohexanephthalate-Pt, and diaminocyclohexanetartrate-Pt. 4. The method of Claim 1 wherein said carboxylic acid is selected from the succinic acid, glutaric acid, adipic acid, pimelic acid, maleic acid, fumaric acid, azelaic acid, suberic acid, sebasic acid, tartaric acid and phthalic acid. 5. The method of Claim 3 wherein said diaminocyclohexane-dicarboxylate-Pt is diaminocyclohexanemalonate-Pt. 6. The method of Claim 1 wherein said phospholipid is selected from the group consisting of dimyristoylphosphatidylcholine, dimyristoylphosphatidylglycerol, distearoylphosphatidyl-choline, distearoylphosphatidylglycerol, and any combination thereof. 7. The method of Claim 6 wherein said phospholipid is a mixture of dimyristoylphosphatidylcholine, dimyristoylphosphatidyl-glycerol. 8. The method of Claim 7 wherein said dimyristoylphosphatidylcholine is present in said mixture in a weight ratio to said dimyristoylphosphatidylglycerol of about 7:3. 9. The method of Claim 1 wherein said phospholipid complex and said water-insoluble platinum dicarboxylate forms a colloidal dispersion when reconstituted with a pharmaceutically acceptable aqueous diluent. 10. The method of Claim 1 wherein said phospholipid complex and said water-insoluble complex of platinum dicarboxylate is a lyophilizate. 11. The method of Claim 10 wherein said composition further comprises a pharmaceutically acceptable excipient. 12. The method of Claim 11 wherein said excipient is mannitol. 13. The method of Claim 10 wherein said composition further comprises cholesterol or a hemisuccinate derivative thereof. 14. The method of Claim 10 wherein said lipid complex forms a colloidal dispersion when reconstituted with a physiologically acceptable aqueous diluent. |
