Amphotericin B liposome preparation

Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Liposomes

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514 31, 536 65, A61K 9127, A61K 3170, C07H 100

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active

059651563

ABSTRACT:
A novel composition and method for solubilizing amphiphilic drugs in a small amount of organic solvent for use in improved liposomes is disclosed. A phosphatidylglycerol is acidified in a small amount of organic solvent. The amphiphilic drug, such as Amphotericin B, suspended in organic solvent is then added to the acidified phosphatidylycerol and a soluble complex is formed between the phosphatidylglycerol and the amphiphilic drug. When the liposome composition incorporating the soluble complex is hydrated, the final pH of the hydrating aqueous buffer is carefully controlled. The Amphotericin B liposomes formed have markedly reduced toxicity.

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