Pharmaceutical compositions comprising ascomycin derivatives

A - Human Necessities – 61 – K

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A61K 9/107 (2006.01) A61K 31/436 (2006.01) A61K 47/12 (2006.01) A61K 47/24 (2006.01) A61P 27/02 (2006.01) B01F 17/00 (2006.01)

Patent

CA 2678707

A process for preparing an emulsion composition comprising a cyclosporin, a rapamycin or an ascomycin or a derivative thereof as active agent, which process comprises the step of admixing to a placebo fat emulsion a concentrate comprising a) the active agent, b) a stabiliser selected from a phospholipid, a glycolipid, a sphingolipid, a diacylphosphatidyl glycerol, an egg-phosphatidylglycerol, a soy- phosphatidylglycerol, a diacyl-phosphatidylglycerol, or a salt thereof; or a saturated, mono- or di- unsaturated (C12-24) fatty acid, or a salt thereof, and c) an organic solvent, wherein the weight ratio of active agent to stabiliser is between 400:1 and 0.5:1. The invention also provides ready-to-use emulsions, e.g. for intravenous administration, prepared using the above process.

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