Phospholipid delivery vehicle for aqueous-insoluble active...

A - Human Necessities – 61 – K

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167/163, 167/216

A61K 9/51 (2006.01) A61K 9/107 (2006.01) A61K 9/127 (2006.01) A61K 31/53 (2006.01)

Patent

CA 1314213

ABSTRACT Compositions comprising phospholipid-encapsulated vesicles of active ingredient and triglyceride are described. In a preferred embodiment the vesicles are composed of a hexa- methylmelamine active ingredient, with trilaurin or trimyristin as the triglyceride and a mixture of distearoylphosphatidyl- choline, distearoylphosphatidylglycerol and cholesterol in the phospholipid outer layer. Preferably the molar ratios of active ingredient: triglyceride : DSPC : CHOL : DSPG will be from about 1:4:2:1:0 to about 1:4:1:1:1. Glycerol may be added to the carrier phase to reduce agglomeration. The composition may be used to deliver otherwise aqueous-insoluble agents to humans or animals to treat, for example, tumors.

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