Pharmaceutical compositions for parenteral administration

摘要

The invention comprises various aqueous PEG-carbohydrate-lipid based formulations of pharmaceutical active ingredients including compositions for intravenous injections. This invention relates to methods and compositions for improving solubility and the safety profile of pharmaceutical compounds. More particularly, the present invention relates to employing PEG-carbohydrate-lipid conjugates for formulating drug compositions having increased solubility or dispersivity and enhanced stability.

主权项

1. A pharmaceutical composition for parenteral administration of a pharmaceutical active ingredient, the composition comprising:
a) an aqueous solution or mixture; b) a pharmaceutical active ingredient; and c) a solubility enhancer comprising dioleoylglyceroldiethylenetriamine-monomethoxyl polyethylene glycol ether lactobionate:wherein:
X1, X2, X3 and Xi are the same or different linking groups comprising at least one of oxy, amide, succinyl and, carbonyl; B is a central backbone comprising at least one of glycerol or glycerol-like analogues, polyamine, amino acid, triamine, diethylenetriamine, tetramine, diethylenetetramine, triethylenetetramine, aminoalcohol, and aminopropanediol; L is a lipid comprising at least one of diacylglycerol, fatty acids, and bile acids; S is carbohydrate comprising saccharide; and P is polymer comprising PEG.