A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 47/24 (2006.01) A61K 9/10 (2006.01) A61K 9/127 (2006.01) A61K 9/50 (2006.01) A61K 39/39 (2006.01)
Patent
CA 2078990
Water-insoluble drugs are rendered injectable by formulation as aqueous suspensions of phospholipid-coated microcrys- tals. The crystalline drug is reduced to 50 nm to 10 um dimensions by sonication or other processes inducing high shear in the presence of membrane-forming amphipathic lipids. The membrane-forming lipid stabilizes the microcrystal by both hydrophobic and hydrophilic interactions, coating and enveloping it and thus protecting it from coalescence, and rendering the drug in solid form less irritating to tissue. Additional protection against coalescence is obtained by a secondary coating by additional mem- brane-forming lipid in vesicular form associated with and surrounding but not enveloping the lipid-encapsulated drug particles. Tissue-compatible formulations containing drug in concentrations up to 40 % (w/v) are described.
Haynes Duncan H.
Jagotec Ag
Ridout & Maybee Llp
LandOfFree
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