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US 9,849,088 B2Granted
Depot formulations of a hydrophobic active ingredient and methods for preparation thereof
AssigneePainreform Ltd.
InventorsShimon Amselem, Michael Naveh
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Abstract
The invention provides extended release pro-liposomal, non-aqueous, pharmaceutical formulations of a hydrophobic active pharmaceutical ingredient (API) of low water solubility but readily dissolved in alcohols and methods for making same. The formulations can be administered by infiltration into an incision, or by injection.
Claims20
A pro liposomal non aqueous pharmaceutical depot composition consisting essentially of:
- a hydrophobic active pharmaceutical ingredient having a Log P hydrophobicity value of at least 1.5;
- about 40% to about 70% by weight of a natural phospholipid;
- about 20% to about 60% by weight of an oil as a non-aqueous pharmaceutically acceptable carrier;
- and
- about 0.5% to about 12% by weight of an alcohol as a viscosity regulator,
- wherein said composition is in the form of a clear oleaginous liquid solution, stable at
- ambient temperature, devoid of water, and has viscosity below 2500 cP.
4 more elements
A method for making a depot composition comprising:
- (a) mixing an oil as a non-aqueous pharmaceutically acceptable carrier with:
- (i) a hydrophobic active pharmaceutical ingredient (API);
- (ii) a natural phospholipid or pharmaceutically acceptable salt thereof;
- and
- (iii) alcohol as a viscosity regulator;
- to form a non-aqueous oleaginous liquid solution;
- (b) removing all or a portion of the viscosity regulator from the non-aqueous solution;
- and
- (c) adding the alcohol viscosity regulator to the non-aqueous solution to a total amount of about 2% to about 12% by weight,
- wherein the depot composition consists essentially of about 40% to about 70% by weight of the natural phospholipid and about 20% to about 60% by weight of the oil.
7 more elements
Dependencies are inferred from the claim text.