Polymeric composition for solubilizing poorly water soluble drugs and process for the preparation thereof
AssigneeSamyang Corporation
InventorsMin-Hyo Seo, In-Ja Choi
Life of this patent
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Abstract
A composition capable of forming a micelle in body fluids or in an aqueous medium and that can be injected into the body undiluted or as a diluted solution in an aqueous medium and method of preparation are disclosed. The composition comprises an amphiphilic block copolymer having a hydrophilic poly(alkyleneglycol) component and hydrophobic biodegradable polymer component, suspended in a poly (alkyleneglycol) medium. Such composition is used in the solubilization and administration of a poorly water-soluble drug.
Claims16
A composition capable of forming a polymeric micelle in a body fluid or an aqueous medium, said composition comprising an amphiphilic block copolymer having a hydrophilic poly(alkylene glycol) A block component and hydrophobic biodegradable polymer B block component, said amphiphilic block copolymer being suspended in a liquid poly(ethylene glycol) medium wherein the poly (ethylene glycol) is represented by the formula:
- R—O—CH2 CH2—(O CH2 CH2)n—O—R
- wherein R is hydrogen, C1-C4 alkyl, benzyl, or acyl;
- and n is an integer of 3-220, wherein the poly (ethylene glycol) has an average molecular weight in the range of 200 to 10,000 Daltons.
A hydrophobic drug containing biodegradable polymeric composition capable of solubilizing said hydrophobic drug in a hydrophilic environment to form a solution, said composition comprising a hydrophobic drug physically entrapped within but not covalently bound to a biodegradable polymeric drug carrier comprising an amphiphilic block copolymer having a hydrophilic poly(alkylene glycol) component and hydrophobic biodegradable polymer component being suspended in a poly(ethylene glycol) medium wherein the poly (ethylene glycol) is represented by the formula:
- R—O—CH2 CH2—(O CH2 CH2)n—O—R
- wherein R is hydrogen, C1-C4 alkyl, benzyl, or acyl;
- and n is an integer of 3-220, wherein the poly (ethylene glycol) has an average molecular weight in the range of 200 to 10,000 Daltons.
A method for preparing a hydrophobic drug containing biodegradable polymeric micelle composition capable of solubilizing said hydrophobic drug in a hydrophilic environment to form a solution, comprising the steps of:
- 1) preparing a mixture containing an amphiphilic block copolymer having a hydrophilic poly(alkylene glycol) component and hydrophobic biodegradable polymer component, a hydrophobic drug, and a poly(ethylene glycol);
- 2) subjecting the resulting mixture to one step selecting from the group consisting of:
- (a) stirring at 30 to 100° C.;
- (b) stirring at 30 to 100° C. while adding an organic solvent into said mixture;
- and
- (c) dissolving said mixture in an organic solvent followed by evaporating the solvent.
Dependencies are inferred from the claim text.