Adhesive matrix with hydrophilic and hydrophobic domains and a therapeutic agent
AssigneeCorium, Inc.
InventorsEun Soo Lee, Amit K. Jain, Parminder Singh
Life of this patent
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Abstract
An adhesive matrix and adhesive formulation are described. The adhesive matrix is comprised of a hydrophilic domain and a hydrophobic domain, and a therapeutically active agent contained in the matrix in a supersaturated, stable, condition. The hydrophilic domain and the hydrophobic domain are co-soluble in a solvent system, to provide a homogeneous blend in which the active agent is solubilized. The proportion of the hydrophilic domain and hydrophobic domain is selected to optimize, or maximize, solubility of active agent in the matrix.
Claims26
An adhesive matrix, comprising:
- a hydrophilic domain comprising a polyvinylpyrrolidone-vinyl acetate copolymer;
- a hydrophobic domain comprising one or both of a polyisobutylene and an acrylic acid/vinyl acetate copolymer;
- and
- an active agent is characterized by (a) a melting point of less than about 250° C. or (b) a solubility in water of less than about 500 mg/L or (c) an oil/water partition coefficient of between about 2.1 and about 5;
- wherein the hydrophilic domain and the hydrophobic domain are co-soluble in a solvent system and present in the adhesive matrix in a proportion to one another to solubilize an amount of active agent greater than the amount of active agent soluble in either domain alone.
A formulation for preparation of an adhesive matrix, comprising:
- about 10-25 wt % polyvinylpyrrolidone-vinyl acetate copolymer, about 35-75 wt % of polyisobutylene and polybutene, about 40-64 wt % of an acrylate adhesive, and about 5-50 wt % of an active agent in a solvent system comprised of an organic solvent in which the polyvinylpyrrolidone-vinyl acetate copolymer, the polyisobutylene and polybutene and soluble, wherein the active agent is characterized by (a) a melting point of less than about 250° C. or (b) a solubility in water of less than about 500 mg/L or (c) an oil/water partition coefficient of between about 2.1 and about 5.
A method for the manufacture of an adhesive matrix, comprising:
- (i) solubilizing a polyvinylpyrrolidone-vinyl acetate copolymer in a first solvent;
- (ii) solubilizing polyisobutylene and polybutene in a second solvent;
- (iii) mixing (i) and (ii) to form a homogeneous solution;
- (iv) adding to the homogeneous solution an acrylate adhesive solubilized in a third solvent to form an adhesive solution;
- (v) adding to the adhesive solution an active agent characterized by (a) a melting point of less than about 250° C. or (b) a solubility in water of less than about 500 mg/L or (c) an oil/water partition coefficient of between about 2.1 and about 5;
- and
- (v) forming an adhesive matrix from the adhesive solution with the active agent that comprises between about 35-80 wt % acrylate, between about 0.01-30 wt % polyisobutylene and polybutene mixture, between about 10-25 wt % polyvinylpyrrolidone-vinyl acetate copolymer, and between about 5-50 wt % active agent.
Dependencies are inferred from the claim text.