Hybrid system for solubilizing pharmaceutically active substances in polymer matrices
AssigneeBeiersdorf AG
InventorsJens Nierle, Christian Gäde
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Abstract
The present invention is directed to a hybridized polymer matrix, a method of making such, and products incorporating such a matrix. The hybridized polymer matrix comprises a solvent-free polymer matrix base, a hybridized matrix comprising one or more poly(1-vinyl-2-pyrrolidones) and dimethyl sulfoxide, and at least one active substance. The hybridized polymer matrix is useful in the preparation of transdermal therapeutic systems, particularly making possible the introduction of pharmaceutically active substances which are otherwise difficult to dissolve, such as ibuprofen, into a non-polar matrix.
Claims22
A method of preparing a hybridized polymer matrix comprising a polar pharmaceutically active substance, wherein the method comprises
- (a) providing a polymer matrix base which comprises one or more hydrophobic polymers;
- (b) combining the polymer matrix base of (a) with a hybrid system comprising
- (i) dimethyl sulfoxide and
- (ii) one or more substances selected from poly(1-vinyl-2-pyrrolidones) of formula
- wherein n ranges from 350 to 13,500 and copolymers thereof to provide a matrix base/hybrid system mixture;
- and
- (c) combining the matrix base/hybrid system mixture of (b) with one or more polar pharmaceutically active substances;
- wherein the hybridized polymer matrix is prepared without the use of additional solvents.
A method of preparing a hybridized polymer matrix comprising a polar pharmaceutically active substance, wherein the method comprises
- (a) providing a polymer matrix base which comprises one or more hydrophobic polymers;
- (b) combining the polymer matrix base of (a) with a hybrid system comprising
- (i) dimethyl sulfoxide and
- (ii) one or more substances selected from poly(1-vinyl-2-pyrrolidones) of formula
- wherein n is such that an average molecular weight of the one or more substances is from 2,000 to 1,500,000 g/mol
- to provide a matrix base/hybrid system mixture;
- and
- (c) combining the matrix base/hybrid system mixture of (b) with one or more polar pharmaceutically active substances;
- wherein the hybridized polymer matrix is prepared without the use of additional solvents.
Dependencies are inferred from the claim text.