Pharmaceutical forms for the release of active compounds
AssigneeLaboratorios Farmaceuticos Rovi, S.A.
InventorsGuillermo Franco Rodriguez, Ibon Gutierro Aduriz
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Abstract
A pharmaceutical composition containing a sulfated glycosaminoglycan drug and a polycationic polymer or copolymer wherein the proportion of ammonium groups in the pharmaceutical composition is between 0.01-2.0 μmol ammonium groups/mg pharmaceutical composition, the proportion of glycosaminoglycan in the pharmaceutical form is between 15% to 50% w/w, and the pharmaceutical composition possesses a moisture content of 10% wt or less. A pharmaceutical dosage form containing the pharmaceutical composition, and their use for the treatment of diseases or disorders therapeutically responsive to the glycosaminoglycan.
Claims66
A pharmaceutical form comprising a glycosaminoglycan with anions and a compound presenting cations of pH independent quaternary ammonium groups, which compound is a structure of polymers and copolymers derived from acrylic and methacrylic acids esters, wherein:
- the proportion of ammonium groups in the pharmaceutical form is between 0.01 to 2.0 μmol ammonium/mg pharmaceutical form,
- the proportion of glycosaminoglycan in the pharmaceutical form is between 15% to 50% w/w, and
- the pharmaceutical form presents a humidity percentage (w/w) lower than 10%,
- wherein the anions of the glycosaminoglycan are only partially neutralized with the cations.
A solid pharmaceutical dosage form comprising a compressed composition consisting essentially of an admixture of:
- 15%-50% wt. of polyanionic sulfated glycosaminoglycan comprising anionic sulfate groups;
- and
- 85%-50% wt. of polycationic copolymer of acrylic acid ester and methacrylic acid ester comprising cationic pH independent quaternary ammonium groups;
- wherein
- the compressed composition has a moisture content of about 10% wt. or less;
- and
- the mole ratio of sulfate groups to ammonium groups in the composition is greater than one, whereby less than the total of sulfate groups of the glycosaminoglycan are neutralized by or complexed with the total of ammonium groups present.
A solid pharmaceutical dosage form comprising a compressed composition consisting essentially of an admixture of:
- 15%-50% wt. of polyanionic sulfated glycosaminoglycan comprising anionic sulfate groups;
- and
- 85%-50% wt. of polycationic copolymer of acrylic acid ester and methacrylic acid ester comprising cationic pH independent quaternary ammonium groups;
- wherein
- the compressed composition has a moisture content of about 10% wt. or less;
- and
- the weight ratio of glycosaminoglycan to cationic polymer is in the range of 1:1 to 1:4;
- the molar content of ammonium groups in the composition ranges from 0.1 to 3.0 micromoles of ammonium groups per mg of composition;
- the molar content of sulfate groups in the composition ranges from 0.2 to 2.5 micromoles of sulfate groups per mg of composition;
- the mole ratio of ammonium groups to sulfate groups is in the range of 5:95 to 48.1-51.5, and
- the percentage of sulfate groups complexed with or neutralized by the ammonium groups is in the range of 5-95%.
Dependencies are inferred from the claim text.