Solid dosage forms comprising an enteric coating with accelerated drug release
View Patent ↗The present invention provides a solid dosage form including an inner coating located between a core containing a pharmaceutically active ingredient and an outer enteric coating; wherein the inner coating includes a partially neutralized anionic polymeric material, and at least a carboxylic acid having 2 to 16 carbon atoms the salts thereof or mixtures of the acid and its salt; wherein the outer coating includes an anionic polymeric material which is less or not at all neutralized than the material of the inner coating.
1. A solid dosage form comprising
an inner coating located between a core containing a pharmaceutically active ingredient and an outer enteric coating;
wherein said inner coating comprises a partially neutralized anionic polymeric material, and at least a carboxylic acid having 2 to 16 carbon atoms, the salts thereof or mixtures of said acid and its salt;
wherein said outer coating comprises an anionic polymeric material which is less neutralized than the material of the inner coating or not at all neutralized.
2. The solid dosage form according to claim 1 ,
wherein the difference in the neutralization between the inner coating and the outer coating is at least 5 percentage points.
3. The solid dosage form according to claim 1 ,
wherein the degree of neutralization of anionic groups of the outer coating is at most 10 percent.
4. The solid dosage form according to claim 1 , wherein the anionic polymeric material of the inner coating and the outer coating, respectively, is independently selected from the group consisting of polymethacrylates, cellulose acetate phthalate, polyvinyl acetate phthalate, hydroxypropyl methylcellulose phthalate, hydroxypropyl methylcellulose acetate succinate (HPMC-AS), cellulose acetate trimellitate, and shellac.
5. The solid dosage form according to claim 1 ,
wherein the inner coating is made of a partially neutralized anionic (meth)acrylate copolymer consisting of free-radical polymerized units of 25 to 95% by weight C 1 - to C 4 -alkyl esters of acrylic or methacrylic acid and 5 to 75% by weight (meth)acrylate monomers having an anionic group, wherein 1 to 80% of the contained anionic groups are neutralized by an alkaline agent;
and wherein the outer coating is made of an anionic (meth)acrylate copolymer consisting of free-radical polymerized units of 25 to 95% by weight C 1 - to C 4 -alkyl esters of acrylic or methacrylic acid and 5 to 75% by weight (meth)acrylate monomers having an anionic group.
6. The solid dosage form according to claim 1 , wherein the salt is an alkali metal salt, an alkaline earth metal salt, an ammonium salt or a soluble metal salt.
7. The solid dosage form according to claim 1 , wherein the carboxylic acid having 2 to 16 carbon atoms comprises 1, 2 or 3 carboxyl groups.
8. The solid dosage form according to claim 1 , wherein the carboxylic acid is selected from the group consisting of sorbic acid, benzoic acid, fumaric acid, adipic acid, citric acid, succinic acid, glutaric acid, malic acid, tartaric acid, acetic acid, glycolic acid, malonic acid, propanoic acid, glyceric acid, trans-crotonic acid, itaconic acid, mesaconic acid, trimethylacetic acid, isocitric acid, hexanoic acid, 4-methylpentanoic acid, gallic acid, terephthalic acid, phenylacetic acid, mandelic acid, alpha-phenylpropanoic acid, beta-phenylpropanoic acid, lauric acid, caprylic acid, caprinic acid, myristic acid and mixtures thereof, the salts thereof and mixtures of said acid and its salt.
9. The solid dosage form according to claim 1 , wherein the carboxylic acid is adipic acid or citric acid.
10. The solid dosage form according to claim 1 . wherein each of the inner and the outer coatings contain 2 to 10 mg/cm 2 polymer weight gain.
11. The solid dosage form according to claim 1 , wherein the relation between the inner and the outer coating is 10:90 to 90:10 by weight of dry polymer.