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Claims for Patent: 6,224,905

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Claims for Patent: 6,224,905

Title: Biconvex rapidly disintegrating dosage forms
Abstract:A method for preparing solid rapidly disintegrating dosage forms shaped as biconvex tablets having symmetrical top and bottom surfaces and dosage forms obtainable thereby.
Inventor(s): Lawrence; Janice (Gregory, MI), Posage; Gary (Rochester Hills, MI)
Assignee: Janssen Pharmaceutica N.V. (BE)
Application Number:09/194,808
Patent Claims: 1. A process for the preparation of a solid rapidly disintegrating dosage form comprising a porous network of matrix forming materials, wherein said matrix forming materials comprise

i) a water-soluble, hydratable gel or foam-forming material,

ii) a rigidifying agent for the gel or foam-forming material and optionally

iii) one or more amino acids and

which process comprises:

overfilling a mold with a predetermined amount of an aqueous composition comprising the matrix forming materials so that a convex meniscus is created on top of the mold;

freezing the aqueous composition in the mold; and

removing the solvent from the frozen composition by subjecting it to lyophilization or to solid state dissolution, thus leaving a porous network of matrix forming materials;

characterized in that the shape of the bottom surface of the mold is a mirror-image of the shape of the frozen meniscus on the top, the mirror-plane being parallel to the plane defined by the rim of the mold, thus yielding a dosage form shaped as a biconvex tablet having symmetrical top and bottom surfaces.

2. A process according to claim 1 wherein the volume of the mold is in the range of 300 to 2,000 mm3 (0.3 to 2 ml) and the volume of the dosage form is in the range of 350 to 2,500 mm3 (0.35 to 2.5 ml).

3. A process according to claim 2 wherein the volume of the mold is in the range of 350 to 800 mm3 (0.35 to 0.8 ml) and the volume of the dosage form is in the range of 450 to 1,000 mm3 (0.45 to 1 ml).

4. A process according to claim 1 wherein the maximum depth of the mold is in the range of 3.4 to 6 mm; or the maximum thickness of the frozen composition in the mold is in the range of 5.0 to 8.5 mm.

5. A process according to claim 1 wherein the area of the surface defined by the rim of the mold is in the range of 100 to 500 mm2 and has a rounded shape.

6. A process according to claim 5 wherein said rounded shape is circular, elliptical, oblong, oblate or polygonal, the latter with rounded corners if the internal angle.sup.2 90.degree..

7. A process according to claim 1 wherein the mold is a depression in a sheet of filmic plastic material or in a metal plate.

8. A process according to claim 7 wherein the mold is a thermoformed cup in a polypropylene sheet, the surface of which is optionally siliconized.

9. A process according to claim 1 wherein the aqueous composition is a solution, a suspension, a dispersion, an emulsion, or a foam.

10. A sheet made of filmic plastic material or of metal for use in the process of claim 1 which comprises a plurality of molds arranged in a regular pattern, characterized in that the shape of the bottom surface of each mold is a mirror-image of the shape of a predetermined convex meniscus on the top, the mirror-plane being parallel to the plane defined by the rim of the mold, the sheet thus being suitable for preparing dosage forms shaped as biconvex tablets having symmetrical top and bottom surfaces.

11. process according to claim 1 wherein the gel or foam forming material is selected from the group consisting of gelatin, gelatin A, gelatin B, fluid gelatin, modified fluid gelatin, gelatin derivatives, albumin, soy fiber protein, wheat, psyllium seed proteins, potato protein, papain, coacervate egg lecithin, lecithin, acacia, guar, agar, locust bean, xanthan, tragacanth gum, alginates, polymannuronic acid, chitosan, carrageenans, dextrans, dextrins, maltodextrins, pectins, polygalacturonic acid, microcrystalline cellulose, corn syrup solids, konjac flour, rice flour, wheat gluten, polyvinylpyrrolidone, sodium carboxymethyl-cellulose, sodium starch glycolate, hydroxyethylcellulose; and gelatin-acacia complexes, each singly or in combination.

12. A process according to claim 10 wherein the rigidifying material is selected from the group consisting of a mono-saccharide, a linear or cyclic oligosaccharide, a polysaccharide, an inorganic substance, and any combination thereof.

13. A process according to claim 12 wherein the rigidifying material is selected from the group consisting of mannitol, xylitol, sorbitol, dextrose, fructose, sucrose, lactose, maltose, galactose, trehalose, beta-cyclodextrin, 2-hydroxypropyl-beta-cyclodextrin, dextran, dextrin, sodium phosphate, sodium chloride, a magnesium aluminum silicate, magnesium trisilicate, and a natural clay, or any combination thereof.

14. A process according to claim 1 wherein the amino acid is glycine, L-aspartic acid, L-glutamic acid, L-hydroxyproline, L-isoleucine, L-phenylalanine, or a combination thereof.

15. A process according to claim 1 wherein the matrix forming materials comprise:

i) from 0.1% to 15% (w/w) of a water-soluble, hydratable gel or foam-forming material;

ii) from 0.5% to 10% (w/w) of a rigidifying agent for the gel or foam-forming material; and optionally;

iii) from 0.5% to 10% (w/w) of one or more amino acids.

16. A process according to claim 15 wherein the matrix forming materials comprise:

i) from 1.2% to 3% (w/w) of a water-soluble, hydratable gel or foam-forming material;

ii) from 1% to 4% (w/w) of a rigidifying agent for the gel or foam-forming material, and optionally;

iii) from 0.8% to 2.5% (w/w) of one or more amino acids.

17. A process according to claim 1 wherein the weight by weight ratio of the total amount of amino acids to that of the water-soluble, hydratable gel or foam-forming material is from 1:1 to 1:3; the weight by weight ratio of the amount of the water-soluble, hydratable gel or foam-forming material to that of the rigidifying agent is from 2:1 to 1:2; and the weight by weight ratio of the total amount of non-solvent components to that of the water in the aqueous composition ranges from 1:9 to 1:33.

18. A process according to claim 17 wherein the weight by weight ratio of the total amount of amino acids to that of the water-soluble, hydratable gel or foam-forming material is 1:1.5; the weight by weight ratio of the amount of the water-soluble, hydratable gel or foam-forming material to that of the rigidifying agent is 1.5:2; and the weight by weight ratio of the total amount of non-solvent components to that of the water in the aqueous composition ranges from 1:13 to 1:30.

19. A process according to claim 1 wherein the aqueous composition comprises a drug substance for human or veterinary use as an active ingredient.

20. A process according to claim 19 wherein the aqueous composition further comprises a substance selected from the group consisting of nutrients, vitamins, other active ingredients, sweeteners, flavouring agents, colouring agents, surfactants, preservatives, antioxidants, viscosity enhancers, minerals, diagnostics, fertilizers and insecticides.

21. A process according to claim 19 wherein the drug is cisapride [(.+-.)-cis-4-amino-5-chloro-N-[1-[3-(4-fluorophenoxy)propyl]-3-methoxy-4- piperidinyl]-2-methoxy-benzamide monohydrate].

22. A process according to claim 1 wherein the matrix material can be disintegrated by water at 20.degree. C. within 10 seconds.

23. A solid rapidly disintegrating dosage form obtainable by the process of claim 1.
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