Mucosal delivery tablet

• US 20070048369A1
• Filed: 08/26/2005
• Published: 03/01/2007
• Est. Priority Date: 08/26/2005
• Status: Abandoned Application

• Current Assignee: Henkel AG & Co KGaA
• Original Assignee: National Starch and Chemical Investment Holding Corporation (Ingredion Incorporated)
• Inventors: Foreman, Paul, Puri, Reema, Zhang, Yeli
• Application Number:
  US11/212,437
• Publication Number:
  US 20070048369A1
• Time in Patent Office: Days
• US Class Current: 424/464
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2059 Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
• CPC Class Codes: A61K 9/2095 Tabletting processes; Dosage units made by direct compression of powders or specially processed granules, by eliminating solvents, by melt-extrusion, by injection molding, by 3D printing mechanical aspects A61J3/00
• CPC Class Codes: A61P 1/02 Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
• CPC Class Codes: A61P 29/00 Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

Abstract

Mucoadhesive tablets have a convex surface, a diameter to cup depth ratio of 4-20 and a cup depth to edge thickness ratio of greater than 0.75 swiftly adheres and conforms to the contacting tissue. The tablets are used to administer actives such as, for example, benzocaine.

Claims

1. A tablet having at least one convex surface, said tablet having a ratio of tablet diameter D to the cup depth d (D/d) of 4-20 and a ratio of cup depth d to edge thickness h (d/h) of greater than 0.75.

2. The tablet of claim 1 wherein the ratio of tablet diameter D to the cup depth d (Did) is from 4-14 and ratio of cup depth d to edge thickness h (d/h) of greater than 0.90.

3. The tablet of claim 1 comprising a bioadhesive composition and an active.

4. The tablet of claim 3 wherein the bioadhesive composition comprises a mixture of a polysaccharide and a polycarboxylated polymer.

5. The tablet of claim 4 wherein said mixture is a co-spray-dried mixture.

6. The tablet of claim 4 wherein the bioadhesive composition comprises from about 15% by weight to about 25% by weight of at least one synthetic polycarboxylated polymer.

7. The tablet of claim 6 wherein the polysaccharide is a starch and the polycarboxylated polymer is a cross-linked poly(acrylic acid).

8. The tablet of claim 6 wherein the starch is a waxy starch.

14. A method of administering a therapeutic agent to an individual comprising administering to the individual the tablet of claim 1, which tablet contains a therapeutic agent.

15. The method of claim 14 wherein the tablet is applied to a mucosal surface of the individual.

16. The method of claim 15 wherein the tablet is administered to the buccal, intestinal, nasal, ocular, sub-lingual, vaginal or rectal mucosa.

17. A method of administering an active ingredient to an individual needing or desiring said active ingredient comprising applying the active-containing tablet of claim 3 to a mucosal surface of said individual.

18. The method of claim 17 wherein the therapeutic agent is benzocaine.

9. A method of producing a bioadhesive system comprising preparing a solution comprising at least one solvent and a polymer mixture wherein the polymer mixture comprises at least one synthetic polycarboxylated polymer component and at least one polysaccharide component and drying the solution to form a solid, and compressing the solid to form a tablet, said tablet having at least one convex surface and having a ratio of tablet diameter D to the cup depth d (D/d) of 4-20 and a ratio of cup depth d to edge thickness h (d/h) of greater than 0.75.

10. The method of claim 9 wherein the solution is dried by spray-drying.

11. The method of claim 10 wherein the solvent is water, the polysaccharide is a starch and the polycarboxylated polymer is cross-linked poly(acrylic acid).

12. A bioadhesive system prepared by the method of claim 9.

13. The bioadhesive system of claim 12 further comprising a drug as the active ingredient.

19. A buccal delivery tablet comprising a bioadhesive composition and an active agent, tablet having at least one convex surface, said tablet having a ratio of tablet diameter D to the cup depth d (D/d) of 4-20 and a ratio of cup depth d to edge thickness h (d/h) of greater than 0.75.

20. The tablet of claim 19 wherein the active agent is benzocaine.