Coated tablet formulation and method

• US 20050266080A1
• Filed: 05/25/2005
• Published: 12/01/2005
• Est. Priority Date: 05/28/2004
• Status: Active Grant

• Current Assignee: Astrazeneca AB (Astrazeneca PLC)
• Original Assignee: Bristol-Myers Squibb Company
• Inventors: Desai, Divyakant S., Li, Bing V.
• Granted Patent: US 7,951,400 B2
• Time in Patent Office: Days
• US Class Current: 424/472
• CPC Class Codes: A61K 31/403 condensed with carbocyclic rings, e.g. carbazole
• CPC Class Codes: A61K 9/2086 Layered tablets, e.g. bilayer tablets; Tablets of the type inert core-active coat active cores with a complete drug-free outer coat A61K9/28
• CPC Class Codes: A61K 9/284 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone
• CPC Class Codes: A61K 9/2886 having two or more different drug-free coatings; Tablets of the type inert core-drug layer-inactive layer of the type active core-drug layer-inactive layer A61K9/209
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

Abstract

A coated tablet formulation is provided which includes a medicament such as the DPP4-inhibitor, saxaglipitin or its HCl salt, which is subject to intra-molecular cyclization, which formulation includes a tablet core containing one or more fillers, and other conventional excipients, which tablet core includes a coating thereon which may include two or more layers, at least one layer of which is an inner seal coat layer which is formed of one or more coating polymers, a second layer of which is formed of medicament which is the DPP4-inhibitor and one or more coating polymers, and an optional, but preferable third outer protective layer which is formed of one or more coating polymers. A method for forming the coated tablet is also provided.

Claims

1. A coated tablet comprising a tablet core and

a) an inner seal coating layer coated on the tablet core;

b) a second coating layer comprising a medicament coated on the inner seal coating of the tablet core; and

c) optionally an outer protective coating layer coated on the second coating layer of the tablet core.

2. The coated tablet as defined in claim 1 wherein the medicament is labile and may undergo degradation.

3. The coated tablet as defined in claim 1 wherein the medicament is saxaglipitin (DPP4 inhibitor)

4. The coated tablet as defined in claim 1 wherein said inner seal coating layer comprises a coating polymer formulation comprising a PVA based polymer, said second coating layer comprises a medicament which is saxaglipitin, and a coating polymer formulation comprising a PVA based polymer, and said other protective coating layer comprises a coating layer formulation comprising a PVA based polymer.

5. The coated tablet as defined in claim 1 wherein said second coating layer is comprised of from about 0.1 to about 70% by weight medicament and from about 30 to about 99.5% by weight coating polymer, based on the weight of the second coating layer.

6. The coated tablet as defined in claim 4 wherein the coating polymer formulation in the second coating layer is at least about 2 mg with a 200 mg tablet core, and the medicament is at least about 0.2 mg.

7. The coated tablet as defined in claim 1 further including a third outer protective coating layer disposed on said second coating layer.

8. The coated tablet as defined in claim 7 wherein said second coating layer comprises a PVA based polymer.

9. The coated tablet as defined in claim 7 wherein each of the inner seal coating layer and the outer protective layer comprises a PVA based polymer.

10. The coated tablet as defined in claim 9 wherein the PVA based polymer in the second coating layer is substantially the same as the PVA based polymer in the other coating layers.

11. The coated tablet as defined in claim 8 wherein the PVA based polymer is comprised of polyvinyl alcohol.

12. The coated tablet as defined in claim 1 where in second coating layer the medicament is present in an amount within the range from about 0.2 to about 140 mg and the coating polymer is present in an amount within the range from about 2 to about 140 mg, and in each of the inner seal coating layer and optionally outer protective coating layer, the coating polymer is being present in an amount within the range from about 1 to about 100 mg.

13. The coated tablet as defined in claim 1 wherein the tablet core is comprised of one or more fillers, optionally one or more binders, optionally one or more disintegrants and optionally one or more tableting lubricants.

14. The coated tablet as defined in claim 13 wherein the tablet core is comprised of microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, and magnesium stearate.

15. The coated tablet as defined in claim 1 having the following composition:

16. The coated tablet as defined in claim 1 where for a 5 mg potency the second coating layer is comprised of 5 mg medicament and 5 mg polymer based coating and for a 2.5 mg potency the coating layer is comprised of 2.5 mg medicament and 20 mg polymer based coating.

17. A method for preparing a coated tablet comprising:

a) providing a tablet core;

b) coating the tablet with an inner seal coating layer formulation which includes at least one coating polymer;

c) drying the coated tablet to form an inner seal coating thereon;

d) coating the so-coated tablet with a second coating layer formulation which includes medicament and at least one coating polymer;

e) drying the so-coated tablet to form a second coating layer (containing medicament) thereon; and

f) optionally coating the so-coated tablet with a third outer protective coating layer formulation which includes at least one coating polymer; and

g) drying the so-coated tablet to form the coated tablet of the invention.

18. The method as defined in claim 17 wherein the coating layers are applied as a suspension of the coating polymer.