Coated tablet formulation and method

• US 7,951,400 B2
• Filed: 05/25/2005
• Issued: 05/31/2011
• 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.
• Primary Examiner(s): Sheikh; Humera N
• Application Number:
  US11/137,068
• Publication Number:
  US 20050266080A1
• Time in Patent Office: 2,197 Days
• Field of Search: None
• 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) a tablet core;

(b) an inner seal coating layer coated on the tablet core wherein the inner seal coating layer comprises about 1 mg to about 100 mgs of a polyvinyl alcohol based formulation wherein the polyvinyl alcohol based formulation comprises polyvinyl alcohol;

(c) a second coating layer coated on the inner seal coating of the tablet core, wherein the second coating layer comprises about 0.2 mgs to about 140 mgs of saxagliptin, or a pharmaceutically acceptable salt thereof, and about 2 mgs to about 140 mgs of a polyvinyl alcohol based formulation wherein the polyvinyl alcohol based formulation comprises polyvinyl alcohol; and

(d) an outer protective coating layer coated on the second coating layer of the tablet core wherein the outer protective coating layer comprises about 1 mg to about 100 mgs of a polyvinyl alcohol based formulation wherein the polyvinyl alcohol based formulation comprises polyvinyl alcohol.

2. 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.

3. The coated tablet as defined in claim 2 wherein the tablet core is comprised of microcrystalline cellulose, lactose monohydrate, croscarmellose sodium, and magnesium stearate.

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

5. The coated tablet as defined in claim 1 where for a 5 mg potency the second coating layer is comprised of 5 mg saxagliptin, and at least 5 mg polyvinyl alcohol based formulation and for a 2.5 mg potency the second coating layer is comprised of 2.5 mg saxagliptin, and 20 mg polyvinyl alcohol based formulation.

10. The coated tablet as defined in claim 1 wherein saxagliptin is the hydrochloride salt.

6. A coated tablet comprising:

a) a tablet core comprising about 49.5% lactose monohydrate, about 45% microcrystalline cellulose, about 5% croscarmellose sodium, and about 0.5% magnesium stearate;

b) an inner seal coating layer coated on the tablet core, wherein the inner seal coating layer comprises about 40% polyvinyl alcohol, about 20% polyethylene glycol, about 15% talc, and about 25% titanium dioxide;

c) a second coating layer coated on the inner seal coating of the tablet core, wherein the second coating layer comprises saxagliptin or a pharmaceutically acceptable salt thereof, polyvinyl alcohol, polyethylene glycol, talc, and titanium dioxide; and

d) optionally an outer protective coating layer coated on the second coating layer of the tablet core, wherein the outer protective coating comprises polyvinyl alcohol, polyethylene glycol, talc, and titanium dioxide.

7. The coated tablet as defined in claim 6 wherein the second coating layer comprises saxagliptin or a pharmaceutically acceptable salt thereof, and a coating material comprising about 40% polyvinyl alcohol, about 20% polyethylene glycol, about 15% talc, and about 25% titanium dioxide.

8. The coated tablet as defined in claim 7 wherein the outer protective coating layer comprises about 40% polyvinyl alcohol, about 20% polyethylene glycol, about 15% talc, and about 25% titanium dioxide.

9. The coated tablet as defined in claim 8 wherein saxagliptin is the hydrochloride salt.