Once daily pharmaceutical tablet having a unitary core

• US 6,485,748 B1
• Filed: 12/12/1997
• Issued: 11/26/2002
• Est. Priority Date: 12/12/1997
• Status: Expired due to Term

• Current Assignee: Allergan Sales LLC (Abbvie Incorporated)
• Original Assignee: Andrx Pharmaceuticals (NC), Inc. (Abbvie Incorporated)
• Inventors: Chen, Chih-Ming, Chou, Joseph C. H.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): SHEIKH, HUMERA N
• Application Number:
  US08/990,129
• Time in Patent Office: 1,810 Days
• Field of Search: 424/480, 424/465, 424/482, 424/464, 424/473, 424/495, 424/461, 424/489
• US Class Current: 424/482
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
• CPC Class Codes: A61K 9/2826 Sugars or sugar alcohols, e.g. sucrose; Derivatives thereof
• CPC Class Codes: A61K 9/2846 Poly(meth)acrylates
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• 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

Abstract

A controlled release tablet is disclosed which comprises:

(a) a homogeneous compressed core which comprises:

(i) a medicament which is very slightly soluble to practically insoluble in water at 25° C.;

(ii) a water soluble osmotic compound

(iii) one or more osmotic polymers; and

(b) a membrane coating which completely covers said core tablet which comprises a mixture of a:

(i) a water insoluble pharmaceutically acceptable polymer; and

(ii) a pH dependent polymer such as an enteric coating polymer, the weight ratio of the pH dependent polymer to the water insoluble pharmaceutically acceptable polymer being 0.1:1 to 0.75:1.

A controlled release tablet which comprises:

(a) a medicament

(a) a homogeneous compressed core which comprises:

(i) a medicament;

(ii) a water soluble osmotic compound

(iii) one or more osmotic polymers; and

(b) a membrane coating which completely covers said core tablet which comprises a mixture of:

(i) a water insoluble pharmaceutically acceptable polymer; and

(ii) an enteric polymer.

Claims

1. A controlled release tablet which comprises:

(a) a homogeneous compressed core which comprises;

(i) a medicament which is very slightly soluble to practically insoluble in water at 25°

C.;

(ii) a water soluble osmotic compound

(iii) one or more osmotic polymers which comprise poly(ethylene oxide); and

(b) a membrane coating which completely covers said core tablet which comprises a mixture of a;

(i) a water insoluble pharmaceutically acceptable polymer; and

(ii) a pH dependent polymer such as an enteric coating polymer, the weight ratio of the pH dependent polymer to the water insoluble pharmaceutically acceptable polymer being 0.1;

1 to 0.75;

1.

2. A controlled release pharmaceutical tablet as defined in claim 1 wherein the medicament is a calcium channel blocker compound.

3. A controlled release pharmaceutical tablet as defined in claim 2 wherein the medicament is nifedipine.

4. A controlled release pharmaceutical tablet as defined in claim 1 which includes two osmotic polymers.

5. A controlled release pharmaceutical tablet as defined in claim 1 wherein one of the osmotic polymers is a water swellable osmotic polymer.

6. A controlled release pharmaceutical tablet as defined in claim 5 wherein the membrane around the core contains an enteric polymer which is a methacrylic acid/methyl methacrylate polymer.

7. A controlled release pharmaceutical tablet as defined in claim 1 wherein the water insoluble polymer in the membrane around the core is a water insoluble cellulose derivative.

8. A controlled release pharmaceutical tablet as defined in claim 7 wherein the water insoluble cellulose derivative in the membrane around the core is cellulose acetate.

9. A controlled release pharmaceutical tablet as defined in claim 1 wherein the mixture of the water insoluble polymer and the enteric polymer contain a plasticizer.

10. A controlled release pharmaceutical tablet as defined in claim 1 wherein the plasticizer is triacetin.

11. A controlled release pharmaceutical tablet as defined in claim 9 wherein the mixture of the water insoluble polymer and the enteric polymer contain a water soluble channeling agent.

12. A controlled release pharmaceutical tablet as defined in claim 9 wherein the mixture of the water insoluble polymer and the enteric polymer is overcoated with an additional layer of an enteric polymer.

13. A controlled release pharmaceutical tablet as defined in claim 12 wherein the enteric polymer overcoat is hydroxypropyl methylcellulose phthalate which is plasticized with acetyltributyl citrate.

14. A controlled release tablet which comprises:

(a) a homogeneous compressed core which comprises;

(i) a medicament which is very slightly soluble to practically insoluble in water at 25°

C.;

(ii) a water soluble osmotic compound

(iii) poly(ethylene oxide); and

(b) a membrane coating which completely covers said core tablet which consists essentially of a mixture of a;

(i) cellulose acetate;

(ii) a plasticizer;

(iii) a water soluble channeling agent; and

(iv) poly(methacrylic acid-methylmethacrylate polymer having a 1;

2 ratio of polymethacrylic acid to methylmethacrylate and a number average molecular weight of 135,000, the weight ratio of cellulose acetate to said poly(methacrylic acid, methylmethacrylate polymer being 0.1;

1 to 0.75;

1.