Composition containing hydroxypropylmethylcellulose and/or ethylcellulose as disintegrants and process for producing it

• US 6,531,151 B1
• Filed: 10/29/1999
• Issued: 03/11/2003
• Est. Priority Date: 07/30/1997
• Status: Expired due to Fees

• Current Assignee: Galenix Developpement
• Original Assignee: Galenix Developpement
• Inventors: Besse, Jerome
• Primary Examiner(s): Dees, Jose′ G.
• Assistant Examiner(s): Haghighatian, M.
• Application Number:
  US09/430,341
• Time in Patent Office: 1,229 Days
• Field of Search: 424/464, 424/465, 424/472, 424/490, 424/468, 424/400, 424/466
• US Class Current: 424/464
• CPC Class Codes: A61K 31/167 having the nitrogen of a carboxamide group directly attached to the aromatic ring, e.g. lidocaine, paracetamol
• CPC Class Codes: A61K 31/196 the amino group being directly attached to a ring, e.g. anthranilic acid, mefenamic acid, diclofenac, chlorambucil
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2077 Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
• CPC Class Codes: A61K 9/209 containing drug in at least two layers or in the core and in at least one outer layer

Abstract

Pharmaceutical composition comprising at least one active ingredient and hydroxypropylmethylcellulose, highly substituted hydroxypropylcellulose, and/or ethylcellulose as disintegrants, in quantities less than 15% by weight of the composition and in a form providing a disintegrant effect while avoiding the formation of a continuous matrix.

Claims

1. A pharmaceutical composition in the form of a powder, granule or tablet comprising at least one active ingredient and at least one member selected from the group consisting of hydroxypropylmethylcellulose, hydroxypropylcellulose containing a minimum of 50% of substitution by hydroxypropoxy groups, and ethylcellulose as disintegrants, in an amount of less than 15% by weight of the composition and in a form providing a disintegrant effect while avoiding the formation of a continuous matrix and wherein the composition comprises at least about 80% of active ingredients by weight of the composition.

2. The composition of claim 1 wherein it contains less than about 10% by weight of the disintegrant.

3. The composition of claim 1 wherein it contains between about 1.5 and 7% by weight of disintegrant.

4. The composition of claim 1 wherein the hydroxypropylmethylcellulose advantageously has a substitution level by hydroxypropoxy groups of between about 2 and 45% and by methoxy groups of between 10 and 40%.

5. The composition of claim 1 wherein the disintegrant is in micronized form.

6. The composition of claim 1 wherein the disintegrant is in the form of powders with an average diameter of less than about 50 μ

m.

7. The composition of claim 1 wherein it contains at least 85% by weight of the active ingredient.

8. The composition of claim 1 wherein it additionally contains at least one binding agent.

9. A tablet or granule of claim 1.

10. A tablet or granule of claim 11 wherein it comprises at least two layers.

11. A tablet or granule of claim 9 wherein the active ingredient and the disintegrant are comprised in the same layer.

12. A tablet or granule of claim 9 wherein the active ingredient and the disintegrant are comprised in two layers.

13. A tablet or granule of claim 9 wherein the active ingredient or ingredients and the disintegrant are comprised in different layers.

14. A tablet or granule of claim 9 wherein it is composed of an inner core and an outer core, the inner core comprising a composition of claim 1, and the outer core comprising at least one compound with a disintegrant effect and an effective amount of the active ingredient contained in the inner core.

15. A pharmaceutical composition in the form of a powder, granule or tablet comprising at least one active ingredient of paracetamol or diclofenac and at least one member selected from the group consisting of hydroxypropylmethylcellulose, hydroxypropylcellulose containing a minimum of 50% of substitution by hydroxypropoxy groups, and ethylcellulose as disintegrants, in an amount of less than 15% by weight of the composition and in a form providing a disintegrant effect while avoiding the formation of a continuous matrix and wherein the composition comprises at least 80% of active ingredients by weight of the composition.