Once daily analgesic tablet

Details Once daily analgesic tablet Once daily analgesic tablet

1999-12-02

2001-01-23

Spear, James M. (Department: 1615)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Tablets, lozenges, or pills

C424S470000, C424S474000, C514S770000, C514S772300, C514S781000, C514S784000

Reexamination Certificate

active

06177102

ABSTRACT:

BACKGROUND OF THE INVENTION
The present invention relates to oral controlled release dosage formulations containing an analgesic. More specifically, the present invention relates to an oral dosage formulation in the form of a tablet comprising a nonsteroidal anti-inflammatory drug (NSAID), such as salicylic acid, indomethacin, ibuprofen, naproxen, naproxen sodium, flubiprofen, indoprofen, ketoprofen, piroxicam, diclofenac, etodolac, ketorolac or their pharmaceutically acceptable derivatives. Most preferably the NSAID is a pyranocarboxylic acid such as etodolac.
Numerous techniques are in the prior art for preparing sustained or controlled release pharmaceutical formulations. One common technique involves surrounding an osmotically active drug core with a semipermeable membrane. The drug is released from the core over time by allowing a fluid such as gastric or intestinal fluid to permeate the coating membrane and dissolve the drug so the dissolved drug can permeate the membrane. In some cases a hydrogel is employed to push the active ingredient through a passageway in the membrane. Some representative examples of these osmotic tablet systems can be found in U.S. Pat. Nos. 3,845,770, 3,916,899, 3,952,741, 4,034,758, 4,077,407 and 4,783,337.
Another common technique for preparing controlled release pharmaceutical formulations is to encapsulate a plurality of beads, pellets or tablets that are coated with varying levels of a diffusion barrier and/or different types of the diffusion barriers. Examples of these beaded formulations can be found in U.S. Pat. Nos. 5,376,384, 5,529,790, 5,470,584, 5,002,776, 5,445,829 and 5,578,321.
Still another common technique for preparing controlled release pharmaceutical formulations involve the use of a matrix or carrier base system wherein the active ingredient is mixed or dispersed throughout a controlled release substance. Examples of the carrier based system are described in U.S. Pat. Nos. 4,369,172, 4,389,393 and 4,966,768. U.S. Pat. No. 4,966,768 describes a carrier base controlled release pharmaceutical formulation containing etodolac and a release modifying agent. The carrier base described in U.S. Pat. No. 4,966,768 comprises a mixture of ethylcellulose and hydroxypropyl methylcellulose wherein the hydroxypropyl methylcellulose has an average molecular weight of less than 50,000 and a viscosity of 80 to 120 cps in a 2% aqueous solution.
SUMMARY OF THE INVENTION
The present invention is directed to an analgesic controlled release dosage form comprising:
(a) 40-80 weight percent of an analgesic based on the total weight of the dosage form;
(b) 10-30 weight percent of a pharmaceutically acceptable filler based on the total weight of the dosage form; and
(c) 10-30 weight percent of a carrier base based on the total weight of the dosage form wherein the carrier base comprises 5-40 weight percent based on the weight of the carrier base of a high molecular weight hydroxypropyl methylcellulose, optionally, less than 15 weight percent of a water insoluble binder based on the total weight of the carrier base and the remaining portion of the carrier base comprising a water soluble binder.
A preferred embodiment the present invention comprises a controlled release tablet comprising:
(a) a core of compressed granules comprising:
(i) 40-80 weight percent of an analgesic based on the total weight of the dosage form;
(ii) 10-30 weight percent of a pharmaceutically acceptable filler based on the total weight of the dosage form; and
(iii) 10-30 weight percent of a carrier base based on the total weight of the dosage form wherein the carrier base comprises 5-40 weight percent based on the weight of the carrier base of a high molecular weight hydroxypropyl methylcellulose, 0-15 weight percent of a water insoluble binder based on the total weight of the carrier base and the remaining portion of the carrier base comprising a water soluble binder; and
(b) optionally, a water soluble or rapidly disintegrating color coat surrounding the compressed core.
The high molecular weight hydroxypropyl methylcellulose should have an average molecular weight greater than 50,000, preferably higher than 100,000 and most preferably higher than 200,000.
The controlled release dosage formulation of the present invention may also optionally comprise 0.01-10, preferably 0.1-5, weight percent based upon the total weight of the dosage form of a surfactant and 0.01-10, preferably 0.1-5, weight percent based upon the total weight of the dosage form of a pharmaceutically acceptable lubricant and/or anti-sticking agent.
It is an object of the present invention to provide a controlled or sustained release dosage formulation for an analgesic that employs a carrier base system that comprises a high molecular weight hydroxypropyl methyl cellulose.
It is an additional object of the present invention to provide a controlled or sustained release dosage formulation for an analgesic that can provide continuous and non-pulsating therapeutic levels of the analgesic to an animal or human in need of such treatment over a twelve hour to twenty-four hour period.


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Physician's Desk Reference 52th Edition pp. 3062-3066.

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