Extended release formulation of etodolac

Abstract

A sustained release formulation of etodolac for once daily administration is described.

Description

field of invention

[0001] The present invention relates to sustained-release formulations of etodolac for once-daily administration. Background of the invention

[0002] U.S. Patent 3,939,178 discloses etodolac (1,8-diethyl-1,3,4,9-tetrahydropyrano(3,4-b)-indole-1-acetic acid or its pharmaceutically acceptable It has been reported to have analgesic and anti-inflammatory properties. It can also treat gout by reducing the level of uric acid in human blood (US Patent 4,663,345), and treat rheumatoid arthritis by reducing rheumatoid factor in blood (US Patent 4,742,076).

[0003] Etodolac is approved to control the symptoms and symptoms of osteoarthritis, rheumatoid arthritis, and to control pain. The usual dosage is 800 mg to 1200 mg, given in 2-4 divided doses. This dosing regimen is problematic because it is very inconvenient to the patient and makes it difficult for the patient to comply. Those skilled in the art know that sustained release systems can reduce the frequen...

Examples

Embodiment Construction

[0008] The etodolac used in the present invention is preferably micronized to increase its total surface area and improve its solubility. Hydroxypropyl cellulose (HPC) is a partially substituted poly(hydroxypropyl) ether of cellulose available from Klucel under the tradename TM (Aqualon), Methocel TM (Dow Chemical Co.) and Nisso HPC TM . According to the invention, the carrier base material preferably comprises one or more viscosity grades of HPC. More preferably, the hydroxypropylcellulose is selected from viscosity grades (2% in water at 20°C) of 6.0-10.0 centipoise (HPC-L) and 150-400 centipoise (HPC-M). HPC-L is present in an amount of about 5-40% by weight of the formulation, preferably 5-20% by weight of the formulation, and HPC-M is present in an amount of about 5-25% by weight, more preferably about 5% by weight of the formulation. -15% by weight. HPC-L is a fast-swelling material that allows for controlled initial drug release from the dosage form. HPC-M control...

field of invention

[0001] The present invention relates to sustained-release formulations of etodolac for once-daily administration. Background of the invention

[0002] U.S. Patent 3,939,178 discloses etodolac (1,8-diethyl-1,3,4,9-tetrahydropyrano(3,4-b)-indole-1-acetic acid or its pharmaceutically acceptable It has been reported to have analgesic and anti-inflammatory properties. It can also treat gout by reducing the level of uric acid in human blood (US Patent 4,663,345), and treat rheumatoid arthritis by reducing rheumatoid factor in blood (US Patent 4,742,076).

[0003] Etodolac is approved to control the symptoms and symptoms of osteoarthritis, rheumatoid arthritis, and to control pain. The usual dosage is 800 mg to 1200 mg, given in 2-4 divided doses. This dosing regimen is problematic because it is very inconvenient to the patient and makes it difficult for the patient to comply. Those skilled in the art know that sustained release systems can reduce the frequen...

Examples

Embodiment Construction

[0008] The etodolac used in the present invention is preferably micronized to increase its total surface area and improve its solubility. Hydroxypropyl cellulose (HPC) is a partially substituted poly(hydroxypropyl) ether of cellulose available from Klucel under the tradename TM (Aqualon), Methocel TM (Dow Chemical Co.) and Nisso HPC TM . According to the invention, the carrier base material preferably comprises one or more viscosity grades of HPC. More preferably, the hydroxypropylcellulose is selected from viscosity grades (2% in water at 20°C) of 6.0-10.0 centipoise (HPC-L) and 150-400 centipoise (HPC-M). HPC-L is present in an amount of about 5-40% by weight of the formulation, preferably 5-20% by weight of the formulation, and HPC-M is present in an amount of about 5-25% by weight, more preferably about 5% by weight of the formulation. -15% by weight. HPC-L is a fast-swelling material that allows for controlled initial drug release from the dosage form. HPC-M control...