Novel pharmaceutical modified release dosage form composition comprising cyclooxygenase enzyme inhibitor

Abstract

Pharmaceutical modified release dosage form comprising at least one cyclooxygenase enzyme inhibitor or its pharmaceutically acceptable salts, esters, prodrugs, solvates, hydrates, or derivatives thereof as active agent, with a pharmaceutically acceptable carrier for controlling the release of the cyclooxygenase enzyme inhibitor is provided. The dosage form preferably provides a release of not more than about 60 % of the cyclooxygenase enzyme inhibitor in 1 hour and not less than about 75 % of the cyclooxygenase enzyme inhibitor after 12 hours when tested in accordance with the dissolution method (I) described herein employing Distilled water with 2.0 % Sodium lauryl sulphate as the dissolution medium or in accordance with the dissolution method (II) described herein employing pH 7.0 Phosphate buffer with 2.0% Sodium lauryl sulphate as the dissolution medium or in accordance with the dissolution method (III) described herein employing 0.001 N Hydrochloric acid with 1.0 % Sodium lauryl sulphate as dissolution medium. Further, the pharmaceutical composition of the present invention when tested in a group of healthy humans preferably achieves a mean peak plasma concentration (Cmax) after at least about 1 hour of administration of the dosage form,. The present invention also provides process of preparing such dosage form compositions and prophylactic and / or therapeutic methods of using such dosage form.

Description

technical field [0001] The present invention relates to a pharmaceutical controlled release dosage form comprising as active agent at least one cyclooxygenase inhibitor or a pharmaceutically acceptable salt, ester, prodrug, solvate, hydrate or derivative thereof, and A pharmaceutically acceptable carrier for controlling the release of the cyclooxygenase inhibitor. Furthermore, the pharmaceutical composition of the present invention is used to administer a therapeutically and / or prophylactically effective amount of said active agent. In addition, when according to the dissolution test method (I) described herein, distilled water containing 2.0% sodium lauryl sulfate was used as the dissolution medium, or according to the dissolution test method (II) described herein, distilled water containing 2.0% sodium lauryl sulfate was used as the dissolution medium. Phosphate buffered saline with a pH of 7.0 of sodium alkyl sulfate as the dissolution medium, or when tested according to t...

AI Technical Summary

Problems solved by technology

[0003] Drug levels can be maintained above lower plasma therapeutic levels for longer periods of time by administering larger doses of conventionally formulated dosage forms, but this approach may produce toxic effects due to high plasma drug concentrations

Alternatively, another approach is to administer the drug at regular intervals, which results in fluctuations in drug levels, the so-called peak-to-trough effect

This approach is often accompanied by several potential problems, such as large peak (toxic effects) and trough (inactive drug levels) effects, and lack of patient compliance, leading to ineffectiveness or failure of drug therapy

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