ORAL DOSAGE FORMS FOR OXYGEN-CONTAINING ACTIVE AGENTS AND OXYL-CONTAINING POLYMER

摘要

The disclosed invention is drawn to pharmaceutical tablets that provide delivery of active agents having at least three oxygen-containing groups, as well as a second active ingredient. Non-limiting examples of three oxygen-containing group active agents include guaifenesin, codeine, hydrocodone, and their pharmaceutically acceptable salts. In one embodiment, a pharmaceutical tablet for oral administration once every 12 hours is provided. The tablet includes a first active agent that is a tri-oxy active agent, a second active agent, and a release rate controlling non-ionic oxyl-containing hydrophilic polymer. The total oxyl content of the hydrophilic polymer in the tablet is about 4×10−4 moles to about 2.0×10−3 moles.

主权项

1. A method of treatment, said method comprising:
administering to an individual having cough or cold, twice a day, a pharmaceutical composition which is a solid tablet comprising 54 mg of codeine phosphate and 8 mg chlorpheniramine maleate or a pharmaceutically acceptable salt of chlorpheniramine; said method providing (i) a mean AUCinf of codeine and chlorpheniramine that is 70% to 135% of the respective mean AUCinf provided by an immediate release dosage administered to a subject under fasted conditions every 4 to 6 hours over a 12 hour time period, where the cumulative dosage amount administered over the 12 hour time period of codeine and chlorpheniramine in the immediate release oral dosage is equivalent to the respective amount in said pharmaceutical composition; and wherein (ii) the variation in a pharmacokinetic parameter for codeine and chlorpheniramine in the oral dosage form is not more than about 40% as compared to the same pharmacokinetic parameter measured in the same subject when the pharmaceutical composition is administered under fed versus fasted condition.