Formulations of (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione

摘要

Pharmaceutical compositions and single unit dosage forms of apremilast, i.e., (+)-2-[1-(3-ethoxy-4-methoxyphenyl)-2-methylsulfonylethyl]-4-acetylaminoisoindoline-1,3-dione, or a pharmaceutically acceptable stereoisomer, prodrug, salt, solvate, hydrate, or clathrate, are provided herein. Also provided are methods of treating, managing, or preventing various disorders, such as diseases or disorders ameliorated by the inhibition of TNF-α production in mammals.

主权项

1. An immediate-release oral dosage form comprising about 10-30% by weight of apremilast, about 40-50% by weight of lactose, about 20-30% by weight of cellulose, about 1-5% by weight of carboxymethyl cellulose, about 1-5% by weight of fumed silica and about 0.1-2% by weight of magnesium stearate and about 1-5% by weight of a coat, wherein about 100% of said apremilast is released in about 1 hour in an aqueous buffer solution of about pH 3 with a paddle speed of 75 rpm.