Pharmaceutical composition for combination of piperidinoalkanol-decongestant

Abstract

The present invention provides a pharmaceutical composition in the form of a bilayer tablet comprising, (a) a first discrete zone made with Formulation (A) which comprises, a therapeutically effective decongestant amount of a sympathomimetic drug, or a pharmaceutically acceptable salt thereof, in an amount of about 18% to about 39% by weight of Formulation (A), and a first carrier base material, the first carrier base material comprising a mixture of; (I) carnauba wax in an amount of about 59% to about 81% by weight of Formulation (A); and (ii) a suitable antiadherent in an amount of about 0.25% to about 2.00% by weight of Formulation (A); wherein said first carrier base material provides a sustained release of the sympathomimetic drug; and (b) a second discrete zone made with Formulation (B) which comprises a therapeutically effective antihistaminic amount of a piperidinoalkanol, or a pharmaceutically acceptable salt thereof, in an amount of about 15% to about 30% by weight of Formulation (B) and a second carrier base material, the second carrier base comprising a mixture of; (I) a cellulose diluent in an amount of about 27% to about 73% by weight of Formulation (B); (ii) pregelatinized starch in an amount of about 15% to about 30% by weight of Formulation (B); (iii) a suitable disintegrant in an amount of about 0.25% to about 6.00% by weight of Formulation (B); and (iv) a suitable lubricant in an amount of about 0.25% to about 2.00% by weight of Formulation (B); wherein said second carrier base material provides an immediate release of the piperidinoalkanol or the pharmaceutically acceptable salt thereof.

Description

Background of the invention [0001] Various piperidinoalkanol compounds have been identified as antihistamines, antiallergics and bronchodilators, see eg US Patent Nos. 3,878,217, 4,254,129 and 4,285,957. Several examples of formulations of these various piperidinoalkanol compounds are disclosed below. [0002] J. Domet and D. Shah in U.S. Patent No. 4,929,625 describe a pharmaceutical composition in solid unit dosage form comprising a therapeutically effective amount of a piperidinoalkanol compound or a pharmaceutically acceptable salt thereof, The pharmaceutically acceptable nonionic or cationic surfactant accounts for about 0.1-6% by weight of the composition, and the pharmaceutically acceptable carbonate salt accounts for about 2-50% by weight of the composition. [0003] N. Web and G. Hammer in U.S. Patent No. 4,996,061 describe a pharmaceutical composition in the form of a multilayer compressed tablet comprising two separate regions made of different compositions, the co...

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Problems solved by technology

However, this formulation was also unsuccessful as some of the samples collected during tablet compression and used to test content uniformity did not meet United States Pharmacopeia (USP) requirements

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