Novartis Ag

Emisphere Technologies, Inc.

Joseph Ault

Simon David Bateman

Moise Azria

Joseph Sikora

Michael M Goldberg

Rajesh K Agarwal

Kiran Chaudhary

Subash Patel

Rebecca F Yang

Joseph Zielinski

Shingai Majuru

JoAnne P Corvino

William Elliot Bay

William Elliott Bay

James F McLeod

Mosise Azria

Gregory Sparta

Rebecca Fai-ying Yang

Jie Xiao

Shingai Majura

JoAnne P Russo

The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. Preferred delivery agents include, but are not limited to, N-(5-chlorosalicyloyl)-8-aminocaprylic acid (5-CNAC), N-(10-[2-hydroxybenzoyl]amino)decanoic acid (SNAD), and sodium N-(8-[2-hydroxybenzoyl]amino)caprylate (SNAC). The invention also provides methods of preparing the disodium salt, ethanol solvate, and hydrate and compositions containing the disodium salt, ethanol solvate, and/or hydrate.

Disodium salts, monohydrates, and ethanol solvates for delivering active agents

The inventors have discovered that the disodium salt of certain delivery agents has surprisingly greater efficacy for delivering active agents than the corresponding monosodium salt. Furthermore, the inventors have discovered that the disodium salts of these delivery agents form solvates with ethanol and hydrates with water. The delivery agents have the formula wherein

A method for orally administering a parathyroid hormone, PTH, comprising orally co-administering to a patient in need of PTH an effective amount of a PTH and an effective amount of calcitonin. The method according to the invention allows for the oral administration of PTH without the hypercalcemia, hypercalcuria and nephrolithiasis side effects.

Orally administering parathyroid hormone and calcitonin

Solid pharmaceutical compositions suitable for the oral delivery of pharmacologically active agents, e.g. peptides, comprising a therapeutically-effective amount of a pharmacologically active agent; a crospovidone or povidone; and a delivery agent for said pharmacologically active agent are disclosed. The compositions provide excellent oral bioavailability of pharmacologically active agents, particularly calcitonin.

Pharmaceutical compositions for the oral delivery of pharmacologically active agents

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Blairstown, NJ, United States of America

Joseph Ault