Novartis Ag

Emisphere Technologies, Inc.

Nordic Bioscience A/s

Novartis Pharma Gmbh

Simon David Bateman

Moise Azria

Joseph Ault

Joseph Sikora

Michael M Goldberg

Shoufeng Li

Rajesh K Agarwal

Joseph Zielinski

Kiran Chaudhary

Subash Patel

Rebecca F Yang

Shingai Majuru

JoAnne P Corvino

William Elliot Bay

Alan Edward Royce

Anasuya Ashok Ghosh

William Elliott Bay

Claus Christiansen

James F McLeod

Shingai Majura

JoAnne P Russo

Mosise Azria

Gregory Sparta

Rebecca Fai-ying Yang

Jie Xiao

Joseph M Ault

Joanne P Russo

Joseph Murray Ault

Joseph L Zielinski

Rebecca Fai-Ying Yang

The present invention provides oral pharmaceutical compositions that enable the successful delivery of drugs in a pharmaceutically effective amount, particularly poly (amino acids) such as peptides, peptidomimetics and proteins. e.g. hormones to a subject via oral administration to accomplish the desired therapeutic effect. The oral pharmaceutical composition comprising a poly (amino acid) as the active ingredient, e.g. a peptide or protein, shows a rapid disintegration and/or dissolution such that the active ingredient is able to attain a therapeutic effect.

Pharmaceutical composition

Pharmaceutical compositions for the effective oral delivery of a parathyroid hormone, PTH, as well as methods for administration of the compositions are provided. Additionally, methods for stimulating new bone formation and treating and/or preventing osteoporosis are also provided.

5-CNAC as oral delivery agent for parathyroid hormone fragments

The present invention relates to a novel use of calcitonin in osteoarthritis, and to methods of treating and/or preventing osteoarthritis in mammals, particularly humans.

Use of calcitonin in osteoarthritis

Solid pharmaceutical compositions and methods of their use 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 utilize micronized forms of the delivery agent which provides enhanced bioavailability of pharmacologically active agents, particularly calcitonin.

Method for treating bone related diseases and calcium disorders

A method of inhibiting blood platelet aggregation in a mammal is provided. The method comprises the administration of a platelet aggregation inhibiting amount of a modified amino acid or pharmaceutically acceptable salt thereof.

Modified amino acid for the inhibition of platelet aggregation

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

Orally dosed pharmaceutical compositions comprising a delivery agent in micronized form

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

Disclosed is a particular method of orally administering pharmaceutical compositions comprising calcitonin in combination with oral delivery agents, prior to the consumption of food in humans, and a method of treatment of disorders responsive to the action of calcitonin employing such method of administration; also oral calcitonin pharmaceutical compositions with particular ratios of the amount of oral delivery agent to the amount of calcitonin.

Oral administration of 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

Growing community of inventors

Randolph, NJ, United States of America

Simon David Bateman