Rhone-Poulenc Rorer Pharmaceuticals Inc.

Aventis Pharmaceuticals Inc.

Aventis Pharmaceuticals Products Inc.

Zofia J Chrzan

Matthew R Powers

Benoit J Vanasse

Adam W Sledeski

James P Sherbine

Walter Rodriguez

James J Mencel

Rick G Woodward

Robert C Liu

Gregory G Kubiak

Mark P Warchol

Vincent Windisch

David Toledo-Velasquez

Anthony J Gardetto

Narasimha M Vemuri

Diane C Salazar

Diane C Salazar, Deceased

STABLE NON-HYGROSCOPIC CRYSTALLINE FORM OF N-&lsqb;N-&lsqb;N-(4-(PIPERIDIN-4-YL)BUTANOYL)-N-ETHYLGLYCYL&rsqb;ASPARTYL&rsqb;-L-&bgr;-CYCLOHEXYL ALANINE AMIDE, INTERMEDIATES THEREOF, AND PREPARATION THEREOF AND OF ANTITHROMBOTIC AZACYCLOALKYLALKANOYL PEPTIDES AND PSEUDOPEPTIDES

The invention is directed to a non-hygroscopic stable crystalline form of the antithrombotic compound N-[N-[N-(4-piperdin-4-yl)butanoyl)-N-ethylglycyl]-(L)-aspartyl]-(L)-.beta. -cyclohexyl-alanine amide, to processes for preparing said stable crystalline form, to a pharmaceutical composition thereof, and intermediates thereof, and the invention is directed also to processes for preparing a compound of the formula ##STR1## wherein: A, B, Z, E.sup.1, E.sup.2, G, R, m, n, and p are as defined herein.

Stable non-hygroscopic crystalline form of

In a method in which an ionizable pharmaceutical material, such as theophylline, having a pharmaceutically-active anionic group is bonded to an anion exchange resin having cationic groups bonded to displacable anionic groups by bringing said material and said resin into contact with each other under conditions such that the pharmaceutically-active anionic group of said material is bonded to the cationic group of said resin and replaces the anionic group thereof, the improvement comprising effecting said contact in an environment which is substantially free of carbon dioxide and/or bicarbonate ion, a pharmacologically active composition comprising said pharmaceutically active anion and said resin, including a composition in which at least about 40% of the binding capacity of the resin comprises said pharmaceutically active anion, and a sustained release pharmaceutical composition, including enteric coated particles of the composition, and stabilizing said composition by maintaining it in an environment substantially free of bicarbonate and/or carbon dioxide.

Binding pharmaceuticals to ion exchange resins

Binding theophylline to ion exchange resins

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Sellersville, PA, United States of America

Zofia J Chrzan