Schering Corporation

Charles G Eckhart

Pui-Ho C Yuen

Michael B Mitchell

Nancy Levine

Teresa Etlinger

Doris P Schumacher

John S Chiu

Junning Lee

Tsong-Toh Yang

Paul E McNamara

John K Jenkins

Stanley Rosenhouse

Stephen K C Yu

Naneshwar S Sawant

Lawrence R Rogers

Richard E Youngstrom

Methods of preparing particulates for agglomeration, having a specified particle size distribution and desired convertible amorphous content, are described. The method involves a plurality of micronizing steps at least two of which are separated by a curing step. In the curing step, a stimulus such as humidity may be used to crystallize at least some, and in many instances preferably all, of the convertible amorphous content.

Method of preparing particles for agglomeration

8-chloro-6,11-dihydro-11-(4-piperidylidine)-5H-benzo&lsqb;5,6&rsqb;cyclohepta&lsqb;1-2-b&rsqb; pyridine

The invention relates to the novel compound mometasone furoate monohydrate, process for its preparation and pharmaceutical compositions containing said compound.

Process for making mometasone furoate monohydrate

Mometasone furoate monohydrate, process for making same and

A novel, stable, crystalline sodium (5R,6S,8R)-6-(1-hydroxyethyl)-2-(2-carbamoyloxyethylthio)-penem-3-carboxyl ate (designated as Form II) is prepared by forming a homogenous solution of sodium (5R,6S,8R)-6-(1-hydroxyethyl)-2-(2-carbamoyloxyethylthio)-penem-3-carboxyl ate combined with stirring the homogenous solution for a time and at a temperature sufficient to produce Form II and recovering Form II. Form II may also be prepared by contacting a first solution obtained by dissolving (5R,6S,8R)-6-(1-hydroxyethyl)-2-(2-carbamoyloxyethylthio)-penem-3-carboxyl ic acid in dimethylacetamide with a second solution obtained by dissolving a sodium salt of an organic acid having a pKa of up to about 5, e.g., sodium 2-ethylhexanoate in acetone, in the presence of at least 5 volume percent water while stirring the reaction mixture so formed at a temperature and for a time sufficient to produce Form II followed by recovering Form II. Form II exhibits a greater physical stability and increased solid state chemical stability and reduced hygroscopicity over that of the amorphous form (e.g., Form I) which renders Form II greatly superior to Form I as a clinically suitable antibacterial agent.

Crystalline sodium (5R, 6S,

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Scotch Plains, NJ, United States of America

Charles G Eckhart