Bristol-Myers Squibb Compnay

Otsuka Pharmaceutical Company, Limited

Sanofi-Aventis

Sanofi-Synthelabo

San Kiang

Chenkou Wei

Olivier Monnier

Mark D Lindrud

Christian Hoff

Bruno Franc

Deniz Erdemir

Shih-Ying Chang

Soojin Kim

Divyakant S Desai

Zhenrong Guo

Tamar Rosenbaum

Lifen Shen

Donald C Kientzler

Margaret M Gleeson

Donald Kientzler

Margaret Gleeson

The present disclosure relates to methods for making extended-release formulations of water-soluble active pharmaceutical ingredients such as metformin HCl. In one aspect, the disclosure provides a method that includes adding an aqueous solution of an active pharmaceutical ingredient to an agitated mixture of one or more release-modifying polymers and optionally one or more binders in one or more organic solvents, the one or more organic solvents together being an antisolvent for the active pharmaceutical ingredient, water being sufficiently soluble in the one or more organic solvents such that the water added as part of the aqueous solution dissolves in the mixture, the addition thereby precipitating the active pharmaceutical ingredient; separating the active pharmaceutical ingredient and the one or more release-modifying polymers and, if present, the one or more binders from the one or more organic solvents to yield co-processed particles; and drying the co-processed particles. The methods can be used to make dosage forms such as tablets having reduced amounts of release-modifying polymers.

Extended release pharmaceutical formulations of water-soluble active pharmaceutical ingredients and methods for making the same

A process for the production of a formulation of HIV attachment inhibitor piperazine tris salt prodrug compound involves dissolving the prodrug compound in a solvent to form a solution; adding a first quantity of a first anti-solvent to the solution; then dispersing a first quantity of HPMC in the solution; adding a second quantity of the first anti-solvent to the solution; dispersing a second quantity of HPMC in the solution; then adding a second anti-solvent to the solution so as to crystallize the compound with the HPMC and thereby form the formulation, wherein the second anti-solvent is a combination of acetone and isopropyl acetate (IPAC). The formulation is then washed, and dried.

Co-processing method and formulations for HIV attachment inhibitor prodrug compound and excipients

A process is provided for making sterile aripiprazole having an average particle size less than 100 microns but preferably greater than 25 microns employing an impinging jet crystallization procedure. The resulting bulk aripiprazole of desired particle size may be used to form a sterile freeze-dried aripiprazole formulation, which upon constitution with water and intramuscular injection releases aripiprazole over a period of at least about one week and up to about eight weeks.

Process for making sterile aripiprazole of desired mean particle size

The present invention provides a method for making glycoside compounds including the steps of: (a) lithiating an aromatic reactant having a leaving group using a lithium reagent in a first microreactor under non-cryogenic conditions to form a lithiated anion species, and (b) coupling the lithiated anion species with a carbonyl substituted reactant to form a glycoside.

Non-cryogenic process for forming glycosides

The invention relates to a novel crystalline form of irbesartan to pharmaceutical compositions containing it, to processes for preparing it, and to a method for treating cardiovascular diseases utilizing it.

Form of irbesartan, processes for obtaining the said and pharmaceutical compositions containing it

The invention relates to a novel crystalline form of irbesartan, to pharmaceutical compositions containing it, to processes for preparing it, and to a method for treating cardiovascular diseases utilizing it.

Form of irbesartan, methods for obtaining said form and pharmaceutical compositions containing same

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Madison, NJ, United States of America

San Kiang