Merck Sharp + Dohme Corp.

Merck + Co., Inc.

Acryspharm LLC

Istituto Di Ricerche Di Biologia Molecolare P. Angeletti Spa

Hsien-Hsin Tung

Benjamin Cohen

Aaron S Cote

Craig B Ikeda

Robert A Reed

Justin Moser

Erik A Dienemann

Vincent R Capodanno

Jeannie Chow Wong

Brian Sell

Qingxi Wang

Cindy Starbuck

Pavol Rajniak

Kimberly Gallagher

Kevin Michael Belyk

Daniel J Kumke

Amar J Mahajan

Henry G Morrison

Vanessa Pruzinsky

Lawrence Wai

Philip Jones

Thomas Allen Miller

John M Williams

Ulf H Dolling

Vincenzo Summa

Raymond Cvetovich

Philip J Pye

Louis S Crocker

Daniel Richard Sidler

Robert Wenslow

Joseph Kukura, Ii

Scott D Reynolds

Remy Angelaud

Brian K Johnson

Danny Mancheno

V Brett Cooper

Stanley Waterson

Daniel Sidler

Joseph Ii Kukura

Louis Crocker

Kevin M Belyk

A pharmaceutical composition of high drug loading comprising an active pharmaceutical ingredient (API) and pharmaceutical acceptable additives, which include glass-solution forming additive and/or eutectic-mixture forming additive, is provided. The composition is dispersed uniformly to form a hybrid solid dispersion consisting of crystalline-suspension, glass-solution and/or eutectic-mixture, where the crystalline API is uniformly distributed in the hybrid solid dispersion and exists in nano/micro particle size range. The amorphous API, when present, is uniformly distributed in the hybrid solid dispersion. The API may exist in different chemical and/or physical forms. The API is present in an amount of from more than about 50% wt/wt to about 90% wt/wt with respect to the total amount of the active pharmaceutical ingredient and the pharmaceutically acceptable glass-solution forming and/or eutectic-mixture forming additives. At least about 50% wt/wt of the API is dispersed in the crystalline-suspension and at least about 5% wt/wt of the API is dispersed in the glass-solution and/or eutectic-mixture. The pharmaceutical composition offers excellent dissolution rate, superior chemical and physical stability, and minimum drug-drug/drug-excipient incompatibility. The composition is beneficial for reducing the overall tablet/capsule size for low water-soluble drugs requiring high drug loading or dosage, including combination drugs.

High drug loading pharmaceutical compositions

The present invention provides a pharmaceutical composition or crystalline composition with a specific dissolution profile, which comprises suberoylanilide hydroxamic acid or a pharmaceutically acceptable salt or hydrate thereof as an active ingredient. The present invention provides a process of producing said crystalline composition or pharmaceutical composition. The present invention also provides compositions with a specific particle size distribution.

Formulations of suberoylanilide hydroxamic acid and methods for producing same

Potassium salts of Compound A and methods for their preparation are disclosed, wherein Compound A is of formula: Compound A is an HIV integrase inhibitor useful for treating or prophylaxis of HIV infection, for delaying the onset of AIDS, and for treating or prophylaxis of AIDS.

Process for preparing N-alkylated hydroxypyrimidinone compounds

Formulations of suberoylanilide hydroxamic acid and methods for producing the same

Potassium salt of an HIV integrase inhibitor

The present invention relates to a process for reducing the levels of organic solvents to pharmaceutically acceptable levels in thermally unstable crystalline carbapenem solids represented by formula I:or a salt thereof, wherein Rand R, are the same or different, and are selected from H, alkyl, aryl, and heteroaryl, comprising washing a carbapenem solid containing organic solvent with an organic solvent containing water; and using vacuum and/or inert gas (hydrated or dry) at low temperature to produce a compound of formula I containing pharmaceutically acceptable levels of organic solvents, wherein the water content of the crystalline carbapenem solid, correcting for organic solvents, is maintained at about 13% to about 25% during the process.

Process for making carbapenem compounds

A process is disclosed for the formation and resolution of (S)-ibuprofen-(S)-lysine. The process employs preferential crystallization to separate a pair of diasteromeric salts, (S)-ibuprofen-(S)-lysine and (R)-ibuprofen-(S)-lysine.

Formation and resolution of ibuprofen lysinate

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Edison, NJ, United States of America

Hsien-Hsin Tung