Bristol-myers Squibb Compnay

Krishnaswamy Srinivas Raghavan

Sailesh A Varia

Timothy M Malloy

Andrea Panaggio

Rebanta Bandyopadhyay

Sunanda A Ranadive

Sailesh Amilal Varia

Jack Z Gougoutas

Vijay H Naringrekar

John D DiMarco

Francis Y F Lee

Robert K Perrone

William L Parker

Ismat Ullah

Christopher P Price

Ann W Newman

Martha Davidovich

Rajesh Babulal Gandhi

Miriam K Franchini

Sachin S Chandran

Thomas A Haby

Jaquan Kalani Levons

Veronique Trognon

Kenneth S Bembenek

Richard G Corrao

Loutfy Benkerrour

Luigi Esposito

Marvin Barry Cohen

Robert Kevin Perrone

Sachin Chandran

A process for formulating certain epothilone analogs for parenteral administration is disclosed wherein the analog is dissolved in a mixture of at least 50% by volume tertiary-butanol in water, the mixture is lyophilized, the resulting lyophilized product is packaged in one vial with a sufficient amount of solvent comprising anhydrous ethanol and a suitable nonionic surfactant in a second vial. All steps are carried out with protection from light. In use, the contents of the second or diluent vial are added to the lyophilized product and mixed to constitute the epothilone analog and the resulting solution is diluted with a suitable diluent to produce a solution for intravenous injection containing the epothilone analog in a concentration of from about 0.1 mg/mL to about 0.9 mg/mL. A preferred surfactant is polyethoxylated castor oil and a preferred diluent is Lactated Ringer's Injection.

Parenteral formulation for epothilone analogs

Pharmaceutical capsule compositions containing the active compound (2R)-2-[[(4-chlorophenyl)sulfonyl][[2-fluoro-4-(1,2,4-oxadiazol-3-yl)phenyl]methyl]amino]-5,5,5-trifluoropentanamide, and polyethylene glycol (PEG), Vitamin E polyethylene glycol succinate, polyvinylpryrrolidone (PVP) or copovidone (PVP-Polyvinyl acetate), with or without citric acid, are provided.

Bioavailable capsule compositions of amorphous alpha-(N-sulfonamido)acetamide compound

The invention relates to methods of increasing the bioavailability of orally administered epothilones. Epothilones administered by the methods of the invention are sufficiently bioavailable to have a pharmacological effect. The invention further relates to pharmaceutical compositions, pharmaceutical dosage forms, and kits for use in the methods of the invention.

Pharmaceutical compositions, dosage forms and methods for oral administration of epothilones

Pharmaceutical compositions containing C-21 modified epothilone derivatives, methods for their preparation and dosing regimen for administration of these epothilone compounds are provided. The compositions are stable and readily prepared for administration by dissolution in aqueous vehicles suitable for intravenous administration. A process for formulating C-21 modified epothilone derivatives for oral and parenteral administration is disclosed.

Pharmaceutical compositions and methods of using C-21 modified epothilone derivatives

Methods of administering epothilone analogs for the treatment of cancer

There is provided in accordance with the present invention the quinolone antibacterial gatifloxacin adequately taste-masked so that it can be utilized for pediatric formulations. A crystalline co-precipitate of gatifloxacin and one or both of stearic acid and palmitic acid in a narrow weight ratio has been found to effectively mask the bitter taste of gatifloxacin. The taste of gatifloxacin is effectively masked in the mouth and in aqueous suspension through a full dosage cycle, typically fourteen days. Gatifloxacin in the subject crystalline co-precipitates has been found to be readily available for absorption from the stomach.

Pediatric formulation of gatifloxacin

The invention relates to methods of increasing the bioavailability of orally administered epothilones. Epothilones administered by the methods of the invention are sufficiently bioavailable to have a pharmacological effect The invention further relates to pharmaceutical compositions, pharmaceutical dosage forms, and kits for use in the methods of the invention.

Gatifloxacin pentahydrate

A ras-farnesyltransferase inhibitor complex formed of ras-farnesyltransferase inhibitor or a pharmaceutically acceptable salt thereof, of the formula I

Complex of ras-farnesyltransferase inhibitor and sulfobutylether-7-&bgr;-cyclodextrin or 2-hydroxypropyl-&bgr;-cyclodextrin and method

Growing community of inventors

Cranbury, NJ, United States of America

Krishnaswamy Srinivas Raghavan