Merck Sharp + Dohme Corp.

University of Houston System

Opko Health, Inc.

Pranav Gupta

Jiansheng Wan

Diana Shu-Lian Chow

David Monteith

Dong Liang

Yulan Qi

Robert K Evans

Akhilesh Bhambhani

Scott Trzaska

Soumendu Bhattacharya

Ronald L Smith

Donna M Williams

Jason Wan

Peter Wisniecki

Scott T Trzaska

Jaymin Shah

A composition comprising (S)&#x2014;N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide and hypromellose acetate succinate for pharmaceutical preparations, especially capsule preparations.

(S)-N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide compositions for pharmaceutical preparations

(S)-N-(3-6-isopropoxypyridin-3-3YL)-1H-indazol-5-yl)-1-(2-(4-4(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H-yl)-2-oxoethyl)-3(methylthio)pyrrolidine-3-carboxamide compositions for pharmaceutical preparations

The present invention provides a process for preparing enterically-coated lyospheres comprising a therapeutic agent comprising: a.) providing lyospheres comprising the therapeutic agent; b.) coating said lyospheres with an enteric polymer coating composition; and c.) isolating said enterically-coated lyospheres. In other embodiments, the invention provides dosage forms comprising a lyosphere comprising an effective amount of a therapeutic agent and an enteric polymer coating. In some embodiments, the therapeutic agent in the process or dosage form is a polypeptide, a protein, a peptide, a lipopeptide, a glycoprotein, a fusion protein, a protein conjugate, a cytokine, an enzyme, an antibody, an oligonucleotide, a vaccine vector, small molecule, a live virus, an inactivated virus, a virus-like particle, a viral protein subunit, an adjuvant, microbiome, a prebiotic, a probiotic, or an ectobiotic. In some embodiments of the present invention, after oral administration the dosage forms containing the enterically-coated lyospheres provide a method of delivering a therapeutic agent to the ileum, ileo-caecal junction, colon or a combination thereof in a subject.

Process for preparing formulations for gastrointestinal-targeted therapies

A composition comprising (S)&#x2014;N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide and hypromellose acetate succinate for pharmaceutical preparations, especially capsule preparations.

Disclosed are formulations and tablets made therefrom comprising the compound of Formula IA or Formula IB which have sustained-release properties, and the dispersion containing the compounds of Formula IA or IB which facilitates such sustained release: Formula IA, Formula IB. 

Sustained release formulation and tablets prepared therefrom

Provided herein are drug delivery systems, such as self-nanoemulsifying drug delivery systems, self-emulsifying drug delivery systems and parenteral microemulsion formulations, suitable for parenteral or oral delivery to a subject. The drug delivery systems may comprise a benzimidazole derivative, e.g., mebendazole, an oil, a surfactant, a cosurfactant and a dipolar aprotic solvent in a microemulsion formulation. Also provided are methods for improving the bioavailability of a benzimidazole derivative during treatment of a pathophysiological condition by using a formulation combining a particular emulsion droplet diameter and ratio of the surfactant:cosurfactant therein, for increasing concentration and retention of a benzimidazole derivative in the lung via a parenterally administerable microemulsion with droplet size of about 35 nm to less than 100 nm and for defining hemolytically safe microemulsions of a benzimidazole derivative during a therapeutic treatment via a parenterally administerable microemulsion with a surfactant:cosurfactant content by weight of about 6% to 48%.

Parenteral and oral formulations of benzimidazoles

Pharmaceutical compositions for intravenous administration comprising the compound of Formula I or pharmaceutically acceptable salts, hydrates or prodrugs thereof are described herein. Methods of preparing the pharmaceutical compositions and methods for treating nausea and/or emesis with the pharmaceutical compositions are also described herein.

Intravenous formulations of neurokinin-1 antagonists

Growing community of inventors

Short Hills, NJ, United States of America

Pranav Gupta