Wockhardt Limited

Wockhart Limited

Habil Fakhruddin Khorakiwala

Mahesh Vithalbhai Patel

Noel John De Souza

Dilip J Upadhyay

Nishith Chandra Chaturvedi

Nitin Shetty

Shivkumar Agarwal

Sreenivas Kandepu

Abraham Thomas

Satish B Bhawsar

Milind Chintaman Shukla

Shrikant V Gupte

Vinay K Sharma

Javed Hussain

Sheela Chandresekharan Nair

Mohammed A Jafri

The present invention relates to optically pure S-(&#x2212;)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof, substantially free of their R-(+)-isomers, to processes for preparation of the optically pure S-(&#x2212;)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof substantially free of their R-(+)-isomers, and to pharmaceutical compositions comprising the S(&#x2212;)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof.

Antibacterial optically pure benzoquinolizine carboxylic acids, processes, compositions and methods of treatment

Compounds are described which are efflux pump inhibitors of cellular efflux pumps of microbes. Also described are methods of preparing such compounds, methods of using such efflux pump inhibitor compounds and pharmaceutical compositions which include such compounds.

Inhibitors of cellular efflux pumps of microbes

The present invention relates to optically pure S-(&minus;)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof, substantially free of their R-(&plus;)-isomers, to processes for preparation of the optically pure S-(&minus;)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof substantially free of their R-(&plus;)-isomers, and to pharmaceutical compositions comprising the S(&minus;)-benzoquinolizine carboxylic acids, their derivatives, salts, pseudopolymorphs, polymorphs and hydrates thereof. These compounds and compositions can be used to systemically and topically treat bacterial Gram-positive, Gram-negative and anaerobic infections, specially resistant Gram-positive organism infections, Gram-negative organism infections, mycobacterial infections and emerging nosocomial pathogen infections, while avoiding toxic effects associated with the administration of the racemic mixture of RS-(&plusmn;)-benzoquinolizine carboxylic acid. The compounds and compositions of this invention can also be used to treat diseases and disorders caused by Gram-positive, Gram-negative and anaerobic bacteria, and diseases and disorders caused by resistant Gram-positive organisms, Gram-negative organisms, mycobacteria and nosocomial pathogens.

A once-a-day controlled release drug delivery system of diltiazem hydrochloride is provided, which is bioequivalent in plasma profile of Cardizem CD. The fast, medium, and slow release fractions are prepared using various compositions and weight gains. The individual fill weights are computed and then are filled into the same capsule using specialized encapsulation equipment using a triple-filling process. A preferred membrane dispersion that is used for preparing the fast release fraction contains 0.2% of sodium lauryl sulfate along with 20% of water soluble plasticizer (triethyl citrate), and 2% silicone dioxide, based on quaternary polymethacrylate on the weight basis. This combination provides an initial pulsatile burst after a lag time of 2 hours, leading to in-vivo bioequivalence. The preferred membrane dispersion that is used for preparing the medium release and the slow release fractions contain 16% of water soluble plasticizer along with 5% silicone dioxide, based on quaternary polymethacrylate. This combination provides an optimal glass transition temperature that allows for the preparation of exceptionally increased weight gains. Additionally, it provides targeted input of drug release for achieving bioequivalence. Regardless of significant in-vitro inequivalence to the release rate profile of the innovator product, the in vivo-equivalence data comply with required regulatory guidelines.

Composition for pulsatile delivery of diltiazem and process of manufacture

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Mumbai, India

Habil Fakhruddin Khorakiwala