Gilead Sciences, Inc.

Kalvista Pharmaceuticals Limited

Eyegate Pharmaceuticals, Inc.

Evonik Corporation

Eyetech Inc.

Gary Paul Cook

Choung U Kim

Michael A Patane

Zheng-Yu Yang

John C Rohloff

Gong-Xin He

Perry Calias

Jianying Wang

Xiaoqin Cheng

Mike Jaffe

Manoj C Desai

William A Lee

Edward Doerffler

Garry Thomas Gwozdz

Theodore Patrick Laslo

Pericles Calias

Michael John Frodsham

Kathleen M Campbell

Richard Simon Todd

Jamie Joseph Farrar

Robert Neil Ward

Michael Bryan Roe

Mary A Ganley

John Herman Collett

The present invention relates to oral solid dosage forms comprising a plasma kallikrein inhibitor, in particular a solid form (Form 1) of the compound of Formula A. Also provided are methods of preparing oral solid dosage forms comprising the compound of Formula A using Form 1 of the compound of Formula A.

Dosage forms comprising a plasma kallikrein inhibitor

The invention relates to aqueous suspension pharmaceutical compositions of poorly water soluble drugs, wherein said drugs are selected from compounds of formula I wherein R-Rare defined herein; processes for preparing these compositions and their use in medicine, especially their use in the treatment of ocular diseases.

Pharmaceutical compositions

Disclosed herein are formulations of dexamethasone or a prodrug thereof suitable for delivery by ocular iontophoresis and methods of use thereof.

Ocular iontophoretic delivery of dexamethasone and formulations thereof

The invention relates to aqueous suspension pharmaceutical compositions of poorly water soluble drugs, wherein said drugs are selected from compounds of formula (I) (Formula (I)), wherein R-Rare defined herein; processes for preparing these compositions and their use in medicine, especially their use in the treatment of ocular diseases. 

Pharmaceutical compositions suitable for parenteral administration comprising aqueous suspensions of benzylamine derivatives having low solubilities

Delivery of corticosteroids through iontophoresis

The compositions disclosed herein are for use as controlled release therapeutics for the treatment of a wide variety of diseases. In particular, the compositions provide water soluble bioactive agents, organic ions and polymers where the bioactive agent is efficiently released over time with minimal degradation products. The resulting controlled release composition is capable of administration in a decreased dose volume due to the high drug content and predominance of non-degraded bioactive agent after release. Additionally, the compositions, of the present invention are capable of long term, sustained releases.

Controlled release compositions

Formulations for controlled, sustained release of biologically active agents for the treatment of ocular disorders have been developed. These formulations are based on solid microparticles formed of the combination of biodegradable, synthetic polymers such as poly(lactic acid) (PLA), poly(glycolic acid) (PGA), and copolymers thereof. The microparticles are characterized by low burst levels and efficient drug loading and sustained release.

Controlled release microparticles

The methods disclosed herein are of use for the production of controlled release compositions. In particular, the methods provide the contacting of an organic phase containing a bioactive agent and a polymer with an aqueous phase containing an organic ion to create controlled release compositions containing bioactive agents. The present invention also includes controlled release compositions including a polymer, an organic ion and a bioactive agent. The present invention also includes methods of using such controlled release compositions. The usefulness of the present invention is that the methods result in the production of controlled release compositions containing bioactive agent capable of administration in a concentrated low-dose form, having low burst and reduced production of degraded bioactive agent.

Method for the preparation of controlled release formulations

Compounds and compositions of Formula I are described, useful as anti-proliferative agents, and in particular anti-HPV, wherein:

Anti-proliferative compounds, compositions, and methods of use thereof

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Westford, MA, United States of America

Gary Paul Cook