Paladin Labs Inc.

Paladin Labs (barbados) Inc.

Paladin Labs Europe Limited

Altus Formulation Inc.

Angelini Pharma, Inc.

Labopharm Inc.

Labopharm Europe Limited

Labopharm (barbados) Limited

Angelini Labopharm, LLC

Endo Ventures Limited

Damon Smith

Sonia Gervais

Miloud Rahmouni

Vinayak Sant

Ali Bichara

Jean-Michel Ndong

Ali El-Jammal

Shams Rustom

Frederic Duffayet

Rachid Ouzerourou

Angela Ferrada

Fouzia Soulhi

Pauline Contamin

My Linh Ma

Bobby-Ernst Boursiquot

Vincent Lenaerts

Wilms Baille

Piotr Kujawa

Marc Lemieux

Bradut Mitrasca

Dorothee Le Garrec

Sylvain Chemtob

David Lessard

Sylvie Bouchard

Sandra Gori

Laibin Luo

Francois Ravenelle

François Ravenelle

Johnatan Bacon

Patricia Laure Ouadji-Njiki

Patricia Laure Ouadji-Nijki

Jonathan Bacon

Rachid Ouzérourou

Samy Omri

Patricia Ouadji

Shiva Gosein

Vincent Lemaire

Samir Taga

Alexander Cunningham

Anna-Maria Szczesniak

Robert Zalega

Dorothée Le Garrec

Sybil Roberston

Louise Fortier

Dorothee Legarrec

Patricia Ouajdi

Abdelaziz Tafer

Melanie Kelly

Mohamed Nabil Khalid

Frédéric Duffayet

Milloud Rahmouni

Shams Rustoms

There are provided PVP-PLA block copolymers as defined in Formula (1): I wherein, x is an initiator alcohol having a boiling point greater than I 45° C., n is, on average, from 20 and 40, and m is, on average, from 10 and 40, wherein the block copolymers have a number average molecular weight (Mn) of at least 3000 Da. Polymers demonstrating flexibility in formulating multiple low solubility active pharmaceutical ingredients (APis) are described. Liquid and dry pharmaceutical formulations comprising an API are described, along with delivery methods, uses, and kits. APis may include, e.g. 11urbiprofon, celecoxib, acetaminophen, or propofol. Also provided is a method of synthesizing the PVP-PLA block copolymers by (i) initiating polymerization of D,L-Lactide from the initiator alcohol x to form poly(lactic acid), adding a xanthate to form a PLA macroinitiator, and polymerizing NVP onto the PLA macroinitiator, by controlled polymerization, to form the block copolymer compound of Formula (I).

Non-ionic PVP-PLA block copolymers and liquid pharmaceutical compositions derived therefrom

There is provide an extended release dosage form comprising a release modifying excipient comprising high amylose starch, cross-linked hydroxypropylated amylopectin, and a pre-gelatinized common starch; wherein the release modifying excipient is substantially free of crosslinks between amylose and amylopectin and substantially free of crosslinks between amylose and amylose. It has been found that the extended release properties of conventional cross-linked high amylose starches (e.g., Contramid&#xae;) can be reproduced by intimately mixing i) cross-linked chemically modified amylopectin; ii) a high amylose, non-chemically modified starch and; iii) a pre-gelatinized common starch. Producing a release modifying excipient in this way means that no chemical cross linking between (a) amylose and amylopectin or (b) amylose and amylose has occurred&#x2014;properties heretofore considered vital for Contramid&#xae; function. The release modifying excipient blends overcome problems associated with use of Contramid, and provide a flexible platform for formulation of active pharmaceutical ingredients for controlled release applications.

Starch-based release modifying excipients and pharmaceutical compositions derived therefrom

There are provided PVP-PLA block copolymers as defined in Formula (I): I wherein, x is an initiator alcohol having a boiling point greater than 145&#xb0; C., n is, on average, from 20 and 40, and m is, on average, from 10 and 40, wherein the block copolymers have a number average molecular weight (M) of at least 3000 Da. Polymers demonstrating flexibility in formulating multiple low-solubility active pharmaceutical ingredients (APIs) are described. Liquid and dry pharmaceutical formulations comprising an API are described, along with delivery methods, uses, and kits. APIs may include, e.g. flurbiprofen, celecoxib, acetaminophen, or propofol. Also provided is a method of synthesizing the PVP-PLA block copolymers by (i) initiating polymerization of D,L-Lactide from the initiator alcohol x to form poly(lactic acid), adding a xanthate to form a PLA macroinitiator, and polymerizing NVP onto the PLA macroinitiator, by controlled polymerization, to form the block copolymer compound of Formula (I). 

Non-ionic block PVP PLA block copolymers and pharmaceutical compositions derived therefrom

The instant invention relates to a solid product comprising a liquid biologically active agent which is intimately associated to a stabilizing agent; particularly a solid product that can be reconstituted to a clear, stable, stabilized nanodispersion or loaded micelles comprising a polymer as a stabilizing agent and a liquid, preferably water immiscible, biologically active agent. The instant invention is further directed toward a process for the production of the above solid product; particularly to micelles or nanodispersions produced by hydration of a cake or powder of the solid product, produced via an effective treatment of a stabilized solution comprising for example a polymer as a stabilizing agent, such as an amphiphilic block copolymer or a small molecular weight surfactant, loaded with a liquid biologically active agent, such as propofol, an optional additive, and a suitable solvent.

Solid formulations of liquid biologically active agents

The invention relates to a once a day formulation of trazodone or a trazodone derivative. The formulation contains trazodone or a trazodone derivative and a controlled release excipient so that, once administered orally, the trazodone or the trazodone derivative is maintained at a therapeutic plasma concentration from at least 1 hour to at least 24 hours after initial administration. After administration, the initial therapeutic action takes effect within the first hour and lasts at least about 24 hours. This therapeutic effect remains relatively and substantially stable for the remaining period of 24 hours. The formulations can be used for treating depression and/or sleeping disorders.

Trazodone composition for once a day administration

The invention relates to a sustained release formulation for delivering one or more pharmaceutically active agents. The formulation comprises cross-linked high amylose starch and at least one pharmaceutically active agent, and optionally can be subdivided into smaller dosage forms where the smaller dosage forms have substantially the same sustained release properties as the formulation from which they were derived. The formulations can provide sustained release for up to at least 24 hours, and because of their divisability permits a recipient of the active agent or the person administering the active agent to titrate the dosage of the agent.

Sustained drug release composition

Disclosed is a misuse preventative, controlled release composition in the form of a multilayered oral dosage form. A first layer contains a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed therein. A second layer comprises a pharmaceutically active agent that can be the same or different from the pharmaceutically active agent in the microparticles. The composition further comprises a superabsorbent material disposed within the first layer, the second layer, or both the first layer and the second layer. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material swells to encapsulate the microparticles, which remain substantially intact thereby retarding the release of the pharmaceutically active agent from the composition.

Misuse preventative, controlled release formulation

Disclosed is a misuse preventative, controlled release composition in the form of a multilayered oral dosage form. A first layer contains a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed therein. A second layer comprises a superabsorbent material. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material creates a hard gel that traps the microparticles. The hard gel and microparticles provide controlled release of the pharmaceutically active agent.

Disclosed is a misuse preventative, controlled release formulation comprising a core comprising a superabsorbent material (for example, polycarbophil), a controlled release coat surrounding the core, and a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed within the core, the coat, or both the core and the coat. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material present in the coreswells to encapsulate the microparticles, which remain substantially intact thereby retarding the release of the pharmaceutically active agent from the formulation. Also disclosed is a method of using the misuse preventative, controlled release formulation to deliver a pharmaceutically active agent to a mammal, for example, a human, in need thereof.

Disclosed is a misuse preventative, controlled release formulation comprising a core comprising a first layer and a second layer. The core comprises a superabsorbent material (for example, polycarbophil), and a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed within the core. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material present in the core swells to create a hard gel that traps the microparticles. The hard gel and microparticles provide controlled release of the pharmaceutically active agent. Also disclosed is a method of using the misuse preventative, controlled release formulation to deliver a pharmaceutically active agent to a mammal, for example, a human, in need thereof.

The invention relates to a bilayer composition for the delivery of acetaminophen and tramadol over at least a twelve hour period following initial administration. A single administration of the bilayer composition can provide analgesia starting in less than half an hour to about one hour after initial administration with a duration of at least twelve hours after initial administration.

Bilayer composition for the sustained release of acetaminophen and tramadol

Sustained drug release compositions

Disclosed is a misuse preventative, controlled release formulation comprising a core comprising a superabsorbent material (for example, polycarbophil), a controlled release coat surrounding the core, and a plurality of controlled release microparticles having a pharmaceutically active agent (for example, an opioid analgesic) disposed within the core, the coat, or both the core and the coat. When crushed, either intentionally or accidentally, and exposed to an aqueous medium, the superabsorbent material present in the core swells to encapsulate the microparticles, which remain substantially intact thereby retarding the release of the pharmaceutically active agent from the formulation. Also disclosed is a method of using the misuse preventative, controlled release formulation to deliver a pharmaceutically active agent to a mammal, for example, a human, in need thereof.

Growing community of inventors

Saint-Laurent, Canada

Damon Smith