Flamel Technologies

Rhodia Chimie

Other

Flamel Ireland Limited

Cécile Bonnet-Gonnet

You-Ping Chan

Olivier Breyne

Olivier Soula

Alain Constancis

Frédéric Checot

Mathias Destarac

Arnaud Cadix

Etienne Fleury

Remi Meyrueix

Yvette Pescher

David Chognot

The present invention relates to novel pharmaceutical formulations based on aqueous colloidal suspensions for the prolonged release of one or more active principles, and to the applications, especially therapeutic applications, of these formulations. Formulations may include an aqueous colloidal suspension of low viscosity based on micrometric particles of a water-soluble, biodegradable, amphiphilic polymer carrying hydrophobic groups and ionizable hydrophilic groups that are at least partially ionized, said particles being capable of associating spontaneously and non-covalently with an active principle, at pH=7.0, under isotonic conditions. This suspension contains multivalent ions of opposite polarity to that of the hydrophilic groups, the ratio r, defined by the formula r=n&#xd7;([IM]/[GI]), where n is the valency of said multivalent ions, [IM] is the molar concentration of multivalent ions, [GI] is the molar concentration of ionizable groups GI, being between 0.3 and 10.

Pharmaceutical formulations for the prolonged release of active principle(s), and their applications, especially therapeutic applications

The present invention relates to novel biodegradable materials based on modified polyamino acids that are useful in particular in the vectorization of active principle(s) (APs). The invention is also directed to novel pharmaceutical, cosmetic, health-food or plant-protection compositions based on these polyamino acids. The aim of the invention is to provide a novel polymeric starting material which can be used for AP vectorization and which satisfy all the requirements: biocompatibility, biodegradability, ability to easily associate with or dissolve numerous active principles and to release these active principles in vivo. This goal is achieved by the present invention, which relates to novel polyglutamates modified by cationic groups, which, if they can be deprotonated, exhibit a pKa equal to or greater than 7, and by hydrophobic groups comprising from 8 to 30 carbon atoms. These polyglutamates modified by cationic groups are easily and economically converted into particles for the vectorization of active principles, these particles being themselves capable of forming stable aqueous colloidal suspensions. These modified polyglutamates exhibit the advantage of being less viscous than other analogous polymers while retaining an ability to associate proteins, such as insulin. Some are soluble in water at acidic pH and become insoluble at physiological pH (7.4) and should thus, during subcutaneous injection, precipitate on the site of injection.

Polyglutamic acids functionalized by cationic groups and hydrophobic groups and applications thereof, in particular therapeutic applications thereof

The present invention relates to novel particles comprising polyelectrolyte polymers which are transporters of active principle (AP), in particular protein and peptide active principle, and to novel modified-release pharmaceutical formulations comprising said AP microparticles. These novel particles loaded with AP release the AP over a prolonged period of time of several days, or even several weeks. The invention relates, in a first aspect, to particles comprising: The invention also relates to the process for the preparation of these particles, to a pharmaceutical formulation comprising such particles and to a process for the preparation of medicaments.

Modified-release particles of polyelectrolytes and pharmaceutical formulations thereof

The present invention relates to pharmaceutical formulations for the release of an active principle (AP) over a sustained period of time. The invention relates to a liquid formulation comprising at least one active principle (AP) and an aqueous suspension based on colloidal particles of a polymer (PO), wherein said formulation satisfies the following four conditions: (a) the PO is a polyamino acid comprising glutamic residues, wherein some glutamic residues each carry a pendant cationic group (CG), said CG being identical or different from one another, and other glutamic residues each carry a pendent hydrophobic group (GH), said GH being identical or different from one another, (b) the pHf value of the pH of said formulation is between 3.0 and 6.5; (c) at the pHf value, the PO forms a colloidal solution which associates spontaneously and noncovalently with the AP; (d) 1 ml of said formulation precipitates during mixing with a volume of 1 ml of a test buffer solution Tp.

Self-precipitating pharmaceutical formulations for the modified release of an active principle

The invention relates to the use of a block copolymer having at least one block that comprises phosphate and/or phosphonate functions, as an additive for film-forming compositions, such as paint, latex or mastic which is optionally siliconised in order to ensure or promote the adhesion of the aforementioned compositions on a metallic surface or to protect said metallic surface against corrosion. The invention also relates to film-forming compositions comprising the abovementioned block copolymers.

Use of block copolymers bearing phosphate and/or phosphonate functions as adhesion promoters or as protecting agents against the corrosion of a metallic surface

The invention relates to a particular polymer which is derived from a copolymer polysaccharide formed by a main chain comprising similar or different anhydrohexose units and branches including at least one neutral or anionic anhydropentose and/or anhydrohexose unit. Moreover, the invention relates to the use of said polymer in the treatment of aqueous media, in particular the treatment of aqueous effluents containing heavy metals, the treatment of waste water, drinking water and for sludge conditioning. Said derivative polymer comprises one or more units bearing an oxime function at least at position C2.

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Lyons, France

Cécile Bonnet-Gonnet