Abstract: The present invention relates to novel nanoparticles formed by at least one active ingredient and by at least two polyelectrolytes of opposite polarity, in particular characterized in that at least one of the two polyelectrolytes bears hydrophobic side groups and at least one of the two polyelectrolytes bears side groups of the polyalkylene glycol type, said nanoparticles having an average diameter ranging from 10 to 100 nm and comprising a quantity of groups of the polyalkylene glycol type such that the mass ratio wPAG of polyalkylene glycol relative to the total polymer is greater than or equal to 0.05.

Abstract: The present invention relates to a novel method for the preparation of nanoparticles with a diameter smaller than or equal to 500 nm, comprising bringing a solution (1) comprising nanoparticles of a first polyelectrolyte in the charged state, bearing hydrophobic side groups, together with (2) at least one second polyelectrolyte of opposite polarity to that of the first polyelectrolyte, characterized in that the ratio Z of the number of cationic groups relative to the number of anionic groups in the mixture of the two polyelectrolytes is comprised between 0.1 and 0.75 or between 1.3 and 2; and the total mass concentration C of polyelectrolytes is strictly less than 2 mg/g of the mixture.

Abstract: The invention concerns an oral galenic form for prolonged release of anti-hyperglycaemic (metformin) active principles. Said medicine enables to obtain an efficient therapeutic protection over 24 hours by overcoming the problems of bypass of the absorption window and the massive localised release of active principles. Therefor, said medicine comprises several thousand anti-hyperglycaemic (metformin) microcapsules each consisting of a core comprising at least an anti-hyperglycaemic agent and of a coating film applied on the core and enabling the prolonged release in vivo of the anti-hyperglycaemic agent. Said microcapsules have a grain size distribution ranging between 50 and 100 microns. The reproducibility of the transit kinetics and hence of bioavailability are very high. There results for the patient a lesser risk of hyperglycaemic or hypoglycaemic. The invention also concerns the preparation of said medicine and the use of a plurality of said microcapsules for making an anti-hyperglycaemic medicine.

Abstract: The invention relates to a microparticulate system for the delayed and controlled release of active principles (AP) whose absorption window in vivo is essentially limited to the upper parts of the gastrointestinal tract, this system being intended for oral administration. The object of the invention is to provide a system ensuring that the AP is released with certainty by means of a dual mechanism of “time-dependent” and “pH-dependent” release. To achieve this object, the invention proposes a multimicrocapsular oral galenical form which is designed so as to guarantee therapeutic efficacy, and in which the release of the AP is governed by a dual release triggering mechanism that is “time-triggering” and “pH-triggering”. This system comprises of microcapsules (200 to 600 ?m) comprising a core of AP coated with a film (maximum 40% by weight) comprising a hydrophilic polymer A (Eudragit® L) and a hydrophobic compound B (vegetable wax, melting point=40-90° C.), B/A being between 0.2 and 1.5.

Abstract: The present invention relates to novel pharmaceutical formulations based on stable, fluid aqueous colloidal suspensions for the prolonged release of active principle(s), particularly protein active principle(s), and to the applications, especially therapeutic applications, of these formulations. The object of the invention is to propose a fluid pharmaceutical formulation for the prolonged release of active principle(s) that makes it possible, after parenteral injection, to increase significantly the in vivo release time of a therapeutic protein while at the same time reducing the plasma concentration peak of the active protein, said formulation furthermore being stable on storage and also being biocompatible, biodegradable, non-toxic and non-immunogenic and having a good local tolerance.

Abstract: The invention relates to injectable long-acting insulin formulations for the treatment of types I and II diabetes in humans and animals. The essential object of the invention is to provide an injectable long-acting insulin formulation in the form of a colloidal suspension which is stable, which has a good local tolerance and toxicity compatible with the chronic treatment of diabetics, and which maintains a substantial hypoglycemic effect extending over at least 24 hours after a single administration, e.g. by the subcutaneous route. To achieve this object, the invention relates to a stable aqueous colloidal formulation of insulin-laden nanoparticles of at least one poly(Leu-block-Glu) in which the pH is between 5.8 and 7.0, the osmolarity O (in mOsmol) . . . : 270?O?800, and the viscosity v (in mPa·s) is low, namely v?40. The nanoparticles of poly(Leu-block-Glu) have a mean hydrodynamic diameter Dh such that: 15?Dh?40.

Abstract: The field of the present invention is that of oral pharmaceutical forms of at least one active principle AP whose solubility varies greatly as a function of the gastric pH, and also treatments and administration methods relating thereto. The invention relates to the use, in an oral pharmaceutical form comprising AP, of a coating or of a matrix including the said AP and allowing the controlled release of the said AP, in order for this form administered orally to a sample of individuals to lead, irrespective of the fed or fasted state of the individuals, to a reduction in the inter- and/or intra-individual standard deviation of the Cmax, which makes it possible to ensure lower variability of the efficacy and of the therapeutic safety of the pharmaceutical form, compared with an immediate-release AP pharmaceutical form administered to this same sample of individuals, at the same dose.

Abstract: The present invention relates to new amphiphilic polymers comprising hydrophobic groups and methionine groups. It also relates to compositions with a controlled release profile comprising such polymers, non-covalently combined with an active ingredient, in particular an active ingredient such as a peptide or a protein comprising in their sequence at least one amino acid which is sensitive to oxidation.

Abstract: The invention concerns liquid pharmaceutical formulations, for oral delivery, with modified release of amoxicillin and consisting of suspensions of coated particles of amoxicillin (microcapsules). The microcapsules constituting the dispersed phase of the suspension are designed, according to the invention, to enable modified release of amoxicillin, in accordance with a profile which remains unaltered during the shelf life of the liquid suspension. Therefor, the invention consists in selecting a coating composition specific to the microcapsules consisting of at least four components enabling preservation of said microcapsules in water without altering their properties of modified release of amoxicillin, said liquid phase being furthermore saturated with amoxicillin.

Abstract: The present invention relates to a novel family of polymers of acrylic and/or methacrylic type, comprising alpha-tocopherol grafts, capable of forming nanoparticles in an aqueous medium at a neutral pH. It also relates to the use of such nanoparticles, non-covalently combined with an active ingredient, in particular an active ingredient of low or average aqueous solubility, for conveying, solubilizing and/or increasing the aqueous solubilization of said active ingredient.

Abstract: The invention relates to liquid pharmaceutical formulations for oral administration with the modified release of active principle(s), excluding amoxicillin, said formulations consisting of suspensions of coated particles of active principles (microcapsules). According to the invention, the microcapsules constituting the disperse phase of the suspension are designed to allow the modified release of the active principle(s) according to a profile that does not change during the storage of the liquid suspension. To do this the inventors propose the selection of a specific coating composition for the microcapsules which consists of at least four components that allow these microcapsules to be stored in water without modifying their properties of modified release of the active principle, this liquid phase furthermore being saturated with active principle(s).

Abstract: The object of the present invention is to minimize the risks of dose dumping associated with the concomitant consumption of alcohol and certain modified-release pharmaceutical or dietetic forms. The invention relates to an oral form comprising microparticles of the reservoir type for the modified release of at least one active principle (AP), characterized in that it is resistant to immediate dumping of the dose of AP in the presence of alcohol. In particular, the oral form according to the invention is characterized in that the time taken to release 50% of the AP in an alcoholic solution is not reduced more than 3-fold relative to the time taken to release 50% of the AP in an alcohol-free aqueous medium. The form comprises an agent 13, which is a pharmaceutically acceptable compound whose hydration or solvation rate or capacity is greater in an alcohol-free aqueous medium than in alcoholic solution.

Abstract: The present invention relates to a solid oral pharmaceutical form, with modified release of at least one active ingredient, containing at least microparticles containing said active ingredient and at least one viscosifying agent in a form isolated from said microparticles of active ingredient, characterized in that said microparticles possess an average diameter ranging from 100 to 600 ?m, and are formed by a core containing at least said active ingredient and coated with at least one coating layer, said core being formed by a support particle covered by a layer comprising at least said active ingredient, said coating layer being formed by a material composed of at least 25 to 70% by weight relative to the total weight of said coating, of at least one polymer A insoluble in water, 30 to 75% by weight relative to the total weight of said coating, of at least one polymer B insoluble in water below pH 5 and soluble in water above pH 7, and 0 to 25% by weight relative to the total weight of said coating, of at

Abstract: The invention relates to novel materials based on biodegradable polyamino acids, particularly useful for the vectorisation of active principals (PA). The invention further relates to novel, pharmaceutical, cosmetic, dietary or phytosanitary compositions. The invention provides novel polymeric raw material, for use in the vectorisation of PA and with an optimal match for all the requirements of the type: biocompatibility, biodegradability, stability, ability to easily associate with numerous active principals or to solubilise the same and to liberate said active principals in vivo. Said aim is achieved with polyamino acids comprising aspartic and/or glutamate units, some of which carry at least one graft, characterised in that at least one of said grafts is bonded to an aspartic or glutamate unit by means of an amino acids spacer based on Leu, and/or Ileu, and/or Val, and/or Phe and a hydrophobic group with C6-C30 is connected by an ester bond to the spacer.

Abstract: The invention relates to liquid pharmaceutical formulations for oral administration with the modified release of amoxicillin, said formulations consisting of suspensions of coated particles of amoxicillin (microcapsules). According to the invention, the microcapsules constituting the disperse phase of the suspension are designed to allow the modified release of the amoxicillin according to a profile that does not change during the storage of the liquid suspension. To do this the inventors propose the selection of a specific coating composition for the microcapsules which consists of at least four components that allow these microcapsules to be stored in water without modifying their properties of modified release of the amoxicillin, this liquid phase furthermore being saturated with amoxicillin.

Abstract: The invention concerns liquid pharmaceutical formulations, for oral delivery, with modified release of active principle(s) excluding amoxicillin and consisting of suspensions of coated particles of active principles (microcapsules). The microcapsules constituting the dispersed phase of the suspension are designed, according to the invention, to enable modified release of the active principle(s), in accordance with a profile which remains unaltered during the shelf life of the liquid suspension. Therefor, the invention consists in selecting a coating composition specific to the microcapsules consisting of at least four components enabling preservation of said microcapsules in water without altering their properties of modified release of the active principle, said liquid phase being furthermore saturated with active principle(s).

Abstract: The invention concerns a galenic system with prolonged/controlled release of the medicinal and/or nutritional active principle, for oral administration. The aim is to provide a system enabling to obtain with one single tolerable and acceptable dose of active principle, efficient therapeutic protection over 24 hours (increasing the bioabsorption time without affecting bioavailability).

Abstract: The invention relates to a pharmaceutical composition comprising a plurality of controlled-release coated microparticles each comprising a floating core, on the surface of which is deposited a layer containing at least one active principle, said layer being covered with a controlled-release coating, characterized by the fact that said floating core is composed of cellulose acetate phthalate and has an apparent density of less than or equal to 0.6 g/mL and said coated microparticles have a density of less than or equal to 0.7 g/mL.

Abstract: The invention relates to solid microparticulate oral dosage forms having a composition that prevents the misuse of the active pharmaceutical ingredient (API) contained therein. The aim of the invention is to prevent the improper use of solid oral drugs for any use other than the therapeutic use(s) officially approved by the appropriate public health authorities. Another aim of the invention is to provide novel analgesic drugs which can be used to: prevent the misuse of, and addiction to certain analgesics and/or to control plasma concentration variability and/or to facilitate oral; administration; and/or to combine analgesics with one another and/or with one or more active ingredients in the same oral form.

Abstract: The present invention relates to a composition comprising at least one active ingredient with low aqueous solubility, said active ingredient being present therein in a form noncovalently associated with nanoparticles formed by at least one POM polymer of formula (I), and in which said active ingredient is present in a proportion of at least 5 ?mol/g of POM. It is also directed towards the use of such nanoparticles, noncovalently associated with an active ingredient, with a view to increasing the aqueous solubilization of said active ingredient.