Abstract: An oral solid dosage form containing one or several active principle(s) having analgesic properties, the composition of said dosage form being such that it prevents the misuse of said dosage form through the liquid extraction of the active principle(s) contained therein, using commonly available solvents. Said oral solid dosage form containing at least one salt of at least one analgesic active principle, and an anti-misuse system comprising at least one quenching agent, said quenching agent being suitable for inducing complexation of said analgesic active principle salt when the analgesic active principle salt is improperly extracted, notably by a drug abuser, in vitro in solution from said oral solid dosage form.

Abstract: The present invention is directed to microcapsules for reliably modified release and adapted to industrial reproduction of an active principle hardly water-soluble, other than anti-hyperglycemia agents. Each of said microcapsules comprises a core of hardly soluble active principle and a coating film applied on the core. Their mean diameter is less than 1000 microns. The coating film contains a film-forming polymer (PI) insoluble in gastrointestinal tract fluids, a water-soluble polymer (P2), a plasticizer (PL), and optionally a lubricating surfactant (TA). Said coating film represents at least 4% p/p of dry matter of their total weight, and its components P1, P2, PL satisfy the following characteristics: dry weight mass fraction of PI relative to the total coating weight ranging between 40 and 90%; dry matter weight fraction of PL/P1+P2 ranging between 15 and 60%; dry matter weight fraction of PL/P1+P2 ranging between 1 and 30%.

Abstract: The invention relates to substituted anionic compounds consisting of a backbone made up of a discrete number u of between 1 and 8 (1?u?8) of identical or different saccharide units, linked via identical or different glycosidic bonds, said saccharide units being chosen from the group consisting of pentoses, hexoses, uronic acids, N-acetylhexosamines in cyclic form or in open reduced form, which are randomly substituted. It also relates to the process for the preparation thereof and to the pharmaceutical compositions comprising same.

Abstract: The field of the invention is that of oral pharmaceutical medicinal products or compositions, more particularly of the type of those comprising one or more active principles. The aim of the invention is to provide an improved oral medicinal product that can be administered in one or more daily doses, with modified release of active principle (in particular an active principle), for improving the prophylactic and therapeutic efficacy of such a medicinal product. This aim is achieved by means of the multimicrocapsular oral pharmaceutical form according to the invention in which the release of the AP is controlled by means of a double mechanism of triggering the release: “time triggering” and “pH triggering”. This medicinal product comprises microcapsules with modified release of active principle, each containing a core comprising the active principle and one or more swelling agents, and at least one coating making possible the modified release of the active principle.

Abstract: The invention relates to a composition in aqueous solution, including insulin and at least one substituted anionic compound chosen from substituted anionic compounds consisting of a backbone formed from a discrete number u of between 1 and 8 (1?u?8) of identical or different saccharide units, linked via identical or different glycoside bonds, said saccharide units being chosen from the group consisting of hexoses, in cyclic form or in open reduced form, said compound comprising partially substituted carboxyl functional groups, the unsubstituted carboxyl functional groups being salifiable. The invention also relates to a pharmaceutical formulation comprising a composition as claimed in any one of the preceding claims.

Abstract: The invention relates to a complex between an insulin and a polysaccharide comprising carboxyl functional groups, said polysaccharide being chosen from polysaccharides functionalized with at least one phenylalanine derivative, noted Phe, said phenylalanine derivative being chosen from the group consisting of phenylalanine and its alkali metal cation salts, phenylalaninol, phenylalaninamide and ethylbenzylamine or from phenylalanine esters, and said insulin being either a human insulin or an insulin analog. The invention also relates to a pharmaceutical composition comprising at least one complex according to the invention, especially in the form of an injectable solution.

Abstract: The invention relates to a dextran functionalized by at least one hydrophobic alpha-amino acid radical, said alpha-amino acid being grafted or bonded to the dextran by a bonding arm and a functional group. A hydrophobic amino acid radical is understood as being the product of coupling between the amine of the amino acid and an acid carried by the bonding arm, said dextran being amphiphilic at neutral pH. In an embodiment, the hydrophobic amino acid is selected from tryptophan derivatives, such as tryptophan, tryptophanol, tryptophanamide, 2-indole ethyl-amine and their alkaline cation salts. The present invention relates also to a pharmaceutical composition comprising one of the dextrans according to the invention.

Abstract: Osteogenic compositions composed of a coprecipitate that contains at least one insoluble calcium salt and at least one complex between an osteogenic protein and a polysaccharide, the coprecipitate being in divided form, are described. Kits are also described, as are a process for preparing the coprecipitate in divided form, containing at least one insoluble calcium salt and at least one complex between an osteogenic protein and a polysaccharide.

Abstract: A polysaccharide comprising carboxyl functional groups, at least one of which is substituted with at least one hydrophobic radical: the hydrophobic radical being a residue of a hydrophobic alcohol having a linear, branched or cyclic alkyl chain containing at least 6 carbon atoms, the hydrophobic radical being bonded to a linker arm R by a function G, the linker arm R being bonded to a carboxyl function of the polysaccharide by a bond F, R being an at least divalent radical of a chain including between 1 and 15 carbons, which is optionally branched and/or unsaturated, optionally including one or more heteroatoms, chosen amongst O, N and/or S, F being an amide function, G being a carbamate function, the unsubstituted carboxyl functions of the polysaccharide being in the form of a cation carboxylate, said cation being chosen amongst alkali metal cation.

Abstract: A composition in aqueous solution, including an insulin and at least one oligosaccharide whose average degree of polymerization is between 3 and 13 and whose polydispersity index PDI is above 1.0, the oligosaccharide having partially substituted carboxyl functional groups, the unsubstituted carboxyl functional groups being salifiable.

Abstract: Osteogenic compositions composed of a coprecipitate that contains at least one insoluble calcium salt and at least one complex between an osteogenic protein and a polysaccharide, the coprecipitate being in divided form, are described. Kits are also described, as are a process for preparing the coprecipitate in divided form, containing at least one insoluble calcium salt and at least one complex between an osteogenic protein and a polysaccharide.

Abstract: The invention relates to a polysaccharide comprising carboxyl functional groups, one at least of which is substituted by a derivative of a hydrophobic alcohol. The invention also relates to a pharmaceutical composition comprising one of the polysaccharides according to the invention and at least one active principle. It also relates to a pharmaceutical composition, wherein the active principle is chosen from the group consisting of proteins, glycoproteins, peptides and nonpeptide therapeutic molecules. The invention also relates to the use of the functionalized polysaccharides according to the invention in the preparation of pharmaceutical compositions as described above.

Abstract: A composition in the form of an injectable aqueous solution, the pH of which is between 6.0 and 8.0, includes at least a basal insulin, the isoelectric point pI of which is between 5.8 and 8.5; and a dextran substituted by radicals carrying carboxylate charges and hydrophobic radicals. Single-dose formulations at a pH of between 7 and 7.8 includes a basal insulin whose isoelectric point is between 5.8 and 8.5 and a prandial insulin.

Abstract: The invention relates to an amphiphilic-BMP polymer complex which is physically and chemically stable and soluble in water, characterized in that: the amphiphilic polymers comprise a hydrophilic polysaccharide skeleton functionalized with hydrophobic substituents and hydrophilic groups the BMP is selected from the group of therapeutically active BMPs (Bone morphogenetic Proteins), the polymer/BMP mass ratio is lower than or equal to 700. The invention also relates to the process for preparing the amphiphilic-BMP polymer complex in an aqueous medium and in the absence of organic solvents likely to denature the protein. The invention also relates to therapeutic compositions of an amphiphilic-BMP polymer complex according to the invention.

Abstract: The invention relates to a complex consisted of a polysaccharide and an HBP, said polysaccharide being consisted from glycoside bonds of (1,6) and/or (1,4) and/or (1,3) and/or (1,2) type and functionalized with at least one salifiable or salified tryptophan derivative. The invention also relates to a pharmaceutical composition comprising a complex according to the invention and to the use of a polysaccharide consisted of glycoside bonds of (1,6) and/or (1,4) and/or (1,3) and/or (1,2) type and functionalized with at least one salifiable or salified tryptophan derivative, for the preparation of a pharmaceutical formulation of stable HBPs.

Abstract: Physically and chemically stable, water-soluble, amphiphilic polymer-PDGF complex, characterized in that the amphiphilic polymers include a hydrophilic polymeric backbone functionalized with hydrophobic substituents and hydrophilic groups.

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: A complex between an insulin and a polysaccharide comprising carboxyl functional groups is described, the polysaccharide being chosen from polysaccharides functionalized with at least one phenylalanine derivative, noted Phe, the phenylalanine derivative being chosen from phenylalanine and its alkali metal cation salts, phenylalaninol, phenylalaninamide and ethylbenzylamine or from phenylalanine esters, and the insulin being either a human insulin or an insulin analog. A pharmaceutical composition including at least one complex, especially in the form of an injectable solution, is also described.

Abstract: Dextran of the following general formula I: is described, wherein R represents a chain containing from 1 to 15 carbon atoms and having at least one acid functional group prior to attachment to AA, the chain optionally being branched and/or unsaturated and containing one or more heteroatoms, such as O, N or/and S, F represents an ester, a carbamate or an ether, AA represents a hydrophobic amino acid radical, L or D, derived from a coupling between an amine of an amino acid and at least one acid functional group of R; the amino acid, prior to attachment to R, being selected from the group consisting of tryptophan, phenylalanine, leucine, isoleucine, alanine and valine, and alcohol, amide or decarboxylated derivatives thereof, and alkaline cation salts thereof, i represents the molar fraction of substituent F—R-[AA]n per glycosidic unit and is from 0.1 to 2, n represents the molar fraction of R groups substituted by AA and is from 0.

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.