Abstract: The present invention relates to novel microparticles formed of amphiphilic polyamino acids which transport active principle(s), AP(s), in particular protein and peptide active principle(s), and to novel modified-release pharmaceutical formulations comprising said AP microparticles. Microparticles of amphiphilic polyamino acid (PO) may include at least one AP (associated noncovalently) which spontaneously form a colloidal suspension of nanoparticles in water, at pH 7.0, under isotonic conditions. The microparticles may be obtained by atomization of a solution or colloidal suspension of PO comprising at least one AP, may have a size of between 0.5 and 100 microns, and may be dispersible in colloidal suspension.

Abstract: The present invention provides N-phosphonomethylglycine guanidine salts. The N-phosphonomethylglycine guanidine salts have improved herbicidal efficacy over glyphosate alone. The present invention also provides guanidine compounds and salts thereof.

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 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 invention relates to oral medicaments having a modified release of proton pump inhibitors (PPI's) that are, in particular, useful in preventing and treating gastrointestinal disorders. The aim of the invention is to provide a novel oral medicament based on PPI's ideally having all or some of the following characteristics: a) quickly providing relief to the patient by increasing the gastric pH after oral administration of the medicament; b) accelerating the recovery of patients while maintaining this increase in the gastric pH for as long as possible after oral administration of the medicament and, in particular, during the night; c) improving the observance of the treatment and the comfort of the patient by taking the medicament once daily.

Abstract: The invention concerns novel biodegradable polyaminoacid materials, useful in particular for vectoring active principles(s). The invention also concerns novel pharmaceutical, cosmetic dietetic or phytosanitary compositions based on said polyaminoacids. The invention aims at providing a novel polymer raw material, capable of being used for vectoring active principles and enabling optimal fulfillment of all specified requirements: biocompatibility, biodegradability, easy and inexpensive transformation into particles vectoring active principles, said particles being themselves capable of forming colloidal suspensions, of being easily associated with numerous active principles, and of releasing said active principles in vivo.

Abstract: The invention relates to novel biodegradable materials based on modified polyamino acids and suitable, in particular, for vectoring active substance(s) (AS). Said invention also relates to novel pharmaceutical, cosmetic, dietary or plant protective compositions which are based on said polyamino acids. The aim of said invention is to provide a novel polymer raw material usable for vectoring the AS and capable to optimally meet all specification in this area: biocompatibility, biodegradability, ability to become easily associated with many active substances or to solubilise them and to release said active substances in vivo. The aim is attained to 30 carbon atoms. Said polyglutamates modified by histidine derivatives are soluble with pH lower than 5 and are easily and economically convertible into active substance vectorization particles which are able to form stable aqueous colloidal suspensions. On the contrary, said modified polyglutamates are insoluble in water with a physiological pH (7.

Abstract: The present invention aims to propose novel microparticle oral forms for the modified release of active ingredient(s), in particular protein or peptide in nature. It also relates to the uses, in particular therapeutic or cosmetic, of these microparticle oral forms.

Abstract: The invention relates to pharmaceutical compositions of acetylsalicylic acid-based microcapsules to selectively inhibit the COX in the portal vein and/or in the liver to reduce the production of thromboxane. Further, the pharmaceutical composition minimizes COX inhibition in the systemic circulation to optimize the inhibition of platelet aggregation. Certain embodiments also address methods of prevention and/or treatment of these diseases, using these oral compositions such as enhancing the safety of antithrombotic treatments. Other embodiments contemplate oral pharmaceutical compositions that combine acetylsalicylic acid with anti-platelet aggregation drugs, without inducing gastric side effects.

Abstract: The invention relates to oral pharmaceutical forms with modified release of ARB, and to related treatments and delivery methods. The invention concerns a form with modified release of ARB which prolongs the bioabsorption time and enables the pharmaceutical form to be administered only once daily.

Abstract: The present invention relates to a solid form, intended for the administration by oral route of at least one active ingredient and capable of guaranteeing a double release mechanism of said active ingredient, the first being determined by time and the second being determined by the pH, characterized in that said active ingredient is present there in the form of a microparticle system the microparticles of which possess a core formed wholly or partly by said active ingredient and coated with at least one layer determining said release profile of said active ingredient and formed by a material composed at least (i) 25 to 75% by weight relative to the total weight of said coating of at least one polymer A which is insoluble in the gastro-intestinal fluids, (ii) 25 to 75% by weight relative to the total weight of said coating of at least one polymer B possessing a solubilization pH value comprised within the pH range from 5 to 7, and (iii) 0 to 25% by weight relative to the total weight of said coating of at leas

Abstract: The field of the present invention is that of oral pharmaceutical forms of losartan, and also treatments and administration methods relating thereto. The invention relates to the use, in an oral pharmaceutical form comprising losartan, of a coating or matrix including said losartan and allowing controlled release of said losartan, such that this form orally administered to a sample of individuals leads, irrespective of the fed or fasted state of the individuals, to a reduction of the interindividual standard deviation of the Cmax, which ensures lower variability of the efficacy and of the therapeutic safety of the pharmaceutical form relative to an immediate-release pharmaceutical form of losartan administered to this same sample of individuals, at the same dose. Another aim of the invention is to provide an oral pharmaceutical form of losartan that can be administered once a day and that is just as effective as the “one dose intake per day” forms and the “two dose intakes per day” forms.

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 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.

Abstract: 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.

Abstract: The present invention relates to novel pharmaceutical formulations for the release of an active principle (AP) over a sustained period of time of several days, or even several weeks. The invention relates, in a first aspect, to a liquid formulation comprising at least one active principle (AP) and an aqueous suspension based on colloïdal particles of a polymer (PO), wherein said formulation satisfies the following four conditions: (a) the polymer (PO) is a polyamino acid comprising glutamic residues, wherein some glutamic residues each carry a pendant cationic group (CG), said cationic groups being identical or different from one another, and other glutamic residues each carry a pendent hydrophobic group (GH), said hydrophobic groups (GH) being identical or different from one another, (b) the pHf value of the pH of said formulation is between 3.0 and 6.

Abstract: The invention relates to injectable pharmaceutical compositions for the prolonged release of at least one active principle, comprising at least one active principle in an aqueous phase of amphiphilic polymer, said aqueous phase being in the form of a dispersion in a continuous lipid phase. The composition is in the form of a water-in-oil emulsion comprising: a pharmaceutically acceptable, continuous lipid phase, an aqueous disperse phase containing at least one amphiphilic polymer and at least one active principle not covalently bonded to said amphiphilic polymer, and at least one pharmaceutically acceptable surfactant.

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.