Laboratorios Farmaceuticos Rovi S.a.

Laboratorios Farmaceutics Rofi S.a.

Laboratories Farmacéuticos Rovi, S.a.

Laboratorios Farmacéticos Rovi, S.a.

Ibon Gutierro Aduriz

Guillermo Franco Rodriguez

Maria Teresa Gomez Ochoa

Guillermo Franco Rodríguez

Philippe Maincent

Elena Cebadera Miranda

Maria Garcia Amo

Ivan Lopez-Belmonte Encina

Javier Martinez Gonzalez

Iván López-Belmonte Encina

María Teresa GÓMEZ Ochoa

Maria GARCÍA Amo

María Teresa Gomez Ochoa

A method of treating an episode of acute exacerbation of schizophrenia by intramuscular administration of a long-acting injectable depot composition containing risperidone is provided. The method provides a substantial reduction in PANSS (both positive and negative scales) and CGI-S scores within about eight days after administration of the composition and for up to at least four weeks. The method is used to treat a subject suffering a first-time episode of or a relapse of severe to moderate symptoms associated with schizophrenia. The method does not require loading doses of risperidone in the depot composition and does not require supplementation with oral risperidone after administration of the depot composition.

Method of treating acute exacerbation of schizophrenia with long-acting injectable depot composition

The present invention is directed to an injectable intramuscular depot composition suitable for forming an in situ solid implant in a body, comprising a drug which is risperidone and/or paliperidone or any pharmaceutically acceptable salt thereof in any combination, a biocompatible copolymer based on lactic and glycolic acid having a monomer ratio of lactic to glycolic acid of about 50:50 and a DMSO solvent, wherein the composition releases the drug with an immediate onset of action and continuously for at least 4 weeks and wherein the composition has a pharmacokinetic profile in vivo that makes it suitable to be administered each 4 weeks or even longer periods.

Risperidone or paliperidone implant formulation

An injectable depot composition suitable for forming an in situ intramuscular implant is provided. The composition includes sterile biodegradable thermoplastic polymer of polylactic acid (PLA), solvent for the PLA, and drug. After administration to a subject, a corresponding implant administers 0.1-2 milligrams of nonsteroidal aromatase inhibitor every day throughout a dosing period of about six months to about one year. The composition is used to treat subjects in need thereof.

Injectable composition

A sterile procedure for the filing of solids into pharmaceutical containers and the sealing thereof under sterile conditions is provided. Exemplary containers include syringes, vials, capsules, ampoules, single-dose devices or cartridges. The containers can be filled with powder, granules, nanoparticles or microparticles. After sealing, the containers are airtight. More specifically, the procedure minimizes adherence of those solids to the interior surfaces of the containers during the filling and sealing steps, thus ensuring airtightness of the seal and precision of the weight of the solid dispensed into the containers.

Procedure for the filling of solids in pharmaceutical containers and the sealing thereof under sterile conditions

The present invention provides a composition suitable for forming an intramuscular implant. It comprises a biodegradable thermoplastic polymer of polylactic acid (PLA), DMSO and an aromatase inhibitor compound. The invention also provides a kit suitable for the in situ formation of the composition and its use as a medicine for treating cancer, especially breast cancer.

Injectable composition with aromatase inhibitor

A system for and method of gravimetric filling of a solid product in sterile conditions in a pharmaceutical container of small dimensions including syringes, vials, capsules, ampoules, single-dose devices, inhalers, bottles, carpules, well(s) of blister pack(s), sachets or bags with solid substances selected from the group formed by powder, lyophilizate, granules, pellets, nanoparticles or microparticles. More particularly, it relates to a process for the gravimetric filling of pharmaceutical containers with one or more sterile solid pharmaceutical substances or sterile excipients dosed and prepared in an aseptic environment.

Process and equipment assembly for aseptic gravimetric filling of solids into a container

The present invention is directed to a composition that can be used to deliver an antipsychotic drug such as risperidone, paliperidone or a combination thereof, as an injectable in-situ forming biodegradable implant for extended release providing therapeutic plasma levels from the first day. The composition is in the form of drug suspension on a biodegradable and biocompatible copolymer or copolymers solution using water miscible solvents that is administered in liquid form. Once the composition contacts the body fluids, the polymer matrix hardens retaining the drug, forming a solid or semisolid implant that releases the drug in a continuous manner. Therapeutic plasma levels of the drug can be achieved from the first day up to at least 14 days or more even up to at least four weeks.

Antipsychotic injectable depot composition

Injectable depot compositions comprising a biocompatible polymer which is a polymer or copolymer based on lactic acid and/or lactic acid plus glycolic acid having a monomer ratio of lactic to glycolic acid in the range from 48:52 to 100:0, a water-miscible solvent having a dipole moment of about 3.7-4.5 D and a dielectric constant of between 30 and 50, and a drug, were found suitable for forming in-situ biodegradable implants which can evoke therapeutic drug plasma levels from the first day and for at least 14 days.

Methods for the preparation of injectable depot compositions

An injectable intramuscular depot composition suitable for forming an in situ solid implant in a body, comprising a drug which is paliperidone and/or its pharmaceutical acceptable salts in any combination thereof, a biocompatible copolymer based on lactic and glycolic acid having a monomer ratio of lactic to glycolic acid of about 50:50 and DMSO as solvent, wherein the composition releases the drug with an immediate onset of action and continuously for at least 8 weeks and wherein the composition has a pharmacokinetic profile in vivo suitable for the formulation to be administered each 8 weeks or even longer periods.

Paliperidone implant formulation

The present invention is directed to an injectable intramuscular depot composition suitable for forming an in situ solid implant in a body, comprising a drug which is risperidone and/or paliperidone or any pharmaceutically acceptable salt thereof in any combination, a biocompatible copolymer based on lactic and glycolic acid having a monomer ratio of lactic to glycolic acid of about 50:50 and DMSO solvent, wherein the composition releases the drug with an immediate onset of action and continuously for at least 4 weeks and wherein the composition has a pharmacokinetic profile in vivo that makes it suitable to be administered each 4 weeks or even longer periods.

Growing community of inventors

Granada, Spain

Ibon Gutierro Aduriz