Laboratorios Farmaceuticos Rovi S.a.

Guillermo Franco Rodriguez

Ibon Gutierro Aduriz

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

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

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.

A nuclear magnetic resonance method of analysis for glycosaminoglycans in general, and of heparins and low molecular weight heparins and their derivatives in particular, is provided. The method allows for their identification and for relative quantification of respective characteristic signals byH-NMR and/orH-C HSQC.

Method for the analysis of glycosaminoglycans, and their derivatives and salts by nuclear magnetic resonance

An analytical method employing nuclear magnetic resonance of glycosaminoglycans in general, and of heparins and low molecular weight heparins and their derivatives in particular, is provided. The method is used for identification and the relative quantification of characteristic signals byH-NMR and/orH-C HSQC.

A pharmaceutical composition containing a sulfated glycosaminoglycan drug and a polycationic polymer or copolymer wherein the proportion of ammonium groups in the pharmaceutical composition is between 0.01-2.0 &#x3bc;mol ammonium groups/mg pharmaceutical composition, the proportion of glycosaminoglycan in the pharmaceutical form is between 15% to 50% w/w, and the pharmaceutical composition possesses a moisture content of 10% wt or less. A pharmaceutical dosage form containing the pharmaceutical composition, and their use for the treatment of diseases or disorders therapeutically responsive to the glycosaminoglycan.

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Madrid, Spain

Guillermo Franco Rodriguez