Risperidone or Paliperidone Implant Formulation
AssigneeLaboratorios Farmaceuticos Rovi, S.A.
InventorsIbon GUTIERRO ADURIZ, Guillermo FRANCO RODRIGUEZ
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Abstract
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.
Claims52
1) A method of administering an injectable depot composition to a subject in need thereof, the method comprising administering to said subject an injectable composition consisting of
- about 13% wt of drug which is risperidone and/or paliperidone or any pharmaceutically acceptable salt thereof in any combination;
- and
- a polymeric solution consisting of DMSO and biocompatible poly(lactide-co-glycolide) (PLGA) copolymer having a monomer ratio of lactic acid to glycolic acid of about 50:50 and an inherent viscosity in the range of 0.25-0.30 dl/g measured by gel permeation chromatography in tetrahydrofuran at 30° C. using a flow rate of 1 ml/min;
- wherein
- the mass ratio of polymeric solution to drug is about 6.5:1 to about 7:1;
- and
- the mass ratio of DMSO to drug is about 4:1 to about 5:1.
14) A method of administering an injectable depot composition to a subject in need thereof, the method comprising administering to said subject an injectable composition consisting of about 13% wt of drug which is risperidone and/or paliperidone or any pharmaceutically acceptable salt thereof in any combination;
- DMSO;
- and
- biocompatible poly(lactide-co-glycolide) (PLGA) copolymer having a monomer ratio of lactic acid to glycolic acid of about 50:50 and an inherent viscosity in the range of 0.25-0.29 dl/g measured by gel permeation chromatography in tetrahydrofuran at 30° C. using a flow rate of 1 ml/min;
- wherein
- the mass ratio of drug to (polymer+drug) is about 33%, expressed as the percentage of the drug weight with respect to total weight of the drug plus polymer;
- and
- the mass ratio of DMSO to drug is about 4.66:1.
27) A method of administering an injectable depot composition to a subject in need thereof, the method comprising administering to said subject an injectable composition consisting of about 13% wt of drug which is risperidone and/or paliperidone or any pharmaceutically acceptable salt thereof in any combination;
- DMSO;
- and
- 25-27% wt of biocompatible poly(lactide-co-glycolide) (PLGA) copolymer having a monomer ratio of lactic acid to glycolic acid of about 50:50 and an inherent viscosity in the range of 0.25-0.30 dl/g measured by gel permeation chromatography in tetrahydrofuran at 30° C. using a flow rate of 1 ml/min;
- wherein the mass ratio of DMSO to drug is about 4:1 to about 5:1.
40) A method of administering an injectable depot composition to a subject in need thereof, the method comprising administering to said subject an injectable composition consisting of
- about 13% wt of drug which is risperidone and/or paliperidone or any pharmaceutically acceptable salt thereof in any combination;
- DMSO;
- and
- 25-27% wt of biocompatible poly(lactide-co-glycolide) (PLGA) copolymer having a monomer ratio of lactic acid to glycolic acid of about 50:50 and a molecular weight in the range of 28-43 kDa;
- wherein
- the mass ratio of DMSO to drug is about 4:1 to about 5:1.
Dependencies are inferred from the claim text.