Antipsychotic Injectable Depot Composition
First Claim
1. An injectable depot composition consisting ofdrug, which is risperidone, paliperidone or a combination thereof, present as particles having a particle size distribution of not more than 10% of the total volume of drug particles is less than 10 microns in size, not more than 10% of the total volume of drug particles is greater than 225 microns in size, and the d0.5 of the size distribution is in the range of about 60-130 microns;
- andpolymeric solution consisting ofDMSO; and
biocompatible poly(lactide-co-glycolide)(PLGA) copolymer comprising lactic acid and glycolic acid monomers, wherein the monomers are present at a monomer ratio of lactic to glycolic acid of about 50;
50, the copolymer has an inherent viscosity in the range of 0.25-0.48 dl/g as measured in chloroform at 25°
C. and at a concentration of 0.1% wt/v with an Ubbelohde size 0c glass capillary viscometer;
whereinthe polymeric solution has a viscosity in the range of about 0.7 Pa·
s to about 3.0 Pa·
s; and
whereinthe drug content is about 13% wt with respect to the total composition weight;
the DMSO to drug mass ratio is about 4;
1 to 5;
1; and
the polymeric solution to drug mass ratio is about 6.5;
1 to 7;
1.
1 Assignment
0 Petitions
Accused Products
Abstract
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.
-
Citations
26 Claims
-
1. An injectable depot composition consisting of
drug, which is risperidone, paliperidone or a combination thereof, present as particles having a particle size distribution of not more than 10% of the total volume of drug particles is less than 10 microns in size, not more than 10% of the total volume of drug particles is greater than 225 microns in size, and the d0.5 of the size distribution is in the range of about 60-130 microns; - and
polymeric solution consisting of DMSO; and biocompatible poly(lactide-co-glycolide)(PLGA) copolymer comprising lactic acid and glycolic acid monomers, wherein the monomers are present at a monomer ratio of lactic to glycolic acid of about 50;
50, the copolymer has an inherent viscosity in the range of 0.25-0.48 dl/g as measured in chloroform at 25°
C. and at a concentration of 0.1% wt/v with an Ubbelohde size 0c glass capillary viscometer;
whereinthe polymeric solution has a viscosity in the range of about 0.7 Pa·
s to about 3.0 Pa·
s; andwherein the drug content is about 13% wt with respect to the total composition weight; the DMSO to drug mass ratio is about 4;
1 to 5;
1; andthe polymeric solution to drug mass ratio is about 6.5;
1 to 7;
1. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20)
- and
-
21. An injectable depot composition consisting of
drug, which is risperidone, paliperidone or a combination thereof, present as particles having a particle size distribution of not more than 10% of the total volume of drug particles is less than 10 microns in size, not more than 10% of the total volume of drug particles is greater than 225 microns in size, and the d0.5 of the size distribution is in the range of about 60-130 microns; - and
polymeric solution consisting of DMSO; and biocompatible poly(lactide-co-glycolide)(PLGA) copolymer comprising lactic acid and glycolic acid monomers, wherein the monomers are present at a monomer ratio of lactic to glycolic acid of about 50;
50, the copolymer has an inherent viscosity in the range of 0.25-0.48 dl/g as measured in chloroform at 25°
C. and at a concentration of 0.1% wt/v with an Ubbelohde size 0c glass capillary viscometer;
whereinthe polymeric solution has a viscosity in the range of about 0.7 Pa.s to about 3.0 Pa·
s;the drug content is about 13% wt with respect to the total composition weight; the DMSO to drug mass ratio is about 4.66;
1; andthe polymeric solution to drug mass ratio is about 6.66;
1. - View Dependent Claims (22, 23, 24)
- and
-
25. An injectable depot composition consisting of
drug, which is risperidone, paliperidone or a combination thereof, present as particles having a particle size distribution of not more than 10% of the total volume of drug particles is less than 10 microns in size, not more than 10% of the total volume of drug particles is greater than 225 microns in size, and the d0.5 of the size distribution is in the range of about 60-130 microns; - and
polymeric solution consisting of DMSO; and biocompatible poly(lactide-co-glycolide) (PLGA) copolymer comprising lactic acid and glycolic acid monomers, wherein the monomers are present at a monomer ratio of lactic to glycolic acid of about 50;
50, the copolymer has an inherent viscosity in the range of 0.25-0.48 dl/g as measured in chloroform at 25°
C. and at a concentration of 0.1% wt/v with an Ubbelohde size 0c glass capillary viscometer;
whereinthe polymeric solution has a viscosity in the range of about 0.7 Pa.s to about 3.0 Pa·
s; andwherein the drug content is about 13% wt with respect to the total composition weight; the DMSO to drug mass ratio is about 4;
1 to 5;
1;the polymeric solution to drug mass ratio is about 6.5;
1 to 7;
1;wherein the injectable composition provides a drug plasma profile defined as follows - View Dependent Claims (26)
- and
Specification