US 7,465,462 B1 · Multiparticulate controlled release selective serotonin reuptake inhibitor formulations

A multiparticulate controlled release selective serotonin reuptake inhibitor (SSRI) composition for oral administration comprising two quantities of particles, each of the particles comprising

(i) an inert non-pareil core,
(ii) an SSRI layer comprising fluvoxamine or a pharmaceutically-acceptable salt thereof disposed over the inert core, and
(iii) a coating of a rate-controlling polymeric acrylate, methacrylate lacquer, or a mixture thereof disposed over the fluvoxamine,
wherein the composition allows the controlled release of the fluvoxamine over a period of not less than about 12 hours following oral administration, wherein the rate-controlling polymeric acrylate or methacrylate lacquer coating of the first quantity of particles is present in a first amount, and the rate-controlling polymeric acrylate or methacrylate lacquer coating of the second quantity of particles is present in a second amount that is different from the first amount, and wherein the fluvoxamine release rate from the composition exhibits the following in vitro dissolution pattern when measured using a USP type II dissolution apparatus (paddle) according to US Pharmacopeia XXII in 0.05 M phosphate buffer at pH 6.8:
(a) no more than about 15% of the total fluvoxamine is released after 0.5 of an hour of measurement in the apparatus;
(b) no more than about 25% of the total fluvoxamine is released after 1 hour of measurement in the apparatus;
(c) between about 20% and 75% of the total fluvoxamine is released after 2 hours of measurement in the apparatus;
(d) not less than about 75% of the total fluvoxamine is released after 4 hours of measurement in the apparatus;
and
(e) not less than about 85% of the total fluvoxamine is released after 6 hours of measurement in the apparatus.

7 more elements

A multiparticulate controlled release selective serotonin reuptake inhibitor (SSRI) composition for oral administration comprising two quantities of particles, each of the particles comprising

(i) an inert non-pareil core,
(ii) an SSRI layer comprising fluvoxamine or a pharmaceutically-acceptable salt thereof disposed over the inert core, and
(iii) a coating of a rate-controlling polymeric acrylate, methacrylate lacquer, or a mixture thereof disposed over the fluvoxamine,
wherein the composition allows the controlled release of the fluvoxamine over a period of not less than about 12 hours following oral administration, wherein the rate-controlling polymeric acrylate or methacrylate lacquer coating of the first quantity of particles is present in a first amount, and the rate-controlling polymeric acrylate or methacrylate lacquer coating of the second quantity of particles is present in a second amount that is different from the first amount, and wherein the fluvoxamine release rate from the composition exhibits the following in vitro dissolution pattern when measured using a USP type II dissolution apparatus (paddle) according to US Pharmacopeia XXII in 0.05 M phosphate buffer at pH 6.8:
(a) no more than about 20% of the total fluvoxamine is released after 4 hours of measurement in the apparatus;
(b) no more than about 45% of the total fluvoxamine is released after 6 hours of measurement in the apparatus;
(c) between about 45% and 80% of the total fluvoxamine is released after 8 hours of measurement in the apparatus;
(d) not less than about 70% of the total fluvoxamine is released after 10 hours of measurement in the apparatus;
and
(c) not less than about 80% of the total fluvoxamine is released after 12 hours of measurement in the apparatus.

7 more elements

A multiparticulate controlled release selective serotonin reuptake inhibitor (SSRI) composition for oral administration comprising two quantities of particles, each of the particles comprising

(i) an inert non-pareil core,
(ii) an SSRI layer comprising fluvoxamine or a pharmaceutically-acceptable salt thereof disposed over the inert core, and
(iii) a coating of a rate-controlling polymeric acrylate, methacrylate lacquer, or a mixture thereof disposed over the fluvoxamine,
wherein the composition allows the controlled release of the fluvoxamine over a period of not less than about 12 hours following oral administration, wherein the rate-controlling polymeric acrylate or methacrylate lacquer coating of the first quantity of particles is present in a first amount, and the rate-controlling polymeric acrylate or methacrylate lacquer coating of the second quantity of particles is present in a second amount that is different from the first amount, and wherein the fluvoxamine release rate from the composition exhibits the following in vitro dissolution pattern when measured using a USP type II dissolution apparatus (paddle) according to US Pharmacopeia XXII in 0.05 M phosphate buffer at pH 6.8:
(a) no more than 20% of the total fluvoxamine is released after 1 hour of measurement in the apparatus;
(b) no more than 60% of the total fluvoxamine is released after 2 hours of measurement in the apparatus;
(c) not less than 20% of the total fluvoxamine is released after 4 hours of measurement in the apparatus;
(d) not less than 35% of the total fluvoxamine is released after 6 hours of measurement in the apparatus;
(e) not less than 50% of the total fluvoxamine is released after 8 hours of measurement in the apparatus;
(f) not less than 70% of the total fluvoxamine is released after 10 hours of measurement in the apparatus;
and
(g) not less than 75% of the total fluvoxamine is released after 12 hours of measurement in the apparatus.

9 more elements

A multiparticulate controlled release selective serotonin reuptake inhibitor (SSRI) composition for oral administration comprising two quantities of particles, each of the particles comprising

(i) an inert non-pareil core,
(ii) an SSRI layer comprising fluvoxamine or a pharmaceutically-acceptable salt thereof disposed over the inert core, and
(iii) a coating of a rate-controlling polymeric acrylate, methacrylate lacquer, or a mixture thereof disposed over the fluvoxamine,
wherein the composition allows the controlled release of the fluvoxamine over a period of not less than about 12 hours following oral administration, wherein the rate-controlling polymeric acrylate or methacrylate lacquer coating of the first quantity of particles is present in a first amount, and the rate-controlling polymeric acrylate or methacrylate lacquer coating of the second quantity of particles is present in a second amount that is different from the first amount, and wherein the fluvoxamine release rate from the composition exhibits the following in vitro dissolution pattern when measured using a USP type II dissolution apparatus (paddle) according to US Pharmacopeia XXII in 0.05 M phosphate buffer at pH 6.8:
(a) no more than about 20% of the total fluvoxamine is released after 1 hour of measurement in the apparatus;
(b) no more than about 45% of the total fluvoxamine is released after 2 hours of measurement in the apparatus;
(c) between about 20% and about 70% of the total fluvoxamine is released after 4 hours of measurement in the apparatus;
(d) between about 35% and about 85% of the total fluvoxamine is released after 6 hours of measurement in the apparatus;
(e) not less than about 50% of the total fluvoxamine is released after 8 hours of measurement in the apparatus;
(f) not less than about 70% of the total fluvoxamine is released after 10 hours of measurement in the apparatus;
and
(g) not less than about 75% of the total fluvoxamine is released after 12 hours of measurement in the apparatus.

9 more elements

A method for the treatment of depression or obsessive compulsive disorder treatable with an SSRI, comprising administering to a patient suffering from one of the conditions a therapeutically effective amount of a multiparticulate controlled release selective serotonin reuptake inhibitor (SSRI) composition for oral administration comprising two quantities of particles, each of the particles comprise

(i) an inert non-pareil core,
(ii) an SSRI layer comprising fluvoxamine or a pharmaceutically-acceptable salt thereof disposed over the inert core, and
(iii) a coating of a rate-controlling polymeric acrylate, methacrylate lacquer, or a mixture thereof disposed over the fluvoxamine,
wherein the composition allows the controlled release of the fluvoxamine over a period of not less than about 12 hours following oral administration, and wherein the rate-controlling polymeric acrylate or methacrylate lacquer coating of the first quantity of particles is present in a first amount, and the rate-controlling polymeric acrylate or methacrylate lacquer coating of the second quantity of particles is present in a second amount that is different from the first amount, and wherein the fluvoxamine release rate from the composition exhibits the following in vitro dissolution pattern when measured using a USP type II dissolution apparatus (paddle) according to US Pharmacopeia XXII in 0.05 M phosphate buffer at pH 6.8:
(a) no more than about 15% of the total fluvoxamine is released after 0.5 of an hour of measurement in the apparatus;
(b) no more than about 25% of the total fluvoxamine is released after 1 hour of measurement in the apparatus;
(c) between about 20% and 75% of the total fluvoxamine is released after 2 hours of measurement in the apparatus;
(d) not less than about 75% of the total fluvoxamine is released after 4 hours of measurement in the apparatus;
and
(c) not less than about 85% of the total fluvoxamine is released after 6 hours of measurement in the apparatus.

7 more elements

A method for the treatment of depression or obsessive compulsive disorder treatable with an SSRI, comprising administering to a patient suffering from one of the conditions a therapeutically effective amount of a multiparticulate controlled release selective serotonin reuptake inhibitor (SSRI) composition for oral administration comprising two quantities of particles, each of the particles comprise

(i) an inert non-pareil core,
(ii) an SSRI layer comprising fluvoxamine or a pharmaceutically-acceptable salt thereof disposed over the inert core, and
(iii) a coating of a rate-controlling polymeric acrylate, methacrylate lacquer, or a mixture thereof disposed over the fluvoxamine,
wherein the composition allows the controlled release of the fluvoxamine over a period of not less than about 12 hours following oral administration, and wherein the rate-controlling polymeric acrylate or methacrylate lacquer coating of the first quantity of particles is present in a first amount, and the rate-controlling polymeric acrylate or methacrylate lacquer coating of the second quantity of particles is present in a second amount that is different from the first amount, and wherein the fluvoxamine release rate from the composition exhibits the following in vitro dissolution pattern when measured using a USP type II dissolution apparatus (paddle) according to US Pharmacopeia XXII in 0.05 M phosphate buffer at pH 6.8:
(a) no more than about 20% of the total fluvoxamine is released after 4 hours of measurement in the apparatus;
(b) no more than about 45% of the total fluvoxamine is released after 6 hours of measurement in the apparatus;
(c) between about 45% and 80% of the total fluvoxamine is released after 8 hours of measurement in the apparatus;
(d) not less than about 70% of the total fluvoxamine is released after 10 hours of measurement in the apparatus;
and
(e) not less than about 80% of the total fluvoxamine is released after 12 hours of measurement in the apparatus.

7 more elements

A method for the treatment of depression or obsessive compulsive disorder treatable with an SSRI, comprising administering to a patient suffering from one of the conditions a therapeutically effective amount of a multiparticulate controlled release selective serotonin reuptake inhibitor (SSRI) composition for oral administration comprising two quantities of particles, each of the particles comprise

(i) an inert non-pareil core,
(ii) an SSRI layer comprising fluvoxamine or a pharmaceutically-acceptable salt thereof disposed over the inert core, and
(iii) a coating of a rate-controlling polymeric acrylate, methacrylate lacquer, or a mixture thereof disposed over the fluvoxamine,
wherein the composition allows the controlled release of the fluvoxamine over a period of not less than about 12 hours following oral administration, and wherein the rate-controlling polymeric acrylate or methacrylate lacquer coating of the first quantity of particles is present in a first amount, and the rate-controlling polymeric acrylate or methacrylate lacquer coating of the second quantity of particles is present in a second amount that is different from the first amount, and wherein the fluvoxamine release rate from the composition exhibits the following in vitro dissolution pattern when measured using a USP type II dissolution apparatus (paddle) according to US Pharmacopeia XXII in 0.05 M phosphate buffer at pH 6.8:
(a) no more than 20% of the total fluvoxamine is released after 1 hour of measurement in the apparatus;
(b) no more than 60% of the total fluvoxamine is released after 2 hours of measurement in the apparatus;
(c) not less than 20% of the total fluvoxamine is released after 4 hours of measurement in the apparatus;
(d) not less than 35% of the total fluvoxamine is released after 6 hours of measurement in the apparatus;
(e) not less than 50% of the total fluvoxamine is released after 8 hours of measurement in the apparatus;
(f) not less than 70% of the total fluvoxamine is released after 10 hours of measurement in the apparatus;
and
(g) not less than 75% of the total fluvoxamine is released after 12 hours of measurement in the apparatus.

9 more elements

A method for the treatment of depression or obsessive compulsive disorder treatable with an SSRI, comprising administering to a patient suffering from one of the conditions a therapeutically effective amount of a multiparticulate controlled release selective serotonin reuptake inhibitor (SSRI) composition for oral administration comprising two quantities of particles, each of the particles comprise

(i) an inert non-pareil core,
(ii) an SSRI layer comprising fluvoxamine or a pharmaceutically-acceptable salt thereof disposed over the inert core, and
(iii) a coating of a rate-controlling polymeric acrylate, methacrylate lacquer, or a mixture thereof disposed over the fluvoxamine,
wherein the composition allows the controlled release of the fluvoxamine over a period of not less than about 12 hours following oral administration, and wherein the rate-controlling polymeric acrylate or methacrylate lacquer coating of the first quantity of particles is present in a first amount, and the rate-controlling polymeric acrylate or methacrylate lacquer coating of the second quantity of particles is present in a second amount that is different from the first amount, and wherein the fluvoxamine release rate from the composition exhibits the following in vitro dissolution pattern when measured using a USP type II dissolution apparatus (paddle) according to US Pharmacopeia XXII in 0.05 M phosphate buffer at pH 6.8:
(a) no more than about 20% of the total fluvoxamine is released after 1 hour of measurement in the apparatus;
(b) no more than about 45% of the total fluvoxamine is released after 2 hours of measurement in the apparatus;
(c) between about 20% and about 70% of the total fluvoxamine is released after 4 hours of measurement in the apparatus;
(d) between about 35% and about 85% of the total fluvoxamine is released after 6 hours of measurement in the apparatus;
(e) not less than about 50% of the total fluvoxamine is released after 8 hours of measurement in the apparatus;
(f) not less than about 70% of the total fluvoxamine is released after 10 hours of measurement in the apparatus;
and
(g) not less than about 75% of the total fluvoxamine is released after 12 hours of measurement in the apparatus.

9 more elements

Multiparticulate controlled release selective serotonin reuptake inhibitor formulations

Life of this patent

Multiparticulate controlled release selective serotonin reuptake inhibitor formulations

Life of this patent

Abstract

Claims45