Osmotic delivery device comprising an insulinotropic peptide and uses thereof
First Claim
Patent Images
1. A suspension formulation comprising:
- a particle formulation comprising;
an insulinotropic peptide, an antioxidant, and a buffer, wherein the insulinotropic peptide is at least one of exenatide, a derivative of exenatide, and an analogue of exenatide; and
a non-aqueous, single-phase suspension vehicle that comprises about 20 wt % to about 60 wt % solvent and about 80 wt % to about 40 wt % pyrrolidone polymer, the suspension vehicle having a viscosity from 5,000 poise to 50,000 poise at 33°
C.;
wherein;
the solvent is at least one of lauryl lactate, lauryl alcohol, and benzyl benzoate;
30 to 90% by weight of the particle formulation is the insulinotropic peptide;
the particle formulation has a wt % ratio of insulinotropic peptide to antioxidant of 2.5/1 to 10/1; and
the particle formulation is dispersed in the suspension vehicle.
5 Assignments
0 Petitions
Accused Products
Abstract
A suspension formulation of an insulinotropic peptide (e.g., glucagon-like peptide-1 (GLP-1) or exenatide) is described. The suspension formulation comprises (i) a non-aqueous, single-phase vehicle, comprising one or more polymer and one or more one solvent, wherein the vehicle exhibits viscous fluid characteristics, and (ii) a particle formulation comprising the insulinotropic peptide, wherein the peptide is dispersed in the vehicle. The particle formulation further includes a stabilizing component comprising one or more stabilizers, for example, carbohydrates, antioxidants, amino acids, and buffers. Devices for delivering the suspension formulations and methods of use are also described.
-
Citations
30 Claims
-
1. A suspension formulation comprising:
-
a particle formulation comprising; an insulinotropic peptide, an antioxidant, and a buffer, wherein the insulinotropic peptide is at least one of exenatide, a derivative of exenatide, and an analogue of exenatide; and a non-aqueous, single-phase suspension vehicle that comprises about 20 wt % to about 60 wt % solvent and about 80 wt % to about 40 wt % pyrrolidone polymer, the suspension vehicle having a viscosity from 5,000 poise to 50,000 poise at 33°
C.;wherein; the solvent is at least one of lauryl lactate, lauryl alcohol, and benzyl benzoate; 30 to 90% by weight of the particle formulation is the insulinotropic peptide; the particle formulation has a wt % ratio of insulinotropic peptide to antioxidant of 2.5/1 to 10/1; and the particle formulation is dispersed in the suspension vehicle. - View Dependent Claims (2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16)
-
-
17. A delivery device comprising a suspension formulation, the suspension formulation comprising:
a particle formulation comprising; an insulinotropic peptide, an antioxidant, and a buffer, wherein the insulinotropic peptide is at least one of exenatide, a derivative of exenatide, and an analogue of exenatide; and a non-aqueous, single-phase suspension vehicle that consists essentially of about 20 wt % to about 60 wt % solvent and about 80 wt % to about 40 wt % pyrrolidone polymer, the suspension vehicle having a viscosity from 5,000 poise to 50,000 poise at 33°
C.;wherein; the solvent is at least one of lauryl lactate, lauryl alcohol, and benzyl benzoate; 30 to 90% by weight of the particle formulation is the insulinotropic peptide; the particle formulation has a wt % ratio of insulinotropic peptide to antioxidant of 2.5/1 to 10/1; and the particle formulation is dispersed in the suspension vehicle. - View Dependent Claims (18, 19, 20, 21, 22, 23, 24, 25, 26)
-
27. A method of treating type II diabetes in a subject in need of such treatment, the method comprising:
delivering a suspension formulation from a delivery device at a substantially uniform rate for a period of about one month to about one year, the suspension formulation comprising; a particle formulation comprising; an insulinotropic peptide, an antioxidant, and a buffer, wherein the insulinotropic peptide is at least one of exenatide, a derivative of exenatide, and an analogue of exenatide; and a non-aqueous, single-phase suspension vehicle that consists essentially of about 20 wt % to about 60 wt % solvent and about 80 wt % to about 40 wt % pyrrolidone polymer, the suspension vehicle having a viscosity from 5,000 poise to 50,000 poise at 33°
C.;wherein; the solvent is at least one of lauryl lactate, lauryl alcohol, and benzyl benzoate; 30 to 90% by weight of the particle formulation is the insulinotropic peptide; the particle formulation has a wt % ratio of insulinotropic peptide to antioxidant of 2.5/1 to 10/1; and the particle formulation is dispersed in the suspension vehicle. - View Dependent Claims (28)
-
29. A method for the reduction of at least one of body weight in a subject, glucose concentrations in blood of the subject, and HbA1C levels in the subject, the method comprising:
delivering a suspension formulation from a delivery device at a substantially uniform rate for a period of about one month to about one year, the suspension formulation comprising; a particle formulation comprising; an insulinotropic peptide, an antioxidant, and a buffer, wherein the insulinotropic peptide is at least one of exenatide, a derivative of exenatide, and an analogue of exenatide; and a non-aqueous, single-phase suspension vehicle that consists essentially of about 20 wt % to about 60 wt % solvent and about 80 wt % to about 40 wt % pyrrolidone polymer, the suspension vehicle having a viscosity from 5,000 poise to 50,000 poise at 33°
C.;wherein; the solvent is at least one of lauryl lactate, lauryl alcohol, and benzyl benzoate; 30 to 90% by weight of the particle formulation is the insulinotropic peptide; the particle formulation has a wt % ratio of insulinotropic peptide to antioxidant of 2.5/1 to 10/1; and the particle formulation is dispersed in the suspension vehicle. - View Dependent Claims (30)
Specification