Liquid pharmaceutical formulations of topiramate
OwnerNilesh Parikh, William Hiteinventors
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Abstract
Certain embodiments of the present disclosure provide liquid pharmaceutical formulations, suitable for oral administration, that contain a therapeutically effective amount of topiramate that is from 50 mg/ml to 100 mg/ml and amounts of polyethylene glycol (“PEG”) 400 and glycerol sufficient to result in a greater than a prior art taught calculated maximum amount of the topiramate being in the solution phase of the formulation, at room temperature.
Claims20
A liquid pharmaceutical formulation, suitable for oral administration, that consists of a therapeutically effective amount of topiramate and:
- (a) 10% w/w polyethylene glycol (“PEG”) 400 and a quantity of glycerol, from 72.5% w/w to 86% w/w, that brings the formulation to 100% w/w, wherein from 25 mg/ml to 70 mg/ml of the topiramate is, at room temperature, in the solution phase of the formulation;
- (b) 15% w/w PEG 400 and a quantity of glycerol, from 67.5% w/w to 81% w/w, that brings the formulation to 100% w/w, wherein from 32.5 mg/ml to 70 mg/ml of the topiramate is, at room temperature, in the solution phase of the formulation;
- (c) 20% w/w PEG 400 and a quantity of glycerol, from 62.5% w/w to 76% w/w, that brings the formulation to 100% w/w, wherein from 40 mg/ml to 70 mg/ml of the topiramate is, at room temperature, in the solution phase of the formulation;
- or
- (d) 25% w/w PEG 400 and a quantity of glycerol, from 57.5% w/w to 71% w/w, that brings the formulation to 100% w/w, wherein from 47.5 mg/ml to 70 mg/ml of the topiramate is, at room temperature, in the solution phase of the formulation.
A liquid pharmaceutical formulation, suitable for oral administration, that consists of about 4% w/w to about 8% w/w topiramate and:
- (a) 10% w/w PEG 400 and a quantity of glycerol, from 81% w/w to 86% w/w, that brings the formulation to 100% w/w, wherein from 25 mg/ml to 70 mg/ml of the topiramate is, at room temperature, in the solution phase of the formulation;
- (b) 15% w/w PEG 400 and a quantity of glycerol, from 76% w/w to 81% w/w, that brings the formulation to 100% w/w, wherein from 32.5 mg/ml to 70 mg/ml of the topiramate is, at room temperature, in the solution phase of the formulation;
- (c) 20% w/w PEG 400 and a quantity of glycerol, from 71% w/w to 76% w/w, that brings the formulation to 100% w/w, wherein from 40 mg/ml to 70 mg/ml of the topiramate is, at room temperature, in the solution phase of the formulation;
- or
- (d) 25% w/w PEG 400 and a quantity of glycerol, from 65% w/w to 69% w/w, that brings the formulation to 100% w/w, wherein from 47.5 mg/ml to 70 mg/ml of the topiramate is, at room temperature, in the solution phase of the formulation.
A liquid pharmaceutical formulation, suitable for oral administration, that consists of a therapeutically effective amount of topiramate, from 0.01% w/w to 2.0% w/w of a sweetener, from 0.01% w/w to 2.0% w/w of a flavorant, or a combination the sweetener and the flavorant, and:
- (a) 10% w/w polyethylene glycol (“PEG”) 400 and a quantity of glycerol, from 72.5% w/w to 86% w/w, that brings the formulation to 100% w/w, wherein from 25 mg/ml to 70 mg/ml of the topiramate is, at room temperature, in the solution phase of the formulation;
- (b) 15% w/w PEG 400 and a quantity of glycerol, from 67.5% w/w to 81% w/w, that brings the formulation to 100% w/w, wherein from 32.5 mg/ml to 70 mg/ml of the topiramate is, at room temperature, in the solution phase of the formulation;
- (c) 20% w/w PEG 400 and a quantity of glycerol, from 62.5% w/w to 76% w/w, that brings the formulation to 100% w/w, wherein from 40 mg/ml to 70 mg/ml of the topiramate is, at room temperature, in the solution phase of the formulation;
- or
- (d) 25% w/w PEG 400 and a quantity of glycerol, from 57.5% w/w to 71% w/w, that brings the formulation to 100% w/w, wherein from 47.5 mg/ml to 70 mg/ml of the topiramate is, at room temperature, in the solution phase of the formulation.
A liquid pharmaceutical formulation, suitable for oral administration, that consists of about 4% w/w to about 8% w/w topiramate, and:
- (a) 10% w/w PEG 400 and a quantity of glycerol, from 81% w/w to 86% w/w, that brings the formulation to 100% w/w, wherein from 25 mg/ml to 70 mg/ml of the topiramate is, at room temperature, in the solution phase of the formulation;
- (b) 15% w/w PEG 400 and a quantity of glycerol, from 76% w/w to 81% w/w, that brings the formulation to 100% w/w, wherein from 32.5 mg/ml to 70 mg/ml of the topiramate is, at room temperature, in the solution phase of the formulation;
- (c) 20% w/w PEG 400 and a quantity of glycerol, from 71% w/w to 76% w/w, that brings the formulation to 100% w/w, wherein from 40 mg/ml to 70 mg/ml of the topiramate is, at room temperature, in the solution phase of the formulation;
- or
- (d) 25% w/w PEG 400 and a quantity of glycerol, from 65% w/w to 69% w/w, that brings the formulation to 100% w/w, wherein from 47.5 mg/ml to 70 mg/ml of the topiramate is, at room temperature, in the solution phase of the formulation,
- wherein each of (a), (b), (c), and (d) further consist of:
- (i) from 0.01% w/w to 2.0% w/w of a sweetener, (ii) from 0.01% w/w to 2.0% w/w of a flavorant, or (iii) a combination of the sweetener and the flavorant.
Dependencies are inferred from the claim text.