Amlodipine formulations
AssigneeSilvergate Pharmaceuticals, Inc.
InventorsScott BRAUER, Gerold L. MOSHER
Life of this patent
Estimating the term…
Abstract
Provided herein are stable amlodipine liquid formulations. Also provided herein are methods of using amlodipine liquid formulations for the treatment of certain diseases including hypertension and Coronary Artery Disease (CAD).
Claims30
A suspension comprising amlodipine benzoate particles having a D50 value between about 5 μm and about 40 μm, the suspension made by the process comprising:
- (i) providing an aqueous mixture of an amlodipine salt that is more soluble in aqueous media than amlodipine benzoate;
- (ii) adding sodium benzoate to the aqueous mixture to form a first mixture;
- and
- (iii) subjecting the first mixture to ultrasonic agitation thereby forming a second mixture comprising amlodipine benzoate.
A suspension comprising amlodipine benzoate particles having a D50 value between about 5 μm and about 40 μm, the suspension made by the process comprising:
- (i) providing an aqueous mixture of an amlodipine salt that is more soluble in aqueous media than amlodipine benzoate;
- (ii) adding sodium benzoate to the aqueous mixture to form a first mixture;
- and
- (iii) subjecting the first mixture to ultrasonic agitation thereby forming a second mixture comprising amlodipine benzoate,
- wherein the suspension comprises:
- (i) amlodipine benzoate in an amount corresponding to about 0.8 mg/ml to about 1.2 mg/ml of amlodipine free base;
- (ii) a citrate buffer in an amount between about 1 mM and about 5 mM;
- (iii) about 0.1 mg/ml to about 5.0 mg/ml sodium benzoate;
- (iv) about 0.1 mg/ml to about 1.0 mg/ml of silicon dioxide;
- (v) about 3 mg/ml to about 10 mg/ml of hydroxypropyl methylcellulose;
- (vi) about 0.1 mg/ml to about 1.0 mg/ml of simethicone;
- (vii) about 0.1 mg/ml to about 2 mg/ml of polysorbate 80;
- and
- (viii) water.
A suspension comprising amlodipine benzoate particles having a D50 value between about 5 μm and about 40 μm, the suspension made by the process comprising:
- (i) providing an aqueous mixture of an amlodipine salt that is more soluble in aqueous media than amlodipine benzoate;
- (ii) adding sodium benzoate to the aqueous mixture to form a first mixture;
- and
- (iii) subjecting the first mixture to ultrasonic agitation thereby forming a second mixture comprising amlodipine benzoate,
- wherein the suspension comprises:
- (i) amlodipine benzoate in an amount corresponding to about 1.0 mg/ml of amlodipine free base;
- (ii) about 3 mM of a citrate buffer;
- (iii) about 0.1 mg/ml to about 5.0 mg/ml sodium benzoate;
- (iv) about 0.5 mg/ml of silicon dioxide;
- (v) about 7.5 mg/ml of hydroxypropyl methylcellulose;
- (vi) about 0.15 mg/ml of simethicone;
- (vii) about 1.0 mg/ml of polysorbate 80;
- and
- (viii) water,
- wherein the suspension is stable at about 5±5° C. for at least 12 months.
Dependencies are inferred from the claim text.