Enalapril compositions
View Patent ↗Provided herein are stable enalapril powder compositions for oral liquid formulation. Also provided herein are methods of using enalapril oral liquid formulations for the treatment of certain diseases including hypertension, heart failure and asymptomatic left ventricular dysfunction.
1. A pharmaceutical powder that is reconstituted into an oral liquid formulation, the powder consisting essentially of:
(a) enalapril or a pharmaceutically acceptable salt thereof,
(b) a stability agent, and
(c) colloidal silicon dioxide,
wherein, when the powder is reconstituted into an oral liquid, the liquid is homogenous and stable for at least 12 weeks at about 25±5° C. and 55±10% relative humidity.
2. The pharmaceutical powder of claim 1 , wherein the enalapril or pharmaceutically acceptable salt thereof is enalapril maleate.
3. The pharmaceutical powder of claim 1 , wherein the stability agent is lactose, sucrose or mannitol.
4. The pharmaceutical powder of claim 1 , wherein the stability agent is lactose.
5. The pharmaceutical powder of claim 1 , wherein the stability agent is sucrose.
6. The pharmaceutical powder of claim 1 , wherein the stability agent is mannitol.
7. The pharmaceutical powder of claim 1 , wherein the enalapril or a pharmaceutically acceptable salt thereof is about 14% (w/w) of the powder.
8. The pharmaceutical powder of claim 1 , wherein the stability agent is about 85% (w/w) of the powder.
9. The pharmaceutical powder of claim 1 , wherein the colloidal silicon dioxide is about 1% (w/w) of the powder.
10. The pharmaceutical powder of claim 1 , wherein the powder consists essentially of
(a) about 14% (w/w) enalapril or a pharmaceutically acceptable salt thereof,
(b) about 85% (w/w) of the stability agent, and
(c) about 1% (w/w) colloidal silicon dioxide.
11. The pharmaceutical powder of claim 1 , wherein the powder is reconstituted in water for the oral liquid.
12. The pharmaceutical powder of claim 1 , wherein the powder is reconstituted in syrup for the oral liquid.
13. The pharmaceutical powder of claim 1 , wherein the powder is stable for at least six months at ambient, accelerated or refrigerated conditions.
14. A pharmaceutical powder that is reconstituted into an oral liquid formulation, the powder consisting essentially of:
(a) enalapril or a pharmaceutically acceptable salt thereof,
(b) mannitol, and
(c) colloidal silicon dioxide,
wherein, when the powder is reconstituted into an oral liquid, the liquid is homogenous and stable for at least 12 weeks at about 25±5° C. and 55±10% relative humidity.
15. The pharmaceutical powder of claim 14 , wherein the powder consists essentially of
(a) about 14% (w/w) enalapril or a pharmaceutically acceptable salt thereof,
(b) about 85% (w/w) mannitol, and
(c) about 1% (w/w) colloidal silicon dioxide.
16. The pharmaceutical powder of claim 1 , wherein the liquid comprises
(a) about 1 mg/ml enalapril or a pharmaceutically acceptable salt thereof,
(b) about 6 mg/ml mannitol, and
(c) about 0.07 mg/ml colloidal silicon dioxide.
17. The pharmaceutical powder of claim 1 , wherein the powder consists essentially of about 150 mg enalapril, about 890 mg mannitol and 10 mg colloidal silicon dioxide.