Enalapril compositions
Inventors
Rajewski, Lian G. • Rajewski, Roger A. • Haslam, John L. • Heppert, Kathleen • Beckloff, Michael C. • SEGRAVE FRANK, null • Seagrave, Frank • Mauro, Robert • Colabuono, Peter
Assignees
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Publication Number
US-8568747-B1
Publication Date
2013-10-29
Expiration Date
Abstract
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.
Core Innovation
The invention relates to a pharmaceutical powder that is reconstituted into an oral liquid formulation. The powder consists of about 14% (w/w) enalapril or a pharmaceutically acceptable salt thereof, about 85% (w/w) mannitol, and about 1% (w/w) colloidal silicon dioxide.
When reconstituted, the oral liquid is described as homogenous and stable. The powder formulation is defined by stability performance of the reconstituted oral liquid, including stability for at least 12 weeks at about 25±5°C and 55±10% relative humidity.
The document describes the enalapril powder composition as enabling stable, homogeneous oral liquids upon reconstitution. The formulation includes a specific glidant component in the form of colloidal silicon dioxide to support the described stability and homogeneity of the reconstituted oral liquid.
Claims Coverage
The provided independent claim defines 1 core inventive feature centered on the reconstitutable powder composition and the stability and homogeneity requirement for the resulting oral liquid. Dependent claims refine salt form identity, reconstitution vehicle, additional stability duration, and specific component amounts.
Enalapril-mannitol-colloidal silicon dioxide powder yielding a homogeneous, stable oral liquid
A pharmaceutical powder reconstituted into an oral liquid formulation, consisting of about 14% (w/w) enalapril or a pharmaceutically acceptable salt thereof, about 85% (w/w) mannitol, and about 1% (w/w) colloidal silicon dioxide, wherein the liquid is homogenous and stable for at least 12 weeks at about 25±5°C and 55±10% relative humidity.
Enalapril as enalapril maleate or a pharmaceutically acceptable salt
The powder is described as containing enalapril as enalapril maleate or a pharmaceutically acceptable salt thereof.
Reconstitution into an oral liquid using syrup
The pharmaceutical powder is reconstituted in syrup to form an oral liquid.
Reconstituted oral liquid stable for at least six months under multiple storage conditions
The powder is described as stable for at least six months under ambient, accelerated, or refrigerated conditions.
Specific component amounts for the reconstitutable powder
The powder includes 150 mg enalapril, 890 mg mannitol, and 10 mg colloidal silicon dioxide.
Across the independent and dependent claim refinements, the central claim coverage centers on a specific enalapril/mannitol powder with about 1% colloidal silicon dioxide that reconstitutes into a homogenous, stable oral liquid meeting defined stability conditions, with dependent claims specifying enalapril salt form, reconstitution vehicle, additional stability duration categories, and specific component quantities.
Stated Advantages
Reconstituted oral liquid is described as homogenous and stable for at least 12 weeks at about 25±5°C and 55±10% relative humidity.
Reconstituted oral liquid is described as stable for at least six months under ambient, accelerated, or refrigerated conditions.
Documented Applications
Use of the reconstituted oral liquid formulation in the context of treating conditions associated with enalapril, including hypertension, heart failure, and asymptomatic left ventricular dysfunction, as described in the document.
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