Oral pharmaceutical composition of desmopressin
Inventors
Carbajal Navarro, Nuria • Boix Montanes, Antonio • Nieto Abad, Carlos • Parente Duena, Antonio • Mis Vizcaino, Ricard • Garcia Plumed, Cesar
Assignees
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Publication Number
US-8993521-B2
Publication Date
2015-03-31
Expiration Date
Abstract
The present invention relates to a liquid oral pharmaceutical composition of desmopressin, and its use for the treatment of central diabetes insipidus, primary nocturnal enuresis, bleeding in patients with Hemophilia A, with von Willebrand-Jürgens disease and postoperative bleeding.
Core Innovation
The invention relates to an oral pharmaceutical composition comprising desmopressin or a pharmaceutically acceptable salt thereof as a therapeutically effective amount in a stable, liquid and flexible-dose aqueous solution. The composition is maintained at a pH between 3.5 and 5.0 for oral administration and is free of osmotic agents and absorption enhancing agents.
The composition includes one or several pharmaceutically acceptable auxiliary agents selected from preservatives, antibacterial and antifungal agents, and one or several acids for adjusting the pH of the composition. The preservatives, antibacterial and antifungal agents are selected from parabens, salts or mixtures thereof, and the acids are selected from hydrochloric acid, nitric acid, phosphoric acid, sulfuric acid, acetic acid and citric acid, or mixtures thereof.
The stability description includes maintenance of pH and desmopressin assay at 25°C over about 12 months. The composition is also described as a drops presentation for oral administration absorbed through the oral and/or sublingual mucosa.
Claims Coverage
The independent claim defines 3 inventive features centered on a stable, liquid, flexible-dose aqueous oral desmopressin composition with pH between 3.5 and 5.0, using specified auxiliary agents while excluding osmotic agents and absorption enhancing agents.
Stable liquid flexible-dose oral aqueous desmopressin composition at pH 3.5 to 5.0
A stable, liquid and flexible-dose composition in aqueous solution form of pH between 3.5 and 5.0 for oral administration that comprises neither osmotic agents nor absorption enhancing agents.
Auxiliary agents selected from parabens preservatives and acids for pH adjustment
The composition includes one or several pharmaceutically acceptable auxiliary agents selected from preservatives, antibacterial and antifungal agents, and one or several acids for adjusting the pH of the composition, where the preservatives, antibacterial and antifungal agents are selected from parabens, salts or mixtures thereof.
Acid selection for adjusting pH
The acids are selected from hydrochloric acid, nitric acid, phosphoric acid, sulfuric acid, acetic acid and citric acid, or mixtures thereof.
Overall, the claim coverage centers on an aqueous, flexible-dose, stable oral desmopressin formulation with pH 3.5–5.0, using paraben-based preservative, antibacterial and antifungal auxiliary agents and specified acids for pH adjustment, while excluding osmotic agents and absorption enhancing agents.
Stated Advantages
Stable liquid and flexible-dose composition for oral administration with pH between 3.5 and 5.0.
Maintained pH and desmopressin assay over storage at 25°C for about 12 months.
Excludes osmotic agents.
Excludes absorption enhancing agents.
Documented Applications
Treatment of central diabetes insipidus.
Treatment of primary nocturnal enuresis.
Treatment of bleeding in patients with Hemophilia A.
Treatment of von Willebrand-Jürgens disease.
Treatment of postoperative bleeding.
Administration as drops for oral administration absorbed through the oral and/or sublingual mucosa.
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