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US 2021/0061771 A1Published application
Method for solubilizing 5-amino-2,3-dihydro-1,4-phthalazinedione
AssigneeMetrioPharm AG
InventorsIngo Saar, Wolfgang Brysch
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Abstract
The present invention relates to a method for solubilizing 5-amino-2,3-dihydro-1,4-phthalazinedione or salts thereof, to the solubilisate produced by this method and respective uses in pharmaceutical dosage forms. A phosphatidylcholine-based solubilization method is disclosed.
Claims15
A method for solubilizing 5-amino-2,3-dihydro-1,4-phthalazinedione, comprising the following steps:
- a) Providing 5-amino-2,3-dihydro-1,4-phthalazinedione in the overall range of 0.1% to 25% per weight at room temperature and a pressure of 0.2 bar to 1 bar;
- b) Adding in any sequence the solubilization agents of at least one phosphatidylcholine in the overall range of 20% to 80% per weight,
- at least one medium-chained triglyceride in the overall range of 10% to 70% per weight,
- at least one lysophosphatidylcholine in the overall range of 1% to 15% per weight,
- at least one C2 to C4 alcohol in the overall range of 1% to 20% per weight, and at least one of glyceryl stearate and/or a saturated or unsaturated C14 to C20 fatty acid in the overall range of 0.5% to 10% per weight, respectively,
- wherein the relative weight percentages of all ingredients add up to 100% and all solubilization agents are independently from one another a food additive and/or a pharmaceutically acceptable excipient;
- c) Cautiously heating the resulting mixture by continuously increasing the temperature with a continuous temperature increment of 0.5° C./min-3° C./min over a period of 20-60 minutes;
- d) Stopping the temperature increase in a temperature range of 30° C. to 125° C. as soon as a clear solution is reached;
- and
- e) Letting the resulting solubilisate cool down to room temperature.
7 more elements
Dependencies are inferred from the claim text.