Soluble salts of ibuprofen and naproxen with N-(2-hydroxyethyl) pyrrolidine and pharmaceutic compositions containing said salts
AssigneeAltergon S.A.
InventorsElisabetta Donati, Irina Rapaport, Paolo Lualdi
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Abstract
The salts, in the crystalline form, of ibuprofen and naproxen with N-(2-hydroxyethyl) pyrrolidine are prepared by dissolving ibuprofen and naproxen respectively in a suitable organic solvent, by adding N-(2-hydroxyethyl) pyrrolidine, by letting the compounds react, by removing the solvent and by crystallizing the obtained salt from a solution in an apolar and aprotic solvent. Said salts have a high solubility in water and are used for preparing pharmaceutic compositions for oral and other administrations.
Claims8
Soluble salt, in the crystalline form, of a non-steroid anti-inflammatory drug (NSAID) selected from the group consisting of ibuprofen (2-(4-isobutylphenyl)proprionic acid) and naproxen (6-methoxy-.alpha.-methyl-2-naphthalenacetic acid) with N-(2-hydroxyethyl)pyrrolidine.
A process for preparing soluble salts, in the crystalline form, of non-steroid anti-inflammatory drugs (NSAID) selected from the group consisting of ibuprofen(2-(4-isobutylphenylpropionic acid) and naproxen (6-methoxy-.alpha.-methyl-2-naphthalenacetic acid) with N-(2-hydroxyethyl)pyrrolidine wherein:
- a. Naproxen or Ibuprofen are dissolved in a suitable organic solvent and N-(2-hydroxyethyl)pyrrolidine is added to the solution:
- b. the mixture is let react at a temperature ranging from 20.degree. to 30.degree. C.;
- c. the raw product is separated by cooling at a temperature ranging from -10.degree. to -40.degree. C., followed by solvent filtration or evaporation;
- d. the obtained raw product is dissolved again in an aprotic, apolar and anhydrous solvent and crystallized at a temperature ranging from -10.degree. to -40.degree. C.
Pharmaceutic compositions, useful in the anti-inflammatory therapy, containing therapeutically active amounts of a soluble in the crystalline form, salt consisting of a non-steroid anti-inflammatory drug (NSAID) selected from the group consisting of ibuprofen and naproxen with N-(2-hydroxyethyl)pyrrolidine together with pharmaceutic excipients suitable for oral, parenteral and topic administration.
Dependencies are inferred from the claim text.