US2007276015A1PendingUtilityA1
Crystal modification of torasemide
Est. expiryOct 2, 2018(expired)· nominal 20-yr term from priority
Inventors:Darko FilicMiljenko DumicAleksandar DanilovskiBozena KlepicInes FistricMarina OresicJasna Horvat Mikulcic
A61P 7/10A61P 9/12A61P 9/00A61P 35/00A61P 7/02A61P 9/10A61P 27/06A61P 25/08A61P 11/00A61P 11/06C07D 213/71A61K 31/44C07D 213/74C07D 213/53
53
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Claims
Abstract
The present invention relates to the characterization of a new crystal modification III of torasemide, to a process for the preparation thereof by the use of controlled acidifying of alkaline solutions of torasemide with inorganic or organic acids with or without addition of a crystal seed, to its use as a raw material for the preparation of the crystal modification I of torasemide and of pharmaceutically acceptable salts of torasemide as well as to pharmaceutical forms containing this new crystal modification III of torasemide.
Claims
exact text as granted — not AI-modified1 . New crystal modification III of torasemide, characterized in that the characteristic X-ray powder pattern of its sample is represented by the following spacings between lattice planes:
New crystal
modification III
of torasemide
d(Å)
15.3898
12.5973
11.4565
9.7973
9.5493
8.6802
8.2371
7.6351
7.3356
6.9759
6.5351
6.3240
6.1985
5.9521
5.6237
5.5623
5.4040
5.1119
4.8738
4.7865
4.6986
4.5985
4.4602
4.3405
4.2552
4.1829
4.0768
3.9377
3.8659
3.8429
3.7801
3.7248
3.6239
3.5556
3.4825
3.4130
3.3055
3.2298
3.1786
3.1278
3.0699
3.0078
2.9549
2.9056
2.8541
2.7686
2.6988
2.6610
2.6293
2.5549
2.5236
2.4485
2.4161
2.3671
2.3133
2.2788
2.2312
2.1852
2.1468
2.0957
2.0617
2.0273
1.9896
1.9688
1.9274
1.8853
1.7931
1.7449
1.7169
1.6512
1.6122
1.5601
1.5320
1.5057
1.4521
1.3773
2 . New crystal modification III of torasemide according to claim 1 , characterized in that in accordance with X-ray diffraction on its sample monocrystal it is represented by the following basis crystallographic data:
New crystal
modification of
Parameter
torasemide
Crystal composition
monoclinic
space group
P 2 1 /c
a (Å)
11.430
b (Å)
19.090
c (Å)
16.695
β (°)
93.903
V (Å 3 )
3634.7
Z
4 × 2
3 . New crystal modification III of torasemide according to claim 1 , characterized in that it is chemically pure.
4 . New crystal modification III of torasemide according to claim 1 , characterized in that it does not contain water.
5 . New crystal modification III of torasemide according to claim 1 , characterized in that it does not contain a solvent.
6 . Process for the preparation of a new crystal modification III of torasemide according to claim 1 , characterized in that an alkaline torasemide solution is subjected to controlled acidifying with inorganic or organic acids with or without addition of a seed crystal at a temperature between 0° C. to 35° C. within 15 minutes to 25 hours.
7 . Process for the preparation of a new crystal modification III of torasemide according to claim 6 , characterized in that as the alkaline torasemide solution an alkaline extract of the original reaction mixture for the synthesis of torasemide is used.
8 . Process for the preparation of a new crystal modification III of torasemide according to claim 6 , characterized in that as the alkaline torasemide solution an alkaline solution of any crystal modification I, II or III of torasemide or an alkaline solution of any mutual mixture of crystal modifications I, II or III of torasemide is used.
9 . Process according to claim 6 , characterized in that for the preparation of the alkaline torasemide solutions water solutions of lithium, sodium and potassium hydroxide and water solutions of sodium and potassium carbonate are used.
10 . Process according to claim 6 , characterized in that for acidifying inorganic acids such as hydrochloric, sulfuric, phosphoric or nitric acid or organic acids such as formic, acetic, propionic, oxalic, tartaric, methanesulfonic or p-toluensulfonic acid are used.
11 . Process according to claim 6 , characterized in that as the crystal seed crystal powder of one of the isocrystallinic substances is used, most preferably crystal powder of a crystal modification III of torasemide.
12 . A new crystal modification III of torasemide according to claim 1 , characterized in that it is used as a raw material for the preparation of crystal modification I of torasemide.
13 . A new crystal modification III of torasemide according to claim 1 , characterized in that it is used as a raw material for the preparation of pharmaceutically acceptable salts of torasemide.
14 . A new crystal modification III of torasemide according to claim 1 , characterized in that it is used as a form of torasemide as a diuretic, as an agent for preventing heart or heart tissue damages caused by metabolic or ionic abnormalities associated with ischemia, in the treatment of thrombosis, angina pectoris, asthma, hypertension, nephroedema, pulmonary edema, primary and secondary aldosteronism, Bartter's syndrome, tumours, glaucoma, for decreasing intraocular pressure, acute or chronic bronchitis, in the treatment of cerebral edema caused by trauma, ischemia, concussion of the brain, metastases or epileptic attacks and in the treatment of nasal infections caused by allergens.
15 . A pharmaceutical form, characterized in that it contains as the active ingredient the new crystal modification III of torasemide according to claim 1 combined for this purpose with pharmaceutically acceptable one or more carriers, additives or diluents.
16 . A pharmaceutical form according to claim 15 , characterized in that it is in tablet form.Join the waitlist — get patent alerts
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