Patent EA-005003-B1 (EA)
Title: Novel polymorph v of torasemide
Inventor: FILIC DARKO
IPC: A61P11/00
Filed: 2000-09-25
Abstract: 1. Novel polymorph V of torasemide characterized by the following data: DSC: exothermic maximum at about 157.59 degree C (onset at about 150.74 degree C) with the heating rate of 10 degree C/min; X-ray powder pattern (2 theta): 5.610; 6.130; 7.480; 7.970; 9.310; 9.615; 10.835; 11.020; 12.340; 13.075; 13.460; 13.920; 14.200; 15.090; 16.080; 16.710; 17.445; 17.720; 18.460; 18.850; 19.825; 20.340; 20.990; 21.980; 22.075; 22.630; 22.935; 23.410; 23.845; 24.880; 25.560; 26.035; 27.285; 27.540; 28.170; 28.645; 29.350; 29.975; 30.575; 31.265; 32.300; 34.050; 35.650; 36.375; 37.100, and 38.145; IR-characteristic absorption bands at 2671 to 3327 and at 1468 to 1705cm<-1>. 2. Novel polymorph V of torasemide according to claim 1, characterized in that it is chemically pure. 3. Novel polymorph V of torasemide according to claim 1, characterized in that it contains no water. 4. Novel polymorph V of torasemide according to claim 1, characterized in that it contains no solvent. 5. Process for the preparation of the novel polymorph V of torasemide according to claim 1, characterized in that an alkaline solution of torasemide is subjected to a rapid acidification during 15-120 sec. with inorganic or organic acids at temperatures between 0 degree C and 35 degree C. 6. Process for the preparation of the novel polymorph V of torasemide according to claim 5, characterized in that as torasemide modifications there are used crystalline modifications I, II and III of torasemide, an amorphous torasemide modification or the novel polymorph V of torasemide or any mutual mixture of crystalline modifications I, II and III of torasemide, an amorphous torasemide modification or the novel polymorph V of torasemide. 7. Process for the preparation of the novel polymorph V of torasemide according to claim 5, characterized in that for the preparation of alkaline solutions of torasemide aqueous solutions of lithium hydroxide, sodium hydroxide and potassium hydroxide as well as aqueous solutions of sodium carbonate and potassium carbonate are used. 8. Process for the preparation of the novel polymorph V of torasemide according to claim 5, characterized in that for the acidification inorganic acids such as hydrochloric, sulfuric, phosphoric or nitric acid, and organic acids such as formic, acetic, propionic, oxalic, tartaric, methanesulfonic or p-toluenesulfonic acid are used. 9. Novel polymorph V of torasemide according to claim 1, characterized in that it is used as a raw material for the preparation of the crystalline modifications I, II and III torasemide or of an amorphous torasemide modification. 10. Novel polymorph V 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. 11. Novel polymorph V of torasemide according to claim 1, characterized in that it may be used as a suitable torasemide form serving as a diuretic or 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, decreasing of 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. 12. Pharmaceutical form, characterized in that as an active ingredient it contains an effective amount of the novel polymorph V of torasemide according to claim 1, without or in combination with one or more pharmaceutically acceptable additives such as sugar, starch, starch derivatives, cellulose, cellulose derivatives, mould release agents, and antiadhesive agents and possibly agents for regulating flowability. 13. Pharmaceutical form according to claim 12, characterized in that it is a tablet, a capsule or an injection.