Valsartan salts
View Patent ↗The invention relates to new salts of valsartan or crystalline, also partly crystalline and amorphous salts of valsartan, the respective production and usage, and pharmaceutical preparations containing such a salt.
1. A calcium salt of valsartan in a crystalline, partially crystalline or an amorphous form.
2. The calcium salt of valsartan according to claim 1 as a tetrahydrate.
3. The tetrahydrate according to claim 2 , characterised by
(i) an X-ray powder pattern taken with a Guinier camera comprising the following interlattice plane intervals: d in [Å]: 16.1±0.3, 9.9±0.2, 9.4±0.2, 7.03±0.1, 6.50±0.1, 5.87±0.05, 5.74±0.05, 4.95±0.05, 4.73±0.05, 4.33±0.05, 4.15±0.05, 4.12±0.05, 3.95±0.05; or
(ii) an ATR-IR spectrum having the following absorption bands expressed in reciprocal wavenumbers (cm −1 ): 1621(st), 1578(m), 1458(m), 1441(m), 1364(m), 1012(m), 758(m), 738(m), 696(m), 666(m).
4. A salt according to claim 1 in the form of a solvate.
5. A salt according to claim 1 in the form of a hydrate.
6. A pharmaceutical composition comprising a a calcium salt of valsartan according to claim 1 and a pharmaceutically acceptable excipient or additive.
7. A pharmaceutical composition according to claim 6 , in combination with at least one composition selected from the group consisting of:
(i) HMG-Co-A reductase inhibitor or a pharmaceutically salt thereof,
(ii) angiotensin converting enzyme (ACE) inhibitor or a pharmaceutically acceptable salt thereof,
(iii) calcium channel blacker or a pharmaceutically acceptable salt thereof,
(iv) aldosterone synthase inhibitor or a pharmaceutically acceptable salt thereof,
(v) aldosterone antagonist or a pharmaceutically acceptable salt thereof,
(vi) dual angiotensin converting enzyme/neutral endopeptidase (ACE/NEP) inhibitor or a pharmaceutically acceptable salt thereof,
(vii) endothelin antagonist or a pharmaceutically acceptable salt thereof,
(viii) renin inhibitor or a pharmaceutically acceptable salt thereof, and
(ix) diuretic or a pharmaceutically acceptable salt thereof.
8. A method for the treatment of diseases and conditions which can be inhibited by blocking the AT 1 receptor comprising administering a therapeutically effective amount of the calcium salt of valsartan of claim 1 to a patient in need thereof.