Generated: April 29, 2017
|Title:||.alpha. crystalline form of the arginine salt of perindopril, a process for its preparation and pharmaceutical compositions containing it|
|Abstract:||.alpha.-crystalline form of the compound of formula (I): ##STR00001## characterized by its powder X-ray diffraction diagram. Medicinal products containing the same which are useful as inhibitors of angiotensin I converting enzyme.|
|Inventor(s):||Coquerel; Gerard (Boos, FR), Lefebvre; Loic (Mont Saint Aignan, FR), Souvie; Jean-Claude (Pau, FR), Authouart; Pascale (Les Trois Pierres, FR)|
|Assignee:||Les Laboratoires Servier (Suresnes Cedex, FR)|
1. An .alpha.-crystalline form of the L-arginine salt of perindopril of formula (I): ##STR00003## exhibiting essentially the following powder X-ray diffraction peaks,
measured using a diffractometer with a copper anti-cathode and expressed in terms of Bragg's angle 2 theta (.degree.): 4.5, 7.9 and 13.5.
2. The .alpha.-crystalline form of the compound of formula (I) according to claim 1, characterised by the following powder X-ray diffraction peaks, measured using a diffractometer with a copper anti-cathode and expressed in terms of Bragg's angle 2 theta)(.degree.): 4.5, 7.9, 13.5, 17.5 and 20.6.
3. The a-crystalline form of the compound of formula (I) of claim 1, exhibiting essentially the following powder X-ray diffraction diagram measured using a diffractometer (copper anticathode) and expressed in terms of inter-planar distance d, Bragg's angle 2 theta, intensity and relative intensity (expressed as a percentage of the most intense line): TABLE-US-00004 Inter-planar Relative intensity Angle 2 theta (.degree.) distance d (.ANG.) Intensity (%) 4.52 19.53 2211 88.7 7.94 11.12 2080 83.5 12.152 7.277 682 27.4 13.480 6.563 2492 100.0 14.029 6.308 422 16.9 14.948 5.922 552 22.1 15.873 5.579 493 19.8 17.531 5.055 1600 64.2 18.787 4.719 363 14.5 19.579 4.530 1078 43.3 20.635 4.301 1794 72.0 22.616 3.928 798 32.0 23.367 3.804 473 19.0 23.807 3.735 362 14.5 24.434 3.640 409 16.4 27.148 3.282 450 18.1 28.214 3.160 417 16.7
4. A process for the preparation of the .alpha.-crystalline form of the compound of formula (I) of claims 1, wherein perindopril is dissolved in water with L-arginine, and an apolar solvent and a polar solvent are added, wherein the apolar solvent is selected from methylcvclohexane, cyclohexane and toluene, and the polar solvent is selected from dimethyl sulphoxide, N,N-dimethylformamide, N,N-dimethylacetamide and N-methyl-2-pyrrolidinone, and the crystals obtained are filtered off, washed and dried.
5. The process of claim 4, wherein the apolar solvent is methylcyclohexane and the polar solvent is dimethyl sulphoxide.
6. A pharmaceutical composition comprising as active ingredient the compound of claim 1, in combination with one or more pharmaceutically acceptable, inert, non-toxic carriers.
7. The pharmaceutical composition of claim 6, further comprising a diuretic.
8. The pharmaceutical composition of claim 7, wherein the diuretic is indapamide.
9. A method for treating arterial hypertension and heart failure, comprising the step of administering to a living animal body, including a human, a therapeutically effective amount of the compound of claim 1.
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