| 摘要 |
<p>#CMT# #/CMT# Beta crystalline form of perindopril arginine salt (I), characterized by the X-ray diffraction diagram on powder, measured by a diffractometer (copper anticathode) and exhibited a Bragg angle 2 theta (expressed in percentage in relation to the most intense line), an interreticular distance (d), an intensity and a relative intensity, as given in table of the specification, is new. #CMT# : #/CMT# Beta crystalline form of perindopril arginine salt of formula (I), characterized by the X-ray diffraction diagram on powder, measured by a diffractometer (copper anticathode) and exhibited a Bragg angle 2 theta (expressed in percentage in relation to the most intense line), an interreticular distance (d), an intensity and a relative intensity, as given in table of the specification, is new. Independent claims are included for: (1) a composition comprising (I) in combination with inert and nontoxic vehicles; and (2) the preparation of (I). #CMT#ACTIVITY : #/CMT# Cardiovascular-Gen; Hypotensive; Cardiant. #CMT#MECHANISM OF ACTION : #/CMT# Angiotensin I converting enzyme inhibitor. No biological data given. #CMT#USE : #/CMT# (I) is useful: for the manufacture of medicaments as an inhibitor of angiotensin I converting enzyme; and to treat the cardiovascular diseases (claimed), preferably arterial hypertension and cardiac insufficiency. #CMT#ADVANTAGE : #/CMT# (I) has excellent stability, hygroscopicity, processability of powder, filterability of solid, crushing and retention of solvent. (I) has pharmacological properties. #CMT#ORGANIC CHEMISTRY : #/CMT# Preparation Claimed: Preparation of (I) comprises heating (L)-arginine salt of perindopril in toluene or acetonitrile reflux and filtering the obtained crystals under hot and dry environment. Preferred Composition: The composition further comprises a diuretic, where the diuretic is the indapamide. #CMT#ADMINISTRATION : #/CMT# Administration of (I) is 500 mg/day, orally, parenterally (intravenously or subcutaneously) or nasally. #CMT#EXAMPLE : #/CMT# Perindopril (L)-arginine salt (100 g) and acetonitrile (5 l) were introduced in a reactor under agitation. The mixture was set in reflux under agitation. The solid was solubilized completely and after a few minutes precipitated under hot environment. Then the obtained crystals were filtered at 80[deg]C after one hour of agitation under reflux. The obtained crystals were dried to obtain anhydrous form of beta crystalline perindopril arginine salt.</p> |
