Physico-chemical properties and stabilities of the highly potent calcium antagonist benidipine hydrochloride.
(+/-)-(R*)-2,6-Dimethyl-4-(m-nitrophenyl)-1,4-dihydropyridine-3, 5-dicarboxylic acid (R*)-1-benzyl-3-piperidinyl ester, methyl ester hydrochloride (benidipine hydrochloride, KW-3049), a highly potent calcium antagonist, was examined to clarify its physico-chemical properties, i.e. melting point, spectra (UV, IR, NMR, MS), X-ray diffraction pattern, thermal analysis, solubilities, pKá, partition coefficient and chromatography (TLC, HPLC). The stabilities of KW-3049 were studied under various conditions by HPLC. KW-3049 in solid state was very stable to heat and moisture, and fairly stable to light.
Suzuki
H
H
Pharmaceutical Research Laboratories, Kyowa Hakko Kogyo Co., Ltd., Shizuoka, Japan.
Ono
E
E
Ueno
H
H
Takemoto
Y
Y
Nakamizo
N
N
D000959:Antihypertensive Agents / Q000032:analysis*; D002121:Calcium Channel Blockers / Q000032:analysis*; D002152:Calorimetry, Differential Scanning; D055598:Chemical Phenomena; D002621:Chemistry; D002851:Chromatography, High Pressure Liquid; D002855:Chromatography, Thin Layer; D004055:Differential Thermal Analysis; D004355:Drug Stability; D006358:Hot Temperature; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D015394:Molecular Structure; D008970:Molecular Weight; D009543:Nifedipine / Q000031:analogs & derivatives* / Q000032:analysis; D012995:Solubility; D013055:Spectrophotometry, Infrared; D013056:Spectrophotometry, Ultraviolet; D013818:Thermogravimetry; D014961:X-Ray Diffraction
D000959:Antihypertensive Agents; D002121:Calcium Channel Blockers; C050883:benidipine hydrochloride; D009543:Nifedipine