TY - JOUR
T1 - Comparison of photosensitivity of five dihydropyridines
AU - Mei, Qibing
AU - Shang, Peng
AU - Zhao, Dehua
PY - 1998/5
Y1 - 1998/5
N2 - OBJECTIVES: To compare the photosensitivity of five 1, 4- dihydropyridines (1, 4-DHPs) to sunlight, diffused light and tungsten lamp and study the quantitative structure-activity relationship of five 1, 4-DHPs between the photosensitivity and 4-substituents and 4-substituented phenyl group. METHODS: Five 1, 4-DHPs were exposed to sunlight, diffused light and tungsten lamp respectively. Samples taken at different time were analyzed by reversed-phase high performance liquid chromatography. Photochemical degradation rate constant (K(app)) and half-time (t( 1/4 )) of each 1, 4-DHPs were determined. The QSAR of five 1, 4-DHPs between the V(x) and 4- substituents and K(app) and t( 1/4 ) was worked out respectively. RESULTS: Nifedipine was photochemically degraded in first order reaction when exposed to sunlight, diffused light and tungsten lamp, and the K(app) was (1.02 ± 0.20)min-1, (0. 022 ± 0. 006)min-1 and (0. 015 ± 0. 004) min-1, respectively. m-nifedipine, furandipine, chlorophenyldipine and phenyldipine were photochemically stable when exposed to diffused light and tungsten lamp. However, they were photochemically degradable when exposed to direct sunlight and the K(app) of them was (0.21 ± 0.07)h-1, (0.03 ± 0.02)h-1, (0.019 ± 0.003)h-1 and (0.012 ± 0.001)h-1, respectively. The t( 1/4 ) of five 1, 4-DHPs when exposed to sunlight was 0.68 min, 3.3, 24, 37 and 58 h, respectively. QSAR equation: K(app)= 2.008 1 - 2.987 6 V(x) + 1. 088 5(V(x))2 - 2.574 9 x 10-5(V(x))3(r = 0. 904 6). CONCLUSION: The photosensitivity of 1, 4-DHPs are related not only to 4-substituents, but also to the properties and positions of the substituents on 4-phenyl group.
AB - OBJECTIVES: To compare the photosensitivity of five 1, 4- dihydropyridines (1, 4-DHPs) to sunlight, diffused light and tungsten lamp and study the quantitative structure-activity relationship of five 1, 4-DHPs between the photosensitivity and 4-substituents and 4-substituented phenyl group. METHODS: Five 1, 4-DHPs were exposed to sunlight, diffused light and tungsten lamp respectively. Samples taken at different time were analyzed by reversed-phase high performance liquid chromatography. Photochemical degradation rate constant (K(app)) and half-time (t( 1/4 )) of each 1, 4-DHPs were determined. The QSAR of five 1, 4-DHPs between the V(x) and 4- substituents and K(app) and t( 1/4 ) was worked out respectively. RESULTS: Nifedipine was photochemically degraded in first order reaction when exposed to sunlight, diffused light and tungsten lamp, and the K(app) was (1.02 ± 0.20)min-1, (0. 022 ± 0. 006)min-1 and (0. 015 ± 0. 004) min-1, respectively. m-nifedipine, furandipine, chlorophenyldipine and phenyldipine were photochemically stable when exposed to diffused light and tungsten lamp. However, they were photochemically degradable when exposed to direct sunlight and the K(app) of them was (0.21 ± 0.07)h-1, (0.03 ± 0.02)h-1, (0.019 ± 0.003)h-1 and (0.012 ± 0.001)h-1, respectively. The t( 1/4 ) of five 1, 4-DHPs when exposed to sunlight was 0.68 min, 3.3, 24, 37 and 58 h, respectively. QSAR equation: K(app)= 2.008 1 - 2.987 6 V(x) + 1. 088 5(V(x))2 - 2.574 9 x 10-5(V(x))3(r = 0. 904 6). CONCLUSION: The photosensitivity of 1, 4-DHPs are related not only to 4-substituents, but also to the properties and positions of the substituents on 4-phenyl group.
KW - Chlorophenyldipine
KW - Dihydropyridines
KW - Furandipine
KW - m- nifedipine
KW - Nifedipine
KW - Phenyldipine
KW - Photochemistry
KW - QSAR
UR - http://www.scopus.com/inward/record.url?scp=0344972988&partnerID=8YFLogxK
M3 - 文章
AN - SCOPUS:0344972988
SN - 1001-2494
VL - 33
SP - 291
EP - 294
JO - Chinese Pharmaceutical Journal
JF - Chinese Pharmaceutical Journal
IS - 5
ER -