Photo-stability of the new antiplatelet agent, KBT-3022 (ethyl 2-[4,5-bis(4-methoxyphenyl)thiazole-2-yl]pyrrol-1-ylacetate) in aqueous solutions containing acetonitrile.
The photo-stability of ethyl 2-[4,5-bis(4-methoxyphenyl)thiazole-2-yl]pyrrol-1-ylacetate, KBT-3022 in aqueous solutions containing acetonitrile was investigated under the light of a high pressure mercury lamp. Its main photo-degradation product was assumed to be ethyl 5-hydroxy-5-[4,5-bis(4-methoxyphenyl)thiazole-2-yl]-2-oxo-3-pyrrolin+ ++-1-ylacetate. KBT-3022 was also found to undergo ester hydrolysis by heat in both acidic and basic aqueous solutions, but its hydrolysis was confirmed to be negligible in the range of pH 3-9 at room temperature (25 degrees C). Further, its photo-stability with exposure to the high pressure mercury lamp was comparable to that with exposure to a fluorescent lamp. Therefore, it is considered feasible to simulate the photo-stability of KBT-3022 in aqueous solutions containing acetonitrile by exposure to all other light sources including diffuse daylight, if the cumulative number of photons of the light can be determined by actinometry.
Hanamori
M
M
Pharmaceuticals Research Center, Kanebo, Ltd., Osaka, Japan.
Mizuno
T
T
Akimoto
K
K
Nakagawa
H
H
D000097:Acetonitriles / Q000737:chemistry*; D004355:Drug Stability; D006863:Hydrogen-Ion Concentration; D006868:Hydrolysis; D007700:Kinetics; D008027:Light; D010975:Platelet Aggregation Inhibitors / Q000737:chemistry*; D011758:Pyrroles / Q000737:chemistry*; D013056:Spectrophotometry, Ultraviolet; D013696:Temperature; D013844:Thiazoles / Q000737:chemistry*
D000097:Acetonitriles; D010975:Platelet Aggregation Inhibitors; D011758:Pyrroles; D013844:Thiazoles; C064847:KB 3022; C032159:acetonitrile