D. Chen et al., DEGRADATION RATES OF CAPTOPRIL IN AQUEOUS-MEDIUM THROUGH BUFFER-CATALYSIS OXIDATION, Drug development and industrial pharmacy, 21(7), 1995, pp. 781-792
Initial degradation rates of captopril (0.1 mg/mL) in acetate, citric,
and phosphate buffer solutions with different buffer concentrations a
t 80 degrees C (mu=0.5) were studied at pH 6.0. All degradation reacti
ons of captopril solutions fitted an apparent first-order plot. The de
gradation rates of captopril rose with increasing buffer concentration
s. A mechanism involving the buffer-catalysis oxidation reaction of ca
ptopril was proposed in this study. The low apparent first-order degra
dation rates of captopril in citric buffer solutions might have been d
ue to the chelating effect of the citric buffer, which reduced the met
al-catalysis oxidation reaction of captopril. Therefore, using low con
centrations of citric buffer to improve solution stability seems to be
an appropriate approach in a liquid formulation development of captop
ril. To select citric buffer at a low concentration for the dissolutio
n medium might be the right choice for a sustained-release formulation
dissolution study of captopril.