To determine the
pharmacokinetics and relative
bioavailability of domestic and
imported sustained release
capsules of 5 isosorbide mononitrate(5 IM), twelve healthy male volunteers were given 5 IM following a single and multiple oral
dose in an open randomized crossover study. The plasma levels of 5 IM were measured by
gas chromatography with electron captured detector method. The paramaters such as T max , C max , MRT and AUC 0→∞ were calculated and there were no significant differences between the two kinds of capsules. The major pharmacokinetic parameters of domestic and imported 5 IM sustained release capsules with a 5d multiple dose were shown respectively as following: T max (h)4.75±0.45 and 5.58±1.51; C max (ng/ml)440.68±54.83 and \{451.38\}±88;MRT(h)11.01±0.67 and 11.05±0.73;AUC 0→∞ (ng/ml·h) 5955.55±689.83 and 6180.65±\{853.04.\} The fraction of drug absorbed \%in vivo\% was correlated well with the percentage amount of drug released in vitro at corresponding time (P<0.05),and the fluctuation indexes on the fifth day in multiple dose study were not significantly different between the two formulations (P>0.05).The relative bioavailability of the domestic capsules for single and multiple dose were 97.42%±11.79% and 97.16%±10.95%. Domestic 5 IM sustained release capsules showed bioequivalence compared with the imported capsules and provided the same nitrate low interval in the latter part of the 24 h dosing interval.
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