OBJECTIVE To investigate the
bioavailability of
diltiazem hydrochloride sustained release capsules in human.METHODS A single oral dose(180 mg) and a multiple oral dose(180 mg·d -1 × 6 d) diltiazem of reference or test preparations was given to healthy male volunteers according to an open randomized crossover study.The plasma concentrations of diltiazem were determined by a
RP-HPLC method.The pharmacokinetic parameters and biovailability of test
preparation were compared with reference preparation.RESULTS The main pharmacokinetic parameters of the reference preparation and the test preparation were as follows,single dose(SD): c _ max were (80.8±25.0) and (89.0±25.6) μg·L -1 , t _ max were (5.75±2.02) and (6.00±2.55) h, t _ 1/2 were (11.44±1.41) and (10.80±1.44) h,AUC_ 0～t were (1 635.6±355.7) and (1610.5±311.7) μg·h·L -1 ,AUC_ 0→∞ were (1 681.1± 356.9 ) and (1 648.8±312.1) μg·h·L -1 .The relative bioavailability of the reference to test preparation was (100.0±17.1)%.Multiple dose(MD): c _ max were (177.6±47.0) and (164.3±36.8) μg·L -1 , c _ min were (44.3±16.3) and (40.3±14.7) μg·L -1 , t _ max were (3.88±2.21) and (3.73±2.20) h, t _ 1/2 were (10.27±3.05) and (10.73±2.72) h,AUC SS were (2 328.9±637.3) and ( 2 168.8 ±544.5) μg·h·L -1 , c _ av were (97.0±26.6) and (90.4±22.7) μg·L -1 ,DF were (142.9±32.3)% and (139.5±31.3)% respectively.The relative bioavailability of reference to test preparation was (94.6±12.3)%.CONCLUSION The results of statistic analysis showed that the reference preparation and the test preparation were bioequivalent.
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