The pharmacokinetics and bioequivalence of acipimox sustained-release tablets after a single and multiple oral administration in healthy dogs

AimTo study the pharmacokinetics and bioequivalence of acipimox sustained-release tablets (SRT) after a single and multiple oral dose in healthy dogs.MethodsThe plasma concentrations of of SRT and reference capsules with a single and multiple oral doses.ResultsThe drug concentration-time profiles fitted to a noncompartment model.After a single dose administration of sustained-release tablets and capsules,the pharmacokinetic parameters were as follows: AUC were (158±30) and (147±37) μg·h·mL^-1; T_max were (4.3±0.8) and (2.6±1.3) h; C_max were (29±6) and (42±10) μg·mL^-1; T_1/2 were (2.3±0.7) and (1.60±0.10) h; MRT were (6.0±0.8) and (3.9±0.7) h, respectively.The relative bioavailability of the sustained-release tablet was (108±16)%.After a multiple oral administration of sustained-release tablets and capsules,the pharmacokinetic parameters were as follows: AUC were (209±23) and (195±26) μg·h·mL^-1; T_max were (6.3±0.8) and (3.4±1.5) h; C_max were (27±4) and (36±5) μg·mL^-1; Cmin were (2.2±1.0) and (0.20±0.20) μg·mL^-1; C_av were (8.7±1.0) and (8.1±1.1) μg·mL^-1; FI were (293±73)% and (448±91)%, respectively.The relative bioavailability of the sustained-release tablet was (114±19)%.Conclusion The results of two one-side test from single dose administration shown that two preparations were bioequivalent.The C_max of sustained-release tablet was lower than that of capsules, while the T_max and MRT of sustained-release tablet were higher than that of capsule, which indicating a good retarding effect.The results from multiple dose administration also shown that two preparations were bioequivalent and the DF of sustained-release tablet was significant lower than that of capsule.