Bioequivalence of progesterone sustained release suppository in rabbits

Abstract

To study the bioequivalence of a kind of progesterone sustained release suppository, a randomized cross-over study was conducted in 12 rabbits. A single rectal dose of 2.75 mg/kg progesterone sustained released suppository (tested formulation, T) and progesterone suppository (reference formulation, R) was administered; a multiple dose of 2.75 mg/kg was given up to seven times with an interval of 8 h. Concentrations in serum were determined by a competitive enzyme immunoassay. The main parameters of T were: for single and multiple doses, C_max was 48.8±11.8 ng/mL and 43.5±9.4 ng/mL, T_max was 0.5±0.3 h and 0.4±0.3 h, AUC_{(0–24 h)} was 362.4±143 ng·h·mL⁻¹ and 310.6±70.3 ng·h·mL⁻¹, respectively. The relative bioavailability of T to R were (104.2±13.4)% and (111.4±19.1)%, respectively. Statistical analysis showed that the two formulations were bioequivalent and T had sustained released feature.

Keywords

progesterone sustained release suppository / pharmacokinetics / in vivo release

References

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