Pharmacokinetic comparison of two bazedoxifene acetate 20 mg tablet formulations in healthy Korean male volunteers

다국어 초록 (Multilingual Abstract)

Bazedoxifene, used as bazedoxifene acetate, is a selective estrogen receptor modulatorthat selectively affects the uterus, breast tissue, bone metabolism, and lipid metabolism byantagonizing or enhancing estrogens in the estrogen receptor in the tissue. This study wasconducted as an open, randomized, two-period, two-treatment, crossover design to comparethe pharmacokinetic (PK) characteristics and tolerability of two bazedoxifene tablets whenadministered to 50 healthy Korean male volunteers. Enrolled subjects were randomlyallocated to 2 sequences of a single oral administration of a test drug and a reference drug,or vice versa with a 14-day washout period between the two doses. Serial blood sampleswere collected over 96 h for PK analysis. Plasma concentration of bazedoxifene was assayedusing liquid chromatography-tandem spectrometry mass. Forty-five participants completedthe study with no clinically relevant safety issues. The peak concentrations (Cmax, mean ±strandard deviation) of reference drug and test drug were 3.191 ± 1.080 and 3.231 ± 1.346ng/mL, respectively, and the areas under the plasma concentration‐time curve from 0 tothe last measurable concentration (AUClast) were 44.697 ± 21.168 ng∙h/mL and 45.902 ±23.130 ng∙h/mL, respectively. The geometric mean ratios of test drug to reference drug andtheir 90% confidence intervals for Cmax and AUClast were 0.9913 (0.8828–1.1132) and 1.0106(0.9345–1.0929), respectively. The incidence of adverse events between the two formulationswas similar. The present study showed that PK and tolerability of two bazedoxifene tabletformulations were comparable when administered to healthy Korean male volunteers.

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