title: Pharmacokinetics of betamethasone and betamethasone 17-monopropionate in Chinese healthy volunteers after intramuscular injection of betamethasone phosphate/betamethasone dipropionate.
abstract: The aim of this study was to evaluate the pharmacokinetic profiles of betamethasone (BOH, CAS 378-44-9) and betamethasone 17-monopropionate (B17P), the active metabolites of betamethasone phosphate (BSP) and betamethasone dipropionate (BDP), respectively, after administration of betamethasone i.m. (BSP 2 mg and BDP 5 mg). After ten healthy volunteers had received a single-dose intramuscular adminitration of betamethasone i.m., blood samples were collected pre-dose and for 336 h postdose. The plasma levels of B17P and BOH were measured by liquid chromatography-tandem mass spectrometry (LC-MS/ MS). When compared to BOH, B17P exhibited a longer time to maximum concentration (15.0 +/- 9.0 h vs. 2.8 +/- 1.7 h), a lower Cmax (0.6 +/- 0.2 ng/mL vs. 14.5 +/- 3.7 ng/mL), and a much longer half-life (80.8 +/- 22.7 h vs. 9.6 +/- 3.6 h). Betamethasone i.m. produced rapid onset and sustained action through an initial rapid-increased plasma concentration of BOH and a sustained plasma concentration of B17P, respectively.
authors: School of Pharmacy, Nanjing Medical University, Nanjing, The People's Republic of China.
authors: Chunhui
authors: C
authors: He
authors: Hongwei
authors: H
authors: Fan
authors: Jie
authors: J
authors: Tan
authors: Jianjun
authors: J
authors: Zou
authors: Yubing
authors: Y
authors: Zhu
authors: Kun
authors: K
authors: Yang
authors: Qin
authors: Q
authors: Hu
mesh_terms: D000293:Adolescent; D000328:Adult; D000893:Anti-Inflammatory Agents / Q000493:pharmacokinetics*; D001623:Betamethasone / Q000008:administration & dosage / Q000031:analogs & derivatives* / Q000493:pharmacokinetics; D002851:Chromatography, High Pressure Liquid; D004562:Electrocardiography / Q000187:drug effects; D006207:Half-Life; D006801:Humans; D007273:Injections, Intramuscular; D008297:Male; D013058:Mass Spectrometry; D055815:Young Adult
chemical_list: D000893:Anti-Inflammatory Agents; C540427:betamethasone 17-monopropionate; C028994:betamethasone sodium phosphate; C011175:betamethasone-17,21-dipropionate; D001623:Betamethasone