title: Pharmacokinetics of Oral Combination Contraceptive Drugs Containing Ethinyl Estradiol and Levonorgestrel in Healthy Female Chinese Volunteers.
abstract: OBJECTIVE
  A new combination contraceptive tablet containing 0.02 mg ethinyl estradiol (EE) and 0.10 mg levonorgestrel (LNG) with potential advantages has been developed in China. This study was aimed to describe the pharmacokinetic characteristics of this new combination contraceptive tablet in female Chinese volunteers.
  
  
  METHODS
  This study was designed as phase I, open-label, and one-sequence clinical trial. 12 healthy nonpregnant female Chinese volunteers received a single dose (1 tablet) and multiple dose (1 tablet per day) administration for 21 consecutive days under fasting condition. Blood samples were analyzed with 2 validated LC-MS/MS methods for EE and LNG, respectively.
  
  
  CONCLUSIONS
  After the single dose administration, the C max of EE and LNG were 44.76±18.64 pg/mL and 2.256±1.008 ng/mL, respectively. The steady-state condition of EE was achieved on the 6(th) day after the beginning of the multiple dose administration, while the steady-state condition of LNG was achieved on the 21(st) day. For EE, the mean MRT 0-72 and t 1/2 increased by 40.2 and 30.6%, meanwhile the mean Cl/F and Vd/F decreased by 18.5 and 29.1%, respectively from Day 1 to Day 24. For LNG, the mean MRT 0-72 increased by 27.1%, while the mean Cl/F and Vd/F decreased by 62.4 and 86.3%, respectively from Day 1 to Day 24. The t 1/2 remained unchanged for LNG. The exposure of LNG significantly increased with repeated dosing, but that of EE just slightly increased.
authors.affiliation: Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing, China.
authors.forename: X
authors.initials: X
authors.lastname: Xin
authors.affiliation: Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing, China.
authors.forename: Y
authors.initials: Y
authors.lastname: Wu
authors.affiliation: Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing, China.
authors.forename: X
authors.initials: X
authors.lastname: Liu
authors.affiliation: Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing, China.
authors.forename: C
authors.initials: C
authors.lastname: Sun
authors.affiliation: Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing, China.
authors.forename: T
authors.initials: T
authors.lastname: Geng
authors.affiliation: Department of Pharmaceutical Analysis, China Pharmaceutical University, Nanjing, China.
authors.forename: L
authors.initials: L
authors.lastname: Ding
mesh_terms: D000328:Adult; D044466:Asian People; D002681:China; D003278:Contraceptives, Oral, Hormonal / Q000008:administration & dosage / Q000097:blood / Q000493:pharmacokinetics*; D004305:Dose-Response Relationship, Drug; D004338:Drug Combinations; D004997:Ethinyl Estradiol / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D005260:Female; D064368:Healthy Volunteers; D006801:Humans; D016912:Levonorgestrel / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D055815:Young Adult
chemical_list: D003278:Contraceptives, Oral, Hormonal; D004338:Drug Combinations; D004997:Ethinyl Estradiol; D016912:Levonorgestrel