Pharmacokinetics of hard micronized progesterone capsules via vaginal or oral route compared with soft micronized capsules in healthy postmenopausal women: a randomized open-label clinical study
Authors Wang H, Liu M, Fu Q, Deng C
Received 9 February 2019
Accepted for publication 23 May 2019
Published 23 July 2019 Volume 2019:13 Pages 2475—2482
Checked for plagiarism Yes
Review by Single-blind
Peer reviewer comments 2
Editor who approved publication: Dr Anastasios Lymperopoulos
Hanbi Wang,1 Meizhi Liu,1 Qiang Fu,2 Chengyan Deng1
1Reproductive Center, Department of Obstetrics and Gynecology, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences, Beijing, People’s Republic of China; 2Department of Pharmacy, Peking Union Medical College Hospital, Chinese Academy of Medical Sciences, Beijing, People’s Republic of China
Purpose: This study aimed to evaluate the pharmacokinetics of hard micronized progesterone capsules (Yimaxin) via the vaginal or oral route compared with soft micronized progesterone capsules (Utrogestan) in a Chinese population.
Methods: A prospective single-center randomized open-label trial was conducted in 16 healthy postmenopausal women. They were randomized into two groups to receive four phases of treatment: vaginal Yimaxin, vaginal Utrogestan, oral Yimaxin, or oral Utrogestan, with different sequences.
Results: By the vaginal route, steady-state maximum concentration (Cmax) of Yimaxin and Utrogestan was 29.13±8.09 and 12.30±1.60 mg/L, time to Cmax 9.72±10.50 and 11.03±9.62 hours, central compartment volume of distribution 4.26±1.86 and 10.40±2.32 L, clearance rate 0.18±0.05 and 0.38±0.10 L/h, and AUC 261.42±74.36 and 116.83±19.72 h·ng/mL, respectively. By the oral route, Cmax of Yimaxin and Utrogestan was 62.97±40.59 and 169.53±130.24 mg/L, time to Cmax was 2.88±1.35 and 2.06±1.55 hours, central compartment volume of distribution 132.16±52.13 and 85.08±55.07 L, clearance rate 3.43±1.07 and 2.50±1.04 L/h, and AUC 274.86±160.28 and 472.00±250.54 h·ng/mL, respectively. By the vaginal route, Cmax, minimum concentration, AUC0–72, and AUC of Yimaxin were higher than Utrogestan, while by the oral route the Cmax, AUC0–72, and AUC of Utrogestan were higher than Yimaxin.
Conclusion: Pharmacokinetic parameters were different between Yimaxin and Utrogestan on vaginal and oral administration. By the oral route, the metabolism and absorption of Utrogestan was superior to Yimaxin, while by the vaginal route Yimaxin was superior.
Keywords: micronized progesterone hard capsule, micronized progesterone soft capsule, pharmacokinetics, vaginal administration, oral administration
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