Single and multidose pharmacokinetic study of a vaginal micronized progesterone insert (Endometrin) compared with vaginal gel in healthy reproductive-aged female subjects
| Autor: | James Longstreth, Emily J. Blake, Sally Faith Dorfman, Paul M. Norris, Vladimir I. Yankov |
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| Rok vydání: | 2008 |
| Předmět: |
Adult
medicine.medical_specialty Time Factors Adolescent Reproductive Techniques Assisted Drug Administration Schedule Andrology Young Adult Pharmacokinetics Internal medicine medicine Humans Dosing Luteal support Progesterone Dosage Forms Dose-Response Relationship Drug business.industry Reproduction Healthy subjects Vaginal gel Age Factors Obstetrics and Gynecology Micronized progesterone Endometrin Administration Intravaginal Endocrinology Reproductive Medicine Health Vaginal Creams Foams and Jellies Female medicine.drug_brand business Clearance |
| Zdroj: | Fertility and sterility. 94(4) |
| ISSN: | 1556-5653 |
| Popis: | Objective To determine pharmacokinetic profiles of two times a day and three times a day dosage regimens of Endometrin, a micronized progesterone vaginal insert for luteal support in assisted reproductive technology, compared with a gel. Design A single-center, randomized, open-label, single-day, and multiple-day (5 days) parallel design pharmacokinetic study. Setting University clinical research unit. Patient(s) Three groups of six healthy subjects, ages 18 to 40 years. Intervention(s) Endometrin vaginal inserts two times a day or three times a day, or gel daily. Main Outcome Measure(s) Pharmacokinetic profiles. Result(s) Progesterone serum concentrations increased rapidly following administration of Endometrin vaginal insert, producing higher peak concentrations ( C max ) and clearing faster than gel. On the single day of dosing, mean C max was 17.0 ± 2.7 ng/mL in the two times a day group, 19.8 ± 2.9 ng/mL in the three times a day group, and 6.82 ± 1.69 ng/mL in the gel group. Endometrin treatments reached steady state within the first 2 days (24–36 hours), much more rapidly than the gel, which had not reached steady state by 5 days. At 5 days, the Endometrin treatments produced sustained progesterone concentrations exceeding 10 mg/mL across 24 hours. Conclusions Endometrin vaginal inserts reached higher C max , produced greater systemic exposure (area under the curve 0–24), achieved steady state more rapidly, and cleared more rapidly after termination of therapy than the comparator. |
| Databáze: | OpenAIRE |
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