Pharmacokinetics and bioavailability of a new testosterone gel formulation in comparison to Testogel® in healthy men
| Autor: | Håkan, Olsson, Rikard, Sandström, Anders, Neijber, Dario, Carrara, Lars, Grundemar |
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| Rok vydání: | 2013 |
| Předmět: |
Adult
Male Cross-Over Studies Adolescent Hormone Replacement Therapy Metabolic Clearance Rate Drug Compounding Skin Absorption Biological Availability Middle Aged Administration Cutaneous Drug Administration Schedule Healthy Volunteers Young Adult Therapeutic Equivalency Area Under Curve Germany Humans Testosterone Gels Half-Life |
| Zdroj: | Clinical pharmacology in drug development. 3(5) |
| ISSN: | 2160-7648 |
| Popis: | This randomized, open-label, multiple-dose three-way cross-over study compared the pharmacokinetics of a new testosterone gel formulation in two strengths, testosterone gel 1% and testosterone gel 2% (FE 999303), with Testogel® in 11 testosterone-suppressed healthy men. Subjects received one of six treatment sequences; 50 mg of testosterone was administered once daily for 7 consecutive days, with different treatments separated by washout-periods of 6-9 days. Testosterone gel 1% and testosterone gel 2% displayed greater relative bioavailability (2.6- and 1.6-fold, respectively) than Testogel on Day 1, which persisted, to a smaller extent, on Day 7. Initial absorption was highest and most rapid for testosterone gel 1% and 2%, showing apparent first-order absorption kinetics. Maximum serum concentrations (Cmax ) were 6.25 and 2.97 ng/mL, respectively, occurring ∼5-6 hours post-application on Day 1 versus Cmax of 1.71 ng/mL after ∼24 hours with Testogel, showing apparent zero-order absorption kinetics. Similar differences were observed on Day 7. All treatments appeared to reach approximately the same steady-state level within the first 24 hours. No application-site skin reactions occurred with any preparation. In conclusion, the new testosterone formulation showed higher bioavailability, and the ability to deliver more testosterone in a smaller volume. |
| Databáze: | OpenAIRE |
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