Pharmacokinetics and bioavailability of a new testosterone gel formulation in comparison to Testogel® in healthy men
(2014) In Clinical Pharmacology in Drug Development 3(5). p.358-364- Abstract
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... (More)
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.
(Less)
- author
- Olsson, Håkan ; Sandström, Rikard ; Neijber, Anders ; Carrara, Dario and Grundemar, Lars LU
- organization
- publishing date
- 2014-09
- type
- Contribution to journal
- publication status
- published
- subject
- keywords
- Administration, Cutaneous, Adolescent, Adult, Area Under Curve, Biological Availability, Cross-Over Studies, Drug Administration Schedule, Drug Compounding, Gels, Germany, Half-Life, Healthy Volunteers, Hormone Replacement Therapy, Humans, Male, Metabolic Clearance Rate, Middle Aged, Skin Absorption, Testosterone/administration & dosage, Therapeutic Equivalency, Young Adult
- in
- Clinical Pharmacology in Drug Development
- volume
- 3
- issue
- 5
- pages
- 358 - 364
- publisher
- Wiley-Blackwell
- external identifiers
-
- scopus:84908504368
- pmid:27129008
- ISSN
- 2160-763X
- DOI
- 10.1002/cpdd.110
- language
- English
- LU publication?
- no
- additional info
- © 2014, The American College of Clinical Pharmacology.
- id
- 513219c3-eb2f-4f07-88f5-d0cc3b123177
- date added to LUP
- 2019-09-03 12:59:26
- date last changed
- 2024-01-01 18:32:28
@article{513219c3-eb2f-4f07-88f5-d0cc3b123177, abstract = {{<p>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.</p>}}, author = {{Olsson, Håkan and Sandström, Rikard and Neijber, Anders and Carrara, Dario and Grundemar, Lars}}, issn = {{2160-763X}}, keywords = {{Administration, Cutaneous; Adolescent; Adult; Area Under Curve; Biological Availability; Cross-Over Studies; Drug Administration Schedule; Drug Compounding; Gels; Germany; Half-Life; Healthy Volunteers; Hormone Replacement Therapy; Humans; Male; Metabolic Clearance Rate; Middle Aged; Skin Absorption; Testosterone/administration & dosage; Therapeutic Equivalency; Young Adult}}, language = {{eng}}, number = {{5}}, pages = {{358--364}}, publisher = {{Wiley-Blackwell}}, series = {{Clinical Pharmacology in Drug Development}}, title = {{Pharmacokinetics and bioavailability of a new testosterone gel formulation in comparison to Testogel® in healthy men}}, url = {{http://dx.doi.org/10.1002/cpdd.110}}, doi = {{10.1002/cpdd.110}}, volume = {{3}}, year = {{2014}}, }