Title:Two Sustained Release Membranes Used in Formulating Low Strength
Testosterone Reservoir Transdermal Patches
Volume: 21
Issue: 3
Author(s): Ria Vashishth, Monica C. Chuong*, Juan Chang Duarte, Yadnya Gharat and Stephen G. Kerr
Affiliation:
- Department of Pharmaceutical Sciences, MCPHS University, Boston, USA
Keywords:
Testosterone, HPLC stability indication study, FDA Similarity Factor f2 values, CoTran™ membrane film, In vitro paddle over disc dissolution, ethylene vinyl acetate, reservoir transdermal patch.
Abstract:
Introduction: Several Testosterone Replacement Therapies exist for hypogonadism, but an
in-depth analysis of these products reveals a high dosing frequency and a high drug loading, up to 120
mg for a potent drug like Testosterone. This may lead to patient non-compliance and toxicity problems
if used improperly. Androderm® is the only 24-hour marketed transdermal patch. Testopel pellets are
another extended-release product given subcutaneously every 3-6 months. But it requires surgical implantation
and is associated with severe adverse effects. For this reason, the development of other extended-
release testosterone products is needed. The study aims at using different excipients for the exploration
of sustained-release patches.
Methods: Reservoir formulations were prepared using Carbomer 941 and HPMC K100M as the sustained-
release polymers plus CoTran™ 9702 and CoTran™ 9712 as the release membranes. The formulated
patches were subjected to in vitro dissolution for 24 h. The amount of drug release at each time
point was determined using the developed HPLC assay. FDA Similarity Factor, f2, t-test, and ANOVA
were applied to all nine-point collected samples.
Results: CoTran™ 9712 membrane was found to be a better candidate than CoTran™ 9702. The
in vitro release profiles of the four formulations were compared (Carbomer vs. HPMC, and CoTran™
9702 vs. CoTran™ 9712).
Conclusion: CoTran™ 9702 releases testosterone significantly lower. Carbomer and CoTran™ 9712
were the best formulation among all with the highest drug release of 2.16 ± 0.36 mg.
