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Transdermal Testosterone Delivery: Comparison Between Scrotal and Nonscrotal Delivery Systems

The purpose of this investigation was to study the bioequivalence of two testosterone transdermal delivery systems (T-TDSs), Testoderm®, designed to deliver testosterone through scrotal skin, and Androderm®, designed for nonscrotal permeation. In vitro permeation and release kinetics as well as in v...

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Published in:Pharmaceutical development and technology 1999, Vol.4 (3), p.405-414
Main Authors: Lin, Senshang, Xing, Qing-Feng, Chien, Yie W.
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creator Lin, Senshang
Xing, Qing-Feng
Chien, Yie W.
description The purpose of this investigation was to study the bioequivalence of two testosterone transdermal delivery systems (T-TDSs), Testoderm®, designed to deliver testosterone through scrotal skin, and Androderm®, designed for nonscrotal permeation. In vitro permeation and release kinetics as well as in vivo pharmacokinetics in the castrated Yucatan miniature swine (minipigs) model of both T-TDSs were studied side by side under the same experimental conditions. In vitro skin permeation kinetics studies demonstrated that testosterone permeates through minipig dorsal skin at zero-order kinetics from both T-TDSs. The nonscrotal T-TDS, however, has a permeation rate which is ∼13 times higher than that for the scrotal T-TDS. The release of testosterone from the nonscrotal T-TDS showed a biphasic release profile between cumulative amount released and time, whereas a monophasic release profile between cumulative amount released and square root of time was observed for the scrotal T-TDS. Pharmacokinetic analysis of plasma testosterone profiles in minipigs indicated a significant difference (p < 0.001) in daily dose of testosterone delivered (1.20 versus 4.83 mg day), maximum concentration (Cmax) (54.2 versus 218.0 ng dl), and area under concentration-time curve (AUC0-28) [665 versus 3208 (ng dl) × hr] between these T-TDSs. However, there is no difference in time to reach Cmax, mean residence time, and daily-delivered-dose-normalized Cmax and AUC0-28. The difference in pharmacokinetic profiles resulted from the difference in daily doses delivered, which could be attributed remarkably to the difference in permeation rate (∼13-fold) between the nonscrotal and scrotal T-TDSs.
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In vitro permeation and release kinetics as well as in vivo pharmacokinetics in the castrated Yucatan miniature swine (minipigs) model of both T-TDSs were studied side by side under the same experimental conditions. In vitro skin permeation kinetics studies demonstrated that testosterone permeates through minipig dorsal skin at zero-order kinetics from both T-TDSs. The nonscrotal T-TDS, however, has a permeation rate which is ∼13 times higher than that for the scrotal T-TDS. The release of testosterone from the nonscrotal T-TDS showed a biphasic release profile between cumulative amount released and time, whereas a monophasic release profile between cumulative amount released and square root of time was observed for the scrotal T-TDS. 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Pharmacokinetic analysis of plasma testosterone profiles in minipigs indicated a significant difference (p &lt; 0.001) in daily dose of testosterone delivered (1.20 versus 4.83 mg day), maximum concentration (Cmax) (54.2 versus 218.0 ng dl), and area under concentration-time curve (AUC0-28) [665 versus 3208 (ng dl) × hr] between these T-TDSs. However, there is no difference in time to reach Cmax, mean residence time, and daily-delivered-dose-normalized Cmax and AUC0-28. 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Drug treatments</subject><subject>Scrotal</subject><subject>Scrotum - metabolism</subject><subject>Skin Absorption</subject><subject>Swine</subject><subject>Swine, Miniature</subject><subject>Testosterone</subject><subject>Testosterone - administration &amp; dosage</subject><subject>Testosterone - pharmacokinetics</subject><subject>Transdermal</subject><issn>1083-7450</issn><issn>1097-9867</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1999</creationdate><recordtype>article</recordtype><recordid>eNp1kEtPxCAURonR-F66NV0Yd1VoSwvudHwmRk0cl4ZQuMQaCiN0NPPvZTLja-EKbnK-y8dBaI_gI4IZOX44H-cEY4JJ2dQraJNg3uSc1c3q_M7KvKko3kBbMb4minFM19EGwVVZFazeRM_jIF3UEHppszHEwccBgneQnYPt3iHMTrKR7ycydNG77AyGDwCXPargh5SQTmd33sXl-JXJHmdpTR930JqRNsLu8txGT5cX49F1fnt_dTM6vc1VReiQt4VWQKk0mipKGTE8DYwyrHlZg66rhtOSVrUxTLamUIABiDYUmrYgLcflNjpc7J0E_zZNvxB9FxVYKx34aRQ152VRMZ7AfAGmwjEGMGISul6GmSBYzH2K5FN8-0z8_nLxtO1B_6IXAhNwsARkVNKaZFN18YdjnOB6_i5bYJ0zPrn-8MFqMciZ9eErU_5XofkTfQFphxclA4hXPw0uef2n_CdYRKNe</recordid><startdate>1999</startdate><enddate>1999</enddate><creator>Lin, Senshang</creator><creator>Xing, Qing-Feng</creator><creator>Chien, Yie W.</creator><general>Informa UK Ltd</general><general>Taylor &amp; Francis</general><general>Informa Healthcare</general><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>1999</creationdate><title>Transdermal Testosterone Delivery: Comparison Between Scrotal and Nonscrotal Delivery Systems</title><author>Lin, Senshang ; Xing, Qing-Feng ; Chien, Yie W.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c415t-b2dce55afd5c5581f955a8580d936ed647953546ff8abf2ce0ee1df5e7b21b903</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1999</creationdate><topic>Administration, Cutaneous</topic><topic>Animals</topic><topic>Area Under Curve</topic><topic>Biological and medical sciences</topic><topic>Chromatography, High Pressure Liquid</topic><topic>Drug Delivery Systems</topic><topic>General pharmacology</topic><topic>Hormones. Endocrine system</topic><topic>Kinetics</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Nonscrotal</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Scrotal</topic><topic>Scrotum - metabolism</topic><topic>Skin Absorption</topic><topic>Swine</topic><topic>Swine, Miniature</topic><topic>Testosterone</topic><topic>Testosterone - administration &amp; dosage</topic><topic>Testosterone - pharmacokinetics</topic><topic>Transdermal</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Lin, Senshang</creatorcontrib><creatorcontrib>Xing, Qing-Feng</creatorcontrib><creatorcontrib>Chien, Yie W.</creatorcontrib><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Pharmaceutical development and technology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Lin, Senshang</au><au>Xing, Qing-Feng</au><au>Chien, Yie W.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Transdermal Testosterone Delivery: Comparison Between Scrotal and Nonscrotal Delivery Systems</atitle><jtitle>Pharmaceutical development and technology</jtitle><addtitle>Pharm Dev Technol</addtitle><date>1999</date><risdate>1999</risdate><volume>4</volume><issue>3</issue><spage>405</spage><epage>414</epage><pages>405-414</pages><issn>1083-7450</issn><eissn>1097-9867</eissn><abstract>The purpose of this investigation was to study the bioequivalence of two testosterone transdermal delivery systems (T-TDSs), Testoderm®, designed to deliver testosterone through scrotal skin, and Androderm®, designed for nonscrotal permeation. In vitro permeation and release kinetics as well as in vivo pharmacokinetics in the castrated Yucatan miniature swine (minipigs) model of both T-TDSs were studied side by side under the same experimental conditions. In vitro skin permeation kinetics studies demonstrated that testosterone permeates through minipig dorsal skin at zero-order kinetics from both T-TDSs. The nonscrotal T-TDS, however, has a permeation rate which is ∼13 times higher than that for the scrotal T-TDS. The release of testosterone from the nonscrotal T-TDS showed a biphasic release profile between cumulative amount released and time, whereas a monophasic release profile between cumulative amount released and square root of time was observed for the scrotal T-TDS. Pharmacokinetic analysis of plasma testosterone profiles in minipigs indicated a significant difference (p &lt; 0.001) in daily dose of testosterone delivered (1.20 versus 4.83 mg day), maximum concentration (Cmax) (54.2 versus 218.0 ng dl), and area under concentration-time curve (AUC0-28) [665 versus 3208 (ng dl) × hr] between these T-TDSs. However, there is no difference in time to reach Cmax, mean residence time, and daily-delivered-dose-normalized Cmax and AUC0-28. The difference in pharmacokinetic profiles resulted from the difference in daily doses delivered, which could be attributed remarkably to the difference in permeation rate (∼13-fold) between the nonscrotal and scrotal T-TDSs.</abstract><cop>New York, NY</cop><pub>Informa UK Ltd</pub><pmid>10434286</pmid><doi>10.1081/PDT-100101376</doi><tpages>10</tpages></addata></record>
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subjects Administration, Cutaneous
Animals
Area Under Curve
Biological and medical sciences
Chromatography, High Pressure Liquid
Drug Delivery Systems
General pharmacology
Hormones. Endocrine system
Kinetics
Male
Medical sciences
Nonscrotal
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Scrotal
Scrotum - metabolism
Skin Absorption
Swine
Swine, Miniature
Testosterone
Testosterone - administration & dosage
Testosterone - pharmacokinetics
Transdermal
title Transdermal Testosterone Delivery: Comparison Between Scrotal and Nonscrotal Delivery Systems
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