Novel Patch for Transdermal Administration of Morphine
Abstract Context Transdermal absorption of morphine into the systemic circulation through intact skin has not been reported. Objectives To describe a novel transdermal formulation for a morphine hydrochloride patch consisting of polyethylene sponge foam as the retaining agent and adjusted proportion...
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Veröffentlicht in: | Journal of pain and symptom management 2012-10, Vol.44 (4), p.479-485 |
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container_title | Journal of pain and symptom management |
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creator | Inui, Naoki, MD, PhD Kato, Tatsuhisa, PhD Uchida, Shinya, PhD Chida, Kingo, MD, PhD Takeuchi, Kazuhiko, MD, PhD Kimura, Takahito, PhD Watanabe, Hiroshi, MD, PhD |
description | Abstract Context Transdermal absorption of morphine into the systemic circulation through intact skin has not been reported. Objectives To describe a novel transdermal formulation for a morphine hydrochloride patch consisting of polyethylene sponge foam as the retaining agent and adjusted proportions of morphine hydrochloride and adjunctive drugs. Methods In this study, the transdermal morphine hydrochloride patch was administered to intact skin in five subjects and the plasma concentrations of morphine and its metabolites were examined. Results Morphine was absorbed systemically, producing plasma morphine concentrations above the assay detection limit by at least 24 hours after attachment of patches containing a total dose of 180 mg of morphine. The levels gradually increased in a time-dependent manner without serious events. The area under the concentration-time curve from 0 to 72 hours (AUC0–72 ) values for morphine, morphine-6-glucuronide, and morphine-3-glucuronide were 60.4 ± 13.4, 133.7 ± 17.4, and 861.5 ± 126.7 ng·h/mL, respectively. The mean plasma area under the concentration-time curve from 0 to 72 hours ratio for morphine-6-glucuronide relative to morphine was 2.64. Conclusion These data provide useful information for developing a transdermal morphine system. |
doi_str_mv | 10.1016/j.jpainsymman.2011.10.022 |
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Objectives To describe a novel transdermal formulation for a morphine hydrochloride patch consisting of polyethylene sponge foam as the retaining agent and adjusted proportions of morphine hydrochloride and adjunctive drugs. Methods In this study, the transdermal morphine hydrochloride patch was administered to intact skin in five subjects and the plasma concentrations of morphine and its metabolites were examined. Results Morphine was absorbed systemically, producing plasma morphine concentrations above the assay detection limit by at least 24 hours after attachment of patches containing a total dose of 180 mg of morphine. The levels gradually increased in a time-dependent manner without serious events. The area under the concentration-time curve from 0 to 72 hours (AUC0–72 ) values for morphine, morphine-6-glucuronide, and morphine-3-glucuronide were 60.4 ± 13.4, 133.7 ± 17.4, and 861.5 ± 126.7 ng·h/mL, respectively. The mean plasma area under the concentration-time curve from 0 to 72 hours ratio for morphine-6-glucuronide relative to morphine was 2.64. Conclusion These data provide useful information for developing a transdermal morphine system.</description><identifier>ISSN: 0885-3924</identifier><identifier>EISSN: 1873-6513</identifier><identifier>DOI: 10.1016/j.jpainsymman.2011.10.022</identifier><identifier>PMID: 22727949</identifier><identifier>CODEN: JSPME2</identifier><language>eng</language><publisher>New York, NY: Elsevier Inc</publisher><subject>Absorption ; Administration, Cutaneous ; Aged ; Anesthesia & Perioperative Care ; Area Under Curve ; Attachment ; Biological and medical sciences ; Biological Availability ; Detection ; Dosage ; Humans ; Male ; Medical sciences ; Middle Aged ; Morphine ; Morphine - administration & dosage ; Morphine - blood ; Morphine - pharmacokinetics ; Pain Medicine ; pharmacokinetics ; Pharmacology. Drug treatments ; transdermal administration ; Transdermal Patch</subject><ispartof>Journal of pain and symptom management, 2012-10, Vol.44 (4), p.479-485</ispartof><rights>U.S. Cancer Pain Relief Committee</rights><rights>2012 U.S. Cancer Pain Relief Committee</rights><rights>2015 INIST-CNRS</rights><rights>Copyright © 2012 U.S. Cancer Pain Relief Committee. Published by Elsevier Inc. All rights reserved.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c604t-d8a1e1aadb04b80feb4caa23a7b3eb95588d5b2c415810f7c45c091e316944383</citedby><cites>FETCH-LOGICAL-c604t-d8a1e1aadb04b80feb4caa23a7b3eb95588d5b2c415810f7c45c091e316944383</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0885392412001716$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,30977,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=26446548$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/22727949$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Inui, Naoki, MD, PhD</creatorcontrib><creatorcontrib>Kato, Tatsuhisa, PhD</creatorcontrib><creatorcontrib>Uchida, Shinya, PhD</creatorcontrib><creatorcontrib>Chida, Kingo, MD, PhD</creatorcontrib><creatorcontrib>Takeuchi, Kazuhiko, MD, PhD</creatorcontrib><creatorcontrib>Kimura, Takahito, PhD</creatorcontrib><creatorcontrib>Watanabe, Hiroshi, MD, PhD</creatorcontrib><title>Novel Patch for Transdermal Administration of Morphine</title><title>Journal of pain and symptom management</title><addtitle>J Pain Symptom Manage</addtitle><description>Abstract Context Transdermal absorption of morphine into the systemic circulation through intact skin has not been reported. Objectives To describe a novel transdermal formulation for a morphine hydrochloride patch consisting of polyethylene sponge foam as the retaining agent and adjusted proportions of morphine hydrochloride and adjunctive drugs. Methods In this study, the transdermal morphine hydrochloride patch was administered to intact skin in five subjects and the plasma concentrations of morphine and its metabolites were examined. Results Morphine was absorbed systemically, producing plasma morphine concentrations above the assay detection limit by at least 24 hours after attachment of patches containing a total dose of 180 mg of morphine. The levels gradually increased in a time-dependent manner without serious events. The area under the concentration-time curve from 0 to 72 hours (AUC0–72 ) values for morphine, morphine-6-glucuronide, and morphine-3-glucuronide were 60.4 ± 13.4, 133.7 ± 17.4, and 861.5 ± 126.7 ng·h/mL, respectively. The mean plasma area under the concentration-time curve from 0 to 72 hours ratio for morphine-6-glucuronide relative to morphine was 2.64. Conclusion These data provide useful information for developing a transdermal morphine system.</description><subject>Absorption</subject><subject>Administration, Cutaneous</subject><subject>Aged</subject><subject>Anesthesia & Perioperative Care</subject><subject>Area Under Curve</subject><subject>Attachment</subject><subject>Biological and medical sciences</subject><subject>Biological Availability</subject><subject>Detection</subject><subject>Dosage</subject><subject>Humans</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Middle Aged</subject><subject>Morphine</subject><subject>Morphine - administration & dosage</subject><subject>Morphine - blood</subject><subject>Morphine - pharmacokinetics</subject><subject>Pain Medicine</subject><subject>pharmacokinetics</subject><subject>Pharmacology. Drug treatments</subject><subject>transdermal administration</subject><subject>Transdermal Patch</subject><issn>0885-3924</issn><issn>1873-6513</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2012</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>7QJ</sourceid><recordid>eNqNkkuLFDEQgIMo7rj6F6Q9CF56TOXV6YuwDL5gfYDrOaTT1Wza7mRMehbm35tmxgee9hSofPXgqyLkBdAtUFCvx-24tz7k4zzbsGUUoMS3lLEHZAO64bWSwB-SDdVa1rxl4oI8yXmklEqu-GNywVjDmla0G6I-xzucqq92cbfVEFN1k2zIPabZTtVVP_vg85Ls4mOo4lB9iml_6wM-JY8GO2V8dn4vyfd3b292H-rrL-8_7q6ua6eoWOpeW0Cwtu-o6DQdsBPOWsZt03HsWim17mXHnACpgQ6NE9LRFpCDaoXgml-SV6e6-xR_HjAvZvbZ4TTZgPGQDQCTTPO2uQdKNWNca8oL2p5Ql2LOCQezT3626Vggsxo2o_nHsFkNr1_FcMl9fm5z6Gbs_2T-VlqAl2fAZmenofh0Pv_llBBKinXe3YnD4u_OYzLZeQwOe5_QLaaP_l7jvPmvipvKzkrjH3jEPMZDCmVBBkxmhppv60msFwGMUmhA8V_1PLMv</recordid><startdate>20121001</startdate><enddate>20121001</enddate><creator>Inui, Naoki, MD, PhD</creator><creator>Kato, Tatsuhisa, PhD</creator><creator>Uchida, Shinya, PhD</creator><creator>Chida, Kingo, MD, PhD</creator><creator>Takeuchi, Kazuhiko, MD, PhD</creator><creator>Kimura, Takahito, PhD</creator><creator>Watanabe, Hiroshi, MD, PhD</creator><general>Elsevier Inc</general><general>Elsevier</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><scope>7QJ</scope></search><sort><creationdate>20121001</creationdate><title>Novel Patch for Transdermal Administration of Morphine</title><author>Inui, Naoki, MD, PhD ; Kato, Tatsuhisa, PhD ; Uchida, Shinya, PhD ; Chida, Kingo, MD, PhD ; Takeuchi, Kazuhiko, MD, PhD ; Kimura, Takahito, PhD ; Watanabe, Hiroshi, MD, PhD</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c604t-d8a1e1aadb04b80feb4caa23a7b3eb95588d5b2c415810f7c45c091e316944383</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2012</creationdate><topic>Absorption</topic><topic>Administration, Cutaneous</topic><topic>Aged</topic><topic>Anesthesia & Perioperative Care</topic><topic>Area Under Curve</topic><topic>Attachment</topic><topic>Biological and medical sciences</topic><topic>Biological Availability</topic><topic>Detection</topic><topic>Dosage</topic><topic>Humans</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Middle Aged</topic><topic>Morphine</topic><topic>Morphine - administration & dosage</topic><topic>Morphine - blood</topic><topic>Morphine - pharmacokinetics</topic><topic>Pain Medicine</topic><topic>pharmacokinetics</topic><topic>Pharmacology. Drug treatments</topic><topic>transdermal administration</topic><topic>Transdermal Patch</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Inui, Naoki, MD, PhD</creatorcontrib><creatorcontrib>Kato, Tatsuhisa, PhD</creatorcontrib><creatorcontrib>Uchida, Shinya, PhD</creatorcontrib><creatorcontrib>Chida, Kingo, MD, PhD</creatorcontrib><creatorcontrib>Takeuchi, Kazuhiko, MD, PhD</creatorcontrib><creatorcontrib>Kimura, Takahito, PhD</creatorcontrib><creatorcontrib>Watanabe, Hiroshi, MD, PhD</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><collection>Applied Social Sciences Index & Abstracts (ASSIA)</collection><jtitle>Journal of pain and symptom management</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Inui, Naoki, MD, PhD</au><au>Kato, Tatsuhisa, PhD</au><au>Uchida, Shinya, PhD</au><au>Chida, Kingo, MD, PhD</au><au>Takeuchi, Kazuhiko, MD, PhD</au><au>Kimura, Takahito, PhD</au><au>Watanabe, Hiroshi, MD, PhD</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Novel Patch for Transdermal Administration of Morphine</atitle><jtitle>Journal of pain and symptom management</jtitle><addtitle>J Pain Symptom Manage</addtitle><date>2012-10-01</date><risdate>2012</risdate><volume>44</volume><issue>4</issue><spage>479</spage><epage>485</epage><pages>479-485</pages><issn>0885-3924</issn><eissn>1873-6513</eissn><coden>JSPME2</coden><abstract>Abstract Context Transdermal absorption of morphine into the systemic circulation through intact skin has not been reported. Objectives To describe a novel transdermal formulation for a morphine hydrochloride patch consisting of polyethylene sponge foam as the retaining agent and adjusted proportions of morphine hydrochloride and adjunctive drugs. Methods In this study, the transdermal morphine hydrochloride patch was administered to intact skin in five subjects and the plasma concentrations of morphine and its metabolites were examined. Results Morphine was absorbed systemically, producing plasma morphine concentrations above the assay detection limit by at least 24 hours after attachment of patches containing a total dose of 180 mg of morphine. The levels gradually increased in a time-dependent manner without serious events. The area under the concentration-time curve from 0 to 72 hours (AUC0–72 ) values for morphine, morphine-6-glucuronide, and morphine-3-glucuronide were 60.4 ± 13.4, 133.7 ± 17.4, and 861.5 ± 126.7 ng·h/mL, respectively. The mean plasma area under the concentration-time curve from 0 to 72 hours ratio for morphine-6-glucuronide relative to morphine was 2.64. Conclusion These data provide useful information for developing a transdermal morphine system.</abstract><cop>New York, NY</cop><pub>Elsevier Inc</pub><pmid>22727949</pmid><doi>10.1016/j.jpainsymman.2011.10.022</doi><tpages>7</tpages><oa>free_for_read</oa></addata></record> |
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source | Applied Social Sciences Index & Abstracts (ASSIA); MEDLINE; Elsevier ScienceDirect Journals; EZB Electronic Journals Library |
subjects | Absorption Administration, Cutaneous Aged Anesthesia & Perioperative Care Area Under Curve Attachment Biological and medical sciences Biological Availability Detection Dosage Humans Male Medical sciences Middle Aged Morphine Morphine - administration & dosage Morphine - blood Morphine - pharmacokinetics Pain Medicine pharmacokinetics Pharmacology. Drug treatments transdermal administration Transdermal Patch |
title | Novel Patch for Transdermal Administration of Morphine |
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