Formulation and Efficacy Studies of New Topical Anesthetic Creams
Abstract Local anesthetics (lidocaine or tetracaine) spontaneously melted at 25°C when mixed with thymol and aqueous isopropyl alcohol solution (IPA) at proper ratios and formed novel two-phase melt systems (TMS). The TMS consisted of a homogeneous oil phase containing primarily a local anesthetic a...
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Veröffentlicht in: | Drug development and industrial pharmacy 2003-01, Vol.29 (5), p.505-512 |
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description | Abstract
Local anesthetics (lidocaine or tetracaine) spontaneously melted at 25°C when mixed with thymol and aqueous isopropyl alcohol solution (IPA) at proper ratios and formed novel two-phase melt systems (TMS). The TMS consisted of a homogeneous oil phase containing primarily a local anesthetic agent (lidocaine or tetracaine) and thymol, and a homogeneous aqueous phase containing primarily IPA and pH 9.2 buffer. The relationship between melting of the solid components and system composition was determined from the phase diagram obtained by a titration method. A select TMS of a local anesthetic agent (lidocaine or tetracaine) was directly emulsified to prepare an O W cream and tested for the anesthetic efficacy on intact human skin. While both lidocaine (6%) and tetracaine (4%) creams were highly effective for dermal anesthesia with a similar onset time, the tetracaine cream exhibited a significantly longer duration of action than the lidocaine cream. An accelerated stability study indicated that lidocaine was significantly more stable than tetracaine in the creams. |
doi_str_mv | 10.1081/DDC-120018639 |
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Local anesthetics (lidocaine or tetracaine) spontaneously melted at 25°C when mixed with thymol and aqueous isopropyl alcohol solution (IPA) at proper ratios and formed novel two-phase melt systems (TMS). The TMS consisted of a homogeneous oil phase containing primarily a local anesthetic agent (lidocaine or tetracaine) and thymol, and a homogeneous aqueous phase containing primarily IPA and pH 9.2 buffer. The relationship between melting of the solid components and system composition was determined from the phase diagram obtained by a titration method. A select TMS of a local anesthetic agent (lidocaine or tetracaine) was directly emulsified to prepare an O W cream and tested for the anesthetic efficacy on intact human skin. While both lidocaine (6%) and tetracaine (4%) creams were highly effective for dermal anesthesia with a similar onset time, the tetracaine cream exhibited a significantly longer duration of action than the lidocaine cream. An accelerated stability study indicated that lidocaine was significantly more stable than tetracaine in the creams.</description><identifier>ISSN: 0363-9045</identifier><identifier>EISSN: 1520-5762</identifier><identifier>DOI: 10.1081/DDC-120018639</identifier><identifier>PMID: 12779280</identifier><language>eng</language><publisher>Colchester: Informa UK Ltd</publisher><subject>2-Propanol - chemistry ; Administration, Cutaneous ; Adult ; Anesthetics, Local - administration & dosage ; Anesthetics, Local - chemistry ; Anesthetics, Local - pharmacology ; Anesthetics. Neuromuscular blocking agents ; Biological and medical sciences ; Drug Compounding ; Drug Stability ; Efficacy ; Female ; General pharmacology ; Humans ; Lidocaine ; Lidocaine - administration & dosage ; Lidocaine - chemistry ; Lidocaine - pharmacology ; Local anesthetic ; Male ; Medical sciences ; Middle Aged ; Neuropharmacology ; Ointments ; Particle Size ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Skin - drug effects ; Solutions ; Tetracaine ; Tetracaine - administration & dosage ; Tetracaine - chemistry ; Tetracaine - pharmacology ; Thymol - chemistry ; Topical ; Two-phase melt system ; Viscosity</subject><ispartof>Drug development and industrial pharmacy, 2003-01, Vol.29 (5), p.505-512</ispartof><rights>2003 Informa UK Ltd All rights reserved: reproduction in whole or part not permitted 2003</rights><rights>2003 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c485t-4519ef13f54d9822914b4c531fc543a482bc72d4bcfc9b551573eaa55c1fa6303</citedby><cites>FETCH-LOGICAL-c485t-4519ef13f54d9822914b4c531fc543a482bc72d4bcfc9b551573eaa55c1fa6303</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.tandfonline.com/doi/pdf/10.1081/DDC-120018639$$EPDF$$P50$$Ginformaworld$$H</linktopdf><linktohtml>$$Uhttps://www.tandfonline.com/doi/full/10.1081/DDC-120018639$$EHTML$$P50$$Ginformaworld$$H</linktohtml><link.rule.ids>314,776,780,27903,27904,59623,59729,60412,60518,61197,61232,61378,61413</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=14788368$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/12779280$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Kang, Lisheng</creatorcontrib><creatorcontrib>Jun, H. W.</creatorcontrib><title>Formulation and Efficacy Studies of New Topical Anesthetic Creams</title><title>Drug development and industrial pharmacy</title><addtitle>Drug Dev Ind Pharm</addtitle><description>Abstract
Local anesthetics (lidocaine or tetracaine) spontaneously melted at 25°C when mixed with thymol and aqueous isopropyl alcohol solution (IPA) at proper ratios and formed novel two-phase melt systems (TMS). The TMS consisted of a homogeneous oil phase containing primarily a local anesthetic agent (lidocaine or tetracaine) and thymol, and a homogeneous aqueous phase containing primarily IPA and pH 9.2 buffer. The relationship between melting of the solid components and system composition was determined from the phase diagram obtained by a titration method. A select TMS of a local anesthetic agent (lidocaine or tetracaine) was directly emulsified to prepare an O W cream and tested for the anesthetic efficacy on intact human skin. While both lidocaine (6%) and tetracaine (4%) creams were highly effective for dermal anesthesia with a similar onset time, the tetracaine cream exhibited a significantly longer duration of action than the lidocaine cream. An accelerated stability study indicated that lidocaine was significantly more stable than tetracaine in the creams.</description><subject>2-Propanol - chemistry</subject><subject>Administration, Cutaneous</subject><subject>Adult</subject><subject>Anesthetics, Local - administration & dosage</subject><subject>Anesthetics, Local - chemistry</subject><subject>Anesthetics, Local - pharmacology</subject><subject>Anesthetics. Neuromuscular blocking agents</subject><subject>Biological and medical sciences</subject><subject>Drug Compounding</subject><subject>Drug Stability</subject><subject>Efficacy</subject><subject>Female</subject><subject>General pharmacology</subject><subject>Humans</subject><subject>Lidocaine</subject><subject>Lidocaine - administration & dosage</subject><subject>Lidocaine - chemistry</subject><subject>Lidocaine - pharmacology</subject><subject>Local anesthetic</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Middle Aged</subject><subject>Neuropharmacology</subject><subject>Ointments</subject><subject>Particle Size</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Skin - drug effects</subject><subject>Solutions</subject><subject>Tetracaine</subject><subject>Tetracaine - administration & dosage</subject><subject>Tetracaine - chemistry</subject><subject>Tetracaine - pharmacology</subject><subject>Thymol - chemistry</subject><subject>Topical</subject><subject>Two-phase melt system</subject><subject>Viscosity</subject><issn>0363-9045</issn><issn>1520-5762</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2003</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp10M9LwzAUwPEgis7p0av0ordqfjbpccyfIHpwnsNrmrBK28ykZey_N7KpePAUCJ_3eHwROiP4imBFrm9u5jmhGBNVsHIPTYigOBeyoPtoglnB8hJzcYSOY3xPiJZCHKIjQqUsqcITNLvzoRtbGBrfZ9DX2a1zjQGzyV6HsW5szLzLnu06W_hV-m-zWW_jsLRDY7J5sNDFE3TgoI32dPdO0dvd7WL-kD-93D_OZ0-54UoMORektI4wJ3hdKkpLwituBCPOCM6AK1oZSWteGWfKSggiJLMAQhjioGCYTdHldu8q-I8xHaG7JhrbttBbP0YtGVOUFzLBfAtN8DEG6_QqNB2EjSZYfzXTqZn-aZb8-W7xWHW2_tW7SAlc7ADElMAF6E0Tfx2XSrFCJae2ruldqgprH9paD7BpffgeYv_dIP-MLi20w9JAsPrdj6FPYf-5_hM1wZbE</recordid><startdate>20030101</startdate><enddate>20030101</enddate><creator>Kang, Lisheng</creator><creator>Jun, H. W.</creator><general>Informa UK Ltd</general><general>Taylor & Francis</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>20030101</creationdate><title>Formulation and Efficacy Studies of New Topical Anesthetic Creams</title><author>Kang, Lisheng ; Jun, H. W.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c485t-4519ef13f54d9822914b4c531fc543a482bc72d4bcfc9b551573eaa55c1fa6303</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2003</creationdate><topic>2-Propanol - chemistry</topic><topic>Administration, Cutaneous</topic><topic>Adult</topic><topic>Anesthetics, Local - administration & dosage</topic><topic>Anesthetics, Local - chemistry</topic><topic>Anesthetics, Local - pharmacology</topic><topic>Anesthetics. Neuromuscular blocking agents</topic><topic>Biological and medical sciences</topic><topic>Drug Compounding</topic><topic>Drug Stability</topic><topic>Efficacy</topic><topic>Female</topic><topic>General pharmacology</topic><topic>Humans</topic><topic>Lidocaine</topic><topic>Lidocaine - administration & dosage</topic><topic>Lidocaine - chemistry</topic><topic>Lidocaine - pharmacology</topic><topic>Local anesthetic</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Middle Aged</topic><topic>Neuropharmacology</topic><topic>Ointments</topic><topic>Particle Size</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Skin - drug effects</topic><topic>Solutions</topic><topic>Tetracaine</topic><topic>Tetracaine - administration & dosage</topic><topic>Tetracaine - chemistry</topic><topic>Tetracaine - pharmacology</topic><topic>Thymol - chemistry</topic><topic>Topical</topic><topic>Two-phase melt system</topic><topic>Viscosity</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Kang, Lisheng</creatorcontrib><creatorcontrib>Jun, H. 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>Drug development and industrial pharmacy</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Kang, Lisheng</au><au>Jun, H. W.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Formulation and Efficacy Studies of New Topical Anesthetic Creams</atitle><jtitle>Drug development and industrial pharmacy</jtitle><addtitle>Drug Dev Ind Pharm</addtitle><date>2003-01-01</date><risdate>2003</risdate><volume>29</volume><issue>5</issue><spage>505</spage><epage>512</epage><pages>505-512</pages><issn>0363-9045</issn><eissn>1520-5762</eissn><abstract>Abstract
Local anesthetics (lidocaine or tetracaine) spontaneously melted at 25°C when mixed with thymol and aqueous isopropyl alcohol solution (IPA) at proper ratios and formed novel two-phase melt systems (TMS). The TMS consisted of a homogeneous oil phase containing primarily a local anesthetic agent (lidocaine or tetracaine) and thymol, and a homogeneous aqueous phase containing primarily IPA and pH 9.2 buffer. The relationship between melting of the solid components and system composition was determined from the phase diagram obtained by a titration method. A select TMS of a local anesthetic agent (lidocaine or tetracaine) was directly emulsified to prepare an O W cream and tested for the anesthetic efficacy on intact human skin. While both lidocaine (6%) and tetracaine (4%) creams were highly effective for dermal anesthesia with a similar onset time, the tetracaine cream exhibited a significantly longer duration of action than the lidocaine cream. An accelerated stability study indicated that lidocaine was significantly more stable than tetracaine in the creams.</abstract><cop>Colchester</cop><pub>Informa UK Ltd</pub><pmid>12779280</pmid><doi>10.1081/DDC-120018639</doi><tpages>8</tpages></addata></record> |
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subjects | 2-Propanol - chemistry Administration, Cutaneous Adult Anesthetics, Local - administration & dosage Anesthetics, Local - chemistry Anesthetics, Local - pharmacology Anesthetics. Neuromuscular blocking agents Biological and medical sciences Drug Compounding Drug Stability Efficacy Female General pharmacology Humans Lidocaine Lidocaine - administration & dosage Lidocaine - chemistry Lidocaine - pharmacology Local anesthetic Male Medical sciences Middle Aged Neuropharmacology Ointments Particle Size Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Skin - drug effects Solutions Tetracaine Tetracaine - administration & dosage Tetracaine - chemistry Tetracaine - pharmacology Thymol - chemistry Topical Two-phase melt system Viscosity |
title | Formulation and Efficacy Studies of New Topical Anesthetic Creams |
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