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...

Ausführliche Beschreibung

Gespeichert in:
Bibliographische Detailangaben
Veröffentlicht in:Drug development and industrial pharmacy 2003-01, Vol.29 (5), p.505-512
Hauptverfasser: Kang, Lisheng, Jun, H. W.
Format: Artikel
Sprache:eng
Schlagworte:
Online-Zugang:Volltext
Tags: Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
container_end_page 512
container_issue 5
container_start_page 505
container_title Drug development and industrial pharmacy
container_volume 29
creator Kang, Lisheng
Jun, H. W.
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
format Article
fullrecord <record><control><sourceid>proquest_pubme</sourceid><recordid>TN_cdi_pubmed_primary_12779280</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>73382467</sourcerecordid><originalsourceid>FETCH-LOGICAL-c485t-4519ef13f54d9822914b4c531fc543a482bc72d4bcfc9b551573eaa55c1fa6303</originalsourceid><addsrcrecordid>eNp10M9LwzAUwPEgis7p0av0ordqfjbpccyfIHpwnsNrmrBK28ykZey_N7KpePAUCJ_3eHwROiP4imBFrm9u5jmhGBNVsHIPTYigOBeyoPtoglnB8hJzcYSOY3xPiJZCHKIjQqUsqcITNLvzoRtbGBrfZ9DX2a1zjQGzyV6HsW5szLzLnu06W_hV-m-zWW_jsLRDY7J5sNDFE3TgoI32dPdO0dvd7WL-kD-93D_OZ0-54UoMORektI4wJ3hdKkpLwituBCPOCM6AK1oZSWteGWfKSggiJLMAQhjioGCYTdHldu8q-I8xHaG7JhrbttBbP0YtGVOUFzLBfAtN8DEG6_QqNB2EjSZYfzXTqZn-aZb8-W7xWHW2_tW7SAlc7ADElMAF6E0Tfx2XSrFCJae2ruldqgprH9paD7BpffgeYv_dIP-MLi20w9JAsPrdj6FPYf-5_hM1wZbE</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>73382467</pqid></control><display><type>article</type><title>Formulation and Efficacy Studies of New Topical Anesthetic Creams</title><source>MEDLINE</source><source>Business Source Complete</source><source>Taylor &amp; Francis Medical Library - CRKN</source><source>Taylor &amp; Francis Journals Complete</source><creator>Kang, Lisheng ; Jun, H. W.</creator><creatorcontrib>Kang, Lisheng ; Jun, H. W.</creatorcontrib><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><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 &amp; 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 &amp; 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 &amp; 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&amp;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 &amp; 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 &amp; 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 &amp; 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 &amp; 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 &amp; 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 &amp; 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 &amp; 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>
fulltext fulltext
identifier ISSN: 0363-9045
ispartof Drug development and industrial pharmacy, 2003-01, Vol.29 (5), p.505-512
issn 0363-9045
1520-5762
language eng
recordid cdi_pubmed_primary_12779280
source MEDLINE; Business Source Complete; Taylor & Francis Medical Library - CRKN; Taylor & Francis Journals Complete
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
url https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-25T00%3A15%3A06IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_pubme&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=Formulation%20and%20Efficacy%20Studies%20of%20New%20Topical%20Anesthetic%20Creams&rft.jtitle=Drug%20development%20and%20industrial%20pharmacy&rft.au=Kang,%20Lisheng&rft.date=2003-01-01&rft.volume=29&rft.issue=5&rft.spage=505&rft.epage=512&rft.pages=505-512&rft.issn=0363-9045&rft.eissn=1520-5762&rft_id=info:doi/10.1081/DDC-120018639&rft_dat=%3Cproquest_pubme%3E73382467%3C/proquest_pubme%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=73382467&rft_id=info:pmid/12779280&rfr_iscdi=true