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rdf:type |
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lifeskim:mentions |
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pubmed:issue |
4-5
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pubmed:dateCreated |
2008-4-8
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pubmed:abstractText |
6-Beta-naltrexol is the major active metabolite of naltrexone, NTX, a potent mu-opioid receptor antagonist used in the treatment of alcohol dependence and opioid abuse. Compared to naloxone, NTX has a longer duration of action largely attributed to 6-beta-naltrexol. This study was carried out in order to determine percutaneous absorption of a transdermal codrug of naltrexol, 6-beta-naltrexol-hydroxybupropion codrug (CB-NTXOL-BUPOH), in hairless guinea pigs as well as to evaluate the safety of 6-beta-naltrexol for development as a transdermal dosage form. This codrug may be useful in the simultaneous treatment of alcohol dependence and tobacco addiction. The carbonate codrug traversed the skin at a faster rate than 6-beta-naltrexol. 6-Beta-naltrexol equivalent steady state plasma concentrations of 6.4 ng/ml were obtained after application of the codrug as compared to 1.2 ng/ml from 6-beta-naltrexol base. The steady state plasma concentration of hydroxybupropion after codrug application was 6.9 ng/ml. Skin sensitization and irritation tested in the hairless guinea pigs using the Buehler method revealed that 6-beta-naltrexol had no skin sensitizing potential. The method was validated with a known sensitizer, p-phenylenediamine, which induced sensitization in 90% of the animals. 6-beta-Naltrexol caused only mild transient skin irritation after the initial application of the patch. During subsequent applications, erythema was slightly increased but no skin damage was observed. In conclusion, a transdermal codrug of 6-beta-naltrexol could be a viable alternative treatment for alcohol and opiate abuse.
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pubmed:grant |
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pubmed:commentsCorrections |
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-10518654,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-10731624,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-10743909,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-10859147,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-10913750,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-11003204,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-11403727,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-11500258,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-12426011,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-12495797,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-1345133,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-14237604,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-15716384,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-15990301,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-16052561,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-16574034,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-16750868,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-16798000,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-3247326,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-512881,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-6018244,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-6406469,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-6469932,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-702273,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-7637475,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-7861416,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-8132183,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-9283509,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-954353,
http://linkedlifedata.com/resource/pubmed/commentcorrection/18321686-9839147
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pubmed:language |
eng
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pubmed:journal |
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pubmed:citationSubset |
IM
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pubmed:chemical |
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pubmed:status |
MEDLINE
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pubmed:month |
Apr
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pubmed:issn |
0928-0987
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pubmed:author |
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pubmed:issnType |
Print
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pubmed:day |
23
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pubmed:volume |
33
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pubmed:owner |
NLM
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pubmed:authorsComplete |
Y
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pubmed:pagination |
371-9
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pubmed:dateRevised |
2011-9-26
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pubmed:meshHeading |
pubmed-meshheading:18321686-Administration, Cutaneous,
pubmed-meshheading:18321686-Alcohol-Related Disorders,
pubmed-meshheading:18321686-Animals,
pubmed-meshheading:18321686-Bupropion,
pubmed-meshheading:18321686-Chromatography, High Pressure Liquid,
pubmed-meshheading:18321686-Drug Delivery Systems,
pubmed-meshheading:18321686-Female,
pubmed-meshheading:18321686-Guinea Pigs,
pubmed-meshheading:18321686-Male,
pubmed-meshheading:18321686-Mass Spectrometry,
pubmed-meshheading:18321686-Molecular Structure,
pubmed-meshheading:18321686-Naltrexone,
pubmed-meshheading:18321686-Prodrugs,
pubmed-meshheading:18321686-Skin,
pubmed-meshheading:18321686-Skin Absorption,
pubmed-meshheading:18321686-Skin Irritancy Tests,
pubmed-meshheading:18321686-Smoking Cessation
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pubmed:year |
2008
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pubmed:articleTitle |
In vivo evaluation of a transdermal codrug of 6-beta-naltrexol linked to hydroxybupropion in hairless guinea pigs.
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pubmed:affiliation |
Department of Pharmaceutical Sciences, College of Pharmacy, University of Kentucky, 725 Rose Street, Lexington, KY 40536-0082, USA.
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pubmed:publicationType |
Journal Article,
Research Support, N.I.H., Extramural
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