Intranasal absorption of melatonin in vivo bioavailability study
The bioavailability of melatonin in rabbits after nasal administration of two formulations has been studied. In each case, a total amount of 1.5 mg melatonin in 50 μl was administered and compared with 1.5 mg i.v. The test solutions were formulated with 40% polyethylene glycol 300 (PEG 300), one wit...
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| Veröffentlicht in: | International journal of pharmaceutics 1999-05, Vol.182 (1), p.1-5 |
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| creator | Bechgaard, Erik Lindhardt, Karsten Martinsen, Lise |
| description | The bioavailability of melatonin in rabbits after nasal administration of two formulations has been studied. In each case, a total amount of 1.5 mg melatonin in 50 μl was administered and compared with 1.5 mg i.v. The test solutions were formulated with 40% polyethylene glycol 300 (PEG 300), one with 1% sodium glycocholate (+GC) and one without (−GC). The bioavailability for +GC was 94% (S.D.±29%,
n=4), whereas the bioavailability for −GC was 55% (S.D.±17%,
n=6). These results indicate that GC has an enhancer effect (
P |
| doi_str_mv | 10.1016/S0378-5173(99)00019-8 |
| format | Article |
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n=4), whereas the bioavailability for −GC was 55% (S.D.±17%,
n=6). These results indicate that GC has an enhancer effect (
P<0.05). However, the relatively high bioavailability without GC shows that it might not be necessary to use an enhancer for a clinical relevant formulation. The pharmacokinetics of melatonin could be described by a one-compartment model, and the serum half-life was about 13 min. The absorption rate for both formulations was very fast (
t
max=5 min) and
C
max mean was 493±290 ng/ml (
n=4) and 249±125 ng/ml (
n=6) for +GC and −GC, respectively.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/S0378-5173(99)00019-8</identifier><identifier>PMID: 10332069</identifier><identifier>CODEN: IJPHDE</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Absorption ; Administration, Intranasal ; Animals ; Antioxidants - administration & dosage ; Antioxidants - pharmacokinetics ; Bioavailability ; Biological and medical sciences ; Biological Availability ; Body Fluid Compartments ; Chromatography, High Pressure Liquid ; General pharmacology ; Half-Life ; Hormones. Endocrine system ; Injections, Intravenous ; Male ; Medical sciences ; Melatonin ; Melatonin - administration & dosage ; Melatonin - pharmacokinetics ; Nasal ; Nasal Mucosa - metabolism ; Pharmaceutical technology. Pharmaceutical industry ; Pharmaceutical Vehicles - pharmacology ; Pharmacology. Drug treatments ; Polyethylene glycol 300 ; Polyethylene Glycols - pharmacology ; Rabbit ; Rabbits ; Sodium glycocholate</subject><ispartof>International journal of pharmaceutics, 1999-05, Vol.182 (1), p.1-5</ispartof><rights>1999 Elsevier Science B.V.</rights><rights>1999 INIST-CNRS</rights><rights>Copyright.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c390t-7dc0f251cf74f7060a11a43bba462b60a887fc5c476e769fb613fa3894d1cad63</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0378517399000198$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1804271$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/10332069$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Bechgaard, Erik</creatorcontrib><creatorcontrib>Lindhardt, Karsten</creatorcontrib><creatorcontrib>Martinsen, Lise</creatorcontrib><title>Intranasal absorption of melatonin in vivo bioavailability study</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>The bioavailability of melatonin in rabbits after nasal administration of two formulations has been studied. In each case, a total amount of 1.5 mg melatonin in 50 μl was administered and compared with 1.5 mg i.v. The test solutions were formulated with 40% polyethylene glycol 300 (PEG 300), one with 1% sodium glycocholate (+GC) and one without (−GC). The bioavailability for +GC was 94% (S.D.±29%,
n=4), whereas the bioavailability for −GC was 55% (S.D.±17%,
n=6). These results indicate that GC has an enhancer effect (
P<0.05). However, the relatively high bioavailability without GC shows that it might not be necessary to use an enhancer for a clinical relevant formulation. The pharmacokinetics of melatonin could be described by a one-compartment model, and the serum half-life was about 13 min. The absorption rate for both formulations was very fast (
t
max=5 min) and
C
max mean was 493±290 ng/ml (
n=4) and 249±125 ng/ml (
n=6) for +GC and −GC, respectively.</description><subject>Absorption</subject><subject>Administration, Intranasal</subject><subject>Animals</subject><subject>Antioxidants - administration & dosage</subject><subject>Antioxidants - pharmacokinetics</subject><subject>Bioavailability</subject><subject>Biological and medical sciences</subject><subject>Biological Availability</subject><subject>Body Fluid Compartments</subject><subject>Chromatography, High Pressure Liquid</subject><subject>General pharmacology</subject><subject>Half-Life</subject><subject>Hormones. Endocrine system</subject><subject>Injections, Intravenous</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Melatonin</subject><subject>Melatonin - administration & dosage</subject><subject>Melatonin - pharmacokinetics</subject><subject>Nasal</subject><subject>Nasal Mucosa - metabolism</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmaceutical Vehicles - pharmacology</subject><subject>Pharmacology. Drug treatments</subject><subject>Polyethylene glycol 300</subject><subject>Polyethylene Glycols - pharmacology</subject><subject>Rabbit</subject><subject>Rabbits</subject><subject>Sodium glycocholate</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1999</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkEtLxDAQgIMo7vr4CUoPInqoJk2bNCeVxcfCggf1HKZpApFusyZtYf-92e2i3oSBYeCb14fQGcE3BBN2-4YpL9OCcHolxDXGmIi03ENTUnKa0pyzfTT9QSboKITPCLGM0EM0IZjSDDMxRffztvPQQoAmgSo4v-qsaxNnkqVuoHOtbZMYgx1cUlkHA9gGKtvYbp2Erq_XJ-jAQBP06S4fo4-nx_fZS7p4fZ7PHhapogJ3Ka8VNllBlOG54ZhhIARyWlWQs6yKZVlyowoVD9ecCVMxQg3QUuQ1UVAzeowux7kr7756HTq5tEHppoFWuz5IJjij8cEIFiOovAvBayNX3i7BryXBcqNObtXJjRcphNyqk2XsO98t6Kulrv90ja4icLEDIChoTNSmbPjlSpxnnETsbsR0tDFY7WVQVrdK19Zr1cna2X8u-QaAworm</recordid><startdate>19990510</startdate><enddate>19990510</enddate><creator>Bechgaard, Erik</creator><creator>Lindhardt, Karsten</creator><creator>Martinsen, Lise</creator><general>Elsevier B.V</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></search><sort><creationdate>19990510</creationdate><title>Intranasal absorption of melatonin in vivo bioavailability study</title><author>Bechgaard, Erik ; Lindhardt, Karsten ; Martinsen, Lise</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c390t-7dc0f251cf74f7060a11a43bba462b60a887fc5c476e769fb613fa3894d1cad63</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1999</creationdate><topic>Absorption</topic><topic>Administration, Intranasal</topic><topic>Animals</topic><topic>Antioxidants - administration & dosage</topic><topic>Antioxidants - pharmacokinetics</topic><topic>Bioavailability</topic><topic>Biological and medical sciences</topic><topic>Biological Availability</topic><topic>Body Fluid Compartments</topic><topic>Chromatography, High Pressure Liquid</topic><topic>General pharmacology</topic><topic>Half-Life</topic><topic>Hormones. Endocrine system</topic><topic>Injections, Intravenous</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Melatonin</topic><topic>Melatonin - administration & dosage</topic><topic>Melatonin - pharmacokinetics</topic><topic>Nasal</topic><topic>Nasal Mucosa - metabolism</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmaceutical Vehicles - pharmacology</topic><topic>Pharmacology. Drug treatments</topic><topic>Polyethylene glycol 300</topic><topic>Polyethylene Glycols - pharmacology</topic><topic>Rabbit</topic><topic>Rabbits</topic><topic>Sodium glycocholate</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Bechgaard, Erik</creatorcontrib><creatorcontrib>Lindhardt, Karsten</creatorcontrib><creatorcontrib>Martinsen, Lise</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>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Bechgaard, Erik</au><au>Lindhardt, Karsten</au><au>Martinsen, Lise</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Intranasal absorption of melatonin in vivo bioavailability study</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>1999-05-10</date><risdate>1999</risdate><volume>182</volume><issue>1</issue><spage>1</spage><epage>5</epage><pages>1-5</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><coden>IJPHDE</coden><abstract>The bioavailability of melatonin in rabbits after nasal administration of two formulations has been studied. In each case, a total amount of 1.5 mg melatonin in 50 μl was administered and compared with 1.5 mg i.v. The test solutions were formulated with 40% polyethylene glycol 300 (PEG 300), one with 1% sodium glycocholate (+GC) and one without (−GC). The bioavailability for +GC was 94% (S.D.±29%,
n=4), whereas the bioavailability for −GC was 55% (S.D.±17%,
n=6). These results indicate that GC has an enhancer effect (
P<0.05). However, the relatively high bioavailability without GC shows that it might not be necessary to use an enhancer for a clinical relevant formulation. The pharmacokinetics of melatonin could be described by a one-compartment model, and the serum half-life was about 13 min. The absorption rate for both formulations was very fast (
t
max=5 min) and
C
max mean was 493±290 ng/ml (
n=4) and 249±125 ng/ml (
n=6) for +GC and −GC, respectively.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>10332069</pmid><doi>10.1016/S0378-5173(99)00019-8</doi><tpages>5</tpages></addata></record> |
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| subjects | Absorption Administration, Intranasal Animals Antioxidants - administration & dosage Antioxidants - pharmacokinetics Bioavailability Biological and medical sciences Biological Availability Body Fluid Compartments Chromatography, High Pressure Liquid General pharmacology Half-Life Hormones. Endocrine system Injections, Intravenous Male Medical sciences Melatonin Melatonin - administration & dosage Melatonin - pharmacokinetics Nasal Nasal Mucosa - metabolism Pharmaceutical technology. Pharmaceutical industry Pharmaceutical Vehicles - pharmacology Pharmacology. Drug treatments Polyethylene glycol 300 Polyethylene Glycols - pharmacology Rabbit Rabbits Sodium glycocholate |
| title | Intranasal absorption of melatonin in vivo bioavailability study |
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