Bioavailability of Intranasal Scopolamine in Normal Subjects
The bioavailability of scopolamine in three dosage forms was compared in 12 healthy nonsmoking male volunteers. Subjects received 0.4-mg doses of scopolamine bromide in intravenous (IV), intranasal (IN), or oral (PO) dosage forms on three occasions, with at least 2weeks separating the doses. Scopola...
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| Veröffentlicht in: | Journal of pharmaceutical sciences 1996-08, Vol.85 (8), p.899-902 |
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| container_title | Journal of pharmaceutical sciences |
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| creator | Putcha, Lakshmi Tietze, Karen J. Bourne, David W.A. Parise, Cecelia M. Hunter, Robert P. Cintrón, Nitza M. |
| description | The bioavailability of scopolamine in three dosage forms was compared in 12 healthy nonsmoking male volunteers. Subjects received 0.4-mg doses of scopolamine bromide in intravenous (IV), intranasal (IN), or oral (PO) dosage forms on three occasions, with at least 2weeks separating the doses. Scopolamine concentrations in plasma were determined with a combined reverse-phase liquid chromatographic–radioreceptor binding assay. Saliva volume and flow rate and percent suppression of control flow rate were determined from each sample. Absorption after IN and PO scopolamine administration was rapid; plasma concentrations [1680 (IN) and 164pg/mL (PO)] peaked within 1h of dosing [0.37 (IN) and 0.78h (PO)], respectively. IN and IV scopolamine suppressed salivary flow rate to similar extents (95% and 99.7%), respectively. Times to reach maximum effect were 1.05 and 0.27h after IN and IV dosage, respectively. Absolute intranasal bioavailability, calculated from the area under the drug concentration vs time curve, was found to be significantly greater than that of PO scopolamine (83% vs 3.7%, p |
| doi_str_mv | 10.1021/js950327b |
| format | Article |
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Subjects received 0.4-mg doses of scopolamine bromide in intravenous (IV), intranasal (IN), or oral (PO) dosage forms on three occasions, with at least 2weeks separating the doses. Scopolamine concentrations in plasma were determined with a combined reverse-phase liquid chromatographic–radioreceptor binding assay. Saliva volume and flow rate and percent suppression of control flow rate were determined from each sample. Absorption after IN and PO scopolamine administration was rapid; plasma concentrations [1680 (IN) and 164pg/mL (PO)] peaked within 1h of dosing [0.37 (IN) and 0.78h (PO)], respectively. IN and IV scopolamine suppressed salivary flow rate to similar extents (95% and 99.7%), respectively. Times to reach maximum effect were 1.05 and 0.27h after IN and IV dosage, respectively. Absolute intranasal bioavailability, calculated from the area under the drug concentration vs time curve, was found to be significantly greater than that of PO scopolamine (83% vs 3.7%, p<0.05). The IN route may provide a noninvasive, reliable, fast, and effective route for administering scopolamine.</description><identifier>ISSN: 0022-3549</identifier><identifier>EISSN: 1520-6017</identifier><identifier>DOI: 10.1021/js950327b</identifier><identifier>PMID: 8863287</identifier><identifier>CODEN: JPMSAE</identifier><language>eng</language><publisher>New York: Elsevier Inc</publisher><subject>Administration, Intranasal ; Adolescent ; Adult ; Biological and medical sciences ; Biological Availability ; Cholinergic Antagonists - administration & dosage ; Cholinergic Antagonists - blood ; Cholinergic Antagonists - pharmacokinetics ; Digestive system ; Humans ; Male ; Medical sciences ; Pharmacology. Drug treatments ; Reference Values ; Saliva - secretion ; Scopolamine Hydrobromide - administration & dosage ; Scopolamine Hydrobromide - blood ; Scopolamine Hydrobromide - pharmacokinetics ; Space life sciences</subject><ispartof>Journal of pharmaceutical sciences, 1996-08, Vol.85 (8), p.899-902</ispartof><rights>1996 Wiley-Liss, Inc., A Wiley Company</rights><rights>Copyright © 1996 Wiley‐Liss, Inc. and the American Pharmaceutical Association</rights><rights>1996 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://onlinelibrary.wiley.com/doi/pdf/10.1021%2Fjs950327b$$EPDF$$P50$$Gwiley$$H</linktopdf><linktohtml>$$Uhttps://onlinelibrary.wiley.com/doi/full/10.1021%2Fjs950327b$$EHTML$$P50$$Gwiley$$H</linktohtml><link.rule.ids>314,776,780,1411,27901,27902,45550,45551</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=3187929$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/8863287$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Putcha, Lakshmi</creatorcontrib><creatorcontrib>Tietze, Karen J.</creatorcontrib><creatorcontrib>Bourne, David W.A.</creatorcontrib><creatorcontrib>Parise, Cecelia M.</creatorcontrib><creatorcontrib>Hunter, Robert P.</creatorcontrib><creatorcontrib>Cintrón, Nitza M.</creatorcontrib><title>Bioavailability of Intranasal Scopolamine in Normal Subjects</title><title>Journal of pharmaceutical sciences</title><addtitle>J. Pharm. Sci</addtitle><description>The bioavailability of scopolamine in three dosage forms was compared in 12 healthy nonsmoking male volunteers. Subjects received 0.4-mg doses of scopolamine bromide in intravenous (IV), intranasal (IN), or oral (PO) dosage forms on three occasions, with at least 2weeks separating the doses. Scopolamine concentrations in plasma were determined with a combined reverse-phase liquid chromatographic–radioreceptor binding assay. Saliva volume and flow rate and percent suppression of control flow rate were determined from each sample. Absorption after IN and PO scopolamine administration was rapid; plasma concentrations [1680 (IN) and 164pg/mL (PO)] peaked within 1h of dosing [0.37 (IN) and 0.78h (PO)], respectively. IN and IV scopolamine suppressed salivary flow rate to similar extents (95% and 99.7%), respectively. Times to reach maximum effect were 1.05 and 0.27h after IN and IV dosage, respectively. Absolute intranasal bioavailability, calculated from the area under the drug concentration vs time curve, was found to be significantly greater than that of PO scopolamine (83% vs 3.7%, p<0.05). The IN route may provide a noninvasive, reliable, fast, and effective route for administering scopolamine.</description><subject>Administration, Intranasal</subject><subject>Adolescent</subject><subject>Adult</subject><subject>Biological and medical sciences</subject><subject>Biological Availability</subject><subject>Cholinergic Antagonists - administration & dosage</subject><subject>Cholinergic Antagonists - blood</subject><subject>Cholinergic Antagonists - pharmacokinetics</subject><subject>Digestive system</subject><subject>Humans</subject><subject>Male</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Reference Values</subject><subject>Saliva - secretion</subject><subject>Scopolamine Hydrobromide - administration & dosage</subject><subject>Scopolamine Hydrobromide - blood</subject><subject>Scopolamine Hydrobromide - pharmacokinetics</subject><subject>Space life sciences</subject><issn>0022-3549</issn><issn>1520-6017</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1996</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNplkE1P20AQhlcViAbooT-gkg-IE6b7vWuJC0SQUlFaNUUcV-P1WNp0bQevQ8m_r6NEuXAaad5H82oeQj4zeskoZ18XqVBUcFN-IBOmOM01ZeaATCjlPBdKFh_JcUoLSqmmSh2RI2u14NZMyNVN6OAVQoQyxDCss67O7tuhhxYSxGzuu2UXoQktZqHNHru-2WxX5QL9kE7JYQ0x4afdPCFPd7d_pt_yh5-z--n1Q45jt8hZiaoqkFMqtTFKMaattOALZlFKzQTXknuvKIdC-6K0lURQNUqolUKvxAk5395d9t3LCtPgmpA8xggtdqvkjJVSKSNG8MsOXJUNVm7Zhwb6tdu9O-ZnuxySh1iPb_qQ9phg1hS8GLGLLfYvRFzvY0bdxrbb23bff835pjXf4iEN-LbHof_rtBFGuefHmZsb8Zv_mFG34cWWx9HZa8DeJR-w9ViFftTqqi687xL_AdPaj7I</recordid><startdate>199608</startdate><enddate>199608</enddate><creator>Putcha, Lakshmi</creator><creator>Tietze, Karen J.</creator><creator>Bourne, David W.A.</creator><creator>Parise, Cecelia M.</creator><creator>Hunter, Robert P.</creator><creator>Cintrón, Nitza M.</creator><general>Elsevier Inc</general><general>John Wiley & Sons, Inc</general><general>Wiley</general><general>American Pharmaceutical Association</general><scope>BSCLL</scope><scope>IQODW</scope><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>7X8</scope></search><sort><creationdate>199608</creationdate><title>Bioavailability of Intranasal Scopolamine in Normal Subjects</title><author>Putcha, Lakshmi ; Tietze, Karen J. ; Bourne, David W.A. ; Parise, Cecelia M. ; Hunter, Robert P. ; Cintrón, Nitza M.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-e3543-1be5d9e200467755116848ac918e446132642cc502a96c9b8d4ea5fe4af55ec53</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1996</creationdate><topic>Administration, Intranasal</topic><topic>Adolescent</topic><topic>Adult</topic><topic>Biological and medical sciences</topic><topic>Biological Availability</topic><topic>Cholinergic Antagonists - administration & dosage</topic><topic>Cholinergic Antagonists - blood</topic><topic>Cholinergic Antagonists - pharmacokinetics</topic><topic>Digestive system</topic><topic>Humans</topic><topic>Male</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Reference Values</topic><topic>Saliva - secretion</topic><topic>Scopolamine Hydrobromide - administration & dosage</topic><topic>Scopolamine Hydrobromide - blood</topic><topic>Scopolamine Hydrobromide - pharmacokinetics</topic><topic>Space life sciences</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Putcha, Lakshmi</creatorcontrib><creatorcontrib>Tietze, Karen J.</creatorcontrib><creatorcontrib>Bourne, David W.A.</creatorcontrib><creatorcontrib>Parise, Cecelia M.</creatorcontrib><creatorcontrib>Hunter, Robert P.</creatorcontrib><creatorcontrib>Cintrón, Nitza M.</creatorcontrib><collection>Istex</collection><collection>Pascal-Francis</collection><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>MEDLINE - Academic</collection><jtitle>Journal of pharmaceutical sciences</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Putcha, Lakshmi</au><au>Tietze, Karen J.</au><au>Bourne, David W.A.</au><au>Parise, Cecelia M.</au><au>Hunter, Robert P.</au><au>Cintrón, Nitza M.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Bioavailability of Intranasal Scopolamine in Normal Subjects</atitle><jtitle>Journal of pharmaceutical sciences</jtitle><addtitle>J. Pharm. Sci</addtitle><date>1996-08</date><risdate>1996</risdate><volume>85</volume><issue>8</issue><spage>899</spage><epage>902</epage><pages>899-902</pages><issn>0022-3549</issn><eissn>1520-6017</eissn><coden>JPMSAE</coden><abstract>The bioavailability of scopolamine in three dosage forms was compared in 12 healthy nonsmoking male volunteers. Subjects received 0.4-mg doses of scopolamine bromide in intravenous (IV), intranasal (IN), or oral (PO) dosage forms on three occasions, with at least 2weeks separating the doses. Scopolamine concentrations in plasma were determined with a combined reverse-phase liquid chromatographic–radioreceptor binding assay. Saliva volume and flow rate and percent suppression of control flow rate were determined from each sample. Absorption after IN and PO scopolamine administration was rapid; plasma concentrations [1680 (IN) and 164pg/mL (PO)] peaked within 1h of dosing [0.37 (IN) and 0.78h (PO)], respectively. IN and IV scopolamine suppressed salivary flow rate to similar extents (95% and 99.7%), respectively. Times to reach maximum effect were 1.05 and 0.27h after IN and IV dosage, respectively. Absolute intranasal bioavailability, calculated from the area under the drug concentration vs time curve, was found to be significantly greater than that of PO scopolamine (83% vs 3.7%, p<0.05). The IN route may provide a noninvasive, reliable, fast, and effective route for administering scopolamine.</abstract><cop>New York</cop><pub>Elsevier Inc</pub><pmid>8863287</pmid><doi>10.1021/js950327b</doi><tpages>4</tpages></addata></record> |
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| subjects | Administration, Intranasal Adolescent Adult Biological and medical sciences Biological Availability Cholinergic Antagonists - administration & dosage Cholinergic Antagonists - blood Cholinergic Antagonists - pharmacokinetics Digestive system Humans Male Medical sciences Pharmacology. Drug treatments Reference Values Saliva - secretion Scopolamine Hydrobromide - administration & dosage Scopolamine Hydrobromide - blood Scopolamine Hydrobromide - pharmacokinetics Space life sciences |
| title | Bioavailability of Intranasal Scopolamine in Normal Subjects |
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