Investigation of the Bioavailability of WR-158,122
The purpose of the work performed on this contract was to prepare formulations designed to improve the oral bioavailability of the potent antimalarial, 2,4-diamino-6-(2-naphthylsulfonyl)quinazoline (WR-158,122). During the first six months of the program formulations of the drug were prepared with w...
Gespeichert in:
| Hauptverfasser: | , , , , |
|---|---|
| Format: | Report |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext bestellen |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | |
|---|---|
| container_issue | |
| container_start_page | |
| container_title | |
| container_volume | |
| creator | Granchelli,Felix E Yesair,David W Chadwick,Majory Braun,James W Rachwall,Peter C |
| description | The purpose of the work performed on this contract was to prepare formulations designed to improve the oral bioavailability of the potent antimalarial, 2,4-diamino-6-(2-naphthylsulfonyl)quinazoline (WR-158,122). During the first six months of the program formulations of the drug were prepared with water soluble excipients such as polyethylene glycols, polyvinyl pyrrolidone, sugars and citric acid. In addition, water soluble derivatives of the drug were prepared in an attempt to improve its in vivo rate of dissolution. A protocol was developed for determining the bioavailability of various formulations using WR-158,122-2-14C. In those studies where unlabelled WR-158,122 was orally administered, plasma was analyzed for drug equivalents using a fluorospectrophotometric assay. A corn oil-in-water emulsion of WR-158,122 was administered p.o. to rats and beagle dogs. In addition, substantive progress has been made in the preparation of solid dosage forms using water soluble polymers to encapsulate corn oil and the drug.
See also report dated Oct 74, AD/A004 186. |
| format | Report |
| fullrecord | <record><control><sourceid>dtic_1RU</sourceid><recordid>TN_cdi_dtic_stinet_ADA013528</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><sourcerecordid>ADA013528</sourcerecordid><originalsourceid>FETCH-dtic_stinet_ADA0135283</originalsourceid><addsrcrecordid>eNrjZDDyzCtLLS7JTE8syczPU8hPUyjJSFVwysxPLEvMzElMyszJLKkECYcH6RqaWugYGhnxMLCmJeYUp_JCaW4GGTfXEGcP3ZSSzOR4oFl5qSXxji6OBobGpkYWxgSkAYsEJ3Q</addsrcrecordid><sourcetype>Open Access Repository</sourcetype><iscdi>true</iscdi><recordtype>report</recordtype></control><display><type>report</type><title>Investigation of the Bioavailability of WR-158,122</title><source>DTIC Technical Reports</source><creator>Granchelli,Felix E ; Yesair,David W ; Chadwick,Majory ; Braun,James W ; Rachwall,Peter C</creator><creatorcontrib>Granchelli,Felix E ; Yesair,David W ; Chadwick,Majory ; Braun,James W ; Rachwall,Peter C ; LITTLE (ARTHUR D) INC CAMBRIDGE MASS</creatorcontrib><description>The purpose of the work performed on this contract was to prepare formulations designed to improve the oral bioavailability of the potent antimalarial, 2,4-diamino-6-(2-naphthylsulfonyl)quinazoline (WR-158,122). During the first six months of the program formulations of the drug were prepared with water soluble excipients such as polyethylene glycols, polyvinyl pyrrolidone, sugars and citric acid. In addition, water soluble derivatives of the drug were prepared in an attempt to improve its in vivo rate of dissolution. A protocol was developed for determining the bioavailability of various formulations using WR-158,122-2-14C. In those studies where unlabelled WR-158,122 was orally administered, plasma was analyzed for drug equivalents using a fluorospectrophotometric assay. A corn oil-in-water emulsion of WR-158,122 was administered p.o. to rats and beagle dogs. In addition, substantive progress has been made in the preparation of solid dosage forms using water soluble polymers to encapsulate corn oil and the drug.
See also report dated Oct 74, AD/A004 186.</description><language>eng</language><subject>ANTIMALARIALS ; BIOLOGICAL ABSORPTION ; DOSAGE ; Dosage forms ; DRUGS ; FORMULATIONS ; INGESTION(PHYSIOLOGY) ; NAPHTHALENES ; NITROGEN HETEROCYCLIC COMPOUNDS ; Pharmacology ; Quinazoline/diamino-naphthylsulfonyl ; SOLUBILITY</subject><creationdate>1975</creationdate><rights>APPROVED FOR PUBLIC RELEASE</rights><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>230,780,885,27567,27568</link.rule.ids><linktorsrc>$$Uhttps://apps.dtic.mil/sti/citations/ADA013528$$EView_record_in_DTIC$$FView_record_in_$$GDTIC$$Hfree_for_read</linktorsrc></links><search><creatorcontrib>Granchelli,Felix E</creatorcontrib><creatorcontrib>Yesair,David W</creatorcontrib><creatorcontrib>Chadwick,Majory</creatorcontrib><creatorcontrib>Braun,James W</creatorcontrib><creatorcontrib>Rachwall,Peter C</creatorcontrib><creatorcontrib>LITTLE (ARTHUR D) INC CAMBRIDGE MASS</creatorcontrib><title>Investigation of the Bioavailability of WR-158,122</title><description>The purpose of the work performed on this contract was to prepare formulations designed to improve the oral bioavailability of the potent antimalarial, 2,4-diamino-6-(2-naphthylsulfonyl)quinazoline (WR-158,122). During the first six months of the program formulations of the drug were prepared with water soluble excipients such as polyethylene glycols, polyvinyl pyrrolidone, sugars and citric acid. In addition, water soluble derivatives of the drug were prepared in an attempt to improve its in vivo rate of dissolution. A protocol was developed for determining the bioavailability of various formulations using WR-158,122-2-14C. In those studies where unlabelled WR-158,122 was orally administered, plasma was analyzed for drug equivalents using a fluorospectrophotometric assay. A corn oil-in-water emulsion of WR-158,122 was administered p.o. to rats and beagle dogs. In addition, substantive progress has been made in the preparation of solid dosage forms using water soluble polymers to encapsulate corn oil and the drug.
See also report dated Oct 74, AD/A004 186.</description><subject>ANTIMALARIALS</subject><subject>BIOLOGICAL ABSORPTION</subject><subject>DOSAGE</subject><subject>Dosage forms</subject><subject>DRUGS</subject><subject>FORMULATIONS</subject><subject>INGESTION(PHYSIOLOGY)</subject><subject>NAPHTHALENES</subject><subject>NITROGEN HETEROCYCLIC COMPOUNDS</subject><subject>Pharmacology</subject><subject>Quinazoline/diamino-naphthylsulfonyl</subject><subject>SOLUBILITY</subject><fulltext>true</fulltext><rsrctype>report</rsrctype><creationdate>1975</creationdate><recordtype>report</recordtype><sourceid>1RU</sourceid><recordid>eNrjZDDyzCtLLS7JTE8syczPU8hPUyjJSFVwysxPLEvMzElMyszJLKkECYcH6RqaWugYGhnxMLCmJeYUp_JCaW4GGTfXEGcP3ZSSzOR4oFl5qSXxji6OBobGpkYWxgSkAYsEJ3Q</recordid><startdate>197503</startdate><enddate>197503</enddate><creator>Granchelli,Felix E</creator><creator>Yesair,David W</creator><creator>Chadwick,Majory</creator><creator>Braun,James W</creator><creator>Rachwall,Peter C</creator><scope>1RU</scope><scope>BHM</scope></search><sort><creationdate>197503</creationdate><title>Investigation of the Bioavailability of WR-158,122</title><author>Granchelli,Felix E ; Yesair,David W ; Chadwick,Majory ; Braun,James W ; Rachwall,Peter C</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-dtic_stinet_ADA0135283</frbrgroupid><rsrctype>reports</rsrctype><prefilter>reports</prefilter><language>eng</language><creationdate>1975</creationdate><topic>ANTIMALARIALS</topic><topic>BIOLOGICAL ABSORPTION</topic><topic>DOSAGE</topic><topic>Dosage forms</topic><topic>DRUGS</topic><topic>FORMULATIONS</topic><topic>INGESTION(PHYSIOLOGY)</topic><topic>NAPHTHALENES</topic><topic>NITROGEN HETEROCYCLIC COMPOUNDS</topic><topic>Pharmacology</topic><topic>Quinazoline/diamino-naphthylsulfonyl</topic><topic>SOLUBILITY</topic><toplevel>online_resources</toplevel><creatorcontrib>Granchelli,Felix E</creatorcontrib><creatorcontrib>Yesair,David W</creatorcontrib><creatorcontrib>Chadwick,Majory</creatorcontrib><creatorcontrib>Braun,James W</creatorcontrib><creatorcontrib>Rachwall,Peter C</creatorcontrib><creatorcontrib>LITTLE (ARTHUR D) INC CAMBRIDGE MASS</creatorcontrib><collection>DTIC Technical Reports</collection><collection>DTIC STINET</collection></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext_linktorsrc</fulltext></delivery><addata><au>Granchelli,Felix E</au><au>Yesair,David W</au><au>Chadwick,Majory</au><au>Braun,James W</au><au>Rachwall,Peter C</au><aucorp>LITTLE (ARTHUR D) INC CAMBRIDGE MASS</aucorp><format>book</format><genre>unknown</genre><ristype>RPRT</ristype><btitle>Investigation of the Bioavailability of WR-158,122</btitle><date>1975-03</date><risdate>1975</risdate><abstract>The purpose of the work performed on this contract was to prepare formulations designed to improve the oral bioavailability of the potent antimalarial, 2,4-diamino-6-(2-naphthylsulfonyl)quinazoline (WR-158,122). During the first six months of the program formulations of the drug were prepared with water soluble excipients such as polyethylene glycols, polyvinyl pyrrolidone, sugars and citric acid. In addition, water soluble derivatives of the drug were prepared in an attempt to improve its in vivo rate of dissolution. A protocol was developed for determining the bioavailability of various formulations using WR-158,122-2-14C. In those studies where unlabelled WR-158,122 was orally administered, plasma was analyzed for drug equivalents using a fluorospectrophotometric assay. A corn oil-in-water emulsion of WR-158,122 was administered p.o. to rats and beagle dogs. In addition, substantive progress has been made in the preparation of solid dosage forms using water soluble polymers to encapsulate corn oil and the drug.
See also report dated Oct 74, AD/A004 186.</abstract><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext_linktorsrc |
| identifier | |
| ispartof | |
| issn | |
| language | eng |
| recordid | cdi_dtic_stinet_ADA013528 |
| source | DTIC Technical Reports |
| subjects | ANTIMALARIALS BIOLOGICAL ABSORPTION DOSAGE Dosage forms DRUGS FORMULATIONS INGESTION(PHYSIOLOGY) NAPHTHALENES NITROGEN HETEROCYCLIC COMPOUNDS Pharmacology Quinazoline/diamino-naphthylsulfonyl SOLUBILITY |
| title | Investigation of the Bioavailability of WR-158,122 |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-01T20%3A07%3A37IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-dtic_1RU&rft_val_fmt=info:ofi/fmt:kev:mtx:book&rft.genre=unknown&rft.btitle=Investigation%20of%20the%20Bioavailability%20of%20WR-158,122&rft.au=Granchelli,Felix%20E&rft.aucorp=LITTLE%20(ARTHUR%20D)%20INC%20CAMBRIDGE%20MASS&rft.date=1975-03&rft_id=info:doi/&rft_dat=%3Cdtic_1RU%3EADA013528%3C/dtic_1RU%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_id=info:pmid/&rfr_iscdi=true |