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Comparison of the solubility and pharmacokinetics of sildenafil salts
To develop sildenafil lactate, a salt form of sildenafil with improved solubility and bioavailability of poorly water-soluble sildenafil base, this salt form was prepared using a spray dryer. Its solubility and pharmacokinetics in rabbits were evaluated compared with sildenafil base and sildenafil c...
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| Published in: | Archives of pharmacal research 2011, 34(3), , pp.451-454 |
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| cited_by | cdi_FETCH-LOGICAL-c377t-2d7a371b2746ca029d6abfdab621ce9860820163dbd8a62364813590fef2ea9d3 |
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| cites | cdi_FETCH-LOGICAL-c377t-2d7a371b2746ca029d6abfdab621ce9860820163dbd8a62364813590fef2ea9d3 |
| container_end_page | 454 |
| container_issue | 3 |
| container_start_page | 451 |
| container_title | Archives of pharmacal research |
| container_volume | 34 |
| creator | Jung, Si-Young Seo, Youn-Gee Kim, Gun Kook Woo, Jong Soo Yong, Chul Soon Choi, Han-Gon |
| description | To develop sildenafil lactate, a salt form of sildenafil with improved solubility and bioavailability of poorly water-soluble sildenafil base, this salt form was prepared using a spray dryer. Its solubility and pharmacokinetics in rabbits were evaluated compared with sildenafil base and sildenafil citrate. Sildenafil lactate improved the solubility of sildenafil in various solvents including distilled water compared with sildenafil citrate. It provided higher AUC and C
max
and, shorter t
1/2
values than did the other materials, indicating that it improved the oral bioavailability of sildenafil in rabbits. Our results suggest that sildenafil lactate would be useful to deliver sildenafil in a pattern that allows fast absorption and late metabolism. Furthermore, the plasma concentration at 0.25 h in sildenafil lactate was similar to the C
max
value at T
max
(0.5 h) in sildenafil citrate. Thus, sildenafil lactate might provide a faster onset of action and immediate erection compared with sildenafil citrate, the conventional drug. |
| doi_str_mv | 10.1007/s12272-011-0313-y |
| format | article |
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max
and, shorter t
1/2
values than did the other materials, indicating that it improved the oral bioavailability of sildenafil in rabbits. Our results suggest that sildenafil lactate would be useful to deliver sildenafil in a pattern that allows fast absorption and late metabolism. Furthermore, the plasma concentration at 0.25 h in sildenafil lactate was similar to the C
max
value at T
max
(0.5 h) in sildenafil citrate. Thus, sildenafil lactate might provide a faster onset of action and immediate erection compared with sildenafil citrate, the conventional drug.</description><identifier>ISSN: 0253-6269</identifier><identifier>EISSN: 1976-3786</identifier><identifier>DOI: 10.1007/s12272-011-0313-y</identifier><identifier>PMID: 21547677</identifier><language>eng</language><publisher>Heidelberg: Pharmaceutical Society of Korea</publisher><subject>Administration, Oral ; Animals ; Area Under Curve ; Biological Availability ; Drug Compounding ; Erectile Dysfunction - drug therapy ; Male ; Medicine ; Pharmacology/Toxicology ; Pharmacy ; Piperazines - blood ; Piperazines - chemistry ; Piperazines - pharmacokinetics ; Piperazines - pharmacology ; Purines - blood ; Purines - chemistry ; Purines - pharmacokinetics ; Rabbits ; Sildenafil Citrate ; Solubility ; Structure-Activity Relationship ; Sulfones - blood ; Sulfones - chemistry ; Sulfones - pharmacokinetics ; Sulfones - pharmacology ; 약학</subject><ispartof>Archives of Pharmacal Research, 2011, 34(3), , pp.451-454</ispartof><rights>The Pharmaceutical Society of Korea and Springer Netherlands 2011</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c377t-2d7a371b2746ca029d6abfdab621ce9860820163dbd8a62364813590fef2ea9d3</citedby><cites>FETCH-LOGICAL-c377t-2d7a371b2746ca029d6abfdab621ce9860820163dbd8a62364813590fef2ea9d3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,776,780,27901,27902</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/21547677$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink><backlink>$$Uhttps://www.kci.go.kr/kciportal/ci/sereArticleSearch/ciSereArtiView.kci?sereArticleSearchBean.artiId=ART001537322$$DAccess content in National Research Foundation of Korea (NRF)$$Hfree_for_read</backlink></links><search><creatorcontrib>Jung, Si-Young</creatorcontrib><creatorcontrib>Seo, Youn-Gee</creatorcontrib><creatorcontrib>Kim, Gun Kook</creatorcontrib><creatorcontrib>Woo, Jong Soo</creatorcontrib><creatorcontrib>Yong, Chul Soon</creatorcontrib><creatorcontrib>Choi, Han-Gon</creatorcontrib><title>Comparison of the solubility and pharmacokinetics of sildenafil salts</title><title>Archives of pharmacal research</title><addtitle>Arch. Pharm. Res</addtitle><addtitle>Arch Pharm Res</addtitle><description>To develop sildenafil lactate, a salt form of sildenafil with improved solubility and bioavailability of poorly water-soluble sildenafil base, this salt form was prepared using a spray dryer. Its solubility and pharmacokinetics in rabbits were evaluated compared with sildenafil base and sildenafil citrate. Sildenafil lactate improved the solubility of sildenafil in various solvents including distilled water compared with sildenafil citrate. It provided higher AUC and C
max
and, shorter t
1/2
values than did the other materials, indicating that it improved the oral bioavailability of sildenafil in rabbits. Our results suggest that sildenafil lactate would be useful to deliver sildenafil in a pattern that allows fast absorption and late metabolism. Furthermore, the plasma concentration at 0.25 h in sildenafil lactate was similar to the C
max
value at T
max
(0.5 h) in sildenafil citrate. Thus, sildenafil lactate might provide a faster onset of action and immediate erection compared with sildenafil citrate, the conventional drug.</description><subject>Administration, Oral</subject><subject>Animals</subject><subject>Area Under Curve</subject><subject>Biological Availability</subject><subject>Drug Compounding</subject><subject>Erectile Dysfunction - drug therapy</subject><subject>Male</subject><subject>Medicine</subject><subject>Pharmacology/Toxicology</subject><subject>Pharmacy</subject><subject>Piperazines - blood</subject><subject>Piperazines - chemistry</subject><subject>Piperazines - pharmacokinetics</subject><subject>Piperazines - pharmacology</subject><subject>Purines - blood</subject><subject>Purines - chemistry</subject><subject>Purines - pharmacokinetics</subject><subject>Rabbits</subject><subject>Sildenafil Citrate</subject><subject>Solubility</subject><subject>Structure-Activity Relationship</subject><subject>Sulfones - blood</subject><subject>Sulfones - chemistry</subject><subject>Sulfones - pharmacokinetics</subject><subject>Sulfones - pharmacology</subject><subject>약학</subject><issn>0253-6269</issn><issn>1976-3786</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2011</creationdate><recordtype>article</recordtype><recordid>eNp9kL1OwzAYRS0EoqXwACwoG2Iw-LMTOxmrqvxIlZBQmS0ndlq3SVzsZMjbk5LCyHSHe-4dDkK3QB6BEPEUgFJBMQHAhAHD_RmaQiY4ZiLl52hKaMIwpzyboKsQdoQwniTJJZpQSGLBhZii5cLVB-VtcE3kyqjdmii4qsttZds-Uo2ODlvla1W4vW1Ma4twxIKttGlUaasoqKoN1-iiVFUwN6ecoc_n5XrxilfvL2-L-QoXTIgWUy0UE5BTEfNCEZpprvJSq5xTKEyWcpJSApzpXKeKU8bjFFiSkdKU1KhMsxl6GH8bX8p9YaVT9ic3Tu69nH-s3yQAE3FKB_Z-ZA_efXUmtLK2oTBVpRrjuiBTnkAGaUIGEkay8C4Eb0p58LZWvpdA5FG0HEXLQbQ8ipb9sLk7vXd5bfTf4tfsANARCEPVbIyXO9f5ZrDzz-s3w1OIpQ</recordid><startdate>20110301</startdate><enddate>20110301</enddate><creator>Jung, Si-Young</creator><creator>Seo, Youn-Gee</creator><creator>Kim, Gun Kook</creator><creator>Woo, Jong Soo</creator><creator>Yong, Chul Soon</creator><creator>Choi, Han-Gon</creator><general>Pharmaceutical Society of Korea</general><general>대한약학회</general><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><scope>ACYCR</scope></search><sort><creationdate>20110301</creationdate><title>Comparison of the solubility and pharmacokinetics of sildenafil salts</title><author>Jung, Si-Young ; Seo, Youn-Gee ; Kim, Gun Kook ; Woo, Jong Soo ; Yong, Chul Soon ; Choi, Han-Gon</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c377t-2d7a371b2746ca029d6abfdab621ce9860820163dbd8a62364813590fef2ea9d3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2011</creationdate><topic>Administration, Oral</topic><topic>Animals</topic><topic>Area Under Curve</topic><topic>Biological Availability</topic><topic>Drug Compounding</topic><topic>Erectile Dysfunction - drug therapy</topic><topic>Male</topic><topic>Medicine</topic><topic>Pharmacology/Toxicology</topic><topic>Pharmacy</topic><topic>Piperazines - blood</topic><topic>Piperazines - chemistry</topic><topic>Piperazines - pharmacokinetics</topic><topic>Piperazines - pharmacology</topic><topic>Purines - blood</topic><topic>Purines - chemistry</topic><topic>Purines - pharmacokinetics</topic><topic>Rabbits</topic><topic>Sildenafil Citrate</topic><topic>Solubility</topic><topic>Structure-Activity Relationship</topic><topic>Sulfones - blood</topic><topic>Sulfones - chemistry</topic><topic>Sulfones - pharmacokinetics</topic><topic>Sulfones - pharmacology</topic><topic>약학</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Jung, Si-Young</creatorcontrib><creatorcontrib>Seo, Youn-Gee</creatorcontrib><creatorcontrib>Kim, Gun Kook</creatorcontrib><creatorcontrib>Woo, Jong Soo</creatorcontrib><creatorcontrib>Yong, Chul Soon</creatorcontrib><creatorcontrib>Choi, Han-Gon</creatorcontrib><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><collection>Korean Citation Index</collection><jtitle>Archives of pharmacal research</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Jung, Si-Young</au><au>Seo, Youn-Gee</au><au>Kim, Gun Kook</au><au>Woo, Jong Soo</au><au>Yong, Chul Soon</au><au>Choi, Han-Gon</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Comparison of the solubility and pharmacokinetics of sildenafil salts</atitle><jtitle>Archives of pharmacal research</jtitle><stitle>Arch. Pharm. Res</stitle><addtitle>Arch Pharm Res</addtitle><date>2011-03-01</date><risdate>2011</risdate><volume>34</volume><issue>3</issue><spage>451</spage><epage>454</epage><pages>451-454</pages><issn>0253-6269</issn><eissn>1976-3786</eissn><abstract>To develop sildenafil lactate, a salt form of sildenafil with improved solubility and bioavailability of poorly water-soluble sildenafil base, this salt form was prepared using a spray dryer. Its solubility and pharmacokinetics in rabbits were evaluated compared with sildenafil base and sildenafil citrate. Sildenafil lactate improved the solubility of sildenafil in various solvents including distilled water compared with sildenafil citrate. It provided higher AUC and C
max
and, shorter t
1/2
values than did the other materials, indicating that it improved the oral bioavailability of sildenafil in rabbits. Our results suggest that sildenafil lactate would be useful to deliver sildenafil in a pattern that allows fast absorption and late metabolism. Furthermore, the plasma concentration at 0.25 h in sildenafil lactate was similar to the C
max
value at T
max
(0.5 h) in sildenafil citrate. Thus, sildenafil lactate might provide a faster onset of action and immediate erection compared with sildenafil citrate, the conventional drug.</abstract><cop>Heidelberg</cop><pub>Pharmaceutical Society of Korea</pub><pmid>21547677</pmid><doi>10.1007/s12272-011-0313-y</doi><tpages>4</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0253-6269 |
| ispartof | Archives of Pharmacal Research, 2011, 34(3), , pp.451-454 |
| issn | 0253-6269 1976-3786 |
| language | eng |
| recordid | cdi_nrf_kci_oai_kci_go_kr_ARTI_1137482 |
| source | Springer Nature |
| subjects | Administration, Oral Animals Area Under Curve Biological Availability Drug Compounding Erectile Dysfunction - drug therapy Male Medicine Pharmacology/Toxicology Pharmacy Piperazines - blood Piperazines - chemistry Piperazines - pharmacokinetics Piperazines - pharmacology Purines - blood Purines - chemistry Purines - pharmacokinetics Rabbits Sildenafil Citrate Solubility Structure-Activity Relationship Sulfones - blood Sulfones - chemistry Sulfones - pharmacokinetics Sulfones - pharmacology 약학 |
| title | Comparison of the solubility and pharmacokinetics of sildenafil salts |
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