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Improving Tenoxicam Solubility and Bioavailability by Cosolvent System
The formulation study of tenoxicam, a poorly water-soluble drug, was developed by use of a ternary cosolvent system and has significantly enhanced the solubility. Additionally, the relative bioavailability of testing formulation was also evaluated by New Zealand rabbit with a single i.m. injection....
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Published in: | AAPS PharmSciTech 2009, Vol.10 (1), p.166-171 |
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description | The formulation study of tenoxicam, a poorly water-soluble drug, was developed by use of a ternary cosolvent system and has significantly enhanced the solubility. Additionally, the relative bioavailability of testing formulation was also evaluated by New Zealand rabbit with a single i.m. injection. The three-phase diagram for dimethylsulfoxide (DMSO)/propylene glycol/water, DMSO/ethanol/water, and DMSO/polyethoxylated castor oil/ethanol system was developed. The volume ratio of 5:4:1 in the DMSO/polyethoxylated castor oil/ethanol system resulted in a more suitable vehicle than other systems, with a high solubility (20.73 mg/ml) and low viscosity (10.0 Cp). A pharmacokinetic study of bioequivalence (
F
rel
= 0.89) was also obtained. The present study not only provides a novel strategy improving tenoxicam solubility but also helps further scientific knowledge for the development of parenteral formulations. |
doi_str_mv | 10.1208/s12249-009-9189-2 |
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F
rel
= 0.89) was also obtained. The present study not only provides a novel strategy improving tenoxicam solubility but also helps further scientific knowledge for the development of parenteral formulations.</description><identifier>ISSN: 1530-9932</identifier><identifier>EISSN: 1530-9932</identifier><identifier>DOI: 10.1208/s12249-009-9189-2</identifier><identifier>PMID: 19224373</identifier><language>eng</language><publisher>Boston: Springer US</publisher><subject>Animals ; Anti-Inflammatory Agents, Non-Steroidal - administration & dosage ; Anti-Inflammatory Agents, Non-Steroidal - chemistry ; Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics ; Biochemistry ; Biological Availability ; Biomedical and Life Sciences ; Biomedicine ; Biotechnology ; Castor Oil - analogs & derivatives ; Castor Oil - chemistry ; Chemistry, Pharmaceutical ; Dimethyl Sulfoxide - chemistry ; Ethanol - chemistry ; Injections, Intramuscular ; Pharmacology/Toxicology ; Pharmacy ; Piroxicam - administration & dosage ; Piroxicam - analogs & derivatives ; Piroxicam - chemistry ; Piroxicam - pharmacokinetics ; Propylene Glycol - chemistry ; Rabbits ; Research Article ; Solubility ; Solvents - chemistry ; Technology, Pharmaceutical - methods ; Viscosity ; Water - chemistry</subject><ispartof>AAPS PharmSciTech, 2009, Vol.10 (1), p.166-171</ispartof><rights>American Association of Pharmaceutical Scientists 2009</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c471t-6eb32f1ef259bd02bc4a857330d0b6515480ce6728fe0c661d5ebe2da567ac653</citedby><cites>FETCH-LOGICAL-c471t-6eb32f1ef259bd02bc4a857330d0b6515480ce6728fe0c661d5ebe2da567ac653</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC2663679/pdf/$$EPDF$$P50$$Gpubmedcentral$$H</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC2663679/$$EHTML$$P50$$Gpubmedcentral$$H</linktohtml><link.rule.ids>230,314,727,780,784,885,27924,27925,53791,53793</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/19224373$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Yeh, Ming-Kung</creatorcontrib><creatorcontrib>Chang, Li-Chien</creatorcontrib><creatorcontrib>Chiou, Andy Hong-Jey</creatorcontrib><title>Improving Tenoxicam Solubility and Bioavailability by Cosolvent System</title><title>AAPS PharmSciTech</title><addtitle>AAPS PharmSciTech</addtitle><addtitle>AAPS PharmSciTech</addtitle><description>The formulation study of tenoxicam, a poorly water-soluble drug, was developed by use of a ternary cosolvent system and has significantly enhanced the solubility. Additionally, the relative bioavailability of testing formulation was also evaluated by New Zealand rabbit with a single i.m. injection. The three-phase diagram for dimethylsulfoxide (DMSO)/propylene glycol/water, DMSO/ethanol/water, and DMSO/polyethoxylated castor oil/ethanol system was developed. The volume ratio of 5:4:1 in the DMSO/polyethoxylated castor oil/ethanol system resulted in a more suitable vehicle than other systems, with a high solubility (20.73 mg/ml) and low viscosity (10.0 Cp). A pharmacokinetic study of bioequivalence (
F
rel
= 0.89) was also obtained. The present study not only provides a novel strategy improving tenoxicam solubility but also helps further scientific knowledge for the development of parenteral formulations.</description><subject>Animals</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - administration & dosage</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - chemistry</subject><subject>Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics</subject><subject>Biochemistry</subject><subject>Biological Availability</subject><subject>Biomedical and Life Sciences</subject><subject>Biomedicine</subject><subject>Biotechnology</subject><subject>Castor Oil - analogs & derivatives</subject><subject>Castor Oil - chemistry</subject><subject>Chemistry, Pharmaceutical</subject><subject>Dimethyl Sulfoxide - chemistry</subject><subject>Ethanol - chemistry</subject><subject>Injections, Intramuscular</subject><subject>Pharmacology/Toxicology</subject><subject>Pharmacy</subject><subject>Piroxicam - administration & dosage</subject><subject>Piroxicam - analogs & derivatives</subject><subject>Piroxicam - chemistry</subject><subject>Piroxicam - pharmacokinetics</subject><subject>Propylene Glycol - chemistry</subject><subject>Rabbits</subject><subject>Research Article</subject><subject>Solubility</subject><subject>Solvents - chemistry</subject><subject>Technology, Pharmaceutical - methods</subject><subject>Viscosity</subject><subject>Water - chemistry</subject><issn>1530-9932</issn><issn>1530-9932</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2009</creationdate><recordtype>article</recordtype><recordid>eNp9kD9PwzAQxS0EoqXwAVhQJraA_8ROvCBBRaFSJYaW2XIcp7hK4mInFfn2uGoEZeEWn3zvvTv9ALhG8A5hmN17hHHCYwh5zFHGY3wCxogSGHNO8OlRPwIX3m8gxARxcg5GiAcjSckYzOb11tmdadbRSjf2yyhZR0tbdbmpTNtHsimiJ2PlTppKDn95H02tt9VON2207H2r60twVsrK66vhnYD32fNq-hov3l7m08dFrJIUtTHTOcEl0iWmPC8gzlUiM5oSAguYM4pokkGlWYqzUkPFGCqozjUuJGWpVIySCXg45G67vNaFChc4WYmtM7V0vbDSiL-TxnyItd0JzBhhKQ8Bt0OAs5-d9q2ojVe6qmSjbecFRqFohoMQHYTKWe-dLn-WICj29MWBvgj0xZ6-2Htujq_7dQy4gwAfBD6MmrV2YmM71wRi_6R-A6gQkeM</recordid><startdate>2009</startdate><enddate>2009</enddate><creator>Yeh, Ming-Kung</creator><creator>Chang, Li-Chien</creator><creator>Chiou, Andy Hong-Jey</creator><general>Springer US</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>7QO</scope><scope>8FD</scope><scope>FR3</scope><scope>P64</scope><scope>5PM</scope></search><sort><creationdate>2009</creationdate><title>Improving Tenoxicam Solubility and Bioavailability by Cosolvent System</title><author>Yeh, Ming-Kung ; Chang, Li-Chien ; Chiou, Andy Hong-Jey</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c471t-6eb32f1ef259bd02bc4a857330d0b6515480ce6728fe0c661d5ebe2da567ac653</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2009</creationdate><topic>Animals</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - administration & dosage</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - chemistry</topic><topic>Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics</topic><topic>Biochemistry</topic><topic>Biological Availability</topic><topic>Biomedical and Life Sciences</topic><topic>Biomedicine</topic><topic>Biotechnology</topic><topic>Castor Oil - analogs & derivatives</topic><topic>Castor Oil - chemistry</topic><topic>Chemistry, Pharmaceutical</topic><topic>Dimethyl Sulfoxide - chemistry</topic><topic>Ethanol - chemistry</topic><topic>Injections, Intramuscular</topic><topic>Pharmacology/Toxicology</topic><topic>Pharmacy</topic><topic>Piroxicam - administration & dosage</topic><topic>Piroxicam - analogs & derivatives</topic><topic>Piroxicam - chemistry</topic><topic>Piroxicam - pharmacokinetics</topic><topic>Propylene Glycol - chemistry</topic><topic>Rabbits</topic><topic>Research Article</topic><topic>Solubility</topic><topic>Solvents - chemistry</topic><topic>Technology, Pharmaceutical - methods</topic><topic>Viscosity</topic><topic>Water - chemistry</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Yeh, Ming-Kung</creatorcontrib><creatorcontrib>Chang, Li-Chien</creatorcontrib><creatorcontrib>Chiou, Andy Hong-Jey</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Biotechnology Research Abstracts</collection><collection>Technology Research Database</collection><collection>Engineering Research Database</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>PubMed Central (Full Participant titles)</collection><jtitle>AAPS PharmSciTech</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Yeh, Ming-Kung</au><au>Chang, Li-Chien</au><au>Chiou, Andy Hong-Jey</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Improving Tenoxicam Solubility and Bioavailability by Cosolvent System</atitle><jtitle>AAPS PharmSciTech</jtitle><stitle>AAPS PharmSciTech</stitle><addtitle>AAPS PharmSciTech</addtitle><date>2009</date><risdate>2009</risdate><volume>10</volume><issue>1</issue><spage>166</spage><epage>171</epage><pages>166-171</pages><issn>1530-9932</issn><eissn>1530-9932</eissn><abstract>The formulation study of tenoxicam, a poorly water-soluble drug, was developed by use of a ternary cosolvent system and has significantly enhanced the solubility. Additionally, the relative bioavailability of testing formulation was also evaluated by New Zealand rabbit with a single i.m. injection. The three-phase diagram for dimethylsulfoxide (DMSO)/propylene glycol/water, DMSO/ethanol/water, and DMSO/polyethoxylated castor oil/ethanol system was developed. The volume ratio of 5:4:1 in the DMSO/polyethoxylated castor oil/ethanol system resulted in a more suitable vehicle than other systems, with a high solubility (20.73 mg/ml) and low viscosity (10.0 Cp). A pharmacokinetic study of bioequivalence (
F
rel
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subjects | Animals Anti-Inflammatory Agents, Non-Steroidal - administration & dosage Anti-Inflammatory Agents, Non-Steroidal - chemistry Anti-Inflammatory Agents, Non-Steroidal - pharmacokinetics Biochemistry Biological Availability Biomedical and Life Sciences Biomedicine Biotechnology Castor Oil - analogs & derivatives Castor Oil - chemistry Chemistry, Pharmaceutical Dimethyl Sulfoxide - chemistry Ethanol - chemistry Injections, Intramuscular Pharmacology/Toxicology Pharmacy Piroxicam - administration & dosage Piroxicam - analogs & derivatives Piroxicam - chemistry Piroxicam - pharmacokinetics Propylene Glycol - chemistry Rabbits Research Article Solubility Solvents - chemistry Technology, Pharmaceutical - methods Viscosity Water - chemistry |
title | Improving Tenoxicam Solubility and Bioavailability by Cosolvent System |
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