Dissolution of hydrocortisone in human and simulated intestinal fluids
To compare solubility and dissolution rate of hydrocortisone in aspirated human intestinal fluids (HIFs) with simulated intestinal fluids (SIFs) and buffer. Solubility and flux from a rotating disk of hydrocortisone were measured. The bile salt content, pH and osmotic pressure were determined in HIF...
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| Veröffentlicht in: | Pharmaceutical research 2000-02, Vol.17 (2), p.183-189 |
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| creator | PEDERSEN, B. L BRØNDSTED, H LENNERNÄS, H CHRISTENSEN, F. N MÜLLERTZ, A KRISTENSEN, H. G |
| description | To compare solubility and dissolution rate of hydrocortisone in aspirated human intestinal fluids (HIFs) with simulated intestinal fluids (SIFs) and buffer.
Solubility and flux from a rotating disk of hydrocortisone were measured. The bile salt content, pH and osmotic pressure were determined in HIFs.
In fasted state the solubility of hydrocortisone was higher in HIFs than in the buffer and SIFs. The flux of hydrocortisone in HIFs was similar to the flux in the buffer but lower than the flux in SIFs at fasted state. Addition of intestinal surfactants in SIFs increased solubility and flux at both fasted and fed state. The increase in solubility was caused by micelle formation in SIFs. The increase in flux may partly be explained by increased solubility. The bile salt content of the HIFs did not correlate with the solubility or the flux but pH in the HIFs seems to have some effect on the components of the HIFs resulting in increased solubility.
It is possible to perform comparable dissolution tests in HIFs and SIFs. The lack of correlation between the results in HIFs and the bile salt content may be explained by the relatively low lipophilicity of the model drug. |
| doi_str_mv | 10.1023/A:1007517414200 |
| format | Article |
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Solubility and flux from a rotating disk of hydrocortisone were measured. The bile salt content, pH and osmotic pressure were determined in HIFs.
In fasted state the solubility of hydrocortisone was higher in HIFs than in the buffer and SIFs. The flux of hydrocortisone in HIFs was similar to the flux in the buffer but lower than the flux in SIFs at fasted state. Addition of intestinal surfactants in SIFs increased solubility and flux at both fasted and fed state. The increase in solubility was caused by micelle formation in SIFs. The increase in flux may partly be explained by increased solubility. The bile salt content of the HIFs did not correlate with the solubility or the flux but pH in the HIFs seems to have some effect on the components of the HIFs resulting in increased solubility.
It is possible to perform comparable dissolution tests in HIFs and SIFs. The lack of correlation between the results in HIFs and the bile salt content may be explained by the relatively low lipophilicity of the model drug.</description><identifier>ISSN: 0724-8741</identifier><identifier>EISSN: 1573-904X</identifier><identifier>DOI: 10.1023/A:1007517414200</identifier><identifier>PMID: 10751033</identifier><identifier>CODEN: PHREEB</identifier><language>eng</language><publisher>New York, NY: Springer</publisher><subject>Anti-Inflammatory Agents - pharmacokinetics ; Bile ; Biological and medical sciences ; Body Fluids ; Bones, joints and connective tissue. Antiinflammatory agents ; Buffers ; Contact angle ; Diffusion ; Dissolution ; Drugs ; Duodenum - metabolism ; Eating ; Fasting ; Fatty acids ; Fluids ; General pharmacology ; Glycerol ; Glycocholic Acid - chemistry ; Glycocholic Acid - metabolism ; Humans ; Hydrocortisone - pharmacokinetics ; Hydrogen-Ion Concentration ; Intestinal Absorption - physiology ; Jejunum - metabolism ; Medical sciences ; Micelles ; Osmotic Pressure ; Pharmacology. Drug treatments ; Physicochemical properties. Structure-activity relationships ; Rheology ; Salt ; Small intestine ; Sodium ; Solubility ; Surface Tension ; Surfactants</subject><ispartof>Pharmaceutical research, 2000-02, Vol.17 (2), p.183-189</ispartof><rights>2000 INIST-CNRS</rights><rights>Copyright Kluwer Academic Publishers Feb 2000</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c309t-7d3262660fe5c83196cece6b6192f31243ecca5b59d34b29867b73ff1fc957243</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1309682$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/10751033$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>PEDERSEN, B. L</creatorcontrib><creatorcontrib>BRØNDSTED, H</creatorcontrib><creatorcontrib>LENNERNÄS, H</creatorcontrib><creatorcontrib>CHRISTENSEN, F. N</creatorcontrib><creatorcontrib>MÜLLERTZ, A</creatorcontrib><creatorcontrib>KRISTENSEN, H. G</creatorcontrib><title>Dissolution of hydrocortisone in human and simulated intestinal fluids</title><title>Pharmaceutical research</title><addtitle>Pharm Res</addtitle><description>To compare solubility and dissolution rate of hydrocortisone in aspirated human intestinal fluids (HIFs) with simulated intestinal fluids (SIFs) and buffer.
Solubility and flux from a rotating disk of hydrocortisone were measured. The bile salt content, pH and osmotic pressure were determined in HIFs.
In fasted state the solubility of hydrocortisone was higher in HIFs than in the buffer and SIFs. The flux of hydrocortisone in HIFs was similar to the flux in the buffer but lower than the flux in SIFs at fasted state. Addition of intestinal surfactants in SIFs increased solubility and flux at both fasted and fed state. The increase in solubility was caused by micelle formation in SIFs. The increase in flux may partly be explained by increased solubility. The bile salt content of the HIFs did not correlate with the solubility or the flux but pH in the HIFs seems to have some effect on the components of the HIFs resulting in increased solubility.
It is possible to perform comparable dissolution tests in HIFs and SIFs. The lack of correlation between the results in HIFs and the bile salt content may be explained by the relatively low lipophilicity of the model drug.</description><subject>Anti-Inflammatory Agents - pharmacokinetics</subject><subject>Bile</subject><subject>Biological and medical sciences</subject><subject>Body Fluids</subject><subject>Bones, joints and connective tissue. Antiinflammatory agents</subject><subject>Buffers</subject><subject>Contact angle</subject><subject>Diffusion</subject><subject>Dissolution</subject><subject>Drugs</subject><subject>Duodenum - metabolism</subject><subject>Eating</subject><subject>Fasting</subject><subject>Fatty acids</subject><subject>Fluids</subject><subject>General pharmacology</subject><subject>Glycerol</subject><subject>Glycocholic Acid - chemistry</subject><subject>Glycocholic Acid - metabolism</subject><subject>Humans</subject><subject>Hydrocortisone - pharmacokinetics</subject><subject>Hydrogen-Ion Concentration</subject><subject>Intestinal Absorption - physiology</subject><subject>Jejunum - metabolism</subject><subject>Medical sciences</subject><subject>Micelles</subject><subject>Osmotic Pressure</subject><subject>Pharmacology. Drug treatments</subject><subject>Physicochemical properties. Structure-activity relationships</subject><subject>Rheology</subject><subject>Salt</subject><subject>Small intestine</subject><subject>Sodium</subject><subject>Solubility</subject><subject>Surface Tension</subject><subject>Surfactants</subject><issn>0724-8741</issn><issn>1573-904X</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2000</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>ABUWG</sourceid><sourceid>AFKRA</sourceid><sourceid>BENPR</sourceid><sourceid>CCPQU</sourceid><recordid>eNpdkM1LAzEQxYMotlbP3iSIeFvNx26y8VaqVaHgRcHbks0mNCWb1M3m0P--ESuCp4GZ3xveewBcYnSHEaH38weMEK8wL3FJEDoCU1xxWghUfh6DKeKkLOp8m4CzGDcIoRqL8hRM8LcGUToFy0cbY3BptMHDYOB61w1BhWG0MXgNrYfr1EsPpe9gtH1yctRdXo86jtZLB41Ltovn4MRIF_XFYc7Ax_LpffFSrN6eXxfzVaEoEmPBO0oYYQwZXamaYsGUVpq1DAtiKCYl1UrJqq1ER8uWiJrxllNjsFGiymHoDNz-_N0O4StlD01vo9LOSa9Dig3PdZBcRAav_4GbkIZsODaEEMZFtpGhqwOU2l53zXawvRx2zW89Gbg5ADIq6cwgvbLxj8uhWE3oHuFGcr0</recordid><startdate>20000201</startdate><enddate>20000201</enddate><creator>PEDERSEN, B. 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G</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c309t-7d3262660fe5c83196cece6b6192f31243ecca5b59d34b29867b73ff1fc957243</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2000</creationdate><topic>Anti-Inflammatory Agents - pharmacokinetics</topic><topic>Bile</topic><topic>Biological and medical sciences</topic><topic>Body Fluids</topic><topic>Bones, joints and connective tissue. Antiinflammatory agents</topic><topic>Buffers</topic><topic>Contact angle</topic><topic>Diffusion</topic><topic>Dissolution</topic><topic>Drugs</topic><topic>Duodenum - metabolism</topic><topic>Eating</topic><topic>Fasting</topic><topic>Fatty acids</topic><topic>Fluids</topic><topic>General pharmacology</topic><topic>Glycerol</topic><topic>Glycocholic Acid - chemistry</topic><topic>Glycocholic Acid - metabolism</topic><topic>Humans</topic><topic>Hydrocortisone - pharmacokinetics</topic><topic>Hydrogen-Ion Concentration</topic><topic>Intestinal Absorption - physiology</topic><topic>Jejunum - metabolism</topic><topic>Medical sciences</topic><topic>Micelles</topic><topic>Osmotic Pressure</topic><topic>Pharmacology. Drug treatments</topic><topic>Physicochemical properties. Structure-activity relationships</topic><topic>Rheology</topic><topic>Salt</topic><topic>Small intestine</topic><topic>Sodium</topic><topic>Solubility</topic><topic>Surface Tension</topic><topic>Surfactants</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>PEDERSEN, B. L</creatorcontrib><creatorcontrib>BRØNDSTED, H</creatorcontrib><creatorcontrib>LENNERNÄS, H</creatorcontrib><creatorcontrib>CHRISTENSEN, F. N</creatorcontrib><creatorcontrib>MÜLLERTZ, A</creatorcontrib><creatorcontrib>KRISTENSEN, H. 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L</au><au>BRØNDSTED, H</au><au>LENNERNÄS, H</au><au>CHRISTENSEN, F. N</au><au>MÜLLERTZ, A</au><au>KRISTENSEN, H. G</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Dissolution of hydrocortisone in human and simulated intestinal fluids</atitle><jtitle>Pharmaceutical research</jtitle><addtitle>Pharm Res</addtitle><date>2000-02-01</date><risdate>2000</risdate><volume>17</volume><issue>2</issue><spage>183</spage><epage>189</epage><pages>183-189</pages><issn>0724-8741</issn><eissn>1573-904X</eissn><coden>PHREEB</coden><abstract>To compare solubility and dissolution rate of hydrocortisone in aspirated human intestinal fluids (HIFs) with simulated intestinal fluids (SIFs) and buffer.
Solubility and flux from a rotating disk of hydrocortisone were measured. The bile salt content, pH and osmotic pressure were determined in HIFs.
In fasted state the solubility of hydrocortisone was higher in HIFs than in the buffer and SIFs. The flux of hydrocortisone in HIFs was similar to the flux in the buffer but lower than the flux in SIFs at fasted state. Addition of intestinal surfactants in SIFs increased solubility and flux at both fasted and fed state. The increase in solubility was caused by micelle formation in SIFs. The increase in flux may partly be explained by increased solubility. The bile salt content of the HIFs did not correlate with the solubility or the flux but pH in the HIFs seems to have some effect on the components of the HIFs resulting in increased solubility.
It is possible to perform comparable dissolution tests in HIFs and SIFs. The lack of correlation between the results in HIFs and the bile salt content may be explained by the relatively low lipophilicity of the model drug.</abstract><cop>New York, NY</cop><pub>Springer</pub><pmid>10751033</pmid><doi>10.1023/A:1007517414200</doi><tpages>7</tpages></addata></record> |
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| identifier | ISSN: 0724-8741 |
| ispartof | Pharmaceutical research, 2000-02, Vol.17 (2), p.183-189 |
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| language | eng |
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| source | MEDLINE; SpringerLink Journals |
| subjects | Anti-Inflammatory Agents - pharmacokinetics Bile Biological and medical sciences Body Fluids Bones, joints and connective tissue. Antiinflammatory agents Buffers Contact angle Diffusion Dissolution Drugs Duodenum - metabolism Eating Fasting Fatty acids Fluids General pharmacology Glycerol Glycocholic Acid - chemistry Glycocholic Acid - metabolism Humans Hydrocortisone - pharmacokinetics Hydrogen-Ion Concentration Intestinal Absorption - physiology Jejunum - metabolism Medical sciences Micelles Osmotic Pressure Pharmacology. Drug treatments Physicochemical properties. Structure-activity relationships Rheology Salt Small intestine Sodium Solubility Surface Tension Surfactants |
| title | Dissolution of hydrocortisone in human and simulated intestinal fluids |
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