The preparation of agglomerates containing solid dispersions of diazepam by melt agglomeration in a high shear mixer
The aim of this study was to prepare by melt agglomeration agglomerates containing solid dispersions of diazepam as poorly water-soluble model drug in order to evaluate the possibility of improving the dissolution rate. Lactose monohydrate was melt agglomerated with polyethylene glycol (PEG) 3000 or...
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| Veröffentlicht in: | International journal of pharmaceutics 2003-06, Vol.259 (1), p.161-171 |
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| container_title | International journal of pharmaceutics |
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| creator | Seo, Anette Holm, Per Kristensen, Henning Gjelstrup Schæfer, Torben |
| description | The aim of this study was to prepare by melt agglomeration agglomerates containing solid dispersions of diazepam as poorly water-soluble model drug in order to evaluate the possibility of improving the dissolution rate. Lactose monohydrate was melt agglomerated with polyethylene glycol (PEG) 3000 or Gelucire
® 50/13 (mixture of glycerides and PEG esters of fatty acids) as meltable binders in a high shear mixer. The binders were added either as a mixture of melted binder and diazepam by a pump-on procedure or by a melt-in procedure of solid binder particles. Different drug concentrations, maximum manufacturing temperatures, and cooling rates were investigated. It was found to be possible to increase the dissolution rate of diazepam by melt agglomeration. A higher dissolution rate was obtained with a lower drug concentration. Admixing the binders by the melt-in procedure resulted in similar dissolution rates as the pump-on procedure. The different maximum manufacturing temperatures and cooling rates were found to have complex effects on the dissolution rate for formulations containing PEG 3000, whereas only minor effects of the cooling procedure were found with Gelucire 50/13. Gelucire 50/13 resulted in faster dissolution rates compared to PEG 3000. |
| doi_str_mv | 10.1016/S0378-5173(03)00228-X |
| format | Article |
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® 50/13 (mixture of glycerides and PEG esters of fatty acids) as meltable binders in a high shear mixer. The binders were added either as a mixture of melted binder and diazepam by a pump-on procedure or by a melt-in procedure of solid binder particles. Different drug concentrations, maximum manufacturing temperatures, and cooling rates were investigated. It was found to be possible to increase the dissolution rate of diazepam by melt agglomeration. A higher dissolution rate was obtained with a lower drug concentration. Admixing the binders by the melt-in procedure resulted in similar dissolution rates as the pump-on procedure. The different maximum manufacturing temperatures and cooling rates were found to have complex effects on the dissolution rate for formulations containing PEG 3000, whereas only minor effects of the cooling procedure were found with Gelucire 50/13. Gelucire 50/13 resulted in faster dissolution rates compared to PEG 3000.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/S0378-5173(03)00228-X</identifier><identifier>PMID: 12787644</identifier><identifier>CODEN: IJPHDE</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Biological and medical sciences ; Diazepam ; Diazepam - chemistry ; Dissolution rate ; Excipients ; Fats - chemistry ; General pharmacology ; High shear mixer ; Image Processing, Computer-Assisted ; Medical sciences ; Melt agglomeration ; Microscopy, Electron, Scanning ; Neuropharmacology ; Oils - chemistry ; Particle Size ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Polyethylene glycol ; Polyethylene Glycols - chemistry ; Psycholeptics: tranquillizer, neuroleptic ; Psychology. Psychoanalysis. Psychiatry ; Psychopharmacology ; Solid dispersion ; Solubility ; Technology, Pharmaceutical - instrumentation ; Technology, Pharmaceutical - methods ; Temperature ; Viscosity</subject><ispartof>International journal of pharmaceutics, 2003-06, Vol.259 (1), p.161-171</ispartof><rights>2003 Elsevier Science B.V.</rights><rights>2003 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c457t-a5cfab8a2d9e15b217ee5b52e7e859aaa6ab9eeabccce300a137255efdfc8c543</citedby></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0378-5173(03)00228-X$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=14833553$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/12787644$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Seo, Anette</creatorcontrib><creatorcontrib>Holm, Per</creatorcontrib><creatorcontrib>Kristensen, Henning Gjelstrup</creatorcontrib><creatorcontrib>Schæfer, Torben</creatorcontrib><title>The preparation of agglomerates containing solid dispersions of diazepam by melt agglomeration in a high shear mixer</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>The aim of this study was to prepare by melt agglomeration agglomerates containing solid dispersions of diazepam as poorly water-soluble model drug in order to evaluate the possibility of improving the dissolution rate. Lactose monohydrate was melt agglomerated with polyethylene glycol (PEG) 3000 or Gelucire
® 50/13 (mixture of glycerides and PEG esters of fatty acids) as meltable binders in a high shear mixer. The binders were added either as a mixture of melted binder and diazepam by a pump-on procedure or by a melt-in procedure of solid binder particles. Different drug concentrations, maximum manufacturing temperatures, and cooling rates were investigated. It was found to be possible to increase the dissolution rate of diazepam by melt agglomeration. A higher dissolution rate was obtained with a lower drug concentration. Admixing the binders by the melt-in procedure resulted in similar dissolution rates as the pump-on procedure. The different maximum manufacturing temperatures and cooling rates were found to have complex effects on the dissolution rate for formulations containing PEG 3000, whereas only minor effects of the cooling procedure were found with Gelucire 50/13. Gelucire 50/13 resulted in faster dissolution rates compared to PEG 3000.</description><subject>Biological and medical sciences</subject><subject>Diazepam</subject><subject>Diazepam - chemistry</subject><subject>Dissolution rate</subject><subject>Excipients</subject><subject>Fats - chemistry</subject><subject>General pharmacology</subject><subject>High shear mixer</subject><subject>Image Processing, Computer-Assisted</subject><subject>Medical sciences</subject><subject>Melt agglomeration</subject><subject>Microscopy, Electron, Scanning</subject><subject>Neuropharmacology</subject><subject>Oils - chemistry</subject><subject>Particle Size</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Polyethylene glycol</subject><subject>Polyethylene Glycols - chemistry</subject><subject>Psycholeptics: tranquillizer, neuroleptic</subject><subject>Psychology. Psychoanalysis. Psychiatry</subject><subject>Psychopharmacology</subject><subject>Solid dispersion</subject><subject>Solubility</subject><subject>Technology, Pharmaceutical - instrumentation</subject><subject>Technology, Pharmaceutical - methods</subject><subject>Temperature</subject><subject>Viscosity</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2003</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkFGL1DAQx4Mo7t7qR1Dyotw9VJOmabpPhxx6Cgs-uMK-hWk63Y20Tc10xfXTm7qL55swMDD8_jPDj7EXUryRQpZvvwhlqkxLo66FuhEiz6ts94gtZWVUpgpTPmbLv8iCXRF9E0KUuVRP2ULmpjJlUSzZtD0gHyOOEGHyYeCh5bDfd6HHNEDiLgwT-MEPe06h8w1vPI0YKbE0w42HXynd8_rEe-ymf9LzOj9w4Ae_P3A6IETe-58Yn7EnLXSEzy99xb5-eL-9-5htPt9_unu3yVyhzZSBdi3UFeTNGqWuc2kQda1zNFjpNQCUUK8RoXbOoRICpDK51tg2raucLtSKvT7vHWP4fkSabO_JYdfBgOFI1ihVquQogfoMuhiIIrZ2jL6HeLJS2Fm3_aPbzi6tSDXrtruUe3k5cKx7bB5SF78JeHUBgBx0bYTBeXrgikoprVXibs8cJh0_PEZLzuPgsPER3WSb4P_zym9wa6A6</recordid><startdate>20030618</startdate><enddate>20030618</enddate><creator>Seo, Anette</creator><creator>Holm, Per</creator><creator>Kristensen, Henning Gjelstrup</creator><creator>Schæfer, Torben</creator><general>Elsevier B.V</general><general>Elsevier</general><scope>IQODW</scope><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></search><sort><creationdate>20030618</creationdate><title>The preparation of agglomerates containing solid dispersions of diazepam by melt agglomeration in a high shear mixer</title><author>Seo, Anette ; Holm, Per ; Kristensen, Henning Gjelstrup ; Schæfer, Torben</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c457t-a5cfab8a2d9e15b217ee5b52e7e859aaa6ab9eeabccce300a137255efdfc8c543</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2003</creationdate><topic>Biological and medical sciences</topic><topic>Diazepam</topic><topic>Diazepam - chemistry</topic><topic>Dissolution rate</topic><topic>Excipients</topic><topic>Fats - chemistry</topic><topic>General pharmacology</topic><topic>High shear mixer</topic><topic>Image Processing, Computer-Assisted</topic><topic>Medical sciences</topic><topic>Melt agglomeration</topic><topic>Microscopy, Electron, Scanning</topic><topic>Neuropharmacology</topic><topic>Oils - chemistry</topic><topic>Particle Size</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Polyethylene glycol</topic><topic>Polyethylene Glycols - chemistry</topic><topic>Psycholeptics: tranquillizer, neuroleptic</topic><topic>Psychology. Psychoanalysis. Psychiatry</topic><topic>Psychopharmacology</topic><topic>Solid dispersion</topic><topic>Solubility</topic><topic>Technology, Pharmaceutical - instrumentation</topic><topic>Technology, Pharmaceutical - methods</topic><topic>Temperature</topic><topic>Viscosity</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Seo, Anette</creatorcontrib><creatorcontrib>Holm, Per</creatorcontrib><creatorcontrib>Kristensen, Henning Gjelstrup</creatorcontrib><creatorcontrib>Schæfer, Torben</creatorcontrib><collection>Pascal-Francis</collection><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><jtitle>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Seo, Anette</au><au>Holm, Per</au><au>Kristensen, Henning Gjelstrup</au><au>Schæfer, Torben</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>The preparation of agglomerates containing solid dispersions of diazepam by melt agglomeration in a high shear mixer</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2003-06-18</date><risdate>2003</risdate><volume>259</volume><issue>1</issue><spage>161</spage><epage>171</epage><pages>161-171</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><coden>IJPHDE</coden><abstract>The aim of this study was to prepare by melt agglomeration agglomerates containing solid dispersions of diazepam as poorly water-soluble model drug in order to evaluate the possibility of improving the dissolution rate. Lactose monohydrate was melt agglomerated with polyethylene glycol (PEG) 3000 or Gelucire
® 50/13 (mixture of glycerides and PEG esters of fatty acids) as meltable binders in a high shear mixer. The binders were added either as a mixture of melted binder and diazepam by a pump-on procedure or by a melt-in procedure of solid binder particles. Different drug concentrations, maximum manufacturing temperatures, and cooling rates were investigated. It was found to be possible to increase the dissolution rate of diazepam by melt agglomeration. A higher dissolution rate was obtained with a lower drug concentration. Admixing the binders by the melt-in procedure resulted in similar dissolution rates as the pump-on procedure. The different maximum manufacturing temperatures and cooling rates were found to have complex effects on the dissolution rate for formulations containing PEG 3000, whereas only minor effects of the cooling procedure were found with Gelucire 50/13. Gelucire 50/13 resulted in faster dissolution rates compared to PEG 3000.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>12787644</pmid><doi>10.1016/S0378-5173(03)00228-X</doi><tpages>11</tpages></addata></record> |
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| subjects | Biological and medical sciences Diazepam Diazepam - chemistry Dissolution rate Excipients Fats - chemistry General pharmacology High shear mixer Image Processing, Computer-Assisted Medical sciences Melt agglomeration Microscopy, Electron, Scanning Neuropharmacology Oils - chemistry Particle Size Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Polyethylene glycol Polyethylene Glycols - chemistry Psycholeptics: tranquillizer, neuroleptic Psychology. Psychoanalysis. Psychiatry Psychopharmacology Solid dispersion Solubility Technology, Pharmaceutical - instrumentation Technology, Pharmaceutical - methods Temperature Viscosity |
| title | The preparation of agglomerates containing solid dispersions of diazepam by melt agglomeration in a high shear mixer |
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