Delay effect of magnesium stearate on tablet dissolution in acidic medium
[Display omitted] Magnesium stearate (Mg-St) is a common lubricant used for solid pharmaceutical formulations and is known for its property to cause delay of tablet dissolution. In this study, the mechanism underlying the delay caused by Mg-St was investigated with model metformin hydrochloride (HCl...
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| Veröffentlicht in: | International journal of pharmaceutics 2016-09, Vol.511 (2), p.757-764 |
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| container_end_page | 764 |
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| container_issue | 2 |
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| container_title | International journal of pharmaceutics |
| container_volume | 511 |
| creator | Ariyasu, Aoi Hattori, Yusuke Otsuka, Makoto |
| description | [Display omitted]
Magnesium stearate (Mg-St) is a common lubricant used for solid pharmaceutical formulations and is known for its property to cause delay of tablet dissolution. In this study, the mechanism underlying the delay caused by Mg-St was investigated with model metformin hydrochloride (HCl) tablets containing Mg-St by using the stationary disk method, scanning electron microscopy with energy dispersive X-ray spectrometry (SEM-EDS), and Fourier transform infrared spectroscopy (FTIR). The results revealed the process and mechanism of delay: the exposed amount of Mg-St on the tablet surface increases during the dissolution process, and tablet dissolution is limited by the diffusion of Mg-St. In addition, in the case of dissolution in acidic medium, stearic acid derived from Mg-St was detected on the tablet surface by FTIR. Because the solubility of stearic acid is lower than that of Mg-St, the slower dissolution in acidic medium than in neutral medium may be attributed to the generation of stearic acid. |
| doi_str_mv | 10.1016/j.ijpharm.2016.07.034 |
| format | Article |
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Magnesium stearate (Mg-St) is a common lubricant used for solid pharmaceutical formulations and is known for its property to cause delay of tablet dissolution. In this study, the mechanism underlying the delay caused by Mg-St was investigated with model metformin hydrochloride (HCl) tablets containing Mg-St by using the stationary disk method, scanning electron microscopy with energy dispersive X-ray spectrometry (SEM-EDS), and Fourier transform infrared spectroscopy (FTIR). The results revealed the process and mechanism of delay: the exposed amount of Mg-St on the tablet surface increases during the dissolution process, and tablet dissolution is limited by the diffusion of Mg-St. In addition, in the case of dissolution in acidic medium, stearic acid derived from Mg-St was detected on the tablet surface by FTIR. Because the solubility of stearic acid is lower than that of Mg-St, the slower dissolution in acidic medium than in neutral medium may be attributed to the generation of stearic acid.</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/j.ijpharm.2016.07.034</identifier><identifier>PMID: 27444551</identifier><language>eng</language><publisher>Netherlands: Elsevier B.V</publisher><subject>Delayed-Action Preparations - chemistry ; Delayed-Action Preparations - pharmacokinetics ; Dissolution ; Drug Liberation ; Fourier transform infrared spectroscopy ; Hydrogen-Ion Concentration ; Magnesium stearate ; Metformin - chemistry ; Metformin - pharmacokinetics ; Metformin hydrochloride ; Scanning electron microscopy with energy dispersive X-ray spectrometry ; Solid pharmaceutical formulations ; Stearic acid ; Stearic Acids - chemistry ; Tablets - chemistry</subject><ispartof>International journal of pharmaceutics, 2016-09, Vol.511 (2), p.757-764</ispartof><rights>2016</rights><rights>Copyright © 2016. Published by Elsevier B.V.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c365t-c24cd5e0d39e300d4c09a10d8b396e85cbdf78e98fcc1849b3474a7c800c7a633</citedby><cites>FETCH-LOGICAL-c365t-c24cd5e0d39e300d4c09a10d8b396e85cbdf78e98fcc1849b3474a7c800c7a633</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/j.ijpharm.2016.07.034$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,780,784,3550,27924,27925,45995</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/27444551$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Ariyasu, Aoi</creatorcontrib><creatorcontrib>Hattori, Yusuke</creatorcontrib><creatorcontrib>Otsuka, Makoto</creatorcontrib><title>Delay effect of magnesium stearate on tablet dissolution in acidic medium</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>[Display omitted]
Magnesium stearate (Mg-St) is a common lubricant used for solid pharmaceutical formulations and is known for its property to cause delay of tablet dissolution. In this study, the mechanism underlying the delay caused by Mg-St was investigated with model metformin hydrochloride (HCl) tablets containing Mg-St by using the stationary disk method, scanning electron microscopy with energy dispersive X-ray spectrometry (SEM-EDS), and Fourier transform infrared spectroscopy (FTIR). The results revealed the process and mechanism of delay: the exposed amount of Mg-St on the tablet surface increases during the dissolution process, and tablet dissolution is limited by the diffusion of Mg-St. In addition, in the case of dissolution in acidic medium, stearic acid derived from Mg-St was detected on the tablet surface by FTIR. Because the solubility of stearic acid is lower than that of Mg-St, the slower dissolution in acidic medium than in neutral medium may be attributed to the generation of stearic acid.</description><subject>Delayed-Action Preparations - chemistry</subject><subject>Delayed-Action Preparations - pharmacokinetics</subject><subject>Dissolution</subject><subject>Drug Liberation</subject><subject>Fourier transform infrared spectroscopy</subject><subject>Hydrogen-Ion Concentration</subject><subject>Magnesium stearate</subject><subject>Metformin - chemistry</subject><subject>Metformin - pharmacokinetics</subject><subject>Metformin hydrochloride</subject><subject>Scanning electron microscopy with energy dispersive X-ray spectrometry</subject><subject>Solid pharmaceutical formulations</subject><subject>Stearic acid</subject><subject>Stearic Acids - chemistry</subject><subject>Tablets - chemistry</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2016</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1LxDAQhoMoun78BCVHL62TTdKkJxG_QfCi55AmU83SjzVpBf-9kV29ehpmeGaG9yHklEHJgFUXqzKs1u829uUytyWoErjYIQumFS-4UNUuWQBXupBM8QNymNIKAKol4_vkYKmEEFKyBXm8wc5-UWxbdBMdW9rbtwFTmHuaJrTRTkjHgU626XCiPqQ0dvMU8igM1Lrgg6M9-swfk73WdglPtvWIvN7dvlw_FE_P94_XV0-F45WcCrcUzksEz2vkAF44qC0DrxteV6ila3yrNNa6dY5pUTc5i7DKaQCnbMX5ETnf3F3H8WPGNJk-JIddZwcc52SYZgoqCZJlVG5QF8eUIrZmHUNv45dhYH4smpXZWjQ_Fg0oky3mvbPti7nJ4f62frVl4HIDYA76GTCa5AIOLouI2aPxY_jnxTf5OIYN</recordid><startdate>20160925</startdate><enddate>20160925</enddate><creator>Ariyasu, Aoi</creator><creator>Hattori, Yusuke</creator><creator>Otsuka, Makoto</creator><general>Elsevier B.V</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></search><sort><creationdate>20160925</creationdate><title>Delay effect of magnesium stearate on tablet dissolution in acidic medium</title><author>Ariyasu, Aoi ; Hattori, Yusuke ; Otsuka, Makoto</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c365t-c24cd5e0d39e300d4c09a10d8b396e85cbdf78e98fcc1849b3474a7c800c7a633</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2016</creationdate><topic>Delayed-Action Preparations - chemistry</topic><topic>Delayed-Action Preparations - pharmacokinetics</topic><topic>Dissolution</topic><topic>Drug Liberation</topic><topic>Fourier transform infrared spectroscopy</topic><topic>Hydrogen-Ion Concentration</topic><topic>Magnesium stearate</topic><topic>Metformin - chemistry</topic><topic>Metformin - pharmacokinetics</topic><topic>Metformin hydrochloride</topic><topic>Scanning electron microscopy with energy dispersive X-ray spectrometry</topic><topic>Solid pharmaceutical formulations</topic><topic>Stearic acid</topic><topic>Stearic Acids - chemistry</topic><topic>Tablets - chemistry</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Ariyasu, Aoi</creatorcontrib><creatorcontrib>Hattori, Yusuke</creatorcontrib><creatorcontrib>Otsuka, Makoto</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><jtitle>International journal of pharmaceutics</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Ariyasu, Aoi</au><au>Hattori, Yusuke</au><au>Otsuka, Makoto</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Delay effect of magnesium stearate on tablet dissolution in acidic medium</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2016-09-25</date><risdate>2016</risdate><volume>511</volume><issue>2</issue><spage>757</spage><epage>764</epage><pages>757-764</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><abstract>[Display omitted]
Magnesium stearate (Mg-St) is a common lubricant used for solid pharmaceutical formulations and is known for its property to cause delay of tablet dissolution. In this study, the mechanism underlying the delay caused by Mg-St was investigated with model metformin hydrochloride (HCl) tablets containing Mg-St by using the stationary disk method, scanning electron microscopy with energy dispersive X-ray spectrometry (SEM-EDS), and Fourier transform infrared spectroscopy (FTIR). The results revealed the process and mechanism of delay: the exposed amount of Mg-St on the tablet surface increases during the dissolution process, and tablet dissolution is limited by the diffusion of Mg-St. In addition, in the case of dissolution in acidic medium, stearic acid derived from Mg-St was detected on the tablet surface by FTIR. Because the solubility of stearic acid is lower than that of Mg-St, the slower dissolution in acidic medium than in neutral medium may be attributed to the generation of stearic acid.</abstract><cop>Netherlands</cop><pub>Elsevier B.V</pub><pmid>27444551</pmid><doi>10.1016/j.ijpharm.2016.07.034</doi><tpages>8</tpages></addata></record> |
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| source | MEDLINE; Access via ScienceDirect (Elsevier) |
| subjects | Delayed-Action Preparations - chemistry Delayed-Action Preparations - pharmacokinetics Dissolution Drug Liberation Fourier transform infrared spectroscopy Hydrogen-Ion Concentration Magnesium stearate Metformin - chemistry Metformin - pharmacokinetics Metformin hydrochloride Scanning electron microscopy with energy dispersive X-ray spectrometry Solid pharmaceutical formulations Stearic acid Stearic Acids - chemistry Tablets - chemistry |
| title | Delay effect of magnesium stearate on tablet dissolution in acidic medium |
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