Effect of additives on the physicochemical properties of liquid suppository bases

To investigate the effects of additives on the physicochemical properties of in situ gelling and mucoadhesive liquid suppository base, gelation temperature, gel strength and bioadhesive force of liquid suppository base, poloxamer 407 (P 407) and poloxamer 188 (P 188) (15/15%) were evaluated in the p...

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Veröffentlicht in:International journal of pharmaceutics 1999-11, Vol.190 (1), p.13-19
Hauptverfasser: Choi, Han-Gon, Lee, Mi-Kyung, Kim, Moon-Hee, Kim, Chong-Kook
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container_title International journal of pharmaceutics
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creator Choi, Han-Gon
Lee, Mi-Kyung
Kim, Moon-Hee
Kim, Chong-Kook
description To investigate the effects of additives on the physicochemical properties of in situ gelling and mucoadhesive liquid suppository base, gelation temperature, gel strength and bioadhesive force of liquid suppository base, poloxamer 407 (P 407) and poloxamer 188 (P 188) (15/15%) were evaluated in the presence of following additives: solvent (ethanol, propylene glycol, glycerin), ionic strength-controlling agent (sodium chloride) and pH-controlling agent (hydrochloric acid, sodium monohydrogen phosphate, sodium dihydrogen phosphate). Among the additives studied, sodium chloride, sodium monohydrogen phosphate and sodium dihydrogen phosphate increased to a great extent the gel strength and the bioadhesive force of P 407/P 188 (15/15%) with a decrease in gelation temperature. Glycerin slightly decreased the gelation temperature and slightly increased the gel strength and bioadhesive force. However, the addition of 1% of sodium chloride, sodium monohydrogen phosphate or sodium dihydrogen phosphate caused a greater than 60-fold increase in gel strength and over a tenfold increase in bioadhesive force with 2–4°C decrease of gelation temperature within optimal range, compared with P 407/P 188 (15/15%) alone. On the other hand, ethanol, propylene glycol and hydrochloric acid increased the gelation temperature and slightly decreased the gel strength and the bioadhesive force. Taken together, these findings indicate that the effect of additives on the physicochemical properties of liquid suppository bases depends on their bonding capacities, in that additives such as sodium chloride, sodium monohydrogen phosphate and sodium dihydrogen phosphate having strong cross-linking bonds with the components of liquid suppository base increase the strength and bioadhesive force of a gel compared to liquid suppository base alone, while additives such as ethanol, propylene glycol and hydrochloric acid having weaker hydrogen bonding result in a weaker response. Thus, sodium chloride and sodium phosphates appear to be promising additives for in situ gelling and mucoadhesive liquid suppository base, if used in adequate amounts.
doi_str_mv 10.1016/S0378-5173(99)00225-2
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Among the additives studied, sodium chloride, sodium monohydrogen phosphate and sodium dihydrogen phosphate increased to a great extent the gel strength and the bioadhesive force of P 407/P 188 (15/15%) with a decrease in gelation temperature. Glycerin slightly decreased the gelation temperature and slightly increased the gel strength and bioadhesive force. However, the addition of 1% of sodium chloride, sodium monohydrogen phosphate or sodium dihydrogen phosphate caused a greater than 60-fold increase in gel strength and over a tenfold increase in bioadhesive force with 2–4°C decrease of gelation temperature within optimal range, compared with P 407/P 188 (15/15%) alone. On the other hand, ethanol, propylene glycol and hydrochloric acid increased the gelation temperature and slightly decreased the gel strength and the bioadhesive force. 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Among the additives studied, sodium chloride, sodium monohydrogen phosphate and sodium dihydrogen phosphate increased to a great extent the gel strength and the bioadhesive force of P 407/P 188 (15/15%) with a decrease in gelation temperature. Glycerin slightly decreased the gelation temperature and slightly increased the gel strength and bioadhesive force. However, the addition of 1% of sodium chloride, sodium monohydrogen phosphate or sodium dihydrogen phosphate caused a greater than 60-fold increase in gel strength and over a tenfold increase in bioadhesive force with 2–4°C decrease of gelation temperature within optimal range, compared with P 407/P 188 (15/15%) alone. On the other hand, ethanol, propylene glycol and hydrochloric acid increased the gelation temperature and slightly decreased the gel strength and the bioadhesive force. 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Drug treatments</subject><subject>Phosphates - chemistry</subject><subject>Poloxamer</subject><subject>Poloxamer - chemistry</subject><subject>Propylene Glycol - chemistry</subject><subject>Sodium Chloride - chemistry</subject><subject>Solvents - chemistry</subject><subject>Suppositories - chemistry</subject><subject>Temperature</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>1999</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqF0E2LFDEQgOEgijuu_gQlBxE9tFaS7nTnJLKsH7Agop5DOqkwkZ5Jb6p7Yf69mZ1BvXnK5alK8TL2XMBbAUK_-w6qH5pO9Oq1MW8ApOwa-YBtxNCrRrW9fsg2f8gFe0L0CwC0FOoxuxDQyQGM3LBv1zGiX3iO3IWQlnSHxPOeL1vk8_ZAyWe_xV3ybuJzyTOWJR1F5FO6XVPgtM5zprTkcuCjI6Sn7FF0E-Gz83vJfn68_nH1ubn5-unL1YebxredXprRtKigFeCFRGh1PTXETkpjDMLYyqGqECGi1jqGbnROoXbjGGTEcQidumSvTnvrWbcr0mJ3iTxOk9tjXsn2MGghTVthd4K-ZKKC0c4l7Vw5WAH22NLet7THUNYYe9_Syjr34vzBOu4w_DN1ilfByzNwVPvE4vY-0V8n-mFQprL3J4a1xl3CYskn3HsMqdT0NuT0n0t-A6DRkWc</recordid><startdate>19991110</startdate><enddate>19991110</enddate><creator>Choi, Han-Gon</creator><creator>Lee, Mi-Kyung</creator><creator>Kim, Moon-Hee</creator><creator>Kim, Chong-Kook</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>19991110</creationdate><title>Effect of additives on the physicochemical properties of liquid suppository bases</title><author>Choi, Han-Gon ; Lee, Mi-Kyung ; Kim, Moon-Hee ; Kim, Chong-Kook</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c456t-b94e30410c12e046378df522999e0b428456df0fe666fd5baa3e6abbd2feb8d53</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>1999</creationdate><topic>Adhesiveness</topic><topic>Bioadhesive force</topic><topic>Biological and medical sciences</topic><topic>Chemical Phenomena</topic><topic>Chemistry, Physical</topic><topic>Drug Compounding</topic><topic>Ethanol - chemistry</topic><topic>Gel strength</topic><topic>Gelation temperature</topic><topic>Gels</topic><topic>General pharmacology</topic><topic>Glycerol - chemistry</topic><topic>Hydrochloric Acid - chemistry</topic><topic>Hydrogen-Ion Concentration</topic><topic>Liquid suppository base</topic><topic>Medical sciences</topic><topic>Osmolar Concentration</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Phosphates - chemistry</topic><topic>Poloxamer</topic><topic>Poloxamer - chemistry</topic><topic>Propylene Glycol - chemistry</topic><topic>Sodium Chloride - chemistry</topic><topic>Solvents - chemistry</topic><topic>Suppositories - chemistry</topic><topic>Temperature</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Choi, Han-Gon</creatorcontrib><creatorcontrib>Lee, Mi-Kyung</creatorcontrib><creatorcontrib>Kim, Moon-Hee</creatorcontrib><creatorcontrib>Kim, Chong-Kook</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>Choi, Han-Gon</au><au>Lee, Mi-Kyung</au><au>Kim, Moon-Hee</au><au>Kim, Chong-Kook</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effect of additives on the physicochemical properties of liquid suppository bases</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>1999-11-10</date><risdate>1999</risdate><volume>190</volume><issue>1</issue><spage>13</spage><epage>19</epage><pages>13-19</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><coden>IJPHDE</coden><abstract>To investigate the effects of additives on the physicochemical properties of in situ gelling and mucoadhesive liquid suppository base, gelation temperature, gel strength and bioadhesive force of liquid suppository base, poloxamer 407 (P 407) and poloxamer 188 (P 188) (15/15%) were evaluated in the presence of following additives: solvent (ethanol, propylene glycol, glycerin), ionic strength-controlling agent (sodium chloride) and pH-controlling agent (hydrochloric acid, sodium monohydrogen phosphate, sodium dihydrogen phosphate). Among the additives studied, sodium chloride, sodium monohydrogen phosphate and sodium dihydrogen phosphate increased to a great extent the gel strength and the bioadhesive force of P 407/P 188 (15/15%) with a decrease in gelation temperature. Glycerin slightly decreased the gelation temperature and slightly increased the gel strength and bioadhesive force. However, the addition of 1% of sodium chloride, sodium monohydrogen phosphate or sodium dihydrogen phosphate caused a greater than 60-fold increase in gel strength and over a tenfold increase in bioadhesive force with 2–4°C decrease of gelation temperature within optimal range, compared with P 407/P 188 (15/15%) alone. On the other hand, ethanol, propylene glycol and hydrochloric acid increased the gelation temperature and slightly decreased the gel strength and the bioadhesive force. Taken together, these findings indicate that the effect of additives on the physicochemical properties of liquid suppository bases depends on their bonding capacities, in that additives such as sodium chloride, sodium monohydrogen phosphate and sodium dihydrogen phosphate having strong cross-linking bonds with the components of liquid suppository base increase the strength and bioadhesive force of a gel compared to liquid suppository base alone, while additives such as ethanol, propylene glycol and hydrochloric acid having weaker hydrogen bonding result in a weaker response. Thus, sodium chloride and sodium phosphates appear to be promising additives for in situ gelling and mucoadhesive liquid suppository base, if used in adequate amounts.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>10528092</pmid><doi>10.1016/S0378-5173(99)00225-2</doi><tpages>7</tpages></addata></record>
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subjects Adhesiveness
Bioadhesive force
Biological and medical sciences
Chemical Phenomena
Chemistry, Physical
Drug Compounding
Ethanol - chemistry
Gel strength
Gelation temperature
Gels
General pharmacology
Glycerol - chemistry
Hydrochloric Acid - chemistry
Hydrogen-Ion Concentration
Liquid suppository base
Medical sciences
Osmolar Concentration
Pharmaceutical technology. Pharmaceutical industry
Pharmacology. Drug treatments
Phosphates - chemistry
Poloxamer
Poloxamer - chemistry
Propylene Glycol - chemistry
Sodium Chloride - chemistry
Solvents - chemistry
Suppositories - chemistry
Temperature
title Effect of additives on the physicochemical properties of liquid suppository bases
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