Polymethacrylate salts as new low-swellable mucoadhesive materials
The sodium and potassium salts of the methacrylic copolymers Eudragit ® L100 and Eudragit ® S100 were prepared with the aim to develop new low-swellable mucoadhesive materials intended for the preparation of buccal dosage forms. The physico–chemical characterization of the copolymers and the corresp...
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Veröffentlicht in: | Journal of controlled release 2003-02, Vol.88 (1), p.43-53 |
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creator | Cilurzo, F. Minghetti, P. Selmin, F. Casiraghi, A. Montanari, L. |
description | The sodium and potassium salts of the methacrylic copolymers Eudragit
® L100 and Eudragit
® S100 were prepared with the aim to develop new low-swellable mucoadhesive materials intended for the preparation of buccal dosage forms. The physico–chemical characterization of the copolymers and the corresponding sodium and potassium salts was performed by using Fourier-transform infrared (FT-IR) spectroscopy and thermal analysis. When ionization occurred, the carboxylic acid group absorption band (1730 cm
−1) was replaced by another characteristic band at 1560 cm
−1. After salification the
T
g of the two polymers shifted towards higher values and it was not significantly influenced by the contraion nature. The intrinsic dissolution rate at infinite rotation speed (7.354<
G
∞ |
doi_str_mv | 10.1016/S0168-3659(02)00459-5 |
format | Article |
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® L100 and Eudragit
® S100 were prepared with the aim to develop new low-swellable mucoadhesive materials intended for the preparation of buccal dosage forms. The physico–chemical characterization of the copolymers and the corresponding sodium and potassium salts was performed by using Fourier-transform infrared (FT-IR) spectroscopy and thermal analysis. When ionization occurred, the carboxylic acid group absorption band (1730 cm
−1) was replaced by another characteristic band at 1560 cm
−1. After salification the
T
g of the two polymers shifted towards higher values and it was not significantly influenced by the contraion nature. The intrinsic dissolution rate at infinite rotation speed (7.354<
G
∞<9.196) was about 6- to 7-fold higher than that of a low nominal viscosity hydroxypropylmethylcelluloses (HPMC). Moreover, the Eudragit
® salts did not show an evident swelling layer and their dissolution is governed by erosion. The adhesion properties of these materials, evaluated by texture analysis, overlapped with those of Carbopol
® 934P. On the basis of the in vivo bioadhesion test, the prepared methacrylic salts can be considered interesting for the preparation of both buccal tablets and patches with good patient compliance due to their low swelling properties.</description><identifier>ISSN: 0168-3659</identifier><identifier>EISSN: 1873-4995</identifier><identifier>DOI: 10.1016/S0168-3659(02)00459-5</identifier><identifier>PMID: 12586502</identifier><identifier>CODEN: JCREEC</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Algorithms ; Biological and medical sciences ; Calorimetry, Differential Scanning ; Dosage Forms ; Eudragit ; General pharmacology ; Lactose - analogs & derivatives ; Medical sciences ; Methylcellulose - analogs & derivatives ; Mucoadhesion ; Mucoadhesive texture test ; Mucous Membrane ; Oxazines ; Pharmaceutical technology. Pharmaceutical industry ; Pharmacology. Drug treatments ; Polymethacrylic Acids - chemistry ; Solubility ; Spectroscopy, Fourier Transform Infrared ; Swelling ; Tablets ; Thermogravimetry ; Tissue Adhesives - chemistry</subject><ispartof>Journal of controlled release, 2003-02, Vol.88 (1), p.43-53</ispartof><rights>2002 Elsevier Science B.V.</rights><rights>2003 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c391t-cff05eefa885161678ef8e467b7c22f8842f194c6da053a4f392cfd0b650e1a3</citedby><cites>FETCH-LOGICAL-c391t-cff05eefa885161678ef8e467b7c22f8842f194c6da053a4f392cfd0b650e1a3</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://dx.doi.org/10.1016/S0168-3659(02)00459-5$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>315,782,786,3554,27933,27934,46004</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=14665015$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/12586502$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Cilurzo, F.</creatorcontrib><creatorcontrib>Minghetti, P.</creatorcontrib><creatorcontrib>Selmin, F.</creatorcontrib><creatorcontrib>Casiraghi, A.</creatorcontrib><creatorcontrib>Montanari, L.</creatorcontrib><title>Polymethacrylate salts as new low-swellable mucoadhesive materials</title><title>Journal of controlled release</title><addtitle>J Control Release</addtitle><description>The sodium and potassium salts of the methacrylic copolymers Eudragit
® L100 and Eudragit
® S100 were prepared with the aim to develop new low-swellable mucoadhesive materials intended for the preparation of buccal dosage forms. The physico–chemical characterization of the copolymers and the corresponding sodium and potassium salts was performed by using Fourier-transform infrared (FT-IR) spectroscopy and thermal analysis. When ionization occurred, the carboxylic acid group absorption band (1730 cm
−1) was replaced by another characteristic band at 1560 cm
−1. After salification the
T
g of the two polymers shifted towards higher values and it was not significantly influenced by the contraion nature. The intrinsic dissolution rate at infinite rotation speed (7.354<
G
∞<9.196) was about 6- to 7-fold higher than that of a low nominal viscosity hydroxypropylmethylcelluloses (HPMC). Moreover, the Eudragit
® salts did not show an evident swelling layer and their dissolution is governed by erosion. The adhesion properties of these materials, evaluated by texture analysis, overlapped with those of Carbopol
® 934P. On the basis of the in vivo bioadhesion test, the prepared methacrylic salts can be considered interesting for the preparation of both buccal tablets and patches with good patient compliance due to their low swelling properties.</description><subject>Algorithms</subject><subject>Biological and medical sciences</subject><subject>Calorimetry, Differential Scanning</subject><subject>Dosage Forms</subject><subject>Eudragit</subject><subject>General pharmacology</subject><subject>Lactose - analogs & derivatives</subject><subject>Medical sciences</subject><subject>Methylcellulose - analogs & derivatives</subject><subject>Mucoadhesion</subject><subject>Mucoadhesive texture test</subject><subject>Mucous Membrane</subject><subject>Oxazines</subject><subject>Pharmaceutical technology. Pharmaceutical industry</subject><subject>Pharmacology. Drug treatments</subject><subject>Polymethacrylic Acids - chemistry</subject><subject>Solubility</subject><subject>Spectroscopy, Fourier Transform Infrared</subject><subject>Swelling</subject><subject>Tablets</subject><subject>Thermogravimetry</subject><subject>Tissue Adhesives - chemistry</subject><issn>0168-3659</issn><issn>1873-4995</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2003</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkE1LAzEQhoMotn78BGUvih5W87HZzZ5Ei19QULD3kM1OaCTbrcm2pf_etF3s0csMA8_MvDwIXRB8RzDJ779iESnLeXmD6S3GGS9TfoCGRBQszcqSH6LhHzJAJyF8Y4w5y4pjNCCUi5xjOkRPn61bN9BNlfZrpzpIgnJdSFRIZrBKXLtKwwqcU5WDpFnoVtVTCHYZhwh7q1w4Q0cmNjjv-ymavDxPRm_p-OP1ffQ4TjUrSZdqYzAHMEoITnKSFwKMgCwvqkJTaoTIqCFlpvNaxZgqM6yk2tS4ikGBKHaKrndn5779WUDoZGOD3kSbQbsIsmCYCsZIBPkO1L4NwYORc28b5deSYLlxJ7fu5EaMxFRu3Uke9y77B4uqgXq_1cuKwFUPqKCVM17NtA17LssjRjaHHnYcRBtLC14GbWGmobYedCfr1v4T5Rc0QovN</recordid><startdate>20030214</startdate><enddate>20030214</enddate><creator>Cilurzo, F.</creator><creator>Minghetti, P.</creator><creator>Selmin, F.</creator><creator>Casiraghi, A.</creator><creator>Montanari, L.</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>20030214</creationdate><title>Polymethacrylate salts as new low-swellable mucoadhesive materials</title><author>Cilurzo, F. ; Minghetti, P. ; Selmin, F. ; Casiraghi, A. ; Montanari, L.</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c391t-cff05eefa885161678ef8e467b7c22f8842f194c6da053a4f392cfd0b650e1a3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2003</creationdate><topic>Algorithms</topic><topic>Biological and medical sciences</topic><topic>Calorimetry, Differential Scanning</topic><topic>Dosage Forms</topic><topic>Eudragit</topic><topic>General pharmacology</topic><topic>Lactose - analogs & derivatives</topic><topic>Medical sciences</topic><topic>Methylcellulose - analogs & derivatives</topic><topic>Mucoadhesion</topic><topic>Mucoadhesive texture test</topic><topic>Mucous Membrane</topic><topic>Oxazines</topic><topic>Pharmaceutical technology. Pharmaceutical industry</topic><topic>Pharmacology. Drug treatments</topic><topic>Polymethacrylic Acids - chemistry</topic><topic>Solubility</topic><topic>Spectroscopy, Fourier Transform Infrared</topic><topic>Swelling</topic><topic>Tablets</topic><topic>Thermogravimetry</topic><topic>Tissue Adhesives - chemistry</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Cilurzo, F.</creatorcontrib><creatorcontrib>Minghetti, P.</creatorcontrib><creatorcontrib>Selmin, F.</creatorcontrib><creatorcontrib>Casiraghi, A.</creatorcontrib><creatorcontrib>Montanari, L.</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>Journal of controlled release</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Cilurzo, F.</au><au>Minghetti, P.</au><au>Selmin, F.</au><au>Casiraghi, A.</au><au>Montanari, L.</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Polymethacrylate salts as new low-swellable mucoadhesive materials</atitle><jtitle>Journal of controlled release</jtitle><addtitle>J Control Release</addtitle><date>2003-02-14</date><risdate>2003</risdate><volume>88</volume><issue>1</issue><spage>43</spage><epage>53</epage><pages>43-53</pages><issn>0168-3659</issn><eissn>1873-4995</eissn><coden>JCREEC</coden><abstract>The sodium and potassium salts of the methacrylic copolymers Eudragit
® L100 and Eudragit
® S100 were prepared with the aim to develop new low-swellable mucoadhesive materials intended for the preparation of buccal dosage forms. The physico–chemical characterization of the copolymers and the corresponding sodium and potassium salts was performed by using Fourier-transform infrared (FT-IR) spectroscopy and thermal analysis. When ionization occurred, the carboxylic acid group absorption band (1730 cm
−1) was replaced by another characteristic band at 1560 cm
−1. After salification the
T
g of the two polymers shifted towards higher values and it was not significantly influenced by the contraion nature. The intrinsic dissolution rate at infinite rotation speed (7.354<
G
∞<9.196) was about 6- to 7-fold higher than that of a low nominal viscosity hydroxypropylmethylcelluloses (HPMC). Moreover, the Eudragit
® salts did not show an evident swelling layer and their dissolution is governed by erosion. The adhesion properties of these materials, evaluated by texture analysis, overlapped with those of Carbopol
® 934P. On the basis of the in vivo bioadhesion test, the prepared methacrylic salts can be considered interesting for the preparation of both buccal tablets and patches with good patient compliance due to their low swelling properties.</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>12586502</pmid><doi>10.1016/S0168-3659(02)00459-5</doi><tpages>11</tpages></addata></record> |
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subjects | Algorithms Biological and medical sciences Calorimetry, Differential Scanning Dosage Forms Eudragit General pharmacology Lactose - analogs & derivatives Medical sciences Methylcellulose - analogs & derivatives Mucoadhesion Mucoadhesive texture test Mucous Membrane Oxazines Pharmaceutical technology. Pharmaceutical industry Pharmacology. Drug treatments Polymethacrylic Acids - chemistry Solubility Spectroscopy, Fourier Transform Infrared Swelling Tablets Thermogravimetry Tissue Adhesives - chemistry |
title | Polymethacrylate salts as new low-swellable mucoadhesive materials |
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