Effect of buffer pH, buffer concentration and skin with or without enzyme inhibitors on the stability of [Arg 8]-vasopressin
The stability of [Arg 8]-vasopressin (AVP) as a function of buffer pH, buffer concentration, salt concentration, temperature, and skin with and without enzyme inhibitors was investigated. AVP was analyzed by reverse-phase high-performance liquid chromatography. The results indicated that the buffer’...
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| Veröffentlicht in: | International journal of pharmaceutics 2000-03, Vol.197 (1), p.87-93 |
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| creator | Bi, Mingda Singh, Jagdish |
| description | The stability of [Arg
8]-vasopressin (AVP) as a function of buffer pH, buffer concentration, salt concentration, temperature, and skin with and without enzyme inhibitors was investigated. AVP was analyzed by reverse-phase high-performance liquid chromatography. The results indicated that the buffer’s pH affected the degradation rate of AVP. Buffer ions (H
2PO
4
− and HPO
4
2−) and salt concentrations had no effect on the degradation of AVP. Maximum stability was achieved at pH 3.35 among pH values tested. The activation energy for the overall reaction was 21.5 kcal mol
−1 at pH 3.35. From the Arrhenius equation, the shelf-life of AVP at 25°C and pH 3.35 was calculated to be 1.38 years. The degradation rate of AVP in the skin (area: 9 cm
2, thickness: 0.5 mm) was 0.22 h
−1. Bestatin (an aminopeptidase inhibitor) had the best stabilizing effect on the degradation of AVP by skin among the three enzyme inhibitors (i.e. aprotinin, bestatin, and leupeptin) studied. The degradation rate of AVP in the skin was reduced to 0.059 h
−1 in the presence of bestatin in comparison with no inhibitor (0.22 h
−1). |
| doi_str_mv | 10.1016/S0378-5173(99)00459-7 |
| format | Article |
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8]-vasopressin (AVP) as a function of buffer pH, buffer concentration, salt concentration, temperature, and skin with and without enzyme inhibitors was investigated. AVP was analyzed by reverse-phase high-performance liquid chromatography. The results indicated that the buffer’s pH affected the degradation rate of AVP. Buffer ions (H
2PO
4
− and HPO
4
2−) and salt concentrations had no effect on the degradation of AVP. Maximum stability was achieved at pH 3.35 among pH values tested. The activation energy for the overall reaction was 21.5 kcal mol
−1 at pH 3.35. From the Arrhenius equation, the shelf-life of AVP at 25°C and pH 3.35 was calculated to be 1.38 years. The degradation rate of AVP in the skin (area: 9 cm
2, thickness: 0.5 mm) was 0.22 h
−1. Bestatin (an aminopeptidase inhibitor) had the best stabilizing effect on the degradation of AVP by skin among the three enzyme inhibitors (i.e. aprotinin, bestatin, and leupeptin) studied. The degradation rate of AVP in the skin was reduced to 0.059 h
−1 in the presence of bestatin in comparison with no inhibitor (0.22 h
−1).</description><identifier>ISSN: 0378-5173</identifier><identifier>EISSN: 1873-3476</identifier><identifier>DOI: 10.1016/S0378-5173(99)00459-7</identifier><identifier>PMID: 10704796</identifier><identifier>CODEN: IJPHDE</identifier><language>eng</language><publisher>Amsterdam: Elsevier B.V</publisher><subject>Animals ; Arginine Vasopressin - chemistry ; Biological and medical sciences ; Buffer concentration ; Buffers ; Chromatography, High Pressure Liquid ; Drug Stability ; Enzyme inhibitors ; Enzyme Inhibitors - pharmacology ; General pharmacology ; Hydrogen-Ion Concentration ; In Vitro Techniques ; Kinetics ; Medical sciences ; Pharmacology. Drug treatments ; Physicochemical properties. Structure-activity relationships ; Skin ; Skin - drug effects ; Skin - enzymology ; Stability ; Swine ; Temperature ; Vasopressin</subject><ispartof>International journal of pharmaceutics, 2000-03, Vol.197 (1), p.87-93</ispartof><rights>2000 Elsevier Science B.V.</rights><rights>2000 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c390t-bbf5cd5380c2edab41e9c921ba54c9202cc510dbbca8e7d476602fc96418f8413</citedby><cites>FETCH-LOGICAL-c390t-bbf5cd5380c2edab41e9c921ba54c9202cc510dbbca8e7d476602fc96418f8413</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0378517399004597$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27901,27902,65306</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1290018$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/10704796$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Bi, Mingda</creatorcontrib><creatorcontrib>Singh, Jagdish</creatorcontrib><title>Effect of buffer pH, buffer concentration and skin with or without enzyme inhibitors on the stability of [Arg 8]-vasopressin</title><title>International journal of pharmaceutics</title><addtitle>Int J Pharm</addtitle><description>The stability of [Arg
8]-vasopressin (AVP) as a function of buffer pH, buffer concentration, salt concentration, temperature, and skin with and without enzyme inhibitors was investigated. AVP was analyzed by reverse-phase high-performance liquid chromatography. The results indicated that the buffer’s pH affected the degradation rate of AVP. Buffer ions (H
2PO
4
− and HPO
4
2−) and salt concentrations had no effect on the degradation of AVP. Maximum stability was achieved at pH 3.35 among pH values tested. The activation energy for the overall reaction was 21.5 kcal mol
−1 at pH 3.35. From the Arrhenius equation, the shelf-life of AVP at 25°C and pH 3.35 was calculated to be 1.38 years. The degradation rate of AVP in the skin (area: 9 cm
2, thickness: 0.5 mm) was 0.22 h
−1. Bestatin (an aminopeptidase inhibitor) had the best stabilizing effect on the degradation of AVP by skin among the three enzyme inhibitors (i.e. aprotinin, bestatin, and leupeptin) studied. The degradation rate of AVP in the skin was reduced to 0.059 h
−1 in the presence of bestatin in comparison with no inhibitor (0.22 h
−1).</description><subject>Animals</subject><subject>Arginine Vasopressin - chemistry</subject><subject>Biological and medical sciences</subject><subject>Buffer concentration</subject><subject>Buffers</subject><subject>Chromatography, High Pressure Liquid</subject><subject>Drug Stability</subject><subject>Enzyme inhibitors</subject><subject>Enzyme Inhibitors - pharmacology</subject><subject>General pharmacology</subject><subject>Hydrogen-Ion Concentration</subject><subject>In Vitro Techniques</subject><subject>Kinetics</subject><subject>Medical sciences</subject><subject>Pharmacology. Drug treatments</subject><subject>Physicochemical properties. Structure-activity relationships</subject><subject>Skin</subject><subject>Skin - drug effects</subject><subject>Skin - enzymology</subject><subject>Stability</subject><subject>Swine</subject><subject>Temperature</subject><subject>Vasopressin</subject><issn>0378-5173</issn><issn>1873-3476</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2000</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNqFkU1rVTEQhoMo9lr9CUoWIgo9OjlfOVlJKbUVCi7UlUhIcibe6LnJbZJTueKPN_fD1p2rdxbPTDLPEPKUwWsGrH_zERo-VB3jzUshXgG0naj4PbJgA2-qpuX9fbK4RY7Io5S-A0Bfs-YhOWLAoeWiX5Df59aiyTRYqudSRrq-PPlbmuAN-hxVdsFT5UeafjhPf7q8pCHuMsyZov-1WSF1fum0yyEmWui8RJqy0m5yebMd_-U0fqPD1-pGpbCOmJLzj8kDq6aETw55TD6_O_90dlldfbh4f3Z6VZlGQK60tp0Zu2YAU-OodMtQGFEzrbq2JNTGdAxGrY0akI9l9x5qa0TfssEOLWuOyYv93HUM1zOmLFcuGZwm5THMSXIQbcNFV8BuD5oYUopo5Tq6lYobyUButcuddrl1KoWQO-2Sl75nhwdmvcLxn6695wI8PwAqGTXZqLxx6Y6rBQAbCvZ2j2GxceMwymQcliOMLpYryTG4__zkD7nJoKw</recordid><startdate>20000320</startdate><enddate>20000320</enddate><creator>Bi, Mingda</creator><creator>Singh, Jagdish</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>20000320</creationdate><title>Effect of buffer pH, buffer concentration and skin with or without enzyme inhibitors on the stability of [Arg 8]-vasopressin</title><author>Bi, Mingda ; Singh, Jagdish</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c390t-bbf5cd5380c2edab41e9c921ba54c9202cc510dbbca8e7d476602fc96418f8413</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2000</creationdate><topic>Animals</topic><topic>Arginine Vasopressin - chemistry</topic><topic>Biological and medical sciences</topic><topic>Buffer concentration</topic><topic>Buffers</topic><topic>Chromatography, High Pressure Liquid</topic><topic>Drug Stability</topic><topic>Enzyme inhibitors</topic><topic>Enzyme Inhibitors - pharmacology</topic><topic>General pharmacology</topic><topic>Hydrogen-Ion Concentration</topic><topic>In Vitro Techniques</topic><topic>Kinetics</topic><topic>Medical sciences</topic><topic>Pharmacology. Drug treatments</topic><topic>Physicochemical properties. Structure-activity relationships</topic><topic>Skin</topic><topic>Skin - drug effects</topic><topic>Skin - enzymology</topic><topic>Stability</topic><topic>Swine</topic><topic>Temperature</topic><topic>Vasopressin</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Bi, Mingda</creatorcontrib><creatorcontrib>Singh, Jagdish</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>Bi, Mingda</au><au>Singh, Jagdish</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Effect of buffer pH, buffer concentration and skin with or without enzyme inhibitors on the stability of [Arg 8]-vasopressin</atitle><jtitle>International journal of pharmaceutics</jtitle><addtitle>Int J Pharm</addtitle><date>2000-03-20</date><risdate>2000</risdate><volume>197</volume><issue>1</issue><spage>87</spage><epage>93</epage><pages>87-93</pages><issn>0378-5173</issn><eissn>1873-3476</eissn><coden>IJPHDE</coden><abstract>The stability of [Arg
8]-vasopressin (AVP) as a function of buffer pH, buffer concentration, salt concentration, temperature, and skin with and without enzyme inhibitors was investigated. AVP was analyzed by reverse-phase high-performance liquid chromatography. The results indicated that the buffer’s pH affected the degradation rate of AVP. Buffer ions (H
2PO
4
− and HPO
4
2−) and salt concentrations had no effect on the degradation of AVP. Maximum stability was achieved at pH 3.35 among pH values tested. The activation energy for the overall reaction was 21.5 kcal mol
−1 at pH 3.35. From the Arrhenius equation, the shelf-life of AVP at 25°C and pH 3.35 was calculated to be 1.38 years. The degradation rate of AVP in the skin (area: 9 cm
2, thickness: 0.5 mm) was 0.22 h
−1. Bestatin (an aminopeptidase inhibitor) had the best stabilizing effect on the degradation of AVP by skin among the three enzyme inhibitors (i.e. aprotinin, bestatin, and leupeptin) studied. The degradation rate of AVP in the skin was reduced to 0.059 h
−1 in the presence of bestatin in comparison with no inhibitor (0.22 h
−1).</abstract><cop>Amsterdam</cop><pub>Elsevier B.V</pub><pmid>10704796</pmid><doi>10.1016/S0378-5173(99)00459-7</doi><tpages>7</tpages></addata></record> |
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| issn | 0378-5173 1873-3476 |
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| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Arginine Vasopressin - chemistry Biological and medical sciences Buffer concentration Buffers Chromatography, High Pressure Liquid Drug Stability Enzyme inhibitors Enzyme Inhibitors - pharmacology General pharmacology Hydrogen-Ion Concentration In Vitro Techniques Kinetics Medical sciences Pharmacology. Drug treatments Physicochemical properties. Structure-activity relationships Skin Skin - drug effects Skin - enzymology Stability Swine Temperature Vasopressin |
| title | Effect of buffer pH, buffer concentration and skin with or without enzyme inhibitors on the stability of [Arg 8]-vasopressin |
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