A dynamic in vitro lipolysis model: I. Controlling the rate of lipolysis by continuous addition of calcium
Lipolysis by pancreatic lipase was investigated with the aim to establish an in vitro lipolysis model, which can be used to investigate the dissolution of poorly soluble lipophilic drug substances at controlled hydrolysis rates. The effects of three experimental parameters — the concentrations of bi...
Gespeichert in:
| Veröffentlicht in: | European journal of pharmaceutical sciences 2001-09, Vol.14 (2), p.115-122 |
|---|---|
| Hauptverfasser: | , , , |
| Format: | Artikel |
| Sprache: | eng |
| Schlagworte: | |
| Online-Zugang: | Volltext |
| Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
| container_end_page | 122 |
|---|---|
| container_issue | 2 |
| container_start_page | 115 |
| container_title | European journal of pharmaceutical sciences |
| container_volume | 14 |
| creator | Zangenberg, Niels Hønberg Müllertz, Anette Kristensen, Henning Gjelstrup Hovgaard, Lars |
| description | Lipolysis by pancreatic lipase was investigated with the aim to establish an in vitro lipolysis model, which can be used to investigate the dissolution of poorly soluble lipophilic drug substances at controlled hydrolysis rates. The effects of three experimental parameters — the concentrations of bile salts and Ca
2+ and the lipase activity — were investigated. The effect on the rate of hydrolysis of emulsified soybean oil was investigated in experiments in a pH-stat at pH 6.5 and 37°C. The free fatty acids produced by the hydrolysis were titrated at pH 6.5. It was shown that all three investigated parameters influence the initial rate of hydrolysis, whereas only the lipase activity and the concentration of Ca
2+ affect the subsequent stages. It was also shown that the rate of lipolysis can be controlled by the rate of adding Ca
2+. Thus, it is possible to design an in vitro model using readily available and inexpensive materials in which the hydrolysis rate can be controlled by the continuous addition of Ca
2+. |
| doi_str_mv | 10.1016/S0928-0987(01)00169-5 |
| format | Article |
| fullrecord | <record><control><sourceid>proquest_pubme</sourceid><recordid>TN_cdi_proquest_miscellaneous_71085334</recordid><sourceformat>XML</sourceformat><sourcesystem>PC</sourcesystem><els_id>S0928098701001695</els_id><sourcerecordid>71085334</sourcerecordid><originalsourceid>FETCH-LOGICAL-e292t-6c51babbde624f4aa36b9f9eb23ceeeaf73bd38d54621ea6745e8e0d0f2012a53</originalsourceid><addsrcrecordid>eNpN0U1P3DAQBmALtYIt5ScU-VCh9hAYO3E-eqnQqgUkpB4oZ8uxJ-0gx17iBGn_PV7YVpwsjR-NPfMy9knAuQBRX9xBJ9sCurb5AuIr5FJXqAO2Em3TFdBIeMdW_8kR-5DSAwDUbQOH7EgIBSBVs2IPl9xtgxnJcgr8ieYpck-b6LeJEh-jQ_-N35zzdQz5ynsKf_j8F_lkZuRxeGP7LbcZUVjikrhxjmaKYWes8ZaW8SN7Pxif8GR_HrP7nz9-r6-L219XN-vL2wJlJ-eitkr0pu8d1rIaKmPKuu-GDntZWkQ0Q1P2rmydqmop0NRNpbBFcDBIENKo8pidvfbdTPFxwTTrkZJF703A_DXdCGhVWVYZnu7h0o_o9Gai0Uxb_W87GXzeA5PyEMNkgqX0xuUH612f768M81RPhJNOljBYdDShnbWLpAXoXWz6JTa9y0SD0C-xaVU-A60TiiQ</addsrcrecordid><sourcetype>Aggregation Database</sourcetype><iscdi>true</iscdi><recordtype>article</recordtype><pqid>71085334</pqid></control><display><type>article</type><title>A dynamic in vitro lipolysis model: I. Controlling the rate of lipolysis by continuous addition of calcium</title><source>MEDLINE</source><source>Elsevier ScienceDirect Journals</source><creator>Zangenberg, Niels Hønberg ; Müllertz, Anette ; Kristensen, Henning Gjelstrup ; Hovgaard, Lars</creator><creatorcontrib>Zangenberg, Niels Hønberg ; Müllertz, Anette ; Kristensen, Henning Gjelstrup ; Hovgaard, Lars</creatorcontrib><description>Lipolysis by pancreatic lipase was investigated with the aim to establish an in vitro lipolysis model, which can be used to investigate the dissolution of poorly soluble lipophilic drug substances at controlled hydrolysis rates. The effects of three experimental parameters — the concentrations of bile salts and Ca
2+ and the lipase activity — were investigated. The effect on the rate of hydrolysis of emulsified soybean oil was investigated in experiments in a pH-stat at pH 6.5 and 37°C. The free fatty acids produced by the hydrolysis were titrated at pH 6.5. It was shown that all three investigated parameters influence the initial rate of hydrolysis, whereas only the lipase activity and the concentration of Ca
2+ affect the subsequent stages. It was also shown that the rate of lipolysis can be controlled by the rate of adding Ca
2+. Thus, it is possible to design an in vitro model using readily available and inexpensive materials in which the hydrolysis rate can be controlled by the continuous addition of Ca
2+.</description><identifier>ISSN: 0928-0987</identifier><identifier>EISSN: 1879-0720</identifier><identifier>DOI: 10.1016/S0928-0987(01)00169-5</identifier><identifier>PMID: 11500257</identifier><language>eng</language><publisher>Shannon: Elsevier B.V</publisher><subject>Animals ; Bile Acids and Salts - pharmacokinetics ; Bile Acids and Salts - pharmacology ; Bile salts ; Biological and medical sciences ; Calcium - pharmacokinetics ; Calcium - pharmacology ; Dissolution ; Fatty Acids - metabolism ; General pharmacology ; Hydrolysis - drug effects ; Lipase - metabolism ; Lipolysis - drug effects ; Medical sciences ; Models, Chemical ; Pancreatic lipase ; Pharmacology. Drug treatments ; Physicochemical properties. Structure-activity relationships ; Poorly water-soluble drug substances ; Rate of lipolysis ; Sodium Chloride - pharmacokinetics ; Sodium Chloride - pharmacology ; Soybean Oil - metabolism ; Swine ; Titrimetry - methods</subject><ispartof>European journal of pharmaceutical sciences, 2001-09, Vol.14 (2), p.115-122</ispartof><rights>2001 Elsevier Science B.V.</rights><rights>2001 INIST-CNRS</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktohtml>$$Uhttps://www.sciencedirect.com/science/article/pii/S0928098701001695$$EHTML$$P50$$Gelsevier$$H</linktohtml><link.rule.ids>314,776,780,3537,27903,27904,65309</link.rule.ids><backlink>$$Uhttp://pascal-francis.inist.fr/vibad/index.php?action=getRecordDetail&idt=1101264$$DView record in Pascal Francis$$Hfree_for_read</backlink><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/11500257$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Zangenberg, Niels Hønberg</creatorcontrib><creatorcontrib>Müllertz, Anette</creatorcontrib><creatorcontrib>Kristensen, Henning Gjelstrup</creatorcontrib><creatorcontrib>Hovgaard, Lars</creatorcontrib><title>A dynamic in vitro lipolysis model: I. Controlling the rate of lipolysis by continuous addition of calcium</title><title>European journal of pharmaceutical sciences</title><addtitle>Eur J Pharm Sci</addtitle><description>Lipolysis by pancreatic lipase was investigated with the aim to establish an in vitro lipolysis model, which can be used to investigate the dissolution of poorly soluble lipophilic drug substances at controlled hydrolysis rates. The effects of three experimental parameters — the concentrations of bile salts and Ca
2+ and the lipase activity — were investigated. The effect on the rate of hydrolysis of emulsified soybean oil was investigated in experiments in a pH-stat at pH 6.5 and 37°C. The free fatty acids produced by the hydrolysis were titrated at pH 6.5. It was shown that all three investigated parameters influence the initial rate of hydrolysis, whereas only the lipase activity and the concentration of Ca
2+ affect the subsequent stages. It was also shown that the rate of lipolysis can be controlled by the rate of adding Ca
2+. Thus, it is possible to design an in vitro model using readily available and inexpensive materials in which the hydrolysis rate can be controlled by the continuous addition of Ca
2+.</description><subject>Animals</subject><subject>Bile Acids and Salts - pharmacokinetics</subject><subject>Bile Acids and Salts - pharmacology</subject><subject>Bile salts</subject><subject>Biological and medical sciences</subject><subject>Calcium - pharmacokinetics</subject><subject>Calcium - pharmacology</subject><subject>Dissolution</subject><subject>Fatty Acids - metabolism</subject><subject>General pharmacology</subject><subject>Hydrolysis - drug effects</subject><subject>Lipase - metabolism</subject><subject>Lipolysis - drug effects</subject><subject>Medical sciences</subject><subject>Models, Chemical</subject><subject>Pancreatic lipase</subject><subject>Pharmacology. Drug treatments</subject><subject>Physicochemical properties. Structure-activity relationships</subject><subject>Poorly water-soluble drug substances</subject><subject>Rate of lipolysis</subject><subject>Sodium Chloride - pharmacokinetics</subject><subject>Sodium Chloride - pharmacology</subject><subject>Soybean Oil - metabolism</subject><subject>Swine</subject><subject>Titrimetry - methods</subject><issn>0928-0987</issn><issn>1879-0720</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2001</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpN0U1P3DAQBmALtYIt5ScU-VCh9hAYO3E-eqnQqgUkpB4oZ8uxJ-0gx17iBGn_PV7YVpwsjR-NPfMy9knAuQBRX9xBJ9sCurb5AuIr5FJXqAO2Em3TFdBIeMdW_8kR-5DSAwDUbQOH7EgIBSBVs2IPl9xtgxnJcgr8ieYpck-b6LeJEh-jQ_-N35zzdQz5ynsKf_j8F_lkZuRxeGP7LbcZUVjikrhxjmaKYWes8ZaW8SN7Pxif8GR_HrP7nz9-r6-L219XN-vL2wJlJ-eitkr0pu8d1rIaKmPKuu-GDntZWkQ0Q1P2rmydqmop0NRNpbBFcDBIENKo8pidvfbdTPFxwTTrkZJF703A_DXdCGhVWVYZnu7h0o_o9Gai0Uxb_W87GXzeA5PyEMNkgqX0xuUH612f768M81RPhJNOljBYdDShnbWLpAXoXWz6JTa9y0SD0C-xaVU-A60TiiQ</recordid><startdate>20010901</startdate><enddate>20010901</enddate><creator>Zangenberg, Niels Hønberg</creator><creator>Müllertz, Anette</creator><creator>Kristensen, Henning Gjelstrup</creator><creator>Hovgaard, Lars</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>7X8</scope></search><sort><creationdate>20010901</creationdate><title>A dynamic in vitro lipolysis model: I. Controlling the rate of lipolysis by continuous addition of calcium</title><author>Zangenberg, Niels Hønberg ; Müllertz, Anette ; Kristensen, Henning Gjelstrup ; Hovgaard, Lars</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-e292t-6c51babbde624f4aa36b9f9eb23ceeeaf73bd38d54621ea6745e8e0d0f2012a53</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2001</creationdate><topic>Animals</topic><topic>Bile Acids and Salts - pharmacokinetics</topic><topic>Bile Acids and Salts - pharmacology</topic><topic>Bile salts</topic><topic>Biological and medical sciences</topic><topic>Calcium - pharmacokinetics</topic><topic>Calcium - pharmacology</topic><topic>Dissolution</topic><topic>Fatty Acids - metabolism</topic><topic>General pharmacology</topic><topic>Hydrolysis - drug effects</topic><topic>Lipase - metabolism</topic><topic>Lipolysis - drug effects</topic><topic>Medical sciences</topic><topic>Models, Chemical</topic><topic>Pancreatic lipase</topic><topic>Pharmacology. Drug treatments</topic><topic>Physicochemical properties. Structure-activity relationships</topic><topic>Poorly water-soluble drug substances</topic><topic>Rate of lipolysis</topic><topic>Sodium Chloride - pharmacokinetics</topic><topic>Sodium Chloride - pharmacology</topic><topic>Soybean Oil - metabolism</topic><topic>Swine</topic><topic>Titrimetry - methods</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Zangenberg, Niels Hønberg</creatorcontrib><creatorcontrib>Müllertz, Anette</creatorcontrib><creatorcontrib>Kristensen, Henning Gjelstrup</creatorcontrib><creatorcontrib>Hovgaard, Lars</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>MEDLINE - Academic</collection><jtitle>European journal of pharmaceutical sciences</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Zangenberg, Niels Hønberg</au><au>Müllertz, Anette</au><au>Kristensen, Henning Gjelstrup</au><au>Hovgaard, Lars</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>A dynamic in vitro lipolysis model: I. Controlling the rate of lipolysis by continuous addition of calcium</atitle><jtitle>European journal of pharmaceutical sciences</jtitle><addtitle>Eur J Pharm Sci</addtitle><date>2001-09-01</date><risdate>2001</risdate><volume>14</volume><issue>2</issue><spage>115</spage><epage>122</epage><pages>115-122</pages><issn>0928-0987</issn><eissn>1879-0720</eissn><abstract>Lipolysis by pancreatic lipase was investigated with the aim to establish an in vitro lipolysis model, which can be used to investigate the dissolution of poorly soluble lipophilic drug substances at controlled hydrolysis rates. The effects of three experimental parameters — the concentrations of bile salts and Ca
2+ and the lipase activity — were investigated. The effect on the rate of hydrolysis of emulsified soybean oil was investigated in experiments in a pH-stat at pH 6.5 and 37°C. The free fatty acids produced by the hydrolysis were titrated at pH 6.5. It was shown that all three investigated parameters influence the initial rate of hydrolysis, whereas only the lipase activity and the concentration of Ca
2+ affect the subsequent stages. It was also shown that the rate of lipolysis can be controlled by the rate of adding Ca
2+. Thus, it is possible to design an in vitro model using readily available and inexpensive materials in which the hydrolysis rate can be controlled by the continuous addition of Ca
2+.</abstract><cop>Shannon</cop><pub>Elsevier B.V</pub><pmid>11500257</pmid><doi>10.1016/S0928-0987(01)00169-5</doi><tpages>8</tpages></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 0928-0987 |
| ispartof | European journal of pharmaceutical sciences, 2001-09, Vol.14 (2), p.115-122 |
| issn | 0928-0987 1879-0720 |
| language | eng |
| recordid | cdi_proquest_miscellaneous_71085334 |
| source | MEDLINE; Elsevier ScienceDirect Journals |
| subjects | Animals Bile Acids and Salts - pharmacokinetics Bile Acids and Salts - pharmacology Bile salts Biological and medical sciences Calcium - pharmacokinetics Calcium - pharmacology Dissolution Fatty Acids - metabolism General pharmacology Hydrolysis - drug effects Lipase - metabolism Lipolysis - drug effects Medical sciences Models, Chemical Pancreatic lipase Pharmacology. Drug treatments Physicochemical properties. Structure-activity relationships Poorly water-soluble drug substances Rate of lipolysis Sodium Chloride - pharmacokinetics Sodium Chloride - pharmacology Soybean Oil - metabolism Swine Titrimetry - methods |
| title | A dynamic in vitro lipolysis model: I. Controlling the rate of lipolysis by continuous addition of calcium |
| url | https://sfx.bib-bvb.de/sfx_tum?ctx_ver=Z39.88-2004&ctx_enc=info:ofi/enc:UTF-8&ctx_tim=2025-01-27T18%3A53%3A23IST&url_ver=Z39.88-2004&url_ctx_fmt=infofi/fmt:kev:mtx:ctx&rfr_id=info:sid/primo.exlibrisgroup.com:primo3-Article-proquest_pubme&rft_val_fmt=info:ofi/fmt:kev:mtx:journal&rft.genre=article&rft.atitle=A%20dynamic%20in%20vitro%20lipolysis%20model:%20I.%20Controlling%20the%20rate%20of%20lipolysis%20by%20continuous%20addition%20of%20calcium&rft.jtitle=European%20journal%20of%20pharmaceutical%20sciences&rft.au=Zangenberg,%20Niels%20H%C3%B8nberg&rft.date=2001-09-01&rft.volume=14&rft.issue=2&rft.spage=115&rft.epage=122&rft.pages=115-122&rft.issn=0928-0987&rft.eissn=1879-0720&rft_id=info:doi/10.1016/S0928-0987(01)00169-5&rft_dat=%3Cproquest_pubme%3E71085334%3C/proquest_pubme%3E%3Curl%3E%3C/url%3E&disable_directlink=true&sfx.directlink=off&sfx.report_link=0&rft_id=info:oai/&rft_pqid=71085334&rft_id=info:pmid/11500257&rft_els_id=S0928098701001695&rfr_iscdi=true |