An analysis of the biopharmaceutical behaviour of proton pump inhibitors with different physicochemical properties
At present, little information on the biopharmaceutical behaviour of proton pump inhibitors (PPIs) describing their absorption and biodistribution in vivo has been reported because the extreme instability of PPIs in the gastrointestinal environment makes it difficult to analyze such behaviour. In th...
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| Veröffentlicht in: | Life sciences (1973) 2021-12, Vol.286, p.120042-120042, Article 120042 |
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| container_title | Life sciences (1973) |
| container_volume | 286 |
| creator | Jiang, Xindong Shen, Tianxiang Jin, Zhaolei Li, Chunlong Li, Qingpo Qiu, Weigen Cui, Yannan Han, Zhihui Hou, Xuemei You, Jian |
| description | At present, little information on the biopharmaceutical behaviour of proton pump inhibitors (PPIs) describing their absorption and biodistribution in vivo has been reported because the extreme instability of PPIs in the gastrointestinal environment makes it difficult to analyze such behaviour. In this work, a modified rat in situ intestinal perfusion model was employed to investigate absorption in the gastrointestinal tract and subsequent biodistribution of several PPIs (ilaprazole, esomeprazole and rabeprazole), which have different physicochemical properties. Our data indicated that PPIs exhibited significantly enhanced absorption rates in the whole intestine, including the duodenum, jejunum, ileum and colon, corresponding to the increase in the oil-water partition coefficient (LogP). PPIs and corresponding salt types showed no obvious differences in absorption, implying that solubility changes in the PPI have little effect on its absorption in the gastrointestinal tract. Among these PPIs, ilaprazole presented a more stable intestinal absorption behaviour, as well as more distribution and longer residence time in the stomach by HPLC-MS/MS analysis and radioactivity counts after 14C radiolabelling. These results may be useful information for PPI optimization and oral formulation design. |
| doi_str_mv | 10.1016/j.lfs.2021.120042 |
| format | Article |
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In this work, a modified rat in situ intestinal perfusion model was employed to investigate absorption in the gastrointestinal tract and subsequent biodistribution of several PPIs (ilaprazole, esomeprazole and rabeprazole), which have different physicochemical properties. Our data indicated that PPIs exhibited significantly enhanced absorption rates in the whole intestine, including the duodenum, jejunum, ileum and colon, corresponding to the increase in the oil-water partition coefficient (LogP). PPIs and corresponding salt types showed no obvious differences in absorption, implying that solubility changes in the PPI have little effect on its absorption in the gastrointestinal tract. Among these PPIs, ilaprazole presented a more stable intestinal absorption behaviour, as well as more distribution and longer residence time in the stomach by HPLC-MS/MS analysis and radioactivity counts after 14C radiolabelling. These results may be useful information for PPI optimization and oral formulation design.</description><identifier>ISSN: 0024-3205</identifier><identifier>EISSN: 1879-0631</identifier><identifier>DOI: 10.1016/j.lfs.2021.120042</identifier><identifier>PMID: 34678262</identifier><language>eng</language><publisher>Netherlands: Elsevier Inc</publisher><subject>14C-radiolabelled ; 2-Pyridinylmethylsulfinylbenzimidazoles - pharmacology ; Absorption ; Absorption, Physicochemical - drug effects ; Absorption, Physicochemical - physiology ; Adsorption ; Animals ; Biodistribution ; Biological Products - pharmacokinetics ; Biological Products - pharmacology ; Biopharmaceuticals ; Biopharmaceutics ; Chemical Phenomena - drug effects ; China ; Colon ; Design optimization ; Duodenum ; Esomeprazole - pharmacology ; Female ; Gastrointestinal system ; Gastrointestinal tract ; High-performance liquid chromatography ; Ileum ; Ileum - metabolism ; Inhibitors ; Intestinal absorption ; Intestinal Absorption - drug effects ; Intestinal Absorption - physiology ; Intestine ; Jejunum ; Jejunum - metabolism ; Liquid chromatography ; Male ; Omeprazole ; Oral absorption behaviour ; Perfusion ; Physicochemical properties ; Proton pump inhibitors ; Proton Pump Inhibitors - metabolism ; Proton Pump Inhibitors - pharmacokinetics ; Proton Pump Inhibitors - pharmacology ; Protons ; Rabeprazole - pharmacology ; Radioactivity ; Radiolabelling ; Rats ; Rats, Sprague-Dawley ; Stability analysis ; Tandem Mass Spectrometry - methods ; Tissue Distribution - drug effects</subject><ispartof>Life sciences (1973), 2021-12, Vol.286, p.120042-120042, Article 120042</ispartof><rights>2021 Elsevier Inc.</rights><rights>Copyright © 2021 Elsevier Inc. 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In this work, a modified rat in situ intestinal perfusion model was employed to investigate absorption in the gastrointestinal tract and subsequent biodistribution of several PPIs (ilaprazole, esomeprazole and rabeprazole), which have different physicochemical properties. Our data indicated that PPIs exhibited significantly enhanced absorption rates in the whole intestine, including the duodenum, jejunum, ileum and colon, corresponding to the increase in the oil-water partition coefficient (LogP). PPIs and corresponding salt types showed no obvious differences in absorption, implying that solubility changes in the PPI have little effect on its absorption in the gastrointestinal tract. Among these PPIs, ilaprazole presented a more stable intestinal absorption behaviour, as well as more distribution and longer residence time in the stomach by HPLC-MS/MS analysis and radioactivity counts after 14C radiolabelling. These results may be useful information for PPI optimization and oral formulation design.</description><subject>14C-radiolabelled</subject><subject>2-Pyridinylmethylsulfinylbenzimidazoles - pharmacology</subject><subject>Absorption</subject><subject>Absorption, Physicochemical - drug effects</subject><subject>Absorption, Physicochemical - physiology</subject><subject>Adsorption</subject><subject>Animals</subject><subject>Biodistribution</subject><subject>Biological Products - pharmacokinetics</subject><subject>Biological Products - pharmacology</subject><subject>Biopharmaceuticals</subject><subject>Biopharmaceutics</subject><subject>Chemical Phenomena - drug effects</subject><subject>China</subject><subject>Colon</subject><subject>Design optimization</subject><subject>Duodenum</subject><subject>Esomeprazole - pharmacology</subject><subject>Female</subject><subject>Gastrointestinal system</subject><subject>Gastrointestinal tract</subject><subject>High-performance liquid chromatography</subject><subject>Ileum</subject><subject>Ileum - metabolism</subject><subject>Inhibitors</subject><subject>Intestinal absorption</subject><subject>Intestinal Absorption - drug effects</subject><subject>Intestinal Absorption - physiology</subject><subject>Intestine</subject><subject>Jejunum</subject><subject>Jejunum - metabolism</subject><subject>Liquid chromatography</subject><subject>Male</subject><subject>Omeprazole</subject><subject>Oral absorption behaviour</subject><subject>Perfusion</subject><subject>Physicochemical properties</subject><subject>Proton pump inhibitors</subject><subject>Proton Pump Inhibitors - metabolism</subject><subject>Proton Pump Inhibitors - pharmacokinetics</subject><subject>Proton Pump Inhibitors - pharmacology</subject><subject>Protons</subject><subject>Rabeprazole - pharmacology</subject><subject>Radioactivity</subject><subject>Radiolabelling</subject><subject>Rats</subject><subject>Rats, Sprague-Dawley</subject><subject>Stability analysis</subject><subject>Tandem Mass Spectrometry - methods</subject><subject>Tissue Distribution - drug effects</subject><issn>0024-3205</issn><issn>1879-0631</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2021</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kcFu1DAURS0EotPCB7BBltiwyfBsx04iVlVFC1IlNu3acpxnxaMkDrZT1L-vh2lZsGBlWT73Wu8dQj4w2DNg6sthP7m058DZnnGAmr8iO9Y2XQVKsNdkB8DrSnCQZ-Q8pQMASNmIt-RM1KppueI7Ei8XahYzPSafaHA0j0h7H9bRxNlY3LK3ZqI9jubBhy0ekTWGHBa6bvNK_TL63ucQE_3t80gH7xxGXDJdx1Jpgx1x_lNRUivG7DG9I2-cmRK-fz4vyP31t7ur79Xtz5sfV5e3lRUty9XQNegMmDIDCKdcPyg00nR1eR4UGGxb1zQOlYJWgeosU42Qg-hcuffMiQvy-dRbvv61Ycp69sniNJkFw5Y0l23dAu86WdBP_6CHMmxZS6EUSCW7mteFYifKxpBSRKfX6GcTHzUDfRSiD7oI0Uch-iSkZD4-N2_9jMPfxIuBAnw9AVhW8eAx6mQ9LhYHH9FmPQT_n_onWNWc_A</recordid><startdate>20211201</startdate><enddate>20211201</enddate><creator>Jiang, Xindong</creator><creator>Shen, Tianxiang</creator><creator>Jin, Zhaolei</creator><creator>Li, Chunlong</creator><creator>Li, Qingpo</creator><creator>Qiu, Weigen</creator><creator>Cui, Yannan</creator><creator>Han, Zhihui</creator><creator>Hou, Xuemei</creator><creator>You, Jian</creator><general>Elsevier Inc</general><general>Elsevier BV</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>7QP</scope><scope>7QR</scope><scope>7TK</scope><scope>7U7</scope><scope>7U9</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>H94</scope><scope>P64</scope><scope>RC3</scope><scope>7X8</scope></search><sort><creationdate>20211201</creationdate><title>An analysis of the biopharmaceutical behaviour of proton pump inhibitors with different physicochemical properties</title><author>Jiang, Xindong ; Shen, Tianxiang ; Jin, Zhaolei ; Li, Chunlong ; Li, Qingpo ; Qiu, Weigen ; Cui, Yannan ; Han, Zhihui ; Hou, Xuemei ; You, Jian</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c381t-d97efa0a02403f6fbd6ea5a94c38d60ae88f77fe66086069c16735d39f086b1f3</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2021</creationdate><topic>14C-radiolabelled</topic><topic>2-Pyridinylmethylsulfinylbenzimidazoles - pharmacology</topic><topic>Absorption</topic><topic>Absorption, Physicochemical - drug effects</topic><topic>Absorption, Physicochemical - physiology</topic><topic>Adsorption</topic><topic>Animals</topic><topic>Biodistribution</topic><topic>Biological Products - pharmacokinetics</topic><topic>Biological Products - pharmacology</topic><topic>Biopharmaceuticals</topic><topic>Biopharmaceutics</topic><topic>Chemical Phenomena - drug effects</topic><topic>China</topic><topic>Colon</topic><topic>Design optimization</topic><topic>Duodenum</topic><topic>Esomeprazole - pharmacology</topic><topic>Female</topic><topic>Gastrointestinal system</topic><topic>Gastrointestinal tract</topic><topic>High-performance liquid chromatography</topic><topic>Ileum</topic><topic>Ileum - metabolism</topic><topic>Inhibitors</topic><topic>Intestinal absorption</topic><topic>Intestinal Absorption - drug effects</topic><topic>Intestinal Absorption - physiology</topic><topic>Intestine</topic><topic>Jejunum</topic><topic>Jejunum - metabolism</topic><topic>Liquid chromatography</topic><topic>Male</topic><topic>Omeprazole</topic><topic>Oral absorption behaviour</topic><topic>Perfusion</topic><topic>Physicochemical properties</topic><topic>Proton pump inhibitors</topic><topic>Proton Pump Inhibitors - metabolism</topic><topic>Proton Pump Inhibitors - pharmacokinetics</topic><topic>Proton Pump Inhibitors - pharmacology</topic><topic>Protons</topic><topic>Rabeprazole - pharmacology</topic><topic>Radioactivity</topic><topic>Radiolabelling</topic><topic>Rats</topic><topic>Rats, Sprague-Dawley</topic><topic>Stability analysis</topic><topic>Tandem Mass Spectrometry - methods</topic><topic>Tissue Distribution - drug effects</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Jiang, Xindong</creatorcontrib><creatorcontrib>Shen, Tianxiang</creatorcontrib><creatorcontrib>Jin, Zhaolei</creatorcontrib><creatorcontrib>Li, Chunlong</creatorcontrib><creatorcontrib>Li, Qingpo</creatorcontrib><creatorcontrib>Qiu, Weigen</creatorcontrib><creatorcontrib>Cui, Yannan</creatorcontrib><creatorcontrib>Han, Zhihui</creatorcontrib><creatorcontrib>Hou, Xuemei</creatorcontrib><creatorcontrib>You, Jian</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Calcium & Calcified Tissue Abstracts</collection><collection>Chemoreception Abstracts</collection><collection>Neurosciences Abstracts</collection><collection>Toxicology Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>Technology Research Database</collection><collection>Environmental Sciences and Pollution Management</collection><collection>Engineering Research Database</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>Genetics Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Life sciences (1973)</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Jiang, Xindong</au><au>Shen, Tianxiang</au><au>Jin, Zhaolei</au><au>Li, Chunlong</au><au>Li, Qingpo</au><au>Qiu, Weigen</au><au>Cui, Yannan</au><au>Han, Zhihui</au><au>Hou, Xuemei</au><au>You, Jian</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>An analysis of the biopharmaceutical behaviour of proton pump inhibitors with different physicochemical properties</atitle><jtitle>Life sciences (1973)</jtitle><addtitle>Life Sci</addtitle><date>2021-12-01</date><risdate>2021</risdate><volume>286</volume><spage>120042</spage><epage>120042</epage><pages>120042-120042</pages><artnum>120042</artnum><issn>0024-3205</issn><eissn>1879-0631</eissn><abstract>At present, little information on the biopharmaceutical behaviour of proton pump inhibitors (PPIs) describing their absorption and biodistribution in vivo has been reported because the extreme instability of PPIs in the gastrointestinal environment makes it difficult to analyze such behaviour. In this work, a modified rat in situ intestinal perfusion model was employed to investigate absorption in the gastrointestinal tract and subsequent biodistribution of several PPIs (ilaprazole, esomeprazole and rabeprazole), which have different physicochemical properties. Our data indicated that PPIs exhibited significantly enhanced absorption rates in the whole intestine, including the duodenum, jejunum, ileum and colon, corresponding to the increase in the oil-water partition coefficient (LogP). PPIs and corresponding salt types showed no obvious differences in absorption, implying that solubility changes in the PPI have little effect on its absorption in the gastrointestinal tract. Among these PPIs, ilaprazole presented a more stable intestinal absorption behaviour, as well as more distribution and longer residence time in the stomach by HPLC-MS/MS analysis and radioactivity counts after 14C radiolabelling. These results may be useful information for PPI optimization and oral formulation design.</abstract><cop>Netherlands</cop><pub>Elsevier Inc</pub><pmid>34678262</pmid><doi>10.1016/j.lfs.2021.120042</doi><tpages>1</tpages></addata></record> |
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| ispartof | Life sciences (1973), 2021-12, Vol.286, p.120042-120042, Article 120042 |
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| subjects | 14C-radiolabelled 2-Pyridinylmethylsulfinylbenzimidazoles - pharmacology Absorption Absorption, Physicochemical - drug effects Absorption, Physicochemical - physiology Adsorption Animals Biodistribution Biological Products - pharmacokinetics Biological Products - pharmacology Biopharmaceuticals Biopharmaceutics Chemical Phenomena - drug effects China Colon Design optimization Duodenum Esomeprazole - pharmacology Female Gastrointestinal system Gastrointestinal tract High-performance liquid chromatography Ileum Ileum - metabolism Inhibitors Intestinal absorption Intestinal Absorption - drug effects Intestinal Absorption - physiology Intestine Jejunum Jejunum - metabolism Liquid chromatography Male Omeprazole Oral absorption behaviour Perfusion Physicochemical properties Proton pump inhibitors Proton Pump Inhibitors - metabolism Proton Pump Inhibitors - pharmacokinetics Proton Pump Inhibitors - pharmacology Protons Rabeprazole - pharmacology Radioactivity Radiolabelling Rats Rats, Sprague-Dawley Stability analysis Tandem Mass Spectrometry - methods Tissue Distribution - drug effects |
| title | An analysis of the biopharmaceutical behaviour of proton pump inhibitors with different physicochemical properties |
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