An exploratory study of drug concentration and inhibitory effect of cetylpyridinium chloride buccal tablets on SARS-CoV-2 infection among 10 Chinese subjects
It was evidenced that cetylpyridinium-chloride (CPC) mouthwash could inhibit SARS-COV-2 activity and reduce salivary viral load, thus reducing SARS-CoV-2 transmission. However, due to insufficient residence time in the oral cavity, CPC-containing mouthwashes have no prolonged antiviral effect. The d...
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| Veröffentlicht in: | Fundamental & clinical pharmacology 2024-06, Vol.38 (3), p.579-587 |
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| creator | Li, Yanting Xie, Zhenwei Chen, Liming Liu, Xiangxing Li, Shuang Ye, Shichun Tang, Hongyan Lee, Chongyou Gu, Qun Men, Fang Zhang, Jiaojiao Hu, Dingyuan Jiang, Yuanli Wang, Xiaochun Wang, Qian Feng, Yufei Niu, Suping Liu, Yan Fang, Yi |
| description | It was evidenced that cetylpyridinium-chloride (CPC) mouthwash could inhibit SARS-COV-2 activity and reduce salivary viral load, thus reducing SARS-CoV-2 transmission. However, due to insufficient residence time in the oral cavity, CPC-containing mouthwashes have no prolonged antiviral effect. The duration of action of the CPC buccal tablet is expected to be longer than that of the mouthwash. However, there are currently no reports on the salivary drug concentration of CPC buccal tablets.
The study aimed to investigate the salivary drug concentration of CPC buccal tablets and the antiviral effect of CPC on SARS-CoV-2 in vitro.
This is a single-dose, single-arm clinical trial, involving 10 Chinese healthy subjects who received 2-mg CPC buccal tablet to collect saliva samples and to detect saliva concentration at different timepoints within 2 h (Clinical Trial Registration Number: NCT05802628, Registration Date: April 6, 2023).
CPC concentration in saliva was detected by liquid chromatography tandem mass spectrometry (LC-MS/MS), and pharmacokinetic parameters were calculated based on the non-compartmental model. With an in vitro antiviral experiment, the activity of CPC buccal tablets against SARS-CoV-2 and its cellular toxicity was tested.
Drug concentrations in saliva at 15 min, 30 min, 1 h, 1.5 h, and 2 h after administration were 8008.33 (1042.25, 41081.11), 2093.34 (373.15, 5759.83), 1016.58 (378.66, 3480.68), 891.77 (375.66, 6322.07), and 717.43 (197.87, 2152.71) ng/mL. PK parameters of saliva concentration: C
= 8008.33 (1042.25, 41081.11) ng/mL, AUC
= 4172.37 (904.42, 13912.61) ng/mL * h, AUC
= 6712.85 (1856.77, 19971.12) ng/mL * h, T
= 1.22 (0.59, 2.83) h, T
= 0.25 (0.25, 0.25) h. As determined in in vitro experiment, CPC was active on SARS-CoV-2 with cytotoxic and inhibitory activity of CC50 = 35.75 μM (≈12155 ng/mL) and EC50 = 7.39 μM (≈2512.6 ng/mL).
The comparison between the salivary CPC concentration and EC50/CC50 values from in vitro antiviral experiments suggests that CPC buccal tablets may inhibit SARS-CoV-2 activity, and the inhibition may last for approximately 30 min without cytotoxicity. |
| doi_str_mv | 10.1111/fcp.12972 |
| format | Article |
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The study aimed to investigate the salivary drug concentration of CPC buccal tablets and the antiviral effect of CPC on SARS-CoV-2 in vitro.
This is a single-dose, single-arm clinical trial, involving 10 Chinese healthy subjects who received 2-mg CPC buccal tablet to collect saliva samples and to detect saliva concentration at different timepoints within 2 h (Clinical Trial Registration Number: NCT05802628, Registration Date: April 6, 2023).
CPC concentration in saliva was detected by liquid chromatography tandem mass spectrometry (LC-MS/MS), and pharmacokinetic parameters were calculated based on the non-compartmental model. With an in vitro antiviral experiment, the activity of CPC buccal tablets against SARS-CoV-2 and its cellular toxicity was tested.
Drug concentrations in saliva at 15 min, 30 min, 1 h, 1.5 h, and 2 h after administration were 8008.33 (1042.25, 41081.11), 2093.34 (373.15, 5759.83), 1016.58 (378.66, 3480.68), 891.77 (375.66, 6322.07), and 717.43 (197.87, 2152.71) ng/mL. PK parameters of saliva concentration: C
= 8008.33 (1042.25, 41081.11) ng/mL, AUC
= 4172.37 (904.42, 13912.61) ng/mL * h, AUC
= 6712.85 (1856.77, 19971.12) ng/mL * h, T
= 1.22 (0.59, 2.83) h, T
= 0.25 (0.25, 0.25) h. As determined in in vitro experiment, CPC was active on SARS-CoV-2 with cytotoxic and inhibitory activity of CC50 = 35.75 μM (≈12155 ng/mL) and EC50 = 7.39 μM (≈2512.6 ng/mL).
The comparison between the salivary CPC concentration and EC50/CC50 values from in vitro antiviral experiments suggests that CPC buccal tablets may inhibit SARS-CoV-2 activity, and the inhibition may last for approximately 30 min without cytotoxicity.</description><identifier>ISSN: 0767-3981</identifier><identifier>EISSN: 1472-8206</identifier><identifier>DOI: 10.1111/fcp.12972</identifier><identifier>PMID: 37985697</identifier><language>eng</language><publisher>England: Wiley Subscription Services, Inc</publisher><subject>Administration, Buccal ; Adult ; Antiviral agents ; Antiviral Agents - administration & dosage ; Antiviral Agents - pharmacokinetics ; Antiviral Agents - pharmacology ; Cetylpyridinium ; Cetylpyridinium chloride ; China ; Chlorides ; Chromatography ; Clinical trials ; COVID-19 ; COVID-19 Drug Treatment ; Cytotoxicity ; Drugs ; Female ; Humans ; Liquid chromatography ; Male ; Mass spectrometry ; Mass spectroscopy ; Mouthwashes ; Oral cavity ; Parameters ; Pharmacokinetics ; Residence time ; Saliva ; SARS-CoV-2 - drug effects ; Severe acute respiratory syndrome ; Severe acute respiratory syndrome coronavirus 2 ; Tablets ; Toxicity testing ; Viral diseases ; Viral Load - drug effects ; Young Adult</subject><ispartof>Fundamental & clinical pharmacology, 2024-06, Vol.38 (3), p.579-587</ispartof><rights>2023 Société Française de Pharmacologie et de Thérapeutique. Published by John Wiley & Sons Ltd.</rights><rights>2024 John Wiley & Sons, Ltd.</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><cites>FETCH-LOGICAL-c308t-a69f916f7469fbabae64784d10d6f468a3eac1d8b646e104116c55f4b71871783</cites><orcidid>0000-0002-3547-5829</orcidid></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,778,782,27911,27912</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/37985697$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Li, Yanting</creatorcontrib><creatorcontrib>Xie, Zhenwei</creatorcontrib><creatorcontrib>Chen, Liming</creatorcontrib><creatorcontrib>Liu, Xiangxing</creatorcontrib><creatorcontrib>Li, Shuang</creatorcontrib><creatorcontrib>Ye, Shichun</creatorcontrib><creatorcontrib>Tang, Hongyan</creatorcontrib><creatorcontrib>Lee, Chongyou</creatorcontrib><creatorcontrib>Gu, Qun</creatorcontrib><creatorcontrib>Men, Fang</creatorcontrib><creatorcontrib>Zhang, Jiaojiao</creatorcontrib><creatorcontrib>Hu, Dingyuan</creatorcontrib><creatorcontrib>Jiang, Yuanli</creatorcontrib><creatorcontrib>Wang, Xiaochun</creatorcontrib><creatorcontrib>Wang, Qian</creatorcontrib><creatorcontrib>Feng, Yufei</creatorcontrib><creatorcontrib>Niu, Suping</creatorcontrib><creatorcontrib>Liu, Yan</creatorcontrib><creatorcontrib>Fang, Yi</creatorcontrib><title>An exploratory study of drug concentration and inhibitory effect of cetylpyridinium chloride buccal tablets on SARS-CoV-2 infection among 10 Chinese subjects</title><title>Fundamental & clinical pharmacology</title><addtitle>Fundam Clin Pharmacol</addtitle><description>It was evidenced that cetylpyridinium-chloride (CPC) mouthwash could inhibit SARS-COV-2 activity and reduce salivary viral load, thus reducing SARS-CoV-2 transmission. However, due to insufficient residence time in the oral cavity, CPC-containing mouthwashes have no prolonged antiviral effect. The duration of action of the CPC buccal tablet is expected to be longer than that of the mouthwash. However, there are currently no reports on the salivary drug concentration of CPC buccal tablets.
The study aimed to investigate the salivary drug concentration of CPC buccal tablets and the antiviral effect of CPC on SARS-CoV-2 in vitro.
This is a single-dose, single-arm clinical trial, involving 10 Chinese healthy subjects who received 2-mg CPC buccal tablet to collect saliva samples and to detect saliva concentration at different timepoints within 2 h (Clinical Trial Registration Number: NCT05802628, Registration Date: April 6, 2023).
CPC concentration in saliva was detected by liquid chromatography tandem mass spectrometry (LC-MS/MS), and pharmacokinetic parameters were calculated based on the non-compartmental model. With an in vitro antiviral experiment, the activity of CPC buccal tablets against SARS-CoV-2 and its cellular toxicity was tested.
Drug concentrations in saliva at 15 min, 30 min, 1 h, 1.5 h, and 2 h after administration were 8008.33 (1042.25, 41081.11), 2093.34 (373.15, 5759.83), 1016.58 (378.66, 3480.68), 891.77 (375.66, 6322.07), and 717.43 (197.87, 2152.71) ng/mL. PK parameters of saliva concentration: C
= 8008.33 (1042.25, 41081.11) ng/mL, AUC
= 4172.37 (904.42, 13912.61) ng/mL * h, AUC
= 6712.85 (1856.77, 19971.12) ng/mL * h, T
= 1.22 (0.59, 2.83) h, T
= 0.25 (0.25, 0.25) h. As determined in in vitro experiment, CPC was active on SARS-CoV-2 with cytotoxic and inhibitory activity of CC50 = 35.75 μM (≈12155 ng/mL) and EC50 = 7.39 μM (≈2512.6 ng/mL).
The comparison between the salivary CPC concentration and EC50/CC50 values from in vitro antiviral experiments suggests that CPC buccal tablets may inhibit SARS-CoV-2 activity, and the inhibition may last for approximately 30 min without cytotoxicity.</description><subject>Administration, Buccal</subject><subject>Adult</subject><subject>Antiviral agents</subject><subject>Antiviral Agents - administration & dosage</subject><subject>Antiviral Agents - pharmacokinetics</subject><subject>Antiviral Agents - pharmacology</subject><subject>Cetylpyridinium</subject><subject>Cetylpyridinium chloride</subject><subject>China</subject><subject>Chlorides</subject><subject>Chromatography</subject><subject>Clinical trials</subject><subject>COVID-19</subject><subject>COVID-19 Drug Treatment</subject><subject>Cytotoxicity</subject><subject>Drugs</subject><subject>Female</subject><subject>Humans</subject><subject>Liquid chromatography</subject><subject>Male</subject><subject>Mass spectrometry</subject><subject>Mass spectroscopy</subject><subject>Mouthwashes</subject><subject>Oral cavity</subject><subject>Parameters</subject><subject>Pharmacokinetics</subject><subject>Residence time</subject><subject>Saliva</subject><subject>SARS-CoV-2 - drug effects</subject><subject>Severe acute respiratory syndrome</subject><subject>Severe acute respiratory syndrome coronavirus 2</subject><subject>Tablets</subject><subject>Toxicity testing</subject><subject>Viral diseases</subject><subject>Viral Load - drug effects</subject><subject>Young Adult</subject><issn>0767-3981</issn><issn>1472-8206</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2024</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNpdkclqHDEQhkWIicdODnmBIMglPrQjdau1HIchGxgMcZJro9bi0dAtdbRA-mHyrtaMnRxclyqorz4KfgDeYnSNa320arnGrWDtC7DBhLUNbxF9CTaIUdZ0guNzcJHSASHMEKavwHnHBO-pYBvwd-uh-bNMIcoc4gpTLnqFwUIdyz1UwSvjc9254KH0Gjq_d6M7ocZao_KRVSav07JGp513ZYZqX31OGzgWpeQEsxwnkxOsjrvt97tmF341bVUd70_iOfh7iBHc7Z03ycBUxkPdpdfgzMopmTdP_RL8_Pzpx-5rc3P75dtue9OoDvHcSCqswNQyUodRjtJQwjjRGGlqCeWyM1JhzUdKqMGIYExV31syMswZZry7BB8evUsMv4tJeZhdUmaapDehpKHlom0ZJqKv6Ptn6CGU6Ot3Q4d60h3tolJXj5SKIaVo7LBEN8u4DhgNx8yGmtlwyqyy756MZZyN_k_-C6l7AFexkzA</recordid><startdate>202406</startdate><enddate>202406</enddate><creator>Li, Yanting</creator><creator>Xie, Zhenwei</creator><creator>Chen, Liming</creator><creator>Liu, Xiangxing</creator><creator>Li, Shuang</creator><creator>Ye, Shichun</creator><creator>Tang, Hongyan</creator><creator>Lee, Chongyou</creator><creator>Gu, Qun</creator><creator>Men, Fang</creator><creator>Zhang, Jiaojiao</creator><creator>Hu, Dingyuan</creator><creator>Jiang, Yuanli</creator><creator>Wang, Xiaochun</creator><creator>Wang, Qian</creator><creator>Feng, Yufei</creator><creator>Niu, Suping</creator><creator>Liu, Yan</creator><creator>Fang, Yi</creator><general>Wiley Subscription Services, Inc</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>7QL</scope><scope>7QO</scope><scope>7T7</scope><scope>7U7</scope><scope>7U9</scope><scope>8FD</scope><scope>C1K</scope><scope>FR3</scope><scope>H94</scope><scope>P64</scope><scope>7X8</scope><orcidid>https://orcid.org/0000-0002-3547-5829</orcidid></search><sort><creationdate>202406</creationdate><title>An exploratory study of drug concentration and inhibitory effect of cetylpyridinium chloride buccal tablets on SARS-CoV-2 infection among 10 Chinese subjects</title><author>Li, Yanting ; Xie, Zhenwei ; Chen, Liming ; Liu, Xiangxing ; Li, Shuang ; Ye, Shichun ; Tang, Hongyan ; Lee, Chongyou ; Gu, Qun ; Men, Fang ; Zhang, Jiaojiao ; Hu, Dingyuan ; Jiang, Yuanli ; Wang, Xiaochun ; Wang, Qian ; Feng, Yufei ; Niu, Suping ; Liu, Yan ; Fang, Yi</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c308t-a69f916f7469fbabae64784d10d6f468a3eac1d8b646e104116c55f4b71871783</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2024</creationdate><topic>Administration, Buccal</topic><topic>Adult</topic><topic>Antiviral agents</topic><topic>Antiviral Agents - administration & dosage</topic><topic>Antiviral Agents - pharmacokinetics</topic><topic>Antiviral Agents - pharmacology</topic><topic>Cetylpyridinium</topic><topic>Cetylpyridinium chloride</topic><topic>China</topic><topic>Chlorides</topic><topic>Chromatography</topic><topic>Clinical trials</topic><topic>COVID-19</topic><topic>COVID-19 Drug Treatment</topic><topic>Cytotoxicity</topic><topic>Drugs</topic><topic>Female</topic><topic>Humans</topic><topic>Liquid chromatography</topic><topic>Male</topic><topic>Mass spectrometry</topic><topic>Mass spectroscopy</topic><topic>Mouthwashes</topic><topic>Oral cavity</topic><topic>Parameters</topic><topic>Pharmacokinetics</topic><topic>Residence time</topic><topic>Saliva</topic><topic>SARS-CoV-2 - drug effects</topic><topic>Severe acute respiratory syndrome</topic><topic>Severe acute respiratory syndrome coronavirus 2</topic><topic>Tablets</topic><topic>Toxicity testing</topic><topic>Viral diseases</topic><topic>Viral Load - drug effects</topic><topic>Young Adult</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Li, Yanting</creatorcontrib><creatorcontrib>Xie, Zhenwei</creatorcontrib><creatorcontrib>Chen, Liming</creatorcontrib><creatorcontrib>Liu, Xiangxing</creatorcontrib><creatorcontrib>Li, Shuang</creatorcontrib><creatorcontrib>Ye, Shichun</creatorcontrib><creatorcontrib>Tang, Hongyan</creatorcontrib><creatorcontrib>Lee, Chongyou</creatorcontrib><creatorcontrib>Gu, Qun</creatorcontrib><creatorcontrib>Men, Fang</creatorcontrib><creatorcontrib>Zhang, Jiaojiao</creatorcontrib><creatorcontrib>Hu, Dingyuan</creatorcontrib><creatorcontrib>Jiang, Yuanli</creatorcontrib><creatorcontrib>Wang, Xiaochun</creatorcontrib><creatorcontrib>Wang, Qian</creatorcontrib><creatorcontrib>Feng, Yufei</creatorcontrib><creatorcontrib>Niu, Suping</creatorcontrib><creatorcontrib>Liu, Yan</creatorcontrib><creatorcontrib>Fang, Yi</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Bacteriology Abstracts (Microbiology B)</collection><collection>Biotechnology Research Abstracts</collection><collection>Industrial and Applied Microbiology Abstracts (Microbiology A)</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>MEDLINE - Academic</collection><jtitle>Fundamental & clinical pharmacology</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Li, Yanting</au><au>Xie, Zhenwei</au><au>Chen, Liming</au><au>Liu, Xiangxing</au><au>Li, Shuang</au><au>Ye, Shichun</au><au>Tang, Hongyan</au><au>Lee, Chongyou</au><au>Gu, Qun</au><au>Men, Fang</au><au>Zhang, Jiaojiao</au><au>Hu, Dingyuan</au><au>Jiang, Yuanli</au><au>Wang, Xiaochun</au><au>Wang, Qian</au><au>Feng, Yufei</au><au>Niu, Suping</au><au>Liu, Yan</au><au>Fang, Yi</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>An exploratory study of drug concentration and inhibitory effect of cetylpyridinium chloride buccal tablets on SARS-CoV-2 infection among 10 Chinese subjects</atitle><jtitle>Fundamental & clinical pharmacology</jtitle><addtitle>Fundam Clin Pharmacol</addtitle><date>2024-06</date><risdate>2024</risdate><volume>38</volume><issue>3</issue><spage>579</spage><epage>587</epage><pages>579-587</pages><issn>0767-3981</issn><eissn>1472-8206</eissn><abstract>It was evidenced that cetylpyridinium-chloride (CPC) mouthwash could inhibit SARS-COV-2 activity and reduce salivary viral load, thus reducing SARS-CoV-2 transmission. However, due to insufficient residence time in the oral cavity, CPC-containing mouthwashes have no prolonged antiviral effect. The duration of action of the CPC buccal tablet is expected to be longer than that of the mouthwash. However, there are currently no reports on the salivary drug concentration of CPC buccal tablets.
The study aimed to investigate the salivary drug concentration of CPC buccal tablets and the antiviral effect of CPC on SARS-CoV-2 in vitro.
This is a single-dose, single-arm clinical trial, involving 10 Chinese healthy subjects who received 2-mg CPC buccal tablet to collect saliva samples and to detect saliva concentration at different timepoints within 2 h (Clinical Trial Registration Number: NCT05802628, Registration Date: April 6, 2023).
CPC concentration in saliva was detected by liquid chromatography tandem mass spectrometry (LC-MS/MS), and pharmacokinetic parameters were calculated based on the non-compartmental model. With an in vitro antiviral experiment, the activity of CPC buccal tablets against SARS-CoV-2 and its cellular toxicity was tested.
Drug concentrations in saliva at 15 min, 30 min, 1 h, 1.5 h, and 2 h after administration were 8008.33 (1042.25, 41081.11), 2093.34 (373.15, 5759.83), 1016.58 (378.66, 3480.68), 891.77 (375.66, 6322.07), and 717.43 (197.87, 2152.71) ng/mL. PK parameters of saliva concentration: C
= 8008.33 (1042.25, 41081.11) ng/mL, AUC
= 4172.37 (904.42, 13912.61) ng/mL * h, AUC
= 6712.85 (1856.77, 19971.12) ng/mL * h, T
= 1.22 (0.59, 2.83) h, T
= 0.25 (0.25, 0.25) h. As determined in in vitro experiment, CPC was active on SARS-CoV-2 with cytotoxic and inhibitory activity of CC50 = 35.75 μM (≈12155 ng/mL) and EC50 = 7.39 μM (≈2512.6 ng/mL).
The comparison between the salivary CPC concentration and EC50/CC50 values from in vitro antiviral experiments suggests that CPC buccal tablets may inhibit SARS-CoV-2 activity, and the inhibition may last for approximately 30 min without cytotoxicity.</abstract><cop>England</cop><pub>Wiley Subscription Services, Inc</pub><pmid>37985697</pmid><doi>10.1111/fcp.12972</doi><tpages>9</tpages><orcidid>https://orcid.org/0000-0002-3547-5829</orcidid><oa>free_for_read</oa></addata></record> |
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| ispartof | Fundamental & clinical pharmacology, 2024-06, Vol.38 (3), p.579-587 |
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| source | MEDLINE; Wiley Online Library Journals Frontfile Complete |
| subjects | Administration, Buccal Adult Antiviral agents Antiviral Agents - administration & dosage Antiviral Agents - pharmacokinetics Antiviral Agents - pharmacology Cetylpyridinium Cetylpyridinium chloride China Chlorides Chromatography Clinical trials COVID-19 COVID-19 Drug Treatment Cytotoxicity Drugs Female Humans Liquid chromatography Male Mass spectrometry Mass spectroscopy Mouthwashes Oral cavity Parameters Pharmacokinetics Residence time Saliva SARS-CoV-2 - drug effects Severe acute respiratory syndrome Severe acute respiratory syndrome coronavirus 2 Tablets Toxicity testing Viral diseases Viral Load - drug effects Young Adult |
| title | An exploratory study of drug concentration and inhibitory effect of cetylpyridinium chloride buccal tablets on SARS-CoV-2 infection among 10 Chinese subjects |
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