Advantages of Efficacy and Safety of Fixed-Dose Tafluprost/Timolol Combination Over Fixed-Dose Latanoprost/Timolol Combination
To compare the safety and efficacy of fixed-dose tafluprost/timolol combination (Taf/T-FDC) with those of fixed-dose latanoprost/timolol combination (Lat/T-FDC) by measuring the intraocular pressure (IOP)-lowering effect, ocular pharmacokinetics, and ocular surface toxicity. The IOP-lowering effect...
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| Veröffentlicht in: | PloS one 2016-07, Vol.11 (7), p.e0158797 |
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| creator | Fuwa, Masahiro Ueda, Kenji Akaishi, Takahiro Yamashita, Naoko Kirihara, Tomoko Shimazaki, Atsushi Mano, Hidetoshi Kawazu, Kouichi |
| description | To compare the safety and efficacy of fixed-dose tafluprost/timolol combination (Taf/T-FDC) with those of fixed-dose latanoprost/timolol combination (Lat/T-FDC) by measuring the intraocular pressure (IOP)-lowering effect, ocular pharmacokinetics, and ocular surface toxicity.
The IOP-lowering effect of Taf/T-FDC and Lat/T-FDC in ocular normotensive monkeys was evaluated at 4 and 8 h after instillation in study A, at 12, 14, 16, and 18 h after instillation in study B, and at 24, 26, 28, and 30 h after instillation in study C. Drug penetration into the eye was evaluated by measuring the concentrations of timolol, tafluprost acid (active metabolic form of tafluprost), and latanoprost acid (active metabolic form of latanoprost) using liquid chromatography coupled with tandem mass spectrometry after single instillation of Taf/T-FDC or Lat/T-FDC to Sprague Dawley rats. Cytotoxicity following 1-30 min exposure of SV40-transformed human corneal epithelial cells to Taf/T-FDC or Lat/T-FDC was analyzed using 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium assays. Undiluted and 10-fold diluted solutions of each FDC were evaluated.
The IOP-lowering effect of Taf/T-FDC was almost equivalent to that of Lat/T-FDC at 4-8 h after instillation. The peak IOP reduction of Taf/T-FDC and Lat/T-FDC was observed at 8 h after instillation, and there is no difference between the two. The difference between them was observed at 24-30 h after instillation, and Taf/T-FDC demonstrated a significantly greater IOP-lowering effect than Lat/T-FDC at 24-30 h after instillation. The IOP-lowering effect of Taf/T-FDC was sustained up to 30 h after instillation, while that of Lat/T-FDC had almost disappeared at 28 h after instillation. Timolol concentrations in aqueous humor after Taf/T-FDC instillation were higher than those after Lat/T-FDC instillation (Cmax, 3870 ng/mL vs 1330 ng/mL; AUCinf, 3970 ng·h/mL vs 1250 ng·h/mL). The concentrations of tafluprost acid and latanoprost acid in aqueous humor after instillation of Taf/T-FDC and Lat/T-FDC, respectively, were similar to those after instillation of mono-preparations of tafluprost and latanoprost, respectively. The cytotoxic effect of Taf/T-FDC to the human corneal epithelial cells was significantly lower than that of Lat/T-FDC at all evaluated time points in both undiluted and 10-fold diluted FDCs.
Taf/T-FDC provides increased IOP-lowering effect duration and lower potential ocular surface toxicity tha |
| doi_str_mv | 10.1371/journal.pone.0158797 |
| format | Article |
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The IOP-lowering effect of Taf/T-FDC and Lat/T-FDC in ocular normotensive monkeys was evaluated at 4 and 8 h after instillation in study A, at 12, 14, 16, and 18 h after instillation in study B, and at 24, 26, 28, and 30 h after instillation in study C. Drug penetration into the eye was evaluated by measuring the concentrations of timolol, tafluprost acid (active metabolic form of tafluprost), and latanoprost acid (active metabolic form of latanoprost) using liquid chromatography coupled with tandem mass spectrometry after single instillation of Taf/T-FDC or Lat/T-FDC to Sprague Dawley rats. Cytotoxicity following 1-30 min exposure of SV40-transformed human corneal epithelial cells to Taf/T-FDC or Lat/T-FDC was analyzed using 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium assays. Undiluted and 10-fold diluted solutions of each FDC were evaluated.
The IOP-lowering effect of Taf/T-FDC was almost equivalent to that of Lat/T-FDC at 4-8 h after instillation. The peak IOP reduction of Taf/T-FDC and Lat/T-FDC was observed at 8 h after instillation, and there is no difference between the two. The difference between them was observed at 24-30 h after instillation, and Taf/T-FDC demonstrated a significantly greater IOP-lowering effect than Lat/T-FDC at 24-30 h after instillation. The IOP-lowering effect of Taf/T-FDC was sustained up to 30 h after instillation, while that of Lat/T-FDC had almost disappeared at 28 h after instillation. Timolol concentrations in aqueous humor after Taf/T-FDC instillation were higher than those after Lat/T-FDC instillation (Cmax, 3870 ng/mL vs 1330 ng/mL; AUCinf, 3970 ng·h/mL vs 1250 ng·h/mL). The concentrations of tafluprost acid and latanoprost acid in aqueous humor after instillation of Taf/T-FDC and Lat/T-FDC, respectively, were similar to those after instillation of mono-preparations of tafluprost and latanoprost, respectively. The cytotoxic effect of Taf/T-FDC to the human corneal epithelial cells was significantly lower than that of Lat/T-FDC at all evaluated time points in both undiluted and 10-fold diluted FDCs.
Taf/T-FDC provides increased IOP-lowering effect duration and lower potential ocular surface toxicity than Lat/T-FDC.</description><identifier>ISSN: 1932-6203</identifier><identifier>EISSN: 1932-6203</identifier><identifier>DOI: 10.1371/journal.pone.0158797</identifier><identifier>PMID: 27383260</identifier><language>eng</language><publisher>United States: Public Library of Science</publisher><subject>Acids ; Animals ; Antihypertensive Agents - pharmacokinetics ; Antihypertensive Agents - pharmacology ; Area Under Curve ; Bioavailability ; Biology and Life Sciences ; Cell Line ; Chromatography ; Chromatography, Liquid ; Complications and side effects ; Cornea ; Cytotoxicity ; Dilution ; Disease Models, Animal ; Dosage and administration ; Drug Combinations ; Drug dosages ; Epithelial cells ; Female ; Glaucoma ; Glaucoma - drug therapy ; Glaucoma - metabolism ; Glaucoma - physiopathology ; Humans ; Hypertension ; Intraocular pressure ; Intraocular Pressure - drug effects ; Intraocular Pressure - physiology ; Laboratories ; Latanoprost ; Liquid chromatography ; Macaca fascicularis ; Male ; Mass spectrometry ; Mass spectroscopy ; Measurement ; Medicine and Health Sciences ; Metabolic Clearance Rate ; Monkeys ; Ocular Hypertension - drug therapy ; Ocular Hypertension - metabolism ; Ocular Hypertension - physiopathology ; Ophthalmology ; Patients ; Pharmaceutical sciences ; Pharmacokinetics ; Pharmacology ; Physiological aspects ; Pressure effects ; Prostaglandins F - pharmacokinetics ; Prostaglandins F - pharmacology ; Prostaglandins F, Synthetic - pharmacokinetics ; Prostaglandins F, Synthetic - pharmacology ; R&D ; Rats, Sprague-Dawley ; Research & development ; Research and analysis methods ; Safety ; Tafluprost ; Tandem Mass Spectrometry ; Time Factors ; Timolol ; Timolol - pharmacokinetics ; Timolol - pharmacology ; Toxicity ; Treatment Outcome</subject><ispartof>PloS one, 2016-07, Vol.11 (7), p.e0158797</ispartof><rights>COPYRIGHT 2016 Public Library of Science</rights><rights>2016 Fuwa et al. This is an open access article distributed under the terms of the Creative Commons Attribution License: http://creativecommons.org/licenses/by/4.0/ (the “License”), which permits unrestricted use, distribution, and reproduction in any medium, provided the original author and source are credited. Notwithstanding the ProQuest Terms and Conditions, you may use this content in accordance with the terms of the License.</rights><rights>2016 Fuwa et al 2016 Fuwa et al</rights><lds50>peer_reviewed</lds50><oa>free_for_read</oa><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c791t-9f1d82a836100bd00f4cf62ed88e8dbdc842f4f69291de78e78090293c6eece03</citedby><cites>FETCH-LOGICAL-c791t-9f1d82a836100bd00f4cf62ed88e8dbdc842f4f69291de78e78090293c6eece03</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><linktopdf>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4934872/pdf/$$EPDF$$P50$$Gpubmedcentral$$Hfree_for_read</linktopdf><linktohtml>$$Uhttps://www.ncbi.nlm.nih.gov/pmc/articles/PMC4934872/$$EHTML$$P50$$Gpubmedcentral$$Hfree_for_read</linktohtml><link.rule.ids>230,314,723,776,780,860,881,2096,2915,23845,27901,27902,53766,53768,79342,79343</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/27383260$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Fuwa, Masahiro</creatorcontrib><creatorcontrib>Ueda, Kenji</creatorcontrib><creatorcontrib>Akaishi, Takahiro</creatorcontrib><creatorcontrib>Yamashita, Naoko</creatorcontrib><creatorcontrib>Kirihara, Tomoko</creatorcontrib><creatorcontrib>Shimazaki, Atsushi</creatorcontrib><creatorcontrib>Mano, Hidetoshi</creatorcontrib><creatorcontrib>Kawazu, Kouichi</creatorcontrib><title>Advantages of Efficacy and Safety of Fixed-Dose Tafluprost/Timolol Combination Over Fixed-Dose Latanoprost/Timolol Combination</title><title>PloS one</title><addtitle>PLoS One</addtitle><description>To compare the safety and efficacy of fixed-dose tafluprost/timolol combination (Taf/T-FDC) with those of fixed-dose latanoprost/timolol combination (Lat/T-FDC) by measuring the intraocular pressure (IOP)-lowering effect, ocular pharmacokinetics, and ocular surface toxicity.
The IOP-lowering effect of Taf/T-FDC and Lat/T-FDC in ocular normotensive monkeys was evaluated at 4 and 8 h after instillation in study A, at 12, 14, 16, and 18 h after instillation in study B, and at 24, 26, 28, and 30 h after instillation in study C. Drug penetration into the eye was evaluated by measuring the concentrations of timolol, tafluprost acid (active metabolic form of tafluprost), and latanoprost acid (active metabolic form of latanoprost) using liquid chromatography coupled with tandem mass spectrometry after single instillation of Taf/T-FDC or Lat/T-FDC to Sprague Dawley rats. Cytotoxicity following 1-30 min exposure of SV40-transformed human corneal epithelial cells to Taf/T-FDC or Lat/T-FDC was analyzed using 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium assays. Undiluted and 10-fold diluted solutions of each FDC were evaluated.
The IOP-lowering effect of Taf/T-FDC was almost equivalent to that of Lat/T-FDC at 4-8 h after instillation. The peak IOP reduction of Taf/T-FDC and Lat/T-FDC was observed at 8 h after instillation, and there is no difference between the two. The difference between them was observed at 24-30 h after instillation, and Taf/T-FDC demonstrated a significantly greater IOP-lowering effect than Lat/T-FDC at 24-30 h after instillation. The IOP-lowering effect of Taf/T-FDC was sustained up to 30 h after instillation, while that of Lat/T-FDC had almost disappeared at 28 h after instillation. Timolol concentrations in aqueous humor after Taf/T-FDC instillation were higher than those after Lat/T-FDC instillation (Cmax, 3870 ng/mL vs 1330 ng/mL; AUCinf, 3970 ng·h/mL vs 1250 ng·h/mL). The concentrations of tafluprost acid and latanoprost acid in aqueous humor after instillation of Taf/T-FDC and Lat/T-FDC, respectively, were similar to those after instillation of mono-preparations of tafluprost and latanoprost, respectively. The cytotoxic effect of Taf/T-FDC to the human corneal epithelial cells was significantly lower than that of Lat/T-FDC at all evaluated time points in both undiluted and 10-fold diluted FDCs.
Taf/T-FDC provides increased IOP-lowering effect duration and lower potential ocular surface toxicity than Lat/T-FDC.</description><subject>Acids</subject><subject>Animals</subject><subject>Antihypertensive Agents - pharmacokinetics</subject><subject>Antihypertensive Agents - pharmacology</subject><subject>Area Under Curve</subject><subject>Bioavailability</subject><subject>Biology and Life Sciences</subject><subject>Cell Line</subject><subject>Chromatography</subject><subject>Chromatography, Liquid</subject><subject>Complications and side effects</subject><subject>Cornea</subject><subject>Cytotoxicity</subject><subject>Dilution</subject><subject>Disease Models, Animal</subject><subject>Dosage and administration</subject><subject>Drug Combinations</subject><subject>Drug dosages</subject><subject>Epithelial cells</subject><subject>Female</subject><subject>Glaucoma</subject><subject>Glaucoma - drug therapy</subject><subject>Glaucoma - metabolism</subject><subject>Glaucoma - physiopathology</subject><subject>Humans</subject><subject>Hypertension</subject><subject>Intraocular pressure</subject><subject>Intraocular Pressure - drug effects</subject><subject>Intraocular Pressure - physiology</subject><subject>Laboratories</subject><subject>Latanoprost</subject><subject>Liquid chromatography</subject><subject>Macaca fascicularis</subject><subject>Male</subject><subject>Mass spectrometry</subject><subject>Mass spectroscopy</subject><subject>Measurement</subject><subject>Medicine and Health Sciences</subject><subject>Metabolic Clearance Rate</subject><subject>Monkeys</subject><subject>Ocular Hypertension - drug therapy</subject><subject>Ocular Hypertension - metabolism</subject><subject>Ocular Hypertension - physiopathology</subject><subject>Ophthalmology</subject><subject>Patients</subject><subject>Pharmaceutical sciences</subject><subject>Pharmacokinetics</subject><subject>Pharmacology</subject><subject>Physiological aspects</subject><subject>Pressure effects</subject><subject>Prostaglandins F - pharmacokinetics</subject><subject>Prostaglandins F - pharmacology</subject><subject>Prostaglandins F, Synthetic - pharmacokinetics</subject><subject>Prostaglandins F, Synthetic - pharmacology</subject><subject>R&D</subject><subject>Rats, Sprague-Dawley</subject><subject>Research & development</subject><subject>Research and analysis methods</subject><subject>Safety</subject><subject>Tafluprost</subject><subject>Tandem Mass Spectrometry</subject><subject>Time Factors</subject><subject>Timolol</subject><subject>Timolol - pharmacokinetics</subject><subject>Timolol - pharmacology</subject><subject>Toxicity</subject><subject>Treatment Outcome</subject><issn>1932-6203</issn><issn>1932-6203</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2016</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><sourceid>BENPR</sourceid><sourceid>DOA</sourceid><recordid>eNqNk9-LEzEQxxdRvLP6H4guCKIP7eXHbjZ5EUq900Kh4FVfQ5pM2hzbTW-zW64v_u2m172jKydIAgmTz3wnmcwkyVuMRpgW-OLGt3WlytHWVzBCOOeFKJ4l51hQMmQE0ecn-7PkVQg3COWUM_YyOSMF5ZQwdJ78Hpudqhq1gpB6m15a67TS-1RVJr1WFpr9wXzl7sAMv_oA6ULZst3WPjQXC7fxpS_Tid8sXaUa56t0voP6FJ-pRlX-n_zr5IVVZYA33TpIfl5dLibfh7P5t-lkPBvqQuBmKCw2nChOGUZoaRCymbaMgOEcuFkazTNiM8sEEdhAweNEAhFBNQPQgOggeX_U3ZY-yC51QWKOCBaEZXkkpkfCeHUjt7XbqHovvXLy3uDrlVR143QJMqcZoQSWXKs8A8E5NZAJnHFmctDWRK0vXbR2uQGjoWpqVfZE-yeVW8uV38lM0IwXJAp86gRqf9tCaOTGBQ1lqSrw7f29OctzHEMPkg9_oU-_rqNWKj7AVdbHuPogKsdZXmCRFwWL1OgJKg4DG6djnVkX7T2Hzz2HyDRw16xUG4KcXv_4f3b-q89-PGHXoMpmHXzZHkom9MHsCOpYYaEG-5hkjOShTR6yIQ9tIrs2iW7vTj_o0emhL-gfvNcOdw</recordid><startdate>20160706</startdate><enddate>20160706</enddate><creator>Fuwa, Masahiro</creator><creator>Ueda, Kenji</creator><creator>Akaishi, Takahiro</creator><creator>Yamashita, Naoko</creator><creator>Kirihara, Tomoko</creator><creator>Shimazaki, Atsushi</creator><creator>Mano, Hidetoshi</creator><creator>Kawazu, Kouichi</creator><general>Public Library of Science</general><general>Public Library of Science (PLoS)</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>IOV</scope><scope>ISR</scope><scope>3V.</scope><scope>7QG</scope><scope>7QL</scope><scope>7QO</scope><scope>7RV</scope><scope>7SN</scope><scope>7SS</scope><scope>7T5</scope><scope>7TG</scope><scope>7TM</scope><scope>7U9</scope><scope>7X2</scope><scope>7X7</scope><scope>7XB</scope><scope>88E</scope><scope>8AO</scope><scope>8C1</scope><scope>8FD</scope><scope>8FE</scope><scope>8FG</scope><scope>8FH</scope><scope>8FI</scope><scope>8FJ</scope><scope>8FK</scope><scope>ABJCF</scope><scope>ABUWG</scope><scope>AEUYN</scope><scope>AFKRA</scope><scope>ARAPS</scope><scope>ATCPS</scope><scope>AZQEC</scope><scope>BBNVY</scope><scope>BENPR</scope><scope>BGLVJ</scope><scope>BHPHI</scope><scope>C1K</scope><scope>CCPQU</scope><scope>D1I</scope><scope>DWQXO</scope><scope>FR3</scope><scope>FYUFA</scope><scope>GHDGH</scope><scope>GNUQQ</scope><scope>H94</scope><scope>HCIFZ</scope><scope>K9.</scope><scope>KB.</scope><scope>KB0</scope><scope>KL.</scope><scope>L6V</scope><scope>LK8</scope><scope>M0K</scope><scope>M0S</scope><scope>M1P</scope><scope>M7N</scope><scope>M7P</scope><scope>M7S</scope><scope>NAPCQ</scope><scope>P5Z</scope><scope>P62</scope><scope>P64</scope><scope>PATMY</scope><scope>PDBOC</scope><scope>PIMPY</scope><scope>PQEST</scope><scope>PQQKQ</scope><scope>PQUKI</scope><scope>PRINS</scope><scope>PTHSS</scope><scope>PYCSY</scope><scope>RC3</scope><scope>5PM</scope><scope>DOA</scope></search><sort><creationdate>20160706</creationdate><title>Advantages of Efficacy and Safety of Fixed-Dose Tafluprost/Timolol Combination Over Fixed-Dose Latanoprost/Timolol Combination</title><author>Fuwa, Masahiro ; Ueda, Kenji ; Akaishi, Takahiro ; Yamashita, Naoko ; Kirihara, Tomoko ; Shimazaki, Atsushi ; Mano, Hidetoshi ; Kawazu, Kouichi</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c791t-9f1d82a836100bd00f4cf62ed88e8dbdc842f4f69291de78e78090293c6eece03</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2016</creationdate><topic>Acids</topic><topic>Animals</topic><topic>Antihypertensive Agents - pharmacokinetics</topic><topic>Antihypertensive Agents - pharmacology</topic><topic>Area Under Curve</topic><topic>Bioavailability</topic><topic>Biology and Life Sciences</topic><topic>Cell Line</topic><topic>Chromatography</topic><topic>Chromatography, Liquid</topic><topic>Complications and side effects</topic><topic>Cornea</topic><topic>Cytotoxicity</topic><topic>Dilution</topic><topic>Disease Models, Animal</topic><topic>Dosage and administration</topic><topic>Drug Combinations</topic><topic>Drug dosages</topic><topic>Epithelial cells</topic><topic>Female</topic><topic>Glaucoma</topic><topic>Glaucoma - drug therapy</topic><topic>Glaucoma - metabolism</topic><topic>Glaucoma - physiopathology</topic><topic>Humans</topic><topic>Hypertension</topic><topic>Intraocular pressure</topic><topic>Intraocular Pressure - drug effects</topic><topic>Intraocular Pressure - physiology</topic><topic>Laboratories</topic><topic>Latanoprost</topic><topic>Liquid chromatography</topic><topic>Macaca fascicularis</topic><topic>Male</topic><topic>Mass spectrometry</topic><topic>Mass spectroscopy</topic><topic>Measurement</topic><topic>Medicine and Health Sciences</topic><topic>Metabolic Clearance Rate</topic><topic>Monkeys</topic><topic>Ocular Hypertension - drug therapy</topic><topic>Ocular Hypertension - metabolism</topic><topic>Ocular Hypertension - physiopathology</topic><topic>Ophthalmology</topic><topic>Patients</topic><topic>Pharmaceutical sciences</topic><topic>Pharmacokinetics</topic><topic>Pharmacology</topic><topic>Physiological aspects</topic><topic>Pressure effects</topic><topic>Prostaglandins F - pharmacokinetics</topic><topic>Prostaglandins F - pharmacology</topic><topic>Prostaglandins F, Synthetic - pharmacokinetics</topic><topic>Prostaglandins F, Synthetic - pharmacology</topic><topic>R&D</topic><topic>Rats, Sprague-Dawley</topic><topic>Research & development</topic><topic>Research and analysis methods</topic><topic>Safety</topic><topic>Tafluprost</topic><topic>Tandem Mass Spectrometry</topic><topic>Time Factors</topic><topic>Timolol</topic><topic>Timolol - pharmacokinetics</topic><topic>Timolol - pharmacology</topic><topic>Toxicity</topic><topic>Treatment Outcome</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Fuwa, Masahiro</creatorcontrib><creatorcontrib>Ueda, Kenji</creatorcontrib><creatorcontrib>Akaishi, Takahiro</creatorcontrib><creatorcontrib>Yamashita, Naoko</creatorcontrib><creatorcontrib>Kirihara, Tomoko</creatorcontrib><creatorcontrib>Shimazaki, Atsushi</creatorcontrib><creatorcontrib>Mano, Hidetoshi</creatorcontrib><creatorcontrib>Kawazu, Kouichi</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>Gale In Context: Opposing Viewpoints</collection><collection>Gale In Context: Science</collection><collection>ProQuest Central (Corporate)</collection><collection>Animal Behavior Abstracts</collection><collection>Bacteriology Abstracts (Microbiology B)</collection><collection>Biotechnology Research Abstracts</collection><collection>Nursing & Allied Health Database</collection><collection>Ecology Abstracts</collection><collection>Entomology Abstracts (Full archive)</collection><collection>Immunology Abstracts</collection><collection>Meteorological & Geoastrophysical Abstracts</collection><collection>Nucleic Acids Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>Agricultural Science Collection</collection><collection>Health & Medical Collection</collection><collection>ProQuest Central (purchase pre-March 2016)</collection><collection>Medical Database (Alumni Edition)</collection><collection>ProQuest Pharma Collection</collection><collection>Public Health Database</collection><collection>Technology Research Database</collection><collection>ProQuest SciTech Collection</collection><collection>ProQuest Technology Collection</collection><collection>ProQuest Natural Science Collection</collection><collection>Hospital Premium Collection</collection><collection>Hospital Premium Collection (Alumni Edition)</collection><collection>ProQuest Central (Alumni) (purchase pre-March 2016)</collection><collection>Materials Science & Engineering Collection</collection><collection>ProQuest Central (Alumni Edition)</collection><collection>ProQuest One Sustainability</collection><collection>ProQuest Central UK/Ireland</collection><collection>Advanced Technologies & Aerospace Collection</collection><collection>Agricultural & Environmental Science Collection</collection><collection>ProQuest Central Essentials</collection><collection>Biological Science Collection</collection><collection>ProQuest Central</collection><collection>Technology Collection</collection><collection>Natural Science Collection</collection><collection>Environmental Sciences and Pollution Management</collection><collection>ProQuest One Community College</collection><collection>ProQuest Materials Science Collection</collection><collection>ProQuest Central Korea</collection><collection>Engineering Research Database</collection><collection>Health Research Premium Collection</collection><collection>Health Research Premium Collection (Alumni)</collection><collection>ProQuest Central Student</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>SciTech Premium Collection</collection><collection>ProQuest Health & Medical Complete (Alumni)</collection><collection>Materials Science Database</collection><collection>Nursing & Allied Health Database (Alumni Edition)</collection><collection>Meteorological & Geoastrophysical Abstracts - Academic</collection><collection>ProQuest Engineering Collection</collection><collection>ProQuest Biological Science Collection</collection><collection>Agricultural Science Database</collection><collection>Health & Medical Collection (Alumni Edition)</collection><collection>Medical Database</collection><collection>Algology Mycology and Protozoology Abstracts (Microbiology C)</collection><collection>Biological Science Database</collection><collection>Engineering Database</collection><collection>Nursing & Allied Health Premium</collection><collection>Advanced Technologies & Aerospace Database</collection><collection>ProQuest Advanced Technologies & Aerospace Collection</collection><collection>Biotechnology and BioEngineering Abstracts</collection><collection>Environmental Science Database</collection><collection>Materials Science Collection</collection><collection>Publicly Available Content Database</collection><collection>ProQuest One Academic Eastern Edition (DO NOT USE)</collection><collection>ProQuest One Academic</collection><collection>ProQuest One Academic UKI Edition</collection><collection>ProQuest Central China</collection><collection>Engineering Collection</collection><collection>Environmental Science Collection</collection><collection>Genetics Abstracts</collection><collection>PubMed Central (Full Participant titles)</collection><collection>DOAJ Directory of Open Access Journals</collection><jtitle>PloS one</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Fuwa, Masahiro</au><au>Ueda, Kenji</au><au>Akaishi, Takahiro</au><au>Yamashita, Naoko</au><au>Kirihara, Tomoko</au><au>Shimazaki, Atsushi</au><au>Mano, Hidetoshi</au><au>Kawazu, Kouichi</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Advantages of Efficacy and Safety of Fixed-Dose Tafluprost/Timolol Combination Over Fixed-Dose Latanoprost/Timolol Combination</atitle><jtitle>PloS one</jtitle><addtitle>PLoS One</addtitle><date>2016-07-06</date><risdate>2016</risdate><volume>11</volume><issue>7</issue><spage>e0158797</spage><pages>e0158797-</pages><issn>1932-6203</issn><eissn>1932-6203</eissn><abstract>To compare the safety and efficacy of fixed-dose tafluprost/timolol combination (Taf/T-FDC) with those of fixed-dose latanoprost/timolol combination (Lat/T-FDC) by measuring the intraocular pressure (IOP)-lowering effect, ocular pharmacokinetics, and ocular surface toxicity.
The IOP-lowering effect of Taf/T-FDC and Lat/T-FDC in ocular normotensive monkeys was evaluated at 4 and 8 h after instillation in study A, at 12, 14, 16, and 18 h after instillation in study B, and at 24, 26, 28, and 30 h after instillation in study C. Drug penetration into the eye was evaluated by measuring the concentrations of timolol, tafluprost acid (active metabolic form of tafluprost), and latanoprost acid (active metabolic form of latanoprost) using liquid chromatography coupled with tandem mass spectrometry after single instillation of Taf/T-FDC or Lat/T-FDC to Sprague Dawley rats. Cytotoxicity following 1-30 min exposure of SV40-transformed human corneal epithelial cells to Taf/T-FDC or Lat/T-FDC was analyzed using 3-(4,5-dimethylthiazol-2-yl)-5-(3-carboxymethoxyphenyl)-2-(4-sulfophenyl)-2H-tetrazolium assays. Undiluted and 10-fold diluted solutions of each FDC were evaluated.
The IOP-lowering effect of Taf/T-FDC was almost equivalent to that of Lat/T-FDC at 4-8 h after instillation. The peak IOP reduction of Taf/T-FDC and Lat/T-FDC was observed at 8 h after instillation, and there is no difference between the two. The difference between them was observed at 24-30 h after instillation, and Taf/T-FDC demonstrated a significantly greater IOP-lowering effect than Lat/T-FDC at 24-30 h after instillation. The IOP-lowering effect of Taf/T-FDC was sustained up to 30 h after instillation, while that of Lat/T-FDC had almost disappeared at 28 h after instillation. Timolol concentrations in aqueous humor after Taf/T-FDC instillation were higher than those after Lat/T-FDC instillation (Cmax, 3870 ng/mL vs 1330 ng/mL; AUCinf, 3970 ng·h/mL vs 1250 ng·h/mL). The concentrations of tafluprost acid and latanoprost acid in aqueous humor after instillation of Taf/T-FDC and Lat/T-FDC, respectively, were similar to those after instillation of mono-preparations of tafluprost and latanoprost, respectively. The cytotoxic effect of Taf/T-FDC to the human corneal epithelial cells was significantly lower than that of Lat/T-FDC at all evaluated time points in both undiluted and 10-fold diluted FDCs.
Taf/T-FDC provides increased IOP-lowering effect duration and lower potential ocular surface toxicity than Lat/T-FDC.</abstract><cop>United States</cop><pub>Public Library of Science</pub><pmid>27383260</pmid><doi>10.1371/journal.pone.0158797</doi><oa>free_for_read</oa></addata></record> |
| fulltext | fulltext |
| identifier | ISSN: 1932-6203 |
| ispartof | PloS one, 2016-07, Vol.11 (7), p.e0158797 |
| issn | 1932-6203 1932-6203 |
| language | eng |
| recordid | cdi_plos_journals_1802192645 |
| source | MEDLINE; DOAJ Directory of Open Access Journals; Elektronische Zeitschriftenbibliothek - Frei zugängliche E-Journals; PubMed Central; Free Full-Text Journals in Chemistry; Public Library of Science (PLoS) |
| subjects | Acids Animals Antihypertensive Agents - pharmacokinetics Antihypertensive Agents - pharmacology Area Under Curve Bioavailability Biology and Life Sciences Cell Line Chromatography Chromatography, Liquid Complications and side effects Cornea Cytotoxicity Dilution Disease Models, Animal Dosage and administration Drug Combinations Drug dosages Epithelial cells Female Glaucoma Glaucoma - drug therapy Glaucoma - metabolism Glaucoma - physiopathology Humans Hypertension Intraocular pressure Intraocular Pressure - drug effects Intraocular Pressure - physiology Laboratories Latanoprost Liquid chromatography Macaca fascicularis Male Mass spectrometry Mass spectroscopy Measurement Medicine and Health Sciences Metabolic Clearance Rate Monkeys Ocular Hypertension - drug therapy Ocular Hypertension - metabolism Ocular Hypertension - physiopathology Ophthalmology Patients Pharmaceutical sciences Pharmacokinetics Pharmacology Physiological aspects Pressure effects Prostaglandins F - pharmacokinetics Prostaglandins F - pharmacology Prostaglandins F, Synthetic - pharmacokinetics Prostaglandins F, Synthetic - pharmacology R&D Rats, Sprague-Dawley Research & development Research and analysis methods Safety Tafluprost Tandem Mass Spectrometry Time Factors Timolol Timolol - pharmacokinetics Timolol - pharmacology Toxicity Treatment Outcome |
| title | Advantages of Efficacy and Safety of Fixed-Dose Tafluprost/Timolol Combination Over Fixed-Dose Latanoprost/Timolol Combination |
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