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Mat Luoda Tari Train the Time Table That MAT LUODA TARI TRAINUS 20170246235A1 THE TIME TABLE THAT (19 ) United States (12 ) Patent Application Publication (10 ) Pub. No. : US 2017/ 0246235 A1 DUFFIELD (43 ) Pub. Date : Aug . 31, 2017 ( 54 ) GREEN TEA COMPOSITIONS A61K 47/ 14 ( 2006 . 01 ) (71 ) Applicant: Plandai Biotechnology Inc . , Goodyear, A61K 47 / 10 ( 2006 .01 ) AZ (US ) A61K 47 / 12 ( 2006 .01 ) A61K 47744 (2006 . 01) ( 72 ) Inventor: Roger DUFFIELD , London (GB ) A23F 3 / 18 (2006 . 01) A61K 9 / 00 ( 2006 .01 ) (21 ) Appl. No. : 15 /508 , 450 (52 ) U .S . CI. ( 22 ) PCT Filed : Sep . 2 , 2015 CPC .. .. .. A61K 36 / 82 ( 2013 . 01 ) ; A23F 3 / 18 (2013 .01 ) ; A61K 31/ 353 ( 2013 .01 ) ; A61K ( 86 ) PCT No. : PCT/ US2015 / 048190 9 /0014 (2013 .01 ) ; A61K 9 /0053 (2013 .01 ) ; $ 371 ( c ) ( 1 ) , A61K 47 / 10 ( 2013 .01 ) ; A61K 47 /12 ( 2013 .01 ) ; ( 2 ) Date : Mar. 2 , 2017 A61K 47/ 44 ( 2013 .01 ) ; A61K 47/ 14 ( 2013 .01 ) Related U . S . Application Data (57 ) ABSTRACT (60 ) Provisional application No . 62 /045 ,419 , filed on Sep . 3 , 2014 , provisional application No . 62 /077 ,634 , filed Disclosed herein are green tea plant material extracts , and on Nov. 10 , 2014 , provisional application No . 62 /117 , methods of using the extracts , comprising at least one green 390 , filed on Feb . 17 , 2015 , provisional application tea catechin selected from the group consisting of epi No . 62 / 173 , 489, filed on Jun . 10 , 2015 . gallocatechin , catechin , epicatechin , epigallocatechin - 3 - gal Publication Classification late , gallocatechin gallate , epicatechin - 3 -gallate , catechin (51 ) Int . Cl. gallate , and gallocatechin , wherein the compositions of the A61K 36 / 82 ( 2006 .01 ) disclosure provide greater bioavailability of at least one A61K 31/ 353 ( 2006 . 01 ) green tea catechin . -Patent Applicationvandeniu Publicationakciu Augna. 31 , 2017 Sheetseminare 1 of 34 US 2017 / 0246235 A1 FIGURE 1 SCAVENGING FREE RADICALS OTHER INHIBITING BIOACTIVE OXIDATIVE PROPERTIES ENZYMES CATECHINS INDUCING IMPACTING ENDOGENOUS CELL ANTIOXIDANT CYCLE ENZYMES MODULATION OF SIGNAL TRANSDUCTION Patent Application Publication Aug. 31 , 2017 Sheet 2 of 34 US 2017 / 0246235 A1 OH ? OH Gallocatechin3-gallate:R1=0H,R2Galloyl 1 Catechin3-gallate:R1=H,R2Galloyl "ORZ Gallocatechin:R1=OH,R2H MOH Catechin:R1=R2H GlycosideGlycoside Apigeninglycoside OH Y OH HO GlycosideGlycoside FIGURE2 OH ?? Epigallocatechin3-gallate:Rq=0H,R2Galloyl OGlycoside >'"70R2 Kaempferolglycoside:Rq=R2H Quercetinglycoside:R1=0H,R2H Epigallocatechin:R1=OH,R2H Epicatechin3-gallate:R1=H,R2Galloy Myricetinglycoside:R1=R2OH Epicatechin:R2=H ? .HO Patent Application Publication Aug. 31 , 2017 Sheet 3 of 34 US 2017 / 0246235 A1 FIGURE 3 P .falciparum NF54 strain GTWL1 TH • IC50 = 10 . 0 ug /ml § 1 HA %ParasiteSurvival o Log 8 mg/ ml Patent Application Publication Aug. 31 , 2017 Sheet 4 of 34 US 2017 / 0246235 A1 FIGURE 4 A 150 %Nodrugcontrol a vi - 6 - 55 - - 3 log [ Phytofare botanical extract] g /ml B ? § %Nodrugcontrol lo ó - 5 log [Phytofare botanical extract] g /ml Patent Application Publication Aug. 31 , 2017 Sheet 5 of 34 US 2017 / 0246235 A1 FIGURE 5 § %Nodrugcontrol%Nodrugcontrol § - 55 - 4 Log [caffeine ] M § § %control%controlto HHutettiin TII a - 5 Log[ caffeine] M Patent Application Publication Aug. 31 , 2017 Sheet 6 of 34 US 2017 / 0246235 A1 Time concentration curve for epigallocatechin ngepigallocatechin/mLplasma ó40 200 400 600 800 1000 1200 1400 1600 Time (minutes ) - Comparator - - - - - Phytofare FIGURE 6 Patent Application Publication Aug. 31 , 2017 Sheet 7 of 34 US 2017 / 0246235 A1 Time concentration curve for gallocatechin gallate che ô ô nggallocatechingallate/mLplasma ? 0 200 400 600 800 1000 1200 1400 1600 Time (minutes ) - Comparator FIGURE Y - - - - - Phytofare Patent Application Publication Aug. 31 , 2017 Sheet 8 of 34 US 2017 / 0246235 A1 Time concentration curve for epicatechin os ? ngepicatechin/mLplasma ö 200 400 600 800 1000 1200 1400 1600 Time (minutes ) FIGURE 8 - Comparator - - - - - Phytofare Patent Application Publication Aug. 31 , 2017 Sheet 9 of 34 US 2017 / 0246235 A1 Time concentration curve for epicatechin gallate ngepicatechingallate/mLplasma - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - - 0 200 400 600 800 1000 1200 1400 1600 Time (minutes ) - Comparator - - - - - Phytofare FIGURE 9 Patent Application Publication Aug . 31, 2017 Sheet 10 of 34 US 2017 /0246235 A1 Time concentration curve for gallocatechin 90 .00 80 . 00 70 no 60 00 nggallocatechin/mLplasma & 40 .00 30. 00 20. 00 10 . 00 0 . 00 oti 200 400 600 800 1000 1200 1400 1600 Time (minutes ) FIGURE 10 Comparator - - - - - Phytofare Patent Application Publication Aug . 31, 2017 Sheet 11 of 34 US 2017 /0246235 A1 Time concentration curve for epigallocatechin Gallate 9 .00 8 . 00 7 .00 6 . 00 5 . 00 4 .00 ng/mLplasma 3 .00 2 .00 FAL H - - - - - - - - - - - - -- - - do. 200 400 600 800 1000 1200 1400 1600 Time (minutes ) FIGURE 11 Comparator - - - - - Phytofare - - - Poly . (Comparator ) - Poly . (Phytofare ) Patent Application Publication Aug . 31, 2017 Sheet 12 of 34 US 2017 /0246235 A1 Time concentration curve for catechin e ñ ngcatechin/mLplasma ? DITö o o 200 400 600 800 1000 1200 1400 1600 Time (minutes ) - Comparator - - - - - Phytofare FIGURE 12 Patent Application Publication Aug . 31, 2017 Sheet 13 of 34 US 2017 /0246235 A1 Time concentration curve for catechin gallate ??? ??? ??? ngcatechingallate/mlplasma ??? ???? 404 200 400 600 800 1000 1200 1400 1600 - 5 . 00 - Time (minutes ) FIGURE 13 Comparator - - - - - Phytofare Patent Application Publication Aug . 31, 2017 Sheet 14 of 34 US 2017 /0246235 A1 Total catechins plasma concentration curve 1800 . 00 1600 . 00 1400 . 00 1200& 1000 .00 o800 .00 ngtotalcatechins/mLplasma 600 . 00 â400 .00 200 .00 ð 0 . 00 e 200 400 600 800 1000 1200 1400 1600 Time (minutes ) Total Comparator - - - - - Total Phytofare FIGURE 14 - Patent Application Publication Aug . 31, 2017 Sheet 15 of 34 US 2017 /0246235 A1 Enhancement in bioavailability parameters by Phytofare technology o AUC enhancement Phytofare /Comparator Cmax enhancement Phytofare / Comparator i Enhancementfactor ? ? - ? on EpigallocatechinGallocatechin Gallate EpicatechinEpicatechin gallate Gallocatechin CatechinCatechinA Gallate EGCGTotal Catechins FIGURE 15 Patent Application Publication Aug . 31, 2017 Sheet 16 of 34 US 2017 /0246235 A1 40°C75RH 33.05 22.93 23.26 19.65 40°C75RH 73.30 53.16 50.99 30°C70RH 36.23 29.35 28.77 28.25 30°C70RH 73.42 59.77 59.32 25°C60RH 36.23 30.13 30.72 29.75 25°C60RH 81.11 61.95 58.81 Stabilityofcatechinsinoraldosageform FIGURE16 5°C 44.86 37.24 37.31 36.58 5°C 81.82 70.10 69.47 . 43.87 80.17 R? 1)ArmComparator( Phytofare(Arm2) Totalcatechins Release 1month 2months 10weeks 3months Totalcatechins Release 1month 2months 10weeks Patent Application Publicati0ll Aug. 31 , 2017 Sheet 17 of 34 US 2017/ 0246235 Al Stability at different conditions Comparator Phytofare g g ? ?8 8; ? R ? TotalCatechins R? TotalCatechins R - 5°6 8? . 5 ' c . - 25°G _60RH . - 25°c 60RH ? - . - 30' c 70RH ??? - . - 30°c 70RH ? - 40 ' c 75RH - 40°c 75RH ? Release fmonth ,S????? 10Weeks ) 3 months \ Release 1month ' 2months 10weeks ) 3 months FIGUIPF 17 Patent Application Publication Aug . 31 , 2017 Sheet 18 of 34 US 2017 / 0246235 A1 Total 052.35133 0291.4431 Catechin Gallate 0.3547287003885 5873041532239719955.813492812173 053.28143101541423967319 124.3441032257052702580081799179 05744.54078119756821078098 1417961589440353.0297299409234 20.55152923334431706529743809457 15.81314105106877704070913576803 003080297629538391068.6046671516 811.8111496190523123666971527198 602.564250610760471928791164358 708.588904105655712503061148591 799.293133257477919116931572026 673.483136183483116697951347963 561.588313220875916147961171823 558.220314319617412743341069371 447.676067223312931537081039781 550.6684320784231378924582649 35.1350121264439 181.80159270167358 EpicatechinGallocatechinEpigallocatechinCatechin Gallate 54.44890631 FIGURE18 Arm1comparator phytofareArm2 gallate 02.8453143490239095244764 35143680455174440.6492756298598687613425 6767364348104322454624170.39454941193352 4884292825882684464859321.67837252834808 068788128564648459.839851668215851709244 196.208338546757824492518473635676978 8923016696383848822168228.59616680560772 116.721102433049913911841222972452287865 8664214623.7830598147277462017489872224 36912984.27279137824196688703245479296 207.389893647839227526473061766871058668 259.299278451765478126463310497474216284 Summaryofaveragescatechinlevelsparticipantsplasma27inArmArmiand2bioavailabiltiystudy 18.51472328455003842935724935909238517.293348 Epicatechin 3648944441669018080.685532042871599038432904652235. 189864739343084814839738185384605438.243587808 179661778613761269750281324.31781572462909934478 2.2272879633017345269066263468346169654884502435 8233186969837954812934456543.20863240869880784621 ,4827964139361928833.7556085932951115124336656783 13388816239045526332311376939231512.416750048346 Gallocatechin Gallate 07481143. Epigallocatechin 1391803824. 163.8963589 112.2511609 5792092182. 188.9939956 183.3824052 115.0864556 136,1448891 75.37593118 OS90 120 180 300 480 720 1440 so60 90 120 180 300 480 720 1440 Patent Application Publication Aug . 31 , 2017 Sheet 19 of 34 US 2017/ 0246235 A1 Cmax Commercial Phytofare 900 800 - 700 - ? ng/mL ? ? ? 100 EpigallocatechinGallocatechin gallate EpicatechinEpicatechin gallate GallocatechinEpigallocatechin gallate Catechin Catechingallate FIGURE 19 Patent Application Publication Aug . 31, 2017 Sheet 20 of 34
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