I-Paclitaxel (Taxol) CAS 33069-62-4 Assay (HPLC) 97.0~102.0%
I-Shanghai Ruifu Chemical Co., Ltd. ingumkhiqizi ohamba phambili we-Paclitaxel (Taxol) (CAS: 33069-62-4) enekhwalithi ephezulu.I-Ruifu Chemical inganikeza ukulethwa komhlaba wonke, intengo encintisanayo, isevisi enhle kakhulu, amanani amancane kanye nenqwaba etholakalayo.Thenga i-Paclitaxel (Taxol),Please contact: alvin@ruifuchem.com
Igama Lekhemikhali | I-Paclitaxel |
Omqondofana | I-Taxol;I-Abraxane;I-Genaxol;iGenetaxyl;I-OncoGel;Pacliex;(-)-Paclitaxel |
Isimo Sesitoko | Ku-Stock, Commercial Production |
Inombolo ye-CAS | 33069-62-4 |
I-Molecular Formula | I-C47H51NO14 |
Isisindo samangqamuzana | 853.92 g/mol |
I-Melting Point | 211℃(dec.) |
Ukuminyana | 0.200 |
Ukuncibilika kwamanzi | Ayincibiliki Emanzini |
Ukuncibilika | Incibilika Kalula ku-Chloroform, i-acetone nezinye izincibilikisi ze-Organic. |
Ukuzinza | Izinzile.Akuhambisani nama-Ejenti Oxidizing Aqinile.Okuvuthayo. |
I-COA ne-MSDS | Iyatholakala |
Isampula | Iyatholakala |
Umsuka | Shanghai, China |
Ibhrendi | I-Ruifu Chemical |
Izinto | Imininingwane | Imiphumela |
Ukubukeka | I-Crystalline Powder Emhlophe, Ayinaphunga | Iyahambisana |
Ukuhlonza (A) | I-IR: Ihambisana ne-RS | Iyahambisana |
Ukuhlonza (B) | I-HPLC: I-RT Concordant ne-RS | Iyahambisana |
Ukuzungezisa okuqondile | -49.0° ukuya ku-55.0° | -52.3° |
Amanzi nguKarl Fischer | ≤4.00% | 0.91% |
Izinsalela ekushiseni | ≤0.20% | 0.02% |
Izinsimbi Ezisindayo (Pb) | ≤20ppm | <20ppm |
Izithako Ezihlobene | ||
Isamba | ≤2.00% | 0.11% |
10-Deacetylbaccatin III | ≤0.10% | Akutholwanga |
I-Baccatin III | ≤0.20% | Akutholwanga |
I-Photodegradant | ≤0.10% | Akutholwanga |
10-Deacetylpaclitaxel | ≤0.50% | 0.04% |
2-Debenzoylpaclitaxel-2-Pentenoate | ≤0.70% | Akutholwanga |
7-Epipaclitaxel | ≤0.40% | 0.014% |
10,13-Bissidechainpaclitaxel | ≤0.50% | 0.022% |
7-Acetylpaclitaxel | ≤0.60% | Akutholwanga |
13-Tes-baccatin III | ≤0.10% | 0.004% |
7-Tes-Paclitaxel | ≤0.30% | Akutholwanga |
Okunye Ukungcola Komuntu Ngamunye | ≤0.10% | Iyahambisana |
0Ukungcola Okuguquguqukayo | Iyahambisana | |
I-Hexan | ≤290ppm | 31ppm |
I-aceton | ≤5000ppm | 1210ppm |
I-Assay (HPLC) | 97.0~102.0% (kubalwe ngesisekelo se-anhydrous, i-solvent-free) | 99.88% |
Ukuhlolwa Komkhawulo We-Microbial | ||
Isamba se-Aerobic Microbial Count | ≤100 cfu/g | <100 cfu/g |
I-Staphylococcus Aureus | Ukungabikho | Ukungabikho |
I-Salmonella | Ukungabikho | Ukungabikho |
Escherichia Coli | Ukungabikho | Ukungabikho |
Ama-bacterium Endotoxins | ≤0.4EU/mg | <0.4EU/mg |
Isiphetho | Umkhiqizo uhloliwe futhi uhambisana ne-USP43 Paclitaxel |
Iphakheji:Ibhodlela eliFluorinated, isikhwama se-Aluminium foil, 25kg/Cardboard Drum, noma ngokwezidingo zekhasimende.
Isimo Sesitoreji:Gcina isiqukathi sivalwe ngokuqinile futhi usigcine endaweni epholile, eyomile (2~8℃) nengena umoya omuhle kude nezinto ezingahambelani.Vikela ekukhanyeni nakumswakama.
Ukuthumela:Zilethe emhlabeni wonke ngendiza, yi-FedEx/DHL Express.Nikeza ukulethwa okusheshayo nokuthembekile.
I-Paclitaxel
C47H51NO14 853.91
I-Benzenepropanoic acid, -(benzoylamino)--hydroxy-, 6,12b-bis(acetyloxy) -12-(benzoyloxy) -2a,3,4,4a,5,6,9,10,11,12,12a,12b -dodecahydro-4,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-7,11-methano-1H-cyclodeca[3,4]benz[1,2-b]oxet-9-yl i-ester, [2aR-[2a,4,4a,6,9(R*,S*),11,12,12a,12b]]-.
(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-1,2a,3,4,4a,6,9,10,11,12,12a,12b-Dodecahydro-4,6, 9,11,12,12b-hexahydroxy-4a,8,13,13-tetramethyl-7,11-methano-5H-cyclodeca[3,4]-benz[1,2-b]oxet-5-one 6, I-12b-diacetate, i-12-benzoate, i-9-ester ene-(2R,3S)-N-benzoyl-3-phenylisoserine [33069-62-4].
I-Paclitaxel iqukethe amaphesenti angekho ngaphansi kwamaphesenti angu-97.0 futhi hhayi ngaphezu kwamaphesenti angu-102.0 we-C47H51NO14, abalwe ngesisekelo se-anhydrous, i-solvent-free.
[Isixwayiso-I-Paclitaxel iyi-cytotoxic.Kufanele kuqashelwe kakhulu ukuvikela ukuhogela izinhlayiya ze-Paclitaxel nokubeka isikhumba kuso.]
Ukupakisha nokugcina-Londoloza ezitsheni eziqinile, ezikwazi ukumelana nokukhanya, futhi ugcine endaweni yokushisa elawulwayo.
Ukulebula-Ukulebula kubonisa uhlobo lwenqubo esetshenziselwa ukukhiqiza okokusebenza kanye nokuhlolwa kwezinhlanganisela Ezihlobene okuhambisana nakho.
Amazinga ereferensi we-USP <11>-
USP Endotoxin RS
USP Paclitaxel RS Chofoza ukuze Ubuke Isakhiwo
I-USP Paclitaxel Inhlanganisela Ehlobene A RS
I-Cephalomannine.
I-USP Paclitaxel Inhlanganisela Ehlobene B RS
10-Deacetyl-7-Epipaclitaxel.
I-USP Paclitaxel Impurity Mixture RS
Ingxube ye-Paclitaxel nezinhlanganisela ezilandelayo ezihlobene: i-propyl analog, i-cephalomannine, i-sec-butyl analog, i-n-butyl analog, i-benzyl analog, i-baccatin VI, i-pentyl analog, ne-7-epipaclitaxel.
Ukuhlonza-
A: I-Infrared Absorption <197K>.
B: Isikhathi sokugcinwa sesiqongo esikhulu ku-chromatogram yokulungiselelwa kwe-Assay sihambisana naleso esiku-chromatogram yokulungiselelwa Okujwayelekile, njengoba kutholwe ku-Assay.
Ukuzungezisa okuqondile 781S: phakathi kuka-49.0 no-55.0 kokungu-20, kubalwe ngesisekelo se-anhydrous, esingenayo i-solvent.
Isixazululo sokuhlola: 10 mg nge-mL, ku-methanol.
Ukuhlolwa kwe-microbial enumeration <61> kanye nokuhlolwa kwama-microorganisms athile <62>-Inani eliphelele le-aerobic microbial count ayidluli i-100 cfu igremu ngayinye.Ihlangabezana nezidingo zokuhlolwa kokungabikho kwe-Staphylococcus aureus, i-Pseudomonas aeruginosa, izinhlobo ze-Salmonella, ne-Escherichia coli.
I-bacterium endotoxins 85-Ayiqukethe iyunithi ye-Endotoxin engaphezu kuka-0.4 USP ngemg ye-paclitaxel.
Amanzi, Indlela Ic <921>: hhayi ngaphezu kuka-4.0%.
Izinsalela ekushiseni <281>: hhayi ngaphezu kuka-0.2%.
Izinsimbi ezinzima, Indlela II <231>: 0.002%.
Izinhlanganisela Ezihlobene-
ukuhlolwa 1 (okwezinto ezilebulwe njengezihlukanisiwe emithonjeni yemvelo)-Uma okokusebenza kuthobelana nalokhu kuhlolwa, ukulebula kubonisa ukuthi kuhlangabezana nokuhlolwa 1 kwezinhlanganisela Ezihlobene ne-USP.
I-Diluent-Lungiselela njengoba kuqondiswe ku-Assay.
Isixazululo A-Lungiselela i-acetonitrile ehlungiwe futhi ekhishwe umoya.
Isixazululo B-Lungiselela amanzi ahlungiwe nasusiwe.
Isigaba seselula-Sebenzisa izingxube eziguquguqukayo zesisombululo A nesixazululo B njengoba kuqondiswe kusistimu yeChromatographic.Yenza izinguquko uma kudingeka (bona Ukufaneleka Kwesistimu ngaphansi kwe-Chromatography 621).
Isixazululo sokufaneleka kwesistimu-Chaza amanani anesisindo esinembile se-USP Paclitaxel Related Compound A RS kanye ne-USP Paclitaxel Related Compound B RS ku-methanol ukuze uthole isixazululo esinokugxila okwaziwayo okungaba ngu-10 µg we-mL ngayinye.Dlulisa u-5.0 mL walesi sixazululo ku-50-mL ye-volumetric flask, hlambulula nge-Diluent kuya kuvolumu, bese uxuba.
Isixazululo esijwayelekile-Ncibilikisa, ngosizo lwe-sonication, inani elinembile le-USP Paclitaxel RS ku-Diluent, futhi nciphisa ngobuningi, futhi ngokwesinyathelo uma kudingeka, nge-Diluent ukuze uthole isixazululo esinokugxila okwaziwayo okungaba ngu-5 µg ngemL ngayinye.
Isixazululo sokuhlola-Sebenzisa ukulungiswa kwe-Assay.
Isistimu ye-Chromatographic (bona i-Chromatography <621>)-I-chromatograph ewuketshezi ifakwe umtshina ongu-227-nm kanye nekholomu engu-4.6-mm × 25-cm equkethe 5-µm ukupakisha L43.Izinga lokugeleza licishe libe ngu-2.6 mL ngomzuzu.Izinga lokushisa lekholomu ligcinwa liku-30. I-chromatograph ihlelwe kanje.
Isikhathi (imizuzu) Isixazululo A (%) Isixazululo B (%) Ukulinganisa
0–35 35 65 isokhrasi
35–60 35®80 65®20 i-gradient yomugqa
60–70 80®35 20®65 i-gradient yomugqa
70–80 35 65 isocraticChromatograph isixazululo sokufaneleka kweSistimu, futhi urekhode izimpendulo eziphezulu njengoba kuqondiswe Inqubo: izikhathi zokugcinwa okuhlobene zicishe zibe ngu-0.78 wenhlanganisela ehlobene ne-paclitaxel A kanye no-0.86 yenhlanganisela B ehlobene ne-paclitaxel (ngokuhlobene nesikhathi sokugcinwa kwe-paclitaxel etholwe ku-paclitaxel isixazululo sokuhlola);kanye nokulungiswa, R, phakathi kwenhlanganisela ehlobene ne-paclitaxel A kanye nenhlanganisela B ehlobene ne-paclitaxel ayikho ngaphansi kuka-1.0.I-Chromatograph isixazululo Esijwayelekile, bese urekhoda izimpendulo eziphakeme njengoba kuqondiswe kuNqubo: ukuchezuka okujwayelekile okuhlobene kwemijovo eyimpinda akukho ngaphezu kuka-2.0%.
Inqubo-Jonga ivolumu (cishe 15 µL) yesisombululo Sokuhlola ku-chromatograph, rekhoda i-chromatogram, futhi ulinganise izindawo zeziqongo ezinkulu.Bala iphesenti lokungcola ngakunye engxenyeni ye-Paclitaxel ethathwe ifomula:
100(NgoLwesihlanu / rU)
lapho u-F eyisici sokuphendula esihlobene esiqongweni ngasinye sokungcola (bona Ithebula 1 ukuze uthole amanani);i-ri iyindawo ephakeme kakhulu yokungcola komuntu ngamunye;futhi i-rU iyindawo ephakeme kakhulu ye-paclitaxel.
Ithebula 1
Isikhathi Esihlobene Sokugcina Isici Sempendulo Ehlobene (F) Umkhawulo Wegama (%)
0.24 1.29 Baccatin III 0.2
0.53 1.00 10-Deacetylpaclitaxel 0.5
0.57 1.00 7-Xylosylpaclitaxel 0.2
0.78 1.26 I-Cephalomannine (inhlanganisela ehlobene ne-Paclitaxel A) a11
0.78 1.26 2'',3''-Dihydrocephalomanine a21
0.86 1.00 10-Deacetyl-7-epipaclitaxel (inhlanganisela ehlobene ne-Paclitaxel B) 0.5
1.10 1.00 Benzyl analog3 b12
1.10 1.00 3'',4''-Dehydropaclitaxel C b22
1.40 1.00 7-Epicephalomanine 0.3
1.85 1.00 7-Epipaclitaxel 0.5
1 Ukulungiswa kungase kungaphelele kulezi ziqongo, kuye ngamanani ahlobene akhona;isamba sika-a1 no-a2 asidluli ku-0.5%.
2 Ukulungiswa kungase kungaphelele kulezi ziqongo, kuye ngamanani ahlobene akhona;isamba se-b1 ne-b2 asidluli ku-0.5%.
3 Igama lekhemikhali elilandelayo linikezwe isakhi esihlobene, i-benzyl analog:Baccatin III 13-ester ene-(2R,3S) -2-hydroxy-3-phenyl-3-(2-phenylacetylamino)propanoic acid.
Ngaphezu kokungeqi imingcele yokungcola okuhlobene ne-paclitaxel kuThebula 1, akutholakali ngaphezu kuka-0.1% wanoma yikuphi okunye ukungcola okukodwa;futhi akukho ngaphezu kuka-2.0% wokungcola okuphelele okutholakele.
ukuhlolwa 2 (kokubalulekile okulebulwe njengokukhiqizwe inqubo ye-semisynthetic)— Uma okokusebenza kuthobelana nalokhu kuhlolwa, ukulebula kubonisa ukuthi kuhlangabezana nokuhlolwa kwe-USP Okuhlobene Nezinhlanganisela Ezihlobene.
I-Diluent-Sebenzisa i-acetonitrile.
Isixazululo A-Sebenzisa ingxube ehlungiwe nekhishiwe amanzi ne-acetonitrile (3:2).
Isixazululo B-Sebenzisa i-acetonitrile ehlungiwe futhi ekhishwe umoya.
Isigaba seselula-Sebenzisa izingxube eziguquguqukayo zesisombululo A nesixazululo B njengoba kuqondiswe kusistimu yeChromatographic.Yenza izinguquko uma kudingeka (bona Ukufaneleka Kwesistimu ngaphansi kwe-Chromatography 621).
Isixazululo sokufaneleka kwesistimu-Chaza amanani anesisindo esinembile se-USP Paclitaxel RS kanye ne-USP Paclitaxel Related Compound B RS in Diluent, shaking and sonicating uma kudingekile, ukuze uthole isixazululo ngokugxila okwaziwayo okungaba ngu-0.96 mg kanye no-0.008 mg ngemL ngayinye, ngokulandelana.
Isixazululo sokuhlola-Dlulisa cishe u-10 mg we-Paclitaxel, ukalwe ngokunembile, ku-10-mL ye-volumetric flask, ncibilikisa futhi uhlambulule nge-Diluent kuya kuvolumu, ukuthuthumela kanye ne-sonicating uma kunesidingo, bese uxuba.
Isistimu ye-Chromatographic (bona i-Chromatography 621)— I-chromatograph ewuketshezi ifakwe umtshina ongu-227-nm kanye nekholomu engu-4.6-mm × 15-cm equkethe u-3-µm wokupakisha i-L1.Izinga lokugeleza licishe libe ngu-1.2 mL ngomzuzu.Izinga lokushisa lekholomu ligcinwa liku-35. I-chromatograph ihlelwe kanje.
Isikhathi (imizuzu) Isixazululo A (%) Isixazululo B (%) Ukulinganisa
0-20 100 0 isocratic
20-60 100®10 0®90 i-gradient yomugqa
60-62 10®100 90®0 i-gradient yomugqa
62-70 100 0 isocraticChromatograph isixazululo sokufaneleka kweSistimu, futhi urekhode izimpendulo eziphezulu njengoba kuqondiswe Inqubo: izikhathi zokugcinwa okuhlobene zicishe zibe ngu-0.94 kunhlanganisela ehlobene ne-paclitaxel B kanye no-1.0 ye-paclitaxel;isixazululo, R, phakathi kwenhlanganisela ehlobene ne-paclitaxel engu-B ne-paclitaxel ayikho ngaphansi kuka-1.2;futhi ukuchezuka okujwayelekile okuhlobene kwemijovo eyimpinda akukho ngaphezu kuka-2.0%.
Inqubo-Ngokuhlukile jova amavolumu alinganayo (cishe u-15 µL) we-Diluent kanye nesixazululo sokuhlola ku-chromatograph, rekhoda ama-chromatogram, futhi ulinganise izindawo zazo zonke iziqongo.Unganaki noma yiziphi iziqongo ngenxa ye-Diluent.Bala iphesenti lokungcola ngakunye engxenyeni ye-Paclitaxel ethathwe ifomula:
100(Ngolwesihlanu / rs)
lapho u-F eyisici sokuphendula esihlobene sokungcola ngakunye (bheka Ithebula 2 ukuze uthole amanani);i-ri iyindawo ephakeme kakhulu yokungcola ngakunye okutholakala kusixazululo sokuhlola;futhi u-rs uyisamba sezindawo zazo zonke iziqongo ezitholwe kusixazululo sokuhlola.
Ithebula 2
Isikhathi Esihlobene Sokugcina Isici Sempendulo Ehlobene (F) Umkhawulo Wegama (%)
0.11 1.24 10-Deacetylbaccatin III 0.1
0.20 1.29 Baccatin III 0.2
0.42 1.39 Photodegradant2 0.1
0.47 1.00 10-Deacetylpaclitaxel 0.5
0.80 1.00 2-Debenzoylpaclitaxel-2-pentenoate 0.7
0.921 1.00 kuvulwe indandatho ye-Oxetane, i-acetyl ne-benzoyl zithuthelwe2 x1
0.921 1.00 10-Acetoacetylpaclitaxel x2
0.941 1.00 10-Deacetyl-7-epipaclitaxel (inhlanganisela ehlobene ne-Paclitaxel B) x3
1.37 1.00 7-Epipaclitaxel 0.4
1.45 1.00 10,13-Bissidechainpaclitaxel2 0.5
1.54 1.00 7-Acetylpaclitaxel 0.6
1.80 1.75 13-Tes-baccatin III 0.1
2.14 1.00 7-Tes-paclitaxel 0.3
1 Ukulungiswa kungase kungaphelele kulezi ziqongo, kuye ngamanani ahlobene akhona;isamba sika-x1, x2, kanye no-x3 asidluli ku-0.4%.
2 Lawa magama alandelayo amakhemikhali anikezwa izinhlanganisela ezihlobene I-Photodegradant;I-Oxetane ring yavuleka, i-acetyl ne-benzoyl yafuduka;kanye ne-10,13-Bissidechainpaclitaxel:
I-Photodegradant
(1R,2R,4S,5S,7R,10S,11R,12S,13S,15S,16S)-2,10-diacetyloxy-5,13-dihydroxy-4,16,17,17-tetramethyl-8-oxa- 3-oxo-12-phenylcarbonyloxypentacyclo[11.3.1.01,11.04,11.07,10]heptadec-15-yl
(2R,3S)-2-hydroxy-3-phenyl-3-(phenylcarbonylamino)propanoate
Indandatho ye-Oxetane yavulwa, i-acetyl ne-benzoyl yafuduka
(1S,2S,3R,4S,5S,7S,8S,10R,13S)-5,10-diacetyloxy-1,2,4,7-tetrahydroxy-8,12,15,15-tetramethyl-9-oxo- 4-(phenylcarbonyloxymethyl)tricyclo[9.3.1.03,8]pentadec-11-en-13-yl
(2R,3S)-2-hydroxy-3-phenyl-3-(phenylcarbonylamino)propanoate
10,13-Bissidechainpaclitaxel
I-Baccatin III 13-ester ene-(2R,3S)-2-hydroxy-3-phenyl-3-(phenylcarbonylamino)propanoic acid, 10-ester with (2S,3S) -2-hydroxy-3-phenyl-3-(phenylcarbonylamino I-propanoic acid
Ngaphezu kokungeqi imingcele yokungcola okuhlobene ne-paclitaxel kuThebula 2, akutholakali ngaphezu kuka-0.1% wanoma yikuphi okunye ukungcola okukodwa;futhi akukho ngaphezu kuka-2.0% wokungcola okuphelele okutholakele.
ukuhlolwa 3 (okwezinto ezilebulwe njengezikhiqizwe inqubo yokuvutshelwa kweseli lesitshalo)— Uma okokusebenza kuvumelana nalokhu kuhlola, ukulebula kubonisa ukuthi kuhlangabezana nokuhlolwa kwe-USP Okuhlobene Nenhlanganisela yesi-3.
Isixazululo A-Lungiselela ingxube ehlungiwe nekhishiwe amanzi ne-acetonitrile (3:2).
Isixazululo B-Lungiselela i-acetonitrile ehlungiwe futhi ekhishwe umoya.
Isigaba seselula-Sebenzisa izingxube eziguquguqukayo zesisombululo A nesixazululo B njengoba kuqondiswe kusistimu yeChromatographic.Yenza izinguquko uma kudingeka (bona Ukufaneleka Kwesistimu ngaphansi kwe-Chromatography 621).
Isixazululo sokufaneleka kwesistimu-Dissolve USP Paclitaxel Impurity Mixture RS ku-acetonitrile, i-sonicating uma kunesidingo, ukuze uthole isixazululo esinokugxila okwaziwayo okungaba ngu-1 mg nge-mL ngayinye.
Isixazululo esijwayelekile-Chaza isamba esikalwe ngokunembile se-USP Paclitaxel RS ku-acetonitrile, i-sonicating uma kunesidingo, ukuthola isixazululo esinokugxila okwaziwayo okungaba ngu-1 mg nge-mL ngayinye.
Isixazululo sokuhlola-Dlulisa cishe u-10 mg we-Paclitaxel, ukalwe ngokunembile, uye kuflask yevolumu ye-10-mL.Ncibilikisa futhi uhlambulule nge-acetonitrile iye kuvolumu, yenza i-sonicing uma kunesidingo, bese uxuba.
Isistimu ye-Chromatographic (bona i-Chromatography 621)— I-chromatograph ewuketshezi ifakwe umtshina ongu-227-nm kanye nekholomu engu-4.6-mm × 15-cm equkethe u-3-µm wokupakisha i-L1.Izinga lokugeleza licishe libe ngu-1.2 mL ngomzuzu.Ichromatograph ihlelwe kanje.
Isikhathi (imizuzu) Isixazululo A (%) Isixazululo B (%) Ukulinganisa
0-28 100 0 isocratic
28-33 100®98 0®2 i-gradient yomugqa
33–58 98®10 2®90 i-gradient yomugqa
58-60 10 90 isocratic
60-63 10®100 90®0 i-gradient yomugqa
63-70 100 0 isocraticChromatograph isixazululo sokufaneleka kweSistimu, futhi urekhode izimpendulo eziphezulu njengoba kuqondiswe Inqubo: ukulungiswa, R, phakathi kwe-paclitaxel ne-benzyl analog ayikho ngaphansi kuka-1.8.I-Chromatograph isixazululo Esijwayelekile, bese urekhoda izimpendulo eziphakeme njengoba kuqondiswe kuNqubo: ukuchezuka okujwayelekile okuhlobene kwemijovo eyimpinda akukho ngaphezu kuka-2.0%.[inothi—Ngenjongo yokuhlonza inani eliphakeme, izikhathi zokugcinwa ezilinganiselwe ezilinganiselwe zinikezwe kuThebula 3. Izikhathi zokugcinwa okuhlobene zilinganiswa uma kuqhathaniswa ne-Paclitaxel.]
Ithebula 3
Qamba Umkhawulo Wesikhathi Sokugcina Okuhlobene (%)
I-analog ye-Propyl1 0.54 0.2
I-Cephalomannine (inhlanganisela ehlobene ne-Paclitaxel A) 0.76 0.5
isekhondi-Butyl analog2 0.81 0.2
n-Butyl analog3 0.89 0.1
I-analogue ye-Benzyl 1.10 0.4
I-Baccatin VI 1.23 0.2
I-analog ye-Pentyl4 1.31 0.2
7-Epipaclitaxel 1.51 0.4
1 Igama lekhemikhali elilandelayo linikezwe isakhi esihlobene se-Propyl analog:Baccatin III 13-ester ene-(2R,3S) -3-butanoylamino-2-hydroxy-3-phenylpropanoic acid.
2 Igama lekhemikhali elilandelayo linikezwe isakhi esihlobene sec-Butyl analog:Baccatin III 13-ester ene-(2R,3S) -2-hydroxy-3-(2-methylbutanoylamino) -3-phenylpropanoic acid.
3 Igama lekhemikhali elilandelayo linikezwe isakhi esihlobene se-n-Butyl analog:Baccatin III 13-ester ene-(2S,3S) -2-hydroxy-3-(pentanoylamino) -3-phenylpropanoic acid.
4 Igama lekhemikhali elilandelayo linikezwe inhlanganisela ehlobene ye-Pentyl analog:Baccatin III 13-ester ene-(2R,3S) -3-(hexanoylamino) -2-hydroxy-3-phenylpropanoic acid.
Inqubo-Jonga ivolumu (cishe 12 µL) yesisombululo Sokuhlola ku-chromatograph, rekhoda i-chromatogram, futhi ulinganise izindawo zazo zonke iziqongo.Bala iphesenti lokungcola ngakunye engxenyeni ye-Paclitaxel ethathwe ifomula:
100(ri/rU)
lapho ri kuyimpendulo yokungcola komuntu ngamunye;futhi i-rU iyisamba sezindawo zazo zonke iziqongo ezitholakala kusixazululo sokuhlola.Ngaphezu kokungeqi imingcele yokungcola okuhlobene ne-paclitaxel kuThebula 3, akutholakali ngaphezu kuka-0.1% wanoma yikuphi okunye ukungcola okukodwa;futhi akukho ngaphezu kuka-2.0% wokungcola okuphelele okutholakele.
Isivivinyo-
I-Diluent-Lungisa ingxube ye-methanol ne-acetic acid (200:1).
Isigaba seselula-Lungiselela ingxube ehlungiwe nekhishiwe amanzi ne-acetonitrile (11:9).Yenza izinguquko uma kudingeka (bona Ukufaneleka Kwesistimu ngaphansi kwe-Chromatography 621).
Ukulungiselela okujwayelekile-Chaza, usebenzisa i-sonication uma kudingekile, inani elinembile le-USP Paclitaxel RS ku-Diluent, futhi nciphisa ngobuningi, futhi ngokwesinyathelo uma kunesidingo, nge-Diluent ukuze uthole isixazululo esinokugxila okwaziwayo okungaba ngu-1 mg nge-mL ngayinye.
Ukulungiselela i-Assay-Dlulisa cishe u-10 mg we-Paclitaxel, ukalwe ngokunembile, uye kuflask yevolumu ye-10-mL.Ncibilika ku-Diluent, usebenzisa i-sonication uma kunesidingo, nciphisa nge-Diluent kuya kuvolumu, bese uxuba.
Isistimu ye-Chromatographic (bona i-Chromatography <621>)-I-chromatograph ewuketshezi ifakwe umtshina ongu-227-nm kanye nekholomu engu-4.6-mm × 25-cm equkethe 5-µm ukupakisha L43.Izinga lokugeleza licishe libe ngu-1.5 mL ngomzuzu.I-Chromatograph ukulungiselelwa Okujwayelekile, futhi urekhode izimpendulo eziphezulu njengoba kuqondiswe kuNqubo: isici somsila siphakathi kuka-0.7 no-1.3;futhi ukuchezuka okujwayelekile okuhlobene kwemijovo eyimpinda akukho ngaphezu kuka-1.5%.
Inqubo-Ngokuhlukile jova amavolumu alinganayo (cishe u-10 µL) wokulungiselelwa Okujwayelekile kanye nokulungiswa kwe-Assay ku-chromatograph, rekhoda ama-chromatogram, futhi ulinganise izindawo zeziqongo ezinkulu.Bala inani, ngo-mg, le-C47H51NO14 engxenyeni ye-Paclitaxel ethathwe ifomula:
10C(rU / rS)
lapho u-C egxile khona, ngo-mg ngemL ngayinye, ye-USP Paclitaxel RS ekulungiseleleni Okujwayelekile;futhi i-rU ne-rS yizimpendulo eziphezulu ze-paclitaxel ezitholwe ekulungiselelweni kwe-Assay nasekulungiseleleni Okujwayelekile, ngokulandelanayo.
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I-Paclitaxel (Taxol) (CAS: 33069-62-4), umkhiqizo wemvelo ohlukanisiwe namagxolo e-Pacific yew, iyasebenza ekwelapheni umdlavuza we-ovarian we-metastatic refractory.Ngokungafani namanye ama-antineoplastic agents, i-paclitaxel ibonakala inezindlela ezimbalwa zokwenza, okuhlanganisa isenzo se-antimicrotubule ngokukhuthazwa kwe-tubulin polymerization kanye nokuqiniswa kwama-microtubules, ngaleyo ndlela, imise i-mitosis futhi ikhuthaze ukufa kweseli.Ukunikezwa kwe-paclitaxel kukhawulelwe ngobuningi bayo bemvelo obuphansi futhi njengamanje kukhiqizwa umzila owenziwe kancane osuka ku-deacetylbaccatin Ⅲ ohlukanisiwe nezinaliti zesihlahla se-yew.Ukuqedwa kwakamuva kwama-syntheses amabili engqikithi ye-taxol kunqobe ubunkimbinkimbi besakhiwo benhlanganisela yesihloko futhi kungase kube usizo ekutholeni ama-analogue athile ahlobene eduze, amanye atholwe enomsebenzi we-antitumors.I-Paclitaxel ingasetshenziswa ekwelapheni umdlavuza webele we-metastatic, umdlavuza wamaphaphu, umdlavuza wekhanda nentamo, kanye ne-melanoma eyingozi.
Izithako ezinobuthi emagatsheni namaqabunga e-Taxus chinensis zahlukaniswa ngo-1856 futhi zaqanjwa ngokuthi “taxine,” eyahlonzwa njengohlobo lwengxenye ye-alkaloid emhlophe.Njengamanje, phakathi kwayo yonke imishanguzo ye-antitumor, ukuthengiswa kwe-paclitaxel kuba eyokuqala emhlabeni njengesidakamizwa esaziwayo somdlavuza esinomsebenzi onamandla we-spectrum ebanzi.Ngo-Okthoba ka-1995, i-China yaba izwe lesibili ngokukhiqizwa okusemthethweni kwe-paclitaxel kanye nomjovo wayo emhlabeni.Le mpumelelo yatholwa ngaphansi kwemizamo engapheli yabacwaningi e-Institute of Materia Medica, i-Chinese Academy of Medical Sciences.
I-Paclitaxel (CAS: 33069-62-4) iyi-antineoplastic eyayisetshenziselwa ukwelapha iziguli ezinomdlavuza wamaphaphu, i-ovary, umdlavuza webele, umdlavuza wekhanda nentamo, kanye nezinhlobo ezithuthukisiwe ze-Kaposi's sarcoma.I-Paclitaxel iyi-mitotic inhibitor esetshenziswa ekwelapheni umdlavuza.Ibuye isetshenziswe ekutadisheni isakhiwo kanye nokusebenza kwama-microtubles abe yi-tubulin.
I-Paclitaxel inomphumela omuhle kumdlavuza we-ovarian we-refractory kanye nomdlavuza webele onokumelana nezidakamizwa ezifana nomdlavuza we-ovarian ne-platinum, kanye nethemba elihle lokwelashwa komdlavuza wendlala yesinye, umdlavuza wekhanda nentamo, umdlavuza womminzo, i-germ cell tumor, umdlavuza we-endometrial, i-lymphoma, umdlavuza wesinye, umdlavuza womgudu wokugaya ukudla ongenhla, amangqamuzana amancane kanye nomdlavuza wamaphaphu ongewona omncane.
I-Paclitaxel (Taxol) (CAS: 33069-62-4) iyinhlanganisela eyinkimbinkimbi kakhulu, ephilayo ehlukaniswe namagxolo esihlahla se-yew sasePacific.Ibophezela kuma-tubulin dimers kanye ne-microtubulin filaments, ikhuthaza ukuhlangana kwe-filaments futhi ivimbele ukuchithwa kwayo.Lokhu kwanda kokuzinza kwama-microfilaments kubangela ukuphazamiseka kwe-mitosis kanye ne-cytotoxicity futhi kuphazamisa eminye imisebenzi evamile ye-microtubular, njengokuthuthwa kwe-axonal emicu yezinzwa.Indlela enkulu yokumelana ekhonjwe nge-paclitaxel ukuthuthwa kukhishwe kumaseli wesimila, okuholela ekwehleni kokunqwabelana kwezidakamizwa ezingaphakathi kweseli.Lolu hlobo lokumelana luqondiswa yi-multidrug transporter P-glycoprotein.
Ingase ibe nomuzwa wokuchayeka isikhathi eside kumswakama.