Paclitaxel (Taxol) CAS 33069-62-4 Assay (HPLC) 97.0~102.0%

Paclitaxel
C47H51NO14 853.91
Te waikawa Benzenepropanoic, -(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 hākawa, [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, 12b-diacetate, 12-benzoate, 9-ester me (2R,3S) -N-benzoyl-3-phenylisoserine [33069-62-4].
Kei roto i te Paclitaxel te iti iho i te 97.0 paiheneti me te kore e neke ake i te 102.0 paiheneti o C47H51NO14, kua tatauhia i runga i te waikore, te whakarewa-kore.
[Tupato-He cytotoxic a Paclitaxel.Me tino tupato ki te aukati i te tango i nga matūriki o Paclitaxel ka puta te kiri ki reira.]
Packaging me te rokiroki-Whakaorangia i roto i kikī, ipu marama-ātete, me te rokiroki i te pāmahana rūma whakahaeretia.
Tapanga-Ko te tapanga e whakaatu ana i te momo o te tukanga e whakamahia ana ki te whakaputa i nga rawa me te whakamatautau i nga puhui e pa ana ki nga taonga.
Paerewa Tohutoro USP <11>-
USP Endotoxin RS
USP Paclitaxel RS Pāwhiri ki te Tirohanga Hanganga
USP Paclitaxel Pūhui Pātahi A RS
Cephalomannine.
USP Paclitaxel Pūhui Pānga B RS
10-Deacetyl-7-Epipaclitaxel.
USP Paclitaxel Whakaranu poke RS
Te ranunga o te Paclitaxel me nga puhui e whai ake nei: propyl analog, cephalomannine, sec-butyl analog, n-butyl analog, benzyl analog, baccatin VI, pentyl analog, me te 7-epipaclitaxel.
Tautuhinga-
A: Whakangao Infrared <197K>.
B: Ko te wa pupuri o te tihi nui i roto i te chromatogram o te whakaritenga Whakatau e rite ana ki tera i roto i te chromatogram o te whakaritenga Paerewa, i riro mai i te Assay.
Te hurihanga motuhake 781S: i waenganui i te 49.0 me te 55.0 i te 20, ka tatauhia i runga i te waikore, te whakarewa-kore.
Te otinga whakamatautau: 10 mg ia mL, i roto i te mewaro.
Nga whakamatautau tatau moroiti <61> me nga whakamatautau mo nga moroiti kua tohua <62>-Ko te tapeke moroiti aerobic kaore e neke ake i te 100 cfu ia g.Ka tutuki i nga whakaritenga o nga whakamatautau mo te kore o Staphylococcus aureus, Pseudomonas aeruginosa, momo Salmonella, me Escherichia coli.
Endotoxins huakita 85-Kaore e neke ake i te 0.4 USP Endotoxin Unit mo ia mg o te paclitaxel.
Wai, Tikanga Ic <921>: kaua e neke ake i te 4.0%.
Te toenga i runga i te mura <281>: kaua e neke ake i te 0.2%.
Nga konganuku taumaha, Tikanga II <231>: 0.002%.
Pūhui Pātahi-
whakamātautau 1 (mō ngā rawa kua tapaina he wehe mai i ngā mātāpuna māori)-Mena ka ū te rauemi ki tēnei whakamātautau, ka tohu te tapanga e tutuki ana ki ngā pūhui e pā ana ki te USP Whakamātautau 1.
Diluent-Whakaritea rite whakahaua i roto i te Assay.
Rongoā A-Whakaritea te acetonitrile kua tātarihia, kua whakakorehia te hau.
Otinga B-Whakaritea te wai kua tātarihia, kua whakahekehia te wai.
Waahanga pūkoro-Whakamahia nga ranunga rereke o te Rongoa A me te Otinga B e kiia ana mo te punaha Chromatographic.Whakaritea nga whakarereketanga mehemea e tika ana (tirohia te Tikanga Pūnaha i raro i te Chromatography 621).
Te otinga pai o te punaha-Whakarewa tika i nga rahinga o te USP Paclitaxel Related Compound A RS me USP Paclitaxel Related Compound B RS i roto i te methanol kia whiwhi ai i tetahi otinga e mohiotia ana mo te 10 µg o ia mL.Whakawhitihia te 5.0 mL o tenei wairewa ki roto i te ipu 50-mL, waimeha ki te Diluent ki te rōrahi, ka uru.
Wairewa Paerewa-Whakarewa, me te awhina o te sonication, he nui te pauna tika o te USP Paclitaxel RS i roto i te Diluent, me te waimeha ine, me te hikoi mena e tika ana, me te Diluent kia whiwhi ai i tetahi otinga e mohiotia ana mo te 5 µg ia mL.
Whakamātautau otinga-Whakamahia te whakaritenga Assay.
Pūnaha Chromatographic (tirohia te Chromatography <621>)-Ko te chromatograph wai he mea whakakakahu ki te kaitirotiro 227-nm me te 4.6-mm × 25-cm tīwae kei roto 5-µm te tarapi L43.Ko te tere rere he 2.6 mL ia meneti.Ka mau tonu te mahana o te pou ki te 30. Ka whakatakotohia te chromatograph e whai ake nei.
Wā (mēneti) Rongoā A (%) Rongoā B (%) Elution
0–35 35 65 momotu
35–60 35®80 65®20 rōnaki rārangi
60–70 80®35 20®65 rōnaki rārangi
70–80 35 65 isocraticChromatograph te otinga pai o te Pūnaha, me te tuhi i nga whakautu teitei e kiia ana mo te Tikanga: ko nga wa pupuri e pa ana ki te 0.78 mo te puhui paclitaxel A me te 0.86 mo te puhui paclitaxel B (e pa ana ki te wa pupuri mo te paclitaxel i whiwhi mai i te otinga Whakamatau);me te taumira, R, i waenga i te paclitaxel-related compound A me te paclitaxel related compound B kaua e iti iho i te 1.0.Chromatograph te otinga Paerewa, ka tuhi i nga whakautu teitei i runga i te tohutohu mo te Tikanga: ko te inenga paerewa mo nga werohanga tukurua kaua e neke ake i te 2.0%.
Tikanga-Tukuhia he rōrahi (tata ki te 15 µL) o te otinga Whakamātautau ki te chromatograph, tuhia te chromatogram, me te ine i nga waahi mo nga tihi nui.Tātaihia te ōrau o ia poke i te wāhanga o Paclitaxel i tangohia e te tātai:
100(Paraire / rU)
ko te F ko te tauwehe whakautu mo ia tihi poke (tirohia te Ripanga 1 mo nga uara);ko ri te waahi teitei mo ia poke takitahi;ko rU te waahi teitei mo te paclitaxel.
Ripanga 1
Wā Pupuri Pātahi Taupānga Whakautu (F) Tepe Ingoa (%)
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 Cephalomannine (Paclitaxel related compound A) a11
0.78 1.26 2'',3''-Dihydrocephalomannine a21
0.86 1.00 10-Deacetyl-7-epaclitaxel (Paclitaxel pūhui B) 0.5
1.10 1.00 Benzyl analog3 b12
1.10 1.00 3'',4''-Dehydropaclitaxel C b22
1.40 1.00 7-Epicephalomannine 0.3
1.85 1.00 7-Epipaclitaxel 0.5
1 Kare pea he whakaotinga mo enei tihi, i runga ano i te nui o nga moni;ko te tapeke o te a1 me te a2 kaua e neke ake i te 0.5%.
2 Kare pea he whakaotinga mo enei tihi, i runga i te nui o nga moni e noho ana;ko te tapeke o te b1 me te b2 kaua e neke ake i te 0.5%.
3 Ko te ingoa matū e whai ake nei ka tohua ki te pūhui whai pānga, benzyl analog:Baccatin III 13-ester me te (2R,3S) -2-hydroxy-3-phenyl-3-(2-phenylacetylamino)propanoic acid.
I tua atu i te kore e neke ake i nga tepe mo nga poke paclitaxel e pa ana ki te Ripanga 1, kaua e neke ake i te 0.1% o etahi atu poke kotahi ka kitea;a kaua e neke ake i te 2.0% o nga poke katoa ka kitea.
whakamātautau 2 (mō ngā rauemi kua tapaina i hangaia e te hātepe hangahanga)— Ki te rite te rauemi ki tenei whakamatautau, ka tohu te tapanga e tutuki ana ki te USP Related compound Test 2.
Diluent-Whakamahia acetonitrile.
Otinga A-Whakamahia he ranunga kua tātarihia, kua whakahekehia te wai me te acetonitrile (3:2).
Otinga B-Whakamahia te acetonitrile kua tātarihia, kua whakakorehia te hau.
Waahanga pūkoro-Whakamahia nga ranunga rereke o te Rongoa A me te Otinga B e kiia ana mo te punaha Chromatographic.Whakaritea nga whakarereketanga mehemea e tika ana (tirohia te Tikanga Pūnaha i raro i te Chromatography 621).
Te otinga pai o te punaha-Whakarewa tika te pauna o te USP Paclitaxel RS me te USP Paclitaxel Related Compound B RS i roto i te Diluent, te wiri me te sonicating mena e tika ana, kia whiwhi ai i tetahi otinga kua mohiohia he 0.96 mg me te 0.008 mg ia mL.
Te otinga whakamatautau-Whakawhitihia te 10 mg o te Paclitaxel, kua tika te pauna, ki te 10-mL ipu pukapuka, memeha ki roto ka waimeha ki te Diluent ki te rōrahi, wiri me te soniting ki te tika, ka uru.
Pūnaha Chromatography (tirohia te Chromatography 621)— Ko te chromatograph wai he mea whakakakahu ki te kaitahuri 227-nm me tetahi pou 4.6-mm × 15-cm kei roto te 3-µm te whakaemi L1.Ko te tere rere he 1.2 mL ia meneti.Ka mau tonu te mahana o te pou ki te 35. Ko te chromatograph te whakatakotoranga penei.
Wā (mēneti) Rongoā A (%) Rongoā B (%) Elution
0-20 100 0 momotu
20-60 100®10 0®90 rōnaki rārangi
60-62 10®100 90®0 rōnaki rārangi
62-70 100 0 isocraticChromatograph te otinga pai o te Pūnaha, me te tuhi i nga whakautu teitei e kiia ana mo te Tikanga: ko nga wa pupuri e pa ana ki te 0.94 mo te paclitaxel pūhui B me te 1.0 mo te paclitaxel;ko te taumira, R, i waenga i te paclitaxel-related compound B me te paclitaxel kaua e iti iho i te 1.2;me te inenga paerewa mo nga werohanga tukurua kaua e neke ake i te 2.0%.
Tikanga-Tukuhia wehea nga pukapuka rite (mo te 15 µL) o te Diluent me te otinga Whakamatau ki roto i te chromatograph, tuhia nga chromatograms, me te ine i nga waahi mo nga tihi katoa.Kaua e aro ki nga tihi na te Diluent.Tātaihia te ōrau o ia poke i te wāhanga o Paclitaxel i tangohia e te tātai:
100(Paraire / rs)
ko te F ko te tauwehe whakautu mo ia poke (tirohia te Ripanga 2 mo nga uara);ri ko te waahi teitei mo ia poke i puta mai i te otinga Whakamatau;a ko te rs te tapeke o nga waahi o nga tihi katoa i puta mai i te otinga Whakamatau.
Ripanga 2
Wā Pupuri Pātahi Taupānga Whakautu (F) Tepe Ingoa (%)
0.11 1.24 10-Deacetylbaccatin III 0.1
0.20 1.29 Baccatin III 0.2
0.42 1.39 Whakahekenga whakaahua2 0.1
0.47 1.00 10-Deacetylpaclitaxel 0.5
0.80 1.00 2-Debenzoylpaclitaxel-2-penenoate 0.7
0.921 1.00 Kua tuwhera te mowhiti Oxetane, kua heke te acetyl me te benzoyl2 x1
0.921 1.00 10-Acetoacetylpaclitaxel x2
0.941 1.00 10-Deacetyl-7-epaclitaxel (Paclitaxel pūhui 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 Kare pea he whakaotinga mo enei tihi, i runga ano i te nui o nga moni;ko te tapeke o x1, x2, me x3 kaua e neke ake i te 0.4%.
2 Ko nga ingoa matū e whai ake nei ka tohua ki nga pūhui e pa ana Photodegradant;I tuwhera te mowhiti oxetane, kua heke te acetyl me te benzoyl;me te 10,13-Bissidechainpaclitaxel:
Te whakaheke whakaahua
(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
Ka tuwhera te mowhiti oxetane, ka heke te acetyl me te benzoyl
(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
Baccatin III 13-ester me (2R,3S) -2-hydroxy-3-phenyl-3-(phenylcarbonylamino) waikawa propanoic, 10-ester me (2S,3S) -2-hydroxy-3-phenyl-3-(phenylcarbonylamino )waikawa propanoic
I tua atu i te kore e neke ake i nga tepe mo nga poke paclitaxel e pa ana ki te Ripanga 2, kaua e neke ake i te 0.1% o etahi atu poke kotahi ka kitea;a kaua e neke ake i te 2.0% o nga poke katoa ka kitea.
whakamātautau 3 (mō ngā rauemi kua tapaina he mea hanga e te tukanga FERmentation pūtau tipu)— Ki te rite te rauemi ki tenei whakamatautau, ka tohu te tapanga e tutuki ana ki te USP Related compound Test 3.
Rongoā A-Whakaritea he ranunga kua tātarihia, kua whakakorehia te wai me te acetonitrile (3:2).
Otinga B-Whakaritea te acetonitrile kua tātarihia, kua whakakorehia te hau.
Waahanga pūkoro-Whakamahia nga ranunga rereke o te Rongoa A me te Otinga B e kiia ana mo te punaha Chromatographic.Whakaritea nga whakarereketanga mehemea e tika ana (tirohia te Tikanga Pūnaha i raro i te Chromatography 621).
Te otinga pai o te punaha-Whakarewa i te USP Paclitaxel Impurity Mixture RS i roto i te acetonitrile, me te sonicating mena e tika ana, kia whiwhi ai i tetahi otinga e mohiotia ana mo te 1 mg ia mL.
Wairewa Paerewa-Warekahia te rahinga tika o te USP Paclitaxel RS i roto i te acetonitrile, me te sonicating mena e tika ana, kia whiwhi ai i tetahi otinga e mohiotia ana mo te 1 mg ia mL.
Te otinga whakamatautau-Whakawhitihia te 10 mg o Paclitaxel, i tika te pauna, ki te 10-mL ipu rahi.Whakarewa ki roto ka waimeha ki te acetonitrile ki te rōrahi, sonicating ki te tika, ka uru.
Pūnaha Chromatography (tirohia te Chromatography 621)— Ko te chromatograph wai he mea whakakakahu ki te kaitahuri 227-nm me tetahi pou 4.6-mm × 15-cm kei roto te 3-µm te whakaemi L1.Ko te tere rere he 1.2 mL ia meneti.Ko te chromatograph te mea e whai ake nei.
Wā (mēneti) Rongoā A (%) Rongoā B (%) Elution
0-28 100 0 momotu
28-33 100®98 0®2 rōnaki rārangi
33–58 98®10 2®90 rōnaki rārangi
58-60 10 90 tito
60-63 10®100 90®0 rōnaki rārangi
63-70 100 0 isocraticChromatograph te otinga pai o te Pūnaha, me te tuhi i nga whakautu teitei e kiia ana mo te Tikanga: ko te taumira, R, i waenga i te paclitaxel me te benzyl analog kaua e iti iho i te 1.8.Chromatograph te otinga Paerewa, ka tuhi i nga whakautu teitei i runga i te tohutohu mo te Tikanga: ko te inenga paerewa mo nga werohanga tukurua kaua e neke ake i te 2.0%.[Tuhipoka—Mo te tohu tohu teitei, ko nga wa e tata ana ki te pupuri i te Ripanga 3. Ka inehia nga wa pupuri whanaunga ki a Paclitaxel.]
Ripanga 3
Ingoa Tepe Wā Pupuri Whanaunga (%)
Propyl analog1 0.54 0.2
Cephalomannine (Paclitaxel related compound A) 0.76 0.5
hekona-Butyl analog2 0.81 0.2
n-Butyl analog3 0.89 0.1
Benzyl tairitenga 1.10 0.4
Baccatin VI 1.23 0.2
Pentyl analog4 1.31 0.2
7-Epipaclitaxel 1.51 0.4
1 Ko te ingoa matū e whai ake nei ka tohua ki te pūhui Propyl analog:Baccatin III 13-ester me te (2R,3S) -3-buanoylamino-2-hydroxy-3-phenylpropanoic acid.
2 Ko te ingoa matū e whai ake nei ka tohua ki te pūhui e pā ana sec-Butyl analog:Baccatin III 13-ester me te (2R,3S) -2-hydroxy-3-(2-methylbunoylamino) -3-phenylpropanoic acid.
3 Ko te ingoa matū e whai ake nei ka tohua ki te pūhui pūhui n-Butyl analog:Baccatin III 13-ester me te (2S,3S) -2-hydroxy-3-(pentanoylamino) -3-phenylpropanoic acid.
4 Ko te ingoa matū e whai ake nei ka tohua ki te pūhui Pentyl analog:Baccatin III 13-ester me te (2R,3S) -3-(hexanoylamino) -2-hydroxy-3-phenylpropanoic acid.
Tikanga-Tukuhia he rōrahi (e pā ana ki te 12 µL) o te otinga Whakamātautau ki te chromatograph, tuhia te chromatogram, me te ine i nga waahi mo nga tihi katoa.Tātaihia te ōrau o ia poke i te wāhanga o Paclitaxel i tangohia e te tātai:
100(ri / rU)
kei roto ko ri te whakautu o ia poke o ia tangata;a ko rU te tapeke o nga waahi o nga tihi katoa i puta mai i te otinga Whakamatau.I tua atu i te kore e neke ake i nga tepe mo nga poke paclitaxel e pa ana ki te Ripanga 3, kaua e neke ake i te 0.1% o etahi atu poke kotahi ka kitea;a kaua e neke ake i te 2.0% o nga poke katoa ka kitea.
whakamātautau-
Diluent-Whakaritea he ranunga o te mewaro me te waikawa ahetiki (200:1).
Wāhanga pūkoro-Whakaritea he ranunga kua tātarihia, kua whakahekehia te wai me te acetonitrile (11:9).Whakaritea nga whakarereketanga mehemea e tika ana (tirohia te Tikanga Pūnaha i raro i te Chromatography 621).
Whakaritea Paerewa-Wareka, te whakamahi sonication ki te tika, he nui tika paunatia o USP Paclitaxel RS i Diluent, me te waimeha ine, me te stepwise ki te tika, ki Diluent ki te whiwhi i te otinga he kukū mohiotia o e pā ana ki 1 mg ia mL.
Whakaritenga whakamatautau-Whakawhitihia te 10 mg o te Paclitaxel, i tika te pauna, ki te 10-mL ipu pukapuka.Whakarewa i roto i te Diluent, ma te whakamahi i te sonication mena e tika ana, whakamaua ki te Diluent ki te rōrahi, ka uru.
Pūnaha Chromatographic (tirohia te Chromatography <621>)-Ko te chromatograph wai he mea whakakakahu ki te kaitirotiro 227-nm me te 4.6-mm × 25-cm tīwae kei roto 5-µm te tarapi L43.Ko te tere rere he 1.5 mL ia meneti.Chromatograph the Standard preparation, and record the peak responses as directed for Procedure: kei waenganui i te 0.7 me te 1.3 te tauwehe hiku;a ko te inenga paerewa mo nga werohanga tukurua kaua e neke ake i te 1.5%.
Tikanga-Tukuhia wehe nga pukapuka rite (e tata ana ki te 10 µL) o te whakaritenga Paerewa me te whakareri Assay ki te chromatograph, tuhia nga chromatograms, me te ine i nga waahi mo nga tihi nui.Tātaihia te rahinga, i te mg, o C47H51NO14 i te wahanga o Paclitaxel i tangohia e te tauira:
10C(rU / rS)
i roto i te C ko te kukū, i roto i te mg ia mL, o USP Paclitaxel RS i roto i te whakaritenga Paerewa;a ko rU me rS nga whakautu teitei mo te paclitaxel i whiwhi mai i te whakarite Assay me te whakaritenga Paerewa.