Mingzu Yang, Bo Xu
Talosaga R&D Nofoaga Autu
Folasaga
O vaila'au fa'ama'i o se vasega o metabolites lona lua e gaosia e ni meaola ninii (e aofia ai siama, sigi, actinomycetes) po'o mea fa'apena fa'apena e fa'apipi'iina i kemikolo po'o semi-synthesized.O vaila'au fa'ama'i e mafai ona taofia ai le tuputupu a'e ma le ola o isi microorganisms.O le antibiotic muamua na maua e le tagata, penicillin, na maua e le British microbiologist Alexander Fleming i le 1928. Na ia matauina e le mafai ona tupu le siama i tafatafa o le limu i totonu o le staphylococcus culture dish lea na afaina i le limu.Na ia fai mai e tatau ona natia e le limu se mea e puipuia ai siama, lea na ia faaigoaina o le penicillin i le 1928. Peitaʻi, o mea aoga e leʻi faʻamamaina i lena taimi.I le 1939, na filifili ai Ernst Chain ma Howard Florey o le Iunivesite o Oxford e fausia se fualaau e mafai ona togafitia ai siama siama.Ina ua uma ona faʻafesoʻotaʻi Fleming e maua mai faʻamaʻi, na latou aveese ma faʻamama le penicillin mai faʻamaʻi.Mo lo latou atinaʻeina manuia o le penicillin e avea o se vailaʻau faʻamalolo, Fleming, Chain ma Florey faʻasoa le 1945 Nobel Prize in Medicine.
O vailaau fa'ama'i e fa'aaogaina e fai ma vaila'au fa'ama'i e togafitia pe puipuia ai fa'ama'i pipisi.E tele vaega autu o vailaʻau faʻaaogaina e avea ma vailaʻau faʻamaʻi: β-lactam antibiotics (e aofia ai penicillin, cephalosporin, ma isi), aminoglycoside antibiotics, macrolide antibiotics, tetracycline antibiotics, chloramphenicol (total synthetic antibiotic), ma isi mea. fermentation biological, semi-synthesis ma le tuufaatasiga atoa.O vailaʻau faʻamaʻi e maua mai i le faʻafefe o meaola e manaʻomia ona faʻaleleia faʻavae e ala ile vailaʻau ona o le mautu o vailaʻau, aʻafiaga oona, alaleo antibacterial ma isi faʻafitauli.A maeʻa ona faʻaleleia faʻamaʻi, e mafai e vailaʻau faʻamaʻi ona ausia le faʻateleina o le mautu, faʻaitiitia aʻafiaga oona, faʻalauteleina alaleo antibacterial, faʻaitiitia le teteʻeina o vailaʻau, faʻaleleia le bioavailability, ma faʻaleleia ai le aʻafiaga o togafitiga fualaau.O le mea lea, o vailaʻau semi-synthetic o loʻo avea nei ma taʻutaʻua sili ona lauiloa i le atinaʻeina o vailaʻau faʻamaʻi.
I le atinaʻeina o vailaʻau faʻamaʻi semi-synthetic, o vailaʻau faʻamaʻi o loʻo i ai meatotino e maualalo le mama, tele o mea faʻatau ma vaega lavelave talu ai e maua mai i mea faʻafefete microbial.I lenei tulaga, o le auʻiliʻiliga ma le puleaina o mea le mama i vailaʻau semi-synthetic e sili ona taua.Ina ia mafai ona faʻamaonia lelei ma faʻamaonia mea leaga, e manaʻomia le maua o le tele o mea leaga mai le gaosiga faʻapipiʻi o vailaʻau semi-synthetic.Faatasi ai ma le masani ona faʻaaogaina le faʻaogaina o le faʻaogaina o metotia, o le flash chromatography o se auala taugofie ma tulaga lelei e pei o le tele o faʻataʻitaʻiga faʻatauga aofaʻi, tau maualalo, taimi faʻasaoina, ma isi.
I lenei pou, o le eleelea autu o le semi-synthetic aminoglycoside antibiotic na faʻaaogaina e fai ma faʻataʻitaʻiga ma faʻamamāina e le SepaFlash C18AQ pusa faʻatasi ma le masini chromatography flash SepaBean ™.O le oloa faʻatatau e fetaui ma manaʻoga na maua ma le manuia, faʻaalia ai se fofo sili ona lelei mo le faʻamamaina o nei mea.
Vaega Fa'ata'ita'i
O le faʻataʻitaʻiga na tuʻuina atu ma le agalelei e se kamupani vailaʻau faʻapitonuʻu.O le faʻataʻitaʻiga o se ituaiga amino polycyclic carbohydrates ma lona fausaga mole e tutusa ma vailaʻau aminoglycoside.O le polarity o le faʻataʻitaʻiga sa fai si maualuga, e matua solu i le vai.O le ata faʻataʻitaʻiga o le faʻataʻitaʻiga mole mole faʻataʻitaʻiga na faʻaalia i le Ata 1. O le mama o le faʻataʻitaʻiga mata e tusa ma le 88% e pei ona suʻesuʻeina e le HPLC.Mo le faʻamamaina o nei faʻalapotopotoga o le maualuga o le polarity, o le faʻataʻitaʻiga o le a tau le taofia i luga o koluma masani C18 e tusa ai ma o tatou aafiaga muamua.O le mea lea, o se koluma C18AQ na faʻaaogaina mo le faʻamamaina o faʻataʻitaʻiga.
Ata 1. Le ata fa'ata'atia ole fa'ata'ita'iga mole mole fa'ata'ita'iga.
Ina ia saunia le vaifofo faʻataʻitaʻiga, 50 mg faʻataʻitaʻiga mama na faʻamavaeina i le 5 mL vai mama ona faʻauluina lea ina ia mafai ai ona avea ma se vaifofo manino atoatoa.O le vaifofo faʻataʻitaʻi na tui i totonu o le koluma moli e se tui.O le fa'ata'ita'iga fa'ata'ita'iga o le fa'amama moli sa lisiina i le Laulau 1.
Meafaigaluega | SepaBean™ masini 2 | |
Cartridges | 12 g SepaFlash C18AQ RP kesi moli (silika lapotopoto, 20 - 45μm, 100 Å, Numera oka:SW-5222-012-SP(AQ)) | |
Umi ole galu | 204 nm, 220 nm | |
Vaega feavea'i | Solvent A: Vai Solvent B: Acetonitrile | |
Fuafuaga tafe | 15 mL/min | |
Fa'ata'ita'iga uta | 50 mg | |
Gradient | Taimi (min) | Solvent B (%) |
0 | 0 | |
19.0 | 8 | |
47.0 | 80 | |
52.0 | 80 |
I'uga ma Talanoaga
O le chromatogram flash o le faʻataʻitaʻiga i luga o le kalama C18AQ na faʻaalia i le Ata 2. E pei ona faʻaalia i le Ata 2, o le faʻataʻitaʻiga maualuga maualuga na faʻatumauina lelei i luga o le pusa C18AQ.Ina ua maeʻa le lyopholization mo vaega vaega na aoina, o le oloa faʻamoemoe sa i ai le mama o le 96.2% (e pei ona faʻaalia i le Ata 3) e le HPLC suʻesuʻega.O fa'ai'uga na fa'ailoa mai ai e mafai ona fa'aoga atili le oloa fa'amamāina i le isi laasaga su'esu'ega ma atina'e.
Ata 2. O le chromatogram moli o le fa'ata'ita'iga i luga o se kesi C18AQ.
Ata 3. O le HPLC chromatogram o le oloa fa'atatau.
I le faaiuga, o le SepaFlash C18AQ RP flash cartridge fa'atasi ma le flash chromatography system SepaBean™ masini e mafai ona ofoina atu se fofo vave ma aoga mo le fa'amamaina o fa'ata'ita'iga maualuga.
E uiga i pusa moli uila SepaFlash C18AQ RP
O loʻo i ai se faʻasologa o le SepaFlash C18AQ RP faʻapipiʻi moli ma faʻamatalaga eseese mai le Santai Technology (e pei ona faʻaalia i le Laulau 2).
Numera o mea | Tele o le koluma | Fua Faatatau (mL/min) | Max.Omiga (psi/pa) |
SW-5222-004-SP(AQ) | 5.4 g | 5-15 | 400/27.5 |
SW-5222-012-SP(AQ) | 20 g | 10-25 | 400/27.5 |
SW-5222-025-SP(AQ) | 33 g | 10-25 | 400/27.5 |
SW-5222-040-SP(AQ) | 48 g | 15-30 | 400/27.5 |
SW-5222-080-SP(AQ) | 105 g | 25-50 | 350/24.0 |
SW-5222-120-SP(AQ) | 155 g | 30-60 | 300/20.7 |
SW-5222-220-SP(AQ) | 300 g | 40-80 | 300/20.7 |
SW-5222-330-SP(AQ) | 420 g | 40-80 | 250/17.2 |
Fuafuaga 2. SepaFlash C18AQ RP kasini moli.Mea fa'apipi'i: Silika fa'apipi'i sili C18(AQ) maualuga, 20 - 45 μm, 100 Å.
Mo nisi faʻamatalaga i faʻamatalaga auiliili o le SepaBean™ masini, poʻo le faʻatonuga o faʻamatalaga i le SepaFlash series flash cartridges, faʻamolemole asiasi i la matou upega tafaʻilagi.
Taimi meli: Oke-26-2018