Mingzu Yang, Bo Xu
Isicelo se-R&D Centre
Intshayelelo
I-Antibiotics yiklasi yee-metabolites zesibini eziveliswa yi-microorganisms (kubandakanywa ibhaktheriya, i-fungi, i-actinomycetes) okanye iikhompawundi ezifanayo ezixutywe ngeekhemikhali okanye ze-semi-synthesized.Amayeza okubulala iintsholongwane anokuthintela ukukhula kunye nokuphila kwezinye iintsholongwane.I-antibiotic yokuqala efunyenwe ngumntu, i-penicillin, yafunyanwa yi-microbiologist yaseBritani u-Alexander Fleming ngo-1928. Wabona ukuba iibhaktheriya ezikummandla wokungunda azikwazi ukukhula kwisitya senkcubeko ye-staphylococcus esasingcoliswe ngundo.Wachaza ukuba umngundo kufuneka ukhuphe into yokulwa neentsholongwane, awathi wayibiza ngokuba yipenicillin ngo-1928. Nangona kunjalo, izithako ezisebenzayo azizange zihlanjululwe ngelo xesha.Ngowe-1939, uErnst Chain noHoward Florey beYunivesithi yaseOxford bagqiba ekubeni benze iyeza elinokunyanga izifo ezibangelwa ziintsholongwane.Emva kokuqhagamshelana noFleming ukuze bafumane iintlobo, baye bakhupha ngempumelelo kwaye bayihlambulula ipenicillin kwiintlobo.Ngophuhliso lwabo oluyimpumelelo lwepenicillin njengechiza lonyango, uFleming, Chain noFlorey babelane ngeBhaso leNobel kuNyango ngowe-1945.
Ii-antibiotics zisetyenziswa njenge-antibacterial agents ukunyanga okanye ukuthintela usulelo lwebhaktheriya.Kukho iindidi ezininzi ezingundoqo zamayeza okubulala iintsholongwane asetyenziswa njengee-antibacterial agents: i-β-lactam antibiotics (kubandakanywa ne-penicillin, i-cephalosporin, njl.), i-antibiotics ye-aminoglycoside, i-macrolide antibiotics, i-tetracycline antibiotics, i-chloramphenicol (i-total synthetic antibiotic), kunye njl. i-biological fermentation, i-semi-synthesis kunye ne-synthesis epheleleyo.I-antibiotics eveliswa yi-biological fermentation kufuneka iguqulwe ngokwesakhiwo ngeendlela zekhemikhali ngenxa yokuzinza kweekhemikhali, iziphumo ezinobungozi obunobungozi, i-antibacterial spectrum kunye neminye imiba.Emva kokuguqulwa kweekhemikhali, amayeza okubulala iintsholongwane anokuzuza uzinzo olongezelelekileyo, ukunciphisa iziphumo ebezingalindelekanga ezinetyhefu, ukwandiswa kwe-antibacterial spectrum, ukunciphisa ukunganyangeki kwechiza, ukuphucula ukufumaneka kwe-bioavailability, kwaye ngaloo ndlela kuphuculwe isiphumo sonyango lwamachiza.Ke ngoko, i-semi-synthetic antibiotics okwangoku yeyona ndlela idumileyo ekuphuhliseni amayeza okubulala iintsholongwane.
Kuphuhliso lwe-semi-synthetic antibiotics, i-antibiotics ineempawu zokuhlambuluka okuphantsi, ezininzi zeemveliso kunye namacandelo anzima kuba athathwe kwiimveliso ze-microbial fermentation.Kule meko, uhlalutyo kunye nokulawulwa kokungcola kwi-antibiotics ye-semi-synthetic kubaluleke kakhulu.Ukuze uchonge ngokufanelekileyo kwaye ubonakalise ukungcola, kuyimfuneko ukufumana inani elaneleyo lokungcola kwimveliso yokwenziwa kwe-antibiotics ye-semi-synthetic.Phakathi kweendlela ezixhaphakileyo zokulungiselela ukungcola, ichromatography yindlela engabizi kakhulu enezibonelelo ezifana nesampulu enkulu yokulayisha, ixabiso eliphantsi, ukonga ixesha, njl njl.
Kwesi sithuba, ukungcola okuphambili kwe-semi-synthetic aminoglycoside antibiotics kwasetyenziswa njengesampulu kwaye yacocwa yikhatriji ye-SepaFlash C18AQ edityaniswe nenkqubo ye-flash chromatography umatshini we-SepaBean™.Imveliso ekujoliswe kuyo ihlangabezane neemfuno ifunyenwe ngempumelelo, iphakamisa isisombululo esisebenza kakhulu sokucocwa kwezi zixhobo.
iCandelo loMfuniselo
Isampulu inikezelwe ngobubele yinkampani yasekuhlaleni exuba amayeza.Isampuli yayiluhlobo lwe-amino polycyclic carbohydrates kunye nesakhiwo sayo se-molecular sasifana ne-antibiotics ye-aminoglycoside.I-polarity yesampulu yayiphezulu kakhulu, iyenza inyibilike kakhulu emanzini.Umzobo oqingqiweyo wesampulu yesakhiwo semolekyuli uboniswe kuMfanekiso 1. Ukucoceka kwesampulu eluhlaza kwakumalunga ne-88% njengoko kuhlalutywa yi-HPLC.Ukuhlanjululwa kwezi zixhobo ze-polarity ephezulu, isampuli iya kugcinwa ngokungaqhelekanga kwiikholamu zeC18 eziqhelekileyo ngokwamava ethu angaphambili.Ngoko ke, ikholamu ye-C18AQ yayisetyenziselwe ukuhlanjululwa kwesampuli.
Umzobo 1. Umzobo oqingqiweyo wesampulu yesakhiwo semolekyuli.
Ukulungiselela isisombululo sesampulu, i-50 mg isampuli ekrwada yachithwa kwi-5 mL yamanzi acocekileyo kwaye emva koko i-ultrasonicated ukwenzela ukuba ibe yisisombululo esicacileyo ngokupheleleyo.Isisombululo sesampulu sathi safakwa kwikholamu yeflash nge-injector.Ukusetwa kovavanyo lokucocwa kweflash kudweliswe kwiThebhile yoku-1.
| Isixhobo | Umatshini weSepaBean™ 2 | |
| Iikhatriji | 12 g SepaFlash C18AQ RP flash cartridge (silica spherical, 20 - 45μm, 100 Å, inombolo Order: SW-5222-012-SP(AQ)) | |
| Ubude bamaza | 204 nm, 220 nm | |
| Isigaba esiphathwayo | Isinyibilikisi A: Amanzi Isinyibilikisi B: IAcetonitrile | |
| Umgangatho wohambo | 15 mL/min | |
| Ukulayisha isampulu | 50 mg | |
| Umgangatho | Ixesha (min) | Isinyibilikisi B (%) |
| 0 | 0 | |
| 19.0 | 8 | |
| 47.0 | 80 | |
| 52.0 | 80 | |
Iziphumo neengxoxo
I-chromatogram ye-flash yesampuli kwi-cartridge ye-C18AQ iboniswe kwi-Figure 2. Njengoko kuboniswe kwi-Figure 2, isampuli ye-polar kakhulu igcinwe ngokufanelekileyo kwi-cartridge ye-C18AQ.Emva kwe-lyopholization yamacandelo aqokelelweyo, imveliso ekujoliswe kuyo yayinobunyulu be-96.2% (njengoko kuboniswe kuMfanekiso 3) ngohlalutyo lwe-HPLC.Iziphumo zabonisa ukuba imveliso esulungekisiweyo ingaphinda isetyenziswe kwinyathelo elilandelayo lophando nophuhliso.
Umzobo 2. I-chromatogram ye-flash yesampuli kwi-cartridge ye-C18AQ.
Umzobo 3. Ichromatogram ye-HPLC yemveliso ekujoliswe kuyo.
Ukuqukumbela, i-SepaFlash C18AQ RP flash cartridge edityaniswe ne-flash chromatography system Umatshini we-SepaBean™ unokubonelela ngesisombululo esikhawulezayo nesisebenzayo sokucocwa kweesampulu eziphola kakhulu.
Malunga SepaFlash C18AQ RP flash iikhatriji
Kukho uluhlu lwee-cartridges ze-SepaFlash C18AQ RP ezineenkcazo ezahlukeneyo kwi-Santai Technology (njengoko kuboniswe kwiThebhile 2).
| Inombolo yento | Ubungakanani beKholam | Umgangatho wohambo (mL/min) | Uxinzelelo olukhulu (psi/bar) |
| SW-5222-004-SP(AQ) | 5.4 g | 5-15 | 400/27.5 |
| I-SW-5222-012-SP(AQ) | 20 g | 10-25 | 400/27.5 |
| I-SW-5222-025-SP(AQ) | 33 g | 10-25 | 400/27.5 |
| I-SW-5222-040-SP(AQ) | 48 g | 15-30 | 400/27.5 |
| I-SW-5222-080-SP(AQ) | 105 g | 25-50 | 350/24.0 |
| I-SW-5222-120-SP(AQ) | 155 g | 30-60 | 300/20.7 |
| I-SW-5222-220-SP(AQ) | 300 g | 40-80 | 300/20.7 |
| I-SW-5222-330-SP(AQ) | 420 g | 40-80 | 250/17.2 |
Itheyibhile 2. SepaFlash C18AQ RP flash cartridges.Izinto zokupakisha: Ukusebenza okuphezulu kwe-spherical C18 (AQ) -i-silica edibeneyo, i-20 - 45 μm, 100 Å.
Ngolwazi oluthe vetshe ngeenkcukacha zomatshini weSepaBean™, okanye ulwazi lokuodola kwiikhatriji zeSepaFlash, nceda undwendwele iwebhusayithi yethu.
Ixesha lokuposa: Oct-26-2018