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Kuyeretsedwa kwa Zowonongeka Kwambiri za Polar mu Maantibayotiki ndi C18AQ Columns

Kuyeretsedwa kwa Zowonongeka Kwambiri za Polar mu Maantibayotiki ndi C18AQ Columns

Mingzu Yang, Bo Xu
Ntchito R&D Center

Mawu Oyamba
Maantibayotiki ndi gulu la ma metabolites achiwiri opangidwa ndi tizilombo tating'onoting'ono (kuphatikiza mabakiteriya, bowa, actinomycetes) kapena mankhwala ena ofanana omwe amapangidwa ndi mankhwala kapena opangidwa ndi theka.Mankhwala opha tizilombo amatha kulepheretsa kukula ndi kukhala ndi moyo kwa tizilombo tina.Maantibayotiki oyamba omwe adapezeka ndi anthu, penicillin, adapezedwa ndi katswiri wazasayansi waku Britain Alexander Fleming mu 1928. Iye adawona kuti mabakiteriya omwe ali pafupi ndi nkhungu sakanatha kukula mu mbale ya chikhalidwe cha staphylococcus yomwe idaipitsidwa ndi nkhungu.Iye ananena kuti nkhunguyo iyenera kutulutsa mankhwala ophera mabakiteriya, omwe anatcha penicillin mu 1928. Komabe, zosakaniza zomwe zimagwira ntchito sizinayeretsedwe panthawiyo.Mu 1939, Ernst Chain ndi Howard Florey a ku Oxford University anaganiza zopanga mankhwala ochizira matenda oyambitsidwa ndi mabakiteriya.Atalankhulana ndi Fleming kuti apeze tizilombo tating'onoting'ono, adatulutsa ndikuyeretsa penicillin kuchokera kumaguluwo.Chifukwa cha chitukuko chawo chopambana cha penicillin monga mankhwala ochiritsira, Fleming, Chain ndi Florey adalandira Mphotho ya Nobel ya Zamankhwala mu 1945.

Mankhwalawa amagwiritsidwa ntchito ngati antibacterial agents pochiza kapena kupewa matenda a bakiteriya.Pali magulu angapo a maantibayotiki omwe amagwiritsidwa ntchito ngati antibacterial agents: β-lactam antibiotics (kuphatikizapo penicillin, cephalosporin, etc.), maantibayotiki a aminoglycoside, macrolide antibiotics, tetracycline antibiotics, chloramphenicol (okwana opangira mankhwala), ndi zina zotero. biological nayonso mphamvu, theka-kaphatikizidwe ndi okwana kaphatikizidwe.Maantibayotiki opangidwa ndi kuwira kwachilengedwe amayenera kusinthidwa mwadongosolo ndi njira zama mankhwala chifukwa cha kukhazikika kwa mankhwala, zotsatira zoyipa, ma antibacterial sipekitiramu ndi zina.Pambuyo posinthidwa mankhwala, maantibayotiki amatha kukhala okhazikika, kuchepetsa zotsatira zoyipa, kuwonjezera kuchuluka kwa antibacterial, kuchepetsa kukana kwa mankhwala, kupititsa patsogolo kupezeka kwa bioavailability, ndikupangitsa kuti chithandizo chamankhwala chikhale bwino.Chifukwa chake, ma semisynthetic maantibayotiki ndi njira yodziwika kwambiri pakupanga ma antibiotic.

Pakukula kwa maantibayotiki opangidwa ndi theka-synthetic, maantibayotiki amakhala ndi chiyero chochepa, zinthu zambiri zomwe zimapangidwira komanso zigawo zovuta chifukwa zimachokera kuzinthu zowotchera tizilombo.Pankhaniyi, kusanthula ndi kuwongolera zonyansa mu semi-synthetic maantibayotiki ndizofunikira kwambiri.Kuti azindikire bwino ndi kuzindikiritsa zonyansa, ndikofunikira kupeza kuchuluka kokwanira kwa zonyansa kuchokera kuzinthu zopangidwa ndi theka-synthetic maantibayotiki.Pakati pa njira zomwe zimagwiritsidwa ntchito pokonzekera zonyansa, flash chromatography ndi njira yotsika mtengo yomwe ili ndi ubwino monga kuchuluka kwa zitsanzo zotsegula, zotsika mtengo, kupulumutsa nthawi, ndi zina zotero. Flash chromatography yakhala ikugwiritsidwa ntchito kwambiri ndi ofufuza opangira.

Mu positi iyi, zonyansa zazikulu za semi-synthetic aminoglycoside antibiotic zidagwiritsidwa ntchito ngati chitsanzo ndikuyeretsedwa ndi katiriji ya SepaFlash C18AQ yophatikizidwa ndi makina a Flash chromatography system SepaBean™.Chotsatira chomwe chikukwaniritsa zofunikira chidapezedwa bwino, kutanthauza njira yabwino kwambiri yoyeretsera zinthuzi.

Gawo Loyesera
Chitsanzocho chinaperekedwa mokoma mtima ndi kampani yamankhwala yapafupi.Zitsanzozo zinali zamtundu wa amino polycyclic carbohydrates ndipo mawonekedwe ake a maselo anali ofanana ndi maantibayotiki a aminoglycoside.Polarity wa chitsanzo anali m'malo mkulu, kupangitsa kuti sungunuka kwambiri m'madzi.Chithunzi chojambula cha mawonekedwe a mamolekyu a chitsanzocho chinawonetsedwa mu Chithunzi 1. Chiyero cha chitsanzo chaiwisi chinali pafupifupi 88% monga momwe HPLC yafufuzidwa.Pofuna kuyeretsedwa kwa mankhwalawa a polarity apamwamba, chitsanzocho sichidzasungidwa pamizere yokhazikika ya C18 malinga ndi zomwe takumana nazo m'mbuyomu.Chifukwa chake, gawo la C18AQ linagwiritsidwa ntchito poyeretsa zitsanzo.

Chithunzi 1. Chithunzi chojambula cha mawonekedwe a mamolekyu a chitsanzo.
Kukonzekera chitsanzo njira, 50 mg yaiwisi chitsanzo anali kusungunuka 5 mL koyera madzi ndiyeno ultrasonicated kuti likhale lomveka bwino njira.Yankho lachitsanzo lidalowetsedwa mugawo la flash ndi jekeseni.Kukonzekera koyesera kwa kuyeretsa kwa flash kudalembedwa mu Table 1.

Chida

Makina a SepaBean™ 2

Makatiriji

12 g SepaFlash C18AQ RP flash cartridge (silica yozungulira, 20 - 45μm, 100 Å, Nambala ya Order: SW-5222-012-SP(AQ))

Wavelength

204 nm, 220 nm

Gawo la mafoni

Zosungunulira A: Madzi

Zosungunulira B: Acetonitrile

Mtengo woyenda

15 ml / min

Kutsegula kwachitsanzo

50 mg pa

Gradient

Nthawi (mphindi)

Zosungunulira B (%)

0

0

19.0

8

47.0

80

52.0

80

Zotsatira ndi zokambirana
Chromatogram ya flash ya chitsanzo pa cartridge ya C18AQ ikuwonetsedwa mu Chithunzi 2. Monga momwe tawonetsera pa Chithunzi 2, chitsanzo cha polar kwambiri chinasungidwa bwino pa cartridge ya C18AQ.Pambuyo pa lyopholization pazigawo zomwe zasonkhanitsidwa, zomwe tinkafunazo zinali ndi chiyero cha 96.2% (monga momwe tawonetsera pa Chithunzi 3) ndi kusanthula kwa HPLC.Zotsatira zikuwonetsa kuti chinthu choyeretsedwa chikhoza kugwiritsidwanso ntchito pakafukufuku wotsatira ndi chitukuko.

Chithunzi 2. Chromatogram yowala ya chitsanzo pa cartridge ya C18AQ.

Chithunzi 3. Chromatogram ya HPLC ya chinthu chomwe mukufuna.

Pomaliza, SepaFlash C18AQ RP flash cartridge yophatikizidwa ndi flash chromatography system SepaBean™ imatha kupereka yankho lachangu komanso lothandiza pakuyeretsa zitsanzo za polar kwambiri.

Za SepaFlash C18AQ RP flash cartridges
Pali mndandanda wa makatiriji a SepaFlash C18AQ RP omwe ali ndi mawonekedwe osiyanasiyana ochokera ku Santai Technology (monga momwe tawonetsera mu Table 2).

Nambala Yachinthu

Kukula kwa Mzere

Mtengo Woyenda

(mL/mphindi)

Max.Pressure

(psi/bar)

SW-5222-004-SP(AQ)

5.4g pa

5-15

400/27.5

SW-5222-012-SP(AQ)

20 g pa

10-25

400/27.5

SW-5222-025-SP(AQ)

33 g pa

10-25

400/27.5

SW-5222-040-SP(AQ)

48g pa

15-30

400/27.5

SW-5222-080-SP(AQ)

105 g pa

25-50

350/24.0

SW-5222-120-SP(AQ)

155g pa

30-60

300/20.7

SW-5222-220-SP(AQ)

300 g pa

40-80

300/20.7

SW-5222-330-SP(AQ)

420 g pa

40-80

250/17.2

Table 2. SepaFlash C18AQ RP flash cartridges.Zida zonyamula: Silika yolimba kwambiri yozungulira C18(AQ), 20 - 45 μm, 100 Å.

Kuti mumve zambiri zatsatanetsatane wamakina a SepaBean™, kapena kuyitanitsa ma cartridge a SepaFlash, chonde pitani patsamba lathu.


Nthawi yotumiza: Oct-26-2018