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Nsacha nke adịghị ọcha nke ukwuu na ọgwụ nje site na kọlụm C18AQ

Nsacha nke adịghị ọcha nke ukwuu na ọgwụ nje site na kọlụm C18AQ

Mingzu Yang, Bo Xu
Ngwa R&D Center

Okwu mmalite
Ọgwụ nje bụ klaasị metabolites nke abụọ na-emepụta site na microorganisms (gụnyere nje bacteria, fungi, actinomycetes) ma ọ bụ ogige ndị yiri ya nke ejiri kemịkalụ ahazi ma ọ bụ ọkara.Ọgwụ nje nwere ike igbochi uto na nlanarị microorganisms ndị ọzọ.Ọkachamara microbiologist nke Britain bụ Alexander Fleming chọtara ọgwụ nje mbụ mmadụ chọtara na 1928. Ọ chọpụtara na nje nje ndị dị n'akụkụ ebu ahụ enweghị ike itolite na efere omenala staphylococcus bụ́ nke ebu ebu.O kwuputara na ebu ahụ aghaghị izopụta ihe na-egbu nje, bụ́ nke ọ kpọrọ penicillin n’afọ 1928. Otú ọ dị, a sachaghị ihe ndị na-emepụta ihe n’oge ahụ.Na 1939, Ernst Chain na Howard Florey nke Mahadum Oxford kpebiri imepụta ọgwụ nwere ike ịgwọ ọrịa nje.Mgbe ha kpọtụchara Fleming ka ha nweta ụdị ahụ, ha wepụrụ ma sachaa penicillin n'ụdị ahụ nke ọma.Maka mmepe nke penicillin ha na-aga nke ọma dị ka ọgwụ ọgwụgwọ, Fleming, Chain na Florey keere ihe nrite Nobel na Medicine 1945.

A na-eji ọgwụ nje mee ihe dị ka ihe na-egbu nje iji gwọọ ma ọ bụ gbochie nje nje.E nwere ọtụtụ ụdị ọgwụ nje ndị a na-eji dị ka ihe na-egbu nje: β-lactam ọgwụ nje (gụnyere penicillin, cephalosporin, wdg), ọgwụ nje aminoglycoside, ọgwụ nje macrolide, ọgwụ nje tetracycline, chloramphenicol (mkpokọta ọgwụ nje sịntetik), na ihe ndị ọzọ. Isi mmalite nke ọgwụ nje gụnyere gụnyere ọgwụ nje. ndu gbaa ụka, ọkara njikọ na mkpokọta njikọ.Ọ dị mkpa ka ejiri ụzọ kemịkal gbanwee n'ụzọ nhazi ọgwụ nje ndị sitere na gbaa ụka ndu n'ihi nkwụsi ike kemịkalụ, mmetụta ndị na-egbu egbu, ụdị nje bacteria na okwu ndị ọzọ.Mgbe emezichara ya na kemịkalụ, ọgwụ nje nwere ike nweta nkwụsi ike na-abawanye, belata mmetụta ndị na-egbu egbu, gbasaa ụdịdị dị iche iche nke nje bacteria, ibelata nguzogide ọgwụ, mezie bioavailability, wee si otú a kwalite mmetụta ọgwụgwọ ọgwụ.Ya mere, ọgwụ nje ndị na-emepụta ihe na-emepụta ihe bụ ihe ndị kasị ewu ewu ugbu a na mmepe nke ọgwụ nje.

Na mmepe nke ọkara sịntetik ọgwụ nje, ọgwụ nje nwere ihe onwunwe nke ịdị ọcha dị ala, ọtụtụ ngwaahịa na ihe mgbagwoju anya ebe ọ bụ na ha sitere na microbial gbaa ụka ngwaahịa.N'okwu a, nyocha na nchịkwa nke adịghị ọcha na ọgwụ nje ndị na-emepụta ihe na-emepụta ihe dị mkpa karịsịa.Iji chọpụta nke ọma ma mara ihe ndị na-adịghị ọcha, ọ dị mkpa iji nweta oke adịghị ọcha site na ngwaahịa sịntetik nke ọgwụ nje semisynthetic.N'ime usoro nkwadebe adịghị ọcha a na-ejikarị, flash chromatography bụ usoro dị ọnụ ahịa nwere uru dị ka nnukwu ego ntinye ego, ọnụ ala dị ala, ịchekwa oge, wdg. Flash chromatography ejirila ndị nyocha sịntetịt rụọ ọrụ.

N'ime ọkwa a, a na-eji isi ihe adịghị ọcha nke ọgwụ nje aminoglycoside semi-synthetic dị ka ihe nlele ma sachaa ya site na katrij SepaFlash C18AQ jikọtara ya na sistemụ chromatography nke SepaBean ™.E nwetara ngwaahịa ezubere iche iji nweta ihe achọrọ nke ọma, na-atụ aro ngwọta dị oke mma maka ịsacha ogige ndị a.

Ngalaba nnwale
Otu ụlọ ọrụ na-emepụta ọgwụ na mpaghara nyere ihe nlele ahụ.Nlereanya ahụ bụ ụdị carbohydrates amino polycyclic na usoro molekụla ya yiri ọgwụ nje aminoglycoside.Polarity nke sample bụ kama elu, na-eme ka ọ dị nnọọ soluble na mmiri.E gosiputara ihe nlere anya nke usoro ihe nlere anya nke ihe nlere anya na onyogho 1. Idị ọcha nke ihe nlere a na-emepụta bụ ihe dịka 88% dịka HPLC nyochara.Maka ịdị ọcha nke ogige ndị a nke polarity dị elu, a ga-ejigide ihe nlele ahụ na kọlụm C18 oge niile dịka ahụmịhe anyị gara aga.Ya mere, a na-eji kọlụm C18AQ rụọ ọrụ maka nchacha nlele.

Onyonyo 1. Eserese schematic nke usoro ihe omimi nke ihe nlele.
Iji kwadebe ihe ngwọta ihe atụ, 50 mg crude sample na-agbaze na 5 ml mmiri dị ọcha wee ultrasonicated iji mee ka ọ ghọọ ngwọta doro anya.A na-agbanyezi ihe ngwọta nlele ahụ n'ime kọlụm flash site na injector.Edepụtara nhazi nnwale nke nchacha ọkụ na tebụl 1.

Akụrụngwa

Igwe SepaBean™ 2

Katrij

12 g SepaFlash C18AQ RP flash katrij (silica sppherical, 20 - 45μm, 100 Å, Nọmba ịtụ: SW-5222-012-SP(AQ))

Ogologo ogologo

204 nm, 220 nm

Usoro mkpanaka

Ihe mgbaze A: Mmiri

Ihe mgbaze B: Acetonitrile

Ọnụego mgbaba

15 ml / min

Nbudata ihe atụ

50 mg

Gradient

Oge (nkeji)

Ihe mgbaze B (%)

0

0

19.0

8

47.0

80

52.0

80

Nsonazụ na mkparịta ụka
E gosipụtara chromatogram flash nke ihe nlele na katrij C18AQ na eserese 2. Dị ka egosiri na eserese 2, a na-edobe ihe nlele pola nke ọma na katrij C18AQ.Mgbe lyopholization maka ụmụ irighiri ihe anakọtara, ngwaahịa e lekwasịrị anya nwere ịdị ọcha nke 96.2% (dị ka egosiri na eserese 3) site na nyocha HPLC.Nsonaazụ gosiri na enwere ike iji ngwaahịa emechara eme ihe na nyocha na mmepe nke ọzọ.

Ọgụgụ 2. chromatogram flash nke ihe nlele na katrij C18AQ.

Onyonyo 3. HPLC chromatogram nke ngwaahịa ebumnuche.

Na mmechi, SepaFlash C18AQ RP flash katrij jikọtara ya na flash chromatography sistem SepaBean ™ igwe nwere ike na-enye ngwa ngwa na dị irè ngwọta maka ịdị ọcha nke ukwuu pola samples.

Banyere SepaFlash C18AQ RP flash katrij
Enwere usoro nke SepaFlash C18AQ RP flash cartridges nwere nkọwa dị iche iche sitere na teknụzụ Santai (dị ka egosiri na Tebụl 2).

Nọmba ihe

Nha kọlụm

Ọnụego mgbaba

(mL/min)

Oke. Nrụgide

(psi/bar)

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

Tebụl 2. SepaFlash C18AQ RP flash katrij.Ihe nkwakọ ngwaahịa: C18 (AQ) na-arụ ọrụ nke ọma, silica jikọtara ọnụ, 20 - 45 μm, 100 Å.

Maka ozi ndị ọzọ gbasara nkọwa zuru ezu nke igwe SepaBean™, ma ọ bụ ozi ịtụ ihe na sepaFlash series flash cartridges, biko gaa na webụsaịtị anyị.


Oge nzipu: Ọktoba 26-2018