Tauroursodeoxycholate hmoov

1 Kev Taw Qhia

Kev taw qhia luv luv: taurine ursodeoxycholic acid sodium yog ib qho dej-soluble bile acid, uas yog siv los kho gallstones thiab cirrhosis.

Alias: 2 - [(3 , xya - Dihydroxy-24-oxo-5 - cholane-24-yl)amino]-1-ethanesulfonic acid sodium ntsev

Physical Properties thiab Indicators:

Cov tsos mob: dawb mus rau ze li ntawm cov khoom dawb

Solubility:............ Dej: 100mg/ml; DMSO: 100mg / ml; Ethanol: 50mg / ml (sov)

Poob ntawm ziab:............ Tsawg dua lossis sib npaug rau 8.0 feem pua

Cov ntsiab lus (TLC):............ Ntau dua lossis sib npaug li 97 feem pua

Cia tej yam kev mob: 2-8 degree, kaw thiab qhuav, tiv thaiv los ntawm lub teeb thiab noo noo

Kev thauj mus los: kev thauj mus los ntawm qhov kub thiab txias

Kev ua haujlwm lom neeg:

Hauv vitro, taurine ursodeoxycholic acid muaj qhov cuam tshuam rau 17 EG-induced cVA-of-CLF raug mob pom muaj kev tiv thaiv thiab rov qab los. Hauv Mz-ChA-1 cholangiocarcinoma hlwb, taurine ursodeoxycholic acid inhibits cell loj hlob los ntawm Ca2 ntxiv -, PKC -, thiab MAPK-nyob rau hauv txoj kev. Hauv cov nas hepatocytes cais, taurine ursodeoxycholic acid dhau los ntawm 1-integrin-mediated cAMP tsim inhibits kua tsib acid-vim apoptosis.

Hauv vivo txoj kev tshawb fawb: taurine ursodeoxycholic acid (360 μ Mol / kg, iv) cuam tshuam qhov txo qis ntawm cov kua tsib, thiab nce cov dej num ntawm alkaline phosphatase, leucine aminopeptidase thiab alanine transaminase, nrog rau cov concentration ntawm cov cholesterol, phospholipids thiab cov kua tsib. kua qaub.

2 Muaj nuj nqi

Sodium taurine ursodeoxycholic acid, tseem hu ua taurine ursodeoxycholic acid thiab taurine ursodeoxycholic acid, tshuaj lub npe yog 3, xya Dihydroxycholanyl-N-ttaurine, uas feem ntau muaj nyob rau hauv cov kua tsib ntawm dub dais, yog ib tug landmark zoo muaj nyob rau hauv dais bile. Nws muaj antispasmodic, anticonvulsive, anti-inflammatory thiab gallstone dissolving teebmeem. Cov tshuaj hluavtaws niaj hnub taurine ursodeoxycholic acid yog cov kua tsib ua ke tsim los ntawm kev sib xyaw ntawm cov amino pawg ntawm taurine thiab somyl pawg ntawm ursodeoxycholic acid. Taurine ursodeoxycholic acid capsules tau teev nyob rau hauv txawv teb chaws, thiab tau pom zoo muag nyob rau hauv Tuam Tshoj raws li cov tshuaj txawv teb chaws nyob rau hauv 2007. Lawv yog tsuas yog siv rau kev kho mob ntawm cholesterol gallstones, thawj sclerosing cholangitis, thawj biliary cirrhosis thiab kab mob siab C. Tam sim no , tsis muaj kev sau npe tshuaj hauv Suav teb rau cov khoom siv raw ntawm taurine ursodeoxycholic acid thiab nws cov kev npaj. Bovine ursodeoxycholic acid sodium yog cov kua tsib kua qaub uas cais los ntawm Chemicalbook dais bile, uas yog cov tshuaj lom neeg. Nws yog hydrophilic bile acid thiab cov roj cholesterol dissolving tus neeg sawv cev, uas yog ua ke nrog taurine hauv cov kua tsib. Nws tuaj yeem txo qis cov roj cholesterol los ntawm lub siab, txo qis cov roj cholesterol hauv cov kua tsib, txhawb cov kua tsib kua qaub, ua kom cov roj cholesterol nyob hauv cov kua tsib, yaj cov roj cholesterol los yog tiv thaiv kev tsim cov pob zeb. Nws tuaj yeem ua rau kom cov kua tsib tso tawm, so lub sphincter ntawm cov kua tsib lub qhov ncauj thiab tsim cov nyhuv cholagogic, uas yog qhov zoo rau cov pob zeb tawm. Cov khoom no tsis tuaj yeem yaj lwm hom gallstones. Nws muaj feem xyuam rau kev kho mob ntawm cov cholesterol gallstones, hyperlipidemia, bile secretion disorders, thawj biliary cirrhosis, kab mob siab ntev, bile reflux gastritis thiab kev tiv thaiv ntawm acute rejection thiab cov tshuaj tiv thaiv ntawm daim siab transplantation. Lub pob zeb dissolving nyhuv ntawm cov khoom no yog me ntsis weaker tshaj li ntawm chenodeoxycholic acid.

3 Daim ntawv thov

Kev tshawb fawb biochemical; Lipase accelerator; Anion tshem tawm rau cov protein ntau; Kev npaj cov kab mob kab mob nruab nrab (cov kab mob hauv plab hnyuv thiab kev cais tawm); Solubilizing detergent rau lipids thiab cell membrane ciam teb proteins

4 Tus Qauv Zoo

5 Flow Chart

1) Kev npaj ntawm crude taurine ursodeoxycholic acid yog ua raws li nram no: nyob rau hauv lub reactor, ntxiv 4.0KG ursodeoxycholic acid, ntxiv 19KG acetone, ntxiv 1650ml triethylamine nyob rau hauv nplawm, qhib lub tsho tub yees, thiab txo qhov kub ntawm qhov sib tov rau - 10 degree . Ntxiv 1120ml ntawm ethyl chloroformate hauv cov dej ntws, tswj kev ntxiv ceev ntawm ethyl chloroformate, tswj qhov kub ntawm cov tshuaj tiv thaiv ntawm - 5-0 degree , thiab ntxiv rau hauv 30 feeb. Txuas ntxiv tswj qhov kub thiab txias rau cov tshuaj tiv thaiv rau 40 feeb los npaj cov anhydride sib xyaw ntawm ursodeoxycholic acid thiab ethyl chloroformate. Nias thiab lim cov tshuaj tiv thaiv anhydride saum toj no los ntawm lub lim nrog nitrogen rau hauv {{10}} liter reactor uas muaj 4.2KG ntawm cov dej huv huv, 1.4KG ntawm taurine, thiab 0.4KG ntawm sodium hydroxide, Siab do thiab hnov ​​mob rau 3 teev ntxiv los npaj cov khoom nyoos ntawm taurine ursodeoxycholic acid 4.0KG. 2) Kev ua kom zoo ntawm cov khoom nyoos ntawm taurine ursodeoxycholic acid yog ua raws li hauv qab no: (1) Muab 4.0KG taurine ursodeoxycholic acid rau hauv 50L reactor, ntxiv 4KG dej thiab 580ml acetone, kub thiab do kom txog thaum nws yaj tag; (2) Txias mus rau - 5-0 degree nyob rau hauv stirring, crystallization rau 30 teev; (3) Muab cov khoom tso rau hauv lub lim rau kev nqus pom. Tom qab tshem tawm, yaug lub ncuav mog qab zib lim dej nrog dej khov (- 3-0 degree), thiab tom qab ntawd qhuav nws dua kom tau txais taurine ursodeoxycholic acid 3.3KG (purity 99.6 feem pua, HPLC). Cov ntsiab lus ntawm taurine ursodeoxycholic acid yog 0.3 feem pua, thiab cov ntsiab lus siab tshaj plaws ntawm lwm yam impurities yog 0.05 feem pua ​​(txiav txim siab los ntawm cov kua chromatography).

6 NMR

7.MOA

Siv reflux extraction, ultrasonic extraction rau 15, 30 thiab 45 feeb, tshem tawm kom txias, dilute mus rau 50 mL nrog anhydrous ethanol, thiab txiav txim siab tus nqi rho tawm.

Daim duab 1 HPLC daim duab ntawm sodium tauronodeoxycholic acid tswj (A), compound bile gel qauv (B) thiab cov tshuaj tsis zoo (tsis muaj cov kua tsib, C)

Fig.1 HPLC chromatograms ntawm tauroursodeoxycholic acid sodium ntsev (A). kua tsib capsu

Te (B) thiab cov tshuaj tsis zoo (tsis muaj cov kua tsib, C)

(Peak cheeb tsam / qauv hnyav) yog 1618.51647.51886.01891.1 raws. Cov txiaj ntsig tau pom tias qhov kev tshem tawm ultrasonic tau pib ua tiav hauv 45 min, yog li kev ntsuas ultrasonic 45 min tau siv, uas yog, noj 0.5g ntawm cov khoom, ntsuas nws kom raug, muab tso rau hauv ib lub raj mis triangular, ntxiv 45 mL ntawm cov ethanol kiag li. , rho tawm rau 45 feeb, tshem tawm thiab txias nws, thiab ces dilute nws mus rau 50 mL ntawm kiag li ethanol.

2.2.3 Xaus kev tshawb nrhiav kev sib raug zoo: Ntsuas taurine ursodeoxycholic acid sodium aptamer kom raug, npaj 0.24gL-1 siv tshuaj, thiab nqus 6, 8, 10, 1 raws li

6, 23, 25, raws li cov xwm txheej chromatographic, txhaj rau hauv cov kua chromatograph siab, thiab ntsuas qhov chaw siab tshaj. Nrog rau qhov chaw siab tshaj qhov tseem ceeb raws li kev tswj hwm thiab tus nqi ntawm sodium taurocholate (ug) raws li abscissa, kos tus qauv nkhaus thiab xam qhov sib npaug regression. Cov kab zauv kab zauv yog y=292.12x{5}}.445 (r=0.9999). Cov txiaj ntsig tau pom tias sodium tauronodeoxycholate muaj kev sib raug zoo ntawm 1.45 thiab 5.00 Ng.

2.2.4 Precision test Siv 2.4 mg ntawm sodium taurocholate raws li kev tswj hwm, muab tso rau hauv 10ml vial, ntxiv cov theem txawb kom yaj thiab dilute nws mus rau qhov teev, co nws zoo, noj 10 mL ntawm cov cua huv, txhaj cov qauv rau 6 lub sijhawm sib law liag, thiab RSD ntawm thaj chaw ncov ntawm qhov tseem ceeb ntawm cholic acid yog 2.1 feem pua. Qhov tshwm sim qhia tau hais tias qhov ntsuas tau zoo precision.

2.2.5 Stability test Coj tib qhov kev ntsuam xyuas thiab txiav txim siab raws li txoj cai ntawm 0, 4, 8, 12, 16 thiab 24 teev tom qab kev npaj. Qhov tshwm sim yog qhov chaw siab tshaj ntawm ursolic acid

Tus nqi tseem ceeb RSD yog 1.1 feem pua. Qhov tshwm sim qhia tau hais tias qhov kev sim tshuaj yog ruaj khov nyob rau hauv 24 teev.

2.2.6 Repeatability test: Nyhav 6 cov qauv ntawm tib tus lej, npaj lawv raws li kev npaj ntawm cov tshuaj ntsuam xyuas, siv cov txheej txheem chromatographic saum toj no rau kev txiav txim siab, raug nqus 10 mL ntawm txhua tus qauv thiab txhaj tshuaj. rau hauv cov kua chromatograph ua haujlwm siab, sau qhov chaw siab tshaj ntawm txhua tus qauv, RSD 0.67 feem pua, qhia tias txoj kev muaj kev rov ua tau zoo.

2.2.7 Tus nqi rov qab kuaj tau txais cov qauv ntxiv cov txheej txheem rov qab (1: 1 ntxiv). Ua tib yam ntawm cov qauv nrog cov ntsiab lus hnub qub paub, thiab ntsuas lawv hauv huab cua zoo, 0.15051 xoom point ib

{{0}}, 0 160 12, 0 150 60, 0 157 90. 0.{8}}g. Precisely ntxiv cov kev daws teeb meem ntawm sodium taurine deoxycholate sib npaug rau 2 mg ntawm sodium taurine deoxycholate, ntxiv rau hauv 25 ml volumetric hwj, ntxiv anhydrous ethanol rau ultrasound rau 45 min, sau qhov hnyav poob nrog anhydrous ethanol, thiab lim. Los ntawm xim

Saib Table 1 rau cov txiaj ntsig ntawm kev txiav txim siab spectral. Cov txiaj ntsig tau pom tias tus nqi rov qab ntawm cov qauv ntxiv yog nyob nruab nrab ntawm 99.55 feem pua ​​​​thiab 104.8 feem pua, thiab tus nqi rov qab yog qhov zoo.

8 Kev Tsim Nyog

Tom qab xyoo ntawm kev tsim khoom, peb lub tuam txhab tau txais daim ntawv tso cai tsim khoom tsim nyog.

9 Tus khub

Peb muaj ntau tus neeg koom tes mus sij hawm ntev thoob plaws ntiaj teb.

10 Cov neeg siv khoom xyuas

Peb tau txais kev qhuas ntau ntawm lwm lub platform, thiab peb cov neeg siv khoom tau zoo siab heev ntawm cov khoom tsim los ntawm peb lub tuam txhab.

11 Exhibition

Peb lub tuam txhab koom nrog ntau yam kev nthuav qhia hauv tsev thiab txawv teb chaws txhua xyoo, thiab sib txuas lus nrog cov neeg siv khoom ntsej muag.

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