Lappaconitine Hydrobromide

Lappaconitine Hydrobromide(LA) yog ib hom diterpenoid alkaloid, labaconitine, uas yog muab rho tawm thiab cais tawm ntawm aconitum ntawm ranunculus tsev neeg. Nws yog thawj zaug uas tsis yog - yeeb tshuaj analgesic rau hauv nruab nrab paj hlwb hauv Suav teb. Nws muaj cov teebmeem analgesia, antipyretic, detumescence thiab tshuaj loog hauv zos, thiab muaj cov yam ntxwv uas tsis yog -kev quav yeeb quav tshuaj thiab tsis zoo tshwm sim. Nws cov nyhuv analgesic muaj zog dua indomethacin thiab tsis muaj zog dua li morphine. Tam sim no, nws muaj zog analgesic thiab immunomodulatory teebmeem yog tsuas yog siv nyob rau hauv kev kuaj mob thiab kev kho mob kev ua ub no ntawm ntau yam tshwj xeeb, thiab nws yog dav siv nyob rau hauv lub lig analgesia thiab perioperative analgesia ntawm cancer.

Lappaconitine yog ib yam khoom nrov ntawm KINTAI. Tom qab ib xyoo caum ntawm kev tshawb fawb thiab kev loj hlob, KINTAI tau ua tiav kev kov yeej ntau yam teeb meem kev lag luam, ua tiav qhov tshwj xeeb purity hauv txhua pawg. Peb ua raws li cov qauv nruj nruj thiab tswj hwm tus neeg siv khoom - txoj hauv kev zoo, kom ntseeg tau tias txhua yam khoom ua tau raws li cov qauv tshuaj nruj heev - qib. Peb muab cov tuam txhab tshuaj thoob ntiaj teb nrog cov txiaj ntsig zoo thiab muaj kev nyab xeeb botanical intermediates. Raws li kev ntseeg siabtus neeg muag khoomntawm botanical active cov khoom xyaw, peb tuav peb txoj hauj lwm nyob rau hauv botanical extraction technology thiab yog tam sim no lubCov neeg tsim khoom loj tshaj plaws ntawm 96% Lappaconitinenyob rau hauv Suav teb. Thov koj xav tiv tauj peb ntawminfo@kintaibio.com.

 

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Lappaconitine, feem ntau yog muab rho tawm los ntawm cov hauv paus hniav ntawm cov tshuaj ntsuab Aconitum napellus, tau raug kuaj pom tias muaj cov nyhuv analgesic muaj zog, ntev - kev ua tau zoo, thiab ob peb yam kev phiv. Nws yog thawj zaug uas tsis yog - quav tshuaj nyob hauv Suav teb.

LA yog Tuam Tshoj thawj zaug uas tsis yog - quav, tsis yog - opioid analgesic thiab tau suav nrog hauv "thib peb-kauj ruam" tshuaj tua kab mob rau cov neeg mob qog noj ntshav hauv Suav teb. LA's analgesic effect yog qis dua rau morphine, tab sis piv rau pethidine, thiab yog xya npaug zog tshaj li cov tshuaj tua kab mob analgesic aminopyrine. LA muaj qhov pib qeeb ntawm kev ua xua tab sis ntev - cov nyhuv ntev, ua rau nws muaj lwm txoj hauv kev rau tramadol. Cov kev tshawb fawb tau pom tias LA tuaj yeem cuam tshuam cov kab mob ectopic uas tshwm sim los ntawm kev puas tsuaj axonal los ntawm kev cuam tshuam rau qhov hluav taws xob- nyob ntawm sodium thiab calcium channels hauv nruab nrab paj hlwb, yog li thaiv cov paj hlwb. Nws tseem tuaj yeem cuam tshuam kev tso tawm ntawm cov tshuaj P thiab somatostatin los ntawm cov paj hlwb afferent los ntawm inhibiting reuptake ntawm norepinephrine thiab serotonin los ntawm presynaptic daim nyias nyias thiab nce lawv qib nyob rau hauv lub synaptic cleft, li no exerting ib tug muaj zog thiab kav ntev analgesic nyhuv. Nws tuaj yeem ua rau muaj kev ua xua los ntawm inhibiting calcium influx nyob rau hauv cov teeb meem grey nyob ib ncig ntawm lub paj hlwb aqueduct thiab cortical hlwb, nrog rau kev qhia ntawm nuclear factor κB.

(Reference: Kev Tshawb Fawb Kev Tshawb Fawb ntawm Lappaconitine Hydrobromide hauv kev ua kom mob plab, Gong QA, LiM 668-672 (ib.)

1.Tshuaj loog

Laptopaconitine, kuv lub teb chaws thawj zaug uas tsis yog - tshuaj tua kab mob, yog siv los kho ntau yam mob me mus rau nruab nrab, xws li mob qog noj ntshav, mob tom qab phais, thiab sciatica. Clinically, lappaconitine's analgesic efficacy yog xya npaug ntawm aminopyrine, thiab nws tau pom tias muaj kev pab cuam rau cov hniav, trigeminal neuralgia, herpes zoster mob, thiab mob tom qab phais.

2.Anti-inflammatory

Laptopaconitine muaj cov tshuaj tiv thaiv kab mob nruab nrab - mob thiab feem ntau siv hauv cov tshuaj pej xeem los kho cov mob xws li lupus erythematosus, rheumatism, thiab mob caj dab rheumatoid. Laptopaconitine tuaj yeem cuam tshuam tsis muaj kev tsim tawm los ntawm inhibiting NF-κB txoj hauv kev thiab mitogen-activated protein kinase (MAPK) txoj kev taw qhia, yog li txo cov kev qhia ntawm cov kab mob inflammatory (TNF- , IL-1 , IL-6) thiab chemokines (1, Kachiev, MCP-1)

3. Antiarrhythmic

Laptopaconitine's antiarrhythmic effect yog ib qho tshwj xeeb ntawm lappaconitine. Lappaconitine belongs rau Class Ic antiarrhythmic natural product class. Kev ua haujlwm antiarrhythmic ntawm nws cov derivatives yog nyob ntawm halogen ntawm C-5 'txoj hauj lwm ntawm pawg aromatic. Qhov kev txiav txim ntawm halogen hloov pauv cuam tshuam rau kev ua haujlwm lom neeg yog: Br > I > Cl. Lappaconitine hydrobromide yog qhov muaj zog tshaj plaws antiarrhythmic derivative.

4.Anti-Cov nyhuv qog

Lappaconitine sulfate tuaj yeem thaiv A549 hlwb hauv G0 / G1 theem ntawm phosphoinositide 3-kinase / protein kinase B (PI3K / protein kinase B, PKB lossis AKT) qhia txoj hauv kev, ua rau apoptosis, thiab inhibit cell viability thiab proliferation. PI3K / AKT txoj kev taw qhia ua lub luag haujlwm tseem ceeb hauv kev muaj sia nyob ntawm tes, kev loj hlob, thiab kev loj hlob.

5. Tshuaj tiv thaiv -Epileptic Effects

Lappaconitine's inhibition ntawm sodium tam sim no yog siv- nyob ntawm thiab tsis hloov qhov hluav taws xob - nyob ntawm kev ua kom sodium tam sim no thiab inactivation. Lappaconitine xaiv txo lub sijhawm ntawm cov kab mob epileptiform tawm thiab tawg hauv cov neurons uas tshwm sim los ntawm bicuculline, aconitine, lossis Mg2+-dawb sab nraud. Qhov no qhia tau hais tias cov tshuaj tiv thaiv kab mob ntawm lappaconitine tuaj yeem kho los ntawm inhibiting axonal conductance thiab txo cov sodium tam sim no.

Kev Phem Tsis Zoo

Qee lub sij hawm, kiv taub hau, palpitations, urticaria, hauv siab nruj, thiab ua xua pob liab liab tuaj yeem tshwm sim, feem ntau daws nws tus kheej.

Kev txhaj tshuaj tuaj yeem ua rau khaus hauv zos.

Contraindications thiab ceev faj

Cov khoom no yog contraindicated nyob rau hauv cov neeg mob ua xua.

Siv ceev faj rau cov neeg mob uas mob siab lossis lub raum tsis txaus.

Kev nyab xeeb ntawm cov tshuaj no hauv cov poj niam cev xeeb tub thiab lactating tsis paub; kev siv yuav tsum tau ua tib zoo ntsuas qhov kev pheej hmoo.

Siv ceev faj rau cov neeg mob plawv.

Cov tshuaj sib cuam tshuam

Kev siv ua ke nrog rau lwm yam hauv nruab nrab lub paj hlwb kev nyuaj siab (xws li sedatives thiab hypnotics) tuaj yeem txhim kho kev nyuaj siab.

Kev siv ua ke nrog lwm cov tshuaj yog pom zoo nyob rau hauv tus kws kho mob saib xyuas.

Cov Lus Cim Tshwj Xeeb

Kev pib ua haujlwm qeeb: Piv rau ceev- ua cov tshuaj opioids xws li morphine, Lappaconitine Hydrobromide yuav siv li ntawm 30 feeb kom tau txais txiaj ntsig tom qab txhaj tshuaj, ua rau nws tsis haum rau cov xwm txheej hnyav uas yuav tsum tau ua kom muaj tshuaj loog tam sim.

Kev tsim cov lappaconitine feem ntau yog ua raws li cov qauv sib txawv kom tau raws li kev xav tau ntawm kev kho mob sib txawv. Cov hauv qab no yog nws cov ntawv loj npaum li cas thiab cov qauv tsim:

1. Txhaj tshuaj

Qhov no yog cov feem ntau classic thiab ntau npaum li cas daim ntawv, siv rau mob, mob nruab nrab mus rau hnyav.

Formula:

Cov khoom xyaw nquag: lappaconitine hydrobromide

Solvent: Dej rau kev txhaj tshuaj

pH adjuster: Dilute hydrochloric acid los yog sodium hydroxide tov yog feem ntau siv los kho cov pH mus rau qhov tsim nyog ntau yam (feem ntau 4.0-6.0) los xyuas kom meej cov tshuaj stability thiab txo qhov khaus thaum txhaj tshuaj.

Muaj peev xwm excipients: Antioxidants (xws li sodium bisulfite) qee zaum ntxiv los txhim kho kev ruaj ntseg.

Common zog: 4mg / 2ml, 8mg / 2ml, thiab lwm yam.

Txoj kev ntawm kev tswj hwm: kev txhaj tshuaj intramuscular lossis intravenous infusion.

2. ntsiav tshuaj / ntsiav tshuaj

Qhov no yog siv rau kev saib xyuas kev kho mob ntev, mob tsis tu ncua thiab yooj yim rau kev tswj hwm.

Formula:

Cov khoom xyaw nquag: lappaconitine hydrobromide

Bulker: Xws li hmoov txhuv nplej siab, lactose, thiab microcrystalline cellulose, siv los ua kom cov ntsiav tshuaj hnyav. Binders, xws li polyvinylpyrrolidone (PVP) thiab starch slurry, yog siv los khi cov hmoov.

Disintegrants, xws li cross-txuas sodium carboxymethyl cellulose thiab qis- hloov hydroxypropyl cellulose, txhawb cov ntsiav tshuaj disintegration hauv plab hnyuv.

Lubricants, xws li magnesium stearate thiab talc, pab txhawb cov ntsiav tshuaj compression.

Common zog: 5 mg / ntsiav tshuaj.

3. Patches (Transdermal Drug Delivery System)

Daim ntawv tshuaj noj tshiab no muab kev noj qab haus huv, ruaj khov thiab tshwj xeeb tshaj yog rau cov neeg mob uas mob ntev uas yuav tsum tau noj tshuaj ntev ntev (xws li mob qog noj ntshav). Nws zam thawj zaug - kis kab mob siab thiab mob plab hnyuv.

Formulation:

Cov khoom xyaw nquag: Lappaconitine hydrobromide

Siab- cov nplaum nplaum, xws li polyacrylates, silicones, los yog polyisobutylene, ua kom lub thaj ua rau daim tawv nqaij thiab ua haujlwm ua cov dej ntim tshuaj thiab tso tsheb.

Penetration enhancers, xws li aminoketone thiab oleic acid, pab cov tshuaj nkag mus rau stratum corneum.

Cov txheej txheem rov qab: Ib qho dej- zaj duab xis impermeable uas tiv thaiv cov tshuaj evaporation thiab lwm yam kab mob. Anti- txheej nplaum: Ib txheej tiv thaiv kom raug tshem tawm ua ntej siv.

Qhov zoo: Cov tshuaj ntshav ruaj khov siab, ntev - cov nyhuv kav ntev (ntev ntev dua 24 teev), siv tau yooj yim, thiab ua raws li tus neeg mob zoo.

Cim npe nrov: Tuam Tshoj lappaconitine hydrobromide manufacturers, lwm tus neeg, Hoobkas