Liraglutide ntsiav tshuajyog glucagon zoo li peptide-1 (GLP-1) analogue, teej tug mus rau ntev-acting GLP-1 receptor agonists. Txawm hais tias daim ntawv tseem ceeb tam sim no yog txhaj tshuaj, txoj kev xav, yog tias daim ntawv ntsiav tshuaj tau tsim tiav, nws tseem yuav khaws nws cov yam ntxwv tseem ceeb raws li GLP-1 receptor agonist.
Cov qauv molecular ntawm Liraglutide yog tsim los ntawm genetic recombination thev naus laus zis thiab sib koom ua ke 97% homology nrog tib neeg GLP-1. Nws cov qauv tsim tshwj xeeb molecular, xws li fatty acid side chain modification, txuas lub neej ib nrab ntawm cov tshuaj hauv lub cev, ua rau nws tsuas yog tsim nyog los tswj hwm ib hnub ib zaug. Yog tias tsim los rau hauv cov ntsiav tshuaj, cov txheej txheem tshwj xeeb xws li txheej txheej enteric thiab osmotic twj tso kua mis yuav tsum tau ua kom ruaj khov tso tawm thiab nqus cov tshuaj hauv cov hnyuv. Yog tias tsim los ua cov ntsiav tshuaj, cov lus qhia tshwj xeeb yuav raug tsim los rau cov koob tshuaj sib txawv raws li kev kho mob xav tau (xws li 0.6mg, 1.2mg, 1.8mg, thiab lwm yam), uas yuav tsum tau hloov kho raws li tus yam ntxwv nqus thiab bioavailability ntawm cov tshuaj hauv plab hnyuv.
Peb cov khoom
Cov ntaub ntawv ntxiv ntawm chemical compound:
| Khoom npe | Liraglutide Capsule | Kev txhaj tshuaj liraglutide | Liraglutide ntsiav tshuaj |
| Yam khoom | Capsule | Txhaj tshuaj | Cov ntsiav tshuaj |
| Khoom Purity | Ntau dua lossis sib npaug li 99% | Ntau dua lossis sib npaug li 99% | Ntau dua lossis sib npaug li 99% |
| Khoom Specifications | Customizable | Customizable | Customizable |
| Pob khoom | Customizable | Customizable | Customizable |
Peb Cov Khoom
Liraglutide +. COA
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Certificate of Analysis |
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Compound npe |
Liraglutide | |
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CAS Nr. |
204656-20-2 | |
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Qib |
Pharmaceutical qib | |
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Ntau |
Customized | |
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Ntim txheem |
Customized | |
| Chaw tsim tshuaj paus | Shaanxi BLOOM TECH Co., Ltd | |
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Ntau No. |
20250109001 |
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MFG |
Jan 12th 2025 |
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EXP |
Jan 8th 2029 |
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Qauv |
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| TEST STANDARD | GB/T24768-2009 Kev lag luam. Stnndard | |
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Yam khoom |
Enterprise txheem |
Kev txheeb xyuas qhov tshwm sim |
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Qhov tshwm sim |
Dawb los yog yuav luag dawb hmoov |
Ua raws |
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Cov ntsiab lus dej |
Tsawg dua lossis sib npaug li 4.5% |
0.30% |
| Poob rau ziab |
Tsawg dua lossis sib npaug li 1.0% |
0.15% |
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Hnyav Hlau |
Pb Tsawg dua lossis sib npaug li 0.5ppm |
N.D. |
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Tsawg dua lossis sib npaug li 0.5ppm |
N.D. | |
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Hg Tsawg dua lossis sib npaug li 0.5ppm |
N.D. | |
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Cd Tsawg dua lossis sib npaug li 0.5ppm |
N.D. | |
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Purity (HPLC) |
Ntau dua lossis sib npaug li 99.0% |
99.5% |
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Ib leeg impurity |
<0.8% |
0.48% |
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Residue ntawm ignition |
<0.20% |
0.064% |
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Tag nrho microbial suav |
Tsawg dua lossis sib npaug li 750cfu / g |
80 |
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E. Coli |
Tsawg dua lossis sib npaug li 2MPN / g |
N.D. |
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Salmonella |
N.D. | N.D. |
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Ethanol (los ntawm GC) |
Tsawg dua lossis sib npaug li 5000ppm |
400ppm ua |
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Cia |
Khaws rau hauv qhov chaw kaw, tsaus thiab qhuav ntawm -20 degrees |
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Cov tshuaj sib cuam tshuam thiab ceev faj
Cov tshuaj sib cuam tshuam
Cov kev tshawb fawb hauv vitro tau lees paub tias qhov muaj feem cuam tshuam ntawm pharmacokinetic kev sib cuam tshuam ntawmliraglutide ntsiav tshuajthiab lwm yam active tshuaj muaj feem xyuam rau cytochrome P450 thiab plasma protein khi yog tsawg heev. Txawm li cas los xij, qhov qeeb me me hauv plab hnyuv tawm los ntawm liraglutide tuaj yeem cuam tshuam rau kev nqus ntawm lwm cov tshuaj noj ntawm qhov ncauj tib lub sijhawm. Yog li ntawd, yog tias tsim los rau hauv cov ntsiav tshuaj, kev saib xyuas tshwj xeeb yuav tsum tau them rau kev sib cuam tshuam nrog lwm cov tshuaj hauv qhov ncauj, tshwj xeeb tshaj yog cov uas nkag siab zoo rau kev nqus.
Cov kev ceev faj
Kev kho koob tshuaj: Thaum kho cov koob tshuaj liraglutide, tsis tas yuav tsum kuaj ntshav qabzib (tshwj tsis yog nrog kev kho sulfonylurea thiab kho cov koob tshuaj sulfonylurea). Txawm li cas los xij, thaum ua ke nrog cov tshuaj sulfonylurea rau kev kho mob, kev soj ntsuam cov ntshav qabzib kuj yuav tsum tau hloov kho cov tshuaj sulfonylurea.
Kev kho mob tsis pom zoo: Yog tias nws tsis tau txhaj tshuaj, koob tshuaj hnub tom ntej yuav tsum tau siv ncaj qha raws li cov ntawv sau tshuaj, tsis tas yuav muab cov tshuaj ntxiv lossis nce cov koob tshuaj kom them rov qab rau cov tshuaj uas tsis tau. Yog tias ntau dua 3 hnub tau dhau los txij li kev tswj hwm kawg ntawm liraglutide, cov neeg mob yuav tsum rov pib dua ntawm koob tshuaj 0.6mg raws li kev siv tshuaj ntau ntxiv kom txo tau cov kev mob plab hnyuv cuam tshuam nrog kev rov kho dua. Yog tias tsim los ua cov ntsiav tshuaj, cov hauv paus ntsiab lus ntawm kev siv tshuaj rau cov tshuaj tsis raug yuav txawv ntawm cov tshuaj txhaj. Ib qho kev npaj tshwj xeeb ntxiv yuav tsum tau tsim raws li ib nrab ntawm - lub neej thiab lub sijhawm ntawm kev ua ntawm cov tshuaj.
Efficiency leap Precision thiab stability
Qhov chaw txhaj tshuaj: Kev txhaj tshuaj yuav tsum tau txhaj rau hauv plab, ncej puab, lossis sab caj npab, thaum cov ntsiav tshuaj tsis tas yuav xav txog qhov teeb meem ntawm qhov chaw txhaj tshuaj, tab sis yuav tsum tau them nyiaj rau lub sijhawm tshuaj thiab kev noj zaub mov zoo.
Cov tsos mob tshwj xeeb: Nws tau pom tias kev siv lwm cov tshuaj GLP-1 yog txuam nrog kev pheej hmoo ntawm kev tsim kab mob pancreatitis. Yog li, cov neeg mob yuav tsum tau ceeb toom txog cov tsos mob ntawm tus mob pancreatitis (xws li mob plab thiab mob hnyav). Yog tias xav tias mob pancreatitis, liraglutide thiab lwm yam tshuaj uas muaj qhov tsis txaus ntseeg yuav tsum raug txiav tawm.
Kev nqus ntawm Liraglutide tom qab txhaj tshuaj subcutaneous kuj qeeb, ncav cuag nws qhov siab tshaj plaws 8-12 teev tom qab kev tswj hwm. Ib qho kev txhaj tshuaj subcutaneous ntawm Liraglutide 0 Tom qab 6mg, qhov kwv yees siab tshaj plaws ntawm liraglutide yog 9 4nmol / L (qhov hnyav li ntawm 73 kg). Ntawm qhov koob tshuaj ntawm 1.8mg ntawm liraglutide, qhov nruab nrab tsis tu ncua - xeev concentration (AUCT/24) ntawm liraglutide mus txog kwv yees li 34nmol / L (qhov nruab nrab lub cev hnyav ntawm kwv yees li 76kg). Tom qab tswj hwm 3mg rau cov neeg rog rog (BMI 30-40kg / m2), qhov nruab nrab nyob ruaj khov hauv xeev (AUCT / 24) ntawm Liraglutide mus txog 31nmol / L. Cov qib raug ntawm liraglutide txo qis nrog kev nce lub cev hnyav. Qib raug ntawm liraglutide nce proportionally nrog cov koob tshuaj. Qhov sib txawv ntawm tus kheej ntawm qhov sib txawv ntawm thaj chaw nyob rau hauv cov tshuaj lub sij hawm nkhaus (AUC) rau ib koob tshuaj liraglutide yog 11%. Qhov tseeb bioavailability ntawm Liraglutide tom qab txhaj tshuaj subcutaneous yog li 55%.
Qhov pom meej faib ntim tom qab txhaj tshuaj subcutaneous yog 11-17L, thiab qhov nruab nrab faib ntim tom qab txhaj tshuaj yog 0.07L / kg. Rau ib tus neeg hnyav li 100kg, qhov nruab nrab pom meej ntim ntawm kev faib tawm tom qab txhaj tshuaj subcutaneous yog 20-25L. Liraglutide tuaj yeem khi ntau rau plasma proteins.
Tsis pub dhau 24 teev ntawm ib qho kev tswj hwm ntawm radiolabeled [3H]-liraglutide rau cov neeg noj qab haus huv, cov khoom tseem ceeb hauv ntshav yog liraglutide qauv tshuaj. Ob qhov me me ntawm cov ntshav plasma metabolites tau kuaj pom (tsawg dua lossis sib npaug li 9% thiab tsawg dua lossis sib npaug li 5% ntawm tag nrho cov plasma xov tooj cua, feem). Liraglutide yog metabolized zoo ib yam li macromolecular proteins, thiab tsis muaj lub cev tshwj xeeb tau raug txheeb xyuas raws li txoj hauv kev tshem tawm tseem ceeb.
Tom qab kev tswj hwm ntawm [3H] -liraglutide, tsis muaj qhov qubliraglutide ntsiav tshuajtau kuaj pom hauv cov zis thiab quav. Tsuas yog ib feem me me ntawm cov hluav taws xob tau muab tso tawm raws li Liraglutide cuam tshuam cov metabolites hauv cov zis lossis quav (6% thiab 5%, feem). Cov hluav taws xob hluav taws xob hauv cov zis thiab quav feem ntau yog tawm hauv thawj 6-8 hnub, sib xws rau peb qhov me me ntawm cov metabolites. Qhov nruab nrab tshem tawm ntawm Liraglutide tom qab ib qho kev txhaj tshuaj subcutaneous yog li 0.9-1.4 L / teev, thiab tshem tawm ib nrab-lub neej yog li 13 teev.
(1) Poj niam los txiv neej: Raws li kev tshuaj xyuas pharmacokinetic ntawm cov neeg mob rog rog thiab rog, cov poj niam muaj 24% qis dua qhov hnyav dua li cov txiv neej. Cov pab pawg pharmacokinetic txoj kev tshawb fawb ntawm cov txiv neej thiab poj niam cov neeg mob uas muaj ntshav qab zib hom 2 thiab kev tshawb fawb pharmacokinetic ua rau cov kev noj qab haus huv tau pom tias poj niam los txiv neej yuav tsis muaj kev cuam tshuam loj heev rau cov tshuaj pharmacokinetics ntawm lilalutide. Raws li cov ntaub ntawv raug teb, tsis tas yuav kho qhov ntau npaum li cas raws li poj niam txiv neej.
(2) Cov keeb kwm ntawm haiv neeg: Cov txiaj ntsig ntawm kev tshuaj xyuas pharmacokinetic ntawm cov pej xeem suav nrog cov neeg dawb, dub, Neeg Esxias, thiab lus Mev tau pom tias kev sib txawv ntawm haiv neeg tsis muaj qhov cuam tshuam rau kev kho mob rau cov tshuaj pharmacokinetics ntawm liraglutide.
(3) Qhov hnyav: Kev txheeb xyuas pej xeem ntawm cov neeg laus mob ntshav qab zib hom 2 qhia tias lub cev qhov hnyav (BMI) yuav tsis muaj kev cuam tshuam loj rau cov tshuaj pharmacokinetics ntawm rilalutide. Hauv kev soj ntsuam cov lus teb ntawm kev ntsuas kev ntsuas qhov hnyav, kev noj tshuaj txhua hnub ntawm 3.0mg ntawm liraglutide tuaj yeem muab qhov tsim nyog raug rau hauv qhov hnyav ntawm 60-234kg. Qhov cuam tshuam rau liraglutide txo qis nrog kev nce hauv lub cev hnyav. Tsis muaj kev tshawb fawb txog qib ntawm liraglutide raug rau cov neeg mob hnyav dua 234kg.
(4) Liver function impairment: A single dose clinical trial evaluated the pharmacokinetics of liraglutide in subjects with varying degrees of liver function impairment. Compared to healthy subjects, subjects with mild to moderate liver dysfunction had a 13-23% reduction in exposure to liraglutide. The exposure to liraglutide was significantly reduced (44%) in subjects with severe liver dysfunction (ChildPugh score>9).
(5) Lub raum tsis ua haujlwm: Muab piv rau cov neeg mob lub raum ua haujlwm ib txwm muaj, cov neeg mob lub raum tsis ua haujlwm tau txo qis rau liraglutide. Mob me (creatinine tshem tawm tus nqi, CrCl 50-80ml / min), nruab nrab (CrCI 30-50ml / min), thiab hnyav (CrCl<30ml/min) renal impairment and end-stage renal disease subjects requiring dialysis reduced liraglutide exposure by 33%, 14%, 27%, and 28%, respectively. Similarly, in a 26 week clinical trial, the liraglutide exposure of type 2 diabetes patients with moderate renal impairment (creatinine clearance rate 30-59ml/min) was 26% lower than that of a trial of type 2 diabetes patients with normal renal function or mild renal impairment.
(6) Cov poj niam cev xeeb tub: Cov khoom no yuav tsum tsis txhob siv thaum cev xeeb tub, thiab cov tshuaj insulin raug pom zoo rau lub sijhawm no. Yog tias tus neeg mob npaj yuav cev xeeb tub lossis twb xeeb tub thaum lub sijhawm kho, kev kho mob nrog cov khoom no yuav tsum raug tso tseg. Cov poj niam pub niam mis: Vim tsis muaj kev cuam tshuam, cov khoom no yuav tsum tsis txhob siv thaum lactation. Cov tshuaj me nyuam: Tsis tau txais cov ntaub ntawv tseem ceeb, thiab cov khoom no tsis pom zoo siv rau cov tub ntxhais hluas.
Cov kev sib tw thiab kev cia siab ntawm Kev Txhim Kho Cov Ntsiab Lus
Txoj Kev Sib Tw
Formulation technology: Kev txhim kho ntawm Liraglutide yuav tsum tau daws qhov teeb meem ntawm kev tso tawm ruaj khov thiab nqus cov tshuaj hauv plab hnyuv. Cov txheej txheem tshwj xeeb xws li txheej txheej enteric thiab osmotic twj tso kua mis yuav tsum tau ua kom muaj kev ruaj ntseg thiab bioavailability ntawm cov tshuaj nyob rau hauv lub plab zom mov.
Kev sim tshuaj kho mob: Kev sim tshuaj tshiab yuav tsum tau ua kom paub tseeb txog kev ua tau zoo, kev nyab xeeb, thiab kev zam ntawm cov ntsiav tshuaj. Kev sim tshuaj kho mob yuav tsum suav nrog cov koob tshuaj sib txawv, kev siv tshuaj sib txawv, thiab kev tshawb fawb txog kev nyab xeeb ntev ntev -.
Kev sib tw ua lag luam: Tam sim no, Liraglutide kev lag luam txhaj tshuaj yog qhov paub tab, thiab daim ntawv ntsiav tshuaj yuav tsum tau ntsib kev sib tw nrog kev txhaj tshuaj. Peb yuav tsum yeej txoj kev lag luam los ntawm cov tswv yim sib txawv xws li kev siv tshuaj yooj yim, kev ua raws li tus neeg mob, thiab lwm yam.
Kev loj hlob zeem muag
Kev siv tshuaj yooj yim: Daim ntawv ntsiav tshuaj yooj yim dua rau kev tswj hwm piv rau kev txhaj tshuaj, uas tuaj yeem txhim kho kev ua raws li tus neeg mob.
Kev lag luam xav tau: Nrog rau cov neeg mob uas muaj ntshav qab zib hom 2 thiab rog rog ntau zuj zus, qhov kev thov rau cov tshuaj hypoglycemic tshiab thiab cov tshuaj txo qhov hnyav kuj tseem loj tuaj. YogLiraglutide ntsiav tshuajtau tsim ua tiav, lawv yuav ua tau raws li kev lag luam xav tau rau cov tshuaj hypoglycemic tshiab thiab poob phaus.
Kev txhawb nqa txoj cai: Tsoomfwv txoj kev txhawb nqa ntxiv rau kev lag luam biopharmaceutical tau muab txoj cai tswjfwm zoo rau kev tsim cov ntsiav tshuaj Liraglutide.
Cov lus nug nquag
Puas yog liraglutide tuaj hauv daim ntawv tshuaj?
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Liraglutide, cov khoom xyaw nquag hauv Saxenda, tsuas yog muaj raws li kev txhaj tshuaj. Tab sis cov tshuaj zoo sib xws hu ua semaglutide tuaj hauv cov ntawv txhaj tshuaj (Ozempic, Wegovy) thiab ntsiav tshuaj (Rybelsus).
Kev siv liraglutide ntsiav tshuaj yog dab tsi?
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Liraglutide yog siv los txo qhov kev pheej hmoo ntawm cov kab mob plawv (lub plawv nres, mob stroke, lossis tuag) hauv cov neeg uas muaj ntshav qab zib hom 2 thiab mob plawv. Liraglutide kuj tseem siv tau rau lwm yam mob raws li koj tus kws kho mob txiav txim siab. Liraglutide kuj muaj nyob rau hauv ntau hom kev tswj qhov hnyav.
Puas tuaj yeem muab liraglutide rau qhov ncauj?
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Qhov tseem ceeb. Tsim ib qhov ncauj liraglutide nanomicelle rau kev txhim kho cov tshuaj insulin txo qis. Siv ASBT- thauj nruab nrab los txhim kho kev nqus ntawm qhov ncauj. Ua tiav 4.63-fold siab dua qhov ncauj bioavailability tshaj liraglutide unformulated.
Leej twg tsis tuaj yeem noj liraglutide?
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Qhia rau koj tus kws kho mob yog tias koj lossis ib tus neeg hauv koj tsev neeg muaj lossis puas tau muaj qog nqaij hlav qog noj ntshav lossis ntau yam Endocrine Neoplasia syndrome hom 2 (MEN 2; tus mob uas ua rau cov qog nqaij hlav hauv ntau dua ib lub qog hauv lub cev). Yog tias muaj, koj tus kws kho mob yuav hais kom koj tsis txhob siv tshuaj liraglutide.
Qhov twg zoo dua, Ozempic lossis liraglutide?
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Ozempic® (semaglutide) feem ntau ua rau poob phaus ntau dua li cov tshuaj liraglutide xws li Saxenda® lossis Victoza®, ua rau nws muaj kev xaiv muaj zog rau ntau tus neeg. Ntau tus neeg kuj nyiam Ozempic's ib zaug - lub sijhawm txhaj tshuaj txhua lub limtiam tshaj liraglutide noj txhua hnub.
Cim npe nrov: Liraglutide ntsiav tshuaj, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom