CovSemaglutide ntsiav tshuaj 7 mgyog lub ntiaj teb thawj zaug pom zoo glucagon qhov ncauj-zoo li peptide-1 (GLP-1) receptor agonist, muab cov kev xaiv noj tshiab thiab yooj yim rau kev tswj cov ntshav qab zib hom 2. Lub hauv paus ntawm cov khoom no yog nyob rau hauv nws cov cuab yeej tshwj xeeb absorbing enhancer, uas ua rau cov tshuaj peptide no kov yeej cov kua qaub ib puag ncig ntawm lub plab thiab tau txais txiaj ntsig zoo hauv cov hnyuv thiab nkag mus rau hauv cov hlab ntsha. Kev tswj hwm ib zaug ib hnub los ntawm qhov ncauj, nws tuaj yeem txuas ntxiv ua haujlwm ntawm GLP-1 receptor, yog li ntse txhawb kev tsim cov tshuaj insulin, inhibiting glucagon tso tawm, thiab ncua lub plab zom mov kom ua tiav cov ntshav qab zib kom ruaj khov thiab poob qis. Kev sim tshuaj ntsuam xyuas tau pom tias ntawm qhov koob tshuaj no, thaum ua ke nrog kev noj haus thiab kev tawm dag zog, nws tuaj yeem txo qis glycated hemoglobin (HbA1c) qib. Piv nrog rau cov tshuaj txhaj tshuaj, cov ntsiav tshuaj ntawm qhov ncauj tau txhim kho qhov yooj yim ntawm kev tswj hwm tshuaj thiab kev ua raws li tus neeg mob, tab sis nws yog ib qho tseem ceeb uas yuav tsum nco ntsoov tias nws yuav tsum tau noj me me ntawm cov dej ntawm lub plab khoob kom ntseeg tau tias qhov ua tau zoo tshaj plaws.
Peb Cov Khoom Muag Khoom
Semaglutide COA
Txoj kev tsim khoom ntawmSemaglutide ntsiav tshuaj 7 mgkoom nrog ntau cov kauj ruam meej, npog peb yam tseem ceeb: raw khoom synthesis, formulation process optimization, thiab tswj kom zoo. Tus tsim lub hom phiaj los xyuas kom meej qhov ruaj khov, bioavailability, thiab soj ntsuam kev ua tau zoo ntawm cov tshuaj.
API Synthesis: Synergy ntawm Genetic Engineering thiab Tshuaj Hloov Kho
Lub active ingredient ntawm Semaglutide yog synthesized los ntawm genetic engineering. Ua ntej, ib qho kev qhia plasmid yog tsim los ntawm DNA recombination technology thiab nkag mus rau hauv Saccharomyces cerevisiae. Los ntawm cov txheej txheem fermentation, txuas ntxiv Semaglutide precursor yog tsim. Qhov no precursor yuav tsum tau mus rau ntau yam tshuaj hloov kho los txhim kho nws cov pharmacological kev ua ub no:
8th amino acid hloov
Alanine (Ala) yog hloov nrog -amino isobutyric acid (Aib), uas thaiv cov enzymatic cleavage site ntawm dipeptidyl peptidase-4 (DPP-4) los ntawm steric hindrance, txhim kho cov tshuaj tiv thaiv rau enzymatic degradation los ntawm kwv yees li 100 zaug.
34th amino acid optimization
Lysine (Lys) yog hloov nrog Arginine (Arg), txhim kho cov nqi ntawm cov khoom siv molecular, ua kom muaj kev sib raug zoo nrog GLP-1 receptor, thiab ua kom muaj txiaj ntsig zoo ntawm cov receptor ntawm qis concentrations.
Fatty acid sab saw txuas
Ntawm 26th lysine sab saw, 18-carbon fatty acid saw (C18) yog covalently txuas los ntawm valeric acid txuas caj npab, tsim ib qho chaw albumin binding, thiab ua kom lub sijhawm ntev ntawm cov tshuaj hauv lub cev.
Formulation txheej txheem: Breakthrough tsim rau qhov ncauj nqus
Semaglutide ntsiav tshuaj 7 mgtxais yuav tam sim no - tso cov ntsiav tshuaj yaig tshuab. Qhov kev sib tw tseem ceeb nyob rau hauv kev kov yeej qhov kev puas tsuaj ntawm cov tshuaj peptide los ntawm ib puag ncig hauv plab hnyuv. Txhawm rau daws qhov teeb meem no, tus txhawb nqa kev nqus - salcaprozate sodium (SNAC) tau ntxiv rau hauv cov qauv:
Lub mechanism ntawm kev txiav txim ntawm SNAC
SNAC txo tus nqi pH hauv lub plab, tsim kom muaj ib cheeb tsam microenvironment thiab txo qhov kev puas tsuaj rau Semaglutide los ntawm plab acid; Nyob rau tib lub sijhawm, nws lipophilicity txhawb nqa cov tshuaj nkag mus rau hauv lub plab mucosal cell membrane, txhim kho kev nqus tau zoo.
Blister pob tsim
Lub pob hlwv yog dawb rau lub teeb daj hauv cov duab, ntsuas 7.5 × 13.5 hli. Ib sab yog embossed nrog "7" kom paub qhov txawv qhov ntau npaum, thiab sab nraud yog embossed nrog lub logo "Novo". Qhov kev tsim no ua kom cov tshuaj maj mam erodes hauv lub plab, ua kom tiav synchronous tso tawm ntawm Semaglutide thiab SNAC, thiab tswj kom ruaj khov tus nqi nqus.
Optimization ntawm txoj kev tswj hwm
Cov neeg mob yuav tsum nqos cov ntsiav tshuaj ntawm lub plab khoob (tsis noj lossis haus tsawg kawg 30 feeb) kom tsis txhob cuam tshuam los ntawm cov zaub mov ntawm kev sib cuag ntawm cov tshuaj thiab lub plab mucosa. Qhov kev tsim no ua rau kom lub qhov ncauj bioavailability ntawm Semaglutide mus rau kwv yees li 79%, mus txog cov nyhuv ntawm kev txhaj tshuaj formulation.
Kev Tswjhwm Zoo: Kev tswj nruj nruj los ntawm cov khoom siv raw mus rau cov khoom tiav
Cov txheej txheem tsim khoom ua raws li cov qauv kev tswj hwm kev tswj hwm kev lag luam thoob ntiaj teb (GMP), thiab txhua pawg ntawm cov khoom yuav tsum tau ua ntau yam kev ntsuam xyuas:
Raw khoom siv tshuaj ntsuam xyuas
Xws li cov tsos mob (dawb rau tawm- cov hmoov dawb), cov dej noo (Karl Fischer txoj kev), peptide profile txheeb xyuas (RP-UHPLC tuav lub sij hawm sib piv), thiab kev txiav txim siab cov ntsiab lus (RP-UHPLC txoj kev).
Formulation xeem
Ntxiv rau cov khoom siv niaj hnub (xws li qhov sib txawv ntawm qhov hnyav, qhov hnyav, lub sijhawm sib cais), lub hom phiaj yog txhawm rau txheeb xyuas SNAC cov ntsiab lus thiab cov ntsiav tshuaj yaig los xyuas kom meej tias cov tshuaj tso tawm raws li kev cia siab.
Kev kawm ruaj khov
Kev ntsuas nrawm (40℃/ 75%RH) thiab ntev- lub sijhawm kuaj (25℃/ 60%RH) paub meej tias cov ntsiav tshuaj Semaglutide 7mg muaj cov ntsiab lus ruaj khov nyob rau lub sijhawm siv tau (feem ntau 24 lub hlis), thiab qib impurity ua raws li cov qauv thoob ntiaj teb.
Kev tsim khoom sib xws: kev ntseeg siab ntawm loj- nplai kev tsim khoom
Cov txheej txheem tsim khoom tau raug lees paub los xyuas kom meej qhov sib xws thiab rov ua dua ntawm cov txheej txheem tsim khoom rau peb daim ntawv ntau npaum (3mg, 7mg, thiab 14mg). Piv txwv li, cov kab lis kev cai kab lis kev cai rau cov kauj ruam fermentation, cov tshuaj tiv thaiv tsis haum rau kev hloov kho tshuaj (xws li kub, pH tus nqi), thiab cov ntsiav tshuaj nias lub zog hauv cov txheej txheem tsim tau tag nrho cov txheej txheem nruj me ntsis kom txo qis batch - rau -batch sib txawv. Tsis tas li ntawd, cov chaw tsim khoom tau lees paub los ntawm EU EMA thiab US FDA, txhawb nqa thoob ntiaj teb.
Cov pej xeem siv tau
Semaglutide ntsiav tshuaj 7 mgyog ib qho GLP-1 receptor agonist ntawm qhov ncauj, feem ntau yog siv los txhim kho cov ntshav qab zib hauv cov neeg laus uas muaj ntshav qab zib hom 2 thiab txo qhov kev pheej hmoo ntawm cov kab mob plawv hauv cov neeg tshwj xeeb, thaum tseem muaj qhov hnyav poob. Cov pej xeem siv tau yuav tsum nruj me ntsis raws li cov xwm txheej hauv qab no thiab siv raws li kev qhia ntawm tus kws kho mob:
Cov Lus Qhia Tseem Ceeb: Cov neeg laus uas muaj ntshav qab zib hom 2
Cov uas tswj ntshav qab zib tsis zoo
Muaj feem xyuam rau cov neeg laus uas muaj ntshav qab zib hom 2 uas tseem tsis tau ua tiav cov ntshav qab zib kom txaus siab tom qab kev noj zaub mov thiab kev tawm dag zog, ua kev kho mob ntxiv.
Nws tuaj yeem siv tau ib leeg (yog tias tus neeg mob tsis tuaj yeem zam cov tshuaj metformin lossis muaj contraindications), lossis ua ke nrog lwm cov tshuaj hypoglycemic ntawm qhov ncauj (xws li metformin, SGLT-2 inhibitors) lossis basal insulin los txhim kho cov ntshav qab zib.
Cov ntaub ntawv kho mob qhia tau tias koob tshuaj 7mg tuaj yeem txo qis glycated hemoglobin (HbA1c) qib los ntawm 1.0% -1.5%, zoo dua li cov placebo pawg.
Cov kab mob plawv siab - cov neeg raug mob
Muaj feem xyuam rau cov neeg laus uas muaj ntshav qab zib hom 2 uas muaj cov kab mob atherosclerotic cardiovascular (xws li kab mob plawv, mob stroke, peripheral artery disease) lossis ntau yam mob plawv (xws li kub siab, hyperlipidemia, haus luam yeeb).
Rau cov neeg mob zoo li no, Semaglutide tuaj yeem txo qhov kev pheej hmoo ntawm kev mob plawv tsis zoo (MACE, suav nrog kev tuag ntawm cov hlab plawv, tsis yog-fatal myocardial infarction, tsis yog- mob stroke) los ntawm 13%.
Poob Qhov Taw Qhia: Cov neeg rog rog lossis rog rog
Cov neeg mob uas muaj kev rog yooj yim
Muaj feem xyuam rau cov neeg laus uas muaj qhov ntsuas lub cev (BMI) Ntau dua lossis sib npaug li 30 kg / m², raws li kev kho mob hnyav.
Ib koob tshuaj 7mg tuaj yeem ua rau qhov hnyav poob ntawm 4% -6% rau cov neeg mob. Yog tias xav tau kev poob phaus ntxiv, cov koob tshuaj tuaj yeem nce ntxiv mus rau 14mg (nrog cov teebmeem tseem ceeb, nce mus txog 6% -8%).
Cov neeg mob hnyav dua uas muaj teeb meem
Muaj feem xyuam rau cov neeg laus uas muaj BMI Ntau dua lossis sib npaug li 27 kg / m² thiab tsawg kawg ib qho kev rog rog - cuam tshuam txog teeb meem (xws li kub siab, ntshav qab zib hom 2, dyslipidemia).
Rau cov neeg mob zoo li no, Semaglutide tsis tsuas yog txo qhov hnyav xwb tab sis kuj tseem txhim kho cov ntsuas metabolic (xws li ntshav siab, lipid profile), thiab txo qhov kev pheej hmoo ntawm cov kab mob plawv.
Cov neeg hluas rog rog (qee zaum)
Lub Koom Haum Saib Xyuas Kev Noj Qab Haus Huv European tso cai ncua sijhawm ntawm kev tshuaj xyuas cov txiaj ntsig kev sim rau 2-hom ntshav qab zib pawg hauv cov tub ntxhais hluas (hnub nyoog 12 thiab siab dua), tab sis hauv kev kho mob, yog tias tus neeg mob hluas ua tau raws li cov neeg laus qhov hnyav (xws li BMI ntawm 95 feem pua), nws tuaj yeem siv ceev faj tom qab kev soj ntsuam los ntawm tus kws kho mob.
Kev siv tau rau Cov Neeg Tshwj Xeeb
Cov neeg mob lub raum tsis txaus
Cov neeg mob uas mob me mus rau nruab nrab lub raum tsis txaus (eGFR Ntau dua lossis sib npaug li 30 mL / min / 1.73m²) tsis tas yuav hloov tshuaj, tab sis cov neeg mob lub raum tsis txaus (eGFR < 30 mL / min / 1.73m²) yuav tsum tau siv nrog ceev faj thiab yuav tsum tau txo cov koob tshuaj lossis saib xyuas lub raum ua haujlwm.
Cov neeg mob lub siab tsis txaus
Cov neeg mob uas muaj lub siab tsis txaus (Me nyuam-Pugh A qib) tsis tas yuav hloov cov tshuaj, tab sis cov neeg mob uas muaj lub siab tsis txaus siab (Me nyuam-Pugh B/C qib) tej zaum yuav tau txo cov koob tshuaj lossis tsis txhob siv cov tshuaj vim tias cov tshuaj metabolism qeeb qeeb.
Cov neeg laus (Ntau dua lossis sib npaug rau 65 xyoos)
Tsis tas yuav hloov koob tshuaj raws li hnub nyoog, tab sis cov neeg mob laus feem ntau muaj ntau yam kab mob ntev (xws li kab mob plawv, lub raum tsis txaus), thiab yuav tsum muaj kev ntsuam xyuas dav dav txog kev pheej hmoo thiab cov txiaj ntsig.
Contraindications thiab ceev faj
Tsis muaj contraindications
Cov neeg mob uas muaj ntshav qab zib hom 1 lossis ntshav qab zib ketoacidosis: Semaglutide tsis tuaj yeem hloov kho insulin thiab tuaj yeem npog cov tsos mob ketosis acidosis.
Cov neeg mob uas muaj keeb kwm ntawm medullary thyroid carcinoma (MTC) los yog tsev neeg keeb kwm, thiab cov neeg mob uas muaj ntau yam endocrine adenoma syndrome type 2 (MEN2): Tsiaj thwmsim qhia tias Semaglutide tuaj yeem ua rau muaj kev pheej hmoo ntawm cov qog nqaij hlav thyroid C, txawm hais tias tib neeg tsis tau tsim, nws tseem txwv tsis pub.
Cov neeg mob ua xua rau Semaglutide los yog ib qho ntawm cov tshuaj.
Cov txheeb ze Contraindications thiab ceev faj
Cov neeg mob uas muaj keeb kwm ntawm tus mob pancreatitis: Semaglutide tsis tau kawm nyob rau hauv pab pawg neeg mob no thiab tuaj yeem ua rau muaj kev pheej hmoo rov tshwm sim dua. Lwm cov tshuaj hypoglycemic yuav tsum tau xaiv.
Cov poj niam cev xeeb tub thiab lactating: Tsiaj thwmsim qhia tias Semaglutide tuaj yeem muaj kev cuam tshuam tsis zoo rau kev loj hlob ntawm tus menyuam hauv plab, thiab tsis muaj tib neeg cov ntaub ntawv. Yog li ntawd, nws yog txwv tsis pub.
Cov neeg mob uas muaj kab mob gastrointestinal: xws li gastroparesis thiab inflammatory plob tsis so tswj kab mob, cov tshuaj muaj peev xwm mus ncua lub plab khoob tej zaum yuav exacerbate cov tsos mob. Yog li ntawd, nws yuav tsum tau siv nrog ceev faj.
FAQ
1. Yuav ua li cas cov ntsiav tshuaj ntawm qhov ncauj kov yeej lub plab zom mov kom ua tiav kev nqus?
Cov thev naus laus zis tseem ceeb nyob hauv qhov nqus tau zoo (SNAC) hauv cov txheej txheem co-. Nws tuaj yeem nce tus nqi pH ib ntus hauv zos hauv lub plab thiab txhim kho daim nyias nyias permeability, yog li tiv thaiv thiab txhawb kev nqus sai ntawm semaglutide hauv plab es tsis yog los ntawm txoj kev nqus cov hnyuv me.
2. Thaum siv nrog rau lwm cov tshuaj hypoglycemic ntawm qhov ncauj, puas muaj cov cai tshwj xeeb hais txog kev tswj hwm?
Yog lawm. Cov ntsiav tshuaj Semaglutide yuav tsum tau noj ib leeg ntawm lub plab khoob, tsis pub ntau tshaj li ib nrab khob dej. Tom qab noj nws, tos tsawg kawg 30 feeb ua ntej noj mov, haus dej, lossis noj lwm yam tshuaj hauv qhov ncauj kom ntseeg tau tias SNAC yuav siv tau yam tsis muaj kev cuam tshuam.
3. Yuav ua li cas yog tias ib ntsiav tshuaj poob ib zaug?
Yog tias koj tsis noj tshuaj, koj yuav tsum tau noj tam sim ntawd thaum paub txog qhov kev tso tseg, tab sis nco ntsoov tias koj tseem ua tau raws li kev yoo mov (uas yog, tsis muaj zaub mov lossis dej haus tau noj tsawg kawg 30 feeb ua ntej thiab tom qab noj tshuaj). Yog tias nws nyob ze rau lub sijhawm txhaj tshuaj tom ntej, koj yuav tsum hla qhov koob tshuaj uas tsis tau thiab noj cov tshuaj ntxiv raws li tau npaj tseg. Tsis txhob noj ob zaug ib zaug ib zaug.
4. Thaum hloov los ntawm cov tshuaj txhaj rau hauv cov ntsiav tshuaj ntawm qhov ncauj, yuav tsum hloov cov koob tshuaj li cas?
Qhov no tsis yog ib qho yooj yim hloov dua siab tshiab. Piv txwv li, hloov ib koob tshuaj 1mg txhua lub lim tiam ntawm kev txhaj tshuaj rau 7mg txhua hnub ntawm qhov ncauj yog raws li kev tshawb fawb sib npaug ntawm kev kho mob. Ib qho kev hloov pauv hloov pauv yuav tsum tau ua raws li kev soj ntsuam nruj thiab kev taw qhia ntawm tus kws kho mob thiab tsis tuaj yeem ua tiav ntawm tus kheej.
Cim npe nrov: Semaglutide ntsiav tshuaj 7mg, Tuam Tshoj semaglutide ntsiav tshuaj 7mg manufacturers, lwm tus neeg
