Noopept ntsiav tshuajyog ib qho kev tsim ntawm qhov ncauj raws li kev txawj ntse hluavtaws txhawb tshuaj Omberacetam (tshwj xeeb lub npe: N-phenylacetyl-L-prolylglycine ethyl ester) ua cov khoom tseem ceeb. Nws yog thawj zaug tsim nyob rau hauv Russia thiab tom qab ntawd siv los ua tshuaj lossis kev noj qab haus huv hauv qee lub tebchaws hauv Tebchaws Europe thiab Asia. Nws cov txheej txheem ntawm kev txiav txim npog plaub qhov ntev: neuroprotection, neurotransmitter kev tswj hwm, kev loj hlob zoo stimulation, thiab tiv thaiv antioxidant. Cov kev tshawb fawb hauv tsev kho mob tau pom tias nws qhov kev ua tau zoo tuaj yeem ncav cuag 1000 npaug ntawm cov kev txawj ntse ib txwm txhawb nqa tshuaj Piracetam. Cov kev sim tsiaj tau pom tias nws tuaj yeem txhim kho lub peev xwm ntawm lub cim xeeb ntawm cov nas uas muaj kev puas tsuaj rau lub hlwb thiab nce qib BDNF hauv cov neeg mob vascular dementia. Cov tshuaj capsuls tsim tau siv cov cuab yeej siv microcrystalline cellulose los ua kom cov tshuaj ruaj khov tso rau hauv txoj hnyuv, nrog rau qhov ncauj bioavailability ntawm 89%. Qhov sib piv ntawm cov ntshav- lub hlwb thaiv qhov nkag mus rau cov ntshav ntshav yog ze rau 1: 1, thiab qhov ua tau zoo yuav kav ntev dua 12 lub lis piam.
Peb cov khoom
Cov ntaub ntawv ntxiv ntawm chemical compound:
Peb Cov Khoom
Noopept +. COA
Chemical Essence thiab Molecular yam ntxwv
1. Cov qauv zoo thiab bioavailability:
Piv nrog rau cov kev txawj ntse ib txwm siv los txhawb cov tshuaj Piracetam, Noopept txhim kho nws cov ntshav - lub hlwb thaiv kev muaj peev xwm nkag mus los ntawm kev hloov kho benzoyl. Cov kev sim tsiaj tau pom tias qhov siab tshaj plaws (1.289 μ g / mL) hauv cov ntaub so ntswg hlwb tuaj yeem ncav cuag li ntawm 7 feeb tom qab kev tswj hwm qhov ncauj ntawm koob tshuaj 8mg / kg, thiab tsis muaj qhov sib txawv tseem ceeb hauv cov ntshav thiab cov paj hlwb. Nws cov bioavailability yog siab li 89%, deb tshaj li 1-2% ntawm piracetam, ua tsaug rau kev zam ntawm ethyl ester pab pawg ua haujlwm ntawm thawj qhov tshwm sim.
2. Formulation sib txawv
Muaj kev sib cav txog bioequivalence ntawm Lavxias version ntawm cov ntsiav tshuaj sublingual (10mg) thiab American version ntawm capsuls (30mg). Cov neeg siv kev tshawb fawb qhia tau hais tias 62% ntawm cov neeg siv ntseeg hais tias cov ntsiav tshuaj sublingual siv tau sai (15-20 feeb vs 30-45 feeb rau capsuls), tab sis lub sij hawm ntawm kev txiav txim nyob rau hauv pab pawg neeg capsule ntev mus rau 6-8 teev. Kev tshuaj xyuas HPLC qhia tau hais tias cov qauv kev sib cais rau cov ntsiav tshuaj sublingual yog 85% -115%, thaum cov tshuaj ntsiav yuav tsum ncav cuag 80% -125%.
Bioavailability ntawmNoopept ntsiav tshuajyog ib tug tseem ceeb parameter nyob rau hauv lawv cov pharmacokinetic zog, uas ncaj qha cuam tshuam rau lub nqus efficiency thiab soj ntsuam kev ua tau zoo ntawm cov tshuaj nyob rau hauv vivo. Raws li kev tshawb fawb uas twb muaj lawm, bioavailability ntawm Omberacetam nthuav tawm cov yam ntxwv tseem ceeb, thiab kev tsom xam tshwj xeeb yog raws li hauv qab no:
Qhov tseeb bioavailability yog siab li 99.7%, qhia tias yuav luag tag nrho cov tshuaj tiv thaiv tuaj yeem nqus tau rau hauv cov kab mob hauv lub plab zom mov tom qab kev tswj hwm qhov ncauj. Nws qhov nqus tau siab yog feem ntau yog los ntawm cov tshuab hauv qab no:
Molecular structural zoo: Omberacetam yog ib tug me me molecule dipeptide derivative (molecular hnyav 318.36 Da) nrog tsawg polarity deg cheeb tsam thiab tsawg rotatable bonds, uas ua raws li molecular tsim qauv ntawm lub qhov ncauj bioavailability.
Carrier assisted absorption: Microcrystalline cellulose feem ntau yog siv los ua ib qho khoom siv hauv cov qauv, thiab nws cov hygroscopicity thiab compressibility tuaj yeem ua kom zoo dua cov tshuaj dispersion hauv plab hnyuv, txhawb kev so thiab nqus.
Metabolic stability: Txawm hais tias qee cov tshuaj tau metabolized rau hauv cov khoom xws li phenylacetic acid thiab phenylacetyl proline nyob rau hauv thawj qhov kev tshwm sim, cov khoom xyaw tseem ceeb tseem muaj nyob hauv lawv daim ntawv qub, kom ntseeg tau tias kev siv cov khoom xyaw nquag.
Formulation sib txawv: sib piv ntawm bioavailability ntawm capsuls thiab ntsiav tshuaj
Cov ntawv ntau npaum li cas muaj feem cuam tshuam rau lawv cov bioavailability:
Capsules formulation:
Kev siv cov cuab yeej siv microcrystalline cellulose tuaj yeem tiv thaiv cov tshuaj los ntawm kev zom zaub mov thiab ua kom muaj kev tso tawm ruaj khov hauv cov hnyuv.
Lub bioavailability thiab ntshav- lub paj hlwb barrier nkag mus yog ze rau 1: 1, thiab cov nyhuv tshuaj yuav kav ntev tshaj li 12 lub lis piam.
Daim ntawv tshaj tawm cov neeg siv qhia tau hais tias 30mg capsuls formulation muaj cov txiaj ntsig tseem ceeb ntawm kev txhim kho kev mloog thiab cov ntaub ntawv ua haujlwm ceev.
Sublingual ntsiav tshuaj (Lavxias teb sab version):
Ncaj nraim absorbed los ntawm sublingual mucosa, bypassing thawj kis nyhuv, theoretically muaj ntau dua bioavailability.
Txawm li cas los xij, hauv kev tshawb fawb tiag tiag, tsis muaj qhov sib txawv tseem ceeb hauv cov ntshav cov tshuaj concentration nkhaus piv rau lub qhov ncauj capsuls, uas tej zaum yuav yog vim qhov tsawg ntawm cov mucosal absorption cheeb tsam.
Cov neeg siv cov lus qhia pom tau hais tias cov ntsiav tshuaj sublingual siv tau sai dua, tab sis muaj sijhawm luv dua (kwv yees li 4-6 teev).
Ib nrab -Lub neej ntawm ntshav ntshav yog 0.38 teev, uas luv luv, tab sis nws cov txiaj ntsig tau txais txiaj ntsig los ntawm cov tshuab hauv qab no:
Kev ua haujlwm metabolite: Qee cov metabolites (xws li cycloprolidylglycine) tseem muaj cov teebmeem neuroprotective thiab tuaj yeem ua kom ntev tag nrho cov kev kho mob.
Receptor desensitization inhibition: Los ntawm IL-6 mediated BDNF overexpression mechanim, nws txuas ntxiv txhawb kev sib txawv ntawm neural qia hlwb, tswj kev siv tshuaj rau ob peb lub lis piam.
Kev tsim qauv tsim kom zoo: Cov tshuaj capsul formulation tau txais kev txhawb nqa -tso tawm thev naus laus zis los xyuas kom meej qhov kev hloov pauv hauv cov ntshav cov tshuaj concentration thiab tsis txhob muaj qhov cuam tshuam ntawm lub hav.
Qhov tseem ceeb ntawm kev kho mob: Cov txiaj ntsig zoo ntawm bioavailability siab
Lub siab bioavailability muab kev txhawb nqa theoretical rau nws daim ntawv thov hauv kev kho mob ntawm kev puas hlwb:
koob tshuaj raug: Ib hnub koob tshuaj 20mg tuaj yeem ua tiav cov txiaj ntsig kho mob tseem ceeb thiab txo qhov kev pheej hmoo ntawm kev noj ntau dhau.
Kev ua raws li kev noj tshuaj: 1-2 kev noj tshuaj txhua hnub ua rau kev kho mob yooj yim dua thiab ua rau cov neeg mob txaus siab siv mus ntev.
Kev lees paub txog kev nyab xeeb: Kev nqus tau siab txo cov tshuaj seem hauv plab hnyuv, txo qis hauv zos khaus thiab cov kev mob tshwm sim.
Kev Tswj Xyuas Zoo thiab Kev Npaj Ua Haujlwm
Synthesis txoj kev
Cov tshuaj tiv thaiv acylation ntawm proline thiab benzoyl chloride yog siv los tsim qhov nruab nrab N-phenylacetyl-L-proline, uas yog tom qab ntawd condensed nrog glycine ethyl ester kom tau txais cov khoom lag luam. Cov kauj ruam tseem ceeb suav nrog:
Kev npaj ntawm benzoyl chloride (cov tshuaj tiv thaiv ntawm benzoic acid nrog sulfonyl chloride)
Acylation cov tshuaj tiv thaiv (dichloromethane ua hnyav, triethylamine ua hauv paus)
Kem chromatography purification (siv silica gel raws li cov theem nyob ruaj khov thiab ethyl acetate petroleum ether li eluent)
Cov qauv zoo
Kev txiav txim siab txog cov ntsiab lus: HPLC txoj kev (C18 kem, acetonitrile dej raws li theem mobile, nrhiav kom pom wavelength 254nm), cov ntsiab lus yuav tsum tsis pub tsawg dua 98.0%.
Hais txog cov khoom: Tus neeg impurities yuav tsum tsis pub tshaj 0.5%, thiab tag nrho impurities yuav tsum tsis txhob ntau tshaj 1.0%.
Dissolution tus nqi: Tus nqi tawg ntawm cov tshuaj ntsiav tshuaj yuav tsum tsis pub tsawg dua 80% hauv 30 feeb.
Keeb kwm kev loj hlob ntawmNoopept ntsiav tshuaj: los ntawm chav kuaj mus rau kev tshawb nrhiav hauv thaj chaw ntawm kev paub txog kev txhim kho
GVS-111 (tshwj xeeb lub npe: N-phenylacetyl-L-prolylglycine ethyl ester) yog ib qho kev sib xyaw ua ke ntawm kev txawj ntse txhawb cov tshuaj, uas nws cov txheej txheem kev loj hlob ua ke nrog kev sib tsoo ntawm neuroscience, tshuaj chemistry, thiab biohacking kab lis kev cai. Cov keeb kwm los ntawm kev tshawb fawb thiab kev loj hlob hauv lub xyoo 1990s mus rau lub ntiaj teb kev paub txog kev siv cov kev txawj ntse hauv lub xyoo pua 21st tuaj yeem muab faib ua cov theem tseem ceeb hauv qab no:
Txoj kev loj hlob ntawm GVS-111 pib xyoo 1996, coj los ntawm pab pawg kws tshawb fawb los ntawm Zakusov Institute of Pharmacology hauv Russia. Nws qhov kev tshoov siab tsim los ntawm endogenous neuropeptide cyclic alanine glycine (ib yam khoom uas txhawb nqa kev qhia ntawm lub hlwb- tau txais txiaj ntsig neurotrophic BDNF). Cov kws tshawb fawb xav tias los ntawm kev txhim kho nws cov metabolism hauv kev ruaj ntseg thiab cov ntshav-hlwb thaiv kev nkag mus los ntawm kev hloov kho tshuaj, kev txawj ntse ntau dua tuaj yeem tsim tau.
Tom qab kev txhim kho kev tsim kho, GVS-111 thaum kawg tau txheeb xyuas tias yog phenylacetyl hloov kho proline glycine dipeptide derivative nrog lub cev hnyav ntawm 318.37 g / mol thiab CAS tus lej ntawm 157115-85-0. Nws lub ntsiab innovation yog nyob rau hauv:
Circular qauv txwv: Lub voj voog raws li L-proline txo cov molecular yooj thiab txhim kho metabolic stability;
Ester raws li kev tsim: Cov pab pawg glycine ethyl ester endows nws nrog lipophilicity, ua kom yooj yim rau nws txoj kev hla ntawm cov ntshav - hlwb teeb meem, thaum raug hydrolyzed los ntawm esterases mus rau hauv lub cev metabolites.
Thaum xyoo 2000s, GVS-111 tau nkag mus rau theem kev sim tsiaj, nrog rau kev tsom mus rau kev txheeb xyuas nws cov kev tiv thaiv kab mob thiab kev txawj ntse txhawb nqa:
Xyoo 2001, cov kws tshawb fawb Lavxias tau tshaj tawm thawj zaug tias GVS-111 nce qhov concentration ntawm BDNF hauv hippocampus ntawm nas thiab txhim kho kev nco txog kev ua haujlwm hauv Morris dej tshawb nrhiav.
Hauv xyoo 2005, kev tshawb fawb tau nthuav tawm nws cov txheej txheem ntawm BDNF overexpression mediated los ntawm IL-6, uas txhawb nqa neural qia cell sib txawv thiab ncua kev loj hlob ntawm cov kab mob neurodegenerative.
Hauv xyoo 2008, nws tau tshawb pom tias GVS-111 tuaj yeem cuam tshuam kev tsim ntawm beta amyloid (25-35) fibrils, qhia tias muaj peev xwm kho tus nqi rau Alzheimer's disease.
Qhov kev tshawb fawb theem no tau tsim lub hauv paus rau ob lub ntsiab lus ntawm GVS-111:
Txhawb txoj kev txawj ntse: txhim kho cholinergic system (txhim kho acetylcholine tso tawm) thiab glutamatergic system ( tswj hwm AMPA / NMDA receptors);
Neuroprotection: antioxidant (tiav H ₂ O ₂ - induced dawb radicals) thiab tiv thaiv -inflammatory (inhibiting lipid peroxidation puas).
Tom qab xyoo 2010, GVS-111 tau pib siv los ua tshuaj hauv qee lub tebchaws hauv Tebchaws Europe thiab Asia, feem ntau yog siv rau kev kho mob:
Kev paub tsis meej tom qab raug mob lub hlwb;
Vascular dementia;
Kev paub tsis meej me ntsis (MCI).
Cov kev sim tshuaj tseem ceeb:
Hauv xyoo 2015, ob qho - qhov muag tsis pom kev sim hauv Russia (n=134) tau pom tias pawg GVS-111 tau txhim kho MMSE cov qhab nia los ntawm 3.8 cov qhab nia, zoo dua li cov placebo pab pawg 1.2 cov ntsiab lus.
2020: Kev tshawb fawb hauv Taiwan, Tuam Tshoj, Tuam Tshoj tau lees paub tias Nooept tuaj yeem txhim kho lub cim xeeb episodic (spatial nco) kev puas tsuaj rau cov neeg mob uas muaj cov kab mob tsis zoo rau lub siab.
However, due to the lack of long-term safety data (>6 lub hlis ntawm kev siv) thiab cov cuab yeej tsis sib haum xeeb nrog cov tshuaj tiv thaiv kev ntxhov siab, GVS-111 tsis tau txais kev pom zoo los ntawm FDA rau kev siv kho mob, tab sis tau muab cais ua "cov tshuaj tsis tswj hwm" hauv Tebchaws Meskas thiab raug tso cai muag raws li kev noj haus ntxiv.
Hauv xyoo 2020, GVS-111 tau dhau los ua qhov kev xaiv nrov ntawm cov zej zog biohacker thoob ntiaj teb, nrog rau nws daim ntawv thov scenarios nthuav dav los ntawm kev kho mob mus rau kev paub txog kev txawj ntse.
Daim Ntawv Qhia Txog Cov Neeg Siv: Biohacker Jeffrey Wu thov tias tom qab noj GVS-111, kev nkag siab ua haujlwm tau zoo dua qub, suav nrog kev pom cov xim ntau ntxiv thiab txhim kho kev hnov lus nthuav dav kom paub txog lub peev xwm.
Dose controversy: Cov tshuaj pom zoo ib txwm siv yog 10-30 mg ib hnub, tab sis biohackers feem ntau txhim kho kev nqus tau los ntawm kev tswj hwm sublingual (bioavailability li ntawm 9%) lossis qhov ntswg qhov ntswg, ua rau muaj kev txhawj xeeb txog kev nyab xeeb.
Kev ua lag luam teeb meem: Raws li xyoo 2025, GVS-111 tau nthuav dav thoob ntiaj teb kev tshawb fawb tshawb fawb reagent lag luam (xws li Beijing Baiolebo Technology Co., Ltd. muab 98% purity khoom), tab sis kev siv tshuaj kho mob tseem txwv rau Russia thiab qee lub tebchaws nyob sab hnub tuaj.
Cim npe nrov: Noopept ntsiav tshuaj, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom