Shaanxi BLOOM Tech Co., Ltd. yog ib qho ntawm cov tuam ntxhab thiab cov muag khoom ntawm l carnitine spray nyob rau hauv Suav teb. Txais tos rau cov lag luam wholesale bulk zoo l carnitine tshuaj tsuag rau muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.
L Carnitine Txauyog cov tshuaj pleev ib ce nrog L-Carnitine (L-Carnitine) ua cov khoom xyaw tseem ceeb, txhawm rau txhawb cov roj acid oxidation, pab kom poob phaus lossis txhim kho kev tawm dag zog los ntawm kev siv hauv zos. Daim foos tshuaj tsuag tuaj yeem ua tiav cov kev tswj hwm tshuaj hauv zos, zam thawj zaug - dhau los ntawm kev npaj ntawm qhov ncauj (xws li kev hloov pauv hauv plab zom mov thiab lub siab metabolism), thiab ua kom cov tshuaj hauv zos nce ntxiv. Tsis tas li ntawd, cov tshuaj tsuag yog portable thiab siv tau yooj yim, ua rau nws tsim nyog rau kev rov ua kom sai ua ntej thiab tom qab kev tawm dag zog. Cov tawv nqaij barrier txwv qhov transdermal absorption tus nqi.
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L-Carnitine COA
L Carnitine Txau, raws li kev poob phaus sab nraud lossis cov khoom siv metabolic, tau txais qee yam kev xav hauv kev ua lag luam hauv xyoo tas los no. Txawm li cas los xij, los ntawm qhov kev xav ntawm kev ntsuam xyuas cov neeg siv khoom, muaj kev tsis sib haum xeeb txog nws cov txiaj ntsig thiab kev nyab xeeb, thiab cov lus tawm tswv yim los ntawm cov neeg siv khoom sib txawv sib txawv. Cov kev ntsuam xyuas hauv qab no yog ua los ntawm peb yam: kev ntsuam xyuas zoo, kev ntsuam xyuas tsis zoo, thiab cov lus qhia dav dav.
Kev ntsuas qhov zoo: Qee cov neeg siv paub txog nws lub luag haujlwm pabcuam
Txhim kho cov metabolism hauv zos
Qee cov neeg siv tau tshaj tawm tias tom qab siv L-Carnitine Spray, qhov ruaj khov ntawm cov rog hauv zos (xws li lub plab thiab ncej puab) tau txhim kho. Piv txwv li, qee cov neeg siv tau qhia tias thaum ua ke nrog kev tawm dag zog thiab kev tswj hwm kev noj zaub mov, cov tshuaj tsuag tuaj yeem pab ua kom rog rog, tab sis lawv hais tias "cov nyhuv yuav tsum tau ua kom ntev -lub sij hawm persistence".
Kev txhim kho hauv kev ua kis las
Qee cov neeg nyiam kev noj qab haus huv ntseeg tias L-Carnitine Spray tuaj yeem ua rau kev tawm dag zog tsis muaj zog los ntawm kev txhawb nqa oxidation ntawm fatty acids. Piv txwv li, qee cov neeg siv tau hais tias tom qab siv cov tshuaj tsuag ua ntej kev tawm dag zog, kev qaug zog thaum lub sij hawm siab - kev siv lub sij hawm siv sij hawm (HIIT) tau txo qis, tab sis lawv kuj tau taw qhia tias "cov nyhuv txawv ntawm ib tus neeg mus rau lwm tus".
Kev yooj yim yog nyiam
Qhov yooj yim ntawm cov tshuaj tsuag formulation yog ib qho ntawm nws qhov zoo. Cov neeg siv feem ntau ntseeg tias piv nrog rau qhov ncauj L-carnitine tshuaj, tshuaj tsuag yog yooj yim dua rau nqa thiab siv, tshwj xeeb tshaj yog haum rau cov neeg ua haujlwm tsis khoom lossis cov xwm txheej mus ncig.
Kev tshuaj xyuas tsis zoo: Kev txwv tsis pub muaj txiaj ntsig thiab muaj feem cuam tshuam
Cov nyhuv tsis pom tseeb
Cov neeg siv feem ntau tau tshaj tawm tias tsuas yog tso siab rau L-Carnitine Spray yog qhov nyuaj kom ua tiav qhov hnyav hnyav. Piv txwv li, qee cov neeg siv tau tshaj tawm tias "tom qab siv nws rau ib hlis, tsis muaj qhov hloov pauv loj hauv qhov hnyav lossis lub cev rog feem pua", thiab txawm tias qee cov neeg siv tau hais ncaj qha tias "nws yog tag nrho cov se ntawm kev txawj ntse".
Tsawg transdermal absorption tus nqi
Kev tshawb fawb tshawb fawb qhia tau hais tias qhov transdermal absorption tus nqi ntawm L-carnitine yog txwv, feem ntau tsuas yog 10% mus rau 20% ntawm qhov kev tswj qhov ncauj. Ntau tus neeg siv tau tshaj tawm tias cov khoom siv tshuaj tsuag "ua rau cov tawv nqaij zoo li nplaum tom qab daim ntawv thov, tab sis tsis pom kev nqus pom tseeb", thiab txawm tias qee cov neeg siv tau nug "txawm tias cov khoom xyaw tau nkag mus tiag tiag".
Kev ua xua thiab kev phiv
Qee cov neeg siv tau ntsib cov tsos mob ntawm daim tawv nqaij xws li liab thiab khaus tom qab siv. Piv txwv li, qee cov neeg siv cov tawv nqaij rhiab heev tau tshaj tawm, "Tom qab siv nws, kuv daim tawv nqaij liab thiab khaus, thiab kuv yuav tsum tsis txhob siv nws." Tsis tas li ntawd, qee cov neeg siv tau txhawj xeeb tias kev siv sijhawm ntev - tuaj yeem cuam tshuam rau lub plawv mob, tshwj xeeb tshaj yog cov kab mob plawv.
Tus nqi tsis phim tus nqi
Piv nrog rau nws cov txiaj ntsig tiag tiag, qee cov neeg siv xav tias tus nqi ntawm L-Carnitine Spray yog tus nqi siab. Piv txwv li, qee cov neeg siv tau taw qhia tias "tus nqi ntawm ib lub raj mis tshuaj tsuag yog ze li ob npaug ntawm qhov ncauj ntxiv, tab sis nws cov txiaj ntsig tsis zoo dua li ntawm qhov ncauj."
L Carnitine Txauyog ib yam khoom uas tshwm sim los ntawm cov amino acid, uas nws lub luag haujlwm tseem ceeb yog ua lub luag haujlwm tseem ceeb rau ntev -chain fatty acids nkag mus rau mitochondria rau - oxidation. Hauv cov xwm txheej uas xav tau lub zog metabolism hauv siab, xws li kev tawm dag zog thiab kev poob phaus, exogenous supplementation ntawm L-carnitine yog dav ntseeg los txhim kho cov rog rog.
Kev nqus thiab thauj mechanism ntawm L-carnitine
Kev nqus ntawm L-carnitine feem ntau yog nyob ntawm cov organic cation transporter protein 2 (OCTN2, SLC22A5) ntawm txhuam ciam teb daim nyias nyias ntawm cov hnyuv me me epithelial hlwb. OCTN2 yog ib qho affinity siab, sodium dependent transporter nrog tus nqi Km ntawm kwv yees li 20-50 μ M rau L-carnitine. Nws muaj peev xwm thauj carnitine thiab nws cov derivatives nrog ib qho hnyav molecular ntawm<500 Da.
Kev thauj mus los: Dawb L-carnitine nkag mus rau hauv plab hnyuv hlwb los ntawm txoj hnyuv lumen; OCTN2 kho kom haum xeeb thauj khoom thauj carnitine rau hauv hlwb; Carnitine nkag mus rau hauv lub portal venous ncig los ntawm passive diffusion los yog theem nrab active thauj ntawm lub basolateral membrane; Thaum kawg, nws yog metabolized los ntawm daim siab thiab xa mus rau cov ntaub so ntswg thoob plaws hauv lub cev.
Muaj peev xwm txwv ntawm kev thauj mus los
Muaj qhov saturation pib rau kev thauj mus los ntawm OCTN2. Thaum noj cov exogenous carnitine ntau tshaj qhov siab tshaj plaws thauj tus nqi (Vmax) ntawm transporter protein, ntau carnitine tsis tuaj yeem nqus tau, ua rau:
Qhov concentration ntawm carnitine nyob rau hauv txoj hnyuv nce, thiab qhov feem ntawm nws nkag mus rau hauv cov hlab ntsha los ntawm passive diffusion nce (tab sis cov efficiency yog heev tsawg);
Unabsorbed carnitine yog tawm hauv cov quav los yog metabolized los ntawm plab microbiota rau hauv trimethylamine (TMA), uas yog ntxiv hloov mus rau trimethylamine-N-oxide (TMAO) - tom kawg uas cuam tshuam nrog cov kab mob plawv.
Molecular mechanism ntawm koob tshuaj bioavailability inverse kev sib raug zoo
Dose pib rau transporter saturation
Kev txhawb nqa cov ntaub ntawv kho mob:
Tom qab ib qho kev tswj hwm qhov ncauj ntawm 0.5 g ntawm L-carnitine hauv cov neeg noj qab haus huv, qhov siab tshaj plaws plasma concentration (Cmax) yog 48.5 μ mol / L, nrog rau bioavailability ntawm kwv yees li 14-18%;
Thaum cov koob tshuaj tau nce mus rau 2 g, Cmax tsuas yog nce mus rau 60-70 μ mol / L, thiab bioavailability poob qis dua 10%;
Nruam siab - noj tshuaj ntxiv (xws li 3 g ib hnub twg) tuaj yeem ua rau kom muaj kev ruaj khov ntawm cov ntshav plasma carnitine concentration, qhia tias kev thauj mus los tau tag nrho.
Dynamics qauv:
Raws li Michaelis Menten sib npaug, kev sib raug zoo ntawm kev thauj tus nqi (v) thiab substrate concentration ([S]) yog:
Thaum [S] ≫ Km, v ≈ Vmax, Tus nqi hloov pauv tau mus txog qhov txwv siab tshaj. Nyob rau ntawm lub sijhawm no, kev siv tshuaj ntau ntxiv tsuas yog ua rau muaj kev nce ntxiv ntawm cov carnitine uas tsis tau nqus, thiab bioavailability (txhais tau tias cov tshuaj absorbed rau hauv kev ncig / koob tshuaj) yuav inevitably txo.
Kev sib tw inhibition thiab kev tswj hwm metabolic
Kev sib tw ntawm endogenous carnitine
Txoj hnyuv endogenous carnitine (kwv yees li 100-200 mg / hnub, los ntawm kev noj zaub mov thiab kev sib txuas ntawm tus kheej) sib tw nrog cov tshuaj exogenous rau OCTN2 qhov chaw khi. Cov koob tshuaj ntau ntawm exogenous carnitine tuaj yeem "squeeze" thauj cov protein ib ntus, tab sis nyob rau lub sijhawm ntev, qhov kev tso tawm ntawm endogenous carnitine yuav txo tau OCTN2 qhia los ntawm cov lus qhia tsis zoo, ntxiv kev txwv kev nqus.
Induction ntawm Metabolic Enzymes
Cov koob tshuaj ntau ntawm carnitine tuaj yeem ua rau muaj kev ua haujlwm ntawm carnitine metabolizing enzymes (xws li carnitine acetyltransferase thiab carnitine palmitoyltransferase) hauv daim siab thiab cov hnyuv, ua kom nrawm nrawm lossis hloov pauv ntawm carnitine mus rau qhov tsis muaj zog acylcarnitine derivatives, yog li txo qis bioavailability.
Kev cuam tshuam ntawm plab microbiota
Unabsorbed carnitine yog metabolized los ntawm cov kab mob tshwj xeeb (xws li Escherichia coli) hauv cov nyuv rau TMA, uas tom qab ntawd oxidized rau TMAO los ntawm hepatic flavin monooxygenase (FMO). Kev sib sau ntawm TMAO tuaj yeem tawm tswv yim inhibit carnitine nqus los ntawm cov txheej txheem hauv qab no:
Hloov pauv tus nqi pH ntawm txoj hnyuv cuam tshuam rau ion dependent thauj kev ua haujlwm ntawm OCTN2;
Inducing plab hnyuv o thiab cuam tshuam kev ncaj ncees ntawm txoj hnyuv epithelial hlwb;
Kev tswj kev noj qab haus huv ntsig txog cov tshuaj hormones xws li leptin thiab ghrelin los ntawm lub plab lub hlwb axis tsis ncaj qha cuam tshuam rau lub zog metabolism.
Optimization Strategy: Hla los ntawm 'saturation trap'
Formulation txhim kho
Nanotechnology
Encapsulating L-carnitine nyob rau hauv nanoparticles xws li liposomes thiab polymer micelles tuaj yeem txhim kho nws cov solubility thiab mucosal permeability, yog li hla lub peev xwm txwv ntawm OCTN2. Piv txwv li:
Tus nqi nqus ntawm L-carnitine encapsulated hauv liposomes hauv Caco-2 cell qauv yog 3-5 npaug siab dua li hauv nws daim ntawv dawb;
Nanocrystalline formulations tuaj yeem nce bioavailability ntawm carnitine mus rau ntau dua 30%.
Transdermal tshuaj xa system
Kev xa ncaj qha ntawm L-carnitine mus rau txheej txheej dermis los ntawm microneedle array lossis iontophoresis thev naus laus zis tuaj yeem zam cov nyhuv saturation ntawm txoj hnyuv nqus. Cov kev sim tsiaj tau pom tias bioavailability ntawm carnitine los ntawm kev tswj hwm kev hloov pauv tuaj yeem ncav cuag 2-3 npaug ntawm kev tswj qhov ncauj.
Combination therapy zoo
Inhibition of TMAO tiam
Kev sib xyaw ua ke ntawm TMA synthesis inhibitors xws li 3,3-dimethyl-1-butanol (DMB) tuaj yeem txo cov metabolism ntawm cov carnitine uas tsis tau nqus thiab ua kom tsis muaj zog ntxiv rau nws cov bioavailability.
Txoj cai ntawm transporter protein qhia
Kev siv lub sijhawm luv luv ntawm OCTN2 inducers (xws li vitamin C thiab vitamin E) tuaj yeem txhim kho kev thauj mus los, tab sis qhov ntau npaum li cas yuav tsum tau tswj nruj me ntsis kom tsis txhob tawm tswv yim cuam tshuam los ntawm kev siv ntau dhau.
Kev Tsim Kho Tshuaj Kho Mob Tus Kheej
Tsim kom muaj kev noj tshuaj raws li tus neeg sib txawv hauv OCTN2 genotype (xws li SLC22A5 ib leeg nucleotide polymorphism):
Cov tib neeg uas muaj cov metabolism sai (kev ua haujlwm siab OCTN2) tuaj yeem nce lawv cov tshuaj kom tsim nyog;
Cov tib neeg uas muaj cov metabolism hauv qeeb (kev ua haujlwm OCTN2 qis) yuav tsum tau txo lawv cov tshuaj kom tsis txhob noj ntau dhau.
Cov lus nug nquag
Yuav tshuaj tsuag rau ntawm daim tawv nqaij hlawv rog? Nws tau nyob hauv li cas?
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Nws tsis tuaj yeem hlawv roj ncaj qha, tab sis nws tuaj yeem nkag mus rau ntawm daim tawv nqaij tiag tiag. L-carnitine yog hydrophilic molecule uas nyuaj rau hla daim tawv nqaij barrier ntawm nws tus kheej. Cov tshuaj tua kab mob feem ntau vam khom cov tshuaj tiv thaiv kab mob (xws li cawv thiab lecithin) lossis nano liposome thev naus laus zis los pab carnitine molecules nkag mus rau subcutaneous microcirculation los ntawm cov hauv paus plaub hau lossis cov chaw ntawm tes. Nws lub hom phiaj yog nkag mus rau hauv cov ntshav, tsis yog ncaj qha decompose rog nyob rau hauv cov tshuaj tsuag.
Qhov twg yog "ceev" piv rau qhov ncauj tshuaj ntsiav?
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Ceev ceev bypassing thawj pass nyhuv ntawm daim siab. Feem ntau ntawm qhov ncauj L-carnitine yog metabolized los ntawm daim siab, nrog rau bioavailability ntawm tsuas yog 5-15%. Cov tshuaj tsuag yog absorbed los ntawm qhov ncauj mucosa los yog daim tawv nqaij thiab ncaj qha nkag mus rau hauv lub systemic ncig. Raws li txoj cai, cov ntshav concentration nce sai dua. Tab sis qhov tsis zoo yog tias ib koob tshuaj tsuas yog txwv, thiab tag nrho cov kev noj haus feem ntau qis dua qhov noj qhov ncauj.
Vim li cas qee cov tshuaj tsuag yuav tsum tau tub yees? Nws puas yuav tawg hauv lub hnab?
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Vim tias qee qhov siab - kawg tshuaj tsuag siv liposome txheej tshuab. Liposomes yog phospholipid bilayer me me spheres zoo ib yam li cell membranes, uas yog nquag fusion, rupture, los yog to ntawm kub kub, ua rau tsis ua hauj lwm ntawm cov khoom xyaw. Cov khoom lag luam no feem ntau tau sau npe tias yog tub yees ntawm 2-8 ° C, thiab tuaj yeem deteriorate nyob rau hauv ob peb hnub tom qab muab cia rau hauv chav tsev kub.
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