Shaanxi BLOOM Tech Co., Ltd. yog ib qho ntawm cov tuam ntxhab thiab cov muag khoom ntawm flibanserin tee hauv Suav teb. Txais tos rau cov lag luam wholesale bulk zoo flibanserin tee rau muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Flibanserin Dropsyog multi- phiaj xwm neurotransmitter modulator uas tuaj yeem kho tau zoo los ntawm titration ntawm koob tshuaj 5-20 mg / zaug. Kev nqus mucosal tuaj yeem ua luv luv rau 30-60 feeb, ua rau nws siv tau ntau dua rau cov menyuam yaus, cov neeg laus, thiab cov neeg mob nqos cov kab mob. Flibanserin muaj solubility tsawg heev hauv dej (<0.1 mg/mL), so it needs to form salt forms (such as hydrochloride or phosphate), use cyclodextrin inclusion technology, and then add cosolvents (such as propylene glycol, polyethylene glycol 400). At the same time, its bitterness needs to be masked, and ion exchange resin or microencapsulation technology can be used. For dose accuracy, a high-precision dropper is required to ensure that the volume error per drop is less than 5%.
Peb cov khoom
Cov ntaub ntawv ntxiv ntawm chemical compound:
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FlibanserinCOA
Mid seam dorsal nucleus - lub "sab sauv hloov" rau kev pib ua
Hyposexual ntshaw disorder (HSDD) yog ib tug poj niam uas muaj kev sib deev ua tsis taus pa uas tshwm sim los ntawm kev sib deev tsis txaus siab los yog kev xav, kev ntxhov siab loj thaum kev sib deev, thiab tsis tshwm sim los ntawm lwm yam kev mob hlwb, kev phiv tshuaj, lossis teeb meem kev sib raug zoo ntawm tus kheej. Cov poj niam cev xeeb tub ua ntej muaj kev pheej hmoo siab rau HSDD, uas cuam tshuam rau lawv lub neej zoo thiab kev sib raug zoo ntawm tus khub. Raws li lub ntiaj teb thawj cov tshuaj pom zoo rau kev kho HSDD hauv cov poj niam premenopausal, cov txheej txheem tseem ceeb ntawm kev ua ntawmFlibanserin Dropsnyob rau hauv nws cov kev cai ntawm Dorsal Raphe Nucleus (DRN) nyob rau hauv lub hlwb. Lub dorsal raphe nucleus, uas yog lub hauv paus tseem ceeb ntawm 5-hydroxytryptamine (5-HT) hauv lub hlwb, muaj ntau yam neurons xws li dopamine (DA) thiab gamma aminobutyric acid (GABA), thiab ua lub luag haujlwm tseem ceeb hauv kev tswj cov haujlwm xws li kev xav, kev paub, thiab nqi zog. Flubanserin txhim kho HSDD cov tsos mob los ntawm kev tswj cov kab mob neurotransmitter ntawm dorsal raphe nucleus, tsim ib qho "triple regulation" qauv, rov ua kom lub cev muaj zog ntawm kev sib deev kev tswj hwm kev sib deev.
Cov qauv thiab kev ua haujlwm ntawm dorsal nucleus ntawm midline
Anatomical qhov chaw thiab neuronal muaj pes tsawg leeg ntawm dorsal raphe nucleus
Lub dorsal raphe nucleus nyob rau hauv ib qho chaw nqaim ze ntawm qhov nruab nrab ntawm lub hlwb thiab yog qhov chaw tseem ceeb ntawm lub hlwb uas muaj serotonin neurons. Cov pab pawg raphe nucleus suav nrog ntau lub subnuclei, ntawm cov uas raphe dorsal nucleus tau nyiam ntau yam vim nws qhov chaw tshwj xeeb anatomical thiab cov yam ntxwv ua haujlwm. Lub dorsal raphe nucleus tsis tsuas yog muaj ntau ntawm 5-hydroxytryptamine neurons (li ib feem peb ntawm tag nrho cov hom neurons hauv lub nucleus), tab sis kuj tseem muaj dopaminergic, GABAergic, glutamatergic, thiab peptide neurons. Qhov sib txawv ntawm hom neuron no tso cai rau dorsal raphe nucleus los koom nrog kev tswj hwm ntawm ntau lub hlwb ua haujlwm.
Projection fibers thiab kev sib txuas ua haujlwm ntawm dorsal raphe nucleus
Lub ascending projection fibers ntawm dorsal raphe nucleus yog dav faib nyob rau hauv ntau lub cheeb tsam ntawm lub hlwb, nrog rau lub hauv paus grey teeb meem ntawm lub midbrain, hypothalamus, lub parietal nucleus ntawm dorsal thalamus, cerebellum, amygdala pawg, hippocampal qauv, septal nucleus, causdateam thiab pem hauv ntej. Cov phiaj xwm fibers no ua rau lub dorsal raphe nucleus koom nrog hauv kev tswj hwm ntawm ntau yam haujlwm xws li kev xav, kev paub, khoom plig, thiab kev nco. Piv txwv li, qhov projection los ntawm dorsal raphe nucleus mus rau prefrontal cortex plays lub luag haujlwm tseem ceeb hauv kev paub txog kev tswj hwm thiab kev xav; Qhov projection rau amygdala yog koom nrog kev tswj hwm ntawm kev ntshai thiab kev ntxhov siab; Qhov kev kwv yees rau cov nucleus accumbens yog ze ze rau qhov khoom plig thiab kev txhawb siab tus cwj pwm.
Lub luag haujlwm ntawm dorsal raphe nucleus hauv kev tswj kev xav thiab kev paub
5-hydroxytryptamine neurons nyob rau hauv dorsal raphe nucleus ua lub luag haujlwm tseem ceeb hauv kev tswj kev xav. 5-hydroxytryptamine, uas yog ib qho tseem ceeb neuromodulator, koom nrog hauv kev tswj hwm ntau yam kev xav xws li kev nyuaj siab, kev ntxhov siab, thiab kev coj cwj pwm nruj. Cov serotonergic neurons nyob rau hauv dorsal raphe nucleus tso tawm serotonin mus rau ntau lub hlwb hauv cheeb tsam los ntawm lawv qhov kev nthuav dav fiber ntau, yog li tswj hwm cov xwm txheej ntawm cov cheeb tsam hauv lub hlwb. Piv txwv li, qhov projection los ntawm dorsal raphe nucleus mus rau lub prefrontal cortex tuaj yeem cuam tshuam ntau excitation ntawm prefrontal cortex neurons thiab tswj kev xav; Kev kwv yees rau amygdala tuaj yeem txo qis kev ua kom ntau dhau ntawm amygdala thiab txo qis kev ntxhov siab thiab kev ntshai.
Hais txog kev paub txog kev tswj hwm, dopaminergic neurons hauv dorsal raphe nucleus ua lub luag haujlwm tseem ceeb. Cov kev tshawb fawb tsis ntev los no tau pom tias dopaminergic neurons nyob rau hauv dorsal raphe nucleus yog ib qho kev ywj pheej midbrain dopamine subsystem uas muaj nyob rau tib lub sij hawm rau dopaminergic neurons nyob rau hauv lub ventral tegmental cheeb tsam (VTA). Dopaminergic neurons nyob rau hauv dorsal raphe nucleus yog koom nrog hauv kev tswj hwm ntawm qhov tseem ceeb encoding, nco qhia, thiab arousal functions. Piv txwv li, dopaminergic neurons nyob rau hauv dorsal raphe nucleus tuaj yeem nkag siab qhov tseem ceeb ntawm qhov khoom plig thiab kev rau txim cuam tshuam txog stimuli, thiab raug tswj los ntawm tsiaj lub cev lub cev thiab qhov ntau thiab tsawg nqi zog; Nyob rau hauv cov nqe lus ntawm lub cim xeeb qhia, dopaminergic neurons nyob rau hauv lub dorsal raphe nucleus project rau cov cheeb tsam xws li lub amygdala thiab striatum, koom nyob rau hauv lub cim xeeb consolidation thiab retrieval; Nyob rau hauv cov nqe lus ntawm arousal regulation, dopaminergic neurons nyob rau hauv lub dorsal raphe nucleus tswj lub cev lub arousal xeev los ntawm kev txhawb kev ua si nyob rau hauv arousal ntsig txog lub hlwb cheeb tsam.
Hom "triple regulation" ntawm fluobanserin hauv dorsal raphe nucleus
Lub mechanism ntawm kev txiav txim ntawm fluoxetine nyob rau hauv lub dorsal raphe nucleus tuaj yeem muab sau ua "triple regulation" hom, uas tswj cov serotonin, dopamine, thiab noradrenaline systems. Hom no yog pom tau los ntawm cov hauv qab no:
Flubanserin tswj kev ua haujlwm ntawm serotonin system hauv dorsal raphe nucleus los ntawm kev ua kom lub serotonin 1A receptor thiab antagonizing serotonin 2A receptor. Txoj cai tswjfwm no tuaj yeem:
Inhibit ntau excitation ntawm 5-hydroxytryptamine neurons nyob rau hauv lub dorsal raphe nucleus thiab tswj kev xav stability;
Txo cov nyhuv inhibitory ntawm serotonin ntawm dopaminergic thiab noradrenergic neurons, thiab txhim khu kev tso tawm ntawm cov neurotransmitters;
Tswj glutamate kis tau tus mob thiab txhim kho kev txawj ntse tswj kev ua haujlwm;
Los ntawm desensitizing nws tus kheej receptors, nws nruab nrab nce qib ntawm serotonin hauv synaptic cleft kom tsis txhob muaj kev ntxhov siab ntau dhau.
Txoj Cai Thib Ob: Txhim Kho Dopamine System
Flubanserin indirectly txhim khu lub dopamine system muaj nuj nqi ntawm dorsal raphe nucleus los ntawm kev tswj cov serotonin system. Txoj cai tswjfwm no tuaj yeem:
Txhim kho dopamine tso tawm los ntawm dorsal raphe nucleus mus rau lub nucleus accumbens thiab prefrontal cortex, txhim kho kev txhawb zog thiab kev txawj ntse;
Kev tswj hwm dopamine receptor muaj nuj nqi los tiv thaiv kev mob tshwm sim los ntawm kev ua kom ntau dhau ntawm dopamine system;
Ua kom cov dopamine D4 receptors txhawb kev tsim thiab kev saib xyuas ntawm kev sib deev txaus siab.
kev phiv tshuaj
Flibanserin Dropsyog ib qho tshuaj siv los kho tus mob kis tau, tsis muaj libido tsis meej (HSDD) hauv cov poj niam premenopausal. Nws cov txheej txheem ntawm kev ua haujlwm cuam tshuam nrog kev tswj cov neurotransmitters xws li dopamine, norepinephrine, thiab serotonin hauv lub hlwb. Txawm hais tias cov tshuaj muab kev kho mob rau cov neeg mob tshwj xeeb, nws cov kev cuam tshuam tsis zoo yuav raug tsis quav ntsej.
Tej yam tshwm sim tsis zoo
kiv taub hau: Nws yog ib qho teeb meem tshwm sim feem ntau hauv kev kho mob ntawm fluoxetine, nrog rau qhov tshwm sim ntau. Hauv kev sim tshuaj ntsuam xyuas, qhov tshwm sim ntawm kiv taub hau tau nce siab dua hauv cov neeg mob kho nrog fluoxetine dua li hauv pawg placebo. kiv taub hau tuaj yeem cuam tshuam rau cov neeg mob cov dej num niaj hnub xws li taug kev, tsav tsheb, thiab lwm yam, ua rau muaj kev pheej hmoo ntawm kev ntog thiab raug mob.
Pw tsaug zog: Flibanserin muaj lub hauv paus paj hlwb inhibitory nyhuv, uas yuav ua rau cov neeg mob tsaug zog los yog nkees. Qhov kev qaug zog no yuav tshwm sim tshwj xeeb tshaj yog nyob rau theem pib ntawm kev kho mob, cuam tshuam rau tus neeg mob txoj haujlwm ua haujlwm thiab lub neej zoo.
Insomnia: Txawm hais tias Flibanserin feem ntau pom zoo kom noj ua ntej yuav mus pw kom txo tau cov kev phiv xws li qaug zog thiab kiv taub hau, qee cov neeg mob kuj tseem muaj cov tsos mob insomnia. Insomnia tuaj yeem tshwm sim raws li kev nyuaj pw tsaug zog, pw tsaug zog tsis zoo, lossis thaum sawv ntxov, cuam tshuam rau tus neeg mob lub siab lub ntsws thiab lub cev noj qab haus huv.
Kev qaug zog: Kev qaug zog yog lwm qhov tsis zoo tshwm sim ntawm kev kho mob Flibanserin, uas yuav tshwm sim raws li kev qaug zog, tsis muaj zog, thiab lwm yam. Qhov kev xav ntawm kev qaug zog no tuaj yeem tshwm sim, cuam tshuam rau tus neeg mob cov dej num txhua hnub thiab kev ua haujlwm hauv zej zog.
xeev siab: xeev siab yog ib qho ntawm cov kab mob digestive uas tsis zoo tshwm sim hauv kev kho mob ntawm fluconazole. Kev xeev siab tuaj yeem tshwm sim ib leeg lossis nrog cov tsos mob xws li ntuav thiab tsis qab los noj mov, cuam tshuam rau tus neeg mob noj zaub mov noj thiab kev noj qab haus huv ntawm lub cev.
Lub qhov ncauj qhuav: Lub qhov ncauj qhuav yog lwm qhov tsis zoo tshwm sim ntawmFlibanserin DropsKev kho mob, uas yuav tshwm sim raws li qhov ncauj qhuav, nqhis dej, thiab lwm yam. Qhov ncauj qhuav tuaj yeem ua rau muaj kev pheej hmoo ntawm cov hniav caries thiab qhov ncauj kab mob hauv cov neeg mob, thiab cov kev ntsuas qhov ncauj yuav tsum tau ua.
Constipation: Qee cov neeg mob yuav pom cov tsos mob cem quav thaum kho nrog Flibanserin. Kev cem quav tuaj yeem tshwm sim raws li kev txo qis hauv plab, cov quav qhuav thiab tawv, thiab lwm yam, ua rau muaj kev pheej hmoo ntawm cov neeg mob tsim cov kab mob hauv qhov quav thiab qhov quav xws li hemorrhoids thiab qhov quav fissures.
Lub qhov ncauj qhuav, raws li ib qho ntawm cov kev tsis zoo tshwm sim, kuj tseem tuaj yeem ua rau muaj teeb meem xws li ua pa tsis zoo vim qhov txo qis ntawm qhov ncauj tus kheej - muaj peev xwm ntxuav, ntxiv rau cov teeb meem saum toj no - hais txog. Nws yuav tsum tau txo qis los ntawm kev nce dej haus thiab siv cov qaub ncaug dag.
Kev phiv loj heev
Hypotension thiab fainting
Hypotension: Flibanserin tuaj yeem ua rau hypotension, tshwj xeeb tshaj yog thaum cov neeg mob tam sim ntawd sawv ntawm qhov chaw pw lossis zaum. Hypotension tuaj yeem ua rau cov tsos mob xws li kiv taub hau, tsaus muag ntawm lub qhov muag, qaug zog, thiab thaum mob hnyav, nws tuaj yeem ua rau qaug zog.
Kev qaug zog: Kev qaug zog yog ib qho kev tsis zoo ntawm kev kho mob Flibanserin, uas tuaj yeem tshwm sim los ntawm ntau yam xws li hypotension thiab central paj hlwb inhibition. Kev qaug zog tuaj yeem ua rau cov neeg mob poob thiab raug mob, thiab ua rau muaj kev phom sij rau lawv lub neej. Yog li ntawd, cov neeg mob yuav tsum tsis txhob muaj kev hloov pauv ntawm txoj hauj lwm tam sim ntawd, xws li sawv ntsug ntawm qhov dag lossis zaum, thaum kho nrog fluoxetine.
Central paj hlwb kev nyuaj siab
Cov tsos mob tshwm sim: Flibanserin muaj qhov cuam tshuam hauv nruab nrab ntawm lub paj hlwb inhibitory, uas tuaj yeem ua rau cov tsos mob hauv nruab nrab ntawm lub paj hlwb kev nyuaj siab hauv cov neeg mob, xws li ua pa qeeb, ua tsis taus pa, tsis nco qab, thiab nyuaj rau tswj kev tsaug zog.
Yam Tseem Ceeb: Qhov kev pheej hmoo ntawm kev ntxhov siab hauv nruab nrab ntawm lub paj hlwb tuaj yeem nce ntxiv vim tus neeg mob siv lwm yam hauv nruab nrab paj hlwb inhibitors (xws li cawv, sedatives, hypnotics, thiab lwm yam). Yog li ntawd, cov neeg mob yuav tsum tsis txhob haus cawv thiab siv lwm yam hauv nruab nrab paj hlwb inhibitors thaum kho nrog fluoxetine.
Kev ua xua
Cov tsos mob: Flibanserin tuaj yeem ua rau muaj kev tsis haum, nrog rau khaus khaus, khaus khaus, urticaria, angioedema, thiab lwm yam. Kev tsis haum tshuaj hnyav tuaj yeem tshwm sim ua pa nyuaj, laryngeal edema, anaphylactic shock, thiab lwm yam, ua rau tus neeg mob lub neej txaus ntshai.
Kev ntsuas kev kho mob: Yog tias cov neeg mob muaj kev tsis haum tshuaj thaum kho nrog Flibanserin, lawv yuav tsum tsis txhob noj tshuaj tam sim ntawd thiab nrhiav kev kho mob. Cov kws kho mob yuav siv cov kev kho mob raws li qhov hnyav ntawm tus neeg mob cov tsos mob, xws li siv cov tshuaj tiv thaiv kab mob, glucocorticoids, thiab lwm yam kom txo tau cov tsos mob tsis haum, thiab muab kev kho mob ceev yog tias tsim nyog.
Zaj dab neeg ntawm Flubanserin Droplets tsis pib nrog kev tsim nws tus kheej, tab sis nrog kev ua tsis tiav ntawm kev txhim kho tshuaj tiv thaiv kab mob los ntawm German kws tshuaj tuam txhab Boehringer Ingelheim hauv xyoo 1990. Lub sijhawm ntawd, lub khw muag tshuaj kho mob hlwb thoob ntiaj teb tau tsom mus rau kev txhim kho serotonin (5-HT) receptor modulators, thiab Boehringer Ingelheim cov kev tshawb fawb thiab kev loj hlob pab pawg tau tig lawv lub siab rau ib hom tshiab ntawm piperazine derivative - ib qho kev sib txuas codenamed BIMT-17, nrog lub npe tshuaj fluorome (2-4-triyl). phenyl) piperazine-1-) ethyl) -1H-benzimidazol-2-ib.
Nyob rau xyoo 1990s, kev tshawb fawb neuroscience tau lees paub tias kev ua haujlwm tsis zoo ntawm serotonin system tau cuam tshuam nrog kev nyuaj siab. Cov kws tshawb fawb ntawm Boehringer Ingelheim vam tias yuav tsim cov tshuaj tshiab nrog cov kev mob tshwm sim qis dua li cov tshuaj tricyclic antidepressants los ntawm kev ua kom zoo dua qhov kev xaiv ntawm cov tebchaw ntawm 5-HT receptors. Thaum ntxov nyob rau hauv vitro thwmsim pom tau hais tias BIMT-17 muaj excitatory kev ua ub no ntawm 5-HT1A receptors thiab antagonistic ua ub no ntawm 5-HT2A receptors. Qhov kev ua haujlwm thib ob ntawm kev ua haujlwm no tuaj yeem ua rau kev xav zoo dua los ntawm kev tswj hwm kev tso tawm neurotransmitter.
Xyoo 1996, BIMT-17 tau nkag mus rau theem I kev sim tshuaj ntsuam xyuas feem ntau los ntsuas cov yam ntxwv ntawm cov tshuaj pharmacokinetic thiab kev nyab xeeb hauv cov kev noj qab haus huv. Cov txiaj ntsig tau pom tias qhov sib xyaw ua ke mus txog nws cov ntshav siab tshaj plaws 2 teev tom qab kev tswj hwm qhov ncauj, nrog rau ib nrab-lub neej ntawm kwv yees li 11 teev. Nws tau txais txiaj ntsig zoo ntawm koob tshuaj 100mg, tsuas yog ob peb tus neeg tau ntsib cov tsos mob qaug zog me ntsis.
Pab pawg R & D tau pib qhov kev sim tshuaj thib II hauv xyoo 1998, uas suav nrog 237 tus neeg mob uas muaj kev nyuaj siab me me mus rau qhov hnyav. Lawv tau txais koob tshuaj 50mg thiab 100mg ntawm BIMT-17 thiab placebo, raws li, rau lub sijhawm kho ntawm 8 lub lis piam. Txawm li cas los xij, cov txiaj ntsig kev sim tau poob siab: qhov kev txhim kho ntawm cov qhab nia ntawm kev nyuaj siab hauv ob pawg koob tshuaj yog 32% thiab 35%, feem, qis dua li pawg tswj hwm 55%, thiab qhov tshwm sim ntawm kev qaug zog hauv pawg 100mg koob tshuaj tau nce mus rau 27%, uas tsis mus txog qhov kawg ntawm kev kho mob.
Hauv xyoo 2000, pab pawg R&D tau kho cov phiaj xwm thiab pib qhov kev sim thib ob thib ob, sim txhim kho kev ua tau zoo los ntawm kev ncua lub sijhawm tshuaj mus rau 12 lub lis piam thiab ua kom zoo dua cov tshuaj gradient, tab sis cov txiaj ntsig tseem tsis tau raws li tus qauv.
Hauv xyoo 2003 kev soj ntsuam cov ntaub ntawv tshuaj xyuas, cov kws tshawb fawb tau tshawb pom qhov tshwm sim tsis tau xav txog: ntawm 187 tus poj niam cov neeg mob uas muaj kev nyuaj siab suav nrog, 23% ntawm cov neeg koom tau tshaj tawm "qhov tseem ceeb hauv libido" hauv lawv cov ntawv txheeb xyuas tus kheej, thaum qhov kev faib ua feem no tsuas yog 4% ntawm cov txiv neej koom thiab tsis cuam tshuam nrog kev txhim kho cov tsos mob kev nyuaj siab. Qhov kev tshawb pom no tau ua rau cov kws paub txog kev sib daj sib deev - lub sijhawm ntawd, poj niam txiv neej ua haujlwm tsis zoo (HSDD) tau maj mam dhau los ua qhov kev tshawb fawb kho mob hotspot, tab sis tsis muaj cov tshuaj pom zoo pom zoo thoob ntiaj teb. Boehringer Ingelheim tau txiav txim siab tam sim ntawd ncua kev txhim kho cov tshuaj tiv thaiv kev ntxhov siab thiab tig mus rau kev tshawb nrhiav nws cov peev txheej hauv kev noj qab haus huv ntawm kev sib deev.
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