Tianeptine Sodium ntsiav tshuajyog cov tshuaj noj uas muaj lub zog nquag tianeptine sodium. Nws zwm rau qeb ntawm cov tshuaj tiv thaiv kev ntxhov siab thiab feem ntau yog siv los kho kev nyuaj siab thiab cuam tshuam cov kev tsis sib haum xeeb. Sodium Tianeptin txhim kho kev xav thiab txo cov tsos mob depressive los ntawm kev txhim kho cov serotonin hauv lub hlwb, thaum me ntsis cuam tshuam rau dopamine tshuab thiab Noradrenaline tshuab. Feem ntau cov tshuaj tiv thaiv kev ntxhov siab, xws li SSRIS, nce siab los ntawm kev ua haujlwm ntawm kev ua ntawm Tianeptin sodium yog qhov sib txawv tab sis muaj kev sib luag. Nws tuaj yeem muaj cov teebmeem kev cuam tshuam rau kev mob mob ntev, Fibromyalgia, lossis kev ntxhov siab- Cov lus qhia ntsig txog kev kho mob. Nws tuaj yeem ua rau muaj kev cuam tshuam zoo xws li lub qhov ncauj qhuav, quav ntsej muag, kiv taub hau, tsaug zog, xeev siab, lossis xeev siab, lossis kem plab lossis kem plab.
Nyob rau tib lub sijhawm, peb lub tuam txhab tsis tsuas yog muab cov hmoov dawb, tab sis kuj cov ntsiav tshuaj thiab cov tshuaj. Yog tias xav tau, thov koj xav tiv tauj peb txhua lub sijhawm.
Cov ntaub ntawv ntxiv ntawm kev sib txuas lus:
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Tianeptine sodium coa
Tianeptine Sodium ntsiav tshuajyog ib qho tshuaj antidepressantantualant siv los kho kev nyuaj siab thiab cuam tshuam cov kev tsis sib haum xeeb, nrog nws cov txuj ci ua haujlwm tau tianeptine sodium. Cov hauv qab no yog cov lus qhia ntxaws ntxaws ntawm nws cov ntaub ntawv tsim khoom:
Npaj cov khoom siv raw thiab cov khoom siv
Kev npaj cov khoom xyaw (API)
Cov synthesis ntawm Tianeptin sodium yuav tsum muaj ntau cov organic cov tshuaj tiv thaiv, thiab cov ntaub ntawv nyoos muaj xws li:
Pib cov khoom: xws li o - chlorooaniline, cyclohexanone, thiab lwm yam loj dua los yog sib npaug rau 99%.
Nruab nrab: Npaj los ntawm kev hws, kev sib deev, chlorination thiab lwm yam kev tawm tsam, nrog kev tswj hwm nruj me ntsis thiab - cov khoom).
Ntsev teeb tsa cov kev xav: cov kua qaub dawb ntawm Thiametoxam tau ua rau sodium hydroxide los tsim cov ntsev ntau dhau los yog kev rhuav tshem.
Cov Ntsiab Lus Tseem Ceeb: Cov kev tshwm sim ntawm kub (ntsuas kub (kub, catalyst ntau npaum li cas) yuav tsum tau ua kom tsis txhob muaj sab. Purification txheej txheem (xws li recrystallization thiab chromatographic sib cais) yuav tsum tau tshem tawm genotoxic impurities (xws li nitrosamines). Cov txheej txheem ziab khaub ncaws yuav tsum zam cov mob API tshwm sim los ntawm qhov kub siab.
Xaiv thiab Kev Npaj ntawm Cov Ntaub Ntawv
Lub excipients yuav tsum tau ua raws li Suav papaceploeia lossis USP / EP cov qauv, thiab ib txwm siv kev tshuaj uas suav nrog:
Fillers: Lactose, microcrystalline cellulose (kom nce cov ntsiav tshuaj ntim).
Nplaum: polyvinylprolidine (PVP), HydroxyPropyyl methylenculose (HPMC) (txhawb nqa cov txheej txheem sib txawv).
Tshuaj tua kab mob: Cov khaub ncaws hla BARBOKSHNETHNETH Cellulose Sodium (CCNA), Carboxymethyl Starch sodium (CMS cov ntsiav tshuaj tawg).
Lubricants: magnesium stearate, talc hmoov (kom txo kev sib txhuam thaum lub sijhawm compression).
Cov Khoom Siv Txheej: HydroxyPropyyl methylcellose (HPMC), Polyethylene Glycol (txhawm rau txhim kho cov tsos mob thiab npog ntsej muag).
Kuaj cov qauv: Tsis muaj kev sib cuam tshuam ntawm expiient thiab apis (xws li kev zam kev siv sulfite uas muaj kev tiv thaiv oxidative deg). Xav txog cov neeg muaj feem tshwj xeeb (xws li lactose tsis xav tau kev hloov nrog lwm cov fillers).
Synthesis txheej txheem thiab kev npaj tsim
Cov txheej txheem hluavtaws ntawm Tianeptin sodium
Cov kev sib xyaw ua hluav taws xob tau muab faib ua cov kauj ruam hauv qab no:
Kev Cuam Tshuam Cua: Lub hws ntawm O -} chlorooaniline nrog cyclozanone ua rau nruab nrab ntawm norihdrodibethiazine.
Chlorination kev tawm tsam: qhia chlorine atoms raws li kev txiav txim ntawm cov catalyst (xws li fecl α) los ua 3-chloro compounds.
Methylation Cov Yam: Qhia pawg methyl ntawm txoj haujlwm 6 los ntawm methylation reagent xws li Iodomethane.
Amino Sab Txoj saw Taw qhia: reacts nrog 7-aminoheptanoic acid los ua lub hom phiaj molecule.
Ntsev teeb thiab purification: reacts nrog sodium hydroxide los tsim cov ntsev sodigization lossis chromatography kom tau siab {{purity api.
Txheej Txheem Txhim Kho Kom Zoo:
Txais kev hloov pauv khiav ceev nrag kev tawm tsam los txhim kho cov txiaj ntsig (tam sim no chav kuaj theem qis tshaj yog li 65-70%).
Tsim cov catalysts ntsuab (xws li biocativysis) kom txo cov pov tseg.
Ntsiav Tshuaj Npaj Txheej Txheem
Kev ntub dej ntub thiab cov txheej txheem compression (cov txheej txheem tseem ceeb)
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Ua Ntej Sib xyaw
Ua ntej sib xyaw API nrog qee cov fillers (xws li microcrystalline cellulose) los xyuas kom muaj kev sib luag.
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Ntub av granulle
Ntxiv cov tshuaj nplaum (xws li 5% pvp ethanol daws) thiab tsim cov khoom ntub los ntawm high- ceev steelring granulator.
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Kom qhuav thiab granulation
Fluidized txaj ziab (Inlet Kub 50-60 degree), sieving (20-60 mesh) kom tau txais cov khoom sib dhos.
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TAG NRHO NWS
Ntxiv cov neeg tsis sib luag thiab roj nplua nyeem, sib tov rau 10-15 feeb.
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Ntsiav tshuaj nias
Tswj qhov sib txawv hauv cov ntsiav tshuaj hnyav (± 5%), hardness (50-100 n), thiab britleness (tsawg dua los yog sib npaug rau 1%).
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Txoj kev ncaj qha. Siv tau rau api nkag siab rau noo noo thiab cua sov)
Cov ntaub ntawv tso nrog kev hloov kho zoo (xws li txau cov lactose khiav kom qhuav thiab cov hmoov txhuv nplej siab) yuav tsum tau tshuaj xyuas.
Nws yog ib qho tsim nyog los tswj cov av noo ib puag ncig (RAWS tsawg dua lossis sib npaug nrog 40%) kom tiv thaiv cov lus ntawm cov dej noo thiab clumping.
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Txheej Txheej Txheem
Lub Hom Phiaj: Txhawm rau npog cov ntxhiab tsw tsis meej, tiv thaiv noo noo, thiab tswj cov tshuaj tso tawm.
Kev sib xyaw ntawm txheej daws teeb meem: HPMC (3-5%), Peg 400 (1-2%), Titanium Dioxide (1-2%), Talc Hmoov (0.5-1%).
Cov txheej txheem tsis: Inlet huab cua kub ntawm 60-70 degree, txheej qhov hnyav nce ntawm 3-5%.
Kev tswj kom zoo thiab kev sim cov qauv
API Cov Kev Tswjhwm Zoo
| Kuaj cov khoom | Txojkev | Lub hom phiaj |
| HPLC | HPLC (C18, Acetonitrile Phosphate Buffer Mobile Paus) | 98.0%-102.0% |
| Hais txog cov tshuaj | HPLC (Gradient Elfution) | Ib leeg impurity tsawg dua los yog sib npaug rau 0.5%, tag nrho cov impurity tsawg dua los yog sib npaug rau 1.5% |
| Residual Hnyav | GC (HeadSpace Txhaj Tshuaj) | Ethanol tsawg dua lossis sib luag rau 0.5%, methanol tsawg dua lossis sib npaug rau 0.3% |
| Yauv cov ntsiab lus | Karl Fischer txoj kev | Tsawg dua los yog sib npaug rau 3.0% |
| Hnyav Hlau | Atomic nqus spectroscopy | Tsawg dua los yog sib npaug rau 20 ppm |
Ntsiav Tshuaj Tswjhwm Zoo
| Kuaj cov khoom | Txojkev | Lub hom phiaj |
| Cov ntsiab lus sib xyaw | UV {- vis spectrophottometry | +1.8 s tsawg dua lossis sib npaug rau 15 (n =10) |
| Tus lej sib cais | Duav txoj kev (50 rpm, 0.1n hcl 900 ml) | 30 feeb ntau dua los yog sib npaug rau 80% |
| Microbial txwv | Txoj cai dav dav 1105 ntawm Suav Pharmacopoia | Tag nrho cov kab mob aerobic tsawg dua lossis sib npaug ntawm 1000 CFU / g, tag nrho cov pwm thiab cov poov xab tsawg dua lossis sib npaug rau 100 cfu / g |
| Qhov hnyav sib txawv | Uas Txoj Kev | 5% (nruab nrab ntsiav tshuaj hnyav qis dua 0.3 g) lossis ± 7.5% (0.3 g thiab siab dua) |
Cov kev tawm tsam
Tianeptine Sodium ntsiav tshuajyog cov tshuaj tiv thaiv kev ntxhov siab uas tau tawm tsam cov tshuaj tiv thaiv kev ntxhov siab thiab kev ntxhov siab ntawm cov kab mob glutamatergic thiab monoamine neurotransmitters xws li serotonin thiab norepinephrine. Txawm hais tias nws txoj kev ua tau zoo yog, saib xyuas thiab tswj cov tshuaj phiv tsis zoo (ADDRS) yog cov tseem ceeb ntawm kev siv tshuaj tiv thaiv kev siv tshuaj.
Cov kev sib raug zoo ntawm cov kev sib raug zoo tshaj plaws (cuam tshuam ntau dua lossis sib npaug rau 1%)
Kev teb neurological
| Cov kev tawm tsam | yam siab | Kho Mob Ua Haujlwm | lub tshuab | Kev Tswj Cov Lus Taw Qhia |
| Mob taub hau | 5%-15% | Pulsatile los yog mob taub hau tsis tu ncua, feem ntau pom thaum ntxov ntawm kev noj tshuaj | Vascular dilation lossis hloov hauv neural rhiab siab | Cov tsos mob kev kho mob (xws li Acetaminophen), feem ntau tau txais tsis pub dhau 1-2 asthiv |
| Kiv taub hau | 3%-10% | Kaj nti qhuav los yog sib npaug tsis zoo | Cov Ntshav Siab hloov pauv lossis nruab nrab ntawm cov leeg hlwb | Zam txhob sawv ntsug thiab saib xyuas cov ntshav siab |
| Kev kub siab | 2%-8% | Nruab Nruab Nruab Nrab thiab Quaj | H ₁ receptor blockade lossis 5-htergic nyhuv | Zam txhob tsav tsheb lossis kev ua haujlwm tshuab, thiab noj tshuaj thaum hmo ntuj |
| Pw tsis tau | 1%-5% | Nyuaj ntog pw tsaug zog lossis sawv ntxov (tshwj xeeb yog thaum nres cov tshuaj sai) | Da tuaj yeem ua haujlwm lossis pab cov tsos mob | Kev txo qeeb, sib xyaw ua ke nrog luv ua rau cov tshuaj hypnotic (xws li zolpidem) |
| Tshee | 1%-3% | Cov menyuam yaus sib tw (feem ntau pom hauv txhais tes) | Dopamine overactivation | Txo kev tshuaj lossis hloov mus rau xaiv 5-ht repketors (SSRIS) |
Teb Cov Tshuab Digestive
| Cov kev tawm tsam | yam siab | Kho Mob Ua Haujlwm | lub tshuab | Kev Tswj Cov Lus Taw Qhia |
| Xeev siab | 8%-20% | Sab sauv lub plab tsis xis nyob thiab ua kom qab los | 5-ht α receptor ua kom muaj zog lossis qeeb lub plab zom mov | Noj tshuaj nyob rau hauv cov koob tshuaj faib ua ke, noj nrog zaub mov, thiab siv cov tshuaj tiv thaiv kab mob (xws li Ondansetron) |
| Kem plab | 5%-12% | Txo cov zaus ntawm kev tawm tsam thiab qhuav thiab cov quav tawv | Qeeb Rau Kev Mob Hlwb | Nce kev noj haus muaj fiber ntau, dej haus, thiab siv cov tshuaj laxatives (xws li polyethylene glycol) |
| Qhov ncauj qhuav | 3%-8% | Qhuav qhov ncauj mucosa thiab nqhis dej | Cholinergic m receptor thaiv | Siv qab zib dawb khoom qab zib thiab siv cov qaub ncaug khoom siv qaub ncaug |
| Raws plab | 1%-5% | Xoob lossis quav dej (qee zaum pom) | Dysbiosis ntawm plab microbiota lossis 5-htergic cuam tshuam | Ntxiv cov tshuaj probiotics thiab siv tshuaj tiv thaiv kab mob (xws li cov hmoov montmorillonite) |
Teb cov lus teb cardiovascular system
| Cov kev tawm tsam | yam siab | Kho Mob Ua Haujlwm | lub tshuab | Kev Tswj Cov Lus Taw Qhia |
| Ortej lub hypotension | 2%-6% | Kiv taub hau thiab dub thaum sawv | - adrenergic receptor thaiv | Maj mam hloov chaw thiab nce ntsev kom tsawg |
| Kev palpitation | 1%-4% | Consciously nce lossis tsis xwm yeem lub plawv dhia | Kev ua kom muaj kev kub ntxhov siab | Cov tsos mob kev kho mob tom qab tsis suav nrog arhythmia (xws li beta blockers) |
| Ntshav Siab Hloov Ntshav | 1%-3% | Me me nce lossis txo qis hauv systolic / diastolic ntshav siab | Hloov hauv cov vascular nro | Nquag Saib cov ntshav siab thiab kho cov tshuaj |
Kev mob hlwb
| Cov kev tawm tsam | yam siab | Kho Mob Ua Haujlwm | lub tshuab | Kev Tswj Cov Lus Taw Qhia |
| Muaj kev ntxhov siab ntau dua | 1%-5% | Tshee thiab yooj yim chim (tshwj xeeb tshaj yog thaum ntxov ntawm kev noj tshuaj) | 5-ht nyhuv lossis tus kheej rhiab | Kev sib txuas ua ke benzodiazepines (xws li Lorazepam) rau luv - kev siv |
| Muaj zog | 1%-3% | Nyob tsis tswm thiab kev coj cwj pwm | Da ua haujlwm lossis tshuaj yeeb | Txo cov tshuaj lossis hloov mus rau SSRIS |
| Npau suav phem | 1%-2% | Muaj tseeb thiab txaus ntshai npau suav | REM pw tsaug zog | Zam kev noj tshuaj ua ntej yuav mus pw thiab siv luv luv ua tshuaj tiv thaiv antihistamines (xws li Docetamine) |
Lwm yam kev tawm tsam
| Cov kev tawm tsam | yam siab | Kho Mob Ua Haujlwm | lub tshuab | Kev Tswj Cov Lus Taw Qhia |
| Nce phaus | 2%-7% | Lub sij hawm luv (1-3 lub hlis) nce ntawm 2-5 kg | 5-t lub zog cuam tshuam lossis txo cov metabolic tus nqi | Kev tswj kev noj haus, nce kev tawm tsam, thiab kev hnav khaub ncaws hloov yog tias tsim nyog |
| Kev sib daj sib deev Dysfunction | 1%-4% | Erectile kawg, txo libido | 5-ht tuaj yeem inhibit lossis da muaj peev xwm txo qis | Siv phosphodiesterase inhibitors (xws li sildenafil) lossis hloov mus rau bupropion |
| Sawv pob | 1%-3% | Liab thiab khaus (qee zaus urticaria) | kev tsis haum | Antihistamines (xws li cetirizine) yuav tsum tau ua dua nyob rau hauv cov mob hnyav |
Cim npe nrov: Tianeptine Sodium ntsiav tshuaj, lwm tus neeg, chaw tsim khoom, Hoobkas, lag luam wholesale, yuav, nqe, loj, loj, rau muag