Peb lub tuam txhab tsom mus rau kev tsim khoom, kev tshawb fawb thiab kev tsim kho, thiab muab cov khoom siv sildenafil nrog CAS tus lej 139755-83-2. Peb muaj kev tswj xyuas nruj raws li qhov yuav tsum tau ua ntawm peb cov khoom Sildenafil raw khoom yog txiv neej aphrodisiac raw khoom, uas nce mus txog nws cov ntshav siab concentration (cmax) tom qab noj qhov ncauj ntawm lub plab khoob rau 30-120 feeb, thiab tom qab noj qhov ncauj tom qab noj mov rau 90-180 feeb. Cov neeg ua haujlwm pab dawb noj qab haus huv noj ib koob tshuaj ntawm 100mg, thiab tom qab 24 teev, cov tshuaj ntshav siab yog kwv yees li 2ng / ml, nrog rau cmax ntawm 440ng / ml. Lub siab ua haujlwm tsis zoo, lub raum tsis txaus, lossis nce qhov chaw nyob rau hauv qhov nkhaus (AUC) tom qab noj tshuaj rau cov neeg laus hnub nyoog 65 xyoos thiab siab dua. Sildenafil thiab nws cov loj circulating metabolites (N-demethylates) khi kwv yees li 96% rau plasma proteins, thiab cov protein binding tus nqi yog ywj siab ntawm tag nrho cov tshuaj concentration. Cov ntaub so ntswg tau muab faib zoo nrog lub ntim ntim (Vd) ntawm 105L. Sildenafil feem ntau yog tshem tawm los ntawm lub siab lub microsomal enzymes cytochrome P450 3A4 (CYP 3A4, thawj txoj hauv kev) thiab cytochrome P450 2C9 (CYP 2C9, theem nrab txoj hauv kev). Nws lub ntsiab metabolite (N-demethylate) muaj qhov zoo sib xws ntawm PDE xaiv rau sildenafil, nrog rau cov ntshav siab txog li 40% ntawm sildenafil. Yog li, kwv yees li 20% ntawm cov tshuaj pharmacological ntawm sildenafil los ntawm nws cov metabolites. Kev tshem tawm ib nrab ntawm lub neej ntawm sildenafil thiab nws cov metabolites yog kwv yees li 4 teev . 80% ntawm cov tshuaj noj yog tsuas yog tawm hauv daim ntawv ntawm metabolites los ntawm quav, thiab 13% yog tawm los ntawm ob lub raum . 90 feeb tom qab noj cov tshuaj, tus nqi ntawm sildenafil tsawg dua 0% ntawm cov neeg noj qab haus huv tau ntsuas 0. koob. Kev Siv: Phosphodiesterase (PDE) V selective inhibitor, uas tuaj yeem txhim kho cov lus teb physiological ntawm penile erection tshwm sim los ntawm TSIS tso rau hauv kev sib deev stimulation. Feem ntau yog siv rau erectile kawg ntawm noov.
Cov khoom siv
1. Kev siv thiab ntau npaum li cas: Rau cov neeg mob feem ntau, qhov koob tshuaj pom zoo yog 120mg, noj raws li xav tau li ntawm 1 teev ua ntej kev sib deev, thiab tom qab noj cov tshuaj, kev sib deev yog xav tau. Tab sis nws tuaj yeem noj txhua lub sijhawm hauv 0.5-4 teev ua ntej kev sib deev. Raws li kev ua tau zoo thiab kev kam rau siab, koob tshuaj txhua hnub tuaj yeem hloov kho ntawm 100-150mg, thiab yuav tsum tsis txhob ntau tshaj ib hnub. (1) Kev pom zoo pib koob tshuaj rau mob raum tsis txaus (AUC thiab cmax yuav luag ob npaug thaum creatinine tshem tawm tsawg dua lossis sib npaug li 30ml / min) yog 25mg. (2) Qhov pom zoo pib koob tshuaj rau daim siab ua haujlwm tsis zoo (xws li mob siab ua haujlwm siab, AUC thiab cmax nce 84% thiab 47%, feem) yog 25mg.
2: Kev sib cuam tshuam: Thaum siv ua ke nrog CYP450 3A4 enzyme inhibitors (xws li ketoconazole, itraconazole, erythromycin) thiab tsis yog- cov tshuaj inhibitors tshwj xeeb ntawm CYP450 (xws li cimetidine), AUC ntawm sildenafil nce ntxiv thaum qhov kev tshem tawm txo qis. (2) Thaum siv ua ke nrog HIV protease inhibitors xws li saquinavir thiab ritonavir, cmax thiab AUC ntawm sildenafil nce, thaum cov tshuaj pharmacokinetics ntawm saquinavir thiab ritonavir tseem tsis hloov pauv ntawm lub xeev khov kho. (3) Kev siv ua ke nrog lub voj diuretics, potassium sparing diuretics, thiab tsis xaiv beta blockers tuaj yeem nce AUC ntawm cov metabolite ntawm sildenafil (N-demethylsildenafil) los ntawm 62% thiab 102%, raws li, tab sis cov nyhuv no tsis muaj qhov tseem ceeb hauv kev kho mob. (4) Kev tswj hwm nrog cov inducers ntawm CYP4503A4, xws li rifampicin, tuaj yeem txo cov ntshav plasma ntawm sildenafil. (5) Thaum siv ua ke nrog CYP450 2C9 inhibitors xws li tolbutamide thiab warfarin, tsis muaj kev cuam tshuam loj heev. (6) Kev sib xyaw ua ke nrog CYP450 2D6 enzyme inhibitors (xws li xaiv serotonin reuptake inhibitors, tricyclic antidepressants), thiazide tshuaj thiab thiazide diuretics, angiotensin{24}} hloov pauv enzyme inhibitors, calcium channel blockers, thiab lwm yam, tsis muaj kev cuam tshuam rau cov tshuaj pharmacokinetics.
3. Kev lag luam xa tawm: Peb lub tuam txhab tau ua tsis tu ncua optimizing cov khoom lag luam export ntawm sildenafil raw cov ntaub ntawv rau ntau xyoo. Nrog siab - cov khoom zoo thiab cov nqi zoo, peb tau ua tiav xa tawm peb cov khoom mus rau ntau qhov chaw ntawm lub tebchaws. Tau txais kev pabcuam thoob ntiaj teb kev lag luam.
Cov txheej txheem ntau lawm
1. Raw Material Pretreatment: High- purity core raw cov ntaub ntawv tau ua tib zoo xaiv thiab muab tso rau hauv kev tsim khoom tom qab dhau ntau qhov kev ntsuam xyuas (purity Ntau dua lossis sib npaug li 99.5%), tshem tawm impurities thiab teeb meem nyob rau hauv cov ntaub ntawv raw los xyuas kom meej qhov huv ntawm raw cov ntaub ntawv thiab nteg lub hauv paus rau qhov zoo ntawm High Purity Aminotadala Pow.
2. Cov tshuaj tiv thaiv Synthesis: Rau cov neeg mob feem ntau, cov koob tshuaj pom zoo yog 150mg, noj li 1 teev ua ntej kev sib deev; Tab sis nws tuaj yeem noj txhua lub sijhawm hauv 0.5-4 teev ua ntej kev sib deev. Raws li kev ua tau zoo thiab kev kam rau siab, koob tshuaj tuaj yeem nce mus rau 200 milligrams (qhov siab tshaj plaws pom zoo) lossis txo rau 100 milligrams. Nqa nws mus txog ib zaug ib hnub.
Cov hauv qab no cuam tshuam nrog nce qib plasma ntawm sildenafil (AUC): hnub nyoog tshaj 65 xyoo (nce 40%), daim siab puas (xws li cirrhosis, nce 80%), mob raum mob hnyav (creatinine tshem tawm tus nqi.<30ml/min, increased by 100%), concurrent use of potent cytochrome P450 3A4 inhibitors (ketoconazole, itraconazole increased by 200%), erythromycin increased by 182%, and saquinavir increased by 210%. Due to the possibility of increased efficacy and incidence of adverse events in patients with high plasma levels, a starting dose of 25mg is recommended.
3. Hom kev ua: Thaum lub sij hawm kev sib deev stimulation, tsis rau lub raum glandular non cholinergic neurons nyob rau hauv lub corpus cavernosum ntawm noov, nrog rau nitric oxide synthase nyob rau hauv vascular endothelial hlwb, catalyze cov synthesis ntawm nitric oxide los ntawm L-arginine. Lub tom kawg activates guanylate cyclase, ua rau cov synthesis ntawm cyclic guanosine monophosphate, uas nyob rau hauv lem ua rau so ntawm cov nqaij ntshiv ntawm lub corpus cavernosum thiab cov hlab ntsha me, ua rau cov ntshav txhaj rau hauv lub qhov ntswg ntawm qhov chaw mos thiab erection. Lub caij no, cyclic guanosine monophosphate yog hydrolyzed los ntawm phosphodiesterase.
4. Single dose antacids (aluminum hydroxide/magnesium hydroxide) have no effect on the bioavailability of this product; CYP450 2C9 inhibitors (such as tolbutamide, warfarin), CYP450 2D6 inhibitors (such as selective serotonin reuptake inhibitors,>tricyclic antidepressants), thiazide tshuaj thiab thiazide diuretics, angiotensin -hloov enzyme inhibitors, calcium channel blockers, thiab lwm yam, tsis muaj kev cuam tshuam rau cov tshuaj pharmacokinetics ntawm sildenafil.
5. Aseptic Ntim: Sub- ntim yog nqa tawm hauv ib puag ncig aseptic. Kev ntim khoom tsis tu ncua suav nrog 1kg aluminium foil hnab thiab 25kg cardboard nruas (kab nrog ob npaug -cov hnab PE). Me me -loj qauv ntim xws li 10g, 50g thiab 100g tuaj yeem kho raws li cov neeg siv khoom xav tau. Cov khoom npe, CAS naj npawb, purity, batch naj npawb, cia tej yam kev mob thiab lwm yam ntaub ntawv yog kom meej meej cim nyob rau hauv lub ntim, ua raws li thoob ntiaj teb cov qauv kev thauj mus los.
6. Kev Tshawb Fawb Txog Kev Muag Khoom thiab Tawm Tawm: Tom qab ntim khoom, cov khoom raug muab khaws cia rau hauv lub tsev rau khoom tshwj xeeb. Re-kev tshuaj xyuas tau ua dua ua ntej tawm mus kom ntseeg tau tias cov khoom lag luam zoo, ntim khoom thiab cov ntaub ntawv ua raws li tau ua tiav, thiab cov ntaub ntawv tshawb pom thiab cov ntaub ntawv ua raws li suav nrog txhua qhov kev xa khoom los xyuas kom muaj kev txhawj xeeb- pub dawb.
Daim Ntawv Qhia Ua Raws Cai
1: Cov khoom no yog tsim los ntawm sildenafil raw khoom thiab siv rau kev tshawb fawb thiab kev loj hlob. Peb yuav export nws raws li lub teb chaws txoj cai thiab cov kev cai
2. Peb nruj me ntsis ua raws li GMP ntau lawm, thiab tag nrho cov ntaub ntawv raw sildenafil raug kuaj nruj heev. Txhawm rau xyuas kom siab - xa khoom zoo rau koj.
3. Thaum yuav cov khoom no, cov neeg siv khoom yuav tsum muab daim ntawv pov thawj siv raws cai. Peb tsuas yog muab cov neeg siv khoom raws li B2B (cov tuam txhab tshuaj, cov chaw tshawb fawb, thiab lwm yam) thiab nruj me ntsis tshuaj xyuas cov neeg siv khoom tsim nyog kom ntseeg tau tias kev siv khoom raug cai.
