Shaanxi BLOOM Tech Co., Ltd. yog ib qho ntawm cov tuam ntxhab thiab cov muag khoom ntawm terbinafine hydrochloride ntsiav tshuaj hauv Suav teb. Txais tos rau cov lag luam wholesale bulk zoo terbinafine hydrochloride ntsiav tshuaj muag ntawm no los ntawm peb lub hoobkas. Kev pabcuam zoo thiab tus nqi tsim nyog muaj.
Terbinafine hydrochloride ntsiav tshuajyog ib qho tshuaj tiv thaiv kab mob hauv qhov ncauj uas poob rau hauv chav kawm allylamine ntawm cov tshuaj sib txuas. Nws ua haujlwm los ntawm kev xaiv inhibiting fungal enzyme squalene epoxidase, uas nyob rau hauv lem halts lub biosynthesis ntawm ergosterol-ib qho tseem ceeb ntawm cov fungal cell membrane- thiab ua rau intracellular buildup ntawm squalene. Qhov no ob lub tswv yim cuam tshuam cov txheej txheem kev ncaj ncees ntawm cov kab mob fungal cell membrane, ua rau ob qho tib si fungicidal thiab fungistatic ua tawm tsam ntau yam ntawm cov kab mob fungal. Feem ntau qhia rau kev tswj cov kab mob cuam tshuam rau ntawm daim tawv nqaij, plaub hau, thiab rau tes, terbinafine hydrochloride ntsiav tshuaj muaj txiaj ntsig zoo tiv thaiv dermatophytes suav nrog Trichophyton rubrum, Trichophyton mentagrophytes, Microsporum canis, thiab Epidermophyton floccosum. Rau onychomycosis, feem ntau hu ua fungal ntsia thawv kab mob cuam tshuam rau ob tus ntiv tes thiab cov ntiv tes, cov txheej txheem kev kho mob ntev li ntawm 6 lub lis piam mus rau 3 lub hlis, nrog rau cov mob hnyav dua uas yuav tsum tau ncua sijhawm ntev txog 6 lub hlis. Nyob rau hauv cov ntaub ntawv ntawm cov kab mob fungal ntawm daim tawv nqaij xws li tinea corporis (ringworm), tinea cruris (jock khaus), tinea pedis (tus neeg ncaws pob ko taw), thiab tinea capitis (scalp ringworm), lub sij hawm kho mob yog nyob nruab nrab ntawm 2 mus rau 6 lub lis piam. Rau cov kab mob candidiasis tshwm sim los ntawm Candida albicans, qhov kev pom zoo ntawm kev kho mob feem ntau yog 2 mus rau 4 lub lis piam.
Formulation specifications
Cov khoom lag luam uas muaj nyob hauv cov khoom lag luam muaj tus qauv koob tshuaj ntawm 250 mg / thooj, thiab cov ntaub ntawv ntim ntau suav nrog:
Lub raj mis: 30 daim / lub raj mis, 100 daim / lub raj mis, 500 ntsiav tshuaj / lub raj mis, 1000 daim / lub raj mis;
Bubble wrap packaging: 30 pieces/box (packaged in aluminium-plastic npuas qhwv).
Cov tsos ntawm daim yog dawb mus rau lub teeb daj ncig ob lub convex zaj duab xis coated daim, thiab qee cov khoom muaj cov cim luam tawm ntawm qhov chaw (xws li "LAMISIL 250" lossis "IG 209"). Cov khoom siv xws li colloidal silica, hydroxypropyl methylcellulose, magnesium stearate, thiab lwm yam yog feem ntau ntxiv rau cov formulations los txhim kho cov tshuaj stability thiab compressibility. Cov pab pawg allylamine hauv nws cov qauv tshuaj yog ib pawg ua haujlwm tseem ceeb uas inhibits fungal enzyme kev ua haujlwm.
Cov ntaub ntawv ntxiv ntawm chemical compound:
Peb cov khoom tsim
terbinafine hydrochloride +. COA
Terbinafine hydrochloride ntsiav tshuajyog ib qho dav -spectrum antifungal tshuaj uas inhibits cov enzymes tseem ceeb koom nrog hauv fungal cell lining biosynthesis, thaiv ergosterol synthesis thiab inducing squalene tsub zuj zuj, thaum kawg ua rau fungal cell tuag. Nws cov txheej txheem ntawm kev txiav txim siab muaj kev xaiv siab, muaj kev puas tsuaj rau ob qho tib si, thiab ua kom tsis muaj zog, ua rau nws yog cov tshuaj tseem ceeb rau kev kho mob ntawm daim tawv nqaij, plaub hau, thiab tus ntsia thawv fungus. Cov hauv qab no piav qhia txog nws cov txheej txheem ntawm kev ua haujlwm los ntawm cov yam ntxwv ntawm cov hom phiaj molecular, kev cuam tshuam metabolic, tshuaj tua kab mob, thiab cov yam ntxwv ntawm pharmacokinetic.
1. Tshuaj hauv paus ntawm enzyme inhibition
Cov qauv molecular ntawm terbinafine hydrochloride muaj ib pawg allylamine, uas covalently khi rau qhov chaw nquag ntawm fungal squalene epoxidase los ua ib qho irreversible enzyme inhibitor complex. Kev sim tau pom tias nws qhov inhibition tas li (Ki tus nqi) rau cov enzymes tsawg li 30 nM, qhia tias nws muaj kev sib raug zoo heev. Nyob rau hauv sib piv, muaj qhov sib txawv nyob rau hauv lub active centre qauv ntawm homologous enzymes nyob rau hauv tib neeg lub hlwb, uas ua rau lub rhiab heev ntawm terbiafine rau tib neeg lub hlwb tsuas yog ib kaum txhiab ntawm cov fungi, yog li ua kom muaj kev ruaj ntseg ntawm remey.
2. Kev ua rau lom neeg ntawm enzyme inhibition
Squalene cyclooxygenase yog ib qho tseem ceeb ntawm kev txwv enzyme nyob rau hauv txoj kev biosynthesis ntawm ergosterol, lub luag hauj lwm rau catalyzing hloov dua siab tshiab ntawm squalene rau 2,3-oxidosqualene. Cov kauj ruam no yog qhov pib cov tshuaj tiv thaiv rau kev sib txuas ntawm ergosterol, uas yog lub ntsiab lus tseem ceeb ntawm cov kab mob hu ua fungal cell linings thiab tseem ceeb heev rau kev tswj cov txheej txheem kev ncaj ncees thiab fluidity. Terbiafine cuam tshuam ncaj qha rau kev sib txuas ntawm ergosterol los ntawm kev thaiv cov haujlwm ntawm cov enzyme, thaum ua rau muaj kev sib txuam loj ntawm squalene hauv cov kab mob fungal.
1. Toxic los ntawm squalene tsub zuj zuj
Qhov txawv txav ntawm squalene nyob rau hauv cov hlwb muaj dual toxicity:
Kev puas tsuaj rau lub cev: Squalene yog ib qho tsis yog -polar molecule, thiab nws cov khoom sib xyaw ntau dhau tuaj yeem ua rau cov lipid bilayer qauv ntawm cov cell hauv ob sab phlu, ua rau muaj kev hloov pauv hauv cov ntaub ntawv fluidity thiab tsis ua haujlwm.
Oxidative stress: Squalene tuaj yeem catalyzed los ntawm intracellular oxidases los tsim reactive oxygen hom (ROS), ua rau lipid peroxidation thiab protein oxidation, thaum kawg ua rau cell tuag. Qhov kev sim tau lees paub tias tom qab remey nrog terbiafine, intracellular ROS theem ntawm Candida albicans hlwb tau nce thiab muaj kev cuam tshuam zoo nrog cov tshuaj concentration.
2. Kev puas tsuaj ncaj qha los ntawm ergosterol tsis txaus
Qhov tsis txaus ntawm ergosterol ua rau muaj qhov txawv txav ntawm cov kab mob hauv cov kab mob fungal, tshwm sim raws li kev nce hauv cov kab mob permeability, ion to, thiab outflow ntawm cellular ntsiab lus. Electron microscopy soj ntsuam pom tias lub cell hauv ob sab phlu ntawm Trichophyton rubrum kho nrog terbiafine wrinkled thiab ruptured, thaum kawg ua rau cell lysis. Tsis tas li ntawd, ergosterol deficiency tuaj yeem cuam tshuam nrog kev ua haujlwm ntawm cov kab mob hauv cov kab mob xws li ATPase thiab cov neeg thauj khoom, ua rau cov metabolism tsis muaj zog ntxiv ntawm cov kab mob fungal.
1. Muaj zog bactericidal nyhuv ntawm dermatophytes
Terbinafine muaj cov kab mob bactericidal sai tawm tsam dermatophytes xws li Trichophyton rubrum, Trichophyton rubrum, thiab Microsporidia canis. Kev sim hauv vitro tau pom tias nws qhov tsawg kawg nkaus inhibitory concentration (MIC) yog 0.001-0.01 μ g / mL, thiab cov kab mob bactericidal cuam tshuam nrog cov tshuaj concentration. Hauv kev tshawb fawb soj ntsuam, kev kho tus nqi ntawm terbiafine hauv kev kho mob onychomycosis yog 80% -95%, zoo dua li azole tshuaj tiv thaiv kab mob xws li itraconazole thiab fluconazole.
2. Dual teebmeem ntawm cov tshuaj tua kab mob thiab cov kab mob bactericidal ntawm cov poov xab
Candida albicans: Terbinafine nthuav tawm cov tshuaj tiv thaiv kab mob los yog cov kab mob bactericidal rau nws.
Tsawg concentrations (0.1-1 μ g / mL) inhibit hyphal tsim thiab kev loj hlob, thaum siab concentrations (Ntau tshaj los yog sib npaug rau 10 μ g / mL) ncaj qha tua cov poov xab theem hlwb.
Lwm hom kab mob poov xab: Rau hom tsis Candida xws li Candida parapsilosis thiab Candida tropicalis, MIC ntau ntawm terbiafine yog 0.125-2 μ g / mL, thiab nws cov txiaj ntsig zoo piv rau fluconazole.
3. Kev ua haujlwm tawm tsam qee yam pwm
MIC ntawm terbiafine tawm tsam Aspergillus hom (xws li Aspergillus niger thiab Aspergillus flavus) yog 0.5-4 μ g / mL, uas tsis muaj zog dua li amphotericin B tab sis zoo dua li cov tshuaj azole. Ntxiv rau,terbinafine hydrochloride ntsiav tshuajkuj nthuav tawm qee yam kev ua ub no tawm tsam biphasic fungi xws li Blastomyces dermatidis thiab Histoplasma capsule.
1. Kev nqus thiab kev faib tawm
Kev nqus ntawm qhov ncauj: Lub bioavailability yog 70% -90%, tab sis vim yog thawj zaug dhau los, qhov tseeb bioavailability yog li 40% -50%.
Peak lub sij hawm: Tom qab ib zaug noj ntawm qhov ncauj ntawm 250 mg, lub ncov plasma concentration (Cmax) yog 0.7-1.0 μ g / mL, thiab lub sij hawm ncov (Tmax) yog 1.5-2 teev.
2.Kev nkag mus rau hauv lub cev: Qhov concentration ntawm cov tshuaj nyob rau hauv daim tawv nqaij, plaub hau, thiab daim tawv nqaij yog ntau dua li nyob rau hauv plasma, thiab lawv ib nrab - lub neej nyob rau hauv lub stratum corneum yog mus txog 100 teev, uas yuav kav ntev li ob peb lub hlis nyob rau hauv daim tawv nqaij. Qhov no yog lub hauv paus rau lawv lub sijhawm ntev - kev kho mob ntev hauv kev kho onychomycosis.
3. Metabolism thiab excretion
Txoj kev metabolic: Feem ntau metabolized los ntawm daim siab CYP2D6 enzyme, tsim cov metabolites tsis ua haujlwm.
4.Excretion method: Kwv yees li 70% yog tawm hauv daim ntawv ntawm cov metabolites los ntawm cov kua tsib, thiab tsuas yog me me (<0.03%) is excreted in the urine as the prototype drug.
Ib nrab ntawm lub neej: Lub plasma tshem tawm ib nrab-lub neej (T1/2) yog 16-19 teev, tab sis cov ntaub so ntswg ib nrab-lub neej tau ntev heev.
5. pharmacokinetics ntawm cov neeg tshwj xeeb
Lub siab ua haujlwm tsis zoo: Metabolism qeeb qeeb, kev hloov kho ntau npaum lossis txwv tsis pub yuav tsum tau ua.
Lub raum tsis txaus: Raws li nws feem ntau yog tawm los ntawm cov kua tsib, tsis tas yuav kho qhov ntau npaum li cas, tab sis cov neeg mob lub raum tsis ua haujlwm hnyav yuav tsum siv ceev faj.
Cov menyuam yaus: Rau cov uas hnyav dua 40 kg, qhov koob tshuaj yuav tsum tau hloov mus rau 0.625 mg / kg.
- Absorption thiab kev faib tawm
Qhov ncauj bioavailability: 70% -90%, zaub mov tsis muaj txiaj ntsig zoo rau nws qhov nqus;
Lub sijhawm ua haujlwm siab: 1.5-2 teev;
Protein binding rate:>99%, feem ntau khi rau plasma proteins;
Lub koom haum permeability: tuaj yeem nthuav dav hauv stratum corneum, ntsia thawv matrix, thiab cov hauv paus plaub hau, nrog rau kev khaws cia hauv lub lawj ntev txog 6 lub hlis.
- Metabolism thiab excretion
Metabolic txoj kev: Daim siab CYP450 enzyme system (tsuas yog CYP2C9, CYP1A2, CYP3A4);
- Metabolites: demethylated terbinafine (kev ua haujlwm tsuas yog 10% ntawm cov tshuaj qub);
- Excretion method: tso zis:<0.3% prototype drug;Fecal: The main excretion pathway, containing the prototype drug and metabolites.
- pharmacokinetics ntawm cov neeg tshwj xeeb
- Lub siab ua haujlwm tsis zoo: AUC ntawm cov neeg mob uas muaj qhov kawg- kab mob siab siab nce li ntawm 2 zaug, thiab cov tshuaj yuav tsum tau hloov kho;
- Lub raum tsis txaus: Tsis tas yuav kho qhov ntau npaum li cas, vim tias cov tshuaj thiab cov tshuaj metabolites tsuas yog tawm los ntawm cov kua tsib.
Daim Ntawv Qhia Kev Siv, Kev Siv thiab Kev Ua Haujlwm
1. Txuj koob tshuaj tiv thaiv kab mob
Hom kab mob, ntau npaum li cas, remey chav kawm, ceev faj
Cov kab mob fungal ntawm cov ntiv taw: 250 mg / hnub, noj qhov ncauj rau 12 lub lis piam, nrog rau cov tshuaj pleev kom tshem tawm cov kab mob seem
Nail fungus 250 mg / hnub, noj qhov ncauj rau 6 lub lis piam. Tom qab qhov kawg ntawm qhov remey, kev soj ntsuam tas li rau 3 lub hlis yog xav tau
Tinea corporis / tinea crus 250 mg / hnub, noj qhov ncauj rau 1-2 lub lis piam. Tom qab daim tawv nqaij lesions ploj lawm, consolidation remey yuav tsum tau 3 hnub
Tinea pedis 250 mg / hnub, noj qhov ncauj rau 2-4 lub lis piam, scaly keratinization hom yuav tsum tau ncua mus rau 6 lub lis piam.
Tinea versicolor 250 mg / hnub, noj qhov ncauj rau 2 lub lis piam, yuav tsum tau siv cov khoom siv da dej antifungal
2. Cov qauv kev ua haujlwm
(1) Txoj kev tswj hwm
Noj qhov ncauj: tag nrho tabella nqos tau, tuaj yeem noj nrog zaub mov kom txo tau qhov mob plab;
Crush noj ntawm qhov ncauj: Rau cov tsiaj uas nqos tsis tau tag nrho tabella, tabella tuaj yeem raug crushed thiab tov rau hauv zaub mov.
(2) Cia tej yam kev mob
Kub: 20-25℃(chav kub), khaws cia deb ntawm lub teeb;
Humidity: txheeb ze cov av noo tsawg dua los yog sib npaug li 60%, zam cov kab mob los ntawm absorbing noo noo thiab clumping;
Ntim: Lub raj mis thawj yuav tsum muab kaw thiab khaws cia, thiab siv li ntawm 6 lub hlis tom qab qhib.
(3) Kev pov tseg pov tseg
Cov tshuaj tas sij hawm: cais thiab rov ua dua raws li kev kho mob pov tseg, txwv tsis pub muab pov tseg ntawm qhov xav tau;
Lub raj mis khoob: Tom qab ntxuav, nws yuav tsum muab pov tseg raws li cov khib nyiab tsis tu ncua.
Cim npe nrov: terbinafine hydrochloride ntsiav tshuaj, lwm tus neeg, manufacturers, hoobkas, lag luam wholesale, yuav, nqe, tej, kev muag khoom