Minocycline hydrochloride, tshuaj formula C23H28ClN3O7, CAS 13614-98-7, tshwm li daj crystalline hmoov, tsw ntxhiab, tab sis muaj hygroscopicity. Nws yog soluble hauv dej, tab sis nws solubility tsis siab heev, thiab tuaj yeem piav qhia tias "me ntsis soluble" lossis "me ntsis soluble". Tsis tas li ntawd, nws muaj zoo solubility nyob rau hauv methanol, me ntsis soluble nyob rau hauv ethanol, thiab yuav luag insoluble nyob rau hauv ether. Raws li cov organic compound complex, nws cov qauv molecular muaj ntau pab pawg ua haujlwm thiab cov chaw stereoisomeric. Cov yam ntxwv ntawm cov qauv no tsis tsuas yog txiav txim siab lawv lub cev lub cev, tab sis kuj tseem cuam tshuam nrog lawv cov kev ua haujlwm lom neeg thiab cov tshuaj pharmacological. Cov molar refractive index yog 116.04 thiab molar ntim (cm ³ / mol) yog 294.5, uas qhia txog qhov loj thiab cov duab ntawm nws cov molecules. Nws yog ib qho tshuaj tua kab mob tetracycline nrog dav spectrum thiab muaj zog tiv thaiv kab mob. Feem ntau siv rau hauv kev kho mob yog ntsiav tshuaj, tshuaj ntsiav, thiab tshuaj pleev, uas yog ib tug dav-spectrum tetracycline tshuaj tua kab mob. Los ntawm inhibiting cov kab mob protein synthesis, lawv tuaj yeem tiv thaiv kev kis kab mob thiab tsim nyog rau kev kis kab mob los ntawm cov kab mob xws li Staphylococcus aureus, Streptococcus pneumoniae, Shigella, thiab Escherichia coli. Lawv muaj cov kab mob bactericidal thiab tiv thaiv kab mob ntawm cov kab mob xws li folliculitis, urethritis, thiab bronchitis los ntawm cov kab mob ntsig txog, yog li pab ua kom tiav cov hom phiaj kho mob. Peb cov khoom kuaj yog rau kev tshawb fawb tshawb fawb nkaus xwb.
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Tshuaj Formula |
C23H27N3O7 |
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Exact Mass |
457 |
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Molecular Luj |
457 |
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m/z |
457 (100.0%), 458 (24.9%), 459 (2.7%), 459 (1.4%), 458 (1.1%) |
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Elemental Analysis |
C, 60.39; H, 5.95; N, 9.19; O, 24.48 |
Minocycline hydrochloridebelongs rau chav kawm tetracycline ntawm cov tshuaj tua kab mob, thiab nws cov tshuaj pharmacological feem ntau cuam tshuam nrog kev khi rau A txoj haujlwm ntawm ribosomes, inhibiting peptidyl transferase, thiab yog li cuam tshuam peptide saw elongation. Nyob rau tib lub sijhawm, nws tseem tuaj yeem cuam tshuam RNA synthesis thaum lub sijhawm sau ntawv, thaum kawg ua rau muaj kev cuam tshuam cov protein synthesis thiab ua lub luag haujlwm hauv cov tshuaj tua kab mob thiab cov kab mob bactericidal.
Minocycline tuaj yeem khi rau 50S ribosomal subunit ntawm cov kab mob, tiv thaiv aminoacyl-t-RNA los ntawm kev nkag mus rau 30S subunit. Yog li ntawd, nws tuaj yeem cuam tshuam cov txheej txheem ntawm peptide saw txuas ntxiv thiab cov protein biosynthesis, ua rau codons ntawm mRNA tsis tau txais cov t-RNA nqa cov amino acids, uas ua rau kev tawg ntawm peptide daim ntawv cog lus tshiab thiab kev ua kom tiav, ua tiav lub hom phiaj ntawm kev ua haujlwm ntawm cov kab mob.
Thaum minocycline tsis yog covalently crosslinks nrog 50S subunit ntawm cov kab mob 43S complex, nws cuam tshuam qhov txuas ntawm 70S ribosomal subunit rau tub txib RNA, yog li inhibiting cov txheej txheem txhais lus thiab thaum kawg ua tiav cov tshuaj tua kab mob.
Yog tias tus neeg mob muaj cov kab mob sib kis los ntawm cov kab mob rhiab heev, xws li mob ntsws, mob ntsws thiab lwm yam kab mob, tom qab siv cov tshuaj, cov kab mob pathogenic tuaj yeem nyob hauv lub xeev ntawm hypoxia, yog li ua rau tuag taus, uas tuaj yeem siv los kho cov xwm txheej zoo li no.
Minocycline hydrochloride, raws li ib tug semi synthetic tetracycline broad -spectrum tshuaj tua kab mob, yog dav siv nyob rau hauv kev kho mob ntawm ntau yam kab mob vim nws haib antibacterial thiab anti- inflammatory teebmeem.
Antibacterial nyhuv
Nws muaj cov tshuaj tua kab mob muaj zog ntawm ntau yam kab mob Gram zoo thiab tsis zoo, suav nrog Staphylococcus, Streptococcus, Pneumococcus, Neisseria gonorrhoeae, Shigella, Escherichia coli, Klebsiella, Proteus, Pseudomonas aeruginosa, thiab lwm yam, nws tuaj yeem cuam tshuam kev loj hlob thiab kev loj hlob ntawm cov kab mob xws li kev loj hlob thiab kev loj hlob. chlamydia thiab pallidum. Qhov dav -spectrum antibacterial nyhuv no ua rau nws xaiv thawj zaug rau kev kho mob ntawm ntau yam kab mob sib kis.
Kev kho mob kis kab mob
Cov kab mob ua pa: feem ntau siv los kho cov kab mob ua pa xws li mob ntsws thiab mob ntsws, hawb pob bronchitis, bronchiectasis, bronchopneumonia, kab mob ntsws, thiab lwm yam. Nws cov khoom xyaw nquag tuaj yeem nkag mus rau hauv lub ntsws mucosal cov ntaub so ntswg, tshem tawm cov kab mob hauv lub ntsws, pab cov neeg mob kom rov zoo li qub.
Kab mob urinary tract: Nws muaj cov txiaj ntsig zoo rau cov kab mob urinary xws li urethritis, cystitis, prostatitis, thiab lwm yam. Tom qab nkag mus rau hauv cov zis, cov tshuaj tuaj yeem tshem tawm cov kab mob sai sai, txo qhov kev pheej hmoo ntawm kev rov tshwm sim, thiab txhim kho cov tsos mob ntawm cov zis.
Cov kab mob ntawm daim tawv nqaij thiab cov nqaij mos: zoo heev hauv kev kho cov kab mob ntawm daim tawv nqaij xws li pob txuv, folliculitis, pyoderma, boils, thiab abscesses. Nws cov tshuaj tiv thaiv -inflammatory thiab tshuaj tua kab mob tuaj yeem txhim kho daim tawv nqaij o, liab, o, thiab pustules, txo qhov kev pheej hmoo ntawm pob txuv, thiab txhim kho daim tawv nqaij noj qab haus huv.
Lwm yam kab mob: Nws kuj siv tau los kho sepsis, bacteremia, osteomyelitis, peritonitis, cholangitis, cholecystitis thiab lwm yam kab mob sib kis.
Tiv thaiv kom tsis txhob kis kab mob
Minocycline hydrochloride tuaj yeem siv los tiv thaiv thaum phais lossis siab - cov xwm txheej txaus ntshai los txo kev pheej hmoo kis mob. Los ntawm inhibiting cov kab mob proliferation, ua kom muaj kev nyab xeeb ntawm cov chaw phais mob thiab cov kab mob, thiab txo cov kab mob tom qab phais.
Qhov ntom ntawmminocycline hydrochloride
1. Cov ntaub ntawv nyiaj txiag loj
Qhov ntom yog qhov piv ntawm qhov loj ntawm ib yam khoom rau nws lub ntim, thiab yog ib qho tseem ceeb ntawm lub cev ntawm cov khoom. Rau cov khoom siv tshuaj xws li minocycline hydrochlorid, qhov ntom ntom tsis tsuas yog cuam tshuam rau lawv qhov chaw cia thiab kev thauj mus los yooj yim, tab sis kuj tseem cuam tshuam nrog kev solubility, kev ruaj ntseg, thiab kev npaj cov tshuaj.
2. Kev kwv yees ceev ntawm minocycline hydrochlorid
Tetracycline tshuaj tua kab mob feem ntau muaj qhov hnyav molecular (xws li minocycline hydrochlorid nrog qhov hnyav molecular ntawm 493.937), thiab lawv cov qauv molecular yog complex, muaj ntau yam qauv cyclic thiab pab pawg ua haujlwm. Cov yam ntxwv no ua rau muaj qhov ntom ntom ntawm cov tshuaj tiv thaiv tetracycline. Yog li, nws tuaj yeem ua pov thawj tias qhov ntom ntawm minocycline hydrochlorid yuav tsum ntau dua li cov dej (1g / cm³), tab sis tus nqi tshwj xeeb yuav tsum tau txiav txim siab sim.
3. Qhov cuam tshuam ntawm qhov ntom ntom ntawm kev siv tshuaj
Qhov ntom ntawm minocycline hydrochlorid tuaj yeem cuam tshuam rau nws cov dispersibility thiab stability hauv formulations. Piv txwv li, nyob rau hauv kev npaj ntawm cov khoom formulations, cov tshuaj hais nrog ntau dua ntom yuav nyuaj rau uniformly disperse nyob rau hauv excipients; Nyob rau hauv cov kua formulations, qhov sib txawv ceev yuav ua rau delamination ntawm cov tshuaj thiab cov kuab tshuaj. Tsis tas li ntawd, qhov ceev kuj tseem cuam tshuam rau compressibility thiab flowability ntawm cov tshuaj, yog li cuam tshuam rau cov txheej txheem kev npaj thiab cov khoom zoo ntawm formulations.
viscosity ntawm minocycline hydrochlorid
1. Kev txhais thiab qhov tseem ceeb ntawm viscosity
Viscosity yog ib qho kev ntsuas ntawm kev sib txhuam hauv lub zog thaum lub sij hawm ua kua thiab yog ib qho tseem ceeb ntawm lub cev ntawm cov kua. Rau minocycline hydrochlorid, txawm hais tias nws daim ntawv tseem ceeb yog cov hmoov hmoov, nws cov viscosity hauv dej los yog cov kuab tshuaj organic yuav yog ib qho tseem ceeb rau kev txiav txim siab thaum npaj cov kua tshuaj xws li txhaj tshuaj, tshuaj hauv qhov ncauj, thiab lwm yam.
2. Speculation ntawm viscosity ntawm minocycline hydrochlorid tov
Vim qhov tseeb tias minocycline hydrochlorid yog cov hmoov hmoov, nws cov viscosity nws tus kheej tsis haum. Txawm li cas los xij, tom qab kev npaj rau hauv kev daws, nws cov viscosity yuav raug cuam tshuam los ntawm ntau yam xws li hnyav hom, concentration, kub, thiab tshuaj molecule kev sib cuam tshuam.
Feem ntau hais lus, tetracycline tshuaj tua kab mob tsis muaj cov dej solubility hauv dej, yog li cov viscosity ntawm lawv cov tshuaj aqueous tej zaum yuav tsawg. Tab sis nyob rau hauv high concentrations los yog thaum tov nrog lwm cov kuab tshuaj, viscosity ntawm cov tshuaj yuav nce. Tsis tas li ntawd, qhov kub thiab txias kuj tseem muaj feem cuam tshuam rau viscosity ntawm cov tshuaj, feem ntau yuav txo qis thaum qhov kub thiab txias nce.
3. Kev cuam tshuam ntawm viscosity ntawm kev siv tshuaj
Lub viscosity ntawm cov tshuaj minocycline hydrochlorid muaj qhov cuam tshuam loj rau nws cov kev tswj hwm, kev nqus tshuaj, thiab kev faib tawm hauv kev siv tshuaj kho mob. Piv txwv li, thaum npaj cov tshuaj txhaj tshuaj, cov viscosity siab yuav ua rau muaj teeb meem hauv kev txhaj tshuaj lossis tsis sib xws ntawm cov tshuaj; Thaum npaj cov kev daws qhov ncauj, viscosity tuaj yeem cuam tshuam qhov saj thiab kev lees paub ntawm cov neeg mob. Yog li ntawd, thaum npaj cov kua formulations, nws yog ib qho tsim nyog yuav tsum tau ua tib zoo xav txog cov solubility, viscosity, thiab cov kev xav tau tiag tiag ntawm tus neeg mob los txiav txim siab qhov zoo tshaj plaws formulation thiab txheej txheem txheej txheem.
Raws li tetracycline tshuaj tua kab mob, qhov nro ntawm qhov chaw thiab polarizability nyob rau hauv lub cev muaj zog ntawmminocycline hydrochlorideyog ib qho tseem ceeb tsis muaj kev cuam tshuam txog nws cov kev sib cuam tshuam intermolecular thiab cov khoom nto.
Ntog nro
1. Kev txhais thiab qhov tseem ceeb
Nto nro yog qhov macroscopic manifestation ntawm intermolecular kev sib cuam tshuam nyob rau hauv lub nto txheej ntawm cov kua, uas ua rau cov kua nto muaj ib tug nyiam cog lus zoo li ib tug elastic zaj duab xis. Rau cov khoom siv hmoov xws li minocycline hydrochlorid, lawv qhov nro saum npoo yog feem ntau cuam tshuam los ntawm kev ntsuas lawv cov dispersibility hauv dej lossis lwm cov kuab tshuaj. Qhov loj ntawm qhov nro saum npoo yog cuam tshuam nrog cov khoom xws li cov khoom, qhov kub thiab txias, hom hnyav, thiab concentration.
2. Nto nro ntawm minocycline hydrochlorid
Metric Roller Chain Sprocket tuaj yeem siv tau rau hauv yuav luag txhua hom kab ke. Siv rau hauv cov tshuab conveyor xws li conveyors, nws tuaj yeem thauj khoom noj, dej haus, nplej, thiab lwm yam khoom siv los ntawm ib qho chaw mus rau lwm qhov. Siv nyob rau hauv kev sib kis kab mob, nws hloov lub zog los ntawm ib qho chaw xws li lub cav mus rau ntau yam khoom xws li lub log. Yog li, cov khoom lag luam kuj tau siv dav hauv kev lag luam xws li kev tsim tshuab, khoom siv ua liaj ua teb, tsheb, thiab khoom siv tub rog.
3. Kev cuam tshuam ntawm qhov nro
Qhov nro ntawm minocycline hydrochlorid muaj qhov cuam tshuam loj rau nws cov dispersibility, solubility, tshuaj stability, thiab bioavailability hauv formulations. Thaum npaj cov formulations, tshuaj hmoov uas muaj zog saum npoo tej zaum yuav nyuaj rau uniformly disperse nyob rau hauv excipients; Nyob rau hauv cov kua formulations, deg nro tej zaum yuav cuam tshuam tus nqi dissolution thiab℃ntawm cov tshuaj. Tsis tas li ntawd, qhov nro saum npoo kuj tuaj yeem cuam tshuam cov ntub dej thiab nthuav tawm cov khoom ntawm cov tshuaj, yog li cuam tshuam rau lawv qhov nqus thiab kev faib tawm.
Polarization tus nqi
1. Kev txhais thiab qhov tseem ceeb
Polarization tus nqi yog lub cev kom muaj nuj nqis uas piav qhia txog kev faib cov nqi hauv ib lub molecule, xav txog qhov yooj yim ntawm polarization ntawm cov molecule nyob rau hauv qhov kev txiav txim ntawm ib qho hluav taws xob teb. Qhov siab dua qhov polarization tus nqi, qhov ntau dua qhov molecule yuav dhau mus polarization, uas yog, cov nqi xa tawm hauv cov molecule yog qhov cuam tshuam rau cov hluav taws xob sab nraud. Rau cov organic tebchaw xws li minocycline hydrochlorid, lawv cov polarizability muaj feem xyuam rau yam xws li cov qauv molecular, polarity ntawm chemical bonds, thiab kev sib cuam tshuam ntawm intermolecular.
2. Polarity ntawm minocycline hydrochlorid
Raws li cov ntaub ntawv, qhov polarizability ntawm minocycline hydrochlorid yog 46.00 (lub tsev yuav yog 10 ^ -24 cm ³, tab sis cov chav tsev tshwj xeeb yuav txawv nyob ntawm cov ntaub ntawv sib txawv). Tus nqi no qhia tau hais tias tus nqi xa tawm hauv minocycline hydrochlorid molecule yog cov concentrated, thiab muaj kev sib cuam tshuam sib cuam tshuam. Qhov no ua rau minocycline hydrochlorid ua rau polarization nyob rau hauv qhov kev txiav txim ntawm hluav taws xob teb, uas tej zaum yuav cuam tshuam rau nws lub cev thiab tshuaj.
3. Kev cuam tshuam ntawm polarization tus nqi
Lub polarizability ntawm minocycline hydrochloride muaj qhov cuam tshuam loj rau nws tus cwj pwm hauv thaj chaw hluav taws xob, kev cuam tshuam nrog lwm cov molecules, thiab kev ua haujlwm lom neeg ntawm cov tshuaj. Cov molecules nrog polarizability ntau dua yog qhov yooj yim rau kev taw qhia thiab kev tsiv teb tsaws chaw hauv hluav taws xob, uas cuam tshuam rau kev solubility, permeability, thiab nqus cov tshuaj. Tsis tas li ntawd, polarization kuj tseem cuam tshuam rau kev sib cuam tshuam hom thiab lub zog ntawm cov tshuaj thiab lwm yam molecules hauv lub cev, yog li cuam tshuam rau lawv cov txiaj ntsig thiab kev phiv.
Kev Tshawb Fawb
Qhov kev tshawb pom ntawm qhov sib xyaw no tuaj yeem taug qab rov qab mus rau xyoo 1960, thaum cov kws tshawb fawb tau mob siab rau tsim cov tshuaj tua kab mob tetracycline tshiab los daws qhov teeb meem loj zuj zus ntawm cov kab mob ua haujlwm.
Hauv cov ntsiab lus no, minocycline tau ua tiav zoo rau hauv ib qho khoom siv hluav taws xob tetracycline derivative. Nws cov qauv tshuaj tau raug hloov kho raws li tetracycline, ntxiv ob pawg methyl thiab ib pawg dimethylamino. Cov qauv kev hloov pauv no ua rau muaj txiaj ntsig zoo rau nws cov tshuaj tua kab mob thiab cov tshuaj pharmacokinetic. Cov txheej txheem synthesis ntawm minocycline yog complex thiab meej.
Ua ntej, pib los ntawm tetracycline, methyl thiab dimethylamine pawg tau qhia los ntawm cov tshuaj tiv thaiv kab mob. Cov txheej txheem no tsis tsuas yog txhim kho cov lipid solubility ntawm cov tshuaj, tab sis kuj txhim kho nws cov permeability hauv lub cev, ua rau nws qhov kev faib tawm ntau dua hauv lub cev.
Tsis tas li ntawd, cov kev hloov kho cov qauv no kuj txhim kho cov nyhuv inhibitory ntawm minocycline ntawm qee yam tshuaj -cov kab mob resistant. Cov kev tshawb fawb hauv chav sim ua ntej tau pom tias minocycline nthuav dav dav -spectrum antibacterial kev ua haujlwm tawm tsam ntau yam kab mob Gram zoo, kab mob Gram tsis zoo, thiab cov kab mob atypical xws li mycoplasma, chlamydia, thiab rickettsia, thiab muaj kev cuam tshuam loj.
Nws cov qauv tshuaj tshwj xeeb ua rau nws khi zoo dua rau cov kab mob ribosomes, inhibit protein synthesis, thiab yog li siv cov tshuaj tua kab mob. Nrog rau kev ua tiav ntawm kev tshawb fawb hauv chav kuaj, minocycline tau nkag mus rau theem kev sim tshuaj.
Hauv ntau qhov kev sim tshuaj, minocycline tau pom tias muaj kev nyab xeeb thiab ua tau zoo, tshwj xeeb tshaj yog nyob rau hauv kev kho pob txuv, kab mob ua pa, thiab kab mob urinary.
Nws ntev - ua haujlwm tau zoo thiab tsis tshua muaj tshwm sim ntawm cov kev mob tshwm sim ua rau nws nyiam heev hauv kev siv tshuaj kho mob. Cov txheej txheem tshawb pom tsis yog tsuas yog ua kom pom qhov zoo tshaj plaws ntawm cov kws tshawb fawb hauv kev tshawb fawb tshuaj tua kab mob thiab kev txhim kho, tab sis kuj muab cov cuab yeej muaj zog rau cov tshuaj niaj hnub no, txhim kho kev kho mob ntawm cov kab mob kis tau zoo.
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