Procaine hydrochloride CAS:tuaj yeem siv los ua cov khoom siv raw, cov khoom siv tshuaj lom neeg hauv chav kuaj. nws yog ib qho ntsev uas ruaj khov, feem ntau yog cov hmoov dawb crystalline hmoov lossis tsis muaj xim pob tshab. Nws cov xim feem ntau cuam tshuam los ntawm cov tshuaj purity thiab ntau lawm txheej txheem. Lub solubility hauv dej yog heev. Nws tseem tuaj yeem yaj lossis tawg hauv qee cov kuab tshuaj organic, xws li ethanol, ether, chloroform, thiab benzene. Lub melting point yog 154-158 degree . Qhov chaw melting no tuaj yeem siv los ua ib qho ntawm cov qauv rau kev kuaj xyuas nws qhov zoo. Nws yog ib qho tshuaj loog ruaj khov. Nws tuaj yeem ruaj khov ntawm chav tsev kub. Nws tuaj yeem tiv taus oxidation hauv huab cua thiab tsis cuam tshuam los ntawm lub teeb.
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Tshuaj Formula |
C13H21ClN2O2 |
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Exact Mass |
272.13 |
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Molecular Luj |
272.77 |
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m/z |
272.13 (100.0%), 274.13 (32.0%), 273.13 (14.1%), 275.13 (4.5%) |
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Elemental Analysis |
C, 57,24; H, 7,76; Cl, 13. 00; N, 10.27; 11.73 Nws |
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Nws yog ib qho tshuaj loog hauv zos thiab tseem siv los ua cov tshuaj tom khw muag khoom los txo qhov mob me, xws li mob hniav. Nws yog dav siv nyob rau hauv kev kho mob kev lag luam vim hais tias nws yog ib qho kev nyab xeeb thiab zoo tshuaj loog hauv zos. Ntawm no peb yuav tham txog ntau txoj hauv kev los ua ke nws.
1. Cov tshuaj tiv thaiv ntawm Para aminobenzoic acid (PABA) thiab diethylamine ether
Txoj kev npaj ntxov tshaj plaws ntawm cov khoom yog los teb PABA thiab diethylamine los ua procaine nyob rau hauv alkaline tej yam kev mob. Txoj kev no tau tshawb pom los ntawm Ernest Fourneau thiab Pierre Refrain hauv 1905.
Ua ntej, PABA yog acidified nrog concentrated sulfuric acid los tsim cov amide sib raug, thiab tom qab ntawd nws reacts nrog ethylenediamine nyob rau hauv qhov kev txiav txim ntawm sodium hydroxide los ua ib tug procaine puag. Thaum kawg, lub hauv paus procaine yog neutralized nrog hydrochloric acid tov kom tau cov khoom.
2. Cov tshuaj tiv thaiv ntawm Procainamide thiab PABA
Procainamide yog ib qho tshuaj psychotropic siab heev tau txais los ntawm sulfonation cov tshuaj tiv thaiv ntawm procaine. Yog li, procaine reacts nrog p-Toluenesulfonic acid thiab H2SO4 los tsim procaine mide methylated ntawm txoj hauj lwm 14, thiab reacts nrog PABA los tsim HCL ntsev.
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Pure API (Active pharmaceutical ingredient) rau kev tshawb fawb txog kev tshawb fawb nkaus xwb, Cov khoom siv rau kev tsom xam, kev kawm Pharmacokinetic, receptor resistance test thiab lwm yam.Procaine hydrochloride, dawb crystalline lossis crystalline hmoov yog tshuaj loog hauv zos nrog cov nyhuv muaj zog tab sis tsis muaj tshuaj lom thiab siv sijhawm luv luv. Clinical xyaum mas sivprocaine hcl, procaine hcl hmoovrau infiltration anesthesia thiab conduction anesthesia. Vim nws qhov kev nkag mus tsis zoo, nws feem ntau tsis siv rau qhov tshuaj loog.
Chemical Properties:
(a) Kev ruaj ntseg:
Nws tuaj yeem ruaj khov ntawm chav tsev kub thiab siab. Txawm li cas los xij, nws yuav hloov xim, decompose, thiab poob nws cov yam ntxwv hauv tshav ntuj thiab huab cua.
(b) Solubility:
Nws yog yooj yim soluble nyob rau hauv dej thiab muaj tsis tshua muaj volatility. Nws kuj tseem tuaj yeem soluble hauv qee cov kuab tshuaj organic xws li methanol thiab ethanol. Thaum lub solubility yog 25 degree, muaj 8.8g ntawm cov khoom nyob rau hauv txhua txhua 100ml dej.
(c) PH tus nqi:
Cov tshuaj aqueous ntawm nws yog tsis muaj zog acidic, nrog tus nqi pH ntawm kwv yees li 3.0-5 0.
(d) Oxidation-txo cov khoom:
Nws tshwm xiav nyob rau hauv lub xub ntiag ntawm cations xws li Fe3+thiab Cu2+. Nws tuaj yeem raug oxidized los ntawm reagents xws li HI, HNO3, FeCl3 trachoma reagent, Molisch reagent, thiab lwm yam., thiab rhuab nyob rau hauv alkaline tej yam kev mob los tsim ib tug liab doog.
(e) Dilution:
Lub dilution ntawm cov khoom tov maj mam nce, tab sis nws tsis tuaj yeem decompose.
(f) Alkalinity:
Nws tsis muaj zog acidic thiab tuaj yeem decompose rau hauv hydrogen ions thiab ruaj khov hydrochloric acid molecules nrog sib npaug moles.
(g) Instability:
Nws muaj cov kev cai nruj rau kev ruaj ntseg. Nws yuav tsum tau muab khaws cia rau hauv qhov chaw kaw, noo noo-pov thawj, thiab lub teeb pov thawj, thiab tsis txhob sib cuag nrog cov kuab tshuaj alkaline, hlau ions, thiab oxidants.
tshuaj xyuas
Acidity:
Noj {{0}}.40g ntawm cov khoom no, dissolve nws nyob rau hauv 10mL dej, thiab ntxiv 1 tee ntawm methyl liab qhia daws teeb meem. Yog tias nws hloov xim liab, ntxiv 0.20mL ntawm sodium hydroxide titrant (0.02mol / L), thiab cov kab mob yuav tig txiv kab ntxwv.
Clarity ntawm kev daws:
Noj 2.0g ntawm cov khoom no thiab yaj hauv 10mL dej. Txoj kev daws yuav tsum tau meej.
Aminobenzoic acid:
txiav txim siab los ntawm kev ua haujlwm siab ua kua chromatography (General Rule 0512).
Kev daws teeb meem:
Noj cov khoom no, ntsuas nws kom raug, yaj hauv dej, thiab dilute nws kom muaj nuj nqis los npaj cov tshuaj uas muaj 0.2mg ib 1mL.
Kev daws teeb meem:
Noj ib qho tsim nyog tus nqi ntawm para aminobenzoic acid siv tshuaj, ntsuas kom raug, yaj nws hauv dej thiab dilute nws kom muaj nuj nqis los npaj cov tshuaj uas muaj kwv yees li 1 µ g ib 1mL.
System suitability daws:
Siv 1mL ntawm cov tshuaj ntsuam xyuas thiab 9mL ntawm cov tshuaj siv, sib tov zoo.
Txoj kev ntsuas:
Precisely ntsuas cov tshuaj ntsuam xyuas thiab tswj cov tshuaj, txhaj rau hauv cov kua chromatograph cais, thiab sau cov chromatogram.
Qhuav yuag poob:
Nqa cov khoom no thiab ziab nws ntawm 105 ° C mus rau qhov hnyav tas li, nrog qhov hnyav tsis ntau tshaj 0.5% (Txoj Cai 0831).
Hlawv residue:
Noj 1.0g ntawm cov khoom no thiab xyuas raws li txoj cai (Txoj cai dav dav 0841). Qhov seem seem yuav tsum tsis pub tshaj 0.1%.
Txwv:
Yog hais tias muaj chromatographic peaks nyob rau hauv lub chromatogram ntawm cov tshuaj ntsuam xyuas uas muaj tib lub sij hawm tuav raws li lub ncov ntawm para aminobenzoic acid, lub ncov cheeb tsam yuav tsum tsis txhob ntau tshaj 0.5%, xam raws li cov txheej txheem sab nraud.
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Convallis posuere morbi urna molestie elementum pulvinar odio etiam.
Kev xa khoom thoob ntiaj teb
Urna condimentum mattis pellentesque nibh. Integer vitae justo eget magna
Chromatographic tej yam kev mob:
Octadecylsilane bonded silica gel tau siv los ua tus muab tub lim, thiab ib qho {{{0}}}. (68:32) tau siv los ua lub sijhawm txawb. Kev kuaj pom wavelength yog 279nm, thiab qhov ntim ntim yog 10 µ L.
Qhov system haum yuav tsum muaj:
Nyob rau hauv chromatogram ntawm lub system haum rau kev daws teeb meem, lub theoretical phaj tooj xam raws li lub ncov ntawm para aminobenzoic acid yuav tsum tsis txhob tsawg tshaj li 2000, thiab qhov sib cais degree ntawm procaine ncov thiab lub para aminobenzoic acid ncov yuav tsum. yuav ntau dua 2.0.
Hlau ntsev:
Siv cov seem seem nyob rau hauv lub ignition residue, ntxiv 2mL ntawm hydrochloric acid, evaporate nws nyob rau hauv ib da dej, ntxiv 4mL ntawm dilute hydrochloric acid, yaj nyob rau hauv ib tug tsawg kub, ntxiv 30mL dej thiab 5{{ 7}}mg ntawm ammonium persulfate, thiab xyuas raws li txoj cai dav dav 0807. Piv nrog rau kev tswj cov tshuaj ua los ntawm 1.0mL ntawm tus qauv hlau tov, nws yuav tsum tsis txhob tob (0.001%).
Procaine hydrochloridebelongs rau ester tshuaj loog hauv zos, uas muaj tshuaj loog hauv zos, tiv thaiv kab mob, tiv thaiv rheumatic, vasodilator, tiv thaiv arrhythmic thiab lwm yam teebmeem. Nws yog tsuas yog siv nyob rau hauv kev kho mob xyaum rau infiltration tshuaj loog, thaiv anesthesia, lumbar spine anesthesia, thiab lwm yam.
Raws li ester tshuaj loog hauv zos, nws muaj qhov pib sai thiab zoo tshuaj loog, thiab muaj kev cuam tshuam rau cov paj hlwb hauv ntau qhov chaw. Yog li ntawd, nws yog feem ntau siv nyob rau hauv kev kho mob xyaum rau lub zos infiltration tshuaj loog, conduction anesthesia, spinal anesthesia, thiab lwm yam.
Raws li ester tshuaj loog hauv zos, nws muaj kev tiv thaiv kab mob thiab tuaj yeem thaiv cov tshuaj loog. Nws yog feem ntau siv kho mob los txo cov tsos mob xws li mob hniav, mob taub hau, neuralgia, thiab mob pob qij txha.
Nws kuj muaj cov tshuaj tiv thaiv rheumatic, uas tuaj yeem cuam tshuam cov kab mob inflammatory hauv tus neeg mob lub cev, yog li txo cov tsos mob xws li mob pob qij txha thiab o los ntawm kev mob caj dab rheumatoid.
Nws tuaj yeem ua ncaj qha rau cov leeg nqaij leeg, nthuav cov hlab ntsha, ua kom cov ntshav khiav, txhim kho microcirculation, thiab feem ntau yog siv rau hauv kev kho mob kiv taub hau thiab mob taub hau tshwm sim los ntawm ischemic cerebrovascular kab mob, peripheral vascular kab mob, thiab lwm yam.
Nws kuj muaj cov tshuaj tiv thaiv arrhythmic, uas tuaj yeem cuam tshuam lub hauv nruab nrab lub paj hlwb thiab txo cov tsos mob xws li palpitations, hauv siab nruj, thiab kiv taub hau los ntawm arrhythmia.
Nws yuav tsum tau muab sau tseg tias cov tshuaj saum toj no yuav tsum tau siv raws li kev qhia ntawm tus kws kho mob thiab yuav tsum tsis txhob siv qhov muag tsis pom kev kom tsis txhob muaj kev phiv thiab kev puas tsuaj rau lub cev. Tsis tas li ntawd, nws yuav tsum tau contraindicated rau cov neeg mob uas muaj tshuaj loog hauv zos ua xua, siab thiab raum tsis ua haujlwm, thiab lwm yam.
Procaine hydrochloride, raws li ib tug classic tshuaj loog hauv zos, muaj ib tug complex thiab meej mechanism ntawm kev txiav txim uas muaj ntau yam physiological systems thiab molecular kev sib tshuam.
Raws li ester tshuaj loog hauv zos, nws cov tshuaj loog hauv zos yog ua tiav los ntawm kev thaiv cov hlab ntsha ntawm cov hlab ntsha. Lub mechanism tshwj xeeb yog raws li nram no:
(1) Neuronal membrane nkag mus: Procaine molecules cia siab rau cov concentration gradients kom diffuse los ntawm neuronal membrane, uas yog thawj kauj ruam hauv lawv cov tshuaj loog.
(2) Sodium ion channel blockade: Tom qab nkag mus rau cov paj hlwb, procaine xaiv khi rau sodium ion raws ntawm cov cell membrane, tiv thaiv sodium ion influx. Sodium ions yog cov ions tseem ceeb rau tiam neeg thiab kev nthuav tawm ntawm kev ua haujlwm muaj peev xwm hauv cov paj hlwb, thiab lawv cov dej ntws sab hauv raug cuam tshuam, ua rau muaj kev nce ntxiv hauv qhov pib ntawm cov paj hlwb thiab poob ntawm excitability thiab conductivity.
(3) Cov ntaub ntawv kis tau tus mob thaiv: Raws li tiam thiab kev nthuav tawm ntawm cov hlab ntsha impulses cia siab rau cov transmembrane ntws ntawm sodium ions, procaine zoo thaiv cov hlab ntsha impulses los ntawm thaiv cov sodium ion channel, ua tiav cov tshuaj loog hauv zos.
Central paj hlwb cuam tshuam
Qhov cuam tshuam ntawm lub hauv nruab nrab lub paj hlwb yog ze ze rau kev noj tshuaj, tshwj xeeb tshaj yog tshwm sim:
(1) Inhibition effect: Nyob rau hauv cov koob tshuaj, procaine feem ntau exerts inhibitory cuam tshuam rau hauv nruab nrab paj hlwb. Cov neeg mob tuaj yeem ua rau muaj kev ntxhov siab, qhov mob hnyav, thiab txawm tias coma lossis coma. Cov nyhuv inhibitory no pab txo cov neeg mob kev ntxhov siab thiab mob, thiab txhim kho kev nplij siab ntawm kev phais lossis kev kho mob.
(2) Cov nyhuv Excitatory: Nrog rau kev siv tshuaj ntau ntxiv, cov nyhuv inhibitory ntawm procaine ntawm lub hauv nruab nrab lub paj hlwb yuav maj mam txo qis, thiab txawm hloov mus rau hauv cov nyhuv excitatory. Cov neeg mob yuav muaj kev ntxhov siab, mania, thiab thaum mob hnyav, yuav ua rau muaj kev phiv xws li qaug dab peg. Yog li ntawd, thaum siv procaine, cov koob tshuaj yuav tsum tau tswj nruj me ntsis kom tsis txhob siv ntau dhau.
Qhov cuam tshuam ntawm cov hlab plawv kuj tseem cuam tshuam nrog kev siv tshuaj, tshwj xeeb tshaj yog tshwm sim:
(1) Kev hloov hauv lub plawv dhia thiab ntshav siab: tuaj yeem ua rau lub paj hlwb muaj zog, ua rau lub plawv dhia thiab ntshav siab. Txawm li cas los xij, raws li kev noj tshuaj ntau ntxiv, nws tuaj yeem inhibit peripheral vascular dilation, ua rau txo qis ntshav siab. Txoj kev sib raug zoo ntawm koob tshuaj no xav kom cov kws kho mob saib xyuas cov neeg mob lub plawv dhia thiab ntshav siab hloov thaum siv procaine.
(2) Antiarrhythmic nyhuv: Nws kuj muaj cov nyhuv antiarrhythmic. Nws tuaj yeem txo qhov tshwm sim ntawm arrhythmia los ntawm kev thaiv kev sib kis ntawm paj hlwb impulses thiab inhibiting lub excitability ntawm myocardial hlwb. Txawm li cas los xij, txoj haujlwm no yuav tsum tau siv kom tsim nyog raws li kev qhia ntawm tus kws kho mob kom tsis txhob muaj qhov tshwm sim tsis zoo.
Neuromuscular blockade nyhuv
Kev sib tw inhibition ntawm acetylcholine receptors ntawm lub cev muaj zog endplate membrane ua rau tsis muaj txiaj ntsig ntawm cov hlab ntsha impulses mus rau cov leeg hlwb, ua rau muaj kev cuam tshuam neuromuscular. Cov nyhuv no pab txo cov leeg nro thiab mob thaum lub sijhawm phais, thiab txhim kho qhov smoothness ntawm cov txheej txheem phais. Txawm li cas los xij, nws yuav tsum tau muab sau tseg tias qhov cuam tshuam neuromuscular thaiv ntawm procaine tuaj yeem ua rau muaj kev cuam tshuam tsis zoo xws li cov leeg tsis muaj zog lossis tuag tes tuag taw hauv cov neeg mob, yog li nws yuav tsum tau saib xyuas cov kev hloov pauv hauv cov leeg nqaij thaum siv.
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