Hydroxypropyl methylcellulose (HPMC)
Pawg: cov ntaub ntawv txheej; Cov ntaub ntawv membrane; Cov ntaub ntawv polymer tswj ceev rau kev npaj qeeb; Tus neeg sawv cev ruaj khov; Kev pab ncua, cov nplaum ntsiav tshuaj; Tus neeg sawv cev nplaum ruaj khov.
1. Kev taw qhia txog khoom
Cov khoom no yog ib qho tsis yog-ionic cellulose ether, pom sab nraud ua hmoov dawb, tsis muaj ntxhiab thiab tsis qab, yaj hauv dej thiab feem ntau cov kuab tshuaj polar organic, o hauv dej txias kom meej lossis me ntsis turbidized colloidal kua. Cov kua dej muaj kev ua haujlwm ntawm qhov chaw, pob tshab siab thiab kev ua haujlwm ruaj khov. HPMC muaj cov khoom zoo li gel kub. Tom qab cua sov, cov khoom kua dej tsim cov dej nag gel, thiab tom qab ntawd yaj tom qab txias. Qhov kub ntawm gel ntawm cov lus qhia sib txawv yog txawv. Kev yaj hloov pauv nrog viscosity, viscosity qis, qhov ntau dua qhov solubility, cov lus qhia sib txawv ntawm HPMC cov khoom muaj qee qhov sib txawv, HPMC yaj hauv dej tsis cuam tshuam los ntawm pH tus nqi.
Qhov kub ntawm kev sib xyaw ua ke, qhov ceev xoob, qhov ceev tiag tiag thiab qhov kub hloov iav yog 360 ℃, 0.341g / cm3, 1.326g / cm3 thiab 170 ~ 180 ℃, raws li. Tom qab cua sov, nws hloov xim av ntawm 190 ~ 200 ° C thiab hlawv ntawm 225 ~ 230 ° C.
HPMC yuav luag tsis yaj hauv chloroform, ethanol (95%), thiab diethyl ether, thiab yaj hauv qhov sib tov ntawm ethanol thiab methylene chloride, qhov sib tov ntawm methanol thiab methylene chloride, thiab qhov sib tov ntawm dej thiab ethanol. Qee qib ntawm HPMC yaj hauv qhov sib tov ntawm acetone, methylene chloride, thiab 2-propanol, nrog rau lwm cov organic solvents.
Rooj 1: Cov cim qhia txog kev siv tshuab
qhov project
Ntsuas,
60 gd (2910).
65GD (2906)
75GD (2208)
Methoxy%
28.0-32.0
27.0-30.0
19.0-24.0
Hydroxypropoxy%
7.0-12.0
4.0-7.5
4.0-12.0
Kub ntawm cov kua nplaum ℃
56-64.
62.0-68.0
70.0-90.0
Qhov viscosity mpa s.
3,5,6,15,50,4000
50400 0
100400 0150 00100 000
Qhov hnyav poob qhuav%
5.0 los yog tsawg dua
Cov seem hlawv %
1.5 los yog tsawg dua
pH
4.0-8.0
Hlau hnyav
20 los yog tsawg dua
tshuaj arsenic
2.0 los yog tsawg dua
2. Cov yam ntxwv ntawm cov khoom
2.1 Hydroxypropyl methylcellulose yaj rau hauv dej txias kom ua tau cov kua nplaum colloidal. Tsuav yog ntxiv rau hauv dej txias thiab do me ntsis, nws tuaj yeem yaj rau hauv cov kua pob tshab. Ntawm qhov tsis sib xws, nws yeej tsis yaj hauv dej kub saum 60 ℃ thiab tsuas yog tuaj yeem o. Thaum npaj cov kua hydroxypropyl methicellulose aqueous, nws yog qhov zoo tshaj plaws los ntxiv ib feem ntawm hydroxypropyl methicellulose rau hauv ib qho dej, do kom zoo, cua sov rau 80 ~ 90 ℃, thiab tom qab ntawd ntxiv cov hydroxypropyl methicellulose seem, thiab thaum kawg siv dej txias los ntxiv rau qhov xav tau.
2.2 Hydroxypropyl methylcellulose yog cov cellulose ether uas tsis yog ionic, nws cov tshuaj tsis muaj ionic them, tsis cuam tshuam nrog cov ntsev hlau lossis cov organic ionic, yog li kom ntseeg tau tias HPMC tsis cuam tshuam nrog lwm cov ntaub ntawv raw thiab cov khoom siv hauv cov txheej txheem ntawm kev npaj ntau lawm.
2.3 Hydroxypropyl methylcellulose muaj zog tiv thaiv kev rhiab heev, thiab nrog rau kev nce qib ntawm qib hloov pauv hauv cov qauv molecular, qhov kev tiv thaiv kev rhiab heev kuj tau txhim kho. Cov tshuaj siv HPMC ua cov khoom siv muaj qhov zoo ruaj khov dua hauv lub sijhawm ua haujlwm dua li cov tshuaj siv lwm cov khoom siv ib txwm muaj (hmoov txhuv nplej siab, dextrin, suab thaj hmoov).
2.4 Hydroxypropyl methylcellulose tsis muaj zog hauv kev zom zaub mov. Ua ib qho tshuaj ntxiv, nws tsis raug zom lossis nqus, yog li nws tsis muab cua sov rau cov tshuaj thiab zaub mov. Nws muaj kev siv tshwj xeeb rau cov nqi calorific qis, tsis muaj ntsev, tsis ua rau ua xua rau cov tshuaj thiab zaub mov rau cov neeg mob ntshav qab zib.
2.5HPMC ruaj khov rau cov kua qaub thiab cov hauv paus, tab sis yog tias pH tshaj 2 ~ 11 thiab cuam tshuam los ntawm qhov kub siab dua lossis lub sijhawm khaws cia ntev dua, nws yuav txo qhov degree ntawm ripening.
2.6 Hydroxypropyl methylcellulose aqueous solution muaj peev xwm ua rau muaj kev ua haujlwm ntawm qhov chaw, qhia txog qhov nruab nrab ntawm qhov chaw thiab qhov sib txuas ntawm qhov chaw. Nws muaj kev sib xyaw ua ke zoo hauv ob-theem system thiab siv tau ua tus stabilizer thiab colloid tiv thaiv zoo.
2.7 Hydroxypropyl methylcellulose aqueous solution muaj cov yam ntxwv zoo heev rau kev tsim cov zaj duab xis, thiab yog cov khoom siv txheej zoo rau cov ntsiav tshuaj thiab tshuaj ntsiav. Lub membrane uas nws tsim yog tsis muaj xim thiab tawv. Yog tias ntxiv glycerol, nws cov plasticity tuaj yeem nce ntxiv. Tom qab kev kho saum npoo, cov khoom raug tawg hauv dej txias, thiab qhov nrawm ntawm kev yaj tuaj yeem tswj tau los ntawm kev hloov pauv pH ib puag ncig. Nws yog siv rau hauv kev npaj qeeb thiab kev npaj enteric-coated.
3. Daim ntawv thov khoom
3.1. Siv ua cov nplaum thiab cov neeg sawv cev uas yaj
HPMC siv los txhawb kev yaj tshuaj thiab qib kev tso tawm, tuaj yeem yaj ncaj qha rau hauv cov kuab tshuaj ua cov nplaum, viscosity qis ntawm HPMC yaj hauv dej kom ua pob tshab rau cov kua nplaum colloid, ntsiav tshuaj, tshuaj ntsiav, granules ntawm cov nplaum thiab tus neeg sawv cev disintegrating, thiab viscosity siab rau kua nplaum, tsuas yog siv vim yog ntau hom thiab ntau yam kev xav tau, feem ntau yog 2% ~ 5%.
HPMC aqueous kua thiab qee qhov concentration ntawm ethanol los ua ib qho composite binder; Piv txwv li: 2% HPMC aqueous kua sib xyaw nrog 55% ethanol kua tau siv rau pelleting ntawm amoxicillin capsules, yog li qhov nruab nrab yaj ntawm amoxicillin capsules nce ntxiv los ntawm 38% mus rau 90% yam tsis muaj HPMC.
HPMC tuaj yeem ua los ntawm cov nplaum sib xyaw nrog cov concentration sib txawv ntawm cov hmoov txhuv nplej siab tom qab yaj; Kev yaj ntawm erythromycin enteric-coated ntsiav tshuaj nce ntxiv los ntawm 38.26% mus rau 97.38% thaum 2% HPMC thiab 8% hmoov txhuv nplej siab tau ua ke.
2.2. Ua cov khoom siv txheej zaj duab xis thiab cov khoom siv tsim zaj duab xis
HPMC ua cov khoom siv txheej txheej uas yaj tau hauv dej muaj cov yam ntxwv hauv qab no: viscosity nruab nrab ntawm cov tshuaj; Cov txheej txheem txheej yog yooj yim; Cov khoom zoo tsim zaj duab xis; Tuaj yeem khaws cov duab ntawm daim, sau ntawv; Tuaj yeem tiv taus dej noo; Tuaj yeem xim, kho qhov saj. Cov khoom no yog siv ua cov txheej txheej zaj duab xis yaj hauv dej rau cov ntsiav tshuaj thiab cov tshuaj uas muaj VISCOSITY qis, thiab rau cov txheej txheej zaj duab xis uas tsis yog dej nrog VISCOSITY siab, tus nqi siv yog 2% -5%.
2.3, ua tus neeg sawv cev thickening thiab colloidal tiv thaiv kua nplaum
HPMC siv ua tus neeg sawv cev tuab yog 0.45% ~ 1.0%, tuaj yeem siv ua cov tshuaj qhov muag thiab cov kua muag dag thickening agent; Siv los ua kom cov kua nplaum hydrophobic ruaj khov, tiv thaiv cov khoom me me coalescence, nag lossis daus, cov tshuaj ib txwm yog 0.5% ~ 1.5%.
2.4, ua ib qho blocker, cov khoom tso tawm qeeb, tus neeg sawv cev tso tawm tswj thiab tus neeg sawv cev pore
Tus qauv HPMC siab viscosity yog siv los npaj cov blockers thiab cov neeg sawv cev tso tawm tswj ntawm cov khoom sib xyaw ua ke pob txha tso tawm cov ntsiav tshuaj thiab cov ntsiav tshuaj hydrophilic gel pob txha tso tawm tswj. Tus qauv qis-viscosity yog tus neeg sawv cev pore-inducing rau cov ntsiav tshuaj tso tawm lossis tswj-tso tawm kom tau txais cov tshuaj kho mob thawj zaug ntawm cov ntsiav tshuaj no sai, ua raws li kev tso tawm lossis tswj-tso tawm kom tswj tau qhov concentration zoo hauv cov ntshav.
2.5. Cov tshuaj gel thiab cov tshuaj suppository matrix
Cov tshuaj hydrogel suppositories thiab cov tshuaj nplaum hauv plab tuaj yeem npaj tau los ntawm kev siv cov yam ntxwv ntawm kev tsim hydrogel uas feem ntau siv los ntawm HPMC hauv dej.
2.6 Cov khoom siv nplaum uas muaj sia nyob
Metronidazole tau sib xyaw nrog HPMC thiab polycarboxylethylene 934 hauv lub tshuab sib tov los ua cov ntsiav tshuaj bioadhesive tswj kev tso tawm uas muaj 250mg. Kev sim yaj hauv vitro qhia tau hais tias cov tshuaj tau o sai sai hauv dej, thiab kev tso tawm tshuaj tau tswj los ntawm kev sib kis thiab kev so ntawm cov saw hlau carbon. Kev siv tsiaj tau qhia tias lub kaw lus tso tawm tshuaj tshiab muaj cov khoom siv tseem ceeb rau kev sib txuas ntawm cov qog nqaij hlav hauv qab ntawm nyuj.
2.7, ua kev pab txhawb nqa
Qhov HIGH viscosity ntawm cov khoom no yog ib qho kev pabcuam zoo rau kev npaj cov kua dej ncua, nws cov koob tshuaj ib txwm yog 0.5% ~ 1.5%.
4. Cov piv txwv ntawm daim ntawv thov
4.1 Cov tshuaj pleev xim zaj duab xis: HPMC 2kg, talc 2kg, roj castor 1000ml, Twain -80 1000ml, propylene glycol 1000ml, 95% ethanol 53000ml, dej 47000ml, xim kom txaus. Muaj ob txoj hauv kev los ua nws.
4.1.1 Kev npaj cov kua pleev xim uas yaj tau: Ntxiv cov HPMC uas tau teev tseg rau hauv 95% ethanol, muab tso rau hauv dej ib hmos, yaj lwm cov xim vector hauv dej (lim yog tias tsim nyog), muab ob qho kev daws teeb meem sib xyaw thiab do kom sib npaug kom ua tau cov kev daws teeb meem pob tshab. Sib tov 80% ntawm cov kev daws teeb meem (20% rau kev txhuam) nrog cov roj castor, Tween-80, thiab propylene glycol uas tau teev tseg.
4.1.2 Kev npaj cov xim tsis yaj (xws li hlau oxide) txheej kua HPMC tau muab tso rau hauv 95% ethanol ib hmos, thiab ntxiv dej kom ua 2% HPMC pob tshab. 20% ntawm cov tshuaj no tau muab coj mus rau kev txhuam, thiab 80% cov tshuaj seem thiab hlau oxide tau npaj los ntawm kev sib tsoo kua, thiab tom qab ntawd ntxiv cov tshuaj ntxiv rau thiab sib tov kom sib npaug rau kev siv. Cov txheej txheem txheej ntawm cov kua txheej: ncuav cov ntawv nplej rau hauv lub lauj kaub txheej qab zib, tom qab tig, cua kub ua ntej rau 45 ℃, koj tuaj yeem tsuag txheej pub, tswj kev ntws hauv 10 ~ 15ml / feeb, tom qab txau, txuas ntxiv kom qhuav nrog cua kub rau 5 ~ 10 feeb tuaj yeem tawm ntawm lub lauj kaub, muab tso rau hauv lub tshuab ziab kom qhuav ntau dua 8 teev.
Daim nyias nyias ntawm 4.2α-interferon qhov muag 50μg ntawm α-interferon tau yaj rau hauv 10ml 0.01ml hydrochloric acid, sib xyaw nrog 90ml ethanol thiab 0.5GHPMC, lim, coated rau ntawm tus pas iav tig, sterilized ntawm 60 ℃ thiab ziab hauv huab cua. Cov khoom no yog ua rau cov khoom siv zaj duab xis.
4.3 Cov ntsiav tshuaj Cotrimoxazole (0.4g ± 0.08g) SMZ (80 mesh) 40kg, hmoov txhuv nplej siab (120 mesh) 8kg, 3% HPMC kua dej 18-20kg, magnesium stearate 0.3kg, TMP (80 mesh) 8kg, txoj kev npaj yog sib tov SMZ thiab TMP, thiab tom qab ntawd ntxiv hmoov txhuv nplej siab thiab sib tov rau 5 feeb. Nrog prefabricated 3% HPMC kua dej, cov khoom mos, nrog 16 mesh screen granulation, ziab, thiab tom qab ntawd nrog 14 mesh screen tag nrho cov nplej, ntxiv magnesium stearate sib tov, nrog 12 hli puag ncig nrog lo lus (SMZco) stamping ntsiav tshuaj. Cov khoom no feem ntau yog siv ua tus binder. Kev yaj ntawm cov ntsiav tshuaj yog 96% / 20 feeb.
4.4 Cov ntsiav tshuaj Piperate (0.25g) piperate 80 mesh 25kg, hmoov txhuv nplej siab (120 mesh) 2.1kg, magnesium stearate kom txaus. Nws txoj kev tsim khoom yog sib tov pipeoperic acid, hmoov txhuv nplej siab, HPMC kom sib npaug, nrog 20% ethanol mos mos, 16 mesh screen granulate, ziab, thiab tom qab ntawd 14 mesh screen tag nrho cov nplej, ntxiv rau vector magnesium stearate, nrog 100mm siv txoj siv sia (PPA0.25) stamping ntsiav tshuaj. Nrog hmoov txhuv nplej siab ua tus neeg sawv cev disintegrating, qhov nrawm ntawm cov ntsiav tshuaj no tsis tsawg dua 80% / 2 feeb, uas siab dua li cov khoom zoo sib xws hauv Nyiv.
4.5 Kua muag cuav HPMC-4000, HPMC-4500 lossis HPMC-5000 0.3g, sodium chloride 0.45g, potassium chloride 0.37g, borax 0.19g, 10% ammonium chlorbenzylammonium kua 0.02ml, dej ntxiv rau 100ml. Nws txoj kev tsim khoom yog HPMC muab tso rau hauv 15ml dej, ntawm 80 ~ 90 ℃ dej puv, ntxiv 35ml dej, thiab tom qab ntawd muaj cov khoom seem ntawm 40ml aqueous kua sib xyaw sib npaug, ntxiv dej kom tag nrho, tom qab ntawd sib xyaw sib npaug, sawv ib hmos, maj mam nchuav lim, lim rau hauv lub thawv kaw, sterilized ntawm 98 ~ 100 ℃ rau 30 feeb, uas yog, Lub pH ntau ntawm 8.4 ° C txog 8.6 ° C. Cov khoom no yog siv rau kev tsis txaus kua muag, yog ib qho kev hloov pauv zoo rau kev kua muag, thaum siv rau lub tshuab microscopy pem hauv ntej, tuaj yeem nce qhov ntau ntawm cov khoom no, 0.7% ~ 1.5% yog qhov tsim nyog.
4.6 Cov ntsiav tshuaj Meththorphan tswj kev tso tawm meththorphan resin ntsev 187.5mg, lactose 40.0mg, PVP70.0mg, vapor silica 10mg, 40.0 mGHPMC-603, 40.0mg ~ microcrystalline cellulose phthalate-102 thiab magnesium stearate 2.5mg. Nws yog npaj ua cov ntsiav tshuaj los ntawm txoj kev ib txwm muaj. Cov khoom no yog siv ua cov khoom tso tawm tswj.
4.7 Rau cov ntsiav tshuaj avantomycin ⅳ, 2149g avantomycin ⅳ monohydrate thiab 1000ml isopropyl dej sib tov ntawm 15% (qhov hnyav concentration) eudragitL-100 (9:1) tau do, sib tov, granulated, thiab ziab ntawm 35 ℃. Cov granules qhuav 575g thiab 62.5g hydroxypropylocellulose E-50 tau sib tov kom huv si, thiab tom qab ntawd 7.5g stearic acid thiab 3.25g magnesium stearate tau ntxiv rau cov ntsiav tshuaj kom tau txais kev tso tawm tas mus li ntawm vanguard mycin ⅳ ntsiav tshuaj. Cov khoom no yog siv ua cov khoom tso tawm qeeb.
4.8 Cov hmoov Nifedipine uas tso tawm tas mus li 1 feem nifedipine, 3 feem hydroxypropyl methyl cellulose thiab 3 feem ethyl cellulose tau sib xyaw nrog cov kuab tshuaj sib xyaw (ethanol: methylene chloride = 1:1), thiab 8 feem hmoov txhuv nplej siab tau ntxiv los tsim cov hmoov los ntawm txoj kev yaj nruab nrab. Qhov kev tso tawm tshuaj ntawm cov hmoov tsis cuam tshuam los ntawm kev hloov pauv ntawm pH ib puag ncig thiab qeeb dua li cov hmoov uas muaj nyob hauv khw. Tom qab 12 teev ntawm kev noj tshuaj, qhov concentration ntawm cov ntshav tib neeg yog 12mg / ml, thiab tsis muaj qhov sib txawv ntawm tus kheej.
4.9 Propranhaol hydrochloride tshuaj ntsiav tso tawm ntev Propranhaol hydrochloride 60kg, microcrystalline cellulose 40kg, ntxiv 50L dej kom ua cov hmoov. HPMC1kg thiab EC 9kg tau sib xyaw rau hauv cov kuab tshuaj sib xyaw (methylene chloride: methanol = 1: 1) 200L los ua cov tshuaj txheej, nrog tus nqi ntws ntawm 750ml / min tsuag rau ntawm cov khoom kheej kheej dov, txheej cov khoom los ntawm qhov loj me ntawm 1.4mm tshuaj ntsuam tag nrho cov khoom, thiab tom qab ntawd sau rau hauv lub tshuaj ntsiav pob zeb nrog lub tshuab ntim tshuaj ntsiav ib txwm muaj. Txhua lub tshuaj ntsiav muaj 160mg ntawm propranolol hydrochloride cov khoom kheej kheej.
4.10 Cov ntsiav tshuaj Naprolol HCL tau npaj los ntawm kev sib tov naprolol HCL: HPMC: CMC-NA ntawm qhov sib piv ntawm 1: 0.25: 2.25. Tus nqi tso tawm tshuaj ze li ntawm xoom hauv 12 teev.
Lwm cov tshuaj kuj tuaj yeem ua los ntawm cov khoom siv pob txha sib xyaw, xws li metoprolol: HPMC: CMC-NA raws li: 1: 1.25: 1.25; Allylprolol: HPMC raws li 1: 2.8: 2.92 piv. Tus nqi tso tawm tshuaj ze rau xoom hauv 12 teev.
4.11 Cov ntsiav tshuaj pob txha uas muaj cov khoom sib xyaw ntawm cov ethylaminosine derivatives tau npaj los ntawm txoj kev ib txwm siv cov hmoov me me silica gel sib xyaw: CMC-NA: HPMC 1: 0.7: 4.4. Cov tshuaj tuaj yeem tso tawm rau 12 teev ob qho tib si hauv vitro thiab hauv vivo, thiab cov qauv tso tawm kab ncaj qha muaj kev sib raug zoo. Cov txiaj ntsig ntawm kev sim ruaj khov raws li FDA cov cai kwv yees tias lub sijhawm khaws cia ntawm cov khoom no yog txog li 2 xyoos.
4.12 HPMC (50mPa·s) (5 qhov), HPMC (4000 mPa·s) (3 qhov) thiab HPC1 tau yaj rau hauv 1000 qhov dej, ntxiv 60 qhov acetaminophen thiab 6 qhov silica gel, do nrog lub tshuab homogenizer, thiab tsuag kom qhuav. Cov khoom no muaj 80% ntawm cov tshuaj tseem ceeb.
4.13 Cov ntsiav tshuaj Theophylline hydrophilic gel pob txha tau suav raws li tag nrho qhov hnyav ntawm cov ntsiav tshuaj, 18% -35% theophylline, 7.5% -22.5% HPMC, 0.5% lactose, thiab cov roj nplua nyeem hydrophobic tsim nyog feem ntau tau npaj rau hauv cov ntsiav tshuaj tso tawm tswj, uas tuaj yeem tswj tau cov ntshav concentration ntawm tib neeg lub cev rau 12 teev tom qab kev noj haus.
Lub sijhawm tshaj tawm: Cuaj hlis-20-2022