Hydroxypropyl methylcellulose (HPMC)
Qeb: cov ntaub ntawv txheej; Membrane khoom; Ceev-tswj cov ntaub ntawv polymer rau kev npaj qeeb-tso; Stabilizing tus neeg sawv cev; Kev pab cuam ncua kev kawm ntawv, ntsiav tshuaj nplaum; Reinforced adhesion tus neeg sawv cev.
1. Khoom taw qhia
Cov khoom no yog ib qho uas tsis yog-IONIC CELLULOSE ETHER, sab nraud pom raws li cov hmoov dawb, tsis muaj ntxhiab thiab tsis qab, soluble hauv dej thiab feem ntau cov polar organic solvents, o hauv dej txias kom tshem tawm los yog me ntsis turBIdized colloidal tov. Cov tshuaj aqueous muaj cov dej num saum npoo av, siab pob tshab thiab kev ua haujlwm ruaj khov. HPMC muaj cov khoom ntawm cov gel kub. Tom qab cua sov, cov khoom aqueous tov ua gel nag lossis daus, thiab tom qab ntawd yaj tom qab txias. Lub gel kub ntawm txawv specifications txawv. Solubility hloov nrog viscosity, viscosity zhao qis, ntau dua solubility, txawv specifications ntawm HPMC cov khoom muaj qee qhov sib txawv, HPMC yaj hauv dej tsis cuam tshuam los ntawm pH tus nqi.
Qhov kub ntawm qhov kub thiab txias, qhov ntom ntom ntom ntom ntom ntom ntom thiab iav hloov pauv kub yog 360 ℃, 0.341g / cm3, 1.326g / cm3 thiab 170 ~ 180 ℃, feem. Tom qab cua sov, nws tig xim av ntawm 190 ~ 200 ° C thiab kub ntawm 225 ~ 230 ° C.
HPMC yuav luag insoluble nyob rau hauv chloroform, ethanol (95%), thiab diethyl ether, thiab yaj nyob rau hauv ib tug sib tov ntawm ethanol thiab methylene chloride, ib tug sib tov ntawm methanol thiab methylene chloride, thiab ib tug sib tov ntawm dej thiab ethanol. Qee qib ntawm HPMC yog soluble hauv cov khoom sib xyaw ntawm acetone, methylene chloride, thiab 2-propanol, nrog rau lwm cov kuab tshuaj organic.
Table 1: Technical indicators, As
qhov project
Ntsuas,
60 gd (2910).
65 TSI (2906)
75 TSI (2208)
Methoxy%
28.0-32.0 Nws
27.0-30.0 Nws
19.0-24.0 Nws
Hydroxypropoxy%
7.0-12.0 Nws
4.0-7.5
4.0-12.0 Nws
Gel kub ℃
56-64 : kuv.
62.0-68.0 Nws
70.0-90.0 Nws
Viscosity mpa s.
3, 5, 6, 15, 50, 4000
5 04000
100400 0150 00100 000
Qhuav yuag poob%
5.0 los yog tsawg dua
Hlawv residue%
1.5 los yog tsawg dua
pH
4.0-8.0 Nws
Hnyav hlau
20 los yog tsawg dua
arsenic
2.0 los yog tsawg dua
2. Khoom nta
2.1 Hydroxypropyl methylcellulose yog yaj nyob rau hauv dej txias los tsim ib tug viscous colloidal kua. Tsuav nws ntxiv rau dej txias thiab me ntsis nplawm, nws tuaj yeem yaj mus rau hauv cov kua dej pob tshab. Ntawm qhov tsis sib xws, nws yog qhov yooj yim insoluble hauv dej kub siab tshaj 60 ℃ thiab tuaj yeem o tuaj. Hauv kev npaj ntawm hydroxypropyl methicellulose aqueous tov, nws yog qhov zoo tshaj rau ntxiv ib feem ntawm hydroxypropyl methicellulose nyob rau hauv ib tug npaum li cas ntawm cov dej, do vigorously, rhuab mus rau 80 ~ 90 ℃, thiab ces ntxiv cov hydroxypropyl methicellulose ntxiv, thiab thaum kawg siv dej txias ntxiv rau qhov yuav tsum tau muaj.
2.2 Hydroxypropyl methylcellulose yog non-ionic cellulose ether, nws cov tshuaj tsis muaj ionic nqi, tsis cuam tshuam nrog hlau ntsev los yog ionic organic tebchaw, thiaj li yuav xyuas kom meej tias HPMC tsis hnov mob nrog lwm yam raw khoom thiab excipients nyob rau hauv cov txheej txheem ntawm kev npaj ntau lawm.
2.3 Hydroxypropyl methylcellulose muaj zog los tiv thaiv rhiab heev, thiab nrog kev nce qib ntawm kev hloov pauv hauv cov qauv molecular, kev tiv thaiv rhiab heev kuj tseem txhim kho. Cov tshuaj siv HPMC raws li cov khoom siv ntxiv muaj qhov ruaj khov zoo nyob rau lub sijhawm siv tau zoo dua li cov tshuaj siv lwm cov tshuaj ntxiv (cov hmoov txhuv nplej siab, dextrin, hmoov qab zib).
2.4 Hydroxypropyl methylcellulose yog metabolically inert. Raws li ib tug kws tshuaj excipient, nws tsis yog metabolized los yog absorbed, yog li nws tsis muab cua sov nyob rau hauv cov tshuaj thiab zaub mov. Nws muaj qhov tshwj xeeb siv tau rau tus nqi qis calorific, tsis muaj ntsev, tsis muaj tshuaj tsis haum thiab khoom noj rau cov ntshav qab zib.
2.5HPMC yog qhov ruaj khov rau cov kua qaub thiab cov hauv paus, tab sis yog tias pH siab tshaj 2 ~ 11 thiab cuam tshuam los ntawm qhov kub thiab txias dua los yog lub sij hawm cia ntev dua, nws yuav txo qhov degree ntawm ripenness.
2.6 Hydroxypropyl methylcellulose aqueous tov tuaj yeem muab kev ua haujlwm saum npoo, uas qhia qhov nruab nrab ntawm qhov chaw thiab qhov cuam tshuam ntawm qhov nro. Nws muaj emulsification zoo nyob rau hauv ob-theem system thiab yuav siv tau raws li ib tug zoo stabilizer thiab tiv thaiv colloid.
2.7 Hydroxypropyl methylcellulose aqueous kua muaj cov yeeb yaj kiab zoo heev, thiab yog cov khoom siv zoo rau cov ntsiav tshuaj thiab tshuaj. Lub membrane tsim los ntawm nws yog xim tsis muaj xim thiab tawv. Yog tias glycerol ntxiv, nws cov yas tuaj yeem nce ntxiv. Tom qab kev kho saum npoo, cov khoom yog dispersed nyob rau hauv dej txias, thiab tus nqi dissolution yuav tswj tau los ntawm kev hloov pH ib puag ncig. Nws yog siv nyob rau hauv qeeb-tso npaj thiab enteric-coated npaj.
3. Daim ntawv thov khoom
3.1. Siv ua nplaum thiab disintegrating tus neeg sawv cev
HPMC yog siv los txhawb cov tshuaj dissolution thiab qib ntawm kev tso tawm daim ntawv thov, tuaj yeem yaj ncaj qha rau hauv cov kuab tshuaj raws li cov nplaum, tsis tshua muaj viscosity ntawm HPMC yaj hauv dej los ua pob tshab rau cov kua nplaum nplaum nplaum nplaum, ntsiav tshuaj, ntsiav tshuaj, granules ntawm cov nplaum thiab cov khoom tawg, thiab cov viscosity siab rau cov kua nplaum 2% sib txawv, tsuas yog siv cov khoom sib txawv. 5%.
HPMC aqueous tov thiab ib co concentration ntawm ethanol los ua ib tug composite binder; Piv txwv li: 2% HPMC aqueous tov tov nrog 55% ethanol tov yog siv rau pelleting ntawm amoxicillin capsules, kom qhov nruab nrab dissolution ntawm amoxicillin capsules nce los ntawm 38% mus rau 90% tsis muaj HPMC.
HPMC tuaj yeem ua los ntawm cov nplaum nplaum sib txawv nrog qhov sib txawv ntawm cov hmoov txhuv nplej siab slurry tom qab dissolution; Kev sib cais ntawm erythromycin enteric-coated ntsiav tshuaj tau nce los ntawm 38.26% mus rau 97.38% thaum 2% HPMC thiab 8% hmoov txhuv nplej siab tau ua ke.
2.2. Ua zaj duab xis txheej khoom thiab zaj duab xis tsim cov khoom
HPMC raws li cov khoom siv dej-soluble txheej muaj cov yam ntxwv hauv qab no: nruab nrab cov tshuaj viscosity; txheej txheej txheej yog yooj yim; Zoo zaj duab xis tsim cov cuab yeej; tuaj yeem khaws cov duab ntawm daim, sau ntawv; tuaj yeem ua kom tsis muaj dej; Tau xim, kho tsw. Cov khoom no yog siv los ua cov dej-soluble zaj duab xis txheej rau cov ntsiav tshuaj thiab cov ntsiav tshuaj uas tsis tshua muaj viscosity, thiab rau cov ntaub ntawv uas tsis yog-dej-raws li cov ntaub ntawv uas muaj viscosity siab, cov nyiaj siv yog 2% -5%.
2.3, raws li tus neeg sawv cev thickening thiab colloidal tiv thaiv kua nplaum
HPMC siv los ua tus neeg sawv cev thickening yog 0.45% ~ 1.0%, tuaj yeem siv los ua cov tshuaj pleev qhov muag thiab cov khoom tsim kua muag thickening; Siv los ua kom muaj kev ruaj ntseg ntawm cov kua nplaum hydrophobic, tiv thaiv particle coalescence, nag lossis daus, qhov ntau npaum li cas yog 0.5% ~ 1.5%.
2.4, raws li ib tug blocker, qeeb tso khoom, tswj tso tawm tus neeg saib xyuas thiab pore tus neeg sawv cev
HPMC high viscosity qauv yog siv los npaj cov blockers thiab tswj kev tso tawm cov neeg sawv cev ntawm cov khoom sib xyaw pob txha uas txhawb nqa cov ntsiav tshuaj thiab hydrophilic gel skeleton sustained tso cov ntsiav tshuaj. Cov qauv uas tsis muaj viscosity yog cov pore-inducing tus neeg sawv cev rau kev tso tawm-tso tawm lossis tswj-tso cov ntsiav tshuaj kom cov tshuaj thawj zaug ntawm cov ntsiav tshuaj tau txais sai sai, ua raws li kev tso tawm los yog tswj-tso kom tswj tau cov ntshav siab zoo.
2.5. Gel thiab suppository matrix
Hydrogel suppositories thiab gastric adhesive npaj tuaj yeem npaj tau los ntawm kev siv cov yam ntxwv ntawm hydrogel tsim feem ntau siv los ntawm HPMC hauv dej.
2.6 Biological adhesive cov ntaub ntawv
Metronidazole tau tov nrog HPMC thiab polycarboxylethylene 934 nyob rau hauv ib lub tov khoom los ua bioadhesive tswj cov ntsiav tshuaj uas muaj 250mg. Nyob rau hauv vitro dissolution kuaj pom tau hais tias qhov kev npaj sai sai swelled nyob rau hauv dej, thiab cov tshuaj tso tawm yog tswj los ntawm diffusion thiab carbon saw so. Kev siv tsiaj txhu pom tau tias cov tshuaj tso tawm tshiab muaj qhov ua kom muaj roj ntsha tseem ceeb rau bovine sublingual mucosa.
2.7, raws li kev pab cuam ncua
Lub HIGH viscosity ntawm cov khoom no yog ib qho kev pab cuam zoo rau kev tshem tawm cov kua tshuaj, nws cov koob tshuaj ib txwm yog 0.5% ~ 1.5%.
4. Daim ntawv thov piv txwv
4.1 Zaj duab xis txheej: HPMC 2kg, talc 2kg, castor roj 1000ml, Twain -80 1000ml, propylene glycol 1000ml, 95% ethanol 53000ml, dej 47000ml, xim tsim nyog. Muaj ob txoj hauv kev los ua nws.
4.1.1 Kev npaj cov kua dej uas muaj kuab lom cov xim coated: Ntxiv cov nqi ntawm HPMC rau hauv 95% ethanol, tsau rau ib hmos, yaj lwm cov xim xim hauv dej ( lim yog tias tsim nyog), muab ob txoj kev daws teeb meem thiab sib tov sib npaug los tsim cov tshuaj pob tshab. Sib tov 80% ntawm cov tshuaj (20% rau polishing) nrog tus nqi ntawm cov roj castor, Tween-80, thiab propylene glycol.
4.1.2 Kev npaj cov xim tsis muaj kuab lom (xws li hlau oxide) txheej ua kua HPMC tau tsau rau hauv 95% ethanol thaum hmo ntuj, thiab dej ntxiv los ua 2% HPMC pob tshab kua. 20% ntawm cov tshuaj no tau muab tshem tawm rau polishing, thiab 80% cov tshuaj ntxiv thiab hlau oxide tau npaj los ntawm kev sib tsoo ua kua, thiab tom qab ntawd cov tshuaj noj ntawm lwm cov khoom tau ntxiv thiab sib tov sib npaug rau kev siv. Cov txheej txheem txheej txheej ntawm cov kua txheej txheej: ncuav cov ntawv nplej rau hauv lub lauj kaub qab zib, tom qab kev sib hloov, cua kub preheats rau 45 ℃, koj tuaj yeem txau cov txheej txheej, ntws tswj hauv 10 ~ 15ml / min, tom qab txau, txuas ntxiv ziab nrog cua kub rau 5 ~ 10min tuaj yeem tawm ntawm lub lauj kaub, muab tso rau hauv lub tshuab ziab kom qhuav rau ntau tshaj 8 feeb.
4.2α-interferon qhov muag daim nyias nyias 50μg ntawm α-interferon yog yaj nyob rau hauv 10ml0.01ml hydrochloric acid, tov nrog 90ml ethanol thiab 0.5GHPMC, lim, coated rau ib tug rotating iav pas nrig, sterilized ntawm 60 ℃ thiab qhuav hauv huab cua. Cov khoom no yog ua los ntawm cov khoom siv ua yeeb yaj kiab.
4.3 Cotrimoxazole ntsiav tshuaj (0.4g ± 0.08g) SMZ (80 mesh) 40kg, hmoov txhuv nplej siab (120 mesh) 8kg, 3%HPMC aqueous tov 18-20kg, magnesium stearate 0.3kg, TMP (80 mesh) 8kg, cov txheej txheem npaj 5 TMP thiab mix. Nrog prefabricated 3%HPMC aqueous tov, cov khoom muag muag, nrog 16 mesh screen granulation, ziab, thiab tom qab ntawd nrog 14 mesh screen tag nrho cov nplej, ntxiv magnesium stearate mix, nrog 12 hli puag ncig nrog lo lus (SMZco) stamping ntsiav tshuaj. Cov khoom no tsuas yog siv los ua ib daim ntawv khi. Kev sib cais ntawm cov ntsiav tshuaj yog 96% / 20min.
4.4 Piperate ntsiav tshuaj (0.25g) piperate 80 mesh 25kg, starch (120 mesh) 2.1kg, magnesium stearate tsim nyog tus nqi. Nws txoj kev tsim khoom yog sib tov pipeoperic acid, hmoov txhuv nplej siab, HPMC tusyees, nrog 20% ethanol mos cov ntaub ntawv, 16 mesh screen granulate, qhuav, thiab ces 14 mesh screen tag nrho cov nplej, ntxiv rau vector magnesium stearate, nrog 100mm voj siv lo lus (PPA0.25) stamping ntsiav tshuaj. Nrog cov hmoov txhuv nplej siab ua tus neeg sawv cev disintegrating, qhov kev sib cais ntawm cov ntsiav tshuaj no tsis tsawg dua 80% / 2min, uas yog siab dua cov khoom zoo sib xws hauv Nyiv.
4.5 Artificial tear HPMC-4000, HPMC-4500 los yog HPMC-5000 0.3g, sodium chloride 0.45g, potassium chloride 0.37g, borax 0.19g, 10% ammonium chlorbenzylammonium daws 0.02ml, dej ntxiv rau 10ml. Nws txoj kev tsim khoom yog HPMC muab tso rau hauv 15ml dej, ntawm 80 ~ 90 ℃ tag nrho cov dej noj, ntxiv 35ml dej, thiab tom qab ntawd ntxiv cov khoom seem ntawm 40ml aqueous tov sib xyaw, ntxiv dej rau tag nrho cov nyiaj, ces sib tov sib npaug, sawv ntsug ib hmos, maj mam ncuav pom, lim rau hauv lub thawv kaw, sterilized ntawm 10 ℃ 10 8 ℃. Qhov kub ntawm 8.4 ° C mus rau 8.6 ° C. Cov khoom no yog siv rau cov kua muag tsis zoo, yog ib qho khoom siv zoo rau kev tsim kua muag, thaum siv ANTERIOR chamber microscopy, tuaj yeem tsim nyog QHOV TSEEB NTAWM 10.7%.
4.6 Methorphan tswj cov ntsiav tshuaj Methorphan resin ntsev 187.5mg, lactose 40.0mg, PVP70.0mg, vapor silica 10mg, 40.0 mGHPMC-603, 40.0mg ~ microcrystalline cellulose phthalate-102 mg. Nws yog npaj raws li cov ntsiav tshuaj los ntawm txoj kev ib txwm. Cov khoom no yog siv los tswj cov khoom tso tawm.
4.7 Rau avantomycin ⅳ ntsiav tshuaj, 2149g avantomycin ⅳ monohydrate thiab 1000ml isopropyl dej sib tov ntawm 15% (qhov loj ntawm concentration) eudragitL-100 (9: 1) tau nplawm, sib tov, granulated, thiab qhuav ntawm 35 ℃. Cov granules qhuav 575g thiab 62.5g hydroxypropylocellulose E-50 tau sib xyaw kom zoo, 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 li ntawm vanguard mycin ⅳ ntsiav tshuaj. Cov khoom no yog siv los ua cov khoom tso tawm qeeb.
4.8 Nifedipine sustained-tso granules 1 feem nifedipine, 3 qhov chaw hydroxypropyl methyl cellulose thiab 3 qhov chaw ethyl cellulose tau tov nrog tov hnyav (ethanol: methylene chloride = 1: 1), thiab 8 qhov chaw pob kws hmoov txhuv nplej siab tau ntxiv los tsim granules los ntawm txoj kev nruab nrab-soluble. Cov tshuaj tso tawm tus nqi ntawm cov granules tsis cuam tshuam los ntawm kev hloov pauv ntawm ib puag ncig pH thiab qeeb dua li cov khoom lag luam muag. Tom qab 12 teev ntawm kev tswj hwm qhov ncauj, tib neeg cov ntshav siab yog 12mg / ml, thiab tsis muaj qhov sib txawv ntawm tus kheej.
4.9 Propranhaol hydrochloride sustained release capsule Propranhaol hydrochloride 60kg, microcrystalline cellulose 40kg, ntxiv 50L dej los ua granules. HPMC1kg thiab EC 9kg tau muab sib xyaw rau hauv cov kuab tshuaj sib xyaw (methylene chloride: methanol = 1: 1) 200L los ua cov txheej txheem, nrog tus nqi ntws ntawm 750ml / min tsuag ntawm cov dov kheej kheej, coated hais los ntawm qhov pore loj ntawm 1.4mm npo tag nrho cov khoom, thiab tom qab ntawd muab ntim rau hauv lub tshuab capsule. Txhua capsule muaj 160mg ntawm propranolol hydrochloride kheej kheej hais.
4.10 Naprolol HCL skeleton ntsiav tshuaj tau npaj los ntawm kev sib xyaw naprolol HCL:HPMC: CMC-NA ntawm qhov sib piv ntawm 1: 0.25: 2.25. Cov tshuaj tso tawm tus nqi tau ze rau xoom xaj 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. Cov tshuaj tso tawm tus nqi tau ze rau xoom xaj hauv 12 teev.
4.11 Cov pob txha pob txha ntawm cov khoom sib xyaw ntawm ethylaminesine derivatives tau npaj los ntawm txoj kev ib txwm siv kev sib xyaw ntawm micro hmoov silica gel: CMC-NA:HPMC 1: 0.7: 4.4. Cov tshuaj tuaj yeem tso tawm rau 12h ob qho tib si hauv vitro thiab hauv vivo, thiab cov qauv tso tawm tawm tau muaj kev sib raug zoo. Cov txiaj ntsig ntawm kev ntsuas nrawm nrawm raws li FDA cov cai kwv yees tias lub neej cia ntawm cov khoom no yog mus txog 2 xyoos.
4.12 HPMC (50mPa·s) (5 qhov chaw), HPMC (4000 mPa·s) (3 qhov chaw) thiab HPC1 tau yaj nyob rau hauv 1000 qhov chaw ntawm dej, 60 qhov chaw acetaminophen thiab 6 qhov chaw silica gel tau ntxiv, nplawm nrog ib homogenizer, thiab tshuaj tsuag qhuav. Cov khoom no muaj 80% ntawm cov tshuaj tseem ceeb.
4.13 Theophylline hydrophilic gel skeleton ntsiav tshuaj raug xam raws li tag nrho cov ntsiav tshuaj hnyav, 18%-35% theophylline, 7.5%-22.5% HPMC, 0.5% lactose, thiab ib qho tsim nyog ntawm hydrophobic lubricant tau nquag npaj rau hauv cov ntsiav tshuaj tso tawm, uas tuaj yeem tswj hwm cov ntshav siab ntawm tib neeg.
Post lub sij hawm: Sep-20-2022