1. Cov yam ntxwv ntawm HPMC
Hypromellose, lub npe tag nrho hydroxypropyl methylcellulose, alias HPMC.Nws cov mis molecular yog C8H15O8-(C10Hl8O6)n-C8Hl5O8, thiab nws qhov hnyav molecular yog li ntawm 86000. Cov khoom no yog cov khoom siv hluavtaws, uas yog ib feem ntawm methyl thiab ib feem ntawm polyhydroxypropyl ether ntawm cellulose.Nws tuaj yeem tsim los ntawm ob txoj hauv kev: ib qho yog tias qib tsim nyog ntawm methyl cellulose yog kho nrog NaOH, thiab tom qab ntawd ua rau cov propylene oxide nyob rau hauv qhov kub thiab txias.Daim ntawv txuas nrog lub nplhaib anhydroglucose ntawm cellulose, thiab tuaj yeem ncav cuag qib zoo;Lwm qhov yog los kho cov paj rwb linter lossis ntoo pulp fiber nrog caustic soda, thiab hnov mob nrog methyl chloride thiab propylene oxide txuas ntxiv kom tau txais nws, thiab tom qab ntawd ntxiv refine, crushed kom zoo thiab zoo li cov hmoov los yog granules.HPMC yog ntau yam ntawm cov nroj tsuag ntuj cellulose, thiab nws kuj yog ib qho zoo heev tshuaj excipient, uas muaj ntau qhov chaw.Tam sim no, nws yog dav siv nyob rau hauv tsev thiab txawv teb chaws, thiab nws yog ib tug ntawm cov kws tshuaj excipients nrog lub siab tshaj plaws siv tus nqi nyob rau hauv lub qhov ncauj tshuaj.
Cov khoom no yog dawb mus rau milky dawb hauv cov xim, tsis muaj tshuaj lom thiab tsis qab, thiab yog nyob rau hauv daim ntawv ntawm granular los yog fibrous hmoov uas ntws yooj yim.Nws yog ib qho ruaj khov nyob rau hauv lub teeb raug thiab av noo.Nws swells nyob rau hauv dej txias los tsim ib tug milky dawb colloidal tov, uas muaj ib tug tej yam degree ntawm viscosity, thiab cov phenomenon ntawm sol-gel interconversion yuav tshwm sim vim qhov kub thiab txias ntawm ib tug tej yam concentration ntawm cov tshuaj.Nws yog heev soluble nyob rau hauv 70% cawv los yog dimethyl ketone, thiab yuav tsis yaj nyob rau hauv kiag li cawv, chloroform los yog ethoxyethane.
Thaum pH ntawm hypromellose nyob nruab nrab ntawm 4.0 thiab 8.0, nws muaj kev ruaj ntseg zoo, thiab nws tuaj yeem nyob ruaj khov thaum pH nyob nruab nrab ntawm 3.0 thiab 11.0.Thaum qhov kub thiab txias yog 20 ° C thiab cov av noo yog 80%, nws yog khaws cia rau 10 hnub.Cov dej noo nqus coefficient ntawm HPMC yog 6.2%.
Vim muaj cov ntsiab lus sib txawv ntawm methoxy thiab hydroxypropyl hauv cov qauv ntawm hypromellose, ntau hom khoom tau tshwm sim.Hauv cov ntsiab lus tshwj xeeb, ntau hom khoom muaj qhov tshwj xeeb viscosity thiab Thermal gelation kub, yog li ntawd, muaj cov khoom sib txawv thiab tuaj yeem siv rau ntau lub hom phiaj.Cov tshuaj pharmacopoeias ntawm ntau lub teb chaws muaj cov kev cai sib txawv thiab cov sawv cev ntawm cov qauv: European Pharmacopoeia, raws li ntau qib ntawm cov viscosities sib txawv thiab qib ntawm kev hloov pauv ntawm cov khoom muag hauv khw, yog sawv cev los ntawm qib ntxiv rau cov lej, thiab chav tsev yog mPa ·s;Hauv Tebchaws Meskas Pharmacopoeia, lub npe nrov Ntxiv 4 tus lej kawg los qhia cov ntsiab lus thiab hom ntawm txhua qhov hloov pauv ntawm hypromellose, xws li hypromellose 2208, thawj ob tus lej sawv cev rau kwv yees feem pua ntawm methoxy, thiab ob tus lej kawg sawv cev rau hydroxypropyl. Kwv yees li feem pua.
2. Tus txheej txheem ntawm dissolving HPMC hauv dej
2.1 Cov txheej txheem dej kub
Txij li thaum hypromellose tsis yaj hauv dej kub, nws tuaj yeem sib cais hauv dej kub thaum pib, thiab tom qab ntawd txias.Ob txoj kev raug piav raws li hauv qab no:
(1) Muab cov dej kub uas xav tau rau hauv lub thawv, thiab ua kom kub txog li 70 ° C, maj mam ntxiv cov khoom no nyob rau hauv qeeb stirring, thaum pib, cov khoom no ntab rau saum npoo dej, thiab tom qab ntawd maj mam ua ib qho kev sib tw. slurry, stirring Txias lub slurry cia.
(2) Ntxiv 1/3 los yog 2/3 ntawm cov dej xav tau rau hauv lub thawv thiab kub rau 70 ° C kom tawg cov khoom los npaj cov dej kub slurry, tom qab ntawd ntxiv cov dej txias los yog dej khov ntxiv kom txog thaum cov dej kub silts Nyob rau hauv ib tug slurry, qhov sib tov yog txias tom qab stirring.
2.2 Txoj kev sib tov hmoov
Cov hmoov nplej tau tawg tag nrho los ntawm kev sib xyaw qhuav nrog qhov sib npaug lossis ntau dua ntawm lwm cov khoom xyaw hmoov, thiab tom qab ntawd yaj hauv dej.Lub sijhawm no, hypromellose tuaj yeem yaj yam tsis muaj agglomeration.
3. Qhov zoo ntawm HPMC
3.1 Cov dej txias solubility
Soluble hauv dej txias hauv qab 40 ° C lossis 70% ethanol, feem ntau insoluble hauv dej kub siab tshaj 60 ° C, tab sis tuaj yeem gelled.
3.2 Chemical inertness
Hypromellose (HPMC) yog ib hom non-ionic cellulose ether.Nws cov tshuaj tsis muaj ionic nqi thiab tsis cuam tshuam nrog hlau ntsev los yog ionic organic tebchaw.Yog li ntawd, lwm cov excipients tsis hnov mob nrog nws thaum lub sijhawm npaj.
3.3 Kev ruaj ntseg
Nws yog qhov ruaj khov rau cov kua qaub thiab alkali, thiab tuaj yeem khaws cia rau lub sijhawm ntev ntawm pH 3 thiab 1l yam tsis muaj kev hloov pauv hauv viscosity.Cov tshuaj aqueous ntawm hypromellose (HPMC) muaj cov nyhuv anti-mildew thiab tuaj yeem tswj cov viscosity ruaj khov thaum lub sij hawm ntev cia.Pharmaceuticals siv HPMC raws li excipients muaj kev ruaj ntseg zoo dua li cov uas siv cov tshuaj excipients (xws li dextrin, starch, thiab lwm yam).
3.4 viscosity adjustability
Qhov sib txawv viscosity derivatives ntawm HPMC tuaj yeem sib xyaw ua ke raws li qhov sib txawv, thiab nws cov viscosity tuaj yeem hloov pauv raws li qee txoj cai, thiab muaj kev sib raug zoo linear, yog li qhov sib piv tuaj yeem xaiv raws li qhov xav tau.
3.5 Metabolic inertia
HPMC tsis absorbed los yog metabolized nyob rau hauv lub cev, thiab tsis muab tshav kub, yog li nws yog ib tug muaj kev ruaj ntseg tshuaj npaj excipient.
3.6 Kev ruaj ntseg
Nws feem ntau ntseeg tias HPMC yog cov khoom tsis muaj tshuaj lom thiab tsis ua rau khaus.Qhov nruab nrab koob tshuaj tuag rau nas yog 5g / kg, thiab qhov nruab nrab ntawm cov nas tua nas yog 5.2g / kg.Cov koob tshuaj txhua hnub tsis muaj teeb meem rau tib neeg.
4. Kev thov ntawm HPMC hauv kev npaj
4.1 Raws li zaj duab xis txheej khoom thiab zaj duab xis-forming khoom
Siv hypromellose (HPMC) raws li cov khoom siv hauv cov ntsiav tshuaj zaj duab xis, piv nrog cov ntsiav tshuaj coated xws li cov ntsiav tshuaj uas muaj suab thaj, cov ntsiav tshuaj coated tsis muaj qhov zoo tshaj plaws hauv kev npog qhov saj ntawm cov tshuaj thiab cov tsos, tab sis lawv hardness thiab friability, noo noo nqus, disintegration, txheej yuag nce thiab lwm yam zoo qhia tau zoo dua.Cov qib qis viscosity ntawm cov khoom no yog siv los ua cov dej-soluble zaj duab xis txheej cov khoom siv rau cov ntsiav tshuaj thiab cov tshuaj, thiab qib high-viscosity yog siv los ua cov khoom siv zaj duab xis-txheej txheej rau cov kuab tshuaj organic.Cov concentration feem ntau yog 2.0% mus rau 20%.
4.2 Raws li binder thiab disintegrant
Cov qib qis viscosity ntawm cov khoom no tuaj yeem siv los ua ib qho kev sib khi thiab disintegrant rau cov ntsiav tshuaj, tshuaj, thiab granules, thiab qib high-viscosity tsuas yog siv los ua cov ntawv khi.Qhov ntau npaum li cas sib txawv nrog cov qauv sib txawv thiab cov kev xav tau.Feem ntau, qhov ntau npaum li cas ntawm binder rau qhuav granulation ntsiav tshuaj yog 5%, thiab qhov ntau npaum li cas ntawm binder rau ntub granulation ntsiav tshuaj yog 2%.
4.3 Raws li tus neeg sawv cev ncua
Tus neeg sawv cev ncua kev kawm ntawv yog ib qho viscous gel tshuaj nrog hydrophilicity, uas tuaj yeem ua rau qeeb qeeb ntawm cov sedimentation ntawm cov khoom thaum siv rau hauv tus neeg sawv cev tshem tawm, thiab nws tuaj yeem txuas rau saum npoo ntawm cov khoom los tiv thaiv cov khoom los ntawm kev sib sau ua ke thiab shrinking rau hauv lub pob. .Suspending agents ua lub luag haujlwm tseem ceeb hauv kev tshem tawm.HPMC yog ib qho zoo heev ntawm kev tshem tawm cov neeg ua haujlwm, thiab nws cov tshuaj yaj yeeb yaj kiab tuaj yeem txo qhov nro ntawm cov kua-khoom sib cuam tshuam thiab lub zog dawb ntawm cov khoom me me, yog li txhim kho kev ruaj ntseg ntawm cov txheej txheem sib txawv.Cov qib high-viscosity ntawm cov khoom no yog siv los ua ib qho kev ncua-hom kua npaj ua tus neeg sawv cev ncua.Nws muaj qhov cuam tshuam zoo, nws yooj yim rau redisperse, tsis lo rau ntawm phab ntsa, thiab muaj nplua flocculated hais.Cov koob tshuaj ib txwm yog 0.5% mus rau 1.5%.
4.4 Raws li ib tug blocker, sustained-release agent thiab pore-ua tus neeg saib xyuas
Cov qib high-viscosity ntawm cov khoom no yog siv los npaj hydrophilic gel matrix sustained-tso ntsiav tshuaj, blockers thiab tswj-tso cov neeg ua haujlwm rau cov khoom sib xyaw matrix sustained-tso ntsiav tshuaj, thiab muaj cov nyhuv ntawm ncua sij hawm tso tshuaj.Nws siv concentration yog 10% ~ 80% (W / W).Cov qib qis-viscosity yog siv los ua cov pore-forming cov neeg ua haujlwm rau kev tso tawm los yog tswj-tso npaj.Cov koob tshuaj thawj zaug uas xav tau rau kev kho cov nyhuv ntawm hom ntsiav tshuaj no tuaj yeem ua tiav sai, thiab tom qab ntawd ua kom muaj txiaj ntsig-tso tawm lossis tswj-tso tawm, thiab cov tshuaj ntshav muaj txiaj ntsig zoo yog khaws cia hauv lub cev.Thaum hypromellose ntsib dej, nws hydrates los tsim ib txheej gel.Cov txheej txheem ntawm cov tshuaj tso tawm los ntawm cov ntsiav tshuaj matrix feem ntau suav nrog kev nthuav dav ntawm gel txheej thiab yaig ntawm txheej gel.
4.5 Cov kua nplaum tiv thaiv ua cov thickener thiab colloid
Thaum cov khoom no siv los ua cov thickener, feem ntau siv concentration yog 0.45% ~ 1.0%.Cov khoom no tuaj yeem ua rau muaj kev ruaj ntseg ntawm cov kua nplaum hydrophobic, tsim ib qho kev tiv thaiv colloid, tiv thaiv cov khoom los ntawm agglomerating thiab agglomerating, yog li inhibiting qhov tsim ntawm sediment, thiab nws li ib txwm concentration yog 0.5% ~ 1.5%.
4.6 Capsule khoom rau cov tshuaj ntsiav
Feem ntau cov tshuaj capsule plhaub cov khoom siv ntawm cov tshuaj ntsiav yog raws li gelatin.Cov txheej txheem tsim khoom ntawm gelatin capsule plhaub yog yooj yim, tab sis muaj qee qhov teeb meem thiab tshwm sim xws li kev tiv thaiv tsis zoo ntawm cov dej noo thiab cov pa oxygen rhiab heev, cov tshuaj yaj yeeb tsawg tsawg, thiab ncua sij hawm tawg ntawm lub plhaub capsule thaum khaws cia.Yog li ntawd, hypromellose, raws li ib tug hloov rau gelatin tsiav tshuaj, yog siv nyob rau hauv kev npaj ntawm tsiav tshuaj, uas txhim kho cov formability thiab siv cov nyhuv ntawm capsules, thiab tau lug txhawb nyob rau hauv tsev thiab txawv teb chaws.
4.7 raws li bioadhesive
Bioadhesion thev naus laus zis, kev siv cov khoom siv nrog bioadhesive polymers, los ntawm adhesion mus rau cov mucosa lom, txhim khu kev txuas ntxiv thiab nruj ntawm kev sib cuag ntawm kev npaj thiab mucosa, kom cov tshuaj maj mam tso tawm thiab nqus los ntawm mucosa kom ua tiav cov hom phiaj kho.Nws yog tam sim no dav siv Nws yog siv los kho cov kab mob ntawm qhov ntswg kab noj hniav, qhov ncauj mucosa thiab lwm qhov chaw.Gastrointestinal bioadhesion thev naus laus zis yog kev xa tshuaj tshiab tsim nyob rau xyoo tas los no.Nws tsis tsuas yog ncua lub sijhawm nyob ntawm cov tshuaj npaj hauv plab hnyuv, tab sis kuj txhim kho kev sib cuag ntawm cov tshuaj thiab cov cell membrane ntawm qhov chaw nqus, hloov cov fluidity ntawm cov cell membrane, txhim kho qhov nkag ntawm cov tshuaj mus rau txoj hnyuv. epithelial hlwb, yog li txhim kho bioavailability ntawm cov tshuaj.
4.8 Raws li tshuaj pleev gel
Raws li kev npaj nplaum rau ntawm daim tawv nqaij, gel muaj ntau yam zoo xws li kev nyab xeeb, kev zoo nkauj, kev tu yooj yim, tus nqi qis, txheej txheem kev npaj yooj yim, thiab kev sib raug zoo nrog cov tshuaj.kev taw qhia.
Post lub sij hawm: Dec-15-2022