Cov ntaub ntawv muaj feem xyuam hauv tsev thiab txawv teb chaws hauv kev npaj cov tshuaj excipients hydroxypropyl methylcellulose (HPMC) nyob rau xyoo tas los no tau raug tshuaj xyuas, tshuaj xyuas thiab sau cov ntsiab lus, thiab nws daim ntawv thov nyob rau hauv cov khoom npaj, kua npaj, sustained thiab tswj kev tso tawm npaj, tshuaj ntsiav tshuaj, gelatin Qhov tseeb. daim ntawv thov nyob rau hauv daim teb ntawm cov formulations tshiab xws li nplaum formulations thiab bioadhesives. Vim qhov sib txawv ntawm qhov hnyav ntawm tus txheeb ze molecular thiab viscosity ntawm HPMC, nws muaj cov yam ntxwv thiab kev siv ntawm emulsification, adhesion, thickening, viscosity nce, ncua, gelling thiab film-forming. Nws yog dav siv hauv kev npaj tshuaj thiab yuav ua lub luag haujlwm ntau dua hauv kev npaj. Nrog rau kev kawm tob ntawm nws cov khoom thiab kev txhim kho cov txheej txheem tsim, HPMC yuav siv dav dua hauv kev tshawb fawb ntawm cov ntawv siv tshuaj tshiab thiab cov tshuab xa tshuaj tshiab, yog li txhawb kev txhim kho txuas ntxiv ntawm cov formulations.
Hydroxypropyl methylcellulose yog ib qho khoom siv zoo; tshuaj npaj; tshuaj excipients.
Pharmaceutical excipients tsis yog tsuas yog cov khoom siv hauv paus rau kev tsim cov tshuaj ntsuab npaj, tab sis kuj muaj feem xyuam rau qhov nyuaj ntawm cov txheej txheem kev npaj, tshuaj zoo, kev ruaj ntseg, kev nyab xeeb, tshuaj tso tawm tus nqi, hom kev nqis tes ua, kev soj ntsuam zoo, thiab kev tsim kho tshiab. cov ntaub ntawv ntau npaum thiab txoj kev tshiab ntawm kev tswj hwm. zoo sib xws. Qhov tshwm sim ntawm cov tshuaj excipients tshiab feem ntau txhawb kev txhim kho ntawm kev npaj zoo thiab kev tsim cov ntawv tshiab. Hydroxypropyl methylcellulose (HPMC) yog ib qho ntawm cov khoom siv tshuaj nrov tshaj plaws hauv tsev thiab txawv teb chaws. Vim nws qhov sib txawv molecular hnyav thiab viscosity, nws muaj lub luag haujlwm ntawm emulsifying, khi, thickening, thickening, suspending, thiab glueing. Nta thiab siv xws li coagulation thiab zaj duab xis tsim yog dav siv nyob rau hauv kev siv tshuab. Kab lus no tsuas yog tshuaj xyuas daim ntawv thov ntawm hydroxypropyl methylcellulose (HPMC) hauv cov qauv hauv xyoo tas los.
1.Cov yam ntxwv tseem ceeb ntawm HPMC
Hydroxypropyl methyl cellulose (HPMC), cov mis molecular yog C8H15O8-(C10 H18O6) n- C8H15O8, thiab cov txheeb ze molecular loj yog hais txog 86 000. Cov khoom no yog ib tug semi-synthetic khoom, uas yog ib feem ntawm methyl thiab ib feem ntawm polyhydroxypropyl lwm yam. ntawm cellulose. Nws tuaj yeem tsim tau ob txoj hauv kev: Ib qho yog tias methyl cellulose ntawm qib tsim nyog tau kho nrog NaOH thiab tom qab ntawd ua rau propylene oxide nyob rau hauv qhov kub thiab txias. Lub sijhawm cov tshuaj tiv thaiv yuav tsum tau ntev txaus kom tso cai rau methyl thiab hydroxypropyl los ua ether bonds Nws txuas nrog lub nplhaib anhydroglucose ntawm cellulose hauv daim ntawv ntawm cellulose, thiab tuaj yeem ncav cuag qhov xav tau qib; Lwm qhov yog kho cov paj rwb linter lossis ntoo pulp fiber nrog caustic soda, thiab tom qab ntawd hnov mob nrog cov tshuaj chlorinated methane thiab propylene oxide txuas ntxiv, thiab tom qab ntawd ua kom zoo dua ntxiv. , crushed rau hauv nplua thiab uniform hmoov los yog granules.
Cov xim ntawm cov khoom no yog dawb mus rau milky dawb, tsw thiab tsis qab, thiab daim ntawv yog granular los yog fibrous yooj yim-flowing hmoov. Cov khoom no tuaj yeem yaj hauv dej los ua kom pom tseeb rau cov kua mis dawb colloidal nrog ib qho viscosity. Lub sol-gel interconversion tshwm sim tuaj yeem tshwm sim vim qhov kub hloov pauv ntawm cov tshuaj nrog qee qhov concentration.
Vim tias qhov sib txawv ntawm cov ntsiab lus ntawm ob qhov hloov pauv hauv cov qauv ntawm methoxy thiab hydroxypropyl, ntau hom khoom tau tshwm sim. Hauv kev tshwj xeeb, ntau hom khoom muaj cov yam ntxwv tshwj xeeb. Viscosity thiab thermal gelation kub, yog li muaj cov khoom sib txawv thiab tuaj yeem siv rau ntau lub hom phiaj. Pharmacopoeia ntawm ntau lub teb chaws muaj cov kev cai sib txawv thiab cov sawv cev ntawm tus qauv: European Pharmacopoeia yog nyob ntawm ntau qib ntawm cov viscosities sib txawv thiab cov qib sib txawv ntawm kev hloov pauv ntawm cov khoom muag hauv khw, qhia los ntawm qib ntxiv cov lej, thiab chav tsev yog "mPa s ”. Hauv Teb Chaws Asmeskas Pharmacopoeia, 4 tus lej raug ntxiv tom qab lub npe generic los qhia cov ntsiab lus thiab hom ntawm txhua qhov hloov pauv ntawm hydroxypropyl methylcellulose, xws li hydroxypropyl methylcellulose 2208. Thawj ob tus lej sawv cev rau kwv yees tus nqi ntawm pawg methoxy. Feem pua, ob tus lej kawg sawv cev rau kwv yees feem pua ntawm hydroxypropyl.
Calocan's hydroxypropyl methylcellulose muaj 3 series, uas yog E series, F series thiab K series, txhua series muaj ntau yam qauv xaiv los ntawm. E series feem ntau yog siv los ua zaj duab xis txheej, siv rau cov ntsiav tshuaj txheej, kaw cov ntsiav tshuaj cores; E, F series yog siv los ua viscosifiers thiab tso tawm cov tshuaj tiv thaiv rau cov tshuaj tiv thaiv ophthalmic, tshem tawm cov neeg ua haujlwm, cov thickeners rau kev npaj ua kua, ntsiav tshuaj thiab Binders ntawm granules; K series feem ntau yog siv los ua kev tso tawm inhibitors thiab hydrophilic gel matrix cov ntaub ntawv rau qeeb thiab tswj kev npaj tawm.
Cov chaw tsim khoom hauv tsev feem ntau suav nrog Fuzhou No. 2 Chemical Factory, Huzhou Food and Chemical Co., Ltd., Sichuan Luzhou Pharmaceutical Accessories Factory, Hubei Jinxian Chemical Factory No. 1, Feicheng Ruitai Fine Chemical Co., Ltd., Shandong Liaocheng Ahua Pharmaceutical ., Ltd., Xi'an Huian tshuaj nroj tsuag, thiab lwm yam.
2.Qhov zoo ntawm HPMC
HPMC tau dhau los ua ib qho ntawm cov khoom siv tshuaj ntau tshaj plaws hauv tsev thiab txawv teb chaws, vim tias HPMC muaj qhov zoo uas lwm cov excipients tsis muaj.
2.1 Cov dej txias solubility
Soluble nyob rau hauv dej txias hauv qab 40 ℃ los yog 70% ethanol, yeej insoluble nyob rau hauv dej kub saum 60 ℃, tab sis muaj peev xwm gel.
2.2 Chemically inert
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 lwm yam excipients tsis hnov mob nrog nws thaum lub sij hawm tsim cov txheej txheem ntawm kev npaj.
2.3 Kev ruaj ntseg
Nws yog qhov ruaj khov rau ob qho tib si acid thiab alkali, thiab tuaj yeem khaws cia rau lub sijhawm ntev ntawm pH 3 thiab 11 yam tsis muaj kev hloov pauv loj hauv viscosity. Cov tshuaj aqueous ntawm HPMC muaj cov nyhuv anti-mildew thiab tswj kom zoo viscosity stability thaum lub sij hawm ntev cia. Cov tshuaj excipients uas siv HPMC muaj kev ruaj ntseg zoo dua li cov uas siv cov tshuaj excipients (xws li dextrin, starch, thiab lwm yam).
2.4 Viscosity Adjustability
Qhov sib txawv viscosity derivatives ntawm HPMC tuaj yeem sib xyaw ua ke sib txawv, thiab nws cov viscosity tuaj yeem hloov tau raws li qee txoj cai, thiab muaj kev sib raug zoo linear, yog li qhov kev faib ua feem tuaj yeem xaiv raws li qhov xav tau.
2.5 Metabolic inertness
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. 2.6 Kev Nyab Xeeb Feem ntau suav hais tias HPMC yog cov khoom tsis muaj tshuaj lom thiab tsis ua rau khaus, qhov nruab nrab ntawm cov nas tua nas yog 5 g·kg - 1 , thiab qhov nruab nrab ntawm cov nas tua nas yog 5. 2 g · kg - 1 . Cov koob tshuaj txhua hnub tsis muaj teeb meem rau tib neeg lub cev.
3.Kev siv HPMC hauv cov qauv
3.1 Raws li zaj duab xis txheej khoom thiab zaj duab xis-tsim khoom
Siv HPMC raws li cov khoom siv hauv cov ntsiav tshuaj, cov ntsiav tshuaj coated tsis muaj qhov zoo tshaj plaws hauv kev npog qhov saj thiab tsos piv nrog cov ntsiav tshuaj coated xws li qab zib-coated ntsiav tshuaj, tab sis nws hardness, friability, noo noo nqus, disintegration degree. , txheej qhov hnyav nce thiab lwm yam kev ntsuas zoo dua. Cov qib qis viscosity ntawm cov khoom no yog siv los ua cov dej-soluble zaj duab xis txheej cov ntaub ntawv rau cov ntsiav tshuaj thiab tshuaj, thiab qib high-viscosity yog siv raws li ib tug zaj duab xis txheej khoom rau organic solvent systems, feem ntau yog ib tug concentration ntawm 2% mus rau 20. %.
Zhang Jixing et al. siv cov txheej txheem saum npoo los ua kom zoo dua cov txheej txheem premix nrog HPMC ua zaj duab xis txheej. Kev siv cov khoom siv ua yeeb yaj kiab HPMC, tus nqi ntawm polyvinyl cawv thiab plasticizer polyethylene glycol raws li qhov kev tshawb nrhiav, lub zog tensile thiab permeability ntawm cov yeeb yaj kiab thiab cov viscosity ntawm cov txheej txheem zaj duab xis yog qhov kev tshuaj ntsuam xyuas, thiab kev sib raug zoo ntawm kev soj ntsuam. Performance index thiab cov tshuaj ntsuam xyuas tau piav qhia los ntawm tus qauv lej, thiab cov txheej txheem tsim kom zoo yog thaum kawg tau txais. Nws qhov kev siv yog raws li tus neeg sawv cev ua yeeb yaj kiab hydroxypropyl methylcellulose (HPMCE5) 11.88 g, polyvinyl cawv 24.12 g, plasticizer polyethylene glycol 13.00 g, thiab txheej txheej ncua kev kawm viscosity yog 20 mPa·s, qhov zoo tshaj plaws permeability thiab tensile zog ntawm zaj duab xis. . Zhang Yuan tau txhim kho cov txheej txheem kev npaj, siv HPMC los ua cov ntaub ntawv los hloov cov hmoov txhuv nplej siab slurry, thiab hloov cov ntsiav tshuaj Jiahua rau cov ntsiav tshuaj zaj duab xis los txhim kho qhov zoo ntawm nws cov kev npaj, txhim kho nws cov hygroscopicity, yooj yim rau ploj, xoob cov ntsiav tshuaj, splintered thiab lwm yam teeb meem, txhim khu cov ntsiav tshuaj stability. Cov txheej txheem tsim kom zoo tau txiav txim siab los ntawm kev sim orthogonal, uas yog, cov slurry concentration yog 2% HPMC hauv 70% ethanol tov thaum txheej txheej, thiab lub sijhawm nplawm thaum lub sij hawm granulation yog 15 min. Cov txiaj ntsig Jiahua zaj duab xis-coated ntsiav tshuaj tau npaj los ntawm cov txheej txheem tshiab thiab cov ntawv sau tshuaj tau zoo heev hauv cov tsos, lub sijhawm tawg thiab lub zog tseem ceeb dua li cov uas tsim los ntawm cov txheej txheem sau ntawv thawj zaug, thiab qhov tsim nyog tus nqi ntawm cov ntsiav tshuaj zaj duab xis tau txhim kho zoo heev. mus txog ntau dua 95%. Liang Meiyi, Lu Xiaohui, thiab lwm yam kuj tseem siv hydroxypropyl methylcellulose ua cov ntaub ntawv tsim cov yeeb yaj kiab los npaj cov patinae nyuv positioning ntsiav tshuaj thiab matrine nyuv positioning ntsiav tshuaj, feem. cuam tshuam rau kev tso tshuaj. Huang Yunran npaj Dragon's Blood Colon Positioning Tablets, thiab siv HPMC rau cov txheej txheem txheej txheej o, thiab nws cov feem ntau yog 5%. Nws tuaj yeem pom tau tias HPMC tuaj yeem siv dav hauv cov kab mob hauv plab-targeted tshuaj.
Hydroxypropyl methylcellulose tsis yog tsuas yog cov ntaub ntawv zoo tshaj plaws ntawm cov yeeb yaj kiab, tab sis kuj tuaj yeem siv los ua cov khoom siv hauv zaj duab xis formulations. Wang Tongshun thiab lwm yam yog optimized rau cov tshuaj ntawm compound zinc licorice thiab aminolexanol qhov ncauj composite zaj duab xis, nrog lub yooj, uniformity, smoothness, pob tshab ntawm zaj duab xis tus neeg saib xyuas raws li kev soj ntsuam Performance index, tau txais kev pom zoo tshuaj yog PVA 6.5 g, HPMC 0.1 g thiab 6.0 g ntawm propylene glycol ua tau raws li qhov yuav tsum tau ua ntawm kev tso tawm qeeb thiab kev nyab xeeb, thiab tuaj yeem siv los ua kev npaj tshuaj ntawm cov yeeb yaj kiab sib xyaw.
3.2 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 siab 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 ntau npaum li cas ntawm binder rau ntub granulation ntsiav tshuaj yog 2%.
Li Houtao thiab al tshuaj xyuas cov ntawv khi ntawm cov ntsiav tshuaj tinidazole. 8% polyvinylpyrrolidone (PVP-K30), 40% phoov, 10% hmoov txhuv nplej siab slurry, 2.0% hydroxypropyl methylcellulose K4 (HPMCK4M), 50% ethanol tau tshawb xyuas raws li kev sib txuas ntawm tinidazole ntsiav tshuaj nyob rau hauv lem. Kev npaj ntawm tinidazole ntsiav tshuaj. Cov tsos mob hloov pauv ntawm cov ntsiav tshuaj dawb thiab tom qab txheej tau muab piv, thiab qhov friability, hardness, disintegration lub sij hawm txwv thiab dissolution tus nqi ntawm cov ntsiav tshuaj sib txawv tau ntsuas. Cov txiaj ntsig Cov ntsiav tshuaj npaj los ntawm 2.0% hydroxypropyl methylcellulose yog glossy, thiab kev ntsuas friability pom tsis muaj ntug chipping thiab cornering tshwm sim, thiab tom qab txheej txheej, cov ntsiav tshuaj zoo li ua tiav thiab cov tsos zoo. Yog li ntawd, tinidazole ntsiav tshuaj tau npaj nrog 2.0% HPMC-K4 thiab 50% ethanol raws li kev sib khi tau siv. Guan Shihai tau kawm txog cov txheej txheem ntawm Fuganning Tablets, tshuaj xyuas cov nplaum nplaum, thiab tshuaj xyuas 50% ethanol, 15% starch paste, 10% PVP thiab 50% ethanol daws nrog compressibility, smoothness, thiab friability raws li kev ntsuas ntsuas. , 5% CMC-Na thiab 15% HPMC tov (5 mPa s). Cov txiaj ntsig Cov nplooj ntawv npaj los ntawm 50% ethanol, 15% starch paste, 10% PVP 50% ethanol tov thiab 5% CMC-Na muaj ib tug du nto, tab sis tsis zoo compressibility thiab tsawg hardness, uas tsis tuaj yeem ua tau raws li qhov xav tau ntawm txheej txheej; 15% HPMC tov (5 mPa·s), lub ntsej muag ntawm lub ntsiav tshuaj yog du, friability yog tsim nyog, thiab compressibility yog zoo, uas yuav ua tau raws li cov kev xav tau ntawm txheej. Yog li ntawd, HPMC (5 mPa s) raug xaiv los ua cov nplaum.
3.3 as suspending agent
Cov qib high-viscosity ntawm cov khoom no yog siv los ua tus neeg sawv cev ncua kev kawm los npaj cov kua dej ncua kev kawm. Nws muaj cov nyhuv suspending zoo, yog ib qho yooj yim rau redisperse, tsis lo rau ntawm phab ntsa, thiab zoo flocculation hais. Cov koob tshuaj ib txwm yog 0.5% mus rau 1.5%. Song Tian et al. Cov khoom siv feem ntau siv cov ntaub ntawv polymer (hydroxypropyl methylcellulose, sodium carboxymethylcellulose, povidone, xanthan gum, methylcellulose, thiab lwm yam) ua cov tshuaj ncua kev npaj racecadotril. qhuav suspension. Los ntawm cov sedimentation ntim piv ntawm txawv ncua kev kawm ntawv, lub redispersibility Performance index, thiab cov rheology, ncua kev kawm ntawv viscosity thiab microscopic morphology tau soj ntsuam, thiab stability ntawm cov tshuaj hais nyob rau hauv lub accelerated xyaum ua tej yam. Cov txiaj ntsig Kev ncua kev qhuav qhuav npaj nrog 2% HPMC raws li tus neeg sawv cev ncua kev kawm muaj cov txheej txheem yooj yim thiab kev ruaj ntseg zoo.
Piv nrog methyl cellulose, hydroxypropyl methyl cellulose muaj cov yam ntxwv ntawm kev tsim cov tshuaj kom pom tseeb, thiab tsuas yog ib qho me me ntawm cov tshuaj fiber ntau uas tsis muaj kev sib cais, yog li HPMC kuj tau siv los ua tus neeg sawv cev ncua hauv kev npaj tshuaj ophthalmic. Liu Li et al. siv HPMC, hydroxypropyl cellulose (HPC), carbomer 940, polyethylene glycol (PEG), sodium hyaluronate (HA) thiab kev sib xyaw ntawm HA/HPMC raws li cov neeg ua haujlwm tshem tawm los npaj sib txawv rau Ciclovir ophthalmic suspension, sedimentation ntim piv, particle loj thiab redispersibility raug xaiv los ua qhov ntsuas ntsuas los tshuaj xyuas tus neeg saib xyuas kev ncua zoo tshaj plaws. Cov txiaj ntsig tau pom tias acyclovir ophthalmic suspension npaj los ntawm 0.05% HA thiab 0.05% HPMC raws li tus neeg sawv cev ncua kev kawm, cov sedimentation ntim piv yog 0.998, particle loj yog uniform, redispersibility yog zoo, thiab kev npaj yog ruaj khov kev sib deev nce.
3.4 Raws li ib tug blocker, qeeb thiab tswj kev tso tawm tus neeg sawv cev thiab pore-forming tus neeg sawv cev
Cov qib high-viscosity ntawm cov khoom no yog siv rau kev npaj ntawm hydrophilic gel matrix sustained-tso ntsiav tshuaj, blockers thiab tswj-tso cov neeg sawv cev ntawm cov khoom sib xyaw matrix sustained-tso ntsiav tshuaj, thiab muaj cov nyhuv ntawm ncua sij hawm tso tshuaj. Nws cov concentration yog 10% mus rau 80%. Cov qib qis-viscosity yog siv los ua cov tshuaj porogens rau kev tso tawm los yog tswj-tso npaj. Cov koob tshuaj thawj zaug uas xav tau rau kev kho cov nyhuv ntawm cov ntsiav tshuaj no tuaj yeem ncav cuag sai, thiab tom qab ntawd qhov kev tso tawm-tso tawm lossis tswj-tso tawm yog exerted, thiab cov ntshav cov tshuaj muaj txiaj ntsig zoo yog khaws cia hauv lub cev. . Hydroxypropyl methylcellulose yog hydrated los tsim ib txheej gel thaum nws ntsib dej. 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. Jung Bo Shim et al npaj carvedilol sustained-tso ntsiav tshuaj nrog HPMC raws li cov khoom tsim tawm.
Hydroxypropyl methylcellulose kuj tau siv dav hauv cov ntsiav tshuaj uas tau tso tawm matrix ntawm cov tshuaj suav tshuaj, thiab feem ntau ntawm cov khoom xyaw nquag, cov khoom siv tau zoo thiab ib qho kev npaj ntawm cov tshuaj suav tshuaj. Liu Wen et al. siv 15% hydroxypropyl methylcellulose ua cov khoom siv matrix, 1% lactose thiab 5% microcrystalline cellulose ua cov fillers, thiab npaj Jingfang Taohe Chengqi Decoction rau hauv qhov ncauj matrix sustained-tso ntsiav tshuaj. Tus qauv yog qhov sib npaug Higuchi. Cov txheej txheem muaj pes tsawg leeg yog qhov yooj yim, kev npaj tau yooj yim, thiab cov ntaub ntawv tso tawm yog qhov ruaj khov, uas ua tau raws li cov cai ntawm Suav Pharmacopoeia. Tang Guang et al. siv tag nrho cov saponins ntawm Astragalus ua cov qauv tshuaj, npaj HPMC matrix ntsiav tshuaj, thiab tshawb xyuas cov yam tseem ceeb uas cuam tshuam rau cov tshuaj tso tawm los ntawm qhov zoo ntawm cov tshuaj suav tshuaj hauv HPMC matrix ntsiav tshuaj. Cov txiaj ntsig Raws li qhov ntau npaum li cas ntawm HPMC nce, qhov kev tso tawm ntawm astragaloside txo qis, thiab qhov feem pua ntawm cov tshuaj tso tawm muaj ze li ntawm kev sib raug zoo nrog cov kev sib cais ntawm cov matrix. Hauv cov ntsiav tshuaj hypromellose HPMC matrix, muaj qee qhov kev sib raug zoo ntawm kev tso tawm ntawm cov tshuaj suav tshuaj suav tshuaj thiab ntau npaum li cas thiab hom HPMC, thiab cov txheej txheem tso tawm ntawm hydrophilic tshuaj monomer zoo ib yam li nws. Hydroxypropyl methylcellulose tsis yog tsuas yog haum rau hydrophilic compounds, tab sis kuj rau cov khoom uas tsis yog-hydrophilic. Liu Guihua siv 17% hydroxypropyl methylcellulose (HPMCK15M) raws li cov khoom siv txhawb nqa-tso matrix, thiab npaj Tianshan Xuelian sustained-tso matrix ntsiav tshuaj los ntawm ntub granulation thiab ntsiav tshuaj txoj kev. Qhov cuam tshuam-tso tawm tau pom tseeb, thiab cov txheej txheem npaj tau ruaj khov thiab ua tau.
Hydroxypropyl methylcellulose tsis yog tsuas yog siv rau cov ntsiav tshuaj sustained-tso matrix ntawm cov khoom xyaw thiab cov khoom siv zoo ntawm cov tshuaj suav tshuaj, tab sis kuj siv ntau thiab ntau dua hauv cov tshuaj suav tshuaj suav tshuaj. Wu Huichao et al. siv 20% hydroxypropyl methyl cellulose (HPMCK4M) raws li cov khoom siv matrix, thiab siv cov hmoov ncaj qha compression txoj kev npaj Yizhi hydrophilic gel matrix ntsiav tshuaj uas tuaj yeem tso cov tshuaj tsis tu ncua thiab ruaj khov rau 12 teev. Saponin Rg1, ginsenoside Rb1 thiab Panax notoginseng saponin R1 tau siv los ua qhov ntsuas ntsuas los tshawb xyuas qhov tso tawm hauv vitro, thiab cov tshuaj tso tawm sib npaug tau tsim los kawm txog cov tshuaj tso tawm. Cov txiaj ntsig Cov tshuaj tso tawm cov txheej txheem ua raws li xoom-qib kinetic equation thiab Ritger-Peppas kab zauv, nyob rau hauv uas cov geniposide raug tso tawm los ntawm non-Fick diffusion, thiab peb lub Cheebtsam hauv Panax notoginseng tau tso tawm los ntawm skeletal yaig.
3.5 Cov kua nplaum tiv thaiv ua cov thickener thiab colloid
Thaum cov khoom no siv los ua cov thickener, qhov feem pua ntawm cov concentration yog 0.45% mus rau 1.0%. Nws tseem tuaj yeem ua rau kom muaj kev ruaj ntseg ntawm cov kua nplaum hydrophobic, tsim ib qho kev tiv thaiv colloid, tiv thaiv cov khoom los ntawm coalescing thiab agglomerating, yog li inhibiting qhov tsim ntawm sediments. Nws feem ntau concentration yog 0.5% mus rau 1.5%.
Wang Zhen et al. siv L9 orthogonal sim tsim qauv los tshawb xyuas cov txheej txheem kev npaj ntawm cov tshuaj activated carbon enema. Cov txheej txheem zoo tshaj plaws rau kev txiav txim siab zaum kawg ntawm cov tshuaj activated carbon enema yog siv 0.5% sodium carboxymethyl cellulose thiab 2.0% hydroxypropyl methylcellulose (HPMC muaj 23.0% methoxyl pab pawg, hydroxypropoxyl Base 11.6%) ua cov thickener, cov txheej txheem kev pab txhawb nqa. stability ntawm tshuaj activated carbon. Zhang Zhiqiang et al. tsim pH-rhiab heev levofloxacin hydrochloride ophthalmic npaj-rau-siv gel nrog sustained-tso cov nyhuv, siv carbopol raws li cov gel matrix thiab hydroxypropyl methylcellulose ua cov thickening neeg sawv cev. Kev tshuaj xyuas zoo los ntawm kev sim, thaum kawg tau txais kev pom zoo tshuaj yog levofloxacin hydrochloride 0.1 g, carbopol (9400) 3 g, hydroxypropyl methylcellulose (E50 LV) 20 g, disodium hydrogen phosphate 0.35 g, phosphoric acid ntawm sodium 0.45 g sodium dichloride 0.45 g. , 0.03 g ntawm ethyl paraben, thiab dej ntxiv rau ua 100 mL. Hauv qhov kev xeem, tus sau tau tshuaj xyuas cov hydroxypropyl methylcellulose METHOCEL series ntawm Colorcon Company nrog cov kev qhia tshwj xeeb (K4M, E4M, E15 LV, E50LV) los npaj cov thickeners nrog ntau qhov sib txawv, thiab cov txiaj ntsig tau xaiv HPMC E50 LV ua cov thickener. Thickener rau pH-sensitive levofloxacin hydrochloride instant gels.
3.6 raws li cov khoom siv tshuaj ntsiav
Feem ntau, cov khoom siv ntawm lub plhaub capsule ntawm cov tshuaj ntsiav yog tsuas yog gelatin. Cov txheej txheem ntau lawm ntawm lub plhaub capsule yog qhov 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 tshuaj oxygen-rhiab heev, txo cov tshuaj dissolution, thiab qeeb disintegration ntawm lub capsule plhaub thaum lub sij hawm cia. Yog li ntawd, hydroxypropyl methylcellulose yog siv los hloov gelatin capsules rau kev npaj cov tshuaj ntsiav, uas txhim kho lub capsule manufacturing formability thiab cov nyhuv siv, thiab tau lug txhawb nyob rau hauv tsev thiab txawv teb chaws.
Siv theophylline ua tshuaj tswj, Podczeck li al. pom tias cov tshuaj tawg ntawm cov tshuaj ntsiav nrog hydroxypropyl methylcellulose plhaub tau ntau dua li ntawm cov tshuaj ntsiav gelatin. Yog vim li cas rau kev tsom xam yog tias qhov kev puas tsuaj ntawm HPMC yog kev puas tsuaj ntawm tag nrho cov tshuaj ntsiav tib lub sijhawm, thaum lub sij hawm disintegration ntawm gelatin capsule yog disintegration ntawm lub network qauv ua ntej, thiab tom qab ntawd lub disintegration ntawm tag nrho cov tshuaj ntsiav, yog li ntawd lub disintegration ntawm lub gelatin capsule. HPMC capsule yog qhov tsim nyog rau Capsule plhaub rau cov qauv tso tawm tam sim. Chiwele et al. kuj tau txais cov lus xaus zoo sib xws thiab muab piv rau kev sib cais ntawm gelatin, gelatin / polyethylene glycol thiab HPMC plhaub. Cov txiaj ntsig tau pom tias HPMC cov plhaub tau yaj sai sai nyob rau hauv cov pH sib txawv, thaum gelatin capsules Nws cuam tshuam zoo heev los ntawm pH sib txawv. Tang Yue et al. soj ntsuam ib hom tshiab capsule plhaub rau cov tshuaj uas tsis tshua muaj tshuaj dawb paug qhuav hmoov inhaler carrier system. Piv nrog rau lub plhaub capsule ntawm hydroxypropyl methylcellulose thiab capsule plhaub ntawm gelatin, kev ruaj ntseg ntawm lub plhaub capsule thiab cov khoom ntawm cov hmoov nyob rau hauv lub plhaub nyob rau hauv txawv tej yam kev mob raug soj ntsuam, thiab friability xeem tau nqa tawm. Cov txiaj ntsig tau pom tias piv nrog gelatin capsules, HPMC capsule shells zoo dua nyob rau hauv kev ruaj ntseg thiab hmoov tiv thaiv, muaj zog noo noo tsis kam, thiab muaj qis friability dua gelatin capsule shells, yog li HPMC capsule shells yog tsim nyog rau Capsules rau qhuav hmoov inhalation.
3.7 raws li bioadhesive
Bioadhesion technology siv excipients nrog bioadhesive polymers. Los ntawm kev ua raws li cov kab mob lom, nws txhim kho qhov txuas ntxiv thiab nruj ntawm kev sib cuag ntawm kev npaj thiab cov mucosa, kom cov tshuaj maj mam tso tawm thiab nqus los ntawm mucosa kom ua tiav lub hom phiaj ntawm kev kho mob. Nws yog dav siv tam sim no. Kev kho cov kab mob ntawm txoj hnyuv, qhov chaw mos, qhov ncauj mucosa thiab lwm qhov chaw.
Gastrointestinal bioadhesion thev naus laus zis yog ib qho kev xa tshuaj tshiab tsim nyob rau xyoo tas los no. Nws tsis tsuas yog ncua lub sijhawm nyob ntawm kev npaj tshuaj nyob rau hauv lub plab zom mov, 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, thiab ua rau cov tshuaj nkag mus rau hauv cov tshuaj. lub plab hnyuv me epithelial hlwb yog txhim kho, yog li txhim kho bioavailability ntawm cov tshuaj. Wei Keda et al. soj ntsuam cov ntsiav tshuaj tseem ceeb tshuaj nrog cov koob tshuaj ntawm HPMCK4M thiab Carbomer 940 raws li qhov kev tshawb nrhiav, thiab siv cov khoom siv bioadhesion tus kheej los ntsuas qhov tev tawm ntawm cov ntsiav tshuaj thiab simulated biofilm los ntawm qhov zoo ntawm cov dej hauv lub hnab yas. , thiab thaum kawg xaiv cov ntsiab lus ntawm HPMCK40 thiab carbomer 940 yuav tsum yog 15 thiab 27.5 mg nyob rau hauv qhov chaw kho kom zoo ntawm NCaEBT ntsiav tshuaj cores, raws li, los npaj NCaEBT ntsiav tshuaj cores, qhia tias cov ntaub ntawv bioadhesive (xws li hydroxypropyl methylcellulose) tuaj yeem txo qhov Impro. qhov adhesion ntawm kev npaj rau cov ntaub so ntswg.
Kev npaj ntawm qhov ncauj bioadhesive kuj yog hom tshiab ntawm kev xa tshuaj uas tau kawm ntau dua nyob rau xyoo tas los no. Kev npaj ntawm qhov ncauj bioadhesive tuaj yeem ua raws li cov tshuaj mus rau qhov cuam tshuam ntawm lub qhov ncauj kab noj hniav, uas tsis tsuas yog ncua sij hawm nyob ntawm cov tshuaj nyob rau hauv lub qhov ncauj mucosa, tab sis kuj tiv thaiv lub qhov ncauj mucosa. Cov nyhuv kho tau zoo dua thiab txhim kho cov tshuaj bioavailability. Xu Xiaoyan et al. optimized cov tshuaj insulin qhov ncauj nplaum, siv kua pectin, chitosan, carbomer 934P, hydroxypropyl methylcellulose (HPMC K392) thiab sodium alginate ua cov khoom siv bioadhesive, thiab khov-qhuav los npaj cov tshuaj insulin hauv qhov ncauj. Adhesive ob txheej ntawv. Cov ntsiav tshuaj uas npaj cov tshuaj insulin hauv qhov ncauj muaj qhov ntxeem tau zoo li daim txhuam cev, uas yog qhov zoo rau kev tso tawm cov tshuaj insulin, thiab muaj cov txheej txheem tiv thaiv hydrophobic, uas tuaj yeem ua kom ntseeg tau tias cov tshuaj tso tawm unidirectional thiab zam kev poob ntawm cov tshuaj. Hao Jifu et al. kuj tau npaj cov hlaws xiav-daj hlaws qhov ncauj bioadhesive thaj ua rau thaj siv Baiji kua nplaum, HPMC thiab carbomer ua cov khoom siv bioadhesive.
Hauv kev siv tshuaj hauv qhov chaw mos, bioadhesion thev naus laus zis kuj tau siv dav. Zhu Yuting et al. siv cov carbomer (CP) thiab HPMC ua cov ntaub nplaum thiab cov ntaub ntawv tso tawm kom ruaj khov los npaj cov tshuaj clotrimazole bioadhesive qhov chaw mos nrog cov qauv sib txawv thiab qhov sib piv, thiab ntsuas lawv qhov adhesion, adhesion lub sij hawm thiab qhov feem pua o ntawm qhov chaw ntawm qhov chaw mos. , cov tshuaj tsim nyog tau tshuaj xyuas raws li CP-HPMC1: 1, daim ntawv nplaum npaj tau zoo adhesion, thiab cov txheej txheem yog yooj yim thiab ua tau.
3.8 raws li tshuaj pleev gel
Raws li kev npaj ua nplaum, 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 ntawm kev loj hlob. Piv txwv li, transdermal gel yog ib daim ntawv noj tshuaj tshiab uas tau kawm ntau dua nyob rau xyoo tas los no. Nws tuaj yeem tsis tsuas yog zam kev puas tsuaj ntawm cov tshuaj hauv plab hnyuv thiab txo qhov ncov-rau-trough variation ntawm ntshav cov tshuaj concentration, tab sis kuj tau dhau los ua ib qho ntawm cov tshuaj tso tawm tau zoo los kov yeej cov kev mob tshwm sim. .
Zhu Jingjie et al. tau kawm txog cov nyhuv ntawm cov matrices sib txawv ntawm kev tso tawm scutellarin cawv plastid gel hauv vitro, thiab kuaj nrog carbomer (980NF) thiab hydroxypropyl methylcellulose (HPMCK15M) ua gel matrices, thiab tau txais scutellarin haum rau scutellarin. Gel matrix ntawm cawv plastids. Cov txiaj ntsig kev sim qhia tau tias 1. 0% carbomer, 1. 5% carbomer, 1. 0% carbomer + 1. 0% HPMC, 1. 5% carbomer + 1. 0% HPMC li gel matrix Ob leeg haum rau scutellarin cawv plastids. . Thaum lub sij hawm kev sim, nws tau pom tias HPMC tuaj yeem hloov pauv cov tshuaj tso tawm hom carbomer gel matrix los ntawm kev ua kom haum rau kinetic sib npaug ntawm cov tshuaj tso tawm, thiab 1.0% HPMC tuaj yeem txhim kho 1.0% carbomer matrix thiab 1.5% carbomer matrix. Qhov laj thawj yog vim li cas HPMC nthuav dav sai dua, thiab kev nthuav dav sai nyob rau theem pib ntawm qhov kev sim ua rau qhov sib txawv ntawm cov khoom siv carbomer gel loj dua, yog li ua kom nws cov tshuaj tso tawm sai. Zhao Wencui et al. siv carbomer-934 thiab hydroxypropyl methylcellulose ua cov nqa khoom los npaj norfloxacin ophthalmic gel. Cov txheej txheem kev npaj yog qhov yooj yim thiab ua tau, thiab qhov ua tau zoo raws li ophthalmic gel ntawm "Suav Pharmacopoeia" (2010 tsab) Cov kev cai zoo.
3.9 Precipitation inhibitor rau tus kheej-microemulsifying system
Self-microemulsifying drug delivery system (SMEDDS) yog ib hom tshiab ntawm kev siv tshuaj hauv qhov ncauj, uas yog homogeneous, ruaj khov thiab pob tshab sib xyaw uas muaj cov tshuaj, roj theem, emulsifier thiab co-emulsifier. Cov tshuaj muaj pes tsawg leeg yog qhov yooj yim, thiab kev nyab xeeb thiab kev ruaj ntseg zoo. Rau cov tshuaj soluble tsis zoo, dej-soluble fiber ntau cov ntaub ntawv polymer, xws li HPMC, polyvinylpyrrolidone (PVP), thiab lwm yam, feem ntau ntxiv los ua cov tshuaj dawb thiab cov tshuaj encapsulated hauv microemulsion ua tiav supersaturated dissolution hauv plab hnyuv, thiaj li. nce cov tshuaj solubility thiab txhim kho bioavailability.
Peng Xuan et al. npaj ib lub silibinin supersaturated self-emulsifying tshuaj xa system (S-SEDDS). Oxyethylene hydrogenated castor roj (Cremophor RH40), 12% caprylic capric acid polyethylene glycol glyceride (Labrasol) ua co-emulsifier, thiab 50 mg·g-1 HPMC. Ntxiv HPMC rau SSEDDS tuaj yeem supersaturate dawb silibinin kom yaj hauv S-SEDDS thiab tiv thaiv silibinin los ntawm precipitating tawm. Piv nrog rau cov tshuaj self-microemulsion formulations, ib tug loj npaum li cas ntawm surfactant feem ntau yog ntxiv los tiv thaiv cov tshuaj tsis tiav encapsulation. Qhov sib ntxiv ntawm HPMC tuaj yeem ua kom cov solubility ntawm silibinin nyob rau hauv qhov nruab nrab dissolution kuj tsis tu ncua, txo cov emulsification hauv self-microemulsion formulations. dosage ntawm tus neeg sawv cev.
4. Cov lus xaus
Nws tuaj yeem pom tias HPMC tau siv dav hauv kev npaj vim nws lub cev, tshuaj lom neeg thiab cov khoom siv roj ntsha, tab sis HPMC kuj muaj ntau yam tsis txaus hauv kev npaj, xws li qhov tshwm sim ntawm kev tso tawm ua ntej thiab tom qab tawg. methyl methacrylate) los txhim kho. Tib lub sijhawm, qee cov kws tshawb fawb tau tshawb xyuas qhov kev thov ntawm osmotic txoj kev xav hauv HPMC los ntawm kev npaj carbamazepine sustained-tso ntsiav tshuaj thiab verapamil hydrochloride sustained-tso ntsiav tshuaj los kawm ntxiv txog nws txoj kev tso tawm. Hauv ib lo lus, ntau thiab ntau tus kws tshawb fawb tau ua ntau txoj haujlwm rau kev siv HPMC zoo dua hauv kev npaj, thiab nrog rau kev kawm tob ntawm nws cov khoom thiab kev txhim kho ntawm kev npaj technology, HPMC yuav tau siv ntau dua rau hauv cov ntawv noj tshuaj tshiab. thiab cov ntawv noj tshuaj tshiab. Hauv kev tshawb fawb ntawm kev siv tshuaj, thiab tom qab ntawd txhawb kev txhim kho kev lag luam txuas ntxiv.
Post lub sij hawm: Oct-08-2022