Daim Ntawv Thov Cov Tshuaj Excipients Hydroxypropyl Methyl Cellulose hauv Kev Npaj

Cov ntaub ntawv cuam tshuam hauv tsev thiab txawv teb chaws hauv kev npaj cov tshuaj hydroxypropyl methylcellulose (HPMC) xyoo tas los no tau raug tshuaj xyuas, tshuaj xyuas thiab sau ua ke, thiab nws daim ntawv thov hauv kev npaj khoom khov, kev npaj kua, kev npaj tso tawm thiab tswj kev tso tawm, kev npaj tshuaj ntsiav, gelatin. Cov ntawv thov tshiab hauv thaj chaw ntawm cov qauv tshiab xws li cov qauv nplaum thiab bioadhesives. Vim muaj qhov sib txawv ntawm qhov hnyav molecular thiab viscosity ntawm HPMC, nws muaj cov yam ntxwv thiab kev siv ntawm emulsification, adhesion, thickening, viscosity nce, suspending, gelling thiab zaj duab xis-tsim. Nws yog siv dav hauv kev npaj tshuaj thiab yuav ua lub luag haujlwm ntau dua hauv thaj chaw ntawm kev npaj. Nrog rau kev kawm tob txog nws cov khoom thiab kev txhim kho ntawm cov txheej txheem tsim, HPMC yuav siv dav dua hauv kev tshawb fawb ntawm cov ntawv tshuaj tshiab thiab cov txheej txheem xa tshuaj tshiab, yog li txhawb kev txhim kho tas mus li ntawm cov qauv.

hydroxypropyl methylcellulosecov tshuaj kho mob; cov tshuaj ntxiv rau tshuaj.

Cov tshuaj ntxiv tsis yog tsuas yog lub hauv paus rau kev tsim cov tshuaj nyoos xwb, tab sis kuj muaj feem cuam tshuam nrog qhov nyuaj ntawm cov txheej txheem npaj, qhov zoo ntawm cov tshuaj, kev ruaj khov, kev nyab xeeb, tus nqi tso tawm tshuaj, hom kev ua haujlwm, kev ua haujlwm hauv kev kho mob, thiab kev tsim cov ntawv tshuaj tshiab thiab cov kev tswj hwm tshiab. Muaj feem cuam tshuam ze. Kev tshwm sim ntawm cov tshuaj ntxiv tshiab feem ntau txhawb kev txhim kho qhov zoo ntawm kev npaj thiab kev tsim cov ntawv tshuaj tshiab. Hydroxypropyl methylcellulose (HPMC) yog ib qho ntawm cov tshuaj ntxiv nrov tshaj plaws hauv tsev thiab txawv teb chaws. Vim nws qhov sib txawv ntawm qhov hnyav molecular thiab viscosity, nws muaj cov haujlwm ntawm emulsifying, khi, thickening, thickening, suspending, thiab gluing. Cov yam ntxwv thiab kev siv xws li coagulation thiab zaj duab xis tsim tau siv dav hauv kev siv tshuab tshuaj. Tsab xov xwm no feem ntau tshuaj xyuas daim ntawv thov ntawm hydroxypropyl methylcellulose (HPMC) hauv cov qauv hauv xyoo tas los no.

1.Cov khoom tseem ceeb ntawm HPMC

Hydroxypropyl methyl cellulose (HPMC), cov mis molecular yog C8H15O8-(C10 H18O6) n-C8H15O8, thiab qhov hnyav molecular yog li 86 000. Cov khoom no yog cov khoom siv semi-synthetic, uas yog ib feem ntawm methyl thiab ib feem ntawm polyhydroxypropyl ether ntawm cellulose. Nws tuaj yeem tsim tau ob txoj hauv kev: Ib qho yog tias methyl cellulose ntawm qib tsim nyog raug kho nrog NaOH thiab tom qab ntawd reacted nrog propylene oxide nyob rau hauv qhov kub siab thiab siab siab. Lub sijhawm ua haujlwm yuav tsum kav ntev txaus kom tso cai rau methyl thiab hydroxypropyl los tsim cov ether bonds Nws txuas nrog lub nplhaib anhydroglucose ntawm cellulose hauv daim ntawv ntawm cellulose, thiab tuaj yeem ncav cuag qib xav tau; qhov thib ob yog kho paj rwb linter lossis ntoo pulp fiber nrog caustic soda, thiab tom qab ntawd react nrog chlorinated methane thiab propylene oxide ua ntu zus, thiab tom qab ntawd ntxiv refine nws. , crushed rau hauv cov hmoov zoo thiab sib xws lossis granules.

Cov khoom no xim dawb mus rau dawb mis nyuj, tsis muaj ntxhiab thiab tsis qab, thiab daim ntawv yog granular lossis fibrous hmoov yooj yim ntws. Cov khoom no tuaj yeem yaj hauv dej kom ua cov kua dej dawb dawb nrog qee qhov viscosity. Qhov xwm txheej sol-gel interconversion tuaj yeem tshwm sim vim qhov kub hloov pauv ntawm cov kua nrog qee qhov concentration.

Vim muaj qhov sib txawv ntawm cov ntsiab lus ntawm ob qho kev hloov pauv no hauv cov qauv ntawm methoxy thiab hydroxypropyl, ntau hom khoom tau tshwm sim. Hauv cov kev sib xyaw tshwj xeeb, ntau hom khoom muaj cov yam ntxwv tshwj xeeb. Viscosity thiab thermal gelation kub, yog li ntawd muaj cov khoom sib txawv thiab tuaj yeem siv rau ntau lub hom phiaj. Pharmacopoeia ntawm ntau lub tebchaws muaj cov kev cai sib txawv thiab kev sawv cev ntawm tus qauv: European Pharmacopoeia yog raws li ntau qib ntawm ntau yam viscosities thiab ntau qib ntawm kev hloov pauv ntawm cov khoom muag hauv kev ua lag luam, qhia los ntawm qib ntxiv rau cov lej, thiab chav tsev yog "mPa s". Hauv Tebchaws Meskas Pharmacopoeia, 4 tus lej ntxiv tom qab lub npe dav dav los qhia cov ntsiab lus thiab hom ntawm txhua tus neeg hloov pauv ntawm hydroxypropyl methylcellulose, xws li hydroxypropyl methylcellulose 2208. Ob tus lej thawj zaug sawv cev rau tus nqi kwv yees ntawm pawg methoxy. Feem pua, ob tus lej kawg sawv cev rau feem pua ​​kwv yees 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 ua zaj duab xis coatings, siv rau ntsiav tshuaj txheej, kaw ntsiav tshuaj cores; E, F series yog siv ua viscosifiers thiab tso tawm cov neeg sawv cev retarding rau ophthalmic npaj, suspending agents, thickeners rau kua npaj, ntsiav tshuaj thiab Binders ntawm granules; K series feem ntau yog siv ua tso tawm inhibitors thiab hydrophilic gel matrix cov ntaub ntawv rau qeeb thiab tswj kev tso tawm npaj.

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 Co., Ltd., Xi'an Huian chemical plants, thiab lwm yam.

2.Cov txiaj ntsig ntawm HPMC

HPMC tau dhau los ua ib qho ntawm cov tshuaj siv dav tshaj plaws hauv tsev thiab txawv teb chaws, vim tias HPMC muaj cov txiaj ntsig uas lwm cov tshuaj tsis muaj.

2.1 Kev yaj hauv dej txias

Yaj hauv dej txias hauv qab 40 ℃ lossis 70% ethanol, yeej tsis yaj hauv dej kub saum 60 ℃, tab sis tuaj yeem gel.

2.2 Tshuaj lom neeg tsis muaj zog

HPMC yog ib hom non-ionic cellulose ether, nws cov tshuaj tsis muaj ionic them thiab tsis cuam tshuam nrog cov ntsev hlau lossis cov organic ionic, yog li lwm cov tshuaj tsis cuam tshuam nrog nws thaum lub sijhawm tsim khoom ntawm kev npaj.

2.3 Kev Ruaj Ntseg

Nws ruaj khov rau ob qho tib si kua qaub thiab alkali, thiab tuaj yeem khaws cia ntev ntawm pH 3 thiab 11 yam tsis muaj kev hloov pauv tseem ceeb hauv viscosity. Cov kua dej ntawm HPMC muaj cov nyhuv tiv thaiv mildew thiab tswj tau qhov ruaj khov viscosity zoo thaum lub sijhawm khaws cia ntev. Cov tshuaj siv HPMC muaj qhov ruaj khov zoo dua li cov uas siv cov tshuaj ib txwm muaj (xws li dextrin, hmoov txhuv nplej siab, thiab lwm yam).

2.4 Kev Kho Kom Viscosity

Cov viscosity sib txawv ntawm HPMC tuaj yeem sib xyaw ua ke hauv cov feem 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.

2.5 Kev tsis muaj zog ntawm cov metabolism

HPMC tsis nqus lossis metabolized hauv lub cev, thiab tsis muab cua sov, yog li nws yog ib qho tshuaj muaj kev nyab xeeb. 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 tshuaj tua kab mob rau nas yog 5 g · kg - 1, thiab qhov nruab nrab ntawm cov tshuaj tua kab mob rau nas yog 5.2 g · kg - 1. Cov tshuaj txhua hnub tsis muaj teeb meem rau tib neeg lub cev.

3.Daim ntawv thov ntawm HPMC hauv cov qauv

3.1 Ua cov khoom siv txheej zaj duab xis thiab cov khoom siv tsim zaj duab xis

Siv HPMC ua cov khoom siv ntsiav tshuaj uas muaj txheej txheej, cov ntsiav tshuaj uas muaj txheej txheej tsis muaj qhov zoo pom tseeb hauv kev zais qhov saj thiab qhov tsos piv rau cov ntsiav tshuaj uas muaj txheej txheej ib txwm muaj xws li cov ntsiav tshuaj uas muaj txheej txheej qab zib, tab sis nws qhov nyuaj, kev yooj yim tawg, kev nqus dej noo, qib kev tawg, qhov hnyav nce thiab lwm yam ntsuas zoo dua. Qib qis-viscosity ntawm cov khoom no yog siv los ua cov khoom siv txheej txheej zaj duab xis uas yaj tau hauv dej rau cov ntsiav tshuaj thiab cov ntsiav tshuaj, thiab qib siab-viscosity yog siv los ua cov khoom siv txheej txheej zaj duab xis rau cov txheej txheem organic solvent, feem ntau ntawm qhov concentration ntawm 2% txog 20%.

Zhang Jixing thiab lwm tus tau siv txoj kev siv qhov chaw los ua kom cov tshuaj premix zoo dua qub nrog HPMC ua cov txheej txheej zaj duab xis. Siv cov khoom siv ua zaj duab xis HPMC, qhov ntau ntawm polyvinyl cawv thiab plasticizer polyethylene glycol ua cov yam tseem ceeb tshawb nrhiav, lub zog tensile thiab permeability ntawm zaj duab xis thiab viscosity ntawm cov tshuaj txheej zaj duab xis yog qhov ntsuas kev tshuaj xyuas, thiab kev sib raug zoo ntawm qhov ntsuas kev tshuaj xyuas thiab cov yam tseem ceeb tshuaj xyuas tau piav qhia los ntawm tus qauv lej, thiab thaum kawg tau txais cov txheej txheem tsim zoo tshaj plaws. Nws siv yog tus neeg sawv cev ua zaj duab xis hydroxypropyl methylcellulose (HPMCE5) 11.88 g, polyvinyl cawv 24.12 g, plasticizer polyethylene glycol 13.00 g, thiab viscosity ntawm cov txheej txheem ncua yog 20 mPa · s, permeability thiab tensile zog ntawm zaj duab xis tau txais txiaj ntsig zoo tshaj plaws. Zhang Yuan txhim kho cov txheej txheem npaj, siv HPMC ua cov khoom siv los hloov cov hmoov txhuv nplej siab, thiab hloov Jiahua ntsiav tshuaj mus rau cov ntsiav tshuaj txheej zaj duab xis los txhim kho qhov zoo ntawm nws cov kev npaj, txhim kho nws cov hygroscopicity, yooj yim ploj, ntsiav tshuaj xoob, tawg thiab lwm yam teeb meem, txhim kho kev ruaj khov ntawm ntsiav tshuaj. Cov txheej txheem tsim cov tshuaj zoo tshaj plaws tau txiav txim siab los ntawm kev sim orthogonal, uas yog, qhov concentration ntawm slurry yog 2% HPMC hauv 70% ethanol kua thaum lub sijhawm txheej, thiab lub sijhawm do thaum lub sijhawm granulation yog 15 feeb. Cov txiaj ntsig Cov ntsiav tshuaj Jiahua zaj duab xis-txheej uas tau npaj los ntawm cov txheej txheem tshiab thiab daim ntawv qhia tshuaj tau zoo dua qub hauv qhov tsos, lub sijhawm tawg thiab lub zog ntawm lub hauv paus dua li cov uas tau tsim los ntawm cov txheej txheem tshuaj thawj zaug, thiab tus nqi tsim nyog ntawm cov ntsiav tshuaj zaj duab xis-txheej tau zoo dua qub. ncav cuag ntau dua 95%. Liang Meiyi, Lu Xiaohui, thiab lwm yam kuj tau siv hydroxypropyl methylcellulose ua cov khoom siv ua zaj duab xis los npaj cov ntsiav tshuaj patinae colon positioning thiab cov ntsiav tshuaj matrine colon positioning, feem. cuam tshuam rau kev tso tshuaj. Huang Yunran tau npaj Dragon's Blood Colon Positioning Tablets, thiab siv HPMC rau cov tshuaj txheej ntawm cov txheej o, thiab nws cov feem pua ​​​​​​ntawm qhov hnyav yog 5%. Nws tuaj yeem pom tias HPMC tuaj yeem siv dav hauv cov txheej txheem xa tshuaj rau lub plab hnyuv.

Hydroxypropyl methylcellulose tsis yog tsuas yog cov khoom siv zoo heev rau txheej zaj duab xis xwb, tab sis kuj siv tau ua cov khoom siv tsim zaj duab xis hauv cov qauv zaj duab xis. Wang Tongshun thiab lwm yam tau tsim kho kom zoo rau kev sau cov tshuaj zinc licorice thiab aminolexanol hauv qhov ncauj zaj duab xis sib xyaw, nrog rau kev ywj pheej, kev sib npaug, kev du, thiab kev pom tseeb ntawm tus neeg sawv cev zaj duab xis ua qhov ntsuas kev tshawb nrhiav, tau txais cov tshuaj zoo tshaj plaws 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 kom qeeb thiab kev nyab xeeb, thiab tuaj yeem siv ua cov tshuaj npaj ntawm zaj duab xis sib xyaw.

3.2 ua tus binder thiab disintegrant

Cov khoom no qib viscosity qis siv tau ua cov khoom sib txuas thiab cov khoom tawg rau cov ntsiav tshuaj, tshuaj ntsiav thiab granules, thiab qib viscosity siab tsuas yog siv tau ua cov khoom sib txuas. Cov koob tshuaj sib txawv nrog ntau hom qauv thiab cov kev xav tau. Feem ntau, cov koob tshuaj ntawm cov khoom sib txuas rau cov ntsiav tshuaj granulation qhuav yog 5%, thiab cov koob tshuaj ntawm cov khoom sib txuas rau cov ntsiav tshuaj granulation ntub yog 2%.

Li Houtao thiab lwm tus tau tshuaj xyuas cov khoom sib txuas ntawm cov ntsiav tshuaj tinidazole. 8% polyvinylpyrrolidone (PVP-K30), 40% kua txiv hmab txiv ntoo, 10% hmoov txhuv nplej siab, 2.0% hydroxypropyl methylcellulose K4 (HPMCK4M), 50% ethanol tau raug tshuaj xyuas raws li qhov sib txuas ntawm cov ntsiav tshuaj tinidazole. Kev npaj cov ntsiav tshuaj tinidazole. Kev hloov pauv ntawm cov ntsiav tshuaj dawb thiab tom qab txheej tau muab piv rau, thiab qhov friability, hardness, disintegration lub sijhawm txwv thiab disintegration tus nqi ntawm cov ntsiav tshuaj sib txawv tau ntsuas. Cov txiaj ntsig Cov ntsiav tshuaj uas npaj los ntawm 2.0% hydroxypropyl methylcellulose yog glossy, thiab kev ntsuas friability tsis pom muaj ntug chipping thiab cornering tshwm sim, thiab tom qab txheej, cov duab ntsiav tshuaj tiav thiab qhov zoo li zoo. Yog li ntawd, cov ntsiav tshuaj tinidazole npaj nrog 2.0% HPMC-K4 thiab 50% ethanol ua cov khoom sib txuas tau siv. Guan Shihai kawm txog cov txheej txheem tsim cov ntsiav tshuaj Fuganning, tshuaj xyuas cov nplaum, thiab tshuaj xyuas 50% ethanol, 15% hmoov txhuv nplej siab, 10% PVP thiab 50% ethanol daws nrog compressibility, smoothness, thiab friability ua cov ntsuas kev ntsuam xyuas. , 5% CMC-Na thiab 15% HPMC kua (5 mPa s). Cov txiaj ntsig Cov ntawv npaj los ntawm 50% ethanol, 15% hmoov txhuv nplej siab, 10% PVP 50% ethanol kua thiab 5% CMC-Na muaj qhov chaw du, tab sis tsis zoo compressibility thiab qis hardness, uas tsis tuaj yeem ua tau raws li qhov xav tau ntawm txheej; 15% HPMC kua (5 mPa · s), qhov chaw ntawm lub ntsiav tshuaj yog du, qhov friability yog tsim nyog, thiab qhov compressibility yog zoo, uas tuaj yeem ua tau raws li qhov xav tau ntawm txheej. Yog li ntawd, HPMC (5 mPa s) tau raug xaiv los ua cov nplaum.

3.3 ua tus neeg sawv cev ncua

Cov khoom no qib viscosity siab siv ua tus neeg sawv cev rau kev npaj cov kua dej uas raug ncua. Nws muaj cov nyhuv zoo rau kev ncua, yooj yim rau kev tawg dua, tsis lo rau ntawm phab ntsa, thiab muaj cov khoom me me. Cov tshuaj ib txwm muaj yog 0.5% txog 1.5%. Song Tian et al. siv cov khoom siv polymer feem ntau (hydroxypropyl methylcellulose, sodium carboxymethylcellulose, povidone, xanthan gum, methylcellulose, thiab lwm yam) ua cov neeg sawv cev rau kev ncua los npaj racecadotril. kev ncua qhuav. Los ntawm qhov piv ntawm cov dej ntws ntawm cov kev ncua sib txawv, qhov ntsuas kev tawg dua, thiab rheology, kev ncua viscosity thiab microscopic morphology tau pom, thiab qhov ruaj khov ntawm cov tshuaj me me hauv qab kev sim ceev kuj tau tshawb xyuas. Cov txiaj ntsig Kev ncua qhuav npaj nrog 2% HPMC ua tus neeg sawv cev rau kev ncua muaj cov txheej txheem yooj yim thiab ruaj khov zoo.

Piv nrog methyl cellulose, hydroxypropyl methyl cellulose muaj cov yam ntxwv ntawm kev tsim cov tshuaj meej dua, thiab tsuas yog muaj me me ntawm cov tshuaj fibrous uas tsis tawg, yog li HPMC kuj tseem siv tau ua tus neeg sawv cev rau kev ncua hauv kev npaj qhov muag. Liu Jie et al. siv HPMC, hydroxypropyl cellulose (HPC), carbomer 940, polyethylene glycol (PEG), sodium hyaluronate (HA) thiab kev sib xyaw ntawm HA / HPMC ua cov neeg sawv cev ncua los npaj cov lus qhia sib txawv Rau Ciclovir ophthalmic suspension, sedimentation ntim piv, qhov loj me ntawm cov khoom me me thiab redispersibility raug xaiv ua cov ntsuas kev tshuaj xyuas los tshuaj xyuas tus neeg sawv cev ncua zoo tshaj plaws. Cov txiaj ntsig qhia tau hais tias acyclovir ophthalmic suspension npaj los ntawm 0.05% HA thiab 0.05% HPMC ua tus neeg sawv cev ncua, qhov sib piv ntawm sedimentation ntim yog 0.998, qhov loj me ntawm cov khoom me me yog sib xws, qhov redispersibility zoo, thiab kev npaj ruaj khov.

3.4 Ua ib qho blocker, qeeb thiab tswj tau tus neeg sawv cev tso tawm thiab tus neeg sawv cev tsim cov qhov hws

Cov khoom no qib siab viscosity yog siv rau kev npaj cov hydrophilic gel matrix sustained-release tablets, blockers thiab tswj-tso cov neeg sawv cev ntawm cov khoom sib xyaw matrix sustained-release tablets, thiab muaj cov nyhuv ntawm kev ncua kev tso tshuaj. Nws qhov concentration yog 10% txog 80%. Cov qib qis viscosity yog siv ua porogens rau kev tso tshuaj lossis tswj-tso tshuaj. Cov koob tshuaj thawj zaug xav tau rau cov txiaj ntsig kho mob ntawm cov ntsiav tshuaj no tuaj yeem ncav cuag sai, thiab tom qab ntawd qhov kev tso tshuaj lossis tswj-tso tshuaj raug siv, thiab qhov concentration ntawm cov tshuaj ntshav zoo tau khaws cia hauv lub cev. . Hydroxypropyl methylcellulose yog hydrated los tsim ib txheej gel thaum nws ntsib dej. Lub tshuab ntawm cov tshuaj tso tawm los ntawm cov ntsiav tshuaj matrix feem ntau suav nrog kev sib kis ntawm cov txheej gel thiab kev puas tsuaj ntawm cov txheej gel. Jung Bo Shim et al tau npaj cov ntsiav tshuaj carvedilol sustained-release nrog HPMC ua cov khoom tso tshuaj.

Hydroxypropyl methylcellulose kuj siv dav hauv cov ntsiav tshuaj matrix uas tso tawm tas mus li ntawm cov tshuaj suav tshuaj, thiab feem ntau ntawm cov khoom xyaw nquag, cov khoom siv zoo thiab cov tshuaj ib zaug ntawm cov tshuaj suav tshuaj tau siv. Liu Wen et al. siv 15% hydroxypropyl methylcellulose ua cov khoom siv matrix, 1% lactose thiab 5% microcrystalline cellulose ua cov khoom sau, thiab npaj Jingfang Taohe Chengqi Decoction rau hauv cov ntsiav tshuaj matrix uas tso tawm tas mus li. Tus qauv yog Higuchi equation. Lub kaw lus sib xyaw ua ke yooj yim, kev npaj yooj yim, thiab cov ntaub ntawv tso tawm ruaj khov, uas ua tau raws li qhov yuav tsum tau ua ntawm Suav Pharmacopoeia. Tang Guanguang et al. siv tag nrho cov saponins ntawm Astragalus ua cov qauv tshuaj, npaj cov ntsiav tshuaj HPMC matrix, thiab tshawb nrhiav cov yam ntxwv cuam tshuam rau kev tso tawm tshuaj los ntawm cov khoom siv zoo ntawm cov tshuaj suav tshuaj hauv cov ntsiav tshuaj HPMC matrix. Cov txiaj ntsig Raws li qhov ntau npaum li cas ntawm HPMC nce ntxiv, kev tso tawm ntawm astragaloside txo qis, thiab feem pua ​​​​​​ntawm kev tso tawm ntawm cov tshuaj muaj kev sib raug zoo ze li ntawm kab nrog qhov nrawm ntawm cov matrix. Hauv cov ntsiav tshuaj hypromellose HPMC matrix, muaj qee qhov kev sib raug zoo ntawm kev tso tawm ntawm qhov zoo ntawm cov tshuaj suav tshuaj thiab cov koob tshuaj thiab hom HPMC, thiab cov txheej txheem tso tawm ntawm cov tshuaj hydrophilic monomer zoo ib yam li nws. Hydroxypropyl methylcellulose tsis yog tsuas yog tsim rau cov tshuaj hydrophilic xwb, tab sis kuj rau cov tshuaj tsis yog hydrophilic. Liu Guihua siv 17% hydroxypropyl methylcellulose (HPMCK15M) ua cov khoom siv matrix tso tawm tas mus li, thiab npaj Tianshan Xuelian cov ntsiav tshuaj matrix tso tawm tas mus li los ntawm kev ntub dej granulation thiab tableting txoj kev. Cov nyhuv tso tawm tas mus li yog qhov pom tseeb, thiab cov txheej txheem npaj tau ruaj khov thiab ua tau.

Hydroxypropyl methylcellulose tsis yog tsuas yog siv rau cov ntsiav tshuaj matrix uas tso tawm tas mus li ntawm cov khoom xyaw nquag thiab cov khoom siv zoo ntawm cov tshuaj suav ib txwm muaj, tab sis kuj siv ntau dua thiab ntau dua hauv kev npaj tshuaj suav ib txwm muaj. Wu Huichao et al. siv 20% hydroxypropyl methyl cellulose (HPMCK4M) ua cov khoom siv matrix, thiab siv txoj kev nias hmoov ncaj qha los npaj Yizhi hydrophilic gel matrix ntsiav tshuaj uas tuaj yeem tso cov tshuaj tas mus li thiab ruaj khov rau 12 teev. Saponin Rg1, ginsenoside Rb1 thiab Panax notoginseng saponin R1 tau siv ua cov ntsuas kev ntsuas los tshawb xyuas qhov kev tso tawm hauv vitro, thiab cov kab zauv tso tawm tshuaj tau teeb tsa los kawm txog cov txheej txheem tso tawm tshuaj. Cov txiaj ntsig Cov txheej txheem tso tawm tshuaj tau ua raws li cov kab zauv kinetic xoom thiab cov kab zauv Ritger-Peppas, uas geniposide tau tso tawm los ntawm kev sib kis tsis yog Fick, thiab peb yam khoom hauv Panax notoginseng tau tso tawm los ntawm kev tawg pob txha.

3.5 Cov kua nplaum tiv thaiv ua cov khoom ua kom tuab thiab colloid

Thaum siv cov khoom no ua cov khoom ua kom tuab, feem pua ​​​​​​ntawm cov khoom siv feem ntau yog 0.45% txog 1.0%. Nws kuj tseem tuaj yeem ua rau kom cov kua nplaum hydrophobic ruaj khov, tsim cov colloid tiv thaiv, tiv thaiv cov khoom me me los ntawm kev sib sau ua ke thiab sib sau ua ke, yog li ntawd txwv tsis pub tsim cov av noo. Nws feem pua ​​​​​​ntawm cov khoom siv feem ntau yog 0.5% txog 1.5%.

Wang Zhen thiab lwm tus tau siv txoj kev tsim qauv L9 orthogonal los tshawb nrhiav cov txheej txheem npaj cov tshuaj enema uas ua los ntawm cov pa roj carbon. Cov xwm txheej zoo tshaj plaws rau kev txiav txim siab zaum kawg ntawm cov tshuaj enema uas ua los ntawm cov pa roj carbon yog siv 0.5% sodium carboxymethyl cellulose thiab 2.0% hydroxypropyl methylcellulose (HPMC muaj 23.0% methoxyl pawg, hydroxypropoxyl Base 11.6%) ua cov khoom ua kom tuab, cov xwm txheej ntawm cov txheej txheem pab txhim kho kev ruaj khov ntawm cov tshuaj activated carbon. Zhang Zhiqiang thiab lwm tus tau tsim cov tshuaj gel uas rhiab heev rau pH levofloxacin hydrochloride ophthalmic npaj siv nrog cov nyhuv tso tawm tas mus li, siv carbopol ua cov gel matrix thiab hydroxypropyl methylcellulose ua cov khoom ua kom tuab. Los ntawm kev sim tshuaj, thaum kawg tau txais cov tshuaj zoo tshaj plaws yog levofloxacin hydrochloride 0.1 g, carbopol (9400) 3 g, hydroxypropyl methylcellulose (E50 LV) 20 g, disodium hydrogen phosphate 0.35 g, phosphoric acid 0.45 g ntawm sodium dihydrogen, 0.50 g ntawm sodium chloride, 0.03 g ntawm ethyl paraben, thiab dej tau ntxiv rau 100 mL. Hauv kev sim, tus sau tau tshuaj xyuas cov koob hydroxypropyl methylcellulose METHOCEL ntawm Colorcon Company nrog cov lus qhia sib txawv (K4M, E4M, E15 LV, E50LV) los npaj cov thickeners nrog ntau qhov sib txawv, thiab qhov tshwm sim tau xaiv HPMC E50 LV ua cov thickener. Cov thickener rau pH-sensitive levofloxacin hydrochloride instant gels.

3.6 ua cov khoom siv capsule

Feem ntau, cov khoom siv ntawm lub plhaub capsule ntawm cov tshuaj capsule feem ntau yog gelatin. Cov txheej txheem tsim cov plhaub capsule yooj yim, tab sis muaj qee qhov teeb meem thiab cov xwm txheej xws li kev tiv thaiv tsis zoo tiv thaiv cov dej noo thiab cov tshuaj uas rhiab rau oxygen, txo cov tshuaj yaj, thiab qeeb qeeb ntawm lub plhaub capsule thaum khaws cia. Yog li ntawd, hydroxypropyl methylcellulose yog siv los hloov cov tshuaj gelatin rau kev npaj cov tshuaj capsule, uas txhim kho qhov ua tau ntawm kev tsim cov tshuaj capsule thiab cov txiaj ntsig siv, thiab tau txhawb nqa dav hauv tsev thiab txawv teb chaws.

Siv theophylline ua tshuaj tswj, Podczeck et al. pom tias qhov nrawm ntawm kev yaj tshuaj ntawm cov tshuaj ntsiav nrog hydroxypropyl methylcellulose plhaub yog ntau dua li ntawm cov tshuaj ntsiav gelatin. Qhov laj thawj rau kev tshuaj xyuas yog tias qhov kev tawg ntawm HPMC yog qhov kev tawg ntawm tag nrho cov tshuaj ntsiav tib lub sijhawm, thaum qhov kev tawg ntawm cov tshuaj ntsiav gelatin yog qhov kev tawg ntawm cov qauv network ua ntej, thiab tom qab ntawd qhov kev tawg ntawm tag nrho cov tshuaj ntsiav, yog li HPMC capsule yog qhov tsim nyog dua rau Capsule plhaub rau cov qauv tso tawm tam sim ntawd. Chiwele et al. kuj tau txais cov lus xaus zoo sib xws thiab piv rau qhov kev yaj ntawm gelatin, gelatin / polyethylene glycol thiab HPMC plhaub. Cov txiaj ntsig tau qhia tias HPMC plhaub tau yaj sai sai hauv qab cov xwm txheej pH sib txawv, thaum cov tshuaj ntsiav gelatin Nws raug cuam tshuam loj heev los ntawm cov xwm txheej pH sib txawv. Tang Yue et al. tshuaj xyuas hom tshiab ntawm cov tshuaj ntsiav plhaub rau cov tshuaj tsawg-koob dawb qhuav hmoov inhaler carrier system. Piv nrog rau lub plhaub capsule ntawm hydroxypropyl methylcellulose thiab lub plhaub capsule ntawm gelatin, qhov ruaj khov ntawm lub plhaub capsule thiab cov khoom ntawm cov hmoov hauv lub plhaub nyob rau hauv ntau yam mob tau raug tshawb nrhiav, thiab qhov kev sim friability tau ua tiav. Cov txiaj ntsig qhia tau tias piv nrog cov tshuaj ntsiav gelatin, HPMC capsule plhaub zoo dua hauv kev ruaj khov thiab kev tiv thaiv hmoov, muaj zog tiv thaiv dej noo, thiab muaj qhov friability qis dua li cov plhaub gelatin capsule, yog li HPMC capsule plhaub zoo dua rau Capsules rau kev nqus hmoov qhuav.

3.7 ua ib qho bioadhesive

Cov thev naus laus zis bioadhesion siv cov khoom xyaw nrog cov polymers bioadhesive. Los ntawm kev lo rau ntawm cov mucosa ntawm lub cev, nws ua rau muaj kev sib txuas thiab nruj ntawm kev sib cuag ntawm cov tshuaj thiab cov mucosa, yog li cov tshuaj maj mam tso tawm thiab nqus los ntawm cov mucosa kom ua tiav lub hom phiaj ntawm kev kho mob. Nws yog siv dav tam sim no. Kev kho mob ntawm cov kab mob ntawm txoj hnyuv plab, qhov chaw mos, qhov ncauj mucosa thiab lwm qhov chaw.

Kev siv tshuab bioadhesion hauv plab yog ib txoj kev xa tshuaj tshiab uas tau tsim nyob rau xyoo tas los no. Nws tsis tsuas yog ua kom lub sijhawm nyob ntev ntawm cov tshuaj hauv txoj hnyuv plab xwb, tab sis kuj txhim kho kev ua haujlwm ntawm kev sib cuag ntawm cov tshuaj thiab lub cell membrane ntawm qhov chaw nqus, hloov qhov fluidity ntawm lub cell membrane, thiab ua rau qhov nkag mus ntawm cov tshuaj mus rau hauv cov hlwb epithelial me me ntawm txoj hnyuv tau txhim kho, yog li txhim kho qhov bioavailability ntawm cov tshuaj. Wei Keda et al. tau tshuaj xyuas cov tshuaj ntsiav nrog cov koob tshuaj ntawm HPMCK4M thiab Carbomer 940 ua cov yam ntxwv tshawb nrhiav, thiab siv cov khoom siv bioadhesion ua tus kheej los ntsuas lub zog tev ntawm cov tshuaj ntsiav thiab cov biofilm simulated los ntawm qhov zoo ntawm cov dej hauv lub hnab yas. , thiab thaum kawg xaiv cov ntsiab lus ntawm HPMCK40 thiab carbomer 940 kom yog 15 thiab 27.5 mg hauv thaj chaw zoo tshaj plaws 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 txhim kho qhov kev nplaum ntawm kev npaj rau cov ntaub so ntswg.

Cov tshuaj bioadhesive hauv qhov ncauj kuj yog ib hom tshuaj tshiab uas tau kawm ntau dua nyob rau xyoo tas los no. Cov tshuaj bioadhesive hauv qhov ncauj tuaj yeem lo cov tshuaj rau ntawm qhov chaw mob ntawm lub qhov ncauj, uas tsis yog tsuas yog ua kom lub sijhawm nyob ntawm cov tshuaj hauv qhov ncauj ntev dua, tab sis kuj tiv thaiv cov mucosa hauv qhov ncauj. Cov txiaj ntsig kho mob zoo dua thiab txhim kho kev siv tshuaj. Xue Xiaoyan et al. tau ua kom zoo dua cov tshuaj insulin hauv qhov ncauj, siv cov kua txiv 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. Cov ntawv nplaum ob txheej. Cov tshuaj insulin hauv qhov ncauj uas tau npaj muaj cov qauv zoo li daim txhuam cev, uas zoo rau kev tso insulin, thiab muaj txheej tiv thaiv hydrophobic, uas tuaj yeem ua kom cov tshuaj tso tawm ib txoj kev thiab zam kev poob ntawm cov tshuaj. Hao Jifu et al. kuj tau npaj cov hlaws xiav-daj hauv qhov ncauj bioadhesive daim ntawv siv Baiji kua nplaum, HPMC thiab carbomer ua cov khoom siv bioadhesive.

Hauv cov txheej txheem xa tshuaj rau qhov chaw mos, cov thev naus laus zis bioadhesion kuj tau siv dav. Zhu Yuting et al. siv carbomer (CP) thiab HPMC ua cov ntaub ntawv nplaum thiab cov khoom siv tso tawm kom ruaj khov los npaj cov ntsiav tshuaj clotrimazole bioadhesive vaginal nrog cov qauv sib txawv thiab qhov sib piv, thiab ntsuas lawv qhov kev nplaum, lub sijhawm nplaum thiab feem pua ​​​​​​ntawm o hauv qhov chaw ib puag ncig ntawm cov kua dej cuav. , daim ntawv sau tshuaj tsim nyog tau kuaj xyuas raws li CP-HPMC1: 1, daim ntawv nplaum uas tau npaj muaj kev ua tau zoo nplaum, thiab cov txheej txheem yooj yim thiab ua tau.

3.8 ua ib qho gel sab nraud

Ua ib qho kev npaj nplaum, gel muaj ntau yam zoo xws li kev nyab xeeb, kev zoo nkauj, kev ntxuav yooj yim, tus nqi qis, cov txheej txheem npaj yooj yim, thiab kev sib raug zoo nrog cov tshuaj. Kev taw qhia ntawm kev txhim kho. Piv txwv li, transdermal gel yog daim ntawv tshuaj tshiab uas tau kawm ntau dua hauv xyoo tas los no. Nws tsis tsuas yog zam kev puas tsuaj ntawm cov tshuaj hauv txoj hnyuv plab thiab txo qhov sib txawv ntawm cov tshuaj ntshav siab, tab sis kuj tau dhau los ua ib qho ntawm cov txheej txheem tso tawm tshuaj zoo los kov yeej cov kev phiv tshuaj.

Zhu Jingjie et al. tau kawm txog cov nyhuv ntawm cov matrices sib txawv ntawm kev tso tawm ntawm scutellarin cawv plastid gel hauv vitro, thiab tshuaj xyuas 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 ntawm kev sim qhia tau tias 1. 0% carbomer, 1. 5% carbomer, 1. 0% carbomer + 1. 0% HPMC, 1. 5% carbomer + 1. 0% HPMC ua gel matrix Ob qho tib si haum rau scutellarin cawv plastids. Thaum lub sijhawm sim, nws tau pom tias HPMC tuaj yeem hloov hom kev tso tawm tshuaj ntawm carbomer gel matrix los ntawm kev haum rau qhov sib npaug kinetic ntawm kev tso tawm tshuaj, thiab 1.0% HPMC tuaj yeem txhim kho 1.0% carbomer matrix thiab 1.5% carbomer matrix. Qhov laj thawj yuav yog vim HPMC nthuav dav sai dua, thiab qhov nthuav dav sai sai thaum ntxov ntawm 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 dua. Zhao Wencui et al. siv carbomer-934 thiab hydroxypropyl methylcellulose ua cov khoom nqa khoom los npaj norfloxacin ophthalmic gel. Cov txheej txheem npaj yog yooj yim thiab ua tau, thiab qhov zoo ua raws li ophthalmic gel ntawm "Suav Pharmacopoeia" (2010 tsab) Cov kev cai zoo.

3.9 Cov tshuaj tiv thaiv nag lossis daus rau lub kaw lus microemulsifying tus kheej

Lub tshuab xa tshuaj uas siv cov tshuaj microemulsifying los ntawm tus kheej (SMEDDS) yog ib hom tshiab ntawm lub tshuab xa tshuaj hauv qhov ncauj, uas yog ib qho sib xyaw ua ke, ruaj khov thiab pob tshab uas muaj cov tshuaj, roj theem, emulsifier thiab co-emulsifier. Cov khoom xyaw ntawm daim ntawv sau tshuaj yooj yim, thiab kev nyab xeeb thiab kev ruaj khov zoo. Rau cov tshuaj uas yaj tsis tau zoo, cov khoom siv polymer fiber uas yaj tau hauv dej, xws li HPMC, polyvinylpyrrolidone (PVP), thiab lwm yam, feem ntau raug ntxiv rau kom cov tshuaj dawb thiab cov tshuaj uas nyob hauv microemulsion ua tiav cov tshuaj yaj tau zoo hauv txoj hnyuv plab, kom ua rau cov tshuaj yaj tau zoo dua thiab txhim kho kev siv tau.

Peng Xuan thiab lwm tus tau npaj ib lub tshuab xa tshuaj silibinin supersaturated self-emulsifying (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 ua rau cov silibinin dawb supersaturated yaj hauv S-SEDDS thiab tiv thaiv silibinin los ntawm kev tawm. Piv nrog rau cov qauv tshuaj microemulsion ib txwm muaj, feem ntau ntxiv ntau cov surfactant kom tiv thaiv cov tshuaj tsis tiav. Kev ntxiv HPMC tuaj yeem ua rau cov solubility ntawm silibinin hauv cov tshuaj yaj tas li, txo cov emulsification hauv cov qauv tshuaj microemulsion.

4. Xaus Lus

Nws tuaj yeem pom tias HPMC tau siv dav hauv kev npaj vim nws lub cev, tshuaj lom neeg thiab cov khoom siv hauv lub cev, tab sis HPMC kuj muaj ntau qhov tsis txaus hauv kev npaj, xws li qhov tshwm sim ntawm kev tso tawm ua ntej thiab tom qab tawg. methyl methacrylate) kom txhim kho. Tib lub sijhawm, qee tus kws tshawb fawb tau tshawb nrhiav kev siv osmotic theory hauv HPMC los ntawm kev npaj carbamazepine cov ntsiav tshuaj tso tawm thiab verapamil hydrochloride cov ntsiav tshuaj tso tawm kom kawm ntxiv txog nws cov txheej txheem tso tawm. Hauv ib lo lus, ntau thiab ntau tus kws tshawb fawb tab tom ua ntau yam haujlwm rau kev siv zoo dua ntawm HPMC hauv kev npaj, thiab nrog kev kawm tob txog nws cov khoom thiab kev txhim kho ntawm kev npaj thev naus laus zis, HPMC yuav siv dav dua hauv cov ntawv tshuaj tshiab thiab cov ntawv tshuaj tshiab. Hauv kev tshawb fawb ntawm cov txheej txheem tshuaj, thiab tom qab ntawd txhawb kev txhim kho tas mus li ntawm cov khw muag tshuaj.


Lub sijhawm tshaj tawm: Lub Kaum Hli-08-2022