Muaj pes tsawg Cellulose ethers hauv cov tshuaj excipients?

Cov tshuaj ntxiv yog cov tshuaj ntxiv thiab cov tshuaj ntxiv siv rau hauv kev tsim tshuaj thiab tsim cov tshuaj, thiab yog ib feem tseem ceeb ntawm kev npaj tshuaj. Raws li cov khoom siv polymer ntuj tsim, cellulose ether muaj cov yam ntxwv ntawm biodegradability, tsis muaj tshuaj lom, thiab tus nqi qis, xws li sodium carboxymethyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl cellulose,Cov cellulose ethersxws li hydroxyethyl cellulose thiab ethyl cellulose muaj cov txiaj ntsig tseem ceeb hauv kev siv tshuaj. Tam sim no, cov khoom lag luam ntawm feem ntau cov tuam txhab cellulose ether hauv tsev feem ntau yog siv rau hauv cov teb nruab nrab thiab qis kawg ntawm kev lag luam, thiab tus nqi ntxiv tsis siab. Kev lag luam xav tau kev hloov pauv sai thiab txhim kho thiab txhim kho cov ntawv thov siab ntawm cov khoom.

Cov tshuaj ntxiv ua lub luag haujlwm tseem ceeb hauv kev tsim thiab tsim cov tshuaj. Piv txwv li, hauv kev npaj tshuaj uas tso tawm tas mus li, cov khoom siv polymer xws li cellulose ethers yog siv los ua cov tshuaj ntxiv hauv cov pellets uas tso tawm tas mus li, ntau yam matrix uas tso tawm tas mus li, cov tshuaj uas muaj txheej txheem tso tawm tas mus li, cov tshuaj ntsiav uas tso tawm tas mus li, cov yeeb yaj kiab tshuaj uas tso tawm tas mus li, thiab cov tshuaj uas tso tawm tas mus li. Cov tshuaj npaj thiab cov tshuaj uas tso tawm tas mus li tau siv dav. Hauv lub kaw lus no, cov polymers xws li cellulose ethers feem ntau yog siv los ua cov tshuaj nqa khoom los tswj cov tshuaj tso tawm hauv lub cev tib neeg, uas yog, lawv yuav tsum tau tso tawm maj mam hauv lub cev ntawm tus nqi teem tseg hauv ib lub sijhawm tshwj xeeb kom ua tiav lub hom phiaj ntawm kev kho mob zoo.

Raws li cov ntaub ntawv ntawm Lub Tsev Haujlwm Saib Xyuas Kev Pab Tswv Yim thiab Kev Tshawb Fawb, muaj li ntawm 500 hom tshuaj ntxiv rau hauv kev ua lag luam hauv kuv lub tebchaws, tab sis piv rau Tebchaws Meskas (ntau dua 1500 hom) thiab European Union (ntau dua 3000 hom), muaj qhov sib txawv loj, thiab cov hom tseem me me. kuv lub tebchaws cov tshuaj ntxiv Lub peev xwm tsim kho ntawm kev ua lag luam yog loj heev. Nws nkag siab tias kaum cov tshuaj ntxiv rau hauv kev ua lag luam ntawm kuv lub tebchaws yog cov tshuaj gelatin capsules, sucrose, hmoov txhuv nplej siab, zaj duab xis txheej hmoov, 1,2-propylene glycol, PVP, hydroxypropyl methylcellulose (HPMC), thiab microcrystalline fibers. Vegetarian, HPC, lactose.

"Natural cellulose ether yog lub ntsiab lus dav dav rau cov cellulose derivatives tsim los ntawm cov tshuaj tiv thaiv ntawm alkali cellulose thiab etherifying tus neeg sawv cev nyob rau hauv qee qhov xwm txheej, thiab yog cov khoom uas cov hydroxyl pawg ntawm cellulose macromolecule yog ib feem lossis tag nrho hloov los ntawm ether pawg. Cellulose ethers yog siv dav hauv cov teb ntawm roj av, cov ntaub ntawv tsim kho, coatings, khoom noj, tshuaj thiab cov tshuaj txhua hnub. Hauv txhua qhov teb, cov khoom lag luam tshuaj-qib yog qhov tseem ceeb hauv nruab nrab thiab qib siab ntawm kev lag luam thiab muaj tus nqi ntxiv siab. Vim yog qhov yuav tsum tau ua kom zoo, kev tsim cov tshuaj-qib cellulose ethers kuj nyuaj heev. Nws tuaj yeem hais tias qhov zoo ntawm cov khoom lag luam tshuaj-qib tuaj yeem sawv cev rau lub zog ntawm cov tuam txhab cellulose ether. Cellulose ether feem ntau yog ntxiv ua tus retarder, cov khoom siv matrix thiab thickener los ua cov ntsiav tshuaj matrix uas tso tawm tas mus li, cov ntaub ntawv txheej txheej uas yaj hauv plab, cov ntaub ntawv ntim khoom microcapsule uas tso tawm tas mus li, cov ntaub ntawv zaj duab xis tshuaj uas tso tawm tas mus li, thiab lwm yam."

Sodium carboxymethyl cellulose (CMC-Na) yog cov cellulose ether uas muaj cov zis thiab kev siv ntau tshaj plaws hauv tsev thiab txawv teb chaws. Nws yog ib qho ionic cellulose ether ua los ntawm paj rwb thiab ntoo los ntawm alkalization thiab etherification nrog chloroacetic acid. CMC-Na yog ib qho tshuaj siv ntau. Nws feem ntau siv ua ib qho binder rau cov khoom khov kho thiab ua ib qho thickening, thickening thiab suspending agent rau cov kua npaj. Nws kuj tseem siv tau ua ib qho matrix thiab zaj duab xis-tsim cov khoom siv dej-soluble. Nws feem ntau siv ua ib qho tshuaj yeeb yaj kiab-tso tawm cov tshuaj thiab cov ntsiav tshuaj-tso tawm cov tshuaj hauv cov qauv tso tawm (tswj).

Ntxiv rau sodium carboxymethyl cellulose ua cov tshuaj ntxiv, croscarmellose sodium kuj tseem siv tau ua cov tshuaj ntxiv. Cross-linked carboxymethyl cellulose sodium (CCMC-Na) yog ib yam khoom uas tsis yaj hauv dej uas carboxymethyl cellulose teb nrog tus neeg sawv cev txuas ntawm qhov kub thiab txias (40-80 ° C) nyob rau hauv qhov kev ua ntawm cov tshuaj inorganic acid catalyst thiab tau purified. Tus neeg sawv cev txuas tuaj yeem yog propylene glycol, succinic anhydride, maleic anhydride, adipic anhydride, thiab lwm yam. Croscarmellose sodium yog siv ua tus neeg tawg rau cov ntsiav tshuaj, tshuaj ntsiav thiab granules hauv kev npaj noj. Nws vam khom cov capillary thiab o kom ua tiav kev tawg. Nws muaj kev sib zog zoo thiab kev tawg muaj zog. Cov kev tshawb fawb tau qhia tias qib o ntawm croscarmellose sodium hauv dej yog ntau dua li ntawm cov neeg tawg xws li sodium carboxymethyl cellulose uas tsis hloov pauv thiab hydrated microcrystalline cellulose.

Methyl cellulose (MC) yog ib qho non-ionic cellulose monoether ua los ntawm paj rwb thiab ntoo los ntawm alkalization thiab methyl chloride etherification. Methyl cellulose muaj cov dej solubility zoo heev thiab ruaj khov hauv pH ntau ntawm 2.0 txog 13.0. Nws yog siv dav hauv cov tshuaj excipients, thiab siv rau hauv cov ntsiav tshuaj sublingual, intramuscular txhaj tshuaj, ophthalmic preparations, oral capsules, oral suspensions, oral tablets thiab topical preparations. Tsis tas li ntawd, hauv cov formulations-release, MC tuaj yeem siv ua hydrophilic gel matrix sustained-release formulation, gastric-soluble coating khoom, sustained-release microcapsule ntim khoom, sustained-release tshuaj zaj duab xis khoom, thiab lwm yam.

Hydroxypropyl methylcellulose (HPMC) yog cov cellulose sib xyaw ether uas tsis yog ionic ua los ntawm paj rwb thiab ntoo los ntawm alkalization thiab etherification ntawm propylene oxide thiab methyl chloride. Nws tsis muaj ntxhiab, tsis muaj saj, tsis muaj tshuaj lom, yaj hauv dej txias, thiab gels hauv dej kub. Hydroxypropyl methylcellulose yog cov cellulose sib xyaw ether ntau yam uas tau nce sai hauv kev tsim khoom, kev siv thiab zoo hauv 15 xyoo dhau los. Nws kuj yog ib qho ntawm cov tshuaj siv tshuaj loj tshaj plaws hauv tsev thiab txawv teb chaws. Nws tau siv ua cov tshuaj siv tshuaj rau yuav luag 50 xyoo. Xyoo ntawm keeb kwm. Tam sim no, daim ntawv thov ntawm HPMC feem ntau pom tseeb hauv tsib yam hauv qab no:

Ib qho yog ua ib qho binder thiab disintegrant. HPMC ua ib qho binder tuaj yeem ua rau cov tshuaj yooj yim ntub, thiab nws tuaj yeem nthuav dav ntau pua zaus tom qab nqus dej, yog li nws tuaj yeem txhim kho qhov kev yaj lossis tso tawm ntawm cov ntsiav tshuaj. HPMC muaj viscosity muaj zog, thiab tuaj yeem txhim kho qhov viscosity ntawm cov khoom me me thiab txhim kho qhov compressibility ntawm cov khoom siv raw nrog cov qauv crisp lossis tawv. HPMC nrog viscosity qis tuaj yeem siv ua ib qho binder thiab disintegrant, thiab HPMC nrog viscosity siab tsuas yog siv tau ua ib qho binder.

Qhov thib ob, nws yog siv los ua cov khoom siv tso tawm thiab tswj tau rau kev npaj hauv qhov ncauj. HPMC yog cov khoom siv hydrogel matrix feem ntau siv rau hauv kev npaj tso tawm. HPMC ntawm qib viscosity qis (5 ~ 50mPa · s) tuaj yeem siv ua tus binder, tus neeg sawv cev nce viscosity thiab tus neeg sawv cev ncua, thiab HPMC ntawm qib viscosity siab (4000 ~ 100000mPa · s) tuaj yeem siv los npaj cov ntsiav tshuaj sib xyaw matrix ncua-tso tawm thiab cov khoom thaiv-tso tawm rau cov tshuaj ntsiav thiab cov ntsiav tshuaj hydrophilic gel matrix ncua-tso tawm. HPMC yaj tau hauv cov kua hauv plab hnyuv, muaj qhov zoo ntawm kev sib zog zoo, kev ua haujlwm zoo, muaj peev xwm thauj tshuaj muaj zog thiab cov yam ntxwv tso tawm tshuaj tsis cuam tshuam los ntawm pH. Nws yog cov khoom siv hydrophilic tseem ceeb heev hauv cov txheej txheem npaj tso tawm thiab feem ntau siv ua cov khoom siv hydrophilic gel matrix thiab cov khoom siv txheej ntawm kev npaj tso tawm, thiab siv rau hauv kev npaj plab zom mov thiab cov ntaub ntawv pabcuam membrane tso tawm tshuaj.

Qhov thib peb yog ua tus neeg sawv cev tsim cov zaj duab xis txheej.HPMCmuaj cov khoom zoo ua zaj duab xis. Zaj duab xis uas nws tsim yog sib xws, pob tshab, thiab tawv, thiab nws tsis yooj yim rau lo rau thaum lub sijhawm tsim khoom. Tshwj xeeb tshaj yog rau cov tshuaj uas yooj yim nqus cov dej noo thiab tsis ruaj khov, siv nws ua ib txheej cais tuaj yeem txhim kho qhov ruaj khov ntawm cov tshuaj thiab tiv thaiv zaj duab xis hloov xim. HPMC muaj ntau yam viscosity specifications. Yog tias xaiv kom raug, qhov zoo thiab tsos ntawm cov ntsiav tshuaj coated zoo dua li lwm cov ntaub ntawv, thiab nws cov concentration feem ntau yog 2% txog 10%.

Plaub yog siv ua cov khoom siv capsule. Nyob rau xyoo tas los no, nrog rau kev sib kis ntawm cov tsiaj txhu thoob ntiaj teb, piv rau cov tshuaj gelatin capsules, cov tshuaj cog tau dhau los ua qhov kev hlub tshiab ntawm kev lag luam tshuaj thiab khoom noj. Pfizer tau ua tiav rho tawm HPMC los ntawm cov nroj tsuag ntuj thiab npaj VcapTM cov tshuaj zaub capsules. Piv nrog cov tshuaj gelatin hollow capsules ib txwm muaj, cov tshuaj zaub capsules muaj qhov zoo ntawm kev hloov pauv dav, tsis muaj kev pheej hmoo ntawm kev sib txuas lus, thiab kev ruaj khov siab. Tus nqi tso tawm tshuaj yog qhov ruaj khov, thiab qhov sib txawv ntawm tus kheej yog me me. Tom qab disintegration hauv tib neeg lub cev, nws tsis nqus thiab tuaj yeem raug tso tawm. Tshem tawm ntawm lub cev. Hauv cov xwm txheej khaws cia, tom qab ntau qhov kev sim, nws yuav luag tsis brittle nyob rau hauv cov xwm txheej qis qis, thiab cov khoom ntawm lub plhaub capsule tseem ruaj khov nyob rau hauv cov huab cua siab, thiab ntau yam ntsuas ntawm cov tshuaj cog hauv qab cov xwm txheej khaws cia hnyav tsis cuam tshuam. Nrog rau tib neeg nkag siab txog cov tshuaj cog thiab kev hloov pauv ntawm cov tswv yim tshuaj pej xeem hauv tsev thiab txawv teb chaws, kev thov ua lag luam rau cov tshuaj cog yuav loj hlob sai.

Qhov thib tsib yog ua tus neeg sawv cev rau kev ncua. Kev npaj kua dej hom ncua yog ib daim ntawv siv tshuaj kho mob uas siv ntau, uas yog ib qho kev faib tawm heterogeneous uas cov tshuaj khov uas tsis yaj tau raug faib rau hauv cov kua faib tawm. Qhov ruaj khov ntawm lub kaw lus txiav txim siab qhov zoo ntawm kev npaj kua dej ncua. HPMC colloidal kua tuaj yeem txo qhov kev sib txhuam ntawm cov khoom khov-kua, txo qhov chaw dawb zog ntawm cov khoom khov, thiab ua kom lub kaw lus faib tawm heterogeneous ruaj khov. Nws yog ib qho kev ncua zoo heev. HPMC yog siv ua cov khoom tuab rau cov tshuaj qhov muag, nrog cov ntsiab lus ntawm 0.45% txog 1.0%.

Hydroxypropyl cellulose (HPC) yog ib qho non-ionic cellulose monoether ua los ntawm paj rwb thiab ntoo los ntawm alkalization thiab propylene oxide etherification. HPC feem ntau yog soluble hauv dej hauv qab 40 ° C thiab ntau cov kuab tshuaj polar, thiab nws cov kev ua tau zoo yog cuam tshuam nrog cov ntsiab lus ntawm hydroxypropyl thiab qib ntawm polymerization. HPC tuaj yeem sib xws nrog ntau yam tshuaj thiab muaj inertness zoo.

Cov hydroxypropyl cellulose uas muaj cov khoom hloov pauv tsawg(L-HPC)feem ntau yog siv los ua cov tshuaj ntsiav tawg thiab cov khoom siv khi. Nws cov yam ntxwv yog: yooj yim nias thiab tsim, siv tau zoo, tshwj xeeb tshaj yog nyuaj rau tsim, cov ntsiav tshuaj yas thiab tawg yooj yim, ntxiv L-HPC tuaj yeem txhim kho qhov nyuaj ntawm cov ntsiav tshuaj thiab qhov ci ntawm qhov tsos, thiab nws kuj tuaj yeem ua rau cov ntsiav tshuaj tawg sai, txhim kho qhov zoo sab hauv ntawm cov ntsiav tshuaj, thiab txhim kho cov txiaj ntsig kho.

Cov hydroxypropyl cellulose uas muaj ntau yam hloov pauv (H-HPC) siv tau ua tus neeg sawv cev rau cov ntsiav tshuaj, cov granules thiab cov granules zoo hauv kev lag luam tshuaj. H-HPC muaj cov yam ntxwv zoo heev rau kev tsim cov zaj duab xis, thiab cov zaj duab xis uas tshwm sim yog tawv thiab ywj, uas tuaj yeem piv nrog cov plasticizers. Los ntawm kev sib xyaw nrog lwm cov neeg sawv cev tiv thaiv kev ntub dej, kev ua tau zoo ntawm cov zaj duab xis tuaj yeem txhim kho ntxiv, thiab nws feem ntau siv ua cov khoom siv txheej zaj duab xis rau cov ntsiav tshuaj. H-HPC kuj tseem siv tau ua cov khoom siv matrix los npaj cov ntsiav tshuaj matrix sustained-release, sustained-release pellets thiab cov ntsiav tshuaj ob txheej sustained-release.

Hydroxyethyl cellulose (HEC) yog ib qho non-ionic cellulose monoether ua los ntawm paj rwb thiab ntoo los ntawm alkalization thiab ethylene oxide etherification. HEC feem ntau yog siv ua ib qho thickener, colloidal tiv thaiv tus neeg sawv cev, nplaum, dispersant, stabilizer, suspending agent, zaj duab xis-tsim tus neeg sawv cev thiab cov khoom tso tawm qeeb hauv kev kho mob. Nws tuaj yeem siv rau emulsions, tshuaj pleev, thiab qhov muag tee rau tshuaj pleev. Kua hauv qhov ncauj, cov ntsiav tshuaj khov, capsules thiab lwm yam tshuaj. Hydroxyethyl cellulose tau suav nrog hauv US Pharmacopoeia / US National Formulary thiab European Pharmacopoeia.

Ethyl cellulose (EC) yog ib qho ntawm cov cellulose derivatives uas siv dav tshaj plaws hauv dej. EC tsis muaj tshuaj lom, ruaj khov, tsis yaj hauv dej, kua qaub lossis alkaline, thiab yaj hauv cov organic solvents xws li ethanol thiab methanol. Cov kuab tshuaj feem ntau yog cov kuab tshuaj sib xyaw ntawm toluene/ethanol 4/1 (qhov hnyav). EC muaj ntau yam siv rau hauv kev npaj tshuaj uas tso tawm sai, thiab siv dav ua tus nqa thiab microcapsules, txheej zaj duab xis tsim cov ntaub ntawv, thiab lwm yam ntawm kev npaj tshuaj uas tso tawm sai, xws li cov tshuaj ncua ntsiav tshuaj, cov nplaum, cov ntaub ntawv txheej zaj duab xis, thiab lwm yam. Nws yog siv ua zaj duab xis khoom siv matrix los npaj ntau hom matrix tso tawm ntsiav tshuaj, ua cov khoom sib xyaw los npaj cov tshuaj coated tso tawm sai thiab cov pellets uas tso tawm sai, ua cov khoom siv encapsulation los npaj cov microcapsules uas tso tawm sai; nws kuj tseem siv tau dav ua cov khoom siv nqa Nws yog siv los npaj cov khoom sib xyaw; nws tuaj yeem siv dav hauv kev siv tshuab tshuaj ua cov tshuaj tsim zaj duab xis thiab txheej tiv thaiv, thiab nws kuj tseem siv tau ua tus khi thiab muab khoom. Ua ib txheej tiv thaiv rau cov ntsiav tshuaj, nws tuaj yeem txo qhov rhiab heev ntawm cov ntsiav tshuaj rau cov av noo thiab tiv thaiv cov tshuaj kom tsis txhob hloov xim thiab puas tsuaj los ntawm cov av noo; nws kuj tseem tuaj yeem tsim cov kua nplaum qeeb qeeb thiab microencapsulate cov polymer kom txuas ntxiv tso tawm cov tshuaj nyhuv.

Hauv kev xaus, cov dej-soluble sodium carboxymethyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose thiab roj-soluble ethyl cellulose yog txhua yam raws li lawv cov yam ntxwv ntawm cov khoom siv hauv cov tshuaj excipients ua cov nplaum, disintegrants, cov khoom tso tawm thiab tswj hwm rau kev npaj qhov ncauj, cov neeg sawv cev txheej zaj duab xis, cov ntaub ntawv capsule thiab cov neeg sawv cev ncua. Saib lub ntiaj teb, ntau lub tuam txhab txawv teb chaws txawv teb chaws (Shin-Etsu Nyiv, Dow Wolff thiab Ashland) tau pom tias muaj kev lag luam loj heev rau cov tshuaj cellulose hauv Suav teb yav tom ntej, thiab txawm tias nce kev tsim khoom lossis kev sib koom ua ke, lawv tau nce lawv qhov muaj nyob hauv daim teb no. Kev nqis peev hauv daim ntawv thov. Dow Wolff tshaj tawm tias nws yuav ua rau nws mloog zoo rau cov qauv, cov khoom xyaw thiab cov kev xav tau ntawm kev lag luam tshuaj Suav teb, thiab nws cov kev tshawb fawb daim ntawv thov kuj tseem yuav siv zog kom ze rau kev ua lag luam. Lub Wolff Cellulose Division ntawm Dow Chemical thiab Colorcon Corporation ntawm Tebchaws Meskas tau tsim kom muaj kev sib koom tes npaj tso tawm thiab tswj hwm thoob ntiaj teb. Nws muaj ntau tshaj 1,200 tus neeg ua haujlwm hauv 9 lub nroog, 15 lub koom haum khoom vaj khoom tsev thiab 6 lub tuam txhab GMP. Cov kws tshaj lij tshawb fawb siv tau muab kev pabcuam rau cov neeg siv khoom hauv kwv yees li 160 lub tebchaws. Ashland muaj cov chaw tsim khoom hauv Beijing, Tianjin, Shanghai, Nanjing, Changzhou, Kunshan thiab Jiangmen, thiab tau nqis peev rau peb lub chaw tshawb fawb thev naus laus zis hauv Shanghai thiab Nanjing.

Raws li cov ntaub ntawv los ntawm lub vev xaib ntawm Tuam Tshoj Cellulose Association, xyoo 2017, kev tsim khoom hauv tsev ntawm cellulose ether yog 373,000 tons thiab qhov ntim muag khoom yog 360 txhiab tons. Xyoo 2017, qhov ntim muag khoom tiag tiag ntawm ionicCMCyog 234,000 tons, nce 18.61% xyoo-rau-xyoo, thiab qhov ntim muag khoom ntawm non-ionic CMC yog 126,000 tons, nce 8.2% xyoo-rau-xyoo. Ntxiv rau HPMC (qib khoom siv hauv tsev) cov khoom tsis-ionic,HPMC(qib tshuaj), HPMC (qib zaub mov), HEC, HPC, MC, HEMC, thiab lwm yam tau nce siab tawm tsam qhov sib txawv, thiab kev tsim khoom thiab kev muag khoom tau txuas ntxiv mus ntxiv. Cov cellulose ethers hauv tsev tau loj hlob sai rau ntau tshaj kaum xyoo, thiab cov zis tau dhau los ua thawj zaug hauv ntiaj teb. Txawm li cas los xij, feem ntau ntawm cov khoom lag luam cellulose ether feem ntau yog siv rau hauv nruab nrab thiab qis kawg ntawm kev lag luam, thiab tus nqi ntxiv tsis siab.

Tam sim no, feem ntau ntawm cov tuam txhab cellulose ether hauv tsev nyob rau lub sijhawm tseem ceeb ntawm kev hloov pauv thiab kev txhim kho. Lawv yuav tsum txuas ntxiv nce kev tshawb fawb thiab kev txhim kho khoom, txuas ntxiv nplua nuj ntau yam khoom, siv tag nrho Tuam Tshoj, lub ntiaj teb kev lag luam loj tshaj plaws, thiab nce kev siv zog los tsim cov lag luam txawv teb chaws kom cov tuam txhab lag luam yuav muaj peev xwm nthuav dav sai li sai tau. Ua tiav kev hloov pauv thiab kev txhim kho, nkag mus rau nruab nrab-rau-siab kawg ntawm kev lag luam, thiab ua tiav kev txhim kho zoo thiab ntsuab.