Pharmaceutical excipients yog excipients thiab adjuvants siv nyob rau hauv kev tsim cov tshuaj thiab tsim cov tshuaj, thiab yog ib feem tseem ceeb ntawm kev npaj tshuaj. Raws li ib tug natural polymer derived khoom, cellulose ether muaj cov yam ntxwv ntawm biodegradability, non-toxicity, thiab tus nqi qis, xws li sodium carboxymethyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl cellulose,Cellulose ethersxws li hydroxyethyl cellulose thiab ethyl cellulose muaj ib qho tseem ceeb daim ntawv thov nqi nyob rau hauv cov tshuaj excipients. Tam sim no, cov khoom ntawm feem ntau domestic cellulose ether tuam txhab yog tsuas yog siv nyob rau hauv nruab nrab thiab qis-kawg teb ntawm kev lag luam, thiab tus nqi ntxiv yog tsis siab. Kev lag luam ceev ceev yuav tsum tau hloov pauv thiab hloov kho thiab txhim kho cov kev siv high-end ntawm cov khoom.
Pharmaceutical excipients ua lub luag haujlwm tseem ceeb hauv kev txhim kho thiab tsim cov formulations. Piv txwv li, nyob rau hauv sustained-tso npaj, cov ntaub ntawv polymer xws li cellulose ethers yog siv los ua tshuaj excipients nyob rau hauv sustained-tso pellets, ntau yam matrix sustained-tso formulations, coated sustained-tso formulations, sustained-tso capsules, sustained-tso tshuaj yeeb yaj kiab, thiab. Kev npaj thiab ua kua dej-tso tawm kev npaj tau dav siv. Hauv cov txheej txheem no, cov khoom siv polymers xws li cellulose ethers feem ntau yog siv los ua cov neeg nqa tshuaj los tswj cov kev tso tawm ntawm cov tshuaj hauv tib neeg lub cev, uas yog, lawv yuav tsum tau maj mam tso tawm hauv lub cev ntawm tus nqi teev nyob rau hauv qee lub sijhawm kom ua tiav lub hom phiaj ntawm kev kho mob zoo.
Raws li kev txheeb cais ntawm Lub Tsev Haujlwm Saib Xyuas Kev Sib Tham thiab Tshawb Fawb, muaj txog 500 hom excipients ntawm kev ua lag luam hauv kuv lub tebchaws, tab sis piv nrog Tebchaws Meskas (ntau tshaj 1500 hom) thiab European Union (ntau tshaj 3000 hom), muaj qhov sib txawv loj, thiab cov hom tseem me me. kuv lub teb chaws cov tshuaj excipients Lub peev xwm ntawm kev ua lag luam yog loj. Nws tau nkag siab tias kaum sab saum toj ntawm cov tshuaj excipients nyob rau hauv kuv lub teb chaws kev lag luam nplai yog tshuaj gelatin capsules, sucrose, starch, zaj duab xis txheej hmoov, 1,2-propylene glycol, PVP, hydroxypropyl methylcellulose (HPMC), thiab microcrystalline fibers. Neeg tsis noj nqaij, HPC, lactose.
"Natural cellulose ether yog cov ntsiab lus dav dav rau ntau cov cellulose derivatives uas tsim los ntawm cov tshuaj tiv thaiv ntawm alkali cellulose thiab etherifying tus neeg sawv cev nyob rau hauv tej yam kev mob, thiab yog ib yam khoom uas cov hydroxyl pawg ntawm cov cellulose macromolecule yog ib feem los yog kiag li hloov los ntawm ether pawg. Nyob rau hauv tag nrho cov teb, cov kws tshuaj-qib cov khoom yog nyob rau hauv nruab nrab thiab high-end cheeb tsam ntawm kev lag luam thiab muaj siab ntxiv tus nqi Vim nruj zoo yuav tsum tau, zus tau tej cov tshuaj-qib cellulose ethers kuj yog ib qho nyuaj heev Nws yuav hais tau hais tias qhov zoo ntawm cov tshuaj-qib cov khoom muaj peev xwm sawv cev rau cov technical zog ntawm cellulose ethers thickener los ua sustained-tso tawm matrix ntsiav tshuaj, gastric-soluble txheej ntaub ntawv, sustained-tso microcapsule ntim cov ntaub ntawv, sustained-tso tshuaj yeeb yaj duab cov ntaub ntawv, thiab lwm yam.
Sodium carboxymethyl cellulose (CMC-Na) yog cov cellulose ether nrog cov khoom siv loj tshaj plaws thiab siv hauv tsev thiab txawv teb chaws. Nws yog ionic cellulose ether ua los ntawm paj rwb thiab ntoo los ntawm alkalization thiab etherification nrog chloroacetic acid. CMC-Na yog ib qho khoom siv tshuaj uas nquag siv. Nws feem ntau yog siv los ua cov ntawv khi rau cov khoom npaj thiab ua cov thickening, thickening thiab suspending tus neeg sawv cev rau cov kua npaj. Nws kuj tseem siv tau los ua cov dej-soluble matrix thiab cov khoom siv ua yeeb yaj kiab. Nws feem ntau yog siv los ua cov khoom siv tshuaj yeeb yaj kiab uas tau tso tawm thiab cov ntsiav tshuaj uas tau tso tawm matrix hauv sustained (tswj) tso tawm formulations.
Ntxiv rau sodium carboxymethyl cellulose ua cov khoom siv tshuaj, croscarmellose sodium kuj tuaj yeem siv los ua cov tshuaj ntxiv. Hla-txuas carboxymethyl cellulose sodium (CCMC-Na) yog cov dej-insoluble tshuaj uas carboxymethyl cellulose reacts nrog tus neeg sawv cev sib txuas ntawm qhov kub (40-80 ° C) nyob rau hauv qhov kev txiav txim ntawm inorganic acid catalyst thiab yog purified. Tus neeg sawv cev crosslinking tuaj yeem yog propylene glycol, succinic anhydride, maleic anhydride, adipic anhydride, thiab lwm yam. Croscarmellose sodium yog siv los ua disintegrant rau ntsiav tshuaj, tshuaj ntsiav thiab granules hauv qhov ncauj npaj. Nws tso siab rau capillary thiab o los ua kom tiav kev tawg. Nws muaj zoo compressibility thiab muaj zog disintegration. Cov kev tshawb fawb tau pom tias qhov o ntawm croscarmellose sodium nyob rau hauv dej yog ntau dua li ntawm cov disintegrants xws li qis-sodium carboxymethyl cellulose thiab hydrated microcrystalline cellulose.
Methyl cellulose (MC) yog 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 dav siv nyob rau hauv cov tshuaj excipients, thiab yog siv nyob rau hauv sublingual ntsiav tshuaj, intramuscular txhaj, ophthalmic npaj, qhov ncauj capsules, qhov ncauj ncua kev kawm ntawv, qhov ncauj ntsiav tshuaj thiab tshuaj pleev. Tsis tas li ntawd, nyob rau hauv sustained-tso formulations, MC yuav siv tau raws li ib tug hydrophilic gel matrix sustained-tso formulation, gastric-soluble txheej txheej, sustained-tso microcapsule ntim khoom, sustained-tso tshuaj yeeb yaj duab khoom, thiab lwm yam.
Hydroxypropyl methylcellulose (HPMC) yog non-ionic cellulose tov ether ua los ntawm paj rwb thiab ntoo los ntawm alkalization thiab etherification ntawm propylene oxide thiab methyl chloride. Nws yog odorless, tasteless, non-toxic, soluble nyob rau hauv dej txias, thiab gels nyob rau hauv dej kub. Hydroxypropyl methylcellulose yog ib qho cellulose sib xyaw ether ntau yam uas tau nce sai hauv kev tsim khoom, noj thiab ua tau zoo hauv 15 xyoo dhau los. Nws kuj yog ib qho ntawm cov khoom siv tshuaj loj tshaj plaws siv hauv tsev thiab txawv teb chaws. Nws tau siv los ua ib qho tshuaj excipient rau ze li 50 xyoo. Xyoo keeb kwm. Tam sim no, daim ntawv thov ntawm HPMC feem ntau yog tshwm sim hauv tsib yam hauv qab no:
Ib tug yog raws li ib tug binder thiab disintegrant. HPMC raws li ib tug binder tuaj yeem ua rau cov tshuaj yooj yim kom ntub dej, thiab nws tuaj yeem nthuav ntau pua zaus tom qab nqus dej, yog li nws tuaj yeem txhim kho qhov kev sib cais lossis tso tawm ntawm cov ntsiav tshuaj. HPMC muaj viscosity muaj zog, thiab tuaj yeem txhim kho cov viscosity particle thiab txhim kho cov compressibility ntawm raw cov ntaub ntawv nrog crisp los yog tawv zoo nkauj. HPMC uas muaj viscosity tsawg yuav siv tau los ua ib tug binder thiab disintegrant, thiab HPMC uas muaj viscosity siab yuav siv tau raws li ib tug binder.
Thib ob, nws yog siv los ua cov khoom siv txhawb nqa thiab tswj kev tso tawm rau kev npaj qhov ncauj. HPMC yog cov khoom siv hydrogel matrix uas nquag siv hauv kev npaj tso tawm. HPMC ntawm qib viscosity qis (5 ~ 50mPa·s) tuaj yeem siv los ua cov ntawv khi, viscosity nce tus neeg sawv cev thiab tshem tawm tus neeg sawv cev, thiab HPMC ntawm qib viscosity siab (4000～100000mPa·s) tuaj yeem siv los npaj cov khoom sib xyaw matrix sustained-tso tawm cov ntsiav tshuaj thiab cov tshuaj tua kab mob. matrix sustained-tso ntsiav tshuaj. HPMC yog soluble hauv plab hnyuv, muaj qhov zoo ntawm compressibility zoo, zoo fluidity, muaj zog tshuaj loading peev xwm thiab tshuaj tso tawm yam ntxwv tsis cuam tshuam los ntawm pH. Nws yog ib qho tseem ceeb ntawm cov khoom siv hydrophilic carrier nyob rau hauv sustained-tso npaj cov txheej txheem thiab feem ntau yog siv raws li cov hydrophilic gel matrix thiab txheej cov ntaub ntawv ntawm sustained-tso npaj, thiab siv nyob rau hauv gastric floating npaj thiab sustained-tso tshuaj membrane auxiliary cov ntaub ntawv.
Qhov thib peb yog raws li txheej txheej zaj duab xis-forming tus neeg sawv cev.HPMCmuaj zoo zaj duab xis-forming zog. Cov yeeb yaj kiab tsim los ntawm nws yog ib yam, pob tshab, thiab tawv, thiab nws tsis yooj yim rau kev ua raws li kev tsim khoom. Tshwj xeeb tshaj yog rau cov tshuaj uas yooj yim rau nqus dej noo thiab tsis ruaj khov, siv nws los ua ib txheej cais tuaj yeem txhim kho kev ruaj ntseg ntawm cov tshuaj thiab tiv thaiv cov yeeb yaj kiab hloov xim. HPMC muaj ntau yam viscosity specifications. Yog tias xaiv kom raug, qhov zoo thiab cov tsos ntawm cov ntsiav tshuaj coated yog zoo dua li lwm cov ntaub ntawv, thiab nws cov concentration yog 2% mus rau 10%.
Plaub yog siv los ua cov khoom siv tshuaj ntsiav. Nyob rau hauv xyoo tas los no, nrog rau kev sib kis ntawm cov tsiaj thoob ntiaj teb, piv nrog gelatin capsules, cov tshuaj ntsuab cog tau dhau los ua tus hlub tshiab ntawm kev lag luam tshuaj thiab zaub mov. Pfizer tau ntse rho tawm HPMC los ntawm cov nroj tsuag ntuj thiab npaj VcapTM zaub capsules. Piv nrog cov tshuaj gelatin hollow capsules, zaub capsules muaj qhov zoo ntawm kev hloov pauv dav dav, tsis muaj kev pheej hmoo ntawm kev sib txuas cov tshuaj tiv thaiv, thiab kev ruaj ntseg siab. Cov tshuaj tso tawm tus nqi yog qhov ruaj khov, thiab tus neeg sib txawv me me. Tom qab disintegration nyob rau hauv tib neeg lub cev, nws tsis absorbed thiab yuav tsum tau excreted. Excreted los ntawm lub cev. Nyob rau hauv cov nqe lus ntawm kev cia khoom, tom qab ntau qhov kev ntsuam xyuas, nws yuav luag tsis nkig nyob rau hauv cov av noo tsawg, thiab cov khoom ntawm lub capsule plhaub tseem nyob ruaj khov nyob rau hauv high humidity, thiab ntau yam indexes ntawm cov nroj tsuag capsules nyob rau hauv huab cia tej yam kev mob tsis cuam tshuam. Nrog rau tib neeg txoj kev nkag siab ntawm cov tshuaj ntsiav thiab kev hloov pauv ntawm cov tshuaj pej xeem cov ntsiab lus hauv tsev thiab txawv teb chaws, kev lag luam xav tau rau cov tshuaj ntsiav tshuaj yuav loj hlob sai.
Qhov thib tsib yog raws li tus neeg sawv cev ncua. Suspension hom kua npaj yog ib qho kev siv tshuaj kho mob ntau npaum li cas, uas yog ib qho kev sib txawv ntawm cov txheej txheem uas tsis tshua muaj kuab lom cov tshuaj yog dispersed nyob rau hauv cov kua dispersion nruab nrab. Qhov kev ruaj ntseg ntawm lub kaw lus txiav txim siab qhov zoo ntawm kev ncua kev npaj kua. HPMC colloidal tov tuaj yeem txo cov khoom-kua interfacial nro, txo lub zog tsis muaj zog ntawm cov khoom, thiab ruaj khov rau cov txheej txheem sib txawv. Nws yog ib tug zoo heev suspending agent. HPMC yog siv los ua cov thickener rau qhov muag te, nrog cov ntsiab lus ntawm 0.45% mus rau 1.0%.
Hydroxypropyl cellulose (HPC) yog 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 polars, thiab nws cov kev ua tau zoo muaj feem xyuam rau cov ntsiab lus ntawm hydroxypropyl thiab qib ntawm polymerization. HPC tuaj yeem sib xyaw nrog ntau yam tshuaj thiab muaj qhov tsis zoo.
Tsawg-siv hydroxypropyl cellulose(L-HPC)yog siv los ua ntsiav tshuaj disintegrant thiab binder. Nws cov yam ntxwv yog: yooj yim rau nias thiab daim ntawv, muaj zog applicability, tshwj xeeb tshaj yog nyuaj rau daim ntawv, yas thiab nkig ntsiav tshuaj, ntxiv L -HPC tuaj yeem txhim kho lub hardness ntawm cov ntsiav tshuaj thiab lub brightness ntawm cov tsos, thiab nws kuj yuav ua rau cov ntsiav tshuaj disintegrate sai, txhim kho lub internal zoo ntawm cov ntsiav tshuaj, thiab txhim kho cov nyhuv curative.
Kev hloov pauv siab hydroxypropyl cellulose (H-HPC) tuaj yeem siv los ua tus neeg sawv cev khi rau cov ntsiav tshuaj, granules thiab nplua granules hauv kev lag luam tshuaj. H-HPC muaj cov yeeb yaj kiab zoo heev, thiab cov yeeb yaj kiab ua tau yog tawv thiab elastic, uas tuaj yeem muab piv nrog cov yas yas. Los ntawm kev sib xyaw nrog lwm cov tshuaj tiv thaiv ntub dej, kev ua haujlwm ntawm zaj duab xis tuaj yeem txhim kho ntxiv, thiab nws feem ntau yog siv los ua cov khoom siv zaj duab xis rau cov ntsiav tshuaj. H-HPC kuj tseem siv tau los ua cov khoom siv matrix los npaj cov ntsiav tshuaj matrix sustained-tso, sustained-tso pellets thiab ob-txheej sustained-tso ntsiav tshuaj.
Hydroxyethyl cellulose (HEC) yog non-ionic cellulose monoether ua los ntawm paj rwb thiab ntoo los ntawm alkalization thiab ethylene oxide etherification. HEC feem ntau yog siv los ua cov thickener, colloidal tiv thaiv tus neeg sawv cev, nplaum, dispersant, stabilizer, suspending agent, film-forming agent thiab slow-release material in the medical field. Nws tuaj yeem siv rau emulsions, tshuaj pleev, thiab tshuaj pleev qhov muag rau cov tshuaj pleev ib ce. Cov kua hauv qhov ncauj, cov ntsiav tshuaj, cov tshuaj ntsiav thiab lwm hom tshuaj. Hydroxyethyl cellulose tau suav nrog US Pharmacopoeia / US National Formulary thiab European Pharmacopoeia.
Ethyl cellulose (EC) yog ib qho ntawm feem ntau siv dej-insoluble cellulose derivatives. EC yog non-toxic, ruaj khov, insoluble nyob rau hauv dej, acid los yog alkaline daws, thiab soluble nyob rau hauv organic solvents xws li ethanol thiab methanol. Cov kuab tshuaj nquag siv yog cov kuab tshuaj sib xyaw ntawm toluene / ethanol 4/1 (qhov hnyav). EC muaj ntau yam kev siv tshuaj tiv thaiv-tso tawm kev npaj, thiab yog dav siv los ua cov cab kuj thiab microcapsules, txheej txheej zaj duab xis-tsim cov ntaub ntawv, thiab lwm yam ntawm kev npaj-tso tawm, xws li ntsiav tshuaj retarders, nplaum nplaum, zaj duab xis txheej cov ntaub ntawv, thiab lwm yam. sustained-tso npaj thiab sustained-tso pellets, raws li ib tug encapsulation auxiliary khoom los npaj sustained-tso microcapsules; nws tseem tuaj yeem siv dav los ua cov khoom nqa khoom Nws yog siv los npaj cov khoom tawg; nws tuaj yeem siv dav hauv kev siv tshuab thev naus laus zis ua cov yeeb yaj kiab tsim cov khoom siv thiab cov txheej txheem tiv thaiv, thiab nws kuj tuaj yeem siv los ua cov ntawv khi thiab muab tub lim. Raws li kev tiv thaiv txheej rau cov ntsiav tshuaj, nws tuaj yeem txo qhov rhiab heev ntawm cov ntsiav tshuaj rau cov av noo thiab tiv thaiv cov tshuaj los ntawm qhov tsis muaj xim thiab deteriorated los ntawm noo noo; nws tseem tuaj yeem tsim cov kua nplaum qeeb qeeb thiab microencapsulate cov polymer kom tsis tu ncua tso tawm cov nyhuv tshuaj.
Nyob rau hauv cov ntsiab lus, cov dej-soluble sodium carboxymethyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose thiab roj-soluble ethyl cellulose yog tag nrho raws li lawv cov yam ntxwv ntawm cov khoom yog siv nyob rau hauv cov tshuaj excipients raws li adhesives, kev npaj, disintegrant. coating film-forming agents, capsule material thiab suspending agents. Saib ntawm lub ntiaj teb no, ntau lub tuam txhab txawv teb chaws (Shin-Etsu Nyiv, Dow Wolff thiab Ashland) tau paub txog kev lag luam loj rau cov tshuaj cellulose hauv Suav teb yav tom ntej, thiab kev tsim khoom ntau ntxiv lossis kev sib koom ua ke, lawv tau nce lawv qhov chaw nyob hauv daim teb no. Kev nqis peev hauv daim ntawv thov. Dow Wolff tau tshaj tawm tias nws yuav ua rau nws muaj kev mloog zoo rau kev tsim, cov khoom xyaw thiab cov kev xav tau ntawm Tuam Tshoj cov tshuaj npaj ua lag luam, thiab nws daim ntawv thov kev tshawb fawb tseem yuav siv zog los ze zog rau kev ua lag luam. Wolff Cellulose Division ntawm Dow Chemical thiab Colorcon Corporation ntawm Tebchaws Meskas tau tsim kom muaj kev txhawb nqa thiab tswj kev tso tawm kev sib koom ua ke thoob ntiaj teb. Nws muaj ntau dua 1,200 tus neeg ua haujlwm hauv 9 lub nroog, 15 lub tuam txhab cuab yeej cuab tam thiab 6 lub tuam txhab GMP. Cov kws tshaj lij tshawb fawb 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 hauv peb lub chaw tshawb fawb thev naus laus zis hauv Shanghai thiab Nanjing.
Raws li kev txheeb cais 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 muag ntim yog 360 txhiab tons. Nyob rau hauv 2017, qhov tseeb muag ntim ntawm ionicCMCyog 234,000 tons, nce ntawm 18.61% xyoo-rau-xyoo, thiab kev muag khoom ntim ntawm non-ionic CMC yog 126,000 tons, nce 8.2% xyoo-rau-xyoo. Ntxiv rau HPMC (cov khoom siv hauv tsev) cov khoom tsis-ionic,HPMC(pharmaceutical grade), HPMC (khoom noj khoom haus), HEC, HPC, MC, HEMC, thiab lwm yam tau sawv tawm tsam tus qauv, thiab kev tsim khoom thiab muag tau nce ntxiv. Hauv tsev cellulose ethers tau loj hlob sai heev rau ntau tshaj kaum xyoo, thiab cov zis tau dhau los ua lub ntiaj teb thawj zaug. Txawm li cas los xij, feem ntau ntawm cov tuam txhab cellulose ether cov khoom lag luam feem ntau yog siv hauv nruab nrab thiab qis kawg ntawm kev lag luam, thiab tus nqi ntxiv tsis siab.
Tam sim no, feem ntau ntawm cov khoom lag luam hauv tsev cellulose ether yog nyob rau lub sijhawm tseem ceeb ntawm kev hloov pauv thiab hloov kho dua tshiab. Lawv yuav tsum tau nce ntxiv kev tshawb fawb thiab kev loj hlob ntawm cov khoom, tsis tu ncua ntxiv cov khoom ntau yam, ua kom tag nrho ntawm Tuam Tshoj, lub ntiaj teb no cov lag luam loj tshaj plaws, thiab nce kev siv zog los tsim cov lag luam txawv teb chaws kom cov lag luam tuaj yeem nthuav dav sai li sai tau. Ua kom tiav qhov kev hloov pauv thiab hloov kho tshiab, nkag mus rau nruab nrab-rau-siab kawg ntawm kev lag luam, thiab ua tiav benign thiab ntsuab kev loj hlob.
Lub sij hawm xa tuaj: Plaub Hlis-25-2024