Pharmaceutical Excipients Cellulose Ether

Natural cellulose ether yog ib lub ntsiab lus dav dav rau ntau yamderivatives ntawm celluloseua los ntawm cov tshuaj tiv thaiv ntawm alkali cellulose thiab etherifying tus neeg saib xyuas nyob rau hauv tej yam kev mob. Nws yog ib yam khoom uas cov hydroxyl pawg ntawm cellulose macromolecules yog ib feem los yog kiag li hloov los ntawm ether pawg. Cellulose ethers tau siv dav hauv kev lag luam roj av, cov khoom siv hauv tsev, coatings, zaub mov, tshuaj, thiab tshuaj txhua hnub. Hauv ntau qhov chaw, cov khoom siv tshuaj-qib yog qhov tseem ceeb hauv nruab nrab thiab high-end teb ntawm kev lag luam, nrog cov nqi ntxiv. Vim yog cov kev cai nruj nruj, kev tsim cov tshuaj-qib cellulose ether kuj tseem nyuaj. Nws tuaj yeem hais tau tias qhov zoo ntawm cov khoom lag luam-qib tuaj yeem sawv cev rau lub zog ntawm kev lag luam cellulose ether. Cellulose ether feem ntau yog ntxiv raws li blocker, matrix khoom thiab thickener los ua sustained-tso matrix ntsiav tshuaj, gastric-soluble txheej ntaub ntawv, sustained-tso microcapsule txheej ntaub ntawv, sustained-tso tshuaj yeeb yaj duab cov ntaub ntawv, thiab lwm yam.

Sodium carboxymethyl cellulose:

Carboxymethyl cellulose sodium (CMC-Na) yog cov cellulose ether ntau yam nrog kev tsim khoom 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 ib daim ntawv khi rau cov khoom npaj, tus neeg sawv cev thickening, tus neeg sawv cev thickening, thiab tus neeg sawv cev ncua rau kev npaj ua kua. 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 thiab cov ntsiav tshuaj sustained-tso matrix nyob rau hauv kev npaj (tswj) tso tawm.

Ntxiv nrog rau sodium carboxymethylcellulose ua cov khoom siv tshuaj, croscarmellose sodium kuj tuaj yeem siv los ua cov khoom siv tshuaj. Croscarmellose sodium (CCMC-Na) yog cov khoom tsis muaj dej-soluble ntawm carboxymethylcellulose reacting nrog tus neeg sawv cev crosslinking ntawm ib qho kub (40-80 ° C) nyob rau hauv qhov kev txiav txim ntawm inorganic acid catalyst thiab purified. Raws li tus neeg sawv cev crosslinking, propylene glycol, succinic anhydride, maleic anhydride thiab adipic anhydride tuaj yeem siv. 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 tawg. Nws muaj zoo compressibility thiab muaj zog disintegration quab yuam. 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 low-susstituted carmellose sodium thiab hydrated microcrystalline cellulose.

Methylcellulose:

Methyl cellulose (MC) yog non-ionic cellulose ib ether ua los ntawm paj rwb thiab ntoo los ntawm alkalization thiab methyl chloride etherification. Methylcellulose muaj dej solubility zoo heev thiab ruaj khov nyob rau hauv thaj tsam ntawm pH 2.0 ~ 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 kev npaj tso tawm, MC tuaj yeem siv los ua hydrophilic gel matrix sustained-release npaj, gastric-soluble txheej txheej, sustained-tso microcapsule txheej cov ntaub ntawv, sustained-tso tshuaj yeeb yaj kiab cov ntaub ntawv, thiab lwm yam.

Hydroxypropyl methyl cellulose:

Hydroxypropyl methylcellulose (HPMC) yog non-ionic cellulose tov ether ua los ntawm paj rwb thiab ntoo los ntawm alkalization, propylene oxide thiab methyl chloride etherification. Nws yog odorless, tasteless, non-toxic, soluble nyob rau hauv dej txias thiab gelled nyob rau hauv dej kub. Hydroxypropyl methylcellulose yog cellulose sib xyaw ether ntau yam uas nws cov khoom tsim, ntau npaum li cas thiab zoo tau nce sai hauv Suav teb hauv 15 xyoo dhau los. Nws kuj yog ib qho ntawm feem ntau siv tshuaj excipients nyob rau hauv tsev thiab txawv teb chaws. 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. Raws li kev sib khi, HPMC tuaj yeem ua rau cov tshuaj yooj yim ntub dej, thiab nws tuaj yeem nthuav dav ntau pua zaus tom qab nqus dej, yog li nws tuaj yeem txhim kho tus nqi tawg lossis tso tawm ntawm cov ntsiav tshuaj. HPMC muaj viscosity muaj zog, uas tuaj yeem txhim kho cov viscosity particle thiab txhim kho cov compressibility ntawm raw cov ntaub ntawv nrog crisp los yog nkig zoo nkauj. HPMC uas muaj viscosity tsawg tuaj yeem siv los ua kev sib khi thiab tsis sib xws, thiab cov viscosity siab tsuas yog siv los ua cov ntawv khi.

Qhov thib ob yog raws li kev txhawb nqa thiab tswj cov khoom tso tawm rau kev npaj qhov ncauj. HPMC yog cov khoom siv hydrogel matrix uas nquag siv hauv kev npaj tso tawm. Qib qis viscosity (5-50mPa·s) HPMC tuaj yeem siv los ua cov ntawv khi, viscosifier thiab suspending tus neeg sawv cev, thiab qib siab viscosity (4000-100000mPa·s) HPMC tuaj yeem siv los npaj cov khoom sib xyaw thaiv cov tshuaj ntsiav, hydrogel matrix ncua-tso ntsiav tshuaj. HPMC yog soluble hauv plab hnyuv, muaj qhov zoo ntawm compressibility zoo, fluidity zoo, 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 uas muaj nyob rau hauv cov txheej txheem kev npaj tso tawm thiab feem ntau yog siv los ua Hydrophilic gel matrix thiab txheej cov ntaub ntawv rau kev npaj tawm-tso tawm, nrog rau cov khoom siv pabcuam rau kev npaj plab hnyuv thiab kev npaj tshuaj yeeb yaj kiab.

Qhov thib peb yog raws li txheej txheej zaj duab xis-forming tus neeg sawv cev. HPMC muaj cov khoom ua yeeb yaj kiab zoo. Cov yeeb yaj kiab tsim los ntawm nws yog ib yam, pob tshab thiab tawv, thiab nws tsis yooj yim rau lo thaum 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 superior rau lwm cov ntaub ntawv. Cov concentration ib txwm yog 2% mus rau 10%.

Qhov thib plaub yog raws li 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, zaub capsules tau dhau los ua tus hlub tshiab ntawm kev lag luam tshuaj thiab zaub mov. Pfizer ntawm Tebchaws Meskas tau ua tiav HPMC los ntawm cov nroj tsuag ntuj thiab npaj VcapTM zaub capsules. Piv nrog cov tshuaj gelatin hollow capsules, cov tshuaj ntsiav tshuaj muaj qhov zoo ntawm kev hloov pauv dav dav, tsis muaj kev pheej hmoo ntawm kev sib txuas sib txuas 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 yog tsis absorbed thiab yuav tsum tau excreted Cov tshuaj yog excreted los ntawm lub cev. Nyob rau hauv cov nqe lus ntawm kev cia khoom, tom qab ib tug loj tus naj npawb ntawm cov kev ntsuam xyuas, nws yuav luag tsis nkig nyob rau hauv cov av qis, thiab cov khoom ntawm capsule plhaub tseem nyob ruaj khov nyob rau hauv high humidity tej yam kev mob, thiab cov cim qhia ntawm cov nroj tsuag capsules tsis cuam tshuam nyob rau hauv huab cia. tej yam kev mob. 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-type kua npaj yog ib qho kev siv tshuaj kho mob ntau npaum li cas, uas yog ib qho kev sib cais ntawm cov tshuaj uas tsis muaj dej txaus yog dispersed hauv cov kua dispersion nruab nrab. Qhov kev ruaj ntseg ntawm qhov system txiav txim siab qhov zoo ntawm kev ncua kev ua kua ua 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:

Hydroxypropyl cellulose (HPC) yog non-ionic cellulose ib ether 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 tus polar solvents, thiab nws qhov kev ua tau zoo cuam tshuam nrog cov ntsiab lus ntawm hydroxypropyl pawg thiab qib ntawm polymerization. HPC tuaj yeem sib xyaw nrog ntau yam tshuaj thiab muaj qhov zoo inertia.

Tsawg-substituted hydroxypropyl cellulose (L-HPC) yog siv los ua ntsiav tshuaj disintegrant thiab binder. -HPC tuaj yeem txhim kho qhov nyuaj thiab ci ntsa iab ntawm cov ntsiav tshuaj, thiab tseem tuaj yeem ua rau cov ntsiav tshuaj tawg sai sai, txhim kho cov khoom siv sab hauv zoo, thiab txhim kho cov nyhuv curative.

Highly substituted hydroxypropyl cellulose (H-HPC) yuav siv tau raws li ib tug binder rau ntsiav tshuaj, granules, thiab nplua granules nyob rau hauv lub kws tshuaj. H-HPC muaj cov yeeb yaj kiab zoo heev, thiab cov yeeb yaj kiab tau yog tawv thiab elastic, uas tuaj yeem muab piv nrog cov yas yas. Kev ua tau zoo ntawm cov yeeb yaj kiab tuaj yeem txhim kho ntxiv los ntawm kev sib xyaw nrog lwm cov tshuaj tiv thaiv cov dej noo, 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

Hydroxyethyl cellulose (HEC) yog non-ionic cellulose ib ether ua los ntawm paj rwb thiab ntoo los ntawm alkalization thiab etherification ntawm ethylene oxide. Hauv kev lag luam tshuaj, 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 sustained-release material, and can be apply to topical emulsions, ointments, eye drops, Cov kua hauv qhov ncauj, cov ntsiav tshuaj, cov tshuaj ntsiav thiab lwm cov ntawv siv tshuaj. Hydroxyethyl cellulose tau raug kaw nyob rau hauv US Pharmacopoeia / US National Formulary thiab European Pharmacopoeia.

Ethyl cellulose:

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, kua qaub los yog alkali tov, thiab soluble nyob rau hauv organic solvents xws li ethanol thiab methanol. Feem ntau siv cov kuab tshuaj yog toluene / ethanol li 4/1 (qhov hnyav) sib xyaw hnyav. EC muaj ntau yam siv hauv kev npaj tshuaj tiv thaiv-tso tawm, dav siv los ua cov khoom thauj, microcapsules, thiab txheej txheej zaj duab xis-tsim cov ntaub ntawv rau kev npaj-tso tawm, xws li ntsiav tshuaj blockers, nplaum, thiab cov ntaub ntawv txheej txheej, siv los ua cov ntaub ntawv matrix los npaj. ntau hom matrix sustained-tso ntsiav tshuaj, siv los ua cov khoom sib xyaw ua ke los npaj cov txheej txheem tso tawm-tso tawm, txhawb nqa-tso pellets, thiab siv los ua encapsulation auxiliary cov ntaub ntawv los npaj sustained-tso microcapsules; nws kuj tuaj yeem siv dav los ua cov khoom thauj khoom rau kev npaj cov khoom tawg; dav siv nyob rau hauv kev siv tshuaj technology raws li ib tug zaj duab xis-forming tshuaj thiab tiv thaiv txheej, raws li zoo raws li binder thiab muab tub lim. Raws li kev tiv thaiv txheej ntawm 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 kev cuam tshuam los ntawm noo noo, discoloration thiab deterioration; Nws tseem tuaj yeem tsim cov txheej txheem qeeb-tso gel, microencapsulate lub polymer, thiab pab kom muaj kev tso tawm ntawm cov nyhuv tshuaj.