Izinto ezisetshenziswa ekhemisi ziyizinto ezisetshenziswa ekukhiqizweni kwemithi kanye nokwakhiwa kwemithi kadokotela, futhi ziyingxenye ebalulekile yokulungiselela imithi. Njengezinto zemvelo ezithathwe ku-polymer, i-cellulose ether inezici zokubola, ukungabi nobuthi, kanye nentengo ephansi, njenge-sodium carboxymethyl cellulose, i-methyl cellulose, i-hydroxypropyl methyl cellulose, i-hydroxypropyl cellulose,Ama-ether e-cellulosenjenge-hydroxyethyl cellulose kanye ne-ethyl cellulose zinenani elibalulekile lokusetshenziswa ezintweni ezisizayo zemithi. Njengamanje, imikhiqizo yamabhizinisi amaningi e-cellulose ether asekhaya isetshenziswa kakhulu emikhakheni ephakathi nephansi embonini, futhi inani elengeziwe aliphezulu. Imboni idinga ngokushesha ukuguqula nokuthuthukisa nokuthuthukisa ukusetshenziswa kwemikhiqizo okusezingeni eliphezulu.
Izinto ezisizayo zemithi zidlala indima ebalulekile ekuthuthukisweni nasekukhiqizweni kwezakhi. Isibonelo, kumalungiselelo okukhululwa okuqhubekayo, izinto ze-polymer ezifana ne-cellulose ethers zisetshenziswa njengezinto ezisizayo zemithi kuma-pellets akhululwa okuqhubekayo, izinhlobo ezahlukene ze-matrix sustained-release formulations, ezihlanganisiwe ezikhishwa okuqhubekayo, ama-capsules akhululwa okuqhubekayo, amafilimu emithi akhululwa okuqhubekayo, kanye nemithi ye-resin ekhishwa okuqhubekayo. Amalungiselelo kanye namalungiselelo okukhululwa okuqhubekayo okuketshezi asetshenziswe kabanzi. Kulesi simiso, ama-polymers afana ne-cellulose ethers ngokuvamile asetshenziswa njengabathwali bemithi ukulawula izinga lokukhululwa kwemithi emzimbeni womuntu, okungukuthi, kudingeka ukuthi ikhishwe kancane kancane emzimbeni ngesilinganiso esibekiwe ngaphakathi kwesikhathi esithile ukuze kufezwe inhloso yokwelashwa okuphumelelayo.
Ngokwezibalo zoMnyango Wezokubonisana Nocwaningo, kunezinhlobo ezingaba ngu-500 zezinto ezisizayo emakethe ezweni lakithi, kodwa uma kuqhathaniswa ne-United States (izinhlobo ezingaphezu kuka-1500) kanye ne-European Union (izinhlobo ezingaphezu kuka-3000), kunomehluko omkhulu, futhi izinhlobo zisencane. Izinto ezisizayo zemithi ezweni lakithi Amandla okuthuthukiswa kwemakethe makhulu kakhulu. Kuyaqondakala ukuthi izinto ezisizayo zemithi eziyishumi eziphezulu esikalini semakethe yezwe lakithi ama-capsule e-gelatin yezokwelapha, i-sucrose, isitashi, i-powder yokumboza ifilimu, i-1,2-propylene glycol, i-PVP, i-hydroxypropyl methylcellulose (HPMC), kanye ne-microcrystalline fibers. I-Vegetarian, i-HPC, i-lactose.
"I-ether ye-cellulose yemvelo yigama elijwayelekile lochungechunge lwezinto eziphuma ku-cellulose ezikhiqizwa ukusabela kwe-alkali cellulose kanye ne-etherifying agent ngaphansi kwezimo ezithile, futhi ingumkhiqizo lapho amaqembu e-hydroxyl ku-cellulose macromolecule ethathelwa indawo ngokwengxenye noma ngokuphelele amaqembu e-ether. Ama-ether e-cellulose asetshenziswa kabanzi emikhakheni ye-petroleum, izinto zokwakha, izinto zokumboza, ukudla, imithi kanye namakhemikhali ansuku zonke. Kuzo zonke izinkambu, imikhiqizo yezinga lemithi isendaweni ephakathi nendawo ephezulu embonini futhi inenani eliphezulu elengeziwe. Ngenxa yezidingo zekhwalithi eqinile, ukukhiqizwa kwama-ether e-cellulose ezinga lemithi nakho kunzima. Kungashiwo ukuthi ikhwalithi yemikhiqizo yezinga lemithi ingamelela amandla obuchwepheshe ezinkampanini ze-ether ze-cellulose. I-ether ye-Cellulose ivame ukungezwa njenge-retarder, i-matrix material kanye ne-thickener ukwenza amaphilisi e-matrix akhululwayo okuqhubekayo, izinto zokumboza ezincibilika esiswini, izinto zokupakisha ze-microcapsule ezikhululwayo okuqhubekayo, izinto zefilimu yemithi ekhululwayo okuqhubekayo, njll.
I-Sodium carboxymethyl cellulose (CMC-Na) iyi-cellulose ether ekhiqiza kakhulu futhi isetshenziswa ekhaya nakwamanye amazwe. Iyi-ionic cellulose ether eyenziwe ngokotini nangokhuni ngokusebenzisa i-alkalizing kanye ne-etherification nge-chloroacetic acid. I-CMC-Na iyi-excipient yemithi esetshenziswa kakhulu. Ivame ukusetshenziswa njenge-binder yokulungiselela okuqinile kanye ne-ejenti yokuqinisa, ukuqina kanye nokumisa amalungiselelo oketshezi. Ingasetshenziswa futhi njenge-matrix encibilikayo emanzini kanye nezinto zokwakha ifilimu. Ivame ukusetshenziswa njengezinto zefilimu yezidakamizwa ezikhishwa njalo kanye nethebhulethi ye-matrix ekhishwa njalo ekwakhiweni kokukhululwa okuqhubekayo (okulawulwayo).
Ngaphezu kwe-sodium carboxymethyl cellulose njengezinto ezisizayo zemithi, i-croscarmellose sodium ingasetshenziswa futhi njengezinto ezisizayo zemithi. I-Cross-linked carboxymethyl cellulose sodium (CCMC-Na) iyisithako esingancibiliki emanzini i-carboxymethyl cellulose esabela kuso ne-cross-linking agent ekushiseni okuthile (40-80°C) ngaphansi kwesenzo se-inorganic acid catalyst futhi iyahlanzwa. I-crosslinking agent ingaba yi-propylene glycol, i-succinic anhydride, i-maleic anhydride, i-adipic anhydride, nokunye okunjalo. I-Crosscarmellose sodium isetshenziswa njengesithasiselo samathebulethi, ama-capsule nama-granules ekulungiseleleni ngomlomo. Ithembele emiphumeleni ye-capillary kanye nokuvuvukala ukuze ifinyelele ekuqhekekeni. Inokucindezela okuhle kanye nokuqhekeka okunamandla. Izifundo zibonise ukuthi izinga lokuvuvukala kwe-croscarmellose sodium emanzini likhulu kunele-disintegrants ezivamile njenge-low-substituted sodium carboxymethyl cellulose kanye ne-hydrated microcrystalline cellulose.
I-Methyl cellulose (MC) iyi-non-ionic cellulose monoether eyenziwe ngokotini nangokhuni ngokusebenzisa i-alkalization kanye ne-methyl chloride etherification. I-Methyl cellulose inokuncibilika kwamanzi okuhle kakhulu futhi izinzile kububanzi be-pH obungu-2.0 kuya ku-13.0. Isetshenziswa kabanzi ezithakweni zemithi, futhi isetshenziswa kumaphilisi angaphansi kwezilimi, imijovo ye-intramuscular, amalungiselelo omehlo, ama-capsule omlomo, ama-suspension omlomo, amaphilisi omlomo kanye namalungiselelo angaphandle. Ngaphezu kwalokho, ekwakhiweni kokukhululwa okuqhubekayo, i-MC ingasetshenziswa njenge-hydrophilic gel matrix sustainable-release formulation, izinto zokumboza ezincibilikayo esiswini, izinto zokupakisha ze-microcapsule sustainable-release, izinto zefilimu yemithi ekhishwa njalo, njll.
I-Hydroxypropyl methylcellulose (HPMC) iyi-ether exubile ye-cellulose engeyona i-ionic eyenziwe ngokotini nangokhuni ngokusebenzisa i-alkalizing kanye ne-etherification ye-propylene oxide kanye ne-methyl chloride. Ayinaphunga, ayinambitheki, ayinabuthi, iyancibilika emanzini abandayo, kanye nama-gel emanzini ashisayo. I-Hydroxypropyl methylcellulose uhlobo lwe-ether exubile ye-cellulose oluye lwanda ngokushesha ekukhiqizweni, ekusetshenzisweni kanye nasekhwalithini eminyakeni eyi-15 edlule. Futhi ingenye yezinto ezinkulu kakhulu ezisetshenziswa kwezokwelapha ekhaya nakwamanye amazwe. Isetshenziswe njengesithako semithi iminyaka ecishe ibe ngu-50. Iminyaka yomlando. Njengamanje, ukusetshenziswa kwe-HPMC kubonakala kakhulu kulezi zici ezinhlanu ezilandelayo:
Enye injengesihlanganisi futhi ihlukane. I-HPMC njengesihlanganisi ingenza umuthi ube lula ukuwumanzisa, futhi inganwebeka izikhathi ezingamakhulu ngemva kokumunca amanzi, ngakho-ke ingathuthukisa kakhulu ukuncibilika noma ukukhululwa kwethebhulethi. I-HPMC ine-viscosity enamandla, futhi ingathuthukisa i-particle viscosity futhi ithuthukise ukucindezelwa kwezinto zokusetshenziswa ngokuthungwa okuqinile noma okuqinile. I-HPMC ene-viscosity ephansi ingasetshenziswa njenge-binder kanye ne-viscosity, kanti i-HPMC ene-viscosity ephezulu ingasetshenziswa kuphela njenge-binder.
Okwesibili, isetshenziswa njengento yokukhululwa okuqhubekayo nokulawulwayo yokulungiselela ngomlomo. I-HPMC iyinto evame ukusetshenziswa njenge-hydrogel matrix kumalungiselelo okukhululwa okuqhubekayo. I-HPMC yezinga eliphansi le-viscosity (5 ~ 50mPa·s) ingasetshenziswa njenge-binder, i-viscosity increasing agent kanye ne-suspending agent, kanye ne-HPMC yezinga eliphezulu le-viscosity (4000 ~ 100000mPa·s) ingasetshenziswa ukulungiselela amaphilisi e-mixed matrix sustainable-release kanye ne-sustained-release Blocker yama-capsules kanye namaphilisi e-hydrophilic gel matrix sustainable-release. I-HPMC iyancibilika emanzini okugaya ukudla, inezinzuzo zokucindezelwa okuhle, ukugeleza okuhle, amandla okulayisha izidakamizwa aqinile kanye nezici zokukhululwa kwezidakamizwa ezingathinteki yi-pH. Iyinto ebaluleke kakhulu yokuthwala i-hydrophilic ezinhlelweni zokulungiselela ukukhululwa okuqhubekayo futhi ivame ukusetshenziswa njenge-hydrophilic gel matrix kanye nezinto zokumboza zamalungiselelo okukhululwa okuqhubekayo, futhi isetshenziswa kumalungiselelo okuntanta esiswini kanye nezinto ezisizayo ze-membrane yezidakamizwa ezikhishwa okuqhubekayo.
Okwesithathu kunjenge-ejenti yokwenza ifilimu embozwe.I-HPMCinezakhiwo ezinhle zokwakha ifilimu. Ifilimu eyakhiwe yiyo iyafana, icacile, futhi iqinile, futhi akulula ukunamathela ngesikhathi sokukhiqiza. Ikakhulukazi ngemithi okulula ukuyimunca umswakama futhi engazinzile, ukuyisebenzisa njengesendlalelo sokuhlukanisa kungathuthukisa kakhulu ukuzinza komuthi futhi kuvimbele. Ifilimu ishintsha umbala. I-HPMC inezinhlobo ezahlukene ze-viscosity specifications. Uma ikhethwe kahle, ikhwalithi kanye nokubukeka kwamaphilisi amboziwe kungcono kunezinye izinto, futhi ukuhlushwa kwayo okuvamile kungu-2% kuya ku-10%.
I-Four isetshenziswa njengezinto ze-capsule. Eminyakeni yamuva nje, ngokuqubuka okuvamile kwezifo zezilwane emhlabeni jikelele, uma kuqhathaniswa nama-capsule e-gelatin, ama-capsule ezitshalo abe yinto entsha ethandwayo yezimboni zemithi nezokudla. I-Pfizer ikhiphe ngempumelelo i-HPMC ezitshalweni zemvelo futhi yalungisa ama-capsule emifino e-VcapTM. Uma kuqhathaniswa nama-capsule e-gelatin angavamile, ama-capsule emifino anezinzuzo zokuzivumelanisa nezimo kabanzi, akukho bungozi bokusabela okuxhumene, kanye nokuqina okuphezulu. Izinga lokukhishwa kwemithi lizinzile, futhi umehluko ngamunye mncane. Ngemva kokuqhekeka emzimbeni womuntu, awumuncwa futhi ungakhishwa. Ukhishwa emzimbeni. Ngokuphathelene nezimo zokugcina, ngemuva kokuhlolwa okuningi, cishe awukhuli kahle ngaphansi kwezimo zomswakama ophansi, futhi izakhiwo zegobolondo le-capsule zisazinzile ngaphansi komswakama ophezulu, futhi izinkomba ezahlukahlukene zama-capsule ezitshalo ngaphansi kwezimo zokugcina ezibucayi azithinteki. Ngokuqonda kwabantu ama-capsule ezitshalo kanye nokuguqulwa kwemibono yezokwelapha zomphakathi ekhaya nakwamanye amazwe, isidingo semakethe sama-capsule ezitshalo sizokhula ngokushesha.
Okwesihlanu kunjenge-ejenti yokumisa. Ukulungiswa koketshezi lohlobo lokumisa kuyindlela yokwelapha evame ukusetshenziswa, okuwuhlelo lokusabalala olungafani lapho izidakamizwa eziqinile ezingancibiliki kalula zisakazwa endaweni yokusabalala koketshezi. Ukuqina kohlelo kunquma ikhwalithi yamalungiselelo oketshezi lokumisa. Isixazululo se-HPMC colloidal singanciphisa ukungezwani koketshezi oluqinile, sinciphise amandla angenawo umphezulu wezinhlayiya eziqinile, futhi sizinzise uhlelo lokusabalala olungafani. Kuyi-ejenti yokumisa enhle kakhulu. I-HPMC isetshenziswa njengesithambisi samaconsi eso, ngokuqukethwe okungu-0.45% kuya ku-1.0%.
I-Hydroxypropyl cellulose (HPC) iyi-non-ionic cellulose monoether eyenziwe ngokotini nangokhuni ngokusebenzisa i-alkalization kanye ne-propylene oxide etherification. I-HPC ivame ukuncibilika emanzini angaphansi kuka-40°C kanye nenani elikhulu le-polar solvents, futhi ukusebenza kwayo kuhlobene nokuqukethwe kwe-hydroxypropyl kanye nezinga le-polymerization. I-HPC ingahambisana nemithi ehlukahlukene futhi inokungasebenzi kahle.
I-hydroxypropyl cellulose ethathelwe indawo kancane(L-HPC)Isetshenziswa kakhulu njenge-tablet disintegrant kanye ne-binder. Izici zayo yilezi: kulula ukuyicindezela nokuyibumba, ukusebenza kwayo okuqinile, kunzima kakhulu ukuyibumba, amaphilisi epulasitiki naqhekeka kalula, i-L -HPC ingathuthukisa ubulukhuni bethebhulethi kanye nokukhanya kokubukeka, futhi ingenza ithebhulethi iqhekeke ngokushesha, ithuthukise ikhwalithi yangaphakathi yethebhulethi, futhi ithuthukise umphumela wokwelapha.
I-hydroxypropyl cellulose (H-HPC) efakwe esikhundleni esiphezulu ingasetshenziswa njenge-ejenti yokubopha amaphilisi, ama-granule nama-granule amahle emkhakheni wezokwelapha. I-H-HPC inezakhiwo ezinhle kakhulu zokwakha ifilimu, futhi ifilimu ephumayo iqinile futhi iyanwebeka, engaqhathaniswa nama-plasticizer. Ngokuxuba nezinye izinto zokumboza ezilwa nokumanzi, ukusebenza kwefilimu kungathuthukiswa kakhulu, futhi ivame ukusetshenziswa njengezinto zokumboza ifilimu zamaphilisi. I-H-HPC ingasetshenziswa futhi njengezinto ze-matrix ukulungiselela amaphilisi okukhululwa okuqhubekayo kwe-matrix, ama-pellet okukhululwa okuqhubekayo kanye namaphilisi okukhululwa okuqhubekayo aphindwe kabili.
I-Hydroxyethyl cellulose (HEC) iyi-monoether ye-cellulose engeyona i-ionic eyenziwe ngokotini nangokhuni ngokusebenzisa i-alkaliization kanye ne-ethylene oxide etherification. I-HEC isetshenziswa kakhulu njenge-thickener, i-colloidal protective agent, i-adhesive, i-dispersant, i-stabilizer, i-suspending agent, i-film-forming agent kanye nezinto ezikhipha kancane emkhakheni wezokwelapha. Ingasetshenziswa kuma-emulsions, amafutha okugcoba, kanye namaconsi amehlo emithi yokwelapha. Uketshezi lomlomo, amaphilisi aqinile, ama-capsules kanye nezinye izinhlobo zomthamo. I-Hydroxyethyl cellulose ifakiwe ku-US Pharmacopoeia/US National Formulary kanye ne-European Pharmacopoeia.
I-Ethyl cellulose (EC) ingenye yezinto ezisetshenziswa kakhulu ezitholakala kuma-cellulose angancibiliki emanzini. I-EC ayinobuthi, izinzile, ayincibiliki emanzini, ezixazululweni ze-asidi noma ze-alkaline, futhi incibilika ezixazululweni eziphilayo ezifana ne-ethanol ne-methanol. I-solvent evame ukusetshenziswa iyi-solvent exubile ye-toluene/ethanol 4/1 (isisindo). I-EC inokusetshenziswa okuningi kumalungiselelo okukhululwa kwemithi okuqhubekayo, futhi isetshenziswa kabanzi njengesithwali kanye nama-microcapsule, izinto zokwakha ifilimu, njll. zamalungiselelo okukhululwa okuqhubekayo, njengezithambisi zamathebhulethi, izinamathiseli, izinto zokumboza ifilimu, njll. Isetshenziswa njengefilimu yezinto ze-matrix ukulungiselela izinhlobo ezahlukene zamathebhulethi okukhululwa okuqhubekayo, njengento exubile ukulungiselela amalungiselelo okukhululwa okuqhubekayo amboziwe kanye nama-pellets okukhululwa okuqhubekayo, njengento eyisizayo yokufaka i-capsulation ukulungiselela ama-microcapsule okukhululwa okuqhubekayo; ingasetshenziswa futhi kabanzi njengento yokuthwala. Isetshenziselwa ukulungiselela ukuhlakazeka okuqinile; ingasetshenziswa kabanzi kubuchwepheshe bezokwelapha njengento yokwakha ifilimu kanye nesembozo esivikelayo, futhi ingasetshenziswa futhi njengesihlanganisi kanye nesigcwalisi. Njengesembozo esivikela amaphilisi, kunganciphisa ukuzwela kwamaphilisi emswakama futhi kuvimbele imithi ukuthi ingashintshi umbala futhi yonakale ngenxa yomswakama; kungakha futhi ungqimba lweglue olukhipha kancane futhi lufake i-polymer encane ukuze ikhulule umphumela wesidakamizwa njalo.
Ngamafuphi, i-sodium carboxymethyl cellulose encibilika emanzini, i-methyl cellulose, i-hydroxypropyl methyl cellulose, i-hydroxyethyl cellulose kanye ne-ethyl cellulose encibilika uwoyela konke kusekelwe kuzo. Izici zomkhiqizo zisetshenziswa ezintweni ezisizayo zemithi njengezinamathiseli, izincibilikisi, izinto zokukhulula eziqhubekayo nezilawulwayo zokulungiselela ngomlomo, izinto zokwenza ifilimu, izinto ze-capsule kanye nezinto ezimisayo. Uma sibheka umhlaba, izinkampani eziningana zamazwe ngamazwe zakwamanye amazwe (i-Shin-Etsu Japan, i-Dow Wolff kanye ne-Ashland) zithole imakethe enkulu ye-cellulose yemithi eShayina esikhathini esizayo, futhi noma ngabe zandise ukukhiqizwa noma ukuhlanganiswa, zandise ukuba khona kwazo kulo mkhakha. Ukutshalwa kwezimali ngaphakathi kwesicelo. I-Dow Wolff imemezele ukuthi izokwandisa ukunaka kwayo ekwakhiweni, izithako kanye nezidingo zemakethe yokulungiselela imithi yaseShayina, futhi ucwaningo lwayo lokusetshenziswa luzolwela ukusondela emakethe. I-Wolff Cellulose Division ye-Dow Chemical and Colorcon Corporation yase-United States isungule umbimbi lokulungiselela ukukhululwa oluqhubekayo nolulawulwayo emhlabeni jikelele. Inabasebenzi abangaphezu kuka-1,200 emadolobheni angu-9, izikhungo zempahla ezingu-15 kanye nezinkampani ezingu-6 ze-GMP. Ochwepheshe bocwaningo abasebenzayo banikeza izinsizakalo kumakhasimende emazweni angaba ngu-160. I-Ashland inezisekelo zokukhiqiza eBeijing, eTianjin, eShanghai, eNanjing, eChangzhou, eKunshan naseJiangmen, futhi itshale imali ezikhungweni ezintathu zocwaningo lobuchwepheshe eShanghai naseNanjing.
Ngokwezibalo ezivela kuwebhusayithi ye-China Cellulose Association, ngo-2017, ukukhiqizwa kwasekhaya kwe-cellulose ether kwakungamathani angu-373,000 kanti umthamo wokuthengisa wawungamathani ayizinkulungwane ezingu-360. Ngo-2017, umthamo wangempela wokuthengisa we-ionicI-CMCkwakungamathani angu-234,000, ukwanda ngo-18.61% unyaka nonyaka, kanti umthamo wokuthengisa we-non-ionic CMC wawungamathani angu-126,000, ukwanda ngo-8.2% unyaka nonyaka. Ngaphezu kwemikhiqizo engeyona i-ionic ye-HPMC (izinga lezinto zokwakha),I-HPMC(ibanga lemithi), i-HPMC (ibanga lokudla), i-HEC, i-HPC, i-MC, i-HEMC, njll. konke kukhuphuke ngokumelene nomkhuba, futhi ukukhiqizwa nokuthengiswa kuqhubekile nokukhula. Ama-ether e-cellulose asekhaya abelokhu ekhula ngokushesha iminyaka engaphezu kweyishumi, futhi umkhiqizo ube ngowokuqala emhlabeni. Kodwa-ke, imikhiqizo eminingi yezinkampani ze-cellulose ether isetshenziswa kakhulu emkhakheni ophakathi nophansi embonini, futhi inani elengeziwe aliphezulu.
Njengamanje, iningi lamabhizinisi asekhaya e-cellulose ether asesikhathini esibucayi sokuguqulwa nokuthuthukiswa. Kufanele aqhubeke nokwandisa imizamo yocwaningo lomkhiqizo kanye nentuthuko, athuthukise njalo izinhlobo zemikhiqizo, asebenzise ngokugcwele iShayina, imakethe enkulu kunazo zonke emhlabeni, futhi andise imizamo yokuthuthukisa izimakethe zakwamanye amazwe ukuze amabhizinisi akwazi ukwanda ngokushesha okukhulu. Qedela ukuguqulwa nokuthuthukiswa, ungene emkhakheni ophakathi kuya kophezulu wemboni, futhi ufeze intuthuko engeyimbi neluhlaza.
Isikhathi sokuthunyelwe: Ephreli-25-2024