I-Excipients Yezemithi I-Cellulose Ether

I-ether cellulose ether iyitemu elivamile lochungechunge lweama-cellulose derivativesekhiqizwa ukusabela kwe-alkali cellulose kanye ne-ejenti etherifying ngaphansi kwezimo ezithile. Kungumkhiqizo lapho amaqembu e-hydroxyl ku-cellulose macromolecules eshintshwa kancane noma ngokuphelele ngamaqembu e-ether. Ama-cellulose ethers asetshenziswa kakhulu emkhakheni we-petroleum, izinto zokwakha, okokugqoka, ukudla, imithi, namakhemikhali ansuku zonke. Emikhakheni ehlukahlukene, imikhiqizo yezinga lemithi ngokuyisisekelo iphakathi nezinga eliphezulu lemboni, enenani eliphakeme elingeziwe. Ngenxa yezidingo eziqinile zekhwalithi, ukukhiqizwa kwe-ether ye-cellulose ether yezinga lemithi nakho kunzima kakhulu. Kungashiwo ukuthi ikhwalithi yemikhiqizo yezinga lemithi ingamelela ngokuyisisekelo amandla obuchwepheshe amabhizinisi e-cellulose ether. I-cellulose ether ivamise ukungezwa njengesivimbeli, i-matrix material kanye ne-thickener ukuze kwenziwe amaphilisi e-matrix akhishwa njalo, izinto zokumboza ezincibilika esiswini, izinto zokumboza ze-microcapsule ezikhishwa njalo, izinto zefilimu yezidakamizwa ezikhishwa njalo, njll.

I-sodium carboxymethyl cellulose:

I-Carboxymethyl cellulose sodium (CMC-Na) iwuhlobo lwe-cellulose ether enokukhiqizwa nokusetshenziswa okukhulu kakhulu ekhaya naphesheya. I-ionic cellulose ether eyenziwe ngekotini nokhuni ngokusebenzisa i-alkalization kanye ne-etherification nge-chloroacetic acid. I-CMC-Na iyisakhi semithi esetshenziswa kakhulu. Ivame ukusetshenziswa njenge-binder yamalungiselelo aqinile, i-ejenti yokuqina, i-ejenti yokuqina, kanye ne-ejenti yokumisa ukulungiswa koketshezi. Ingasetshenziswa futhi njenge-matrix encibilikayo emanzini kanye nezinto zokwakha ifilimu. Ivamise ukusetshenziswa njengengxenye yefilimu yezidakamizwa ekhishwa njalo kanye nethebhulethi ye-matrix ekhishwa okuqhubekayo kumalungiselelo okukhululwa (okulawulwayo).

Ngaphezu kwe-sodium carboxymethylcellulose njengesamukeli sezemithi, i-croscarmellose sodium ingasetshenziswa futhi njengesithako semithi. I-Croscarmellose sodium (CCMC-Na) iwumkhiqizo ongancibiliki emanzini we-carboxymethylcellulose esabela nge-ejenti exhumanisayo ezingeni lokushisa elithile (40-80°C) ngaphansi kwesenzo se-acid catalyst ye-inorganic futhi yahlanzwa. Njenge-agent ehlanganisayo, i-propylene glycol, i-succinic anhydride, i-anhydride ye-maleic ne-adipic anhydride ingasetshenziswa. I-Croscarmellose sodium isetshenziswa njenge-disintegrant yamaphilisi, amaphilisi kanye nama-granules ekulungiseleleni ngomlomo. Incike emiphumeleni ye-capillary kanye nokuvuvukala ukuze ihlakazeke. Inokucindezela okuhle namandla aqinile okuhlakazeka. Ucwaningo luye lwabonisa ukuthi izinga lokuvuvukala le-croscarmellose sodium emanzini likhulu kunalelo lama-disintegrants avamile njenge-low-substituted carmellose sodium kanye ne-hydrated microcrystalline cellulose.

I-Methylcellulose:

I-Methyl cellulose (MC) iyi-ether engeyona i-ionic cellulose eyenziwe kusuka ukotini nokhuni ngokusebenzisa i-alkalization kanye ne-methyl chloride etherification. I-Methylcellulose inokunyibilika okuhle kakhulu kwamanzi futhi izinzile ebangeni le-pH2.0~13.0. Isetshenziswa kabanzi kuma-excipients emithi, futhi isetshenziswa kumathebulethi angaphansi kwezilimi, imijovo ye-intramuscular, amalungiselelo e-ophthalmic, amaphilisi omlomo, ukumiswa komlomo, amaphilisi omlomo kanye namalungiselelo ama-topical. Ngaphezu kwalokho, emalungiselelweni okukhishwa okuqhubekayo, i-MC ingasetshenziswa njengamalungiselelo okukhishwa okuqhubekayo kwejeli le-hydrophilic, izinto zokumboza ezincibilika esiswini, izinto zokumboza ze-microcapsule ezikhishwa njalo, izinto zefilimu zezidakamizwa ezikhishwa njalo, njll.

I-Hydroxypropyl methyl cellulose:

IHydroxypropyl methylcellulose (HPMC) iyi-ether engeyona ionic cellulose eyenziwe ngokotini nokhuni ngokusebenzisa i-alkalization, i-propylene oxide ne-methyl chloride etherification. Ayinaphunga, ayinambitheki, ayinobuthi, iyancibilika emanzini abandayo futhi ifakwe emanzini ashisayo. IHydroxypropyl methylcellulose iwuhlobo lwe-cellulose exubile ether ukukhiqizwa kwayo, umthamo kanye nekhwalithi kukhule ngokushesha e-China eminyakeni eyi-15 edlule. Futhi ingenye yezinto ezisiza kakhulu ezenza imithi ekhaya naphesheya. iminyaka yomlando. Njengamanje, ukusetshenziswa kwe-HPMC kubonakala kakhulu kulezi zici ezinhlanu ezilandelayo:

Enye injenge-binder ne-disintegrant. Njengesibophezelo, i-HPMC ingenza umuthi ube lula ukumanziswa, futhi inganwebeka izikhathi ezingamakhulu ngemva kokumunca amanzi, ngakho ingathuthukisa kakhulu izinga lokuchithwa noma izinga lokukhululwa kwethebhulethi. I-HPMC ine-viscosity eqinile, engathuthukisa i-viscosity yezinhlayiyana futhi ithuthukise ukuminyana kwezinto ezingavuthiwe ngokuthungwa okuhlanzekile noma okuphukayo. I-HPMC ene-viscosity ephansi ingasetshenziswa njenge-binder ne-disintegrant, futhi lezo ezine-viscosity ephezulu zingasetshenziswa kuphela njenge-binder.

Okwesibili kunjengokukhishwa okuqhubekayo nokulawulwayo kwamalungiselelo omlomo. I-HPMC yinto evame ukusetshenziswa ye-hydrogel matrix kumalungiselelo okukhishwa okuqhubekayo. Ibanga le-viscosity ephansi (5-50mPa·s) I-HPMC ingasetshenziswa njenge-binder, i-viscosifier kanye ne-ejenti elengayo, kanye nebanga le-viscosity ephezulu (4000-100000mPa·s) I-HPMC ingasetshenziswa ukulungisa izinto ezixubile I-ejenti yokuvimba amaphilisi, i-hydrogel matrix. amaphilisi okukhishwa okunwetshiwe. I-HPMC iyancibilika oketshezini lwamathumbu, inezinzuzo zokucindezelwa okuhle, uketshezi oluhle, umthamo oqinile wokulayisha izidakamizwa, nezici zokukhishwa kwezidakamizwa ezingathintwa yi-PH. Kuyimpahla ethwala i-hydrophilic ebaluleke kakhulu ezinhlelweni zokulungiselela ukukhishwa okuqhubekayo futhi ivame ukusetshenziswa njenge-Hydrophilic gel matrix kanye nezinto zokumboza ukuze kulungiselelwe ukukhishwa okuqhubekayo, kanye nezinto ezisizayo zamalungiselelo antantayo esiswini kanye namalungiselelo efilimu ezidakamizwa ezikhishwa njalo.

Okwesithathu kufana ne-ejenti yokuhlanganisa ifilimu. I-HPMC inezinto ezinhle zokwenza ifilimu. Ifilimu eyakhiwe yiyo ifana, isobala futhi iqinile, futhi akulula ukunamathela ngesikhathi sokukhiqiza. Ikakhulukazi izidakamizwa ezilula ukumunca umswakama futhi azinzile, ukuyisebenzisa njengesendlalelo sokuzihlukanisa kungathuthukisa kakhulu ukuzinza kwesidakamizwa futhi kuvimbele Ifilimu ishintsha umbala. I-HPMC inezinhlobonhlobo zokucaciswa kwe-viscosity. Uma kukhethwe kahle, ikhwalithi nokubukeka kwamaphilisi aboshwe kuphakeme kunezinye izinto. Ukugxila okuvamile kungu-2% kuya ku-10%.

Okwesine kunjengempahla ye-capsule. Eminyakeni yamuva nje, njengoba kuqubuke njalo izifo eziwumshayabhuqe zezilwane emhlabeni wonke, uma kuqhathaniswa namaphilisi e-gelatin, amaphilisi emifino asephenduke isithandwa esisha sezimboni zemithi nokudla. I-Pfizer yase-United States ikhiphe ngempumelelo i-HPMC ezitshalweni zemvelo futhi yalungiselela amaphilisi emifino e-VcapTM. Uma kuqhathaniswa namaphilisi e-gelatin angenalutho endabuko, amaphilisi ezitshalo anezinzuzo zokuguquguquka okubanzi, akukho bungozi bokusabela okuxhumanisayo kanye nokuzinza okuphezulu. Izinga lokukhishwa kwezidakamizwa lizinzile, futhi umehluko ngamunye mncane. Ngemva kokuhlakazeka emzimbeni womuntu, awumuncwe futhi ungakhishwa Lo muthi ukhishwa emzimbeni. Ngokuya kwezimo zokugcina, ngemuva kwenani elikhulu lokuhlolwa, cishe ayibiki ngaphansi kwezimo zomswakama ophansi, futhi izakhiwo zegobolondo le-capsule zisazinzile ngaphansi kwezimo zomswakama ophezulu, futhi izinkomba zamaphilisi ezitshalo azithinteki ngaphansi kwesitoreji esiphezulu. izimo. Ngokuqonda kwabantu ngamaphilisi ezitshalo kanye nokuguqulwa kwemiqondo yemithi yomphakathi ekhaya naphesheya, isidingo semakethe samaphilisi ezitshalo sizokhula ngokushesha.

Eyesihlanu injenge-ejenti elengayo. Ukulungiswa koketshezi lohlobo olumisiwe kuyifomu lemithamo yomtholampilo evame ukusetshenziswa, okuwuhlelo lokuhlakazeka oluhlukahlukene lapho izidakamizwa eziqinile ezingancibiliki zihlakazwa endaweni yokusabalalisa uketshezi. Ukuzinza kwesistimu kunquma ikhwalithi yokulungiswa koketshezi lokumiswa. Isixazululo se-HPMC se-colloidal singanciphisa ukungezwani kwe-solid-liquid interfacial, sinciphise amandla angaphandle ezinhlayiya eziqinile, futhi sizinzise uhlelo lokuhlakazeka oluhlukahlukene. Kuyi-ejenti enhle kakhulu yokumisa okwesikhashana. I-HPMC isetshenziswa njenge-thiener yamaconsi esweni, enokuqukethwe okungu-0.45% kuya ku-1.0%.

I-Hydroxypropyl Cellulose:

IHydroxypropyl cellulose (HPC) iyi-ether engeyona ionic cellulose eyenziwe ngokotini nokhuni ngokusebenzisa i-alkalization kanye ne-propylene oxide etherification. I-HPC ivamise ukuncibilika emanzini angaphansi kuka-40 ° C kanye nenani elikhulu lezincibilikisi ze-polar, futhi ukusebenza kwayo kuhlobene nokuqukethwe kweqembu le-hydroxypropyl kanye nezinga le-polymerization. I-HPC ingahambisana nemithi ehlukahlukene futhi ine-inetia enhle.

I-low-substituted hydroxypropyl cellulose (L-HPC) isetshenziswa kakhulu njenge-disintegrant yethebhulethi kanye ne-binder. -I-HPC ingathuthukisa ubulukhuni nokukhanya kwethebhulethi, futhi ingenza ithebhulethi ihlakazeke ngokushesha, ithuthukise ikhwalithi yangaphakathi yethebhulethi, futhi ithuthukise umphumela wokwelapha.

I-hydroxypropyl cellulose (H-HPC) efakwe endaweni ephezulu kakhulu ingasetshenziswa njengesibophezelo samaphilisi, ama-granules, nama-granules amahle emkhakheni wezokwelapha. I-H-HPC inezinto ezinhle kakhulu zokwenza ifilimu, futhi ifilimu etholiwe iqinile futhi iyanwebeka, engafaniswa ne-plasticizers. Ukusebenza kwefilimu kungathuthukiswa ngokuqhubekayo ngokuxubana namanye ama-agent amelana nomswakama, futhi kuvame ukusetshenziswa njengento yokumboza ifilimu yamaphilisi. I-H-HPC ingasetshenziswa futhi njengezinto ze-matrix ukuze kulungiswe amaphilisi akhishwa ngokuqhubekayo e-matrix, amaphilisi akhishwa isikhathi eside kanye namaphilisi akhishwa ngokugcwele anezendlalelo ezimbili.

I-Hydroxyethyl cellulose

I-Hydroxyethyl cellulose (HEC) iyi-ether engeyona ionic cellulose eyenziwe ngokotini nokhuni ngokusebenzisa i-alkalization kanye ne-etherification ye-ethylene oxide. Emkhakheni wezokwelapha, i-HEC isetshenziswa ikakhulukazi njenge-thickener, i-colloidal protective agent, i-adhesive, dispersant, stabilizer, i-ejenti yokumisa, i-ejenti eyenza ifilimu kanye nezinto ezikhishwa okuqhubekayo, futhi ingasetshenziswa kuma-emulsions we-topical, amafutha okugcoba, amaconsi iso, I-Oral liquid, ithebhulethi eqinile, i-capsule namanye amafomu omthamo. I-Hydroxyethyl cellulose irekhodwe ku-US Pharmacopoeia/US National Formulary kanye ne-European Pharmacopoeia.

I-Ethyl cellulose:

I-Ethyl cellulose (EC) ingenye yezinto eziphuma ku-cellulose ezingancibiliki emanzini ezisetshenziswa kakhulu. I-EC ayinabo ubuthi, izinzile, ayincibiliki emanzini, i-asidi noma isixazululo se-alkali, futhi incibilika kuzincibilikisi zemvelo njenge-ethanol ne-methanol. I-solvent evame ukusetshenziswa yi-toluene/ethanol njenge-4/1 (isisindo) esixubene se-solvent. I-EC inokusetshenziswa okuningi ekulungiseleleni ukukhishwa okuqhubekayo kwezidakamizwa, ezisetshenziswa kabanzi njengezithwali, ama-microcapsules, kanye nezinto zokwakha ifilimu zokunameka ukulungiselela ukukhishwa okuqhubekayo, njengezivimbeli zethebhulethi, izinto zokunamathisela, nezinto zokumboza ifilimu, ezisetshenziswa njengefilimu ye-matrix ukuze kulungiswe. izinhlobo ezahlukene zamaphilisi akhishwa njalo e-matrix, asetshenziswa njengezinto ezixubile ukuze kulungiswe amalungiselelo okukhululwa okuqhubekayo okuboshiwe, ama-pellets akhishwa okuqhubekayo, futhi asetshenziswa njengezinto ezisizayo ze-encapsulation ukuze kulungiswe ama-microcapsules akhishwa njalo; ingasetshenziswa kabanzi njengento ethwalayo Ukuze kulungiswe ama-dispersions aqinile; esetshenziswa kabanzi kwezobuchwepheshe bezemithi njengento eyenza ifilimu kanye nenamathela evikelayo, kanye ne-binder ne-filler. Njengendwangu yokuvikela yethebhulethi, inganciphisa ukuzwela kwethebhulethi kumswakama futhi ivimbele umuthi ukuthi ungathinteki umswakama, ukuguquguquka nokuwohloka; ingase futhi yakhe isendlalelo sejeli ekhishwa kancane, i-microencapsulate i-polymer, futhi inike amandla ukukhululwa okuqhubekayo komphumela wesidakamizwa.