Ama-excipients ajwayelekile amafomu omthamo oqinile womlomo

Amalungiselelo aqinile njengamanje angamafomu emithamo asakazwa kakhulu futhi asetshenziswa kakhulu emakethe, futhi ngokuvamile aqukethe izinto ezimbili eziyinhloko nezinto ezisizayo.Ama-excipients, abuye aziwe ngokuthi ama-excipients, abhekisela egameni elivamile lazo zonke izinto ezengeziwe ezilungiselelweni eziqinile ngaphandle komuthi omkhulu.Ngokwezakhiwo nemisebenzi ehlukene yezinto ezisizayo, izinto ezisizayo zamalungiselelo aqinile zivame ukuhlukaniswa zibe: ama-filler, ama-binders, ama-disintegrants, ama-lubricant, izilawuli zokukhulula, futhi kwesinye isikhathi ama-ejenti ombala nama-flavoring agents nawo angangezwa ngokuya ngezidingo zokulungiselela. ukuthuthukisa Noma ukulungisa ukubukeka nokunambitha kokwakheka.
Izinto ezisizayo zamalungiselelo aqinile kufanele zihlangabezane nezidingo zokusetshenziswa komuthi, futhi zibe nezici ezilandelayo: ①Kufanele zibe nokusimama okuphezulu kwamakhemikhali futhi zingabi nokuhlangana komzimba namakhemikhali ngomuthi omkhulu;②Akumele kuthinte umphumela wokwelapha kanye nokunqunywa kokuqukethwe komuthi omkhulu;③Akukho ukulimala emzimbeni womuntu Kuyingozi, ubuthi obuhlanu, akukho ukusabela okubi.
1. Isigcwalisi (encanyana)
Ngenxa yomthamo ophansi womuthi oyinhloko, umthamo wezinye izidakamizwa ngezinye izikhathi ungamamiligremu ambalwa noma ngaphansi, ongahambisani nokwakhiwa kwethebhulethi noma ukuphathwa komtholampilo.Ngakho-ke, lapho okuqukethwe kwesidakamizwa okuyinhloko kungaphansi kwama-50mg, umthamo othile wokugcwalisa, owaziwa nangokuthi i-diluent, udinga ukwengezwa.
Ukugcwalisa okufanelekile kufanele kube okungenzi lutho ngokomzimba namakhemikhali futhi kungaphazamisi i-bioavailability yesithako esisebenzayo somuthi.Izigcwalisi ezisetshenziswa kakhulu zihlanganisa: ① Isitashi, okuhlanganisa isitashi sikakolweni, isitashi sombila, nesitashi samazambane, okukhona phakathi kwawo isitashi sombila sisetshenziswa kakhulu;ezinzile ngokwemvelo, i-hygroscopicity ephansi, kodwa impofu ekucindezelekeni;② i-lactose, inhle kakhulu ngezakhiwo futhi iyacindezeleka, i-fluidity enhle;③ i-sucrose, ine-hygroscopicity eqinile;④ isitashi esenziwe i-pregelatinized, esaziwa nangokuthi isitashi esicindezelayo, sinokucindezelwa okuhle, uketshezi kanye nokuzithambisa;⑤ i-microcrystalline cellulose, ebizwa ngokuthi i-MCC, inekhono eliqinile lokubopha kanye nokucindezelwa okuhle;eyaziwa ngokuthi "i-dry binder";⑥I-Mannitol, uma iqhathaniswa nalezi zigcwalisi ezingenhla, ibiza kancane, futhi ivamise ukusetshenziswa kumaphilisi ahlafunwayo, nawo anokunambitheka okuthambile;⑦ Usawoti we-Inorganic, ikakhulukazi ohlanganisa i-calcium sulfate, i-calcium phosphate, i-calcium carbonate, njll., enezakhiwo zomzimba namakhemikhali ezizinzile.
2. I-ejenti yokumanzisa kanye ne-adhesive
Ama-ejenti wokumanzisa kanye nama-binders angabasizi abengezwe ngesikhathi sesinyathelo se-granulation.I-ejenti yokumanzisa ngokwayo ayiyona i-viscous, kodwa i-liquid eyenza i-viscosity yezinto ngokumanzisa impahla.Ama-ejenti okumanzisa asetshenziswa kakhulu ikakhulukazi afaka amanzi acwengekile kanye ne-ethanol, phakathi kwawo amanzi acwebile ayikhethelo lokuqala.
Ama-Adhesives abhekisela ezintweni ezisizayo ezithembele ku-viscosity yazo ukuze zinikeze izinto ezingezona ezibonakalayo noma ezinganele ngokwanele nge-viscosity efanelekile.Izinamatheliso ezisetshenziswa kakhulu ikakhulukazi zihlanganisa: ① I-starch slurry, okungenye yezinto ezinamathelayo ezisetshenziswa kakhulu, eshibhile, futhi isebenza kahle, futhi ukugxila okuvame ukusetshenziswa ngu-8% -15%;②Methylcellulose, ebizwa ngokuthi i-MC, inokuncibilika okuhle kwamanzi;③I-Hydroxypropylcellulose, ebizwa ngokuthi i-HPC, ingasetshenziswa njenge-powder direct tableting binder;④I-Hydroxypropylmethylcellulose, ebizwa ngokuthi i-HPMC, impahla iyancibilika emanzini abandayo;⑤Carboxymethylcellulose sodium, ebizwa ngokuthi i-CMC-Na, ilungele izidakamizwa ezinokucindezelwa okubi;⑥I-Ethylcellulose, okubizwa ngokuthi EC , impahla ayincibiliki emanzini, kodwa incibilika ku-ethanol;⑦ I-Povidone, ebizwa ngokuthi i-PVP, i-hygroscopic, inyibilika emanzini ne-ethanol;⑧Ngaphezu kwalokho, kukhona i-polyethylene glycol (ebizwa ngokuthi i-PEG), Izinto ezifana ne-gelatin.
3. Disintegrant
Ama-Disintegrants abhekisela ezintweni ezisizayo ezikhuthaza ukuhlukana ngokushesha kwamaphilisi abe yizinhlayiya ezinhle oketshezini lwamathumbu.Ngaphandle kwamaphilisi omlomo anezidingo ezikhethekile ezifana namathebulethi akhishwa njalo, amaphilisi akhishwa okulawulwayo, namaphilisi ahlafunwayo, ama-disintegrant ngokuvamile adinga ukwengezwa.Izibulala-magciwane ezivame ukusetshenziswa yilezi: ① isitashi esomile, esilungele izidakamizwa ezingancibiliki noma ezincibilika kancane;② i-carboxymethyl isitashi sesodium, ebizwa ngokuthi i-CMS-Na, le nto iyi-disintegrant esebenza kahle kakhulu;③ i-hydroxypropyl cellulose efakwe endaweni ephansi, ebizwa ngokuthi i-L -HPC, engavuvuka ngokushesha ngemva kokumunca amanzi;④I-methyl cellulose sodium exhunywe ngokuphambanayo, ebizwa nge-CCMC-Na;impahla ivuvukala kuqala emanzini bese iyancibilika, futhi ayincibiliki ku-ethanol;Okubi ukuthi ine-hygroscopicity eqinile futhi ivame ukusetshenziswa ekuhlanganiseni amaphilisi asebenzayo noma amaphilisi ahlafunwayo;⑥Ama-disintegrants asebenzayo ikakhulukazi ahlanganisa ingxube ye-sodium bicarbonate ne-citric acid, futhi i-citric acid, i-fumaric acid, ne-sodium carbonate nayo ingasetshenziswa , I-Potassium Carbonate ne-Potassium Bicarbonate njll.
4. Okokugcoba
Izinto zokugcoba zingahlukaniswa kabanzi zibe izigaba ezintathu, okuhlanganisa ama-glidants, ama-anti-sticking agents, kanye nezinto zokugcoba ngomqondo omncane.① I-Glidant: umsebenzi wayo oyinhloko ukunciphisa ukungqubuzana phakathi kwezinhlayiya, ukuthuthukisa uketshezi lwempushana, nokusiza ukunciphisa umehluko esisindweni sethebhulethi;② i-ejenti elwa nokunamathela: umsebenzi wayo oyinhloko ukuvimbela ukunamathela ngesikhathi sokucindezelwa kwethebhulethi, Ukuze kuqinisekiswe ukusebenza kahle kokucindezelwa kwethebhulethi, kungathuthukisa nokubukeka kwamaphilisi;③ i-chivalrous lubricant: nciphisa ukungqubuzana phakathi kwezinto ezibonakalayo nodonga lwesikhunta, ukuze uqinisekise ukusebenza kahle kokucindezelwa kwethebhulethi nokuphusha.Izithambisi ezivame ukusetshenziswa (ngomqondo obanzi) zifaka i-talc powder, i-magnesium stearate (MS), ijeli ye-silica emincane, i-polyethylene glycols, i-sodium lauryl sulfate, uwoyela wemifino oyi-hydrogenated, njll.
5. Khipha imojuli
Izilawuli zokukhishwa kumaphilisi omlomo zifanele ukulawula isivinini kanye nezinga lokukhululwa kwezidakamizwa kumalungiselelo omlomo okukhululwa okuqhubekayo, ukuze kuqinisekiswe ukuthi umuthi ulethwa endaweni yesiguli ngesivinini esithile futhi ugcina ukugxila okuthile ezicutshini noma oketshezini lomzimba. , ngaleyo ndlela Thola umphumela wokwelapha olindelekile futhi wehlise ubuthi nemiphumela engemihle.Izilawuli zokukhishwa ezisetshenziswa kakhulu zihlukaniswa ikakhulukazi ngohlobo lwe-matrix, i-polymer ekhishwa kancane ehlanganiswe nefilimu kanye ne-thickener.
(1) Imodeli yokukhululwa yohlobo lwe-Matrix
①I-Hydrophilic gel skeleton material: iyakhukhumala lapho ivezwe emanzini ukuze yakhe umgoqo wejeli ukulawula ukukhululwa kwezidakamizwa, okuvame ukusetshenziswa i-methyl cellulose, i-carboxymethyl cellulose, i-hydroxypropyl cellulose, i-povidone, i-carbomer, i-alginic acid Usawoti, i-chitosan, njll.
② Impahla yohlaka lwamathambo angancibiliki: Impahla yohlaka lwamathambo engancibiliki isho ipholymeri yemolekyuli ephezulu engancibiliki emanzini noma enokuncibilika okuncane kwamanzi.Okuvame ukusetshenziswa kakhulu i-ethyl cellulose, i-polyethylene, i-polyethylene enobuthi emihlanu, i-polymethacrylic acid, i-ethylene-vinyl acetate copolymer, irabha ye-silicone, njll.
③ Izinto zohlaka lwe-Bioerodible: Izinto zohlaka olusetshenziswayo ezivame ukusetshenziswa kakhulu zihlanganisa amafutha ezilwane, amafutha emifino enziwe nge-hydrogenated, ingcina yezinyosi, utshwala be-stearyl, i-carnauba wax, i-glyceryl monostearate, njll. Ingabambezela ukuhlakazwa nokukhulula inqubo yezidakamizwa ezincibilika emanzini.
(2) Isilungisi sokukhulula esinamekwe
① Izinto ze-polymer ezingancibiliki: izinto ezivamile zamathambo ezingancibiliki njenge-EC.
②Izinto ze-polymer ze-Enteric: izinto ezijwayelekile ze-polymer ze-enteric ikakhulukazi zihlanganisa i-acrylic resin, uhlobo lwe-L kanye nohlobo lwe-S, i-hydroxypropylmethylcellulose acetate succinate (HPMCAS), i-cellulose acetate phthalate (CAP ), i-hydroxypropylmethylcellulose phthalate (HPMCP), njll. Isebenzisa izici ze-dissolated ngenhla kwezinto kujusi yamathumbu, futhi incibilika ezingxenyeni ezithile ukuze idlale indima.
6. Ezinye izesekeli
Ngokungeziwe kubasizi abangenhla abavame ukusetshenziswa, ezinye izinto ezisizayo ngezinye izikhathi ziyengezwa ukuze kuhlangatshezwane kangcono nezidingo zokulawulwa kwezidakamizwa, kuthuthukiswe ukuqashelwa kwezidakamizwa noma kuthuthukiswe ukuthobelana.Isibonelo, ama-agent afaka imibala, ama-flavoring kanye nama-sweeteners.
①Umenzeli wombala: Injongo eyinhloko yokwengeza lesi sici ukuthuthukisa ukubukeka kwethebhulethi nokwenza kube lula ukuyibona nokuhlukanisa.Imibala esetshenziswa ngokuvamile kufanele ihlangabezane nokucaciswa kwemithi, futhi inani elengeziwe akufanele lidlule u-0.05%.
②Ama-aromatics nama-sweeteners: Inhloso enkulu yama-aromatics nama-sweeteners ukuthuthukisa ukunambitheka kwemithi, njengamaphilisi ahlafunwayo namaphilisi ahlakazeka ngomlomo.Amakha asetshenziswa ngokujwayelekile ikakhulukazi ahlanganisa izingqikithi, amafutha ahlukahlukene anamakha, njll.;Ama-sweeteners asetshenziswa kakhulu afaka i-sucrose, i-aspartame, njll.