Disebediswa tse thusang meriana ke disebediswa tse thusang tlhahisong ya meriana le ho etsa dihlahiswa tse ngotsweng, mme ke karolo ya bohlokwa ya ditokisetso tsa meriana. Jwalo ka thepa ya tlhaho e tswang ho polymer, cellulose ether e na le dibopeho tsa ho bola ha dibopeho, ho se be le chefo, le theko e tlase, jwalo ka sodium carboxymethyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl cellulose,Li-ether tsa selulosetse kang hydroxyethyl cellulose le ethyl cellulose li na le bohlokoa ba ts'ebeliso ho metsoako ea meriana. Hona joale, lihlahisoa tsa likhoebo tse ngata tsa lapeng tsa cellulose ether li sebelisoa haholo masimong a mahareng le a tlase a indasteri, 'me boleng bo eketsehileng ha bo holimo. Indasteri e hloka ka potlako ho fetola le ho ntlafatsa le ho ntlafatsa lits'ebetso tsa lihlahisoa tsa maemo a holimo.
Di-excipients tsa meriana di bapala karolo ya bohlokwa ntshetsopeleng le tlhahisong ya di-formulations. Mohlala, ditokisetsong tse lokollwang ka nako e telele, thepa ya polymer jwalo ka di-ether tsa cellulose di sebediswa e le di-excipients tsa meriana di-pellets tse lokollwang ka nako e telele, di-formulations tse fapaneng tsa matrix tse lokollwang ka nako e telele, di-formulations tse kwahetsweng tse lokollwang ka nako e telele, di-capsules tse lokollwang ka nako e telele, difilimi tsa meriana tse lokollwang ka nako e telele, le dithethefatsi tsa resin tse lokollwang ka nako e telele. Ditokisetso le ditokisetso tsa metsi tse lokollwang ka nako e telele di sebedisitswe haholo. Tsamaisong ena, di-polymer tse kang di-ether tsa cellulose hangata di sebediswa e le dijari tsa meriana ho laola sekgahla sa ho lokollwa ha dithethefatsi mmeleng wa motho, ke hore, di hlokahala hore di lokollwe butle mmeleng ka sekgahla se behilweng ka nako e itseng ho fihlella morero wa kalafo e sebetsang.
Ho ea ka lipalo-palo tsa Lefapha la Boeletsi le Lipatlisiso, ho na le mefuta e ka bang 500 ea metsoako e 'marakeng naheng ea heso, empa ha e bapisoa le United States (mefuta e fetang 1500) le European Union (mefuta e fetang 3000), ho na le phapang e kholo, 'me mefuta e ntse e le menyenyane. metsoako ea meriana ea naha ea heso Bokhoni ba nts'etsopele ea 'maraka bo boholo. Hoa utloisisoa hore metsoako e leshome e ka sehloohong ea meriana sekala sa 'maraka oa naha ea heso ke li-capsules tsa gelatin tsa meriana, sucrose, starch, phofo ea ho koahela filimi, 1,2-propylene glycol, PVP, hydroxypropyl methylcellulose (HPMC), le likhoele tsa microcrystalline. Vegetarian, HPC, lactose.
"Ether ea cellulose ea tlhaho ke lentsoe le akaretsang bakeng sa letoto la lintho tse hlahisoang ke cellulose tse hlahisoang ke karabelo ea alkali cellulose le moemeli oa etherifying tlas'a maemo a itseng, 'me ke sehlahisoa seo lihlopha tsa hydroxyl tse holim'a macromolecule ea cellulose li nkeloang sebaka ka karolo kapa ka botlalo ke lihlopha tsa ether. Li-ether tsa cellulose li sebelisoa haholo masimong a peterole, thepa ea kaho, liphahlo, lijo, meriana le lik'hemik'hale tsa letsatsi le letsatsi. Masimong 'ohle, lihlahisoa tsa maemo a meriana li libakeng tse bohareng le tse phahameng tsa indasteri 'me li na le boleng bo phahameng bo eketsehileng. Ka lebaka la litlhoko tse thata tsa boleng, tlhahiso ea li-ether tsa cellulose tsa maemo a meriana le eona e thata haholo. Ho ka boleloa hore boleng ba lihlahisoa tsa maemo a meriana bo ka emela matla a tekheniki a likhoebo tsa ether tsa cellulose. Ether ea cellulose hangata e eketsoa e le retarder, thepa ea matrix le thickener ho etsa matlapa a matrix a lokolloang ka mokhoa o tsitsitseng, thepa ea ho roala e qhibilihang ka mpeng, thepa ea ho paka ea microcapsule e lokolloang ka mokhoa o tsitsitseng, thepa ea filimi ea lithethefatsi e lokolloang ka mokhoa o tsitsitseng, jj.
Sodium carboxymethyl cellulose (CMC-Na) ke ether ea cellulose e nang le tlhahiso le tšebeliso e kholo ka ho fetisisa lapeng le kantle ho naha. Ke ether ea ionic cellulose e entsoeng ka k'hothone le patsi ka alkalization le etherification ka chloroacetic acid. CMC-Na ke sesebelisoa sa meriana se sebelisoang haholo. Hangata e sebelisoa e le binder bakeng sa litokisetso tse tiileng le e le moemeli oa ho teteana, ho teteana le ho emisa bakeng sa litokisetso tsa metsi. E ka boela ea sebelisoa e le matrix e qhibilihang ka metsing le thepa e etsang filimi. Hangata e sebelisoa e le thepa ea filimi ea lithethefatsi e lokollang ka nako e telele le letlapa la matrix e lokollang ka nako e telele mefuteng ea tokollo e tsoelang pele (e laoloang).
Ntle le sodium carboxymethyl cellulose e le metsoako ea meriana, croscarmellose sodium e ka boela ea sebelisoa e le metsoako ea meriana. Sodium ea carboxymethyl cellulose e kopantsoeng ka tsela e fapaneng (CCMC-Na) ke ntho e sa qhibiliheng metsing eo carboxymethyl cellulose e arabelang le moemeli oa ho hokahanya mochesong o itseng (40-80°C) tlas'a ts'ebetso ea catalyst ea inorganic acid 'me ea hloekisoa. Moemeli oa ho hokahanya e ka ba propylene glycol, succinic anhydride, maleic anhydride, adipic anhydride, le tse ling tse joalo. Sodium ea Croscarmellose e sebelisoa e le motsoako oa matlapa, li-capsule le li-granules litokisetsong tsa molomo. E itšetlehile ka liphello tsa capillary le ho ruruha ho fihlela ho qhibiliha. E na le ho hatelloa ho hotle le ho qhibiliha ho matla. Lithuto li bontšitse hore tekanyo ea ho ruruha ha sodium ea croscarmellose metsing e kholo ho feta ea li-disintegrants tse tloaelehileng tse kang sodium carboxymethyl cellulose e nkeloang sebaka ke e tlase le cellulose ea microcrystalline e nang le hydrated.
Methyl cellulose (MC) ke monoether ea cellulose e seng ionic e entsoeng ka k'hothone le patsi ka alkalization le methyl chloride etherification. Methyl cellulose e na le ho qhibiliha ho hoholo ha metsi 'me e tsitsitse ho pH ea 2.0 ho isa ho 13.0. E sebelisoa haholo ho metsoako ea meriana, 'me e sebelisoa matlapeng a sublingual, ente ea intramuscular, litokisetso tsa mahlo, li-capsule tsa molomo, li-suspension tsa molomo, matlapa a molomo le litokisetso tsa letlalo. Ho phaella moo, mefuteng ea ho lokolloa ho tsoelang pele, MC e ka sebelisoa e le mokhoa oa hydrophilic gel matrix o lokolloang ho tsitsitseng, thepa ea ho roala e qhibilihang ka mpeng, thepa ea ho paka ea microcapsule e lokolloang ho tsitsitseng, thepa ea filimi ea lithethefatsi e lokolloang ho tsitsitseng, jj.
Hydroxypropyl methylcellulose (HPMC) ke ether e tsoakiloeng ea cellulose e seng ionic e entsoeng ka k'hothone le patsi ka alkalization le etherification ea propylene oxide le methyl chloride. Ha e na monko, ha e na tatso, ha e na chefo, e qhibiliha ka metsing a batang, 'me e na le li-gel ka metsing a chesang. Hydroxypropyl methylcellulose ke mofuta oa ether e tsoakiloeng ea cellulose o ntseng o eketseha ka potlako tlhahisong, tšebelisong le boleng lilemong tse 15 tse fetileng. Hape ke e 'ngoe ea metsoako e meholo ka ho fetisisa ea meriana e sebelisoang lapeng le kantle ho naha. E sebelisitsoe e le motsoako oa meriana ka lilemo tse ka bang 50. Lilemo tsa nalane. Hona joale, ts'ebeliso ea HPMC e bonahala haholo-holo likarolong tse hlano tse latelang:
E 'ngoe ke e le sehokelo le ho qhalana. HPMC e le sehokelo e ka etsa hore moriana o nolofale ho kolobisoa habonolo, 'me e ka atoloha ka makhetlo a makholo ka mor'a ho monya metsi, kahoo e ka ntlafatsa haholo ho qhibiliha kapa ho lokolloa ha letlapa. HPMC e na le viscosity e matla, 'me e ka ntlafatsa viscosity ea likaroloana le ho ntlafatsa ho hatelloa ha thepa e tala ka sebopeho se thata kapa se thata. HPMC e nang le viscosity e tlase e ka sebelisoa e le sehokelo le ho qhalana, 'me HPMC e nang le viscosity e phahameng e ka sebelisoa feela e le sehokelo.
Ea bobeli, e sebelisoa e le thepa ea tokollo e tsitsitseng le e laoloang bakeng sa litokisetso tsa molomo. HPMC ke thepa ea hydrogel matrix e sebelisoang haholo litokisetsong tsa tokollo e tsitsitseng. HPMC ea boemo bo tlase ba viscosity (5～50mPa·s) e ka sebelisoa e le binder, moemeli ea eketsang viscosity le moemeli ea emisang, 'me HPMC ea boemo bo phahameng ba viscosity (4000～100000mPa·s) e ka sebelisoa ho lokisa matlapa a tsoakiloeng a matrix a tokollo e tsitsitseng le Blocker ea tokollo e tsitsitseng bakeng sa li-capsule le matlapa a hydrophilic gel matrix a tokollo e tsitsitseng. HPMC e qhibiliha ka har'a mokelikeli oa mala, e na le melemo ea ho hatelloa hantle, ho phalla hantle, bokhoni bo matla ba ho jara lithethefatsi le litšobotsi tsa tokollo ea lithethefatsi tse sa angoeng ke pH. Ke thepa ea bohlokoa haholo ea hydrophilic carrier litsamaisong tsa ho lokisa tokollo e tsitsitseng 'me hangata e sebelisoa e le hydrophilic gel matrix le thepa ea ho roala ea litokisetso tsa tokollo e tsitsitseng, 'me e sebelisoa litokisetsong tse phaphametseng tsa mpa le lisebelisoa tse thusang tsa membrane ea lithethefatsi tse lokolloang e tsitsitseng.
Ea boraro ke e le moemeli oa ho etsa filimi ea ho koahela.HPMCE na le thepa e ntle ea ho etsa filimi. Filimi e entsoeng ke eona e ts'oana, e bonaletsang, 'me e thata, 'me ha ho bonolo ho e khomarela nakong ea tlhahiso. Haholo-holo bakeng sa meriana e bonolo ho monya mongobo 'me e sa tsitsa, ho e sebelisa e le lera la ho itšehla thajana ho ka ntlafatsa haholo botsitso ba moriana le ho thibela Filimi e fetola 'mala. HPMC e na le mefuta e fapaneng ea litlhaloso tsa viscosity. Haeba e khethiloe hantle, boleng le ponahalo ea matlapa a koahetsoeng li betere ho feta lisebelisoa tse ling, 'me mahloriso a eona a tloaelehileng ke 2% ho isa ho 10%.
Four e sebelisoa e le thepa ea capsule. Lilemong tsa morao tjena, ka ho qhoma khafetsa ha mafu a seoa a liphoofolo lefatšeng ka bophara, ha ho bapisoa le capsule tsa gelatin, capsule tsa limela li fetohile tse ratoang haholo ke indasteri ea meriana le lijo. Pfizer e atlehile ho ntša HPMC limela tsa tlhaho le ho lokisa capsule tsa meroho tsa VcapTM. Ha li bapisoa le capsule tsa setso tsa gelatin tse se nang letho, capsule tsa meroho li na le melemo ea ho ikamahanya le maemo ka bophara, ha ho kotsi ea karabelo ea ho kopanya, le botsitso bo phahameng. Sekhahla sa ho lokolloa ha meriana se tsitsitse, 'me liphapang tsa motho ka mong li nyane. Kamora ho qhalana 'meleng oa motho, ha e monyehe 'me e ka ntšoa. E ntšoa 'meleng. Mabapi le maemo a polokelo, kamora liteko tse ngata, e batla e sa robehe tlas'a maemo a mongobo o tlase, 'me thepa ea khetla ea capsule e ntse e tsitsitse tlas'a mongobo o phahameng, 'me li-index tse fapaneng tsa capsule tsa limela tlas'a maemo a feteletseng a polokelo ha li amehe. Ka kutloisiso ea batho ea capsule tsa limela le phetoho ea likhopolo tsa bongaka ba sechaba lapeng le kantle ho naha, tlhoko ea 'maraka ea capsules ea limela e tla hola ka potlako.
Ea bohlano ke e le moemeli oa ho emisa. Tokisetso ea mokelikeli oa mofuta oa ho emisa ke mokhoa o sebelisoang haholo oa bongaka, e leng sistimi ea ho hasanya e sa tšoaneng moo meriana e tiileng e qhibilihang habonolo e hasanngoang ka har'a mokhoa oa ho hasanya mokelikeli. Botsitso ba sistimi bo khetholla boleng ba litokisetso tsa mokelikeli oa ho emisa. Tharollo ea HPMC colloidal e ka fokotsa tsitsipano ea interfacial e tiileng, ea fokotsa matla a se nang bokaholimo ba likaroloana tse tiileng, le ho tsitsisa sistimi ea ho hasanya e sa tšoaneng. Ke moemeli ea babatsehang oa ho emisa. HPMC e sebelisoa e le setenya bakeng sa marotholi a mahlo, a nang le litaba tsa 0.45% ho isa ho 1.0%.
Hydroxypropyl cellulose (HPC) ke monoether ea cellulose e seng ionic e entsoeng ka k'hothone le patsi ka alkalization le propylene oxide etherification. HPC hangata e qhibiliha ka metsing a ka tlase ho 40°C le bongata bo boholo ba li-solvents tsa polar, 'me ts'ebetso ea eona e amana le litaba tsa hydroxypropyl le tekanyo ea polymerization. HPC e ka lumellana le meriana e fapaneng 'me e na le ho se sebetse hantle.
Hydroxypropyl cellulose e nketsoeng sebaka ke e tlase(L-HPC)e sebelisoa haholo-holo e le letlapa le qhalanang le le kopanyang. Litšobotsi tsa lona ke: ho bonolo ho le tobetsa le ho le bopa, ho sebetsa ka matla, ho thata haholo ho le bopa, matlapa a polasetiki le a robehang habonolo, ho eketsa L -HPC e ka ntlafatsa ho thatafala ha letlapa le khanya ea ponahalo, 'me e ka boela ea etsa hore letlapa le qhalane kapele, ea ntlafatsa boleng ba ka hare ba letlapa, le ho ntlafatsa phello ea phekolo.
Hydroxypropyl cellulose (H-HPC) e nketsoeng sebaka haholo e ka sebelisoa e le moemeli oa ho tlama bakeng sa matlapa, li-granule le li-granule tse ntle lefapheng la meriana. H-HPC e na le thepa e ntle ea ho etsa filimi, 'me filimi e hlahisoang e thata ebile e tenyetseha, e ka bapisoang le li-plasticizer. Ka ho kopanya le li-agent tse ling tsa ho roala tse thibelang metsi, ts'ebetso ea filimi e ka ntlafatsoa le ho feta, 'me hangata e sebelisoa e le thepa ea ho roala filimi bakeng sa matlapa. H-HPC e ka boela ea sebelisoa e le thepa ea matrix ho lokisa matlapa a lokollang matrix ka nako e telele, li-pellet tse lokollang ka nako e telele le matlapa a lokollang ka nako e habeli.
Hydroxyethyl cellulose (HEC) ke monoether ea cellulose e seng ionic e entsoeng ka k'hothone le patsi ka alkalization le etherification ea ethylene oxide. HEC e sebelisoa haholo-holo e le thickener, colloidal protective agent, adhesive, dispersant, stabilizer, suspending agent, agent e etsang filimi le thepa e lokollang butle lefapheng la bongaka. E ka sebelisoa ho emulsions, mafura le marotholi a mahlo bakeng sa meriana ea letlalo. Mokelikeli o nooang, matlapa a tiileng, li-capsules le mefuta e meng ea tekanyo. Hydroxyethyl cellulose e kenyelelitsoe ho US Pharmacopoeia/US National Formulary le European Pharmacopoeia.
Ethyl cellulose (EC) ke e 'ngoe ea lintho tse sebelisoang haholo tse sa qhibiliheng ka metsing tse sebelisoang haholo. EC ha e na chefo, e tsitsitse, ha e qhibilihe ka metsing, litharollong tsa asiti kapa alkaline, 'me e qhibiliha ka har'a li-solvent tsa tlhaho tse kang ethanol le methanol. Solvent e sebelisoang hangata ke solvent e tsoakiloeng ea toluene/ethanol 4/1 (boima). EC e na le ts'ebeliso e mengata litokisetsong tsa ho lokolla lithethefatsi ka nako e telele, 'me e sebelisoa haholo e le carrier le microcapsules, thepa ea ho koahela filimi, jj. ea litokisetso tsa ho lokolla tse tsoelang pele, joalo ka li-tablet retarders, likhomaretsi, thepa ea ho koahela filimi, jj. E sebelisoa e le filimi ea thepa ea matrix ho lokisa mefuta e fapaneng ea matlapa a lokolloang ka nako e telele, e le thepa e tsoakiloeng ho lokisa litokisetso tsa ho lokolla tse koahetsoeng ka nako e telele le li-pellets tse lokolloang ka nako e telele, e le thepa e thusang ea ho koahela ho lokisa li-microcapsule tse lokolloang ka nako e telele; e ka boela ea sebelisoa haholo e le thepa ea ho jara. E sebelisoa ho lokisa li-dispersion tse tiileng; e ka sebelisoa haholo theknolojing ea meriana e le ntho e etsang filimi le sekoahelo se sireletsang, 'me e ka boela ea sebelisoa e le binder le filler. Jwalo ka lesela le sireletsang matlapa, e ka fokotsa kutlwisiso ya matlapa mongobong mme ya thibela meriana ho fetoha mmala le ho senyeha ke mongobo; e ka boela ya etsa lera la sekhomaretsi le lokollang butle mme ya kenya polymer ka microcapsulate ho lokolla phello ya moriana ka ho tswela pele.
Ka bokhutšoanyane, sodium carboxymethyl cellulose e qhibilihang ka metsing, methyl cellulose, hydroxypropyl methyl cellulose, hydroxpropyl cellulose, hydroxyethyl cellulose le ethyl cellulose e qhibilihang ka oli kaofela li ipapisitse le litšobotsi tsa tsona. Litšobotsi tsa sehlahisoa li sebelisoa linthong tse thusang meriana e le likhomaretsi, li-disintegrants, thepa ea ho lokolla e tsitsitseng le e laoloang bakeng sa litokisetso tsa molomo, li-agent tse etsang filimi, thepa ea capsule le li-agent tse emisang. Ha re sheba lefats'e, lik'hamphani tse 'maloa tsa machaba tsa linaha tse ling (Shin-Etsu Japane, Dow Wolff le Ashland) li hlokometse' maraka o moholo oa cellulose ea meriana Chaena nakong e tlang, 'me e ka eketsa tlhahiso kapa ho kopanngoa, li ekelitse boteng ba tsona tšimong ena. Matsete ka har'a kopo. Dow Wolff e phatlalalitse hore e tla eketsa tlhokomelo ea eona ho sebopeho, metsoako le litlhoko tsa' maraka oa ho lokisa meriana oa Chaena, 'me lipatlisiso tsa eona tsa ts'ebeliso le tsona li tla loanela ho atamela' maraka. Karolo ea Wolff Cellulose ea Dow Chemical le Colorcon Corporation ea United States e thehile selekane sa ho lokisa tokollo se tsitsitseng le se laoloang lefatšeng ka bophara. E na le basebetsi ba fetang 1,200 metseng e 9, litsi tse 15 tsa thepa le lik'hamphani tse 6 tsa GMP. Litsebi tsa lipatlisiso tse sebelisitsoeng li fana ka litšebeletso ho bareki linaheng tse ka bang 160. Ashland e na le metheo ea tlhahiso Beijing, Tianjin, Shanghai, Nanjing, Changzhou, Kunshan le Jiangmen, 'me e tsetetse litsing tse tharo tsa lipatlisiso tsa theknoloji Shanghai le Nanjing.
Ho ya ka dipalopalo tse tswang webosaeteng ya Mokgatlo wa China Cellulose, ka 2017, tlhahiso ya lehae ya cellulose ether e ne e le ditone tse 373,000 mme bophahamo ba thekiso e ne e le ditone tse dikete tse 360. Ka 2017, bophahamo ba nnete ba thekiso ya ionicCMCe ne e le lithane tse 234,000, e leng keketseho ea 18.61% selemo le selemo, 'me bophahamo ba thekiso ea CMC e seng ea ionic e ne e le lithane tse 126,000, e leng keketseho ea 8.2% selemo le selemo. Ntle le lihlahisoa tse seng tsa ionic tsa HPMC (sehlopha sa thepa ea kaho),HPMC(sehlopha sa meriana), HPMC (sehlopha sa lijo), HEC, HPC, MC, HEMC, jj. kaofela li phahame khahlanong le mokhoa ona, 'me tlhahiso le thekiso li ntse li eketseha. Li-ether tsa cellulose tsa malapeng li ntse li hola ka potlako ka lilemo tse fetang leshome, 'me tlhahiso e se e le ea pele lefatšeng. Leha ho le joalo, boholo ba lihlahisoa tsa lik'hamphani tsa ether tsa cellulose li sebelisoa haholo-holo bohareng le bo tlase ba indasteri, 'me boleng bo eketsehileng ha bo holimo.
Hona jwale, boholo ba dikgwebo tsa lehae tsa cellulose ether di nakong ya bohlokwa ya phetoho le ntlafatso. Di lokela ho tswela pele ho eketsa dipatlisiso tsa dihlahiswa le maiteko a ntshetsopele, ho ntlafatsa mefuta ya dihlahiswa ka ho tswela pele, ho sebedisa China ka botlalo, e leng mmaraka o moholo ka ho fetisisa lefatsheng, le ho eketsa maiteko a ho ntshetsa pele dimmaraka tsa kantle ho naha e le hore dikgwebo di kgone ho hola kapele kamoo ho ka kgonehang. Phetha phetoho le ntlafatso, kena bohareng ho isa ho bo hodimo ba indasteri, mme o fihlelle ntshetsopele e ntle le e tala.
Nako ea poso: Mmesa-25-2024