Li-excipients tsa meriana ke li-excipients le li-adjuvant tse sebelisoang tlhahiso ea meriana le ho etsa litaelo, 'me ke karolo ea bohlokoa ea litokisetso tsa meriana. Joalo ka thepa ea tlhaho e nkiloeng ke polymer, cellulose ether e na le litšobotsi tsa biodegradability, non-toxicity, le theko e tlase, joalo ka sodium carboxymethyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl cellulose,Li-cellulose ethersjoalo ka hydroxyethyl cellulose le ethyl cellulose li na le boleng ba ts'ebeliso ea bohlokoa ho li-excipients tsa meriana. Hona joale, lihlahisoa tsa lik'hamphani tse ngata tsa malapeng tsa cellulose ether li sebelisoa haholo-holo libakeng tse bohareng le tse tlaase tsa indasteri, 'me boleng bo eketsehileng ha bo phahame. Ka potlako indasteri e hloka ho fetola le ho ntlafatsa le ho ntlafatsa lisebelisoa tsa boleng bo holimo tsa lihlahisoa.
Li-excipients tsa meriana li phetha karolo ea bohlokoa ho nts'etsopele le tlhahiso ea metsoako. Ka mohlala, litokisetsong tse sa khaotseng tsa tokollo, lisebelisoa tsa polymer tse kang cellulose ethers li sebelisoa e le li-excipients tsa meriana ho li-pellets tse tsoelang pele, lihlahisoa tse sa tšoaneng tsa matrix, li-coated-release formulations, li-capsules tse lokolloang ka nako e telele, lifilimi tsa lithethefatsi tse tsitsitseng, le lithethefatsi tse tsitsitseng. Litokisetso le litokiso tsa tokollo ea nako e telele ea mokelikeli li sebelisitsoe haholo. Tsamaisong ena, li-polymers tse kang cellulose ethers hangata li sebelisoa e le bajari ba lithethefatsi ho laola sekhahla sa ho lokolloa ha lithethefatsi 'meleng oa motho, ke hore, ho hlokahala hore butle-butle ba lokolloe' meleng ka tekanyo e behiloeng ka nako e itseng ho finyella morero oa phekolo e sebetsang.
Ho ea ka lipalo-palo tsa Lefapha la Consulting le Research, ho na le mefuta e ka bang 500 ea li-excipients '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 nyenyane. lihlahisoa tsa naha ea heso Melemo ea nts'etsopele ea 'maraka e kholo. Ho utloisisoa hore li-excipients tse leshome tse holimo tsa meriana 'marakeng oa naha ea heso ke li-capsules tsa gelatin tsa meriana, sucrose, starch, phofo ea ho roala filimi, 1,2-propylene glycol, PVP, hydroxypropyl methylcellulose (HPMC), le li-microcrystalline fibers. Vegetarian, HPC, lactose.
"Natural cellulose ether ke lentsoe le akaretsang bakeng sa letoto la li-derivatives tsa cellulose tse hlahisoang ke karabelo ea alkali cellulose le etherifying agent tlasa maemo a itseng, 'me ke sehlahisoa seo lihlopha tsa hydroxyl ho cellulose macromolecule li nkeloang sebaka ke lihlopha tsa ether. masimong, lihlahisoa tsa sehlopha sa meriana ha e le hantle li bohareng le libaka tse phahameng tsa indasteri 'me li na le boleng bo phahameng bo ekelitsoeng ka lebaka la litlhoko tse tiileng tsa boleng, tlhahiso ea li-cellulose ethers tsa sehlopha sa meriana le tsona li thata haholo matlapa a matrix a sa khaotseng, lisebelisoa tsa ho roala ka gastric-solluble, lisebelisoa tsa ho paka tsa microcapsule tse sa khaotseng, lisebelisoa tsa lifilimi tse lokolotsoeng ka nako e telele, jj.
Sodium carboxymethyl cellulose (CMC-Na) ke ether ea cellulose e nang le tlhahiso e kholo ka ho fetisisa le tšebeliso ea lapeng le kantle ho naha. Ke ionic cellulose ether e entsoeng ka k'hothone le patsi ka alkalization le etherification ka chloroacetic acid. CMC-Na ke motsoako o sebelisoang hangata oa meriana. Hangata e sebelisoa e le setlamo bakeng sa litokisetso tse tiileng le e le ntho e teteaneng, e teteaneng le e emisang bakeng sa litokisetso tsa mokelikeli. E ka boela ea sebelisoa e le matrix a qhibilihang ka metsi le thepa ea ho etsa filimi. Hangata e sebelisoa e le thepa ea filimi ea lithethefatsi e sa khaotseng le letlapa la matrix le tsitsitseng ka mokhoa o tsitsitseng (o laoloang) oa tokollo.
Ntle le sodium carboxymethyl cellulose e le li-excipients tsa meriana, croscarmellose sodium e ka boela ea sebelisoa e le li-excipients tsa meriana. Cross-linked carboxymethyl cellulose sodium (CCMC-Na) ke ntho e ke keng ea qhibiliha ka metsing eo carboxymethyl cellulose e sebetsanang le motsoako o kopanyang mocheso o itseng (40-80 ° C) tlas'a ts'ebetso ea "inorganic acid catalyst" 'me ea hloekisoa. Moemeli oa crosslinking e ka ba propylene glycol, succinic anhydride, maleic anhydride, adipic anhydride, joalo-joalo. Croscarmellose sodium e sebelisoa e le disintegrant bakeng sa matlapa, li-capsules le granules litokisetsong tsa molomo. E itšetlehile ka liphello tsa capillary le ho ruruha ho finyella ho arohana. E na le compressibility e ntle le ho arohana ho matla. Liphuputso li bontšitse hore tekanyo ea ho ruruha ha sodium ea croscarmellose ka metsing e kholo ho feta ea li-disintegrants tse tloaelehileng tse kang sodium carboxymethyl cellulose le hydrated microcrystalline cellulose.
Methyl cellulose (MC) ke monoether e seng ionic cellulose e entsoeng ka k'hothone le patsi ka alkalization le methyl chloride etherification. Methyl cellulose e na le ho qhibiliha ha metsi ka tsela e babatsehang 'me e tsitsitse ho pH ea 2.0 ho ea ho 13.0. E sebelisoa haholo ho li-excipients tsa meriana, 'me e sebelisoa ka matlapa a sublingual, liente tsa intramuscular, litokisetso tsa ophthalmic, li-capsules tsa molomo, li-suspension tsa molomo, matlapa a molomo le litokisetso tsa lihlooho. Holim'a moo, mefuteng e sa khaotseng ea tokollo, MC e ka sebelisoa e le sebopeho sa hydrophilic gel matrix-release-release, gastric-soluble coating material, thepa ea packaging ea microcapsule e tsitsitseng, thepa ea filimi ea lithethefatsi e tsitsitseng, joalo-joalo.
Hydroxypropyl methylcellulose (HPMC) ke selulose e se nang ionic e tsoakiloeng ka k'hothone le patsi ka alkalization le etherification ea propylene oxide le methyl chloride. Ha e na monko, ha e latsoehe, ha e chefo, e qhibiliha metsing a batang, le li-gel metsing a chesang. Hydroxypropyl methylcellulose ke mofuta oa cellulose o tsoakiloeng oa ether o ntseng o eketseha ka potlako tlhahiso, tšebeliso le boleng lilemong tse 15 tse fetileng. Hape ke e 'ngoe ea li-excipient tse kholo ka ho fetisisa tsa meriana tse sebelisoang lapeng le linaheng tse ling. E 'nile ea sebelisoa e le motsoako oa meriana ka lilemo tse ka bang 50. Lilemo tsa histori. Hajoale, ts'ebeliso ea HPMC e bonts'oa haholo likarolo tse hlano tse latelang:
E 'ngoe e tšoana le se tlamang le ho arohana. HPMC e le binder e ka etsa hore sethethefatsi se be bonolo ho koloba, 'me se ka atolosa 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 mokhoa o hlakileng kapa o thata. HPMC e nang le viscosity e tlase e ka sebelisoa e le setlamo le disintegrant, 'me HPMC e nang le viscosity e phahameng e ka sebelisoa feela e le setlamo.
Taba ea bobeli, e sebelisoa e le sesebelisoa sa tokollo se tsitsitseng le se laoloang bakeng sa litokisetso tsa molomo. HPMC ke sesebelisoa sa hydrogel matrix se sebelisoang hangata litokisetsong tsa tokollo e tsitsitseng. HPMC ea boemo bo tlase ba viscosity (5～50mPa·s) e ka sebelisoa e le se tlamang, se eketsang viscosity le moemeli ea emisang, le HPMC ea sehlopha se phahameng sa viscosity (4000 ~ 100000mPa·s) e ka sebelisoa ho lokisa lisebelisoa tse tsoakiloeng tsa matrix bakeng sa matlapa a tokollo ea hydrophilic le matlapa a tsitsitseng a hydrophilic. matlapa a lokolloang ka nako e telele. HPMC e qhibiliha ka har'a mokelikeli oa ka mpeng, e na le melemo ea ho hatelloa hantle, metsi a matle, bokhoni bo matla ba ho jara lithethefatsi le litšobotsi tsa tokollo ea lithethefatsi tse sa angoeng ke pH. Ke ntho ea bohlokoa ka ho fetesisa e tsamaisang hydrophilic lits'ebetsong tsa ho lokisoa ha nako e telele, 'me hangata e sebelisoa e le The hydrophilic gel matrix le thepa ea ho roala ea litokisetso tsa tokollo e tsitsitseng, mme e sebelisoa litokisetsong tse phaphametseng ka mpeng le lisebelisoa tse thusang tsa membrane ea lithethefatsi.
Ea boraro ke e le moemeli oa ho roala filimi.HPMCe na le litšobotsi tse ntle tsa ho etsa lifilimi. Filimi e entsoeng ke eona e tšoana, e pepenene ebile e thata, 'me ha ho bonolo ho khomarela nakong ea tlhahiso. Haholo-holo bakeng sa lithethefatsi tse bonolo ho monya mongobo le tse sa tsitsang, ho li sebelisa e le lera la ho itšehla thajana ho ka ntlafatsa haholo botsitso ba lithethefatsi le ho thibela Filimi e fetola 'mala. HPMC e na le litlhaloso tse fapaneng tsa viscosity. Haeba e khethiloe hantle, boleng le ponahalo ea matlapa a koahetsoeng a molemo ho feta lisebelisoa tse ling, 'me mahloriso a eona a tloaelehileng ke 2% ho 10%.
Tse 'nè li 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 li-capsules tsa gelatin, li-capsules tsa semela li fetohile tse ratoang haholo indastering ea meriana le ea lijo. Pfizer e atlehile ho ntša HPMC limela tsa tlhaho le ho lokisa li-capsules tsa meroho tsa VcapTM. Ha ho bapisoa le li-capsules tse tloaelehileng tsa gelatin, li-capsules tsa meroho li na le melemo ea ho ikamahanya le maemo ka bophara, ha li na kotsi ea ho itšoara ka tsela e fapaneng, le botsitso bo phahameng. Sekhahla sa ho lokolloa ha lithethefatsi se batla se tsitsitse, 'me liphapang tsa batho ka bomong li nyane. Ka mor'a ho arohana 'meleng oa motho, ha e monye 'me e ka ntšoa. E ntšitsoeng 'meleng. Mabapi le maemo a polokelo, ka mor'a liteko tse ngata, e batla e sa brittle tlas'a maemo a tlaase a mongobo, 'me thepa ea khetla ea capsule e ntse e tsitsitse tlas'a mongobo o phahameng,' me li-index tse sa tšoaneng tsa li-capsules tsa limela tlas'a maemo a feteletseng a polokelo ha li amehe. Ka kutloisiso ea batho ea li-capsules tsa semela le phetoho ea maikutlo a meriana ea sechaba lapeng le kantle ho naha, tlhoko ea 'maraka ea li-capsules tsa semela e tla hola ka potlako.
Ea bohlano e tšoana le moemeli ea emisang. Tokisetso ea mokelikeli oa mofuta oa suspension ke mofuta o sebelisoang hangata oa litekanyetso tsa bongaka, e leng mokhoa o fapaneng oa ho hasana moo lithethefatsi tse tiileng tse sa qhibiliheng li qhalakantsoeng sebakeng sa phallo ea metsi. Ho tsitsa ha tsamaiso ho etsa qeto ea boleng ba litokisetso tsa mokelikeli oa ho emisa. Tharollo ea colloidal ea HPMC e ka fokotsa tsitsipano e tiileng ea metsi a sefahleho, ea fokotsa matla a mahala a likaroloana tse tiileng, le ho tsitsisa sistimi ea phepelo e fapaneng. Ke moemeli ea khabane oa ho emisa. HPMC e sebelisoa e le motenya bakeng sa marotholi a mahlo, a nang le litaba tsa 0.45% ho isa ho 1.0%.
Hydroxypropyl cellulose (HPC) ke monoether e seng ionic cellulose e entsoeng ka k'hothone le patsi ka alkalization le propylene oxide etherification. Hangata HPC e qhibiliha ka metsing a ka tlase ho 40 ° C le palo e kholo ea li-solvents tsa polar, 'me ts'ebetso ea eona e amana le litaba tsa hydroxypropyl le tekanyo ea polymerization. HPC e ka sebelisana le lithethefatsi tse fapaneng 'me e na le inertness e ntle.
hydroxypropyl cellulose e nkeloang sebaka e tlase(L-HPC)haholo-holo e sebelisoa e le letlapa disintegrant le binder. Litšobotsi tsa eona ke: ho bonolo ho tobetsa le ho theha, ho sebetsa ka matla, haholo-holo ho thata ho theha, matlapa a polasetiki le a brittle, eketsa L -HPC e ka ntlafatsa ho thatafala ha letlapa le ho khanya ha ponahalo, hape e ka etsa hore letlapa le qhalane ka potlako, ho ntlafatsa boleng ba ka hare ba letlapa, le ho ntlafatsa phello ea phekolo.
High substituted hydroxypropyl cellulose (H-HPC) e ka sebelisoa e le ntho e tlamang matlapa, li-granules le li-granules tse ntle lefapheng la meriana. H-HPC e na le thepa e babatsehang ea ho etsa lifilimi, 'me filimi e hlahisoang e thata ebile e le elastic, e ka bapisoang le li-plasticizers. Ka ho kopanya le lisebelisoa tse ling 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 lisebelisoa tsa matrix ho lokisa matlapa a lokolloang ka nako e telele a matrix, li-pellets tse sa khaotseng le matlapa a mabeli a lokolloang ka nako e telele.
Hydroxyethyl cellulose (HEC) ke monoether e seng ionic cellulose e entsoeng ka k'hothone le patsi ka alkalization le ethylene oxide etherification. HEC e sebelisoa haholo-holo e le motenya, moemeli oa tšireletso oa colloidal, sekhomaretsi, dispersant, stabilizer, moemeli oa ho emisa, moemeli oa ho etsa lifilimi le lisebelisoa tse liehang ho lokolloa lefapheng la bongaka. E ka sebelisoa ho li-emulsion, litlolo, le marotholi a mahlo bakeng sa meriana ea lihlooho. Mokelikeli oa molomo, matlapa a tiileng, li-capsules le mefuta e meng ea litekanyetso. 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 tsoang ho selulose e sa keneng ka metsing. EC ha e na chefo, e tsitsitse, ha e qhibilihe ka har'a metsi, asiti kapa alkaline, 'me e qhibiliha ka har'a metsoako ea tlhaho e kang ethanol le methanol. Mokelikeli o sebelisoang hangata ke motsoako o motsoako oa toluene/ethanol 4/1 (boima). EC e na le lisebelisoa tse ngata tsa litokisetso tsa ho lokolloa ha lithethefatsi, 'me e sebelisoa haholo e le sejari le li-microcapsules, ho roala thepa ea ho etsa filimi, joalo-joalo ea litokisetso tse tsitsitseng, tse kang li-table retarders, li-adhesives, thepa ea ho roala filimi, joalo-joalo E sebelisoa e le filimi ea thepa ea matrix ho lokisetsa mefuta e sa tšoaneng ea matrix e tsitsitseng-e lokolloa matlapa le ho lokolla matlapa a tsitsitseng, li-pellets tse sa khaotseng, e le lisebelisoa tse thusang tsa encapsulation ho lokisetsa li-microcapsules tse sa khaotseng; e ka boela ea sebelisoa haholo e le thepa ea thepa E sebelisoa ho lokisetsa li-dispersions tse tiileng; e ka sebelisoa haholo ho thekenoloji ea meriana e le ntho ea ho etsa filimi le ho roala ho sireletsa, hape e ka sebelisoa e le se tlamang le ho tlatsa. E le tšireletso e sireletsang matlapa, e ka fokotsa kutloisiso ea matlapa ho mongobo le ho thibela lithethefatsi hore li se ke tsa senyeha le ho senyeha ke mongobo; e ka boela ea theha sekhomaretsi sa sekhomaretsi se fokolang butle le microencapsulate polymer ho tsoela pele ho lokolla phello ea lithethefatsi.
Ka kakaretso, sodium carboxymethyl cellulose e qhibilihang ka metsing, methyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose le ethyl cellulose e qhibilihang ka oli kaofela li ipapisitse le tsona. litokisetso, ho roala li-agent tse etsang filimi, lisebelisoa tsa capsule le li-suspending agents. Ha re sheba lefats'e, lik'hamphani tse 'maloa tsa linaha tse ngata tse tsoang linaheng tse ling (Shin-Etsu Japane, Dow Wolff le Ashland) li ile tsa hlokomela' maraka o moholo oa selulose ea meriana Chaena nakong e tlang, 'me e ka eketsa tlhahiso kapa ho kopanya, ba ekelitse boteng ba bona tšimong ena. Investment ka hare ho kopo. Dow Wolff o phatlalalitse hore e tla eketsa tlhokomelo ea eona ho theho, metsoako le litlhoko tsa 'maraka oa ho lokisetsa meriana oa Chaena,' me lipatlisiso tsa eona tsa kopo li tla boela li loanele ho atamela haufi le 'maraka. Wolff Cellulose Division ea Dow Chemical le Colorcon Corporation ea United States e thehile selekane se tsitsitseng le se laoloang sa tokollo lefatšeng ka bophara. E na le basebetsi ba fetang 1,200 metseng ea 9, mekhatlo ea thepa ea 15 le lik'hamphani tse 6 tsa GMP. Litsebi tsa lipatlisiso tse sebelisitsoeng li fana ka lits'ebeletso 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 ea ka lipalo-palo tse tsoang ho websaeteng ea Mokhatlo oa Chaena oa Cellulose, ka 2017, tlhahiso ea malapeng ea cellulose ether e ne e le lithane tse 373,000 'me theko ea thekiso e ne e le lithane tse likete tse 360. Ka 2017, palo ea sebele ea thekiso ea ionicCMCe ne e le lithane tse 234,000, keketseho ea 18.61% selemo le selemo, 'me theko ea thekiso ea CMC e seng ea ionic e ne e le lithane tse 126,000, keketseho ea 8,2% selemo le selemo. Ho phaella ho HPMC (mohaho oa thepa ea mohaho) lihlahisoa tse seng tsa ionic,HPMC(sehlopha sa meriana), HPMC (sehlopha sa lijo), HEC, HPC, MC, HEMC, joalo-joalo kaofela li tsohile khahlanong le mokhoa ona, 'me tlhahiso le thekiso li tsoetse pele ho eketseha. Li-ether tsa cellulose tsa malapeng li ’nile tsa hōla ka potlako ka lilemo tse fetang leshome, ’me tlhahiso e fetohile ea pele lefatšeng. Leha ho le joalo, boholo ba lihlahisoa tsa lik'hamphani tsa cellulose ether li sebelisoa haholo-holo bohareng le qetellong ea indasteri, 'me boleng bo eketsehileng ha bo phahame.
Hajoale, likhoebo tse ngata tsa lehae tsa cellulose ether li nakong e mahlonoko ea phetoho le ntlafatso. Ba lokela ho tsoela pele ho eketsa matsapa a lipatlisiso le nts'etsopele ea lihlahisoa, ba tsoele pele ho ntlafatsa mefuta ea lihlahisoa, ba sebelise ka botlalo China, 'maraka o moholo ka ho fetisisa lefatšeng, le ho eketsa matsapa a ho nts'etsapele mebaraka ea kantle ho naha hore likhoebo li tsebe ho hola kapele kamoo ho ka khonehang. Qetella phetoho le ho ntlafatsa, kena bohareng ba boemo bo phahameng ba indasteri, 'me u fihlele tsoelo-pele e ntle le e tala.
Nako ea poso: Apr-25-2024