Ka ho teba ha lipatlisiso tsa tsamaiso ea ho fana ka lithethefatsi le litlhoko tse thata, ho ntse ho hlaha li-excipients tse ncha tsa meriana, tseo har'a tsona hydroxypropyl methylcellulose e sebelisoang haholo. Pampiri ena e hlahloba ts'ebeliso ea malapeng le kantle ho naha ea hydroxypropyl methylcellulose. Mokhoa oa tlhahiso le melemo le mathata a eona, theknoloji ea thepa le menyetla ea ntlafatso ea malapeng, le ts'ebeliso ea eona lefapheng la li-excipients tsa meriana.
Mantsoe a bohlokoa: li-excipients tsa meriana; hydroxypropyl methylcellulose; tlhahiso; kopo
1 Selelekela
Li-excipients tsa meriana li bua ka lentsoe le akaretsang bakeng sa lisebelisoa tse ling tsohle tsa meriana tse kenyelletsoeng ho lokisoa ntle le moriana o ka sehloohong e le hore ho rarolloe sebopeho, ho fumaneha le ho sireletseha ha litokisetso nakong ea ho hlahisa le ho etsa moralo oa ho lokisetsa. Li-excipients tsa meriana li bohlokoa haholo litokisetsong tsa meriana. Ho na le mefuta e mengata ea li-excipients tsa meriana litokisetsong tsa malapeng le tsa linaheng tse ling, empa lilemong tsa morao tjena, litlhoko tsa bohloeki, ho qhibiliha, botsitso, bioavailability ka vivo, ntlafatso ea phello ea phekolo le phokotso ea litla-morao tsa lithethefatsi li ntse li phahama le ho feta. , ho etsa ho hlaha ka potlako ha li-excipients tse ncha le mekhoa ea lipatlisiso e le ho ntlafatsa katleho ea ho lokisetsa lithethefatsi le boleng ba tšebeliso. Palo e kholo ea mohlala oa data e bonts'a hore hydroxypropyl methylcellulose e ka fihlela litlhoko tse kaholimo e le mothusi oa boleng bo holimo oa meriana. Boemo ba hajoale ba lipatlisiso le tlhahiso ea kantle ho naha le ts'ebeliso ea eona lefapheng la litokisetso tsa meriana bo akaretsoa ka ho eketsehileng.
2 Kakaretso ea thepa ea HPMC
HPMC ke phofo e tšoeu kapa e mosehla hanyenyane, e se nang monko, e sa nkheng, e seng chefo e fumanoang ka etherification ea alkali cellulose, propylene oxide le alkyl chloride. E qhibiliha ha bonolo metsing a ka tlase ho 60°C le 70% ethanol le acetone , isoacetone, le dichloromethane motsoako oa solvent; HPMC e na le botsitso bo matla, haholo-holo bo bontšitsoeng: pele, tharollo ea eona ea metsi ha e na tefo ebile ha e sebetsane le letsoai la tšepe kapa metsoako ea ionic; ea bobeli, e boetse e hanyetsana le li-acids kapa metheo. E tsitsitseng. Ke litšobotsi tsa botsitso tsa HPMC tse etsang hore boleng ba meriana e nang le HPMC e be lisebelisoa tse tsitsitseng ho feta tse nang le lisebelisoa tsa setso. Thutong ea toxicology ea HPMC e le li-excipients, ho bontšoa hore HPMC e ke ke ea fetoloa 'meleng,' me ha e kopanele ho metabolism ea 'mele oa motho. Phepelo ea matla, ha ho na chefo le litla-morao bakeng sa lithethefatsi, li-excipients tse sireletsehileng tsa meriana.
3 Lipatlisiso mabapi le tlhahiso ea HPMC ea malapeng le kantle ho naha
3.1 Kakaretso ea theknoloji ea tlhahiso ea HPMC lapeng le kantle ho naha
E le ho sebetsana hamolemo le litlhoko tse ntseng li eketseha le tse ntseng li eketseha tsa litokisetso tsa meriana lapeng le linaheng tse ling, theknoloji ea tlhahiso le ts'ebetso ea HPMC le tsona li ntse li tsoela pele ka tsela e boima le e telele. Ts'ebetso ea tlhahiso ea HPMC e ka aroloa ka mokhoa oa batch le mokhoa o tsoelang pele. Lihlopha tse ka sehloohong. Ts'ebetso e tsoelang pele e sebelisoa ka kakaretso kantle ho naha, athe ts'ebetso ea batch e sebelisoa haholo China. Tokiso ea HPMC e kenyelletsa mehato ea ho itokisa selulose ea alkali, karabelo ea etherification, kalafo ea ho hloekisa, le kalafo e felileng ea sehlahisoa. Har'a bona, ho na le mefuta e 'meli ea litsela tsa ts'ebetso bakeng sa karabelo ea etherification. : Mokhoa oa khase ea khase le mokhoa oa mohato oa mokelikeli. Ha re bua ka mokhoa o fapaneng, mokhoa oa khase ea khase o na le melemo ea matla a maholo a tlhahiso, mocheso o tlase oa karabelo, nako e khuts'oane ea karabelo, le taolo e nepahetseng ea karabelo, empa khatello ea karabelo e kholo, matsete a maholo, mme hang ha bothata bo hlaha, ho bonolo ho e etsa. baka dikotsi tse kgolo. Mokhoa oa mokelikeli ka kakaretso o na le melemo ea khatello e tlase ea karabelo, kotsi e tlase, litšenyehelo tse tlase tsa matsete, taolo e bonolo ea boleng, le ho nkela mefuta e meng sebaka habonolo; empa ka nako e ts'oanang, reactor e hlokoang ke mokhoa oa mokelikeli e ke ke ea e-ba kholo haholo, e leng eona e fokotsang matla a ho arabela. Ha ho bapisoa le mokhoa oa khase ea khase, nako ea karabelo e telele, matla a tlhahiso a nyane, lisebelisoa tse hlokahalang li ngata, ts'ebetso e rarahane, 'me taolo ea boiketsetso le ho nepahala li tlase ho feta mokhoa oa khase ea khase. Hona joale, linaha tse tsoetseng pele tse kang Europe le United States haholo-holo li sebelisa mokhoa oa mohato oa khase. Ho na le litlhoko tse phahameng mabapi le theknoloji le matsete. Ho latela maemo a sebele naheng ea rona, ts'ebetso ea mokelikeli oa mokelikeli e tloaelehile haholo. Leha ho le joalo, ho na le libaka tse ngata Chaena tse ntseng li tsoela pele ho nchafatsa le ho nchafatsa mahlale, ho ithuta ho tsoa maemong a tsoetseng pele a kantle ho naha, le ho qala lits'ebetso tse tsoelang pele. Kapa tsela ea ho hlahisa mokhoa oa khase ea kantle ho naha.
3.2 Ntlafatso ea theknoloji ea tlhahiso ea HPMC ea lapeng
HPMC naheng ea heso e na le menyetla e meholo ea ntlafatso. Tlas'a menyetla e joalo e ntle, ke sepheo sa mofuputsi e mong le e mong ho tsoela pele ho ntlafatsa theknoloji ea tlhahiso ea HPMC le ho fokotsa lekhalo lipakeng tsa indasteri ea lehae ea HPMC le linaha tse tsoetseng pele tsa kantle ho naha. Ts'ebetso ea HPMC Khokahano e 'ngoe le e' ngoe ea ts'ebetso ea ho kopanya e bohlokoa haholo ho sehlahisoa sa ho qetela, seo ho sona alkalization le etherification reactions [6] ke tsa bohlokoa ka ho fetisisa. Ka hona, theknoloji e teng ea tlhahiso ea malapeng ea HPMC e ka etsoa ho tloha mahlakoreng ana a mabeli. Phetoho. Pele ho tsohle, ho lokisoa ha cellulose ea alkali ho lokela ho etsoa ka mocheso o tlase. Haeba sehlahisoa sa viscosity se tlase se lokiselitsoe, li-oxidants tse ling li ka eketsoa; haeba sehlahisoa se nang le viscosity e phahameng se lokiselitsoe, mokhoa oa ho sireletsa khase ea inert o ka sebelisoa. Taba ea bobeli, karabelo ea etherification e etsoa ka mocheso o phahameng. Beha toluene ka thepa ea etherification esale pele, romela selulose ea alkali ka har'a lisebelisoa ka pompo, 'me u kenye palo e itseng ea isopropanol ho latela litlhoko. Fokotsa karo-karolelano ea metsi a tiileng. 'Me u sebelise mokhoa oa ho laola k'homphieutha, o ka potlakisang mocheso oa maikutlo, Mehato ea ts'ebetso e kang khatello le pH e fetoloa ka bo eona. Ha e le hantle, ntlafatso ea theknoloji ea tlhahiso ea HPMC e ka boela ea ntlafatsoa ho tloha tseleng ea ts'ebetso, tšebeliso ea thepa e tala, phekolo ea ho hloekisa le likarolo tse ling.
4 Tšebeliso ea HPMC lefapheng la bongaka
4.1 Tšebeliso ea HPMC ho lokiseng matlapa a tsoelang pele a lokolloa
Lilemong tsa morao tjena, ka ho teba ho tsoelang pele ha lipatlisiso tsa tsamaiso ea ho fana ka lithethefatsi, nts'etsopele ea HPMC e nang le viscosity e phahameng ha ho sebelisoa litokisetso tsa tokollo e tsitsitseng e hohetse tlhokomelo e kholo, 'me phello e tsitsitseng ea tokollo e ntle. Ha ho bapisoa, ho ntse ho na le lekhalo le leholo ts'ebelisong ea matlapa a matrix a sa khaotseng. Ka mohlala, ha ho bapisoa HPMC ea malapeng le ea linaheng tse ling bakeng sa matlapa a nifedipine a lokolloa ka nako e telele 'me e le matrix bakeng sa matlapa a matrix a propranolol hydrochloride, ho fumanoa hore tšebeliso ea HPMC ea malapeng ha ho etsoa litokisetso tsa tokollo e tsitsitseng e hloka ntlafatso e tsoelang pele ho tsoela pele ho ntlafatsa. boemo ba litokisetso tsa malapeng.
4.2 Tšebeliso ea HPMC ho tiea ha mafura a bongaka
Ka lebaka la litlhoko tsa tlhahlobo kapa kalafo ea lisebelisoa tse ling tsa bongaka kajeno, ha ho kena kapa ho tsoa lithong tsa motho le lisele, bokaholimo ba sesebelisoa bo tlameha ho ba le lisebelisoa tse itseng tsa ho tlotsa, 'me HPMC e na le thepa e itseng ea ho tlotsa. Ha ho bapisoa le litlolo tse ling tsa oli, HPMC e ka sebelisoa e le lisebelisoa tsa bongaka tsa lubricating , e ke keng ea fokotsa feela ho roala ha lisebelisoa, empa hape e finyella litlhoko tsa lubrication ea bongaka le ho fokotsa litšenyehelo.
4.3 Ts'ebeliso ea HPMC joalo ka filimi ea tlhaho ea antioxidant e qhibilihang ka metsing le lisebelisoa tsa ho roala filimi le thepa ea ho etsa lifilimi.
Ha ho bapisoa le lisebelisoa tse ling tsa letlapa tse koetsoeng, HPMC e na le melemo e hlakileng mabapi le ho thatafala, friability le ho monya mongobo. HPMC ea limaraka tse fapaneng tsa viscosity e ka sebelisoa e le sephutheloana se qhibilihang ka metsing bakeng sa matlapa le lipilisi. E ka boela ea sebelisoa e le filimi ea ho paka bakeng sa litsamaiso tsa organic solvent. Ho ka boleloa hore HPMC ke sesebelisoa sa ho roala lifilimi se sebelisoang ka ho fetesisa naheng ea heso. Ho phaella moo, HPMC e ka boela ea sebelisoa e le thepa ea ho etsa lifilimi ho moemeli oa lifilimi, 'me filimi ea ho paka e thibelang metsi e qhibilihisang metsi e thehiloeng ho HPMC e sebelisoa haholo ho boloka lijo, haholo-holo litholoana.
4.4 Tšebeliso ea HPMC e le lisebelisoa tsa khetla ea capsule
HPMC e ka boela ea sebelisoa e le thepa ea ho lokisa likhetla tsa capsule. Melemo ea li-capsules tsa HPMC ke hore li hlōla phello ea li-cross-linking tsa gelatin capsules, li lumellana hantle le lithethefatsi, li na le botsitso bo phahameng, li khona ho fetola le ho laola boitšoaro ba ho lokolloa ha lithethefatsi, ho ntlafatsa boleng ba lithethefatsi, E na le melemo ea ho lokolloa ha lithethefatsi ka mokhoa o tsitsitseng. tshebetso. Ha e le hantle, li-capsules tsa HPMC li ka nka sebaka sa li-capsules tsa gelatin ka ho feletseng, tse emelang tataiso ea nakong e tlang ea li-capsules tse thata.
4.5 Kopo ea HPMC joalo ka moemeli ea emisang
HPMC e sebelisoa e le moemeli ea emisang, 'me phello ea eona ea ho emisa e ntle. 'Me liteko li bontša hore ho sebelisa lisebelisoa tse ling tse tloaelehileng tsa polymer e le moemeli oa ho emisa ho lokisetsa ho emisoa ho omileng ho bapisoa le HPMC e le moemeli ea emisang ho lokisa ho emisoa ho omileng. Ho emisoa ho omileng ho bonolo ho itokisetsa mme ho na le botsitso bo botle, 'me ho emisoa ho entsoeng ho finyella litlhoko tsa matšoao a sa tšoaneng a boleng ba ho emisoa ho omileng. Ka hona, HPMC e atisa ho sebelisoa e le moemeli oa ho emisa bakeng sa litokisetso tsa mahlo.
4.6 Ts'ebeliso ea HPMC joalo ka sethibela, moemeli oa ho lokolla butle le porogen
HPMC e ka sebelisoa e le moemeli oa thibelo, moemeli oa tokollo e tsitsitseng le moemeli oa pore ho lieha le ho laola ho lokolloa ha lithethefatsi. Matsatsing ana, HPMC e boetse e sebelisoa haholo litokisetsong tsa nako e telele tsa tokollo le metsoako ea meriana ea setso ea Machaena, joalo ka matlapa a matrix a Tianshan Snow Lotus. Kopo, phello ea eona e tsitsitseng ea ho lokolloa e ntle, 'me mokhoa oa ho lokisetsa o bonolo ebile o tsitsitse.
4.7 Tšebeliso ea HPMC e le sekhomaretsi se setenya le se sireletsang sa colloid
HPMC e ka sebelisoa e le motenya [9] ho etsa li-colloid tse sireletsang, 'me liphuputso tse amehang tsa liteko li bontšitse hore ho sebelisa HPMC joalo ka motenya ho ka matlafatsa botsitso ba khabone e entsoeng ka moriana. Ka mohlala, e atisa ho sebelisoa ha ho etsoa gel ea pH-sensitive levofloxacin hydrochloride ophthalmic e loketseng ho sebelisoa. HPMC e sebelisoa e le motenya.
4.8 Tšebeliso ea HPMC joalo ka bioadhesive
Likhomaretsi tse sebelisoang theknolojing ea bioadhesion ke metsoako ea macromolecular e nang le thepa ea bioadhesive. Ka ho khomarela mucosa ea gastrointestinal, mucosa ea molomo le likarolo tse ling, ho tsoela pele le ho tiea ha ho kopana pakeng tsa lithethefatsi le mucosa ho matlafatsoa ho finyella liphello tse molemo tsa phekolo. . Palo e kholo ea mehlala ea ts'ebeliso e bonts'a hore HPMC e ka fihlela litlhoko tse kaholimo joalo ka bioadhesive.
Ho feta moo, HPMC e ka boela ea sebelisoa e le inhibitor ea pula bakeng sa li-gels tsa li-topical le li-self-microemulsifying systems, 'me indastering ea PVC, HPMC e ka sebelisoa e le tšireletso ea ho hasana ho polymerization ea VCM.
5 Qetello
Ka mantsoe a mang, HPMC e sebelisitsoe haholo litokisetsong tsa meriana le likarolo tse ling ka lebaka la thepa ea eona e ikhethang ea physicochemical le biological. Leha ho le joalo, HPMC e ntse e na le mathata a mangata litokisetsong tsa meriana. Karolo e ikhethileng ea HPMC ke efe ts'ebetsong; mokhoa oa ho tseba hore na e na le phello ea pharmacological; e na le litšobotsi life mochineng oa eona oa ho lokolla, joalo-joalo Ho ka bonoa hore le hoja HPMC e sebelisoa haholo, mathata a mangata a hloka ho rarolloa ka potlako . 'Me bafuputsi ba bangata ba ntse ba etsa mosebetsi o mongata bakeng sa ts'ebeliso e ntle ea HPMC meriana, kahoo ba tsoela pele ho khothalletsa nts'etsopele ea HPMC lefapheng la li-excipients tsa meriana.
Nako ea poso: Nov-02-2022