Lingoliloeng tse amanang le lapeng le kantle ho naha ha ho lokisoa li-excipients tsa meriana hydroxypropyl methylcellulose (HPMC) lilemong tsa morao tjena li ile tsa hlahlojoa, tsa hlahlojoa le ho akaretsoa, 'me li sebelisoa ka litokisetso tse tiileng, litokisetso tsa metsi, litokisetso tse tsitsitseng le tse laoloang tsa tokollo, litokisetso tsa capsule, gelatin lits'ebetso lefapheng la lihlahisoa tse ncha tse kang li-adhesive formulations le li-bioadhesives. Ka lebaka la phapang ea boima ba limolek'hule le viscosity ea HPMC, e na le litšobotsi le ts'ebeliso ea emulsification, adhesion, thickening, viscosity e ntseng e eketseha, ho emisa, gelling le filimi-forming. E sebelisoa haholo litokisetsong tsa meriana 'me e tla phetha karolo e kholo tšimong ea litokisetso. Ka boithuto bo tebileng ba thepa ea eona le ntlafatso ea thekenoloji ea tlhahiso, HPMC e tla sebelisoa haholo lipatlisisong tsa mefuta e mecha ea litekanyetso le litsamaiso tse ncha tsa phano ea lithethefatsi, ka hona ho khothaletsa nts'etsopele e tsoelang pele ea litlhare.
hydroxypropyl methylcellulose; litokisetso tsa meriana; li-excipients tsa meriana.
Li-excipients tsa meriana ha se feela motheo oa ho theha litokisetso tsa lithethefatsi tse tala, empa hape li amana le bothata ba mokhoa oa ho lokisa, boleng ba lithethefatsi, botsitso, polokeho, sekhahla sa ho lokolloa ha lithethefatsi, mokhoa oa ts'ebetso, katleho ea bongaka, le nts'etsopele ea mekhoa e mecha. mefuta ea litekanyetso le litsela tse ncha tsa tsamaiso. e amanang haufi-ufi. Ho hlaha ha li-excipients tse ncha tsa meriana hangata ho khothaletsa ntlafatso ea boleng ba boitokiso le nts'etsopele ea mefuta e mecha ea litekanyetso. Hydroxypropyl methylcellulose (HPMC) ke e 'ngoe ea li-excipient tsa meriana tse tsebahalang haholo lapeng le kantle ho naha. Ka lebaka la boima ba eona bo fapaneng ba limolek'hule le viscosity, e na le mesebetsi ea ho etsa emulsifying, ho tlama, ho tenya, ho tenya, ho emisa le ho khomaretsa. Likarolo le ts'ebeliso e kang coagulation le sebopeho sa lifilimi li sebelisoa haholo theknoloji ea meriana. Sengoliloeng sena haholo-holo se lekola ts'ebeliso ea hydroxypropyl methylcellulose (HPMC) ha e etsoa lilemong tsa morao tjena.
1.Lintho tsa motheo tsa HPMC
Hydroxypropyl methyl cellulose (HPMC), mokhoa oa molek'hule ke C8H15O8- (C10 H18O6) n- C8H15O8, 'me boima ba molek'hule bo ka bang 86 000. Sehlahisoa sena ke thepa ea semi-synthetic, e leng karolo ea methyl le karolo ea polyhydroxypropyl ether ea cellulose. E ka hlahisoa ka litsela tse peli: E 'ngoe ke hore methyl cellulose ea kereiti e loketseng e phekoloa ka NaOH ebe e itšoara ka propylene oxide tlas'a mocheso o phahameng le khatello e phahameng. Nako ea karabelo e tlameha ho nka nako e lekaneng ho lumella methyl le hydroxypropyl hore li thehe litlamo tsa ether E kopantsoe le reng ea anhydroglucose ea selulose ka mokhoa oa cellulose, 'me e ka finyella tekanyo e lakatsehang; e 'ngoe ke ho tšoara linter tsa k'hothone kapa fiber pulp fiber ka soda ea caustic, ebe e arabela ka chlorinated methane le propylene oxide ka tatellano, ebe e tsoela pele ho e hloekisa. , e sithabetseng hore e be phofo e ntle le e tšoanang kapa granules.
'Mala oa sehlahisoa sena o tšoeu ho ea ho o mosoeu oa lebese, ha o na monko ebile ha o latsoehe, 'me sebopeho se na le granular kapa fibrous phofo e phallang habonolo. Sehlahisoa sena se ka qhibiliha ka metsing ho etsa tharollo e hlakileng ea lebese e tšoeu ea colloidal ka viscosity e itseng. Ketsahalo ea sol-gel interconversion e ka etsahala ka lebaka la phetoho ea mocheso oa tharollo ka mahloriso a itseng.
Ka lebaka la phapang lipakeng tsa lintho tsena tse peli tse nkang sebaka ka sebopeho sa methoxy le hydroxypropyl, ho hlahile mefuta e fapaneng ea lihlahisoa. Libakeng tse ikhethileng, mefuta e fapaneng ea lihlahisoa e na le litšobotsi tse ikhethang. Viscosity le mocheso oa mocheso oa gelation, ka hona o na le thepa e fapaneng 'me e ka sebelisoa ka merero e fapaneng. Pharmacopoeia ea linaha tse fapaneng e na le melaoana le litlatsetso tse fapaneng holima mohlala: European Pharmacopoeia e ipapisitse le limaraka tse fapaneng tsa li-viscosities tse fapaneng le likhato tse fapaneng tsa phetisetso ea lihlahisoa tse rekisoang 'marakeng, tse hlahisoang ke limaraka le linomoro, mme yuniti ke "mPa s. ”. US Pharmacopoeia, linomoro tsa 4 li kenyelletsoa ka mor'a lebitso la kakaretso ho bontša litaba le mofuta oa karolo e 'ngoe le e' ngoe ea hydroxypropyl methylcellulose, e kang hydroxypropyl methylcellulose 2208. Linomoro tse peli tsa pele li emela boleng bo hakanyetsoang ba sehlopha sa methoxy. Peresente, linomoro tse peli tsa ho qetela li emela palo e ka bang ea phesente ea hydroxypropyl.
Calocan's hydroxypropyl methylcellulose e na le 3 series, e leng E series, F series le K series, letoto le leng le le leng le na le mefuta e fapaneng ea mefuta eo u ka khethang ho eona. Letoto la E le sebelisoa haholo e le liphahlo tsa filimi, tse sebelisetsoang ho roala letlapa, li-cores tse koetsoeng tsa letlapa; E, F letoto li sebelisoa e le li-viscosifiers le ho lokolla li-agent tse thibelang mahlo bakeng sa litokisetso tsa mahlo, li-agent tse emisang, li-thickeners bakeng sa litokisetso tsa mokelikeli, matlapa le Li-Binders tsa granules; Letoto la K le sebelisoa haholo joalo ka li-release inhibitors le lisebelisoa tsa hydrophilic gel matrix bakeng sa litokisetso tsa tokollo butle le tse laoloang.
Baetsi ba malapeng haholo-holo ba kenyelletsa Fuzhou No. ., Ltd., Xi'an Huian limela tsa lik'hemik'hale, joalo-joalo.
2.Melemo ea HPMC
HPMC e fetohile e 'ngoe ea li-excipients tsa meriana tse sebelisoang ka ho fetisisa lapeng le linaheng tse ling, hobane HPMC e na le melemo eo li-excipients tse ling li se nang eona.
2.1 Ho qhibiliha ha metsi a batang
E qhibiliha ka metsing a batang ka tlase ho 40 ℃ kapa 70% ethanol, ha e le hantle e sa qhibiliheng metsing a chesang a ka holimo ho 60 ℃, empa e ka qhibiliha.
2.2 Ho inehela ka lik'hemik'hale
HPMC ke mofuta oa ether e seng ea ionic cellulose, tharollo ea eona ha e na tefiso ea ionic ebile ha e sebelisane le matsoai a tšepe kapa metsoako ea ionic organic, kahoo li-excipients tse ling ha li sebetsane le eona nakong ea tlhahiso ea litokisetso.
2.3 Botsitso
E batla e tsitsitse ka bobeli ho acid le alkali, 'me e ka bolokoa nako e telele pakeng tsa pH 3 le 11 ntle le phetoho e kholo ea viscosity. Tharollo ea metsi ea HPMC e na le phello e khahlanong le hlobo 'me e boloka botsitso bo botle ba viscosity nakong ea polokelo ea nako e telele. Li-excipients tsa meriana tse sebelisang HPMC li na le botsitso ba boleng bo betere ho feta tse sebelisang li-excipients tsa setso (tse kang dextrin, starch, joalo-joalo).
2.4 Viscosity Adjustable
Mefuta e fapaneng ea viscosity derivatives ea HPMC e ka tsoakoa ka likarolo tse fapaneng, 'me viscosity ea eona e ka fetoloa ho ea ka molao o itseng,' me e na le kamano e ntle ea linear, kahoo karolo e ka khethoa ho ea ka litlhoko.
2.5 Ho se sebetse hantle ha metabolism
HPMC ha e monye kapa ho sebelisoa metabolized 'meleng,' me ha e fane ka mocheso, kahoo ke motsoako o sireletsehileng oa ho lokisetsa meriana. 2.6 Tšireletseho Ka kakaretso ho nkoa hore HPMC ke ntho e se nang chefo le e sa tsitsang, tekanyo e bolaeang ea litoeba ke 5 g·kg - 1, le tekanyo e bolaeang ea likhoto ke 5. 2 g · kg - 1. Tekanyetso ea letsatsi le letsatsi ha e kotsi 'meleng oa motho.
3.Tšebeliso ea HPMC ha ho etsoa metsoako
3.1 Joalo ka thepa ea ho roala filimi le thepa ea ho etsa filimi
E sebelisa HPMC e le thepa ea letlapa e koahetsoeng ka filimi, letlapa le koahetsoeng ha le na melemo e totobetseng ea ho pata tatso le ponahalo ha li bapisoa le matlapa a tloaelehileng a koahetsoeng ka tsoekere, empa ho thatafala ha eona, ho ferekana, ho monya mongobo, tekanyo ea ho arohana. , ho roala boima ba 'mele le matšoao a mang a boleng a molemo. Sehlopha sa "viscosity" sa sehlahisoa sena se sebelisoa e le thepa ea ho roala filimi e qhibilihang ka metsing bakeng sa matlapa le lipilisi, 'me boemo bo phahameng ba viscosity bo sebelisoa e le thepa ea ho roala filimi bakeng sa litsamaiso tsa organic solvent, hangata e le motsoako oa 2% ho isa ho 20. %.
Zhang Jixing et al. e sebelisitse mokhoa oa ho sebelisa mokhoa oa ho ntlafatsa mokhoa oa ho etsa premix le HPMC e le seaparo sa filimi. Ho nka thepa ea ho etsa filimi HPMC, bongata ba joala ba polyvinyl le polasetiki ea polyethylene glycol e le lintlha tsa lipatlisiso, matla a tsitsitseng le ho phunyeletsa ha filimi le The viscosity ea tharollo ea ho roala filimi ke index ea tlhahlobo, le kamano pakeng tsa tlhahlobo. index le lintlha tsa tlhahlobo li hlalosoa ke mohlala oa lipalo, 'me mokhoa o nepahetseng oa ho hlophisa o qetella o fumanoe. Tšebeliso ea eona ke hydroxypropyl methylcellulose (HPMCE5) 11.88 g, polyvinyl alcohol 24.12 g, plasticizer polyethylene glycol 13.00 g, le viscosity ea ho fanyeha ea ho fanyeha ke 20 mPa · . Zhang Yuan o ntlafalitse ts'ebetso ea ho lokisa, a sebelisa HPMC e le setlamo ho nkela starch slurry sebaka, 'me a fetola matlapa a Jiahua hore a be matlapa a koahetsoeng ka filimi ho ntlafatsa boleng ba litokisetso tsa eona, ho ntlafatsa hygroscopicity ea eona, ho le bonolo ho fela, matlapa a hlephileng, a arohaneng le mathata a mang, ntlafatsa botsitso ba letlapa. Mokhoa o nepahetseng oa ho qapa o ne o khethoa ke liteko tsa orthogonal, e leng, slurry concentration e ne e le 2% HPMC ka 70% ea tharollo ea ethanol nakong ea ho roala, 'me nako e susumetsang nakong ea granulation e ne e le 15 min. Liphetho Matlapa a koahetsoeng ka filimi ea Jiahua a lokisitsoeng ke mokhoa o mocha le lengolo la ngaka a ile a ntlafatsoa haholo ka ponahalo, nako ea ho arohana le boima ba mantlha ho feta tse hlahisoang ke mokhoa oa pele oa lengolo la ngaka, 'me tekanyo e tšoanelehang ea matlapa a koahetsoeng ka filimi e ile ea ntlafatsoa haholo. e fihlile ho feta 95%. Liang Meiyi, Lu Xiaohui, joalo-joalo ba boetse ba sebelisa hydroxypropyl methylcellulose e le thepa ea ho etsa filimi ho lokisa letlapa la boemo ba patinae colon le matrine colon positioning tablet, ka ho latellana. ama ho lokolloa ha lithethefatsi. Huang Yunran o ile a lokisa matlapa a Dragon's Blood Colon Positioning, 'me a sebelisa HPMC ho tharollo ea ho roala ea lera la ho ruruha,' me karoloana ea eona e boima e ne e le 5%. Hoa bonahala hore HPMC e ka sebelisoa haholo tsamaisong ea phepelo ea lithethefatsi e lebisitsoeng ho colon.
Hydroxypropyl methylcellulose ha se feela thepa e ntle ea ho roala filimi, empa hape e ka sebelisoa e le thepa ea ho etsa filimi ha ho etsoa lifilimi. Wang Tongshun joalo-joalo ba ntlafalitsoe ho latela lengolo la ngaka la motsoako oa zinc licorice le aminolexanol oral composite film, ka ho feto-fetoha ha maemo, ho ts'oana, ho thella, pepeneneng ea moemeli oa lifilimi joalo ka index ea lipatlisiso, ho fumana lengolo la ngaka ke PVA 6.5 g, HPMC 0.1 g le 6.0 g ea propylene glycol e finyella litlhoko tsa ho lokolloa butle-butle le polokeho, 'me e ka sebelisoa e le taelo ea ho lokisetsa filimi e kopantsoeng.
3.2 joalo ka se tlamang le ho arohana
Sehlopha se tlaase sa viscosity sa sehlahisoa sena se ka sebelisoa e le se tlamella le ho senya matlapa, lipilisi le li-granules, 'me boemo bo phahameng ba viscosity bo ka sebelisoa feela e le se tlamang. Tekanyetso e fapana ho latela mefuta le litlhoko tse fapaneng. Ka kakaretso, tekanyetso ea "binder" bakeng sa matlapa a omileng a granulation ke 5%, 'me tekanyetso ea binder bakeng sa matlapa a metsi a granulation ke 2%.
Li Houtao et al ba ile ba hlahloba setlamo sa matlapa a tinidazole. 8% polyvinylpyrrolidone (PVP-K30), 40% sirapo, 10% starch slurry, 2.0% hydroxypropyl methylcellulose K4 (HPMCK4M), 50% ethanol e ile ea hlahlojoa e le ho khomarela matlapa a tinidazole ka ho latellana. tokiso ea matlapa a tinidazole. Ponahalo e fetoha ea matlapa a hlakileng le ka mor'a ho roala li ile tsa bapisoa, 'me ho lekanngoa ho thata, ho thata, nako ea ho arohana le sekhahla sa ho qhibiliha ha matlapa a fapaneng a lengolo la ngaka. Liphello Matlapa a lokiselitsoeng ke 2.0% hydroxypropyl methylcellulose a ne a benya, 'me tekanyo ea friability ha ea ka ea fumana ntho e ka holimo le ea likhutlong,' me ka mor'a ho roala, sebōpeho sa letlapa se ne se phethehile 'me ponahalo e ne e le ntle. Ka hona, matlapa a tinidazole a lokisitsoeng ka 2.0% HPMC-K4 le 50% ea ethanol e le li-binders a ile a sebelisoa. Guan Shihai o ile a ithuta mokhoa oa ho etsa Fuganning Tablets, a hlahloba li-adhesives, 'me a hlahloba 50% ea ethanol, 15% ea setache se peista, 10% PVP le 50% ea tharollo ea ethanol ka compressibility, boreleli, le friability e le matšoao a tlhahlobo. , 5% CMC-Na le 15% HPMC tharollo (5 mPa s). Liphetho Lipampitšana tse lokiselitsoeng ke 50% ethanol, 15% starch peista, 10% PVP 50% tharollo ea ethanol le 5% CMC-Na e ne e e-na le bokaholimo bo boreleli, empa compressibility e futsanehileng le boima bo tlaase, bo neng bo sitoa ho finyella litlhoko tsa ho roala; 15% Tharollo ea HPMC ( 5 mPa · s), bokaholimo ba letlapa le boreleli, friability e tšoaneleha, 'me compressibility e ntle, e ka finyellang litlhoko tsa ho roala. Ka hona, HPMC (5 mPa s) e khethiloe e le sekhomaretsi.
3.3 joalo ka moemeli ea emisang
Boemo bo phahameng ba viscosity ea sehlahisoa sena se sebelisoa e le moemeli oa ho emisa ho lokisa mokelikeli oa mofuta oa ho emisa. E na le phello e ntle ea ho emisa, e bonolo ho qhaqhoa hape, ha e khomarele lebota, 'me e na le likaroloana tse ntle tsa flocculation. Tekanyetso e tloaelehileng ke 0.5% ho 1.5%. Song Tian et al. e sebelisoang ka tloaelo lisebelisoa tsa polymer (hydroxypropyl methylcellulose, sodium carboxymethylcellulose, povidone, xanthan gum, methylcellulose, joalo-joalo) e le lisebelisoa tse emisang ho lokisa racecadotril. ho emisoa ho omileng. Ka tekanyo ea sedimentation ea molumo oa ho emisoa ho fapaneng, index ea redispersibility, le rheology, viscosity ea ho emisa le morphology ea microscopic e ile ea hlokomeloa, 'me ho ile ha hlahlojoa botsitso ba likaroloana tsa lithethefatsi tlas'a teko e potlakileng. Results Ho emisoa ho omileng ho lokiselitsoeng ka 2% HPMC kaha moemeli oa ho emisa o ne a e-na le mokhoa o bonolo le botsitso bo botle.
Ha ho bapisoa le methyl cellulose, hydroxypropyl methyl cellulose e na le litšobotsi tsa ho etsa tharollo e hlakileng haholoanyane, 'me ho na le lintho tse fokolang haholo tse sa qhalakaneng, kahoo HPMC e boetse e sebelisoa ka tloaelo e le moemeli ea emisang litokisetso tsa mahlo. Liu Jie et al. e sebelisitsoeng HPMC, hydroxypropyl cellulose (HPC), carbomer 940, polyethylene glycol (PEG), sodium hyaluronate (HA) le motsoako oa HA/HPMC e le lisebelisoa tse emisang ho lokisa lintlha tse fapaneng Bakeng sa Ciclovir ophthalmic suspension, sedimentation volume ratio, particle size and redispersibility li khethiloe e le matšoao a tlhahlobo ho hlahloba moemeli ea fanyehang ea molemo ka ho fetisisa. Liphello li bontša hore acyclovir ophthalmic suspension lokiselitsoeng ke 0.05% HA le 0.05% HPMC e le suspending agent, sedimentation volume ratio ke 0.998, particle size is uniform, redispersibility e ntle, 'me ho itokisa ho tsitsitse Ho kopanela liphate ho eketseha.
3.4 Joalo ka sethibela, ntho e lokollang butle le e laoloang le e etsang pore
Sehlopha se phahameng sa viscosity sa sehlahisoa sena se sebelisetsoa ho lokisoa ha matlapa a hydrophilic gel matrix a tsoelang pele a lokolloa, li-blockers le li-agents tse laoloang tsa lisebelisoa tse tsoakiloeng tsa matrix tse tsoelang pele, 'me li na le phello ea ho lieha ho lokolloa ha lithethefatsi. Khatiso ea eona ke 10% ho 80%. Limaraka tse tlase tsa viscosity li sebelisoa e le li-porogens bakeng sa litokisetso tsa tokollo e tsitsitseng kapa tse laoloang. Tekanyo ea pele e hlokahalang bakeng sa phello ea phekolo ea matlapa a joalo e ka finyelloa ka potlako, 'me joale phello e tsitsitseng kapa e laoloang e hlahisoa,' me motsoako o sebetsang oa lithethefatsi oa mali o bolokoa 'meleng. . Hydroxypropyl methylcellulose e tšeloa metsi ho etsa lera la gel ha e kopana le metsi. Mokhoa oa ho lokolloa ha lithethefatsi ho tloha letlapeng la matrix haholo-holo o kenyelletsa ho hasana ha lera la gel le khoholeho ea lera la gel. Jung Bo Shim et al ba lokiselitse matlapa a carvedilol a sa khaotseng a nang le HPMC e le lisebelisoa tse sa khaotseng.
Hydroxypropyl methylcellulose e boetse e sebelisoa haholo matlapeng a matrix a tsoelang pele a meriana ea setso ea Sechaena, 'me boholo ba metsoako e sebetsang, likarolo tse sebetsang hantle le litokisetso tse le' ngoe tsa meriana ea setso ea Sechaena li sebelisoa. Liu Wen et al. e sebelisitse 15% hydroxypropyl methylcellulose e le thepa ea matrix, 1% lactose le 5% microcrystalline cellulose e le li-filler, 'me e lokiselitse Jingfang Taohe Chengqi Decoction ka har'a matlapa a molomo a lokolloang ka nako e telele. Mohlala ke equation ea Higuchi. Sistimi ea sebopeho sa foromo e bonolo, ho lokisoa ho bonolo, mme data ea tokollo e batla e tsitsitse, e fihlelang litlhoko tsa Pharmacopoeia ea China. Tang Guanguang et al. e sebelisitse li-saponins tse felletseng tsa Astragalus e le sethethefatsi sa mohlala, e lokiselitse matlapa a matrix a HPMC, mme a hlahloba lintlha tse amang ho lokolloa ha lithethefatsi likarolong tse sebetsang tsa meriana ea setso ea Machaena matlapeng a matrix a HPMC. Liphetho Ha litekanyetso tsa HPMC li ntse li eketseha, ho lokolloa ha astragaloside ho ile ha fokotseha, 'me peresente ea tokollo ea moriana e ne e na le kamano e batlang e lekana le sekhahla sa ho felisoa ha matrix. Letlapeng la matrix la hypromellose HPMC, ho na le kamano e itseng pakeng tsa ho lokolloa ha karolo e sebetsang ea meriana ea setso ea Chaena le tekanyo le mofuta oa HPMC, 'me mokhoa oa ho lokolloa ha hydrophilic chemical monomer o tšoana le oona. Hydroxypropyl methylcellulose ha e loketse feela metsoako ea hydrophilic, empa le bakeng sa lintho tse seng tsa hydrophilic. Liu Guihua o sebelisitse 17% hydroxypropyl methylcellulose (HPMCK15M) e le lisebelisoa tsa matrix tse sa khaotseng, 'me a lokisa matlapa a matrix a Tianshan Xuelian ka mokhoa o tsitsitseng oa granulation le mokhoa oa tableting. Phello e tsitsitseng ea tokollo e ne e hlakile, 'me mokhoa oa ho lokisetsa o ne o tsitsitse ebile o ka khoneha.
Hydroxypropyl methylcellulose ha e sebelisoe feela matlapeng a matrix a tsitsitseng a metsoako e sebetsang le likarolo tse sebetsang tsa meriana ea setso ea Sechaena, empa hape e sebelisoa ka ho eketsehileng litokisetsong tsa metsoako ea meriana ea setso ea Chaena. Wu Huichao et al. e sebelisitse 20% hydroxypropyl methyl cellulose (HPMCK4M) e le thepa ea matrix, 'me e sebelisitse mokhoa oa ho hatella ka ho toba oa phofo ho lokisa letlapa la matrix la Yizhi hydrophilic gel le neng le ka lokolla lithethefatsi ka ho tsoelang pele le ka botsitso bakeng sa lihora tsa 12. Saponin Rg1, ginsenoside Rb1 le Panax notoginseng saponin R1 li ile tsa sebelisoa e le matšoao a tlhahlobo ho etsa lipatlisiso tsa tokollo ea in vitro, mme equation ea tokollo ea lithethefatsi e ile ea kenngoa ho ithuta mokhoa oa ho lokolla lithethefatsi. Results Mochini oa ho lokolla lithethefatsi o tsamaile le zero-order kinetic equation le Ritger-Peppas equation, moo geniposide e ileng ea lokolloa ke non-Fick diffusion, 'me likarolo tse tharo tsa Panax notoginseng li ile tsa lokolloa ke khoholeho ea masapo.
3.5 Sekhomaretsi se sireletsang joalo ka setenya le colloid
Ha sehlahisoa sena se sebelisoa e le motenya, palo e tloaelehileng ea liperesente ke 0.45% ho isa ho 1.0%. E ka boela ea eketsa botsitso ba sekhomaretsi sa hydrophobic, ho theha colloid e sireletsang, ho thibela likaroloana ho tloha ho coalescing le ho kopanya, ka tsela eo ho thibela ho thehoa ha sediments. Liphesente tse tloaelehileng tsa eona ke 0.5% ho isa ho 1.5%.
Wang Zhen et al. o sebelisitse mokhoa oa moralo oa liteko oa L9 oa orthogonal ho etsa lipatlisiso ka ts'ebetso ea ho lokisoa ha enema ea carbon activated. Maemo a nepahetseng a ts'ebetso bakeng sa qeto ea ho qetela ea moriana o entsoeng ka carbon enema ke ho sebelisa 0.5% sodium carboxymethyl cellulose le 2.0% hydroxypropyl methylcellulose (HPMC e na le 23.0% ea sehlopha sa methoxyl, hydroxypropoxyl Base 11.6%) e le motenya, maemo a thusa ho ntlafatsa. botsitso ba moriana activated carbon. Zhang Zhiqiang et al. e hlahisitse gel ea pH-sensitive levofloxacin hydrochloride ophthalmic e itokiselitseng ho sebelisoa e nang le phello e tsitsitseng, e sebelisa carbopol e le gel matrix le hydroxypropyl methylcellulose e le ntho e teteaneng. Levofloxacin hydrochloride 0.1 g, carbopol (9400) 3 g, hydroxypropyl methylcellulose (E50 LV) 20 g, disodium hydrogen hydrogen 0.35 g, disodium hydrogen phosphate 0.45 g ea sodium chloride 0.45 g ea sodium chloride 0.45 g. , 0.03 g ea ethyl paraben, le metsi li ile tsa kenngoa ho etsa 100 ml. Tekong, mongoli o ile a hlahloba letoto la hydroxypropyl methylcellulose METHOCEL ea Colourcon Company e nang le litlhaloso tse fapaneng (K4M, E4M, E15 LV, E50LV) ho lokisa li-thickeners tse nang le likhakanyo tse fapaneng, 'me sephetho se ile sa khetha HPMC E50 LV e le motenya. Thickener bakeng sa pH-sensitive levofloxacin hydrochloride li-gel hang-hang.
3.6 e le thepa ea capsule
Hangata, thepa ea khetla ea capsule ea li-capsules haholo-holo ke gelatin. Ts'ebetso ea tlhahiso ea khetla ea capsule e bonolo, empa ho na le mathata le liketsahalo tse ling tse kang tšireletso e fokolang khahlanong le mongobo le lithethefatsi tse nang le oksijene, ho fokotsa ho senyeha ha lithethefatsi, le ho lieha ho senyeha ha khetla ea capsule nakong ea polokelo. Ka hona, hydroxypropyl methylcellulose e sebelisoa e le sebaka sa li-capsules tsa gelatin bakeng sa ho lokisoa ha li-capsules, tse ntlafatsang sebopeho sa tlhahiso ea li-capsule le phello ea tšebeliso, 'me e khothalelitsoe haholo lapeng le linaheng tse ling.
Ho sebelisa theophylline e le lithethefatsi tse laolang, Podczeck et al. e fumane hore tekanyo ea ho qhibiliha ha lithethefatsi ea li-capsules tse nang le likhetla tsa hydroxypropyl methylcellulose e ne e le khōlō ho feta ea li-capsules tsa gelatin. Lebaka la tlhahlobo ke hore ho arohana ha HPMC ke ho arohana ha capsule eohle ka nako e le 'ngoe, ha ho arohana ha gelatin capsule ke ho senyeha ha mohaho oa marang-rang pele, ebe joale ho senyeha ha capsule eohle, kahoo HPMC capsule e loketse haholoanyane bakeng sa likhetla tsa Capsule bakeng sa litlhahlobo tsa tokollo hanghang. Chiwele et al. o ile a boela a fumana liqeto tse tšoanang 'me a bapisa ho qhibiliha ha gelatin, gelatin / polyethylene glycol le likhetla tsa HPMC. Liphello li bontšitse hore likhetla tsa HPMC li ile tsa qhibiliha ka potlako tlas'a maemo a fapaneng a pH, athe gelatin capsules E ameha haholo ke maemo a fapaneng a pH. Tang Yue et al. e hlahlobile mofuta o mocha oa khetla ea capsule bakeng sa mokhoa o tlaase oa lithethefatsi o se nang letho o omileng oa phofo ea inhaler carrier system. Ha ho bapisoa le khetla ea capsule ea hydroxypropyl methylcellulose le khetla ea capsule ea gelatin, botsitso ba khetla ea capsule le thepa ea phofo ka har'a khetla tlas'a maemo a fapaneng li ile tsa hlahlojoa, 'me teko ea friability e ile ea etsoa. Liphello li bontša hore ha li bapisoa le li-capsules tsa gelatin, likhetla tsa HPMC tsa capsule li molemo ka botsitso le tšireletso ea phofo, li na le ho hanyetsa mongobo o matla, 'me li na le friability e tlaase ho feta likhetla tsa gelatin capsule, kahoo likhetla tsa HPMC tsa capsule li loketse haholoanyane bakeng sa Capsules bakeng sa ho hema phofo e omileng.
3.7 joalo ka bioadhesive
Theknoloji ea bioadhesion e sebelisa li-excipients tse nang le lipolymers tsa bioadhesive. Ka ho khomarela mucosa ea likokoana-hloko, e ntlafatsa ho tsoela pele le ho tiea ha ho kopana pakeng tsa ho itokisa le mucosa, e le hore moriana o lokolloe butle-butle 'me o kenngoa ke mucosa ho finyella morero oa phekolo. E sebelisoa haholo hona joale. Kalafo ea mafu a pampitšana gastrointestinal, botshehadi, molomo mucosa le likarolo tse ling.
Theknoloji ea bioadhesion ea mala ke mokhoa o mocha oa phepelo ea lithethefatsi o ntlafalitsoeng lilemong tsa morao tjena. Ha e lelefatse feela nako ea ho lula ha litokisetso tsa lithethefatsi ka har'a pampitšana ea gastrointestinal, empa hape e ntlafatsa ts'ebetso ea ho ikopanya pakeng tsa lithethefatsi le lera la sele sebakeng sa ho monya, e fetola metsi a lera la sele, 'me e etsa hore ho kenella ha moriana ho kenelle. lisele tse nyenyane tsa mala epithelial lia ntlafatsoa, kahoo li ntlafatsa bioavailability ea lithethefatsi. Wei Keda et al. e hlahlobile lengolo la mantlha la letlapa le nang le litekanyetso tsa HPMCK4M le Carbomer 940 e le lintlha tsa lipatlisiso, 'me a sebelisa sesebelisoa se iketselitseng sa bioadhesion ho lekanya matla a ho ebola pakeng tsa letlapa le biofilm e etsisitsoeng ka boleng ba metsi a mokotleng oa polasetiki. , 'me qetellong a khetha litaba tsa HPMCK40 le carbomer 940 hore e be 15 le 27.5 mg sebakeng se nepahetseng ka ho fetisisa sa li-tablet tsa NCaEBT, ka ho latellana, ho lokisetsa lisebelisoa tsa letlapa la NCaEBT, tse bontšang hore lisebelisoa tsa bioadhesive (tse kang hydroxypropyl methylcellulose) li ka fokotsa haholo Ntlafatso ea Ntlafatso. ho kgomarela ha tokiso ho dinama.
Litokisetso tsa molomo oa bioadhesive hape ke mofuta o mocha oa mokhoa oa ho fana ka lithethefatsi o ithutoang haholoanyane lilemong tsa morao tjena. Litokisetso tsa li-bioadhesive tsa molomo li ka khomarela lithethefatsi ho karolo e amehileng ea molomo oa molomo, e seng feela ho lelefatsa nako ea ho lula ha lithethefatsi ka har'a mucosa ea molomo, empa hape e sireletsa molomo oa molomo. Phello e ntle ea kalafo le bioavailability e ntlafetseng ea lithethefatsi. Xue Xiaoyan et al. optimized thero ya insulin oral adhesive tablets, sebelisa apple pectin, chitosan, carbomer 934P, hydroxypropyl methylcellulose (HPMC K392) le sodium alginate e le lisebelisoa tsa bioadhesive, le ho omisa ka leqhoa ho lokisetsa insulin ea molomo. Letlapa le khomarelang habeli. Letlapa le lokiselitsoeng la sekhomaretsi sa insulin se na le sebopeho se kang seponche, se loketseng ho lokolloa ha insulin, 'me se na le lera le sireletsang la hydrophobic, le ka netefatsang ho lokolloa ha moriana ka tsela e fapaneng le ho qoba tahlehelo ea moriana. Hao Jifu et al. e boetse e lokisitse lifaha tse boputsoa bo bosehla ka molomo li sebelisa sekhomaretsi sa Baiji, HPMC le carbomer joalo ka thepa ea sekhomaretsi.
Litsamaisong tsa phano ea lithethefatsi ka botšehaling, theknoloji ea bioadhesion e boetse e sebelisoa haholo. Zhu Yuting et al. e sebelisitse carbomer (CP) le HPMC e le lisebelisoa tsa sekhomaretsi le matrix a tsitsitseng-ho lokolloa ho lokisetsa matlapa a clotrimazole bioadhesive vaginal ka mefuta e sa tšoaneng le likaroloana, 'me a lekanya ho khomarela ha bona, nako ea ho khomarela le peresente ea ho ruruha tikolohong ea mokelikeli oa botšehali oa maiketsetso. , lengolo la ngaka le loketseng le ile la hlahlojoa e le CP-HPMC1: 1, letlapa le lokiselitsoeng la sekhomaretsi le ne le e-na le ts'ebetso e ntle ea ho khomarela, 'me mokhoa ona o ne o le bonolo ebile o khoneha.
3.8 joalo ka gel ea sehlooho
E le ho lokisetsa sekhomaretsi, gel e na le letoto la melemo e kang polokeho, botle, ho hloekisa habonolo, theko e tlaase, mokhoa o bonolo oa ho lokisetsa, le ho lumellana hantle le lithethefatsi. Tataiso ea ntlafatso. Mohlala, gel ea transdermal ke mofuta o mocha oa litekanyetso o ithutoang haholo lilemong tsa morao tjena. E ke ke ea qoba feela ho timetsoa ha lithethefatsi ka har'a pampitšana ea gastrointestinal le ho fokotsa phapang ea tlhōrō-to-trough ea khatello ea meriana ea mali, empa hape e fetohile e 'ngoe ea mekhoa e sebetsang ea ho lokolla lithethefatsi ho hlōla litla-morao tsa lithethefatsi. .
Zhu Jingjie et al. o ithutile phello ea matrices a fapaneng ho lokolloa ha scutellarin alcohol plastid gel in vitro, le ho hlahlojoa ka carbomer (980NF) le hydroxypropyl methylcellulose (HPMCK15M) e le matrices a gel, 'me a fumana scutellarin e loketseng scutellarin. Gel matrix ea joala plastids. Liphetho tsa liteko li bontša hore 1. 0% carbomer, 1. 5% carbomer, 1. 0% carbomer + 1. 0% HPMC, 1. 5% carbomer + 1. 0% HPMC e le gel matrix Ka bobeli li loketse scutellarin alcohol plastids . Nakong ea teko, ho ile ha fumanoa hore HPMC e ka fetola mokhoa oa ho lokolloa ha lithethefatsi oa carbomer gel matrix ka ho lumellana le kinetic equation ea ho lokolloa ha lithethefatsi, 'me 1.0% HPMC e ka ntlafatsa 1.0% carbomer matrix le 1.5% carbomer matrix. Lebaka e ka 'na ea e-ba hore HPMC e atoloha ka potlako,' me katoloso e potlakileng qalong ea teko e etsa hore lekhalo la limolek'hule tsa thepa ea gel ea carbomer e be kholoanyane, kahoo e potlakisa sekhahla sa ho lokolloa ha lithethefatsi. Zhao Wencui et al. e sebelisitse carbomer-934 le hydroxypropyl methylcellulose e le bajari ho lokisa norfloxacin ophthalmic gel. Mokhoa oa ho lokisetsa o bonolo ebile o ka khoneha, 'me boleng bo lumellana le gel ea mahlo ea "Chinese Pharmacopoeia" (khatiso ea 2010) Litlhoko tsa boleng.
3.9 Precipitation inhibitor bakeng sa self-microemulsifying system
Self-microemulsifying drug delivery system (SMEDDS) ke mofuta o mocha oa mokhoa oa ho fana ka lithethefatsi ka molomo, e leng motsoako o ts'oanang, o tsitsitseng le o hlakileng o entsoeng ka lithethefatsi, karolo ea oli, emulsifier le co-emulsifier. Sebopeho sa lengolo la ngaka se bonolo, 'me polokeho le botsitso li ntle. Bakeng sa lithethefatsi tse sa qhibilihang hantle, lisebelisoa tsa polymer tse qhibilihang ka metsing, tse kang HPMC, polyvinylpyrrolidone (PVP), joalo-joalo, hangata li ekeletsoa ho etsa hore lithethefatsi tse sa lefelloeng le lithethefatsi tse kentsoeng ka har'a microemulsion li fihlelle ho qhibiliha ha supersaturated ka har'a pampitšana ea mala, e le ho eketsa ho qhibiliha ha lithethefatsi le ho ntlafatsa bioavailability.
Peng Xuan et al. e lokisitse silibinin supersaturated self-emulsifying drug delivery system (S-SEDDS). Oxyethylene hydrogenated castor oil (Cremophor RH40), 12% caprylic capric acid polyethylene glycol glyceride (Labrasol) e le co-emulsifier, le 50 mg·g-1 HPMC. Ho kenyelletsa HPMC ho SSEDDS ho ka fetisa silibinin ea mahala hore e qhibilihe ho S-SEDDS le ho thibela silibinin ho tsoa. Ha ho bapisoa le mekhoa e tloaelehileng ea "self-microemulsion formulations", "surfactant" e kholoanyane e atisa ho eketsoa ho thibela ho kenngoa ha lithethefatsi tse sa fellang. Ho eketsoa ha HPMC ho ka boloka ho qhibiliha ha silibinin sebakeng sa ho qhibiliha ho batla ho sa fetohe, ho fokotsa emulsification ka ho iketsetsa microemulsion formulations. tekanyo ya moemedi.
4.Qetello
Ho ka bonoa hore HPMC e sebelisitsoe haholo litokisetsong ka lebaka la thepa ea eona ea 'mele, ea lik'hemik'hale le ea likokoana-hloko, empa HPMC e boetse e na le mefokolo e mengata litokisetsong, tse kang ts'ebetso ea ho lokolloa pele le ka mor'a ho phatloha. methyl methacrylate) ho ntlafatsa. Ka nako e ts'oanang, bafuputsi ba bang ba ile ba etsa lipatlisiso mabapi le ts'ebeliso ea theory ea osmotic ho HPMC ka ho lokisa matlapa a tokollo ea carbamazepine le matlapa a tokollo e tsitsitseng a verapamil hydrochloride ho tsoela pele ho ithuta mokhoa oa eona oa tokollo. Ka mantsoe a mang, bafuputsi ba bangata ba ntse ba etsa mosebetsi o mongata bakeng sa ts'ebeliso e ntle ea HPMC litokisetsong, 'me ka thuto e tebileng ea thepa ea eona le ntlafatso ea theknoloji ea ho itokisa, HPMC e tla sebelisoa haholo ka mefuta e mecha ea litekanyetso. le mefuta e mecha ea litekanyetso. Lipatlisisong tsa tsamaiso ea meriana, ebe o khothalletsa tsoelo-pele e tsoelang pele ea pharmacy.
Nako ea poso: Oct-08-2022