1. Lintho tsa motheo tsa HPMC
Hydroxypropyl methylcellulose, lebitso la Senyesemane ke hydroxypropyl methylcellulose, e tsejoang hape e le HPMC.Mokhoa oa eona oa molek'hule ke C8H15O8-(C10Hl8O6)N-C8HL5O8, 'me boima ba eona ba molek'hule ke hoo e ka bang 86,000.Sehlahisoa sena ke semi-synthetic, se nang le karolo ea methyl le karolo ea cellulose polyhydroxypropyl ether.E ka etsoa ka mekhoa e 'meli: e' ngoe ke ho tšoara sehlopha se loketseng sa methyl cellulose ka NaOH, ebe o itšoara ka propylene oxide tlas'a mocheso o phahameng le khatello e phahameng.Nako ea karabelo e tlameha ho ts'oaroa e le hore lihlopha tsa methyl le hydroxypropyl li ka fetoloa ethers.Sebopeho se teng 'me se hokahane le selikalikoe sa tsoekere se senyehileng sa cellulose ho isa tekanyong e hlokahalang;e 'ngoe ke ho phekola lesela la k'hothone kapa fiber pulp ea lehong ka soda ea caustic ho arabela ho fumana methane chloride le propylene oxide, e ka hloekisoang le ho ea fatše.Etsa hore e be phofo e ntle le e ts'oanang kapa li-granules.HPMC ke selulose ea semela sa tlhaho le sehlahisoa se setle sa meriana se nang le mehloli e mengata e fapaneng.Hona joale e sebelisoa haholo lapeng le linaheng tse ling 'me ke e' ngoe ea lisebelisoa tsa meriana tse sebelisoang ka ho fetisisa litlhare tse nooang.
Sehlahisoa sena se tšoeu ho ea ho bosoeu ba lebese, ha se chefo, ha se na monko, granular kapa fibrous, phofo e phallang habonolo.E batla e tsitsitse tlas'a khanya le mongobo.E atoloha metsing a batang ho etsa tharollo ea milky colloidal e nang le viscosity e itseng, 'me ketsahalo ea sol-gel interconversion e etsahala ka lebaka la phetoho ea mocheso oa tharollo ka mahloriso a itseng.E qhibiliha haholo ka 70% ea ethanol kapa dimethyl ketone, empa e sa qhibilihe ka ho feletseng ka ethanol, chloroform kapa ethoxyethane.
Phaello ea pH ea hydroxypropyl methylcellulose e pakeng tsa 4.0 le 8.0, 'me e na le botsitso bo botle.Theko ea pH e tsitsitse pakeng tsa 3.0 le 11.0.E ka bolokoa ho 20°C le mongobo o lekanyelitsoeng oa 80% ka matsatsi a 10.Coefficient ea ho monya mongobo ea HPMC ke 6.2%.
Hydroxypropyl methylcellulose e na le mefuta e fapaneng ea lihlahisoa ka lebaka la likahare tse fapaneng tsa lihlopha tsa methoxy le hydroxypropyl mohahong.Libakeng tse ikhethileng, mefuta e fapaneng ea lihlahisoa e na le viscosity e khethehileng le thepa ea mocheso.Mocheso oa mocheso oa gel mme ka hona o na le thepa e fapaneng e ka sebelisetsoang merero e fapaneng.Pharmacopoeia ea naha ka 'ngoe e na le litlhoko le litlhaloso tse fapaneng tsa mohlala: European Pharmacopoeia e ipapisitse le li-viscosities tse fapaneng, likhato tse fapaneng tsa ho nka sebaka, maemo a ts'ebeliso le lipalo tsa limaraka tse fapaneng tsa lihlahisoa tse rekisoang 'marakeng.Yuniti ea United States Pharmacopoeia ke mPa·s, 'me mabitso a tloaelehileng ke a latelang Sebelisa linomoro tse' nè ho emela litaba tsa hydroxypropyl methylcellulose e nang le mefuta e fapaneng le mefuta e fapaneng, joalo ka hydroxypropyl methylcellulose, 2208. Linomoro tse peli tsa pele li emela palo e ka bang teng lekholong. ea lihlopha tsa methoxy, 'me linomoro tse peli tsa ho qetela li emela sehlopha sa hydroxyl.Hoo e ka bang peresente ea propyl.
2. HPMC e qhibilihisoa ka mokhoa oa metsi
2.1 Mokhoa oa metsi a chesang
Kaha hydroxypropyl cellulose ha e qhibilihe ka metsing a chesang, e ka qhalakanngoa ka ho lekana metsing a chesang ebe e pholile.Mekhoa e 'meli e tloaelehileng e hlahisoa ka tsela e latelang:
(1) Kenya selekanyo se se tlhokegang sa metsi a a molelo mo setshelong mme o se futhumale mo e ka nnang 70°C.Eketsa sehlahisoa butle-butle ha u ntse u susumetsa butle-butle.Qalong, sehlahisoa se phaphamala holim'a metsi ebe butle-butle se etsa slurry.
(2) Kenya 1/3 kapa 2/3 ea palo e hlokahalang ea metsi ka har'a sets'oants'o 'me ue futhumale ho 70 ° C ho qhala sehlahisoa, lokisa seretse sa metsi a chesang, ebe u eketsa palo e setseng ea metsi a batang kapa eketsa leqhoa. metsi ho isa seretseng sa metsi a chesang.slurry ka metsing, hlohlelletsa motsoako ka mor'a ho pholile.
2.2 Mokhoa oa ho kopanya phofo
Likaroloana tsa phofo li qhalakanngoa ka ho feletseng ka ho kopanya ho omileng ka tekanyo e lekanang kapa e kholo ea lisebelisoa tse ling tse phofshoana ebe li qhibiliha ka metsi, moo HMCS e qhibilihang ntle le ho kopana.
3. Melemo ea HPMC
3.1 E qhibiliha ka metsing a batang
E qhibiliha metsing a batang a ka tlase ho 40 ℃ kapa 70% ethanol, 'me ha e le hantle ha e qhibilihe metsing a chesang a ka holimo ho 60 ℃, empa e ka qhibiliha.
3.2 Ho se sebetse ka lik'hemik'hale
HPMC ke non-ionic cellulose ether.Tharollo ea eona ha e na tefo ea ionic ebile ha e sebelisane le letsoai la tšepe kapa metsoako ea ionic organic.Ka hona, li-excipients tse ling ha li sebetsane le eona nakong ea tlhahiso ea tlhahiso.
3.3 Botsitso
E tsitsitse ho acid le alkali mme e ka bolokoa nako e telele pakeng tsa pH 3 le 1l ntle le phetoho e kholo ea viscosity.Litharollo tsa metsi tsa hydroxypropyl methylcellulose (HPMC) li na le li-antifungal 'me li boloka botsitso bo botle ba viscosity nakong ea polokelo ea nako e telele.Botsitso ba boleng ba HPMC bo molemo ho feta li-excipients tsa setso (tse kang dextrin, starch, joalo-joalo).
3.4 Viscosity e fetolehang
Mefuta e fapaneng ea viscosity derivatives ea HPMC e ka ba ka likarolo tse fapaneng, 'me viscosity ea bona e ka fetoloa ho ea ka litlhoko tsa ho lumellana le melao e itseng le ho ba le kamano e ntle ea linear, kahoo karo-karolelano e ka khethoa ho ea ka litlhoko.
3.5 Ho se sebetse hantle ha metabolism
HPMC ha e monye kapa ha e na metabolized 'meleng' me ha e fane ka mocheso, kahoo ke motsoako o sireletsehileng bakeng sa litokisetso tsa meriana.
3.6 Tšireletseho
Ka kakaretso HPMC e nkoa e le lintho tse se nang chefo, tse sa hloekiseng, tse nang le LD50 ea 5g/kg ho litoeba le 5.2g/kg ho likhoto.Litekanyetso tsa letsatsi le letsatsi ha li kotsi ho batho.
4 Tšebeliso ea HPMC ha ho etsoa litokisetso
4.1 Lisebelisoa tsa ho roala lifilimi le lisebelisoa tsa ho etsa lifilimi
Hydroxypropyl methylcellulose (HPMC) e sebelisoa e le thepa ea ho roala filimi.Matlapa a eona a koahetsoeng ha a na melemo e totobetseng ho feta matlapa a tloaelehileng a koahetsoeng joalo ka matlapa a koahetsoeng ka tsoekere mabapi le ho pata tatso le ponahalo ea lithethefatsi, empa ho thatafala ha eona, brittleness, le hygroscopicity , ho senyeha ho fokolang., ho roala boima ba 'mele le matšoao a mang a boleng a molemo.Sehlopha se tlaase sa viscosity sa sehlahisoa sena se sebelisoa e le thepa ea ho roala filimi e qhibilihang ka metsi bakeng sa matlapa le lipilisi, 'me boemo bo phahameng ba viscosity bo sebelisoa e le thepa ea ho roala filimi bakeng sa lisebelisoa tsa li-solvents tsa organic.Hangata mahloriso ke 2.0% ~ 20%.
4.2 Joalo ka se tlamang le ho arola
Mofuta o tlase oa viscosity oa sehlahisoa sena o ka sebelisoa e le setlamo le ho senya matlapa, lipilisi le li-granules, athe boemo bo phahameng ba viscosity bo ka sebelisoa feela joalo ka setlama.Tekanyetso e fapana ho latela mohlala le litlhoko, hangata ke 5% bakeng sa matlapa a ommeng a granulation le 2% bakeng sa matlapa a metsi a granulation.
4.3 E le thuso ea ho emisa
Moemeli oa ho emisa ke ntho ea gel e nang le viscous e nang le hydrophilic 'me e ka sebelisoa ho fokotsa lebelo la ho emisa la likaroloana le ho khomarela bokaholimo ba likaroloana ho thibela likaroloana hore li se ke tsa kopana ho ba libolo.Lisebelisoa tsa ho fanyeha li phetha karolo ea bohlokoa tlhahisong ea li-suspension agents.HPMC ke kenyelletso e ntle ea ho emisa.Tharollo ea eona ea colloidal e qhibilihisitsoeng e ka fokotsa tsitsipano ea sefahleho sa metsi-e tiileng le matla a mahala a likaroloana tse nyenyane tse tiileng, kahoo e matlafatsa botsitso ba tsamaiso e fapaneng ea ho hasana.Sehlahisoa sena ke tokiso ea ho emisoa e nang le viscosity e phahameng e nang le phello e ntle ea ho emisa, ho hasana habonolo, lerako le se nang thupa, le likaroloana tse ntle tsa flocculation.Tekanyetso ea eona e tloaelehileng ke 0.5% ho isa ho 1.5%.
4.4 Joalo ka sehlahisoa se sa sebetseng, sa tokollo e tšoarellang le porogen
Boemo bo phahameng ba viscosity ea sehlahisoa sena se sebelisetsoa ho lokisa matlapa a hydrophilic gel matrix a tsoelang pele a lokolloa, matlapa a matrix a nako e telele a lokolloang a li-retarders le li-agents tse laoloang.E na le phello ea ho lieha ho lokolloa ha lithethefatsi.Tšebeliso ea eona ke 10% -80% (W / W).Maemo a tlase a viscosity a sebelisoa e le li-inducers tsa pore mekhoeng e tsitsitseng kapa e laoloang ea tokollo.Matlapa a joalo a ka fihlela kapele tekanyo ea pele e hlokahalang bakeng sa phello ea phekolo, ebe a hlahisa phello e tsitsitseng kapa e laoloang ea tokollo, 'me a boloka metsoako e sebetsang ea lithethefatsi ea mali' meleng.Hydroxypropyl methylcellulose e hydrate ka metsing ho etsa lera la gel.Mokhoa oa ho lokolla lithethefatsi oa matlapa a matrix haholo-holo o kenyelletsa ho hasana ha lera la gel le ho qhibiliha ha lera la gel.
4.5 Li-thickeners le li-colloids tse sireletsang
Ha sehlahisoa sena se sebelisoa e le motenya, mohopolo o sebelisoang hangata ke 0.45% ~ 1.0%.Sehlahisoa sena se ka boela sa eketsa botsitso ba sekhomaretsi sa hydrophobic, sa theha colloid e sireletsang, thibela likaroloana ho tloha ho agglomeration le agglomeration, ka tsela eo, ho thibela ho thehoa ha pula.Khatiso ea eona e tloaelehileng ke 0.5% ~ 1.5%.
4.6 Sebelisa e le thepa ea capsule
Hangata, thepa ea khetla ea capsule ea li-capsules ke gelatin.Ts'ebetso ea tlhahiso ea likhetla tsa gelatin capsule e bonolo, empa ho na le mathata le liketsahalo tse kang tšireletso e fokolang khahlanong le lithethefatsi tse nang le mongobo le oksijene, ho fokotsa ho senyeha ha lithethefatsi, le ho lieha ho arohana ha likhetla tsa capsule nakong ea polokelo.Ka hona, hydroxypropyl methylcellulose e sebelisoa e le sebaka sa lisebelisoa tsa capsule ha ho etsoa li-capsules, tse ntlafatsang tlhahiso, ho bōpa le ho sebelisa liphello tsa li-capsules, 'me li khothalelitsoe haholo lapeng le linaheng tse ling.
4.7 E le bioadhesive
Theknoloji ea bioadhesion e sebelisa li-excipients tse nang le li-polymers tsa bioadhesive ho khomarela mucosa ea likokoana-hloko le ho ntlafatsa ho tsitsisa le ho tiisa ho kopana pakeng tsa ho lokisetsa le mucosa, ho lumella moriana hore o lokolloe butle-butle le ho kenngoa ke mucosa ho finyella merero ea phekolo.E le ho finyella morero oa phekolo, hona joale e sebelisoa haholo ho phekola mafu a ka mokokotlong oa nko, mucosa ea molomo le likarolo tse ling tsa 'mele.Theknoloji ea "gastrointestinal bioadhesion" ke mofuta o mocha oa tsamaiso ea ho fana ka lithethefatsi e entsoeng 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 kopana pakeng tsa lithethefatsi le sebaka sa ho monya lesela la sele le ho fetola sebopeho sa lera la sele.Mobility, ke hore, ho kenella ha moriana liseleng tsa mala epithelial, ka tsela eo.
Nako ea poso: Feb-01-2024