Sehlopha: thepa ea ho koahela; Thepa ea lera; Thepa ea polymer e laoloang ka lebelo bakeng sa litokisetso tsa ho lokolla butle; Moemeli oa ho tsitsisa; Thuso ea ho emisoa, sekhomaretsi sa letlapa; Moemeli oa ho khomarela o matlafalitsoeng.
1. Selelekela sa sehlahisoa
SEHLAHISOA sena KE ETHER EA SEBELLOLOSE E SE NANG IONIC, e bonoang kantle e le phofo e tšoeu, e se nang monko ebile ha e na tatso, e qhibilihang ka metsing le li-solvents tse ngata tsa tlhaho tsa polar, e ruruha ka metsing a batang ho ea tharollong e hlakileng kapa e nang le turBId hanyane ea colloidal. Tharollo ea metsi e na le ts'ebetso ea bokaholimo, pepeneneng e phahameng le ts'ebetso e tsitsitseng. HPMC e na le thepa ea gel e chesang. Kamora ho futhumatsa, tharollo ea metsi ea sehlahisoa e etsa pula ea gel, ebe ea qhibiliha kamora ho pholile. Mocheso oa gel oa litlhaloso tse fapaneng oa fapana. Ho qhibiliha hoa fetoha ka viscosity, viscosity zhao e tlase, ha ho qhibiliha ho hoholo, litlhaloso tse fapaneng tsa thepa ea HPMC li na le liphapang tse itseng, HPMC e qhibilihisitsoeng ka metsing ha e angoe ke boleng ba pH.
Mocheso oa ho tuka o sa reroang, boima bo hlephileng, boima ba 'nete le mocheso oa phetoho ea khalase e ne e le 360℃, 0.341g/cm3, 1.326g/cm3 le 170 ~ 180℃, ka ho latellana. Kamora ho futhumatsa, e fetoha sootho ho 190 ~ 200 ° C 'me e chese ho 225 ~ 230 ° C.
HPMC ha e qhibilihe hakaalo ka har'a chloroform, ethanol (95%), le diethyl ether, 'me e qhibilihile ka har'a motsoako oa ethanol le methylene chloride, motsoako oa methanol le methylene chloride, le motsoako oa metsi le ethanol. Maemo a mang a HPMC a qhibiliha ka har'a metsoako ea acetone, methylene chloride, le 2-propanol, hammoho le li-solvents tse ling tsa tlhaho.
Tafole ea 1: Matšoao a tekheniki
projeke
Tekanyo,
60 gd (2910).
65GD(2906)
75GD(2208)
Methoxy %
28.0-32.0
27.0-30.0
19.0-24.0
Hydroxypropoxy %
7.0-12.0
4.0-7.5
4.0-12.0
Mocheso oa gel ℃
56-64.
62.0-68.0
70.0-90.0
Ho teteana ha mpa s.
3,5,6,15,50,4000
50400 0
100400 0150 00100 000
Ho theola boima ba 'mele ka omileng %
5.0 kapa ka tlase ho moo
Masalla a tukang %
1.5 kapa ka tlase ho moo
pH
4.0-8.0
Tšepe e boima
20 kapa ka tlase ho moo
arsenic
2.0 kapa ka tlase ho moo
2. Likarolo tsa sehlahisoa
2.1 Hydroxypropyl methylcellulose e qhibilihisoa ka metsing a batang ho etsa tharollo e viscous colloidal. Hafeela e eketsoa metsing a batang mme e hlohlelletsoa hanyane, e ka qhibilihisoa hore e be tharollo e bonaletsang. Ho fapana le hoo, ha e qhibilihe ka metsing a chesang a fetang 60℃ mme e ka ruruha feela. Ha ho lokisetsoa tharollo e metsi ea hydroxypropyl methicellulose, ho molemo ho eketsa karolo ea hydroxypropyl methicellulose ka bongata bo itseng ba metsi, e hlohlelletse ka matla, e futhumatsoe ho fihlela ho 80 ~ 90℃, ebe o eketsa hydroxypropyl methicellulose e setseng, 'me qetellong o sebelise metsi a batang ho eketsa bongata bo hlokahalang.
2.2 Hydroxypropyl methylcellulose ke ether ea cellulose e seng ea ionic, tharollo ea eona ha e na tjhaja ea ionic, ha e sebelisane le letsoai la tšepe kapa metsoako ea ionic ea organic, e le ho netefatsa hore HPMC ha e arabele le lisebelisoa tse ling tse tala le metsoako e thusang nakong ea tlhahiso ea ho lokisa.
2.3 Hydroxypropyl methylcellulose e na le anti-sensitivity e matla, 'me ka keketseho ea tekanyo ea ho nkeloa sebaka sebopehong sa limolek'hule, anti-sensitivity le eona ea eketseha. Lithethefatsi tse sebelisang HPMC e le li-excipients li na le boleng bo tsitsitseng haholoanyane nakong e sebetsang ho feta lithethefatsi tse sebelisang li-excipients tse ling tsa setso (starch, dextrin, tsoekere e phofshoana).
2.4 Hydroxypropyl methylcellulose ha e sebetse hantle ka lebaka la metabolism. Jwalo ka motswako wa meriana, ha e kenngwe kapa ho monngwa, kahoo ha e fane ka mocheso meriana le dijong. E na le bokgoni bo ikgethang ba ho sebetsa ho boleng bo tlase ba khalori, meriana e se nang letswai, e seng ya allergy le dijo bakeng sa batho ba nang le lefu la tswekere.
2.5HPMC e tsitsitse haholo ho li-acid le metheo, empa haeba pH e feta 2 ~ 11 'me e angoa ke mocheso o phahameng kapa nako e telele ea polokelo, e tla fokotsa tekanyo ea ho butsoa.
2.6 Tharollo ea metsi ea Hydroxypropyl methylcellulose e ka fana ka ts'ebetso ea bokaholimo, e bonts'a boleng bo itekanetseng ba khatello ea bokaholimo le ea interfacial. E na le emulsification e sebetsang tsamaisong ea mekhahlelo e 'meli' me e ka sebelisoa e le stabilizer e sebetsang hantle le colloid e sireletsang.
2.7 Tharollo ea metsi ea Hydroxypropyl methylcellulose e na le thepa e ntle ea ho etsa filimi, 'me ke thepa e ntle ea ho roala bakeng sa matlapa le lipilisi. Lera le entsoeng ke eona ha le na 'mala ebile le tiile. Haeba glycerol e eketsoa, botlolo ba eona bo ka eketsoa. Kamora kalafo ea bokaholimo, sehlahisoa se qhalanngoa ka metsing a batang, 'me sekhahla sa ho qhibiliha se ka laoloa ka ho fetola tikoloho ea pH. E sebelisoa litokisetsong tsa ho lokolla butle le litokisetsong tse koahetsoeng ke enteric.
3. Tšebeliso ea sehlahisoa
3.1. E sebelisoa e le sekhomaretsi le sesebelisoa sa ho qhalana
HPMC e sebelisetsoa ho khothaletsa ho qhibiliha ha moriana le tekanyo ea ts'ebeliso ea tokollo, e ka qhaloa ka ho toba ka har'a solvent e le sekhomaretsi, viscosity e tlase ea HPMC e qhalakantsoeng ka metsing ho etsa tharollo e bonaletsang ea colloid e khomarelang ea lenaka la tlou, matlapa, lipilisi, li-granules holim'a sekhomaretsi le moemeli o qhalanang, le viscosity e phahameng bakeng sa sekhomaretsi, e sebelisoa feela ka lebaka la mefuta e fapaneng le litlhoko tse fapaneng, kakaretso ke 2% ~ 5%.
Tharollo ea metsi ea HPMC le khatello e itseng ea ethanol ho etsa motsoako o kopaneng; Mohlala: Tharollo ea metsi ea 2%HPMC e kopantsoeng le tharollo ea ethanol ea 55% e sebelisitsoe bakeng sa ho pellet ea li-capsule tsa amoxicillin, hoo karolelano ea ho qhibiliha ha li-capsule tsa amoxicillin e ileng ea eketseha ho tloha ho 38% ho isa ho 90% ntle le HPMC.
HPMC e ka etsoa ka sekhomaretsi se kopaneng se nang le mahloriso a fapaneng a seretse sa starch kamora ho qhibiliha; Ho qhibiliha ha matlapa a koahetsoeng ka erythromycin ho eketsehile ho tloha ho 38.26% ho isa ho 97.38% ha 2% HPMC le 8% starch li ne li kopanngoa.
2.2. Etsa thepa ea ho koahela filimi le thepa ea ho etsa filimi
HPMC e le thepa ea ho roala e qhibilihang ka metsing e na le litšobotsi tse latelang: ho hlaka ha tharollo ho itekanetseng; Mokhoa oa ho roala o bonolo; Thepa e ntle ea ho etsa filimi; E ka boloka sebopeho sa sengoathoana, ea ngola; E ka thibela mongobo; E ka 'mala, ea lokisa tatso. SEHLAHISOA sena se sebelisoa e le ho roala filimi e qhibilihang meleng bakeng sa matlapa le lipilisi tse nang le ho hlaka ho tlase, 'me bakeng sa ho roala filimi e sa thehoeng METSI ka ho hlaka ho hoholo, chelete ea tšebeliso ke 2%-5%.
2.3, e le sesebelisoa sa ho teteana le sekhomaretsi sa tšireletso ea colloidal
HPMC e sebelisoang e le sesebelisoa sa ho tiisa ke 0.45% ~ 1.0%, e ka sebelisoa e le marotholi a mahlo le sesebelisoa sa maiketsetso sa ho tiisa meokho; E sebelisoa ho eketsa botsitso ba sekhomaretsi se sa hlokeng metsi, ho thibela ho kopana ha likaroloana, pula, tekanyo e tloaelehileng ke 0.5% ~ 1.5%.
2.4, e le sethibela-mafu, thepa e lokollang butle, moemeli oa ho lokolla o laoloang le moemeli oa ho ntša mantle.
Mohlala oa HPMC o nang le viscosity e phahameng o sebelisetsoa ho lokisa li-blocker le li-release agents tse laoloang tsa matlapa a tsoakiloeng a skeleton sustainable release le matlapa a hydrophilic gel skeleton sustainable release. Mohlala oa low-viscosity ke moemeli o bakang masoba bakeng sa matlapa a tokollo e tsitsitseng kapa a laoloang e le hore tekanyo ea pele ea phekolo ea matlapa a joalo e fumanoe kapele, e lateloe ke tokollo e tsitsitseng kapa e laoloang ho boloka mahloriso a sebetsang maling.
2.5. Gel le matrix ea suppository
Li-suppositories tsa hydrogel le litokisetso tsa sekhomaretsi sa mpa li ka lokisoa ka ho sebelisa tšobotsi ea ho thehoa ha hydrogel e sebelisoang haholo ke HPMC ka metsing.
2.6 Lisebelisoa tsa sekhomaretsi sa baeloji
Metronidazole e ne e kopantswe le HPMC le polycarboxylethylene 934 ka hara motswako ho etsa matlapa a tokollo a laolwang ke bioadhesive a nang le 250mg. Teko ya ho qhibiliha ha in vitro e bontshitse hore tokiso e ile ya kokomoha ka potlako ka metsing, mme tokollo ya moriana e ne e laolwa ke ho hasana le ho phomotsa ketane ya khabone. Ho kenngwa tshebetsong ha diphoofolo ho bontshitse hore sistimi e ntjha ya tokollo ya meriana e ne e na le thepa ya bohlokwa ya ho kgomarela ha diphoofolo ho mucosa ya molomo wa kgomo.
2.7, e le thuso ea ho emisoa
Ho teteana ho hoholo ha sehlahisoa sena ke thuso e ntle ea ho emisa bakeng sa litokisetso tsa mokelikeli oa ho emisa, tekanyo ea sona e tloaelehileng ke 0.5% ~ 1.5%.
4. Mehlala ea ts'ebeliso
4.1 Tharollo ea ho koahela filimi: HPMC 2kg, talc 2kg, oli ea castor 1000ml, Twain -80 1000ml, propylene glycol 1000ml, 95% ethanol 53000ml, metsi 47000ml, pigment e loketseng. Ho na le litsela tse peli tsa ho e etsa.
4.1.1 Ho lokisa mokelikeli o koahetsoeng ka pigment o qhibilihang: Kenya tekanyo e behiloeng ea HPMC ka har'a ethanol ea 95%, e inele bosiu bohle, qhala vector e 'ngoe ea pigment ka metsing (sefa haeba ho hlokahala), kopanya litharollo tse peli 'me u hlohle ka ho lekana ho etsa tharollo e bonaletsang. Kopanya 80% ea tharollo (20% bakeng sa ho bentša) le tekanyo e behiloeng ea oli ea castor, Tween-80, le propylene glycol.
4.1.2 Ho lokisoa ha mokelikeli o koahelang o sa qhibiliheng (joalo ka tšepe oxide) HPMC e ile ea kolobisoa ka har'a ethanol ea 95% bosiu bohle, 'me metsi a eketsoa ho etsa tharollo e bonaletsang ea 2% HPMC. 20% ea tharollo ena e ile ea ntšoa bakeng sa ho bentša, 'me tharollo e setseng ea 80% le oxide ea tšepe li ile tsa lokisoa ka mokhoa oa ho sila ka metsi, ebe bongata ba likarolo tse ling bo ile ba eketsoa 'me ba kopanngoa ka ho lekana bakeng sa tšebeliso. Mokhoa oa ho koahela mokelikeli o koahelang: tšela lakane ea lijo-thollo ka pitseng ea ho koahela tsoekere, kamora ho potoloha, moea o chesang o futhumatsa ho fihlela ho 45℃, o ka fafatsa ho koahela ho fepa, taolo ea phallo ka 10 ~ 15ml/min, kamora ho fafatsa, tsoela pele ho omella ka moea o chesang metsotso e 5 ~ 10 e ka tsoa ka pitseng, e behe ka har'a dryer ho omella nako e fetang lihora tse 8.
Lera la mahlo la 4.2α-interferon 50μg ea α-interferon e qhibilihisitsoe ka har'a hydrochloric acid ea 10ml0.01ml, e kopantsoe le ethanol ea 90ml le 0.5GHPMC, ea sefshoa, ea koaheloa thupeng ea khalase e potolohang, ea hloekisoa mochesong oa 60℃ 'me ea omisoa moeeng. Sehlahisoa sena se entsoe ka thepa ea filimi.
Matlapa a 4.3 a Cotrimoxazole (0.4g±0.08g) SMZ (80 letlooeng) 40kg, starch (120 letlooeng) 8kg, 3% HPMC aqueous solution 18-20kg, magnesium stearate 0.3kg, TMP (80 letlooeng) 8kg, mokhoa oa ho lokisa ke ho kopanya SMZ le TMP, ebe o eketsa starch ebe o kopanya metsotso e 5. Ka tharollo ea metsi ea 3% HPMC e entsoeng esale pele, thepa e bonolo, ka granulation ea skrine ea letlooeng e 16, ho omisa, ebe ka skrine ea letlooeng e 14 letlooeng le feletseng, eketsa motsoako oa magnesium stearate, ka 12mm circle ka matlapa a stamping a word (SMZco). Sehlahisoa sena se sebelisoa haholo e le binder. Ho qhibiliha ha matlapa e ne e le 96%/20min.
4.4 Matlapa a piperate (0.25g) piperate 80 letlooeng 25kg, starch (120 letlooeng) 2.1kg, magnesium stearate ka tekanyo e loketseng. Mokhoa oa eona oa tlhahiso ke ho kopanya pipeoperic acid, starch, HPMC ka ho lekana, ka thepa e bonolo ea ethanol ea 20%, granulate ea skrine ea letlooeng ea 16, e omileng, ebe e kenngoa ka letlooeng la letlooeng la 14, hammoho le vector magnesium stearate, ka matlapa a 100mm circular belt word (PPA0.25). Ka starch e le moemeli oa ho qhalana, sekhahla sa ho qhibiliha ha letlapa lena ha se ka tlase ho 80%/2min, e leng se phahameng ho feta lihlahisoa tse tšoanang Japane.
4.5 Ho taboha ha maiketsetso HPMC-4000, HPMC-4500 kapa HPMC-5000 0.3g, sodium chloride 0.45g, potassium chloride 0.37g, borax 0.19g, 10% ammonium chlorbenzylammonium solution 0.02ml, metsi a ekelitsoeng ho 100ml. Mokhoa oa eona oa tlhahiso ke HPMC e kenngoa ka metsing a 15ml, ka metsi a tletseng a 80 ~ 90℃ nka, eketsa metsi a 35ml, ebe u kenya likarolo tse setseng tsa tharollo ea metsi ea 40ml e tsoakiloeng ka ho lekana, eketsa metsi ho fihlela tekanyo e felletseng, ebe u kopanya ka ho lekana, ema bosiu bohle, tšela sefa ka bonolo, u sefa ka setshelong se koetsoeng, se hloekisoa ka 98 ~ 100℃ metsotso e 30, ke hore, pH e tloha ho 8.4 ° C ho isa ho 8.6 ° C. SEHLAHISOA sena SE SEBELISELOA BAKENG SA KHAEHO EA HO HLŌLA, KE SENTHO SE SETLE SA HO HLŌLA, HA SE SEBELISWA BAKENG SA microscopy ea kamore ea KA PELE, se ka eketsoa ka nepo. Tekanyo ea sehlahisoa sena, 0.7% ~ 1.5% e LOKILE.
Matlapa a 4.6 a tokollo e laoloang ke Meththorphan, letsoai la resin la meththorphan 187.5mg, lactose 40.0mg, PVP70.0mg, vapor silica 10mg, 40.0 mGHPMC-603, 40.0mg ~ microcrystalline cellulose phthalate-102 le magnesium stearate 2.5mg. E lokisitsoe e le matlapa ka mokhoa o tloaelehileng. Sehlahisoa sena se sebelisoa e le thepa e laoloang ea tokollo.
4.7 Bakeng sa matlapa a avantomycin ⅳ, 2149g a avantomycin ⅳ monohydrate le motsoako oa metsi oa isopropyl oa 15% (boima ba mahloriso) eudragitL-100 (9:1) li ile tsa hlohlelletsoa, tsa kopanngoa, tsa granulated, 'me tsa omisoa ka mocheso oa 35℃. Li-granule tse omisitsoeng tsa 575g le 62.5g hydroxypropylocellulose E-50 li ile tsa kopanngoa hantle, 'me ka mor'a moo 7.5g ea stearic acid le 3.25g ea magnesium stearate li ile tsa eketsoa matlapeng ho fumana tokollo e tsoelang pele ea matlapa a vanguard mycin ⅳ. Sehlahisoa sena se sebelisoa e le thepa ea ho lokolla butle.
4.8 Li-granule tsa Nifedipine tse lokollotsoeng ka nako e telele Karolo e le 'ngoe ea nifedipine, likarolo tse 3 tsa hydroxypropyl methyl cellulose le likarolo tse 3 tsa ethyl cellulose li ile tsa kopanngoa le solvent e tsoakiloeng (ethanol: methylene chloride = 1:1), 'me likarolo tse 8 tsa starch ea poone li ile tsa eketsoa ho hlahisa li-granule ka mokhoa o qhibilihang ka mokhoa o mahareng. Sekhahla sa ho lokolloa ha li-granule tsa lithethefatsi ha sea ka sa angoa ke phetoho ea pH ea tikoloho 'me se ne se lieha ho feta sa li-granule tse fumanehang khoebong. Kamora lihora tse 12 tsa ho nooa ka molomo, mahloriso a mali a motho e ne e le 12mg/ml, 'me ho ne ho se na phapang ea motho ka mong.
4.9 Khapsule e lokollang Propranhaol hydrochloride e tsitsitseng Propranhaol hydrochloride 60kg, microcrystalline cellulose 40kg, ho eketsoa metsi a 50L ho etsa di-granule. HPMC1kg le EC 9kg di ile tsa kopanngwa ka hara solvent e kopantsweng (methylene chloride: methanol =1:1) 200L ho etsa tharollo ya ho roala, ka sekgahla sa phallo sa 750ml/min hodima dikarolwana tse chitja tse pitikileng, dikarolwana tse kwahetsweng ka boholo ba pore ya dikarolwana tse feletseng tsa skrine ya 1.4mm, mme tsa tlatswa ka hara khapsule ya lejwe ka mochini o tlwaelehileng wa ho tlatsa khapsule. Khapsule ka nngwe e na le 160mg ya dikarolwana tse chitja tsa propranolol hydrochloride.
Matlapa a masapo a Naprolol HCL a 4.10 a lokisitsoe ka ho kopanya naprolol HCL :HPMC: CMC-NA ka karolelano ea 1:0.25:2.25. Sekhahla sa ho lokolloa ha moriana se ne se le haufi le ho odara ea lefela ka hare ho lihora tse 12.
Meriana e meng e ka boela ea etsoa ka thepa e tsoakiloeng ea masapo, joalo ka metoprolol: HPMC: CMC-NA ho latela: 1:1.25:1.25; Allylprolol:HPMC ho latela karolelano ea 1:2.8:2.92. Sekhahla sa ho lokolloa ha moriana se ne se le haufi le ho odara ea lefela ka hare ho lihora tse 12.
4.11 Matlapa a masapo a lintho tse tsoakiloeng tsa ethylaminosine derivatives a lokisitsoe ka mokhoa o tloaelehileng ho sebelisoa motsoako oa micro powder silica gel: CMC-NA :HPMC 1:0.7:4.4. Moriana o ka lokolloa lihora tse 12 ka bobeli ka vitro le ka vivo, 'me mokhoa oa ho lokolloa ka mola o ne o e-na le kamano e ntle. Liphetho tsa teko ea botsitso e potlakileng ho latela melao ea FDA li bolela esale pele hore bophelo ba polokelo ea sehlahisoa sena ke ho fihlela lilemo tse 2.
4.12 HPMC (50mPa·s) (likarolo tse 5), HPMC (4000 mPa·s) (likarolo tse 3) le HPC1 li qhibilihisitsoe likarolong tse 1000 tsa metsi, likarolo tse 60 tsa acetaminophen le likarolo tse 6 tsa silika gel li ile tsa eketsoa, tsa hlohlelletsoa ka homogenizer, 'me tsa omisoa ka spray. Sehlahisoa sena se na le 80% ea moriana o ka sehloohong.
4.13 Matlapa a masapo a gel a hydrophilic a Theophylline a baliloe ho latela boima bohle ba matlapa, 18%-35% theophylline, 7.5%-22.5% HPMC, 0.5% lactose, le setlolo se loketseng sa hydrophobic hangata li ne li lokisoa ka matlapa a tokollo a laoloang, a ka bolokang khatello e sebetsang ea mali 'meleng oa motho lihora tse 12 kamora ho nooa.
Nako ea poso: Hlakola-05-2024