Hydroxypropyl methylcellulose (HPMC)
Chikamu: zvinhu zvekufukidza; Zvinhu zveMembrane; Zvinhu zvepolymer zvinodzorwa nekukurumidza zvekugadzirira kuburitsa zvishoma nezvishoma; Chinhu chinosimbisa; Chinhu chinobatsira pakumisikidzwa, chinonamira papiritsi; Chinhu chinonamira chakasimbiswa.
1. Sumo yechigadzirwa
CHIGADZIRWA ichi iNON-IONIC CELLULOSE ETHER, inoonekwa kunze seupfu chena, isina hwema uye isina kuravira, inonyungudika mumvura uye yakawanda polar organic solvents, inozvimba mumvura inotonhora kusvika yachena kana kuti ine turBIdized colloidal solution zvishoma. Mhinduro yemvura ine basa repamusoro, yakajeka uye inoshanda zvakagadzikana. HPMC ine hunhu hwegel inopisa. Mushure mekudziya, mhinduro yemvura yemushonga inogadzira gel precipitation, uye yozonyungudika mushure mekutonhora. Tembiricha yegel yemhando dzakasiyana inosiyana. Kunyungudika kunochinja nekunyungudika, viscosity zhao yakaderera, kunyungudika kukuru, magadzirirwo akasiyana ehunhu hweHPMC ane misiyano yakati siyanei, HPMC inonyungudika mumvura haikanganisike ne pH value.
Tembiricha yekupisa inongoerekana yaitika, density yakakurisa, density chaiyo uye tembiricha yekuchinja kwegirazi yaive 360℃, 0.341g/cm3, 1.326g/cm3 uye 170 ~ 180℃, zvichiteerana. Mushure mekudziya, inoshanduka kuita brown pa190 ~ 200 ° C uye inotsva pa225 ~ 230 ° C.
HPMC hainyungudike mu chloroform, ethanol (95%), uye diethyl ether, uye inonyungudika mumusanganiswa we ethanol ne methylene chloride, musanganiswa we methanol ne methylene chloride, uye musanganiswa wemvura ne ethanol. Mamwe mazinga e HPMC anonyungudika mumusanganiswa we acetone, methylene chloride, uye 2-propanol, pamwe chete nezvimwe zvinonyungudutsa zve organic.
Tafura 1: Zviratidzo zvehunyanzvi
purojekiti
Chiyero,
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
Kupisa kwejeli ℃
56-64.
62.0-68.0
70.0-90.0
Kusimba kwe mpa s.
3, 5, 6, 15, 50, 4000
50400 0
100400 0150 00100 000
Kuderedza uremu kwakaoma %
5.0 kana pasi
Kupisa zvakasara %
1.5 kana pasi
pH
4.0-8.0
Simbi inorema
20 kana pasi
arsenic
2.0 kana pasi
2. Zvimiro zvechigadzirwa
2.1 Hydroxypropyl methylcellulose inonyungudutswa mumvura inotonhora kuti igadzire mhinduro ye colloidal ine viscous. Chero bedzi ikaiswa mumvura inotonhora yobva yakurungwa zvishoma, inogona kunyungudutswa kuita mhinduro yakajeka. Asi, hainyunguduke mumvura inopisa iri pamusoro pe60℃ uye inogona kuzvimba chete. Mukugadzirira mhinduro ye hydroxypropyl methicellulose yemvura, zvakanaka kuwedzera chikamu che hydroxypropyl methicellulose mumvura yakati, wokurunga nesimba, wopisa kusvika 80 ~ 90℃, wobva wawedzera hydroxypropyl methicellulose yasara, uye pakupedzisira shandisa mvura inotonhora kuwedzera huwandu hunodiwa.
2.2 Hydroxypropyl methylcellulose i-non-ionic cellulose ether, mhinduro yayo haina ionic charge, haisangani nesimbi munyu kana ionic organic compounds, kuitira kuti HPMC isasanganise nezvimwe zvinhu zvakagadziriswa uye zvinhu zvinobatsira mukugadzirwa kwemushonga.
2.3 Hydroxypropyl methylcellulose ine anti-sensitivity yakasimba, uye nekuwedzera kwedanho rekutsiva muchimiro chemamorekuru, anti-sensitivity inowedzerawo. Mishonga inoshandisa HPMC sezvinhu zvinosanganisa ine mhando yakagadzikana mukati menguva inoshanda kupfuura mishonga inoshandisa zvimwe zvinhu zvechinyakare (starch, dextrin, powdered sugar).
2.4 Hydroxypropyl methylcellulose haina simba rekugadzirisa muviri. Semushonga unobatsira mukurapa, haigayiwi kana kunyudzwa, saka haipe kupisa mumishonga nechikafu. Inoshanda zvakasiyana nemishonga ine simba shoma remacalorie, isina munyu, isingakonzere allergies uye chikafu chevanhu vane chirwere cheshuga.
2.5HPMC inogara kwenguva refu kune acids nemabases, asi kana pH ikadarika 2 ~ 11 uye ikakanganiswa nekupisa kwakanyanya kana nguva yakareba yekuchengetedza, inoderedza kuibva kwemuti.
2.6 Hydroxypropyl methylcellulose mvura inogona kupa basa repamusoro, ichiratidza kusimba kwepakati pepamusoro uye pakati pezvinhu. Ine emulsification inoshanda muhurongwa hwezvikamu zviviri uye inogona kushandiswa se stabilizer inoshanda uye colloid inodzivirira.
2.7 Hydroxypropyl methylcellulose mvura ine hunhu hwakanaka hwekuumba firimu, uye chinhu chakanaka chekufukidza mapiritsi nemapiritsi. Kamudzira kanoumbwa nako hakaoneki uye kakasimba. Kana glycerol ikawedzerwa, plasticity yayo inogona kuwedzerwa. Mushure mekugadzirisa pamusoro, chigadzirwa chinoparadzirwa mumvura inotonhora, uye mwero wekunyungudika unogona kudzorwa nekuchinja pH. Inoshandiswa mukugadzirira kunononoka uye mukugadzirira kwakavharwa ne enteric.
3. Kushandiswa kwechigadzirwa
3.1. Inoshandiswa sechinonamira uye chinoparara
HPMC inoshandiswa kukurudzira kunyungudika kwemushonga uye mwero wekuburitswa kwemushonga, inogona kunyungudika zvakananga mumushonga semushonga unonamira, HPMC yakanyungudika zvishoma mumvura kuti iite mhinduro inoonekera ye colloid inonamira yeivory, mapiritsi, mapiritsi, granules pane chinonamira uye chinoparara, uye glue yakakora, inoshandiswa chete nekuda kwemhando dzakasiyana uye zvinodiwa zvakasiyana, huwandu hwese huri 2% ~ 5%.
Mhinduro yemvura yeHPMC uye huwandu hwakati hweethanol kugadzira chinhu chinosanganisa zvinhu zvakasiyana; Muenzaniso: Mhinduro yemvura ye2%HPMC yakasanganiswa ne55% ethanol solution yakashandiswa pakuputira amoxicillin capsules, zvekuti avhareji yekunyungudika kwemacapsules eamoxicillin yakawedzera kubva pa38% kusvika 90% pasina HPMC.
HPMC inogona kugadzirwa nechinamira chakagadzirwa nestarch slurry yakasiyana mushure mekunyungudika; Kunyungudika kwemapiritsi ane erythromycin enteric-coated kwakawedzera kubva pa38.26% kusvika pa97.38% apo 2% HPMC ne8% starch zvakasanganiswa.
2.2. Gadzira zvinhu zvekufukidza firimu nezvinhu zvinogadzira firimu
HPMC sechipfeko chinonyungudika mumvura chine hunhu hunotevera: kupenya kwemvura kuri pakati nepakati; Maitiro ekuputira ari nyore; Hunhu hwakanaka hwekugadzira firimu; Inogona kuchengetedza chimiro chechigadzirwa, ichinyora; Inogona kudzivirira hunyoro; Inogona kuisa ruvara, uye inonaka. CHIGADZIRWA ichi CHINOSHANDISWA SEKUVHARA FILM INONYUNGURWA NEMVURA KUMAPIRITSI NEMAPIRITSI ANE KUSVIKA, UYE KUNE KUVHARA FILM IRI KUSINA MVURA INE KUSVIKA KWAKAWANDA, MARI YEKUSHANDISA I2%-5%.
2.3, semushonga wekukora uye seglue rekudzivirira colloidal
HPMC inoshandiswa semushonga wekukora ndeye 0.45% ~ 1.0%, inogona kushandiswa semadonhwe emaziso uye mushonga wekukora wemisodzi wekugadzira; Inoshandiswa kuwedzera kugadzikana kweglue rinonyungudika mumvura, kudzivirira kubatana kwezvikamu, mvura inonaya, chiyero chenguva dzose ndeche 0.5% ~ 1.5%.
2.4, semudziviriri, chinhu chinoburitsa zvinhu zvishoma nezvishoma, chinhu chinodzorwa chinoburitsa zvinhu uye chinhu chinodzivirira maburi
Modhi yeHPMC high viscosity inoshandiswa kugadzira ma blockers uye ma controlled release agents ema mixed material skeleton sustainable release tablets uye hydrophilic gel skeleton sustainable release tablets. Modhi ye low-viscosity imushonga unokonzera maburi emapiritsi anosunungurwa kwenguva refu kana anodzorwa kuitira kuti mushonga wekutanga wemapiritsi akadaro uwane nekukurumidza, uchiteverwa nekusunungurwa kwenguva refu kana kudzorwa kwenguva refu kuti urambe uine huwandu hwakanaka muropa.
2.5. Gel uye suppository matrix
Mishonga inonamira hydrogel uye mishonga inonamira mudumbu inogona kugadzirwa uchishandisa hunhu hwekugadzirwa kwehydrogel inowanzoshandiswa neHPMC mumvura.
2.6 Zvinhu zvinonamira zvehupenyu
Metronidazole yakasanganiswa neHPMC nepolycarboxylethylene 934 mumuchina wekusanganisa kuti igadzire mapiritsi anonamira ane 250mg. Kuongororwa kwekunyungudika kwemushonga we in vitro kwakaratidza kuti mushonga uyu wakakurumidza kuzvimba mumvura, uye kuburitswa kwemushonga uyu kwakadzorwa nekupararira uye kudzoreredzwa kwekabhoni. Kushandiswa kwemushonga uyu kwakaratidza kuti nzira itsva yekuburitsa mushonga uyu yaive nehunyanzvi hwakakura hwekunamatira kumuromo wemombe.
2.7, semubatsiri wekumisa
Kusimba kwakanyanya kwechigadzirwa ichi inzira yakanaka yekubatsira pakumisikidza kumiswa kwemvura, chiyero chayo chenguva dzose i0.5% ~ 1.5%.
4. Mienzaniso yekushandisa
4.1 Mushonga wekufukidza firimu: HPMC 2kg, talc 2kg, mafuta emushonga wecastor 1000ml, Twain -80 1000ml, propylene glycol 1000ml, 95% ethanol 53000ml, mvura 47000ml, huwandu hwakakodzera hwepigment. Pane nzira mbiri dzekugadzira.
4.1.1 Kugadzirwa kwemvura inonyungudika yakaputirwa nependi yakanyungudika: Wedzera huwandu hwakatarwa hweHPMC mu95% ethanol, inyike husiku hwese, nyungudutsa imwe pigment vector mumvura (sefa kana zvichidikanwa), sanganisa mhinduro mbiri idzi wobva wasanganisa zvakaenzana kuti ugadzire mhinduro yakajeka. Sanganisa 80% yemhinduro (20% yekupukuta) nehuwandu hwakatarwa hwemafuta emushonga, Tween-80, uye propylene glycol.
4.1.2 Kugadzirwa kwepigment isinganyungudike (yakadai se iron oxide) coating liquid HPMC yakanyikwa mu95% ethanol husiku hwese, uye mvura yakawedzerwa kuti 2% HPMC iite 20% HPMC content translucent. 20% yemhinduro iyi yakatorwa kuti iporishwe, uye yasara 80% solution ne iron oxide zvakagadzirwa nenzira yekukuya, uye huwandu hwezvimwe zvikamu zvakanyorerwa zvakaiswa uye zvakasanganiswa zvakaenzana kuti zvishandiswe. Maitiro ekuputira e coating liquid: dururira pepa rezviyo mupoto yekuputira shuga, mushure mekutenderera, mhepo inopisa inopisa kusvika 45℃, unogona kupfapfaidza feeding coating, flow control mu10 ~ 15ml/min, mushure mekupfapfaidza, ramba uchiomesa nemhepo inopisa kwe5 ~ 10min inogona kubuda mupoto, isa mu dryer kuti iome kweanopfuura maawa masere.
Kamudzira kemaziso ke4.2α-interferon 50μg yeα-interferon yakanyungudutswa mu10ml0.01ml hydrochloric acid, yakasanganiswa ne90ml ethanol ne0.5GHPMC, yakasefetwa, yakafukidzwa negirazi rinotenderera, yakacheneswa pa60℃ uye yakaomeswa mumhepo. Chigadzirwa ichi chakagadzirwa kuita firimu.
4.3 Mapiritsi eCotrimoxazole (0.4g±0.08g) SMZ (80 mesh) 40kg, starch (120 mesh) 8kg, 3%HPMC aqueous solution 18-20kg, magnesium stearate 0.3kg, TMP (80 mesh) 8kg, nzira yekugadzirira ndeyekusanganisa SMZ neTMP, wobva wawedzera starch wosanganisa kwemaminitsi mashanu. Ne 3%HPMC aqueous solution yakagadzirwa kare, zvinhu zvakapfava, ne 16 mesh screen granulation, kuomesa, uye wobva waisa 14 mesh screen whole grain, wedzera magnesium stearate mix, ne 12mm round ne word (SMZco) stamping tablets. Chigadzirwa ichi chinonyanya kushandiswa se binder. Kunyungudika kwemapiritsi kwaive 96%/20min.
4.4 Mapiritsi ePiperate (0.25g) piperate 80 mesh 25kg, starch (120 mesh) 2.1kg, magnesium stearate huwandu hwakakodzera. Nzira yayo yekugadzira ndeyekusanganisa pipeoperic acid, starch, HPMC zvakaenzana, ne20% ethanol soft material, 16 mesh screen granulate, yakaoma, uye wobva waisa 14 mesh screen whole grain, pamwe nevector magnesium stearate, ne100mm circular belt word (PPA0.25) stamping tablets. Nestarch semushonga wekupwanyika, mwero wekunyungudika kwepiritsi iri hausi pasi pe80%/2min, iyo iri pamusoro pezvigadzirwa zvakafanana muJapan.
4.5 Kubvarura kwekugadzira HPMC-4000, HPMC-4500 kana HPMC-5000 0.3g, sodium chloride 0.45g, potassium chloride 0.37g, borax 0.19g, 10% ammonium chlorbenzylammonium solution 0.02ml, mvura yakawedzerwa ku100ml. Nzira yayo yekugadzira ndeye HPMC yakaiswa mumvura ine 15ml, pa 80 ~ 90℃ mvura yakazara tora, wedzera 35ml yemvura, wozoisa zvimwe zvikamu zve 40ml yemvura zvakasanganiswa zvakaenzana, wedzera mvura kusvika pahuwandu hwakazara, wozoisanganisa zvakaenzana, mira husiku hwese, dururira zvinyoro nyoro, svina mumudziyo wakavharwa, wakacheneswa pa 98 ~ 100℃ kwemaminitsi makumi matatu, kureva kuti, pH iri pakati pe 8.4 ° C kusvika 8.6 ° C. Chigadzirwa ichi chinoshandiswa pakushomeka kwekubvaruka, chinotsiva kukuvara kwakanaka, kana chikashandiswa pa microscopy yekamuri repamberi, chinogona kuwedzerwa zvakakodzera. Chiyero cheChigadzirwa ichi, 0.7% ~ 1.5% chakakodzera.
4.6 Mapiritsi ekuburitsa meththorphan anodzorwa neresin munyu wemeththorphan resin 187.5mg, lactose 40.0mg, PVP70.0mg, vapor silica 10mg, 40.0 mGHPMC-603, 40.0mg ~ microcrystalline cellulose phthalate-102 uye magnesium stearate 2.5mg. Inogadzirwa semapiritsi nenzira yakajairika. Chigadzirwa ichi chinoshandiswa sechinhu chinodzorwa neresolution.
4.7 Pamapiritsi eavantomycin ⅳ, 2149g yeavantomycin ⅳ monohydrate nemusanganiswa wemvura we1000ml yeisopropyl we15% (mass concentration) eudragitL-100 (9:1) zvakasanganiswa, zvakasanganiswa, zvakapwanywa, uye zvakaomeswa pa35℃. Magranules akaomeswa e575g ne62.5g ehydroxypropylocellulose E-50 akasanganiswa zvakanaka, uye ipapo 7.5g yestearic acid ne3.25g yemagnesium stearate zvakaiswa pamapiritsi kuti mapiritsi anguard mycin ⅳ abude nguva dzose. Chigadzirwa ichi chinoshandiswa sechinhu chinononoka kuburitsa.
4.8 Nifedipine granules dzakasunungurwa kwenguva refu: chikamu chimwe chenifedipine, zvikamu zvitatu zvehydroxypropyl methyl cellulose uye zvikamu zvitatu zveethyl cellulose zvakasanganiswa ne mixed solvent (ethanol: methylene chloride = 1:1), uye zvikamu zvisere zve corn starch zvakawedzerwa kuti zvigadzire granules nenzira inonyunguduka pakati nepakati. Mwero wekuburitswa kwemishonga yegranules hauna kukanganiswa nekuchinja kwe pH yenharaunda uye wainonoka kupfuura wegranules dzaiwanikwa kutengeswa. Mushure memaawa gumi nemaviri ekushandiswa nemuromo, huwandu hweropa remunhu hwaive 12mg/ml, uye pakanga pasina musiyano wega wega.
4.9 Propranhaol hydrochloride sustainable release capsule Propranhaol hydrochloride 60kg, microcrystalline cellulose 40kg, kuwedzera 50L mvura kugadzira granules. HPMC1kg neEC 9kg zvakasanganiswa mumusanganiswa we solvent (methylene chloride: methanol =1:1) 200L kugadzira coating solution, ine flow rate ye 750ml/min spray pa rolling spreads, yakaputirwa nepakati pe pore size ye 1.4mm screen whole particles, uye yakazadzwa mu stone capsule nemuchina we ordinary capsule filling. Capsule yega yega ine 160mg ye propranolol hydrochloride spherical particles.
Mapiritsi eNaprolol HCL 4.10 akagadziriswa nekusanganisa naprolol HCL :HPMC: CMC-NA pachiyero che1:0.25:2.25. Mwero wekuburitswa kwemushonga waive pedyo ne zero mukati memaawa gumi nemaviri.
Mimwe mishonga inogonawo kugadzirwa nezvinhu zvakasanganiswa zvemapfupa, zvakaita semetoprolol: HPMC: CMC-NA zvichienderana ne: 1:1.25:1.25; Allylprolol:HPMC zvichienderana ne1:2.8:2.92 ratio. Mwero wekuburitswa kwemushonga waive pedyo ne zero order mukati memaawa gumi nemaviri.
4.11 Mapiritsi emapfupa emhando dzakasiyana dze ethylaminosine derivatives akagadzirwa nenzira yakajairika achishandisa musanganiswa we micro powder silica gel: CMC-NA :HPMC 1:0.7:4.4. Mushonga uyu unogona kuburitswa kwemaawa gumi nemaviri mu vitro nemu vivo, uye linear release pattern yaive nehukama hwakanaka. Mhedzisiro yebvunzo yekugadzikana yakakurumidza maererano nemitemo yeFDA inofanotaura kuti hupenyu hwekuchengetwa kwechigadzirwa ichi hunosvika makore maviri.
4.12 HPMC (50mPa·s) (zvikamu zvishanu), HPMC (4000 mPa·s) (zvikamu zvitatu) uye HPC1 zvakanyungudutswa muzvikamu chiuru zvemvura, zvikamu makumi matanhatu zveacetaminophen uye zvikamu zvitanhatu zvesilica gel zvakawedzerwa, zvakasanganiswa nehomogenizer, uye zvakapfapfaidzwa. Chigadzirwa ichi chine 80% yemushonga mukuru.
4.13 Mapiritsi eTheophylline hydrophilic gel skeleton akaverengerwa zvichienderana nehuremu hwepiritsi rose, 18%-35% theophylline, 7.5%-22.5% HPMC, 0.5% lactose, uye huwandu hwakakodzera hwemafuta anonyungudutsa mvura aiwanzogadzirwa mumapiritsi anoburitswa anodzora, ayo aigona kuchengetedza huwandu hweropa remuviri wemunhu kwemaawa gumi nemaviri mushure mekunwa.
Nguva yekutumira: Gunyana-20-2022