Category: kupfeka zvinhu; Membrane material; Speed-inodzorwa polymer zvinhu zvekunonoka-kuburitsa gadziriro; Stabilizing agent; Kuturika rubatsiro, kunamatira piritsi; Yakasimbiswa adhesion agent.
1. Chigadzirwa sumo
Ichi CHIKAMU IS A NON-IONIC CELLULOSE ETHER, kunze inoonekwa sehupfu chena, isinganhuhwi uye isinganakidze, inonyungudika mumvura uye yakawanda polar organic solvents, kuzvimba mumvura inotonhora kujekesa kana zvishoma turBIdized colloidal solution. Mushonga wemvura une basa repamusoro, kujeka kwepamusoro uye kushanda kwakagadzikana. HPMC ine pfuma yejeri rinopisa. Mushure mekupisa, chigadzirwa chine aqueous solution inoumba gel precipitation, uye inonyunguduka mushure mekutonhora. Iyo tembiricha yegel yezvakasiyana zvakasiyana zvakasiyana. Solubility inoshanduka ne viscosity, viscosity zhao yakaderera, iyo yakanyanya kunyungudika, zvakasiyana-siyana zveHPMC zvivakwa zvine mimwe misiyano, HPMC yakanyungudika mumvura haina kukanganiswa ne pH kukosha.
Iyo tembiricha yekupisa inongoerekana yavapo, yakasununguka density, density yechokwadi uye tembiricha yegirazi yekuchinja yaive 360 ℃, 0.341g/cm3, 1.326g/cm3 uye 170 ~ 180 ℃, zvichiteerana. Mushure mekupisa, inoshanduka shava pa190 ~ 200 ° C uye inopisa pa225 ~ 230 ° C.
HPMC inenge isinganyungudike muchloroform, ethanol (95%), uye diethyl ether, uye yakanyungudutswa mumusanganiswa we ethanol uye methylene chloride, musanganiswa wemethanol uye methylene chloride, uye musanganiswa wemvura uye ethanol. Mamwe mazinga eHPMC anonyungudika mumisanganiswa yeacetone, methylene chloride, uye 2-propanol, pamwe chete mune mamwe organic solvents.
Tafura 1: Technical zviratidzo
project
Kuyera,
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
Gel tembiricha ℃
56-64.
62.0-68.0
70.0-90.0
Viscosity mpa s.
3,5,6,15,50,4000
50400 0
100400 0150 00100 000
Dry weight loss%
5.0 kana zvishoma
Kupisa kwasara%
1.5 kana zvishoma
pH
4.0-8.0
Heavy metal
20 zvichidzika
arsenic
2.0 kana zvishoma
2. Zvigadzirwa zvechigadzirwa
2.1 Hydroxypropyl methylcellulose inonyungudutswa mumvura inotonhora kuita viscous colloidal solution. Chero bedzi iyo yakawedzerwa kumvura inotonhora uye zvishoma inobvongodzwa, inogona kunyungudutswa mumhinduro yakajeka. Pane kudaro, haina kunyungudika mumvura inopisa pamusoro pe60 ℃ uye inogona kungozvimba. Mukugadzirira kwehydroxypropyl methiculose aqueous solution, zviri nani kuwedzera chikamu chehydroxypropyl methiccellulose mune imwe huwandu hwemvura, kubvongodza zvine simba, kupisa kusvika 80 ~ 90 ℃, uye wobva wawedzera yasara hydroxypropyl methiculose, uye pakupedzisira shandisa mvura inotonhora kuwedzera. kusvika pamari inodiwa.
2.2 Hydroxypropyl methylcellulose isiri-ionic cellulose ether, mhinduro yayo haitakuri ionic charge, haipindirani nesimbi yemunyu kana ionic organic compounds, kuitira kuti ive nechokwadi chokuti HPMC haiiti nezvimwe zvinhu zvakasvibirira uye zvinobatsira mukugadzirisa. production.
2.3 Hydroxypropyl methylcellulose ine simba rinopesana nekunzwa, uye nekuwedzera kwekutsiva dhigirii mukugadzirwa kwema molecular, anti-sensitivity inowedzerwawo. Mishonga inoshandisa HPMC sezvishandiso zvine hutsika hwakagadzikana mukati menguva inoshanda kupfuura zvinodhaka zvinoshandisa zvimwe zvechinyakare excipients (starch, dextrin, powdered sugar).
2.4 Hydroxypropyl methylcellulose ine metabolically inert. Semushonga wemishonga, haisi kushandiswa kwemasabolism kana kubatwa, saka haipi kupisa mumishonga uye zvokudya. Iyo ine yakasarudzika inoshanda kune yakaderera calorific kukosha, munyu-isina, isiri-allergenic zvinodhaka uye chikafu chevane chirwere cheshuga.
2.5HPMC haina kugadzikana kune maasidhi nemabhesi, asi kana pH ikadarika 2 ~ 11 uye ikakanganiswa netembiricha yepamusoro kana nguva yakareba yekuchengetedza, inoderedza dhigirii rekuibva.
2.6 Hydroxypropyl methylcellulose aqueous solution inogona kupa basa repamusoro, richiratidza mwero wepamusoro uye kupindirana kwehutano hwehutano. Iine emulsification inoshanda mune maviri-phase system uye inogona kushandiswa seyakasimba stabilizer uye inodzivirira colloid.
2.7 Hydroxypropyl methylcellulose aqueous solution ine yakanakisa kugadzira firimu zvinhu, uye yakanaka coating material yemapiritsi nemapiritsi. Iyo membrane inoumbwa nayo haina ruvara uye yakaoma. Kana glycerol yakawedzerwa, plastiki yayo inogona kuwedzerwa. Mushure mekurapwa kwepamusoro, chigadzirwa chinoparadzirwa mumvura inotonhora, uye chiyero chekunyungudika chinogona kudzorwa nekushandura pH nharaunda. Inoshandiswa mukunonoka-kusunungurwa kugadzirira uye enteric-coated kugadzirira.
3. Chigadzirwa chekushandisa
3.1. Inoshandiswa seanonamatira uye inoparadzanisa agent
HPMC inoshandiswa kusimudzira kuparara kwezvinodhaka uye dhigirii rekuburitsa zvikumbiro, inogona kunyungudika zvakananga mukunyungudika sekunamira, yakaderera viscosity yeHPMC yakanyungudika mumvura kuti iite pachena kune yenzou inonamira colloid mhinduro, mahwendefa, mapiritsi, granules pane adhesive uye disintegrated. mumiririri, uye iyo yakakwira viscosity yeglue, shandisa chete nekuda kwemhando dzakasiyana uye zvakasiyana zvinodiwa, general i2% ~ 5%.
HPMC aqueous solution uye imwe concentration ye ethanol kuita composite binder; Muenzaniso: 2% HPMC mvura yemushonga yakasanganiswa ne55% ethanol solution yakashandiswa kupeta macapsules eamoxicillin, kuitira kuti avhareji yekunyunguduka kweamoxicillin capsules iwedzere kubva pa38% kusvika 90% pasina HPMC.
HPMC inogona kugadzirwa necomposite adhesive ine dzakasiyana siyana ye starch slurry mushure mekuparara; Kunyungudutswa kwemapiritsi erythromycin ane enteric-coated kwakawedzera kubva pa38.26% kusvika pa97.38% pakasanganiswa 2% HPMC ne8% starch.
2.2. Gadzira firimu rekuvhara zvinhu uye firimu kugadzira zvinhu
HPMC semvura-soluble coating material ine zvinotevera maitiro: moderate solution viscosity; Nzira yekuputira iri nyore; Yakanaka firimu kugadzira pfuma; Inogona kuchengeta chimiro chechidimbu, kunyora; Inogona kunge isina unyoro; Inogona ruvara, kururamisa kunaka. Ichi chigadzirwa CHINOSHANDISA SEMVURA-SOLUBLE FILM Coating YEMATABETTE NEMAPIRITSI ANE YAkaderera VISCOSITY, UYE NEISINGAVE-MVURA-BASED FILM COATING INE VISCOSITY YAKURU, THE AMOUNT YEKUSHANDISA I2% -5%.
2.3, seyakakora mumiriri uye colloidal kudzivirira glue
HPMC inoshandiswa seyakakora mumiririri ndeye 0.45% ~ 1.0%, inogona kushandiswa semadonhwe emeso uye yekugadzira misodzi yekukora mumiriri; Inoshandiswa kuwedzera kugadzikana kwe hydrophobic glue, kudzivirira particle coalescence, kunaya, iyo yakajairika dosage ndeye 0.5% ~ 1.5%.
2.4, se blocker, inononoka kuburitsa zvinhu, inodzorwa kuburitsa mumiririri uye pore mumiriri
HPMC yakakwira viscosity modhi inoshandiswa kugadzirira zvivhariso uye inodzorwa kuburitsa ejenti yezvakasanganiswa zvinhu skeleton inosimudzira kuburitsa mahwendefa uye hydrophilic gel skeleton inosimudzira kuburitsa mahwendefa. Iyo yakaderera-viscosity modhi inhengo yepore-inducing agent yekugara-kuburitswa kana kudzorwa-kuburitswa mahwendefa kuitira kuti iyo yekutanga dhizaini yekurapa yemapiritsi akadaro inokurumidza kuwanikwa, inoteverwa nekugara-kuburitswa kana kudzorwa-kuburitswa kuchengetedza kunoshanda kwekuisa muropa.
2.5. Gel uye suppository matrix
Hydrogel suppositories uye gastric adhesive gadziriro inogona kugadzirwa nekushandisa hunhu hwe hydrogel kuumbwa kunowanzoshandiswa neHPMC mumvura.
2.6 Biological adhesive zvinhu
Metronidazole yakasanganiswa neHPMC uye polycarboxylethylene 934 mumusanganisi kuita bioadhesive controlled kuburitsa mapiritsi ane 250mg. In vitro dissolution test yakaratidza kuti gadziriro yacho yakakurumidza kuzvimba mumvura, uye kuburitswa kwemushonga kwaidzorwa nekupararira uye kuzorora kweketani. Kuitwa kwemhuka kwakaratidza kuti iyo nyowani yekuburitsa zvinodhaka yaive yakakosha biological adhesion zvivakwa kune bovine sublingual mucosa.
2.7, serubatsiro rwekumiswa
Iyo HIGH viscosity yechigadzirwa ichi yakanaka kumisa rubatsiro rwekumisa gadziriro yemvura, iyo yakajairika dosage ndeye 0.5% ~ 1.5%.
4. Mienzaniso yekushandisa
4.1 Film coating solution: HPMC 2kg, talc 2kg, castor oil 1000ml, Twain -80 1000ml, propylene glycol 1000ml, 95% ethanol 53000ml, mvura 47000ml, pigment yakakodzera mari. Pane nzira mbiri dzekuita.
4.1.1 Gadziriro yekunyungudika pigment yakavharidzirwa mvura yembatya: Wedzera huwandu hwakatarwa hweHPMC mu95% ethanol, inyudze husiku hwose, nyungudutsa imwe pigment vector mumvura (sefa kana zvichidikanwa), batanidza mhinduro mbiri uye kurunga zvakaenzana kugadzira mhinduro inoonekera. . Sanganisa 80% yemhinduro (20% yekupukuta) nehuwandu hwakatarwa hwemafuta emukisi, Tween-80, uye propylene glycol.
4.1.2 Kugadzirira kweinsoluble pigment (yakadai se iron oxide) yekuputira mvura HPMC yakanyoroveswa mu95% ethanol usiku humwe, uye mvura yakawedzerwa kuita 2% HPMC sarudzo yakajeka. 20% yemhinduro iyi yakatorwa kuti icheneswe, uye yakasara 80% mhinduro uye iron oxide zvakagadzirirwa nenzira yemvura yekukuya, uyezve huwandu hwemishonga yezvimwe zvikamu zvakawedzerwa uye zvakasanganiswa zvakaenzana kuti zvishandiswe. Nzira yekuputira yemvura yekuputira: dururira pepa rezviyo muhari yeshuga, mushure mekutenderera, mweya unopisa unopisa kusvika 45 ℃, unogona kupfapfaidza chikafu chekufuka, kuyerera kuyerera mu10 ~ 15ml / min, mushure mekupfapfaidza, ramba uchioma. nemhepo inopisa ye5 ~ 10min inogona kunge iri kunze kwehari, isa muomesi kuti iome kweanopfuura 8h.
4.2α-interferon eye membrane 50μg ye α-interferon yakanyungudutswa mu 10ml0.01ml hydrochloric acid, yakavhenganiswa ne 90ml ethanol uye 0.5GHPMC, yakasvibiswa, yakaputirwa pane girazi rinotenderera tsvimbo, yakasvibiswa pa60 ℃ uye yakaomeswa mumhepo. Ichi chigadzirwa chinogadzirwa kuita firimu zvinhu.
4.3 Cotrimoxazole mapiritsi (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 ndeye sanganisa SMZ neTMP, wobva wawedzera starch wosanganisa kwemaminitsi mashanu. Iine prefabricated 3% HPMC aqueous solution, soft material, ine 16 mesh screen granulation, kuomesa, uyezve ine gumi nemana mesh screen tsanga yakazara, wedzera magnesium stearate musanganiswa, ine 12mm kutenderera nezwi (SMZco) mahwendefa ekudhinda. Ichi chigadzirwa chinonyanya kushandiswa sebhainda. Kuparara kwemapiritsi kwaiva 96%/20min.
4.4 Piperate mapiritsi (0.25g) piperate 80 mesh 25kg, starch (120 mesh) 2.1kg, magnesium stearate yakafanira. Nzira yekugadzirwa kwayo ndeyekusanganisa pipeoric acid, starch, HPMC zvakaenzana, ine 20% ethanol soft material, 16 mesh screen granulate, yakaoma, uyezve gumi nemana mesh screen zviyo zvese, plus vector magnesium stearate, ine 100mm denderedzwa bhandi izwi (PPA0.25) ) stamping mapiritsi. Ne starch sechinhu chinoparadza, chiyero chekuparara kwehwendefa iyi haisi pasi pe80% / 2min, iyo yakakwirira kudarika zvigadzirwa zvakafanana muJapan.
4.5 Artificial tear HPMC-4000, HPMC-4500 kana HPMC-5000 0.3g, sodium chloride 0.45g, potassium chloride 0.37g, borax 0.19g, 10% ammonium chlorbenzylammonium solution 0ml2 toml2 mvura. Nzira yekugadzirwa kwayo ndeye HPMC yakaiswa mumvura 15ml, pa80 ~ 90 ℃ mvura izere tora, wedzera 35ml mvura, uyezve ine zvikamu zvakasara zve 40ml aqueous solution yakasanganiswa zvakaenzana, wedzera mvura kuhuwandu hwakazara, wozosanganiswa zvakaenzana, mira usiku hwose. , zvinyoro nyoro dururira kusefa, kusefa mumudziyo wakavharwa, wakavharwa pa98 ~ 100 ℃ kwe30min, kureva kuti, pH inotangira pa8.4 ° C kusvika pa8.6 ° C. CHIKAMU ichi CHINOSHANDISWA KUTI KUSHAIKWA KWEMISODZI, INOTSIVA YAKANAKA YEMISODZI, KANA ikashandiswa KUTI ANTERIOR chamber microscopy, inogona KUWEDZERA ZVAKAFANIRA MHOMO YECHIBIKO ichi, 0.7% ~ 1.5% INOFANIRA.
4.6 Meththorphan inodzorwa kusunungurwa mapiritsi meththorphan resin munyu 187.5mg, lactose 40.0mg, PVP70.0mg, vapor silica 10mg, 40.0 mGHPMC-603, 40.0mg ~ microcrystalline cellulose phthalate-102 uye magnesium stemga.2 Inogadzirirwa semapiritsi nenzira yakajairika. Ichi chigadzirwa chinoshandiswa seyakadzorwa kuburitsa zvinhu.
4.7 Pamapiritsi avantomycin ⅳ, 2149g avantomycin ⅳ monohydrate uye 1000ml isopropyl mvura musanganiswa we15% (mass concentration) eudragitL-100 (9:1) yakamutswa, yakasanganiswa, granulated, uye yakaomeswa pa35 ℃. Iwo akaomeswa granules 575g uye 62.5g hydroxypropylocellulose E-50 akanyatso kusanganiswa, uye ipapo 7.5g stearic acid uye 3.25g magnesium stearate akawedzerwa kumapiritsi kuti awane kuenderera kuburitswa kwanguard mycin ⅳ mapiritsi. Ichi chigadzirwa chinoshandiswa sechinononoka kuburitsa zvinhu.
4.8 Nifedipine inosimudzira-kusunungurwa granules 1 chikamu nifedipine, 3 zvikamu hydroxypropyl methyl cellulose uye 3 zvikamu ethyl cellulose zvakasanganiswa nemusanganiswa solvent (ethanol: methylene chloride = 1: 1), uye 8 zvikamu zvechibage starch yakawedzerwa kuti ibudise granules ne-medium-soluble. nzira. Mutengo wekuburitswa kwemushonga wemagranules hauna kukanganiswa neshanduko yezvakatipoteredza pH uye wainonoka kupfuura iwo weiyo inotengeswa granules. Mushure memaawa e12 ekutonga kwemuromo, huwandu hweropa revanhu hwakanga huri 12mg / ml, uye pakanga pasina mutsauko wega wega.
4.9 Propranhaol hydrochloride inosimudzira kuburitsa capsule Propranhaol hydrochloride 60kg, microcrystalline cellulose 40kg, ichiwedzera 50L mvura kugadzira granules. HPMC1kg uye EC 9kg zvakasanganiswa mumusanganiswa we solvent (methylene chloride: methanol = 1: 1) 200L kugadzira mhinduro yekuputira, ine kuyerera kwe750ml/min pfapfaidzo pazvimedu zvinotenderera, zvakavharwa zvimedu kuburikidza nehukuru hwepore hwe1.4 mm chidzitiro chakazara zvimedu, uye wobva wazadzwa mukati medombo capsule ine yakajairwa capsule yekuzadza muchina. Imwe neimwe capsule ine 160mg yepropranolol hydrochloride spherical particles.
4.10 Naprolol HCL skeleton mapiritsi akagadzirwa nekusanganisa naprolol HCL :HPMC: CMC-NA pachiyero che1:0.25:2.25. Mwero wekuburitswa kwezvinodhaka waive pedyo ne zero odha mukati memaawa gumi nemaviri.
Mimwe mishonga inogonawo kugadzirwa nezvinhu zvakasanganiswa skeleton, zvakadai semetoprolol: HPMC: CMC-NA maererano ne: 1: 1.25: 1.25; Allylprolol: HPMC maererano 1:2.8:2.92 chiyero. Mwero wekuburitswa kwezvinodhaka waive pedyo ne zero odha mukati memaawa gumi nemaviri.
4.11 Mahwendefa eSkeleton ezvigadzirwa zvakasanganiswa zve ethylaminosine derivatives akagadzirwa nenzira yakajairika achishandisa musanganiswa we micro powder silica gel: CMC-NA :HPMC 1: 0.7: 4.4. Mushonga waigona kuburitswa kwe12h zvese mu vitro uye mu vivo, uye mutsara wekuburitsa pateni yaive nekubatana kwakanaka. Mhedzisiro yekukasira kugadzikana bvunzo zvinoenderana neFDA mirau inofanotaura kuti kuchengetedza hupenyu hwechigadzirwa ichi hunosvika makore maviri.
4.12 HPMC (50mPa · s) (5 zvikamu), HPMC (4000 mPa·s) (3 zvikamu) uye HPC1 zvakanyungudutswa muzvikamu zve1000 zvemvura, 60 zvikamu zveacetaminophen uye 6 zvikamu silica gel zvakawedzerwa, zvakamutswa nehomogenizer, uye pfapfaidzo yakaoma. Ichi chigadzirwa chine 80% yemishonga huru.
4.13 Theophylline hydrophilic gel skeleton mahwendefa akaverengwa maererano nehuwandu hwepiritsi uremu, 18% -35% theophylline, 7.5% -22.5% HPMC, 0.5% lactose, uye chiyero chakakodzera che hydrophobic lubricant yaiwanzogadzirirwa mumapiritsi ekubudiswa akadzora. chengetedza kushanda kweropa kwemuviri wemunhu kwe12h mushure mekutonga nemuromo.
Nguva yekutumira: Feb-05-2024