IHydroxypropyl methylcellulose (HPMC)
Udidi: izinto zokugquma; Izinto zeMembrane; Izixhobo zepolymer ezilawulwa ngokukhawuleza zamalungiselelo okukhululwa kancinci; I-arhente yokuzinzisa; Uncedo lokumiswa, ukuncamathelisa ithebhulethi; I-arhente yokubambelela eyomeleziweyo.
1. Ukwaziswa kwemveliso
Lo MVELISO YI-NON-IONIC CELLULOSE ETHER, ebonwa ngaphandle njengomgubo omhlophe, ongenavumba kunye nencasa, i-soluble emanzini kunye neyona nto ininzi ye-solvents ye-polar organic, ukuvuvukala emanzini abandayo ukucima okanye i-turBIdized solution ye-colloidal kancinane. Isisombululo samanzi sinomsebenzi ongaphezulu, ukukhanya okuphezulu kunye nokusebenza okuzinzileyo. I-HPMC inepropati yejeli eshushu. Emva kokufudumeza, isisombululo se-aqueous yemveliso senza i-gel precipitation, kwaye sinyibilike emva kokupholisa. Ubushushu bejeli beenkcukacha ezahlukeneyo buhlukile. Utshintsho lwe-Solubility kunye ne-viscosity, i-viscosity zhao ephantsi, i-solubility enkulu, i-solubility eyohlukeneyo yeepropati ze-HPMC inomahluko othile, i-HPMC enyibilikisiweyo emanzini ayichaphazeli ixabiso le-pH.
Ubushushu bokutsha obuzenzekelayo, ubuninzi obukhululekileyo, ubuninzi bokwenyani kunye nobushushu beglasi benguqu yayiyi-360℃, 0.341g/cm3, 1.326g/cm3 kunye ne-170 ~ 180℃, ngokulandelelanayo. Emva kokufudumeza, ijika ibemdaka kwi-190 ~ 200 ° C kwaye itshise kwi-225 ~ 230 ° C.
I-HPMC iphantse inganyibiliki kwi-chloroform, i-ethanol (i-95%), kunye ne-diethyl ether, kwaye inyibilika kumxube we-ethanol kunye ne-methylene chloride, umxube we-methanol kunye ne-methylene chloride, kunye nomxube wamanzi kunye ne-ethanol. Amanye amanqanaba e-HPMC anyibilika kwimixube ye-acetone, i-methylene chloride, kunye ne-2-propanol, kunye nakwezinye izinyibilikisi eziphilayo.
Itheyibhile 1: Izalathi zobugcisa
iprojekthi
Igeyiji,
60 gd (2910).
65GD(2906)
75GD(2208)
Indlela %
28.0-32.0
27.0-30.0
19.0-24.0
I-Hydroxypropoxy %
7.0-12.0
4.0-7.5
4.0-12.0
Ubushushu begel ℃
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
Ukwehla kobunzima %
5.0 okanye ngaphantsi
Ukutshisa intsalela %
1.5 okanye ngaphantsi
pH
4.0-8.0
Intsimbi enzima
20 okanye ngaphantsi
iarsenic
2.0 okanye ngaphantsi
2. Iimpawu zemveliso
2.1 I-Hydroxypropyl methylcellulose inyibilika emanzini abandayo ukwenza isisombululo se-viscous colloidal. Ngethuba nje ifakwe emanzini abandayo kwaye ixutywe kancinane, inokuchithwa kwisisombululo esicacileyo. Ngokuchasene noko, ayinyibiliki kumanzi ashushu ngaphezulu kwe-60 ℃ kwaye inokudumba kuphela. Ekulungiseleleni isisombululo se-hydroxypropyl methicellulose yamanzi, kungcono ukongeza inxalenye ye-hydroxypropyl methicellulose kumlinganiselo othile wamanzi, uvuselele ngamandla, ushushu ukuya kwi-80 ~ 90 ℃, uze udibanise i-hydroxypropyl methiculose eseleyo, kwaye ekugqibeleni usebenzise amanzi abandayo ukongeza. kwisixa esifunekayo.
I-2.2 I-Hydroxypropyl methylcellulose i-ether ye-cellulose engeyona i-ionic, isisombululo sayo asithwali i-ionic intlawulo, ayifuni ukusebenzisana neetyuwa zetsimbi okanye i-ionic organic compounds, ukwenzela ukuba kuqinisekiswe ukuba i-HPMC ayifuni kunye nezinye izinto eziphathekayo kunye nabancedisi kwinkqubo yokulungiselela. imveliso.
I-2.3 I-Hydroxypropyl methylcellulose ine-anti-sensitivity enamandla, kwaye ngokunyuka kwedigri yokutshintshwa kwi-molecular structure, i-anti-sensitivity nayo iphuculwe. Amachiza asebenzisa i-HPMC njengabancedisi banomgangatho ozinzile ngakumbi kwixesha elisebenzayo kunamachiza asebenzisa ezinye izinto zemveli (isitatshi, i-dextrin, iswekile engumgubo).
2.4 I-Hydroxypropyl methylcellulose i-inert ye-metabolically inert. Njengomxhasi wamachiza, ayinayo i-metabolized okanye ifakwe, ngoko ayinikeli ukushisa kumachiza kunye nokutya. Inokusebenza okuyingqayizivele kwixabiso eliphantsi le-calorific, ityuwa-free, iziyobisi ezingenayo i-allergenic kunye nokutya kwesifo seswekile.
I-2.5HPMC izinzile ngokwentelekiso kwiiasidi kunye neziseko, kodwa ukuba i-pH idlula i-2 ~ 11 kwaye ichatshazelwa bubushushu obuphezulu okanye ixesha elide lokugcina, iya kunciphisa iqondo lokuvuthwa.
I-2.6 I-Hydroxypropyl methylcellulose isisombululo se-aqueous inokubonelela ngomsebenzi ongaphezulu, obonisa umgangatho ophakathi kunye namaxabiso oxinzelelo lwe-interfacial. Ine-emulsification esebenzayo kwinkqubo yesigaba sesibini kwaye ingasetyenziselwa njenge-stabilizer esebenzayo kunye ne-colloid ekhuselayo.
I-2.7 I-Hydroxypropyl methylcellulose isisombululo se-aqueous sineempawu ezibalaseleyo zokwenza ifilimu, kwaye yinto efanelekileyo yokugqoka iipilisi kunye neepilisi. Inwebu eyenziwe yiyo ayinambala kwaye yomelele. Ukuba i-glycerol yongezwa, iplastiki yayo inokunyuswa. Emva kokunyanga kwendawo, imveliso ihlakazwa emanzini abandayo, kwaye izinga lokuchithwa lingalawulwa ngokutshintsha indawo ye-pH. Isetyenziswe kumalungiselelo okukhutshwa kancinci kunye namalungiselelo afakwe kwi-enteric.
3. Ukusetyenziswa kwemveliso
3.1. Isetyenziswe njenge-adhesive kunye ne-agent edibeneyo
I-HPMC isetyenziselwa ukukhuthaza ukuchithwa kweziyobisi kunye neqondo lokukhululwa kwezicelo, inokunyibilika ngokuthe ngqo kwi-solvent njenge-adhesive, i-viscosity ephantsi ye-HPMC enyibilikisiweyo emanzini ukwenza i-transparent kwisisombululo se-colloid esincangathi sendlovu, iipilisi, iipilisi, iigranules kwi-adhesive kunye nokwahlukana. I-arhente, kunye ne-viscosity ephezulu yeglue, sebenzisa kuphela ngenxa yodidi olwahlukileyo kunye neemfuno ezahlukeneyo, ngokubanzi yi-2% ~ 5%.
Isisombululo samanzi se-HPMC kunye noxinaniso oluthile lwe-ethanol ukwenza i-binder edibeneyo; Umzekelo: I-2% ye-HPMC yesisombululo samanzi esixutywe kunye ne-55% yesisombululo se-ethanol sasetyenziselwa i-pellets ye-amoxicillin capsules, ukwenzela ukuba ukuchithwa okuphakathi kwee-amoxicillin capsules kunyuke ukusuka kwi-38% ukuya kwi-90% ngaphandle kwe-HPMC.
I-HPMC inokwenziwa nge-adhesive edibeneyo kunye noxinaniso olwahlukileyo lwe-starch slurry emva kokuchithwa; Ukuchithwa kweepilisi ze-erythromycin ezine-enteric-coated tablets kunyuke ukusuka kwi-38.26% ukuya kwi-97.38% xa i-2% ye-HPMC kunye ne-8% yesitatshi ziye zadityaniswa.
2.2. Yenza izinto zokugquma ifilimu kunye nezinto zokwenza ifilimu
I-HPMC njengento yokwambathisa enyibilikayo emanzini inezi mpawu zilandelayo: i-viscosity yesisombululo esiphakathi; Inkqubo yokwaleka ilula; Ipropathi elungileyo yokwenza ifilimu; Uyakwazi ukugcina imilo yeqhekeza, ukubhala; Ingakhuseleka ukufuma; Ngaba umbala, ulungiso incasa. Le Mveliso isetyenziswa NJENGOKUGQIBELA IFILM OKUNXULEKILEYO AMANZI KWIITABLE NEEPILWESI EZINE-VISCOSITY EPHANTSI, KWAKUNYE NEFILIMU ENGENZIWA AMANZI NGE-VISCOSITY EPHAKAMILEYO, ISIXA SOKUSEBENZISA ISI-2% -5%.
2.3, njenge-ejenti yokuqina kunye neglue yokukhusela i-colloidal
I-HPMC esetyenziswa njenge-arhente yokutyebisa yi-0.45% ~ 1.0%, ingasetyenziswa njengamathontsi eliso kunye ne-artificial tea thickening agent; Isetyenziselwa ukunyusa ukuzinza kweglue ye-hydrophobic, ukukhusela i-particle coalescence, imvula, i-dosage eqhelekileyo yi-0.5% ~ 1.5%.
2.4, njenge-blocker, i-slow release material, i-ejenti yokukhululwa elawulwayo kunye ne-ejenti ye-pore
Imodeli ye-HPMC ephezulu ye-viscosity isetyenziselwa ukulungisa izithinteli kunye nee-agent ezilawulwayo zokukhululwa kwezinto ezixubeneyo zamathambo azinzileyo kunye neepilisi ze-hydrophilic gel skeleton ezizinzileyo. Imodeli ephantsi ye-viscosity yi-agent-inducing agent ye-pore-inducing-release-release-release-release-release tablets ukwenzela ukuba i-dose yokuqala yonyango yeepilisi ezinjalo ifunyenwe ngokukhawuleza, ilandelwa ukukhululwa okuqhubekayo okanye ukukhutshwa okulawulwayo ukuze kugcinwe ukugxila okusebenzayo kwigazi.
2.5. I-Gel kunye ne-suppository matrix
I-Hydrogel suppositories kunye ne-gastric adhesive preparations ingalungiswa ngokusebenzisa uphawu lokubunjwa kwe-hydrogel esetyenziswa ngokuqhelekileyo yi-HPMC emanzini.
2.6 Izinto ezincamathelayo zebhayoloji
I-Metronidazole yayixutywe kunye ne-HPMC kunye ne-polycarboxylethylene 934 kumxube ukwenza iipilisi zokukhululwa ezilawulwa yi-bioadhesive eziqukethe i-250mg. Uvavanyo lwe-in vitro dissolution lubonise ukuba ukulungiswa kwadumba ngokukhawuleza emanzini, kwaye ukukhutshwa kwechiza kwakulawulwa ngokusasazwa kunye nokuphumla kwe-carbon chain. Ukuphunyezwa kwezilwanyana kubonise ukuba inkqubo entsha yokukhupha ichiza ineempawu ezibalulekileyo zokunamathela kwi-bovine sublingual mucosa.
2.7, njengoncedo lokunqunyanyiswa
I-VIscosity EPHAKAMILEYO yale mveliso iluncedo lokumiswa kakuhle kumalungiselelo olwelo lokumiswa, umthamo wayo oqhelekileyo ngu-0.5% ~ 1.5%.
4. Imizekelo yokusetyenziswa
4.1 Film isisombululo ukutyabeka: HPMC 2kg, talc 2kg, castor oyile 1000ml, Twain -80 1000ml, propylene glycol 1000ml, 95% ethanol 53000ml, amanzi 47000ml, pigment imali efanelekileyo. Kukho iindlela ezimbini zokwenza.
4.1.1 Ukulungiswa kolwelo olunyibilikayo lwepigment egqunywe ngempahla: Yongeza inani elimiselweyo le-HPMC kwi-ethanol engama-95%, yicwilise ubusuku bonke, nyibilikise enye i-pigment vector emanzini (isihluzo ukuba kukho imfuneko), dibanisa izisombululo ezibini kwaye ushukumise ngokulinganayo ukwenza isisombululo esicacileyo. . Hlanganisa i-80% yesisombululo (i-20% yokupolisha) kunye nexabiso elimiselweyo leoli ye-castor, i-Tween-80, kunye ne-propylene glycol.
4.1.2 Ukulungiswa kwe-pigment enganyibilikiyo (efana ne-iron oxide) i-coating liquid HPMC ifakwe kwi-95% ye-ethanol ngobusuku, kwaye amanzi ongezwa ukwenza i-2% HPMC isisombululo esicacileyo. I-20% yesi sisombululo yathatyathelwa ukupolisha, kwaye isisombululo se-80% esiseleyo kunye ne-oxide yentsimbi zalungiswa ngendlela yolwelo lokusila, kwaye isixa somyalelo wezinye izinto zongezwa kwaye zixutywe ngokulinganayo ukuze zisetyenziswe. Inkqubo yokwaleka kolwelo lokugquma: galela iphepha lokutya okuziinkozo embizeni yokwaleka iswekile, emva kokujikeleza, umoya oshushu ushushu ukuya kuthi ga kwi-45 ℃, unokutshiza ukutya okutyayo, ukulawula ukuhamba nge-10 ~ 15ml/min, emva kokutshiza, qhubeka ukoma. kunye nomoya oshushu we-5 ~ 10min unokuba ngaphandle kwembiza, faka kwi-dryer ukuze yome ngaphezu kwe-8h.
I-4.2α-interferon i-membrane yamehlo i-50μg ye-α-interferon yachithwa kwi-10ml0.01ml i-hydrochloric acid, ixutywe ne-90ml ethanol kunye ne-0.5GHPMC, ihluziwe, ifakwe kwintonga yeglasi ejikelezayo, inzalo kwi-60 ℃ kwaye yomiswe emoyeni. Le mveliso yenziwe kwizinto zefilimu.
4.3 Amacwecwe eCotrimoxazole (0.4g±0.08g) SMZ (80 mesh) 40kg, istatshi (120 mesh) 8kg, 3%HPMC isisombululo samanzi 18-20kg, magnesium stearate 0.3kg, TMP (80 mesh) 8kg, indlela yokulungiselela kukuba xuba i-SMZ kunye ne-TMP, uze udibanise isitashi kwaye udibanise i-5min. Nge-prefabricated 3% HPMC isisombululo samanzi, izinto ezithambileyo, kunye ne-16 mesh screen granulation, ukomisa, kwaye emva koko kunye ne-14 mesh screen whole grain, yongeza umxube we-magnesium stearate, kunye ne-12mm ejikelezayo kunye negama (SMZco) iipilisi zokutywina. Le mveliso isetyenziswa ikakhulu njenge-binder. Ukuchithwa kweepilisi kwakuyi-96% / 20min.
4.4 Piperate tablets (0.25g) piperate 80 mesh 25kg, starch (120 mesh) 2.1kg, magnesium stearate isixa esifanelekileyo. Indlela yayo yokuvelisa kukuxuba i-pipeoperic acid, isitatshi, iHPMC ngokulinganayo, kunye ne-20% ye-ethanol ethambileyo yezinto, i-16 mesh screen granulate, eyomileyo, kwaye emva koko i-14 ye-mesh yesikrini esipheleleyo sengqolowa, kunye ne-vector magnesium stearate, ene-100mm yebhanti yesetyhula (PPA0.25) ) isitampu iipilisi. Nge-starch njenge-agent edibeneyo, izinga lokuchithwa kwale tablet alikho ngaphantsi kwe-80% / 2min, eliphakamileyo kuneemveliso ezifanayo eJapan.
4.5 Artificial tear HPMC-4000, HPMC-4500 okanye HPMC-5000 0.3g, sodium chloride 0.45g, potassium chloride 0.37g, borax 0.19g, 10% ammonium chlorbenzylammonium isisombululo 0.02ml. Indlela yayo yokuvelisa i-HPMC ibekwe kumanzi ayi-15ml, ku-80 ~ 90℃ amanzi agcweleyo athathe, yongeza amanzi angama-35ml, aze aqulathe amacandelo aseleyo e-40ml yesisombululo esinamanzi esixutywe ngokulinganayo, yongeza amanzi kwisixa esipheleleyo, emva koko ixutywe ngokulinganayo, yima ubusuku bonke. , uthele ngobunono ukuhluza, hluza kwisitya esitywiniweyo, sifakwe inzalo kwi-98 ~ 100℃ ye-30min, oko kukuthi, Uluhlu lwe-pH ukusuka kwi-8.4 ° C ukuya kwi-8.6 ° C. Le mveliso isetyenziselwa ukunqongophala kweenyembezi, IXESHA ELILUNGILEYO LOKUKHAMBA, XA KUSETYENZISWA I-microscopy ye-ANTERIOR yegumbi, INOKUNYUSWA NGOKUFANELEKILEYO UMGANGATHO WALE MVELISO, 0.7% ~ I-1.5% iFANELEKILE.
4.6 Meththorphan elawulwa ukukhululwa tablets meththorphan resin ityuwa 187.5mg, lactose 40.0mg, PVP70.0mg, umphunga silica 10mg, 40.0 mGHPMC-603, 40.0mg ~ microcrystalline cellulose phthalate-102 kunye ne-magnesium stemga.2 Ilungiswa njengeepilisi ngendlela eqhelekileyo. Le mveliso isetyenziswa njengento elawulwayo yokukhululwa.
4.7 Kwiipilisi ze-avantomycin ⅳ, i-2149g avantomycin ⅳ monohydrate kunye ne-1000ml isopropyl umxube wamanzi we-15% (i-mass concentration) i-eudragitL-100 (9: 1) yaxutywa, yaxutywa, yaxutywa, kwaye yomiswa kwi-35℃. I-granules eyomileyo i-575g kunye ne-62.5g i-hydroxypropylocellulose E-50 yayixutywe ngokucokisekileyo, kwaye emva koko i-7.5g ye-stearic acid kunye ne-3.25g ye-magnesium stearate yongezwa kwiipilisi ukuze kufumaneke ukukhululwa okuqhubekayo kwe-mineard mycin ⅳ tablets. Le mveliso isetyenziswa njengento yokukhulula kancinci.
I-4.8 I-Nifedipine i-granules ekhutshwe ngokuqhubekayo i-1 inxalenye ye-nifedipine, i-3 iinxalenye ze-hydroxypropyl methyl cellulose kunye ne-3 iindawo ze-ethyl cellulose zixutywe kunye ne-solvent exutywe (ethanol: i-methylene chloride = 1: 1), kunye ne-8 inxalenye ye-corn starch yongezwa ukuvelisa i-granules nge-medium-soluble. indlela. Izinga lokukhutshwa kweziyobisi kwi-granules alizange lichaphazeleke kutshintsho lwe-pH yokusingqongileyo kwaye lalicotha kunolo lweegranules ezifumanekayo zorhwebo. Emva kweeyure ze-12 zokulawulwa komlomo, ukuxinwa kwegazi lomntu kwakuyi-12mg / ml, kwaye kwakungekho mmahluko ngamnye.
I-4.9 I-Propranhaol hydrochloride eqhubekayo yokukhululwa kwe-capsule Propranhaol hydrochloride 60kg, i-microcrystalline cellulose 40kg, yongeza i-50L yamanzi ukwenza i-granules. I-HPMC1kg kunye ne-EC 9kg zixutywe kwi-solvent edibeneyo (i-methylene chloride: i-methanol = 1: 1) i-200L ukwenza isisombululo sokugquma, kunye nesantya sokuhamba kwe-750ml / min yokutshiza kwi-spherical particles, i-coated particles ngobukhulu be-pore ye-1.4 mm amasuntswana apheleleyo esikrini, kwaye emva koko yazaliswa kwi-capsule yamatye ngomatshini oqhelekileyo wokuzalisa i-capsule. I-capsule nganye iqulethe i-160mg yepropranolol hydrochloride spherical particles.
4.10 I-Naprolol HCL skeleton tablets zalungiswa ngokuxuba i-naprolol HCL :HPMC: CMC-NA kumlinganiselo we-1:0.25:2.25. Izinga lokukhutshwa kweziyobisi lalisondele kwi-odolo ye-zero kwiiyure ze-12.
Amanye amachiza anokwenziwa ngezinto ezixubeneyo zamathambo, njengemetoprolol: HPMC: CMC-NA ngokwe: 1:1.25:1.25; Allylprolol :HPMC ngokwe 1:2.8:2.92 ratio. Izinga lokukhutshwa kweziyobisi lalisondele kwi-odolo ye-zero kwiiyure ze-12.
I-4.11 Iipilisi ze-Skeleton zezinto ezixubileyo ze-ethylaminosine derivatives zalungiswa ngendlela eqhelekileyo ngokusebenzisa umxube we-micro powder silica gel: CMC-NA :HPMC 1: 0.7: 4.4. Ichiza linokukhululwa kwi-12h zombini kwi-vitro kunye ne-vivo, kwaye ipateni yokukhululwa ehambelanayo yayinonxibelelwano oluhle. Iziphumo zovavanyo olukhawulezayo lokuzinza ngokwemigaqo ye-FDA iqikelela ukuba ubomi bokugcinwa kwale mveliso bufikelela kwiminyaka emi-2.
I-4.12 HPMC (i-50mPa·s) (i-5 iinxalenye), i-HPMC (4000 mPa·s) (i-3 iinxalenye) kunye ne-HPC1 yachithwa kwiindawo ze-1000 zamanzi, i-60 iinxalenye ze-acetaminophen kunye ne-6 iinxalenye ze-silica gel zongezwa, zixutywe nge-homogenizer, kwaye isitshizi somisiwe. Le mveliso iqulethe i-80% yeyeza eliphambili.
I-4.13 i-Theophylline hydrophilic gel skeleton tablets ibalwe ngokwesisindo se-tablet esipheleleyo, i-18% -35% ye-theophylline, i-7.5% -22.5% ye-HPMC, i-0.5% ye-lactose, kunye nexabiso elifanelekileyo le-lubricant ye-hydrophobic yayidla ngokulungiswa kwiipilisi zokukhululwa ezilawulwayo. gcina uxinzelelo lwegazi olusebenzayo lomzimba womntu kwi-12h emva kokulawulwa komlomo.
Ixesha lokuposa: Sep-20-2022