Isigaba: Izinto zokuhlanganisa; Indwangu ye-membrane; Izinto ezisetshenziswayo ze-polymer ezilawulwa ngamalungiselelo wokukhulula kancane; Umenzeli wokuzinza; Usizo Lokumiswa, Ukunamathela Kwethebhulethi; I-agesion ejensi eqinisiwe.
1 Isingeniso Somkhiqizo
Lo mkhiqizo yi-ether ye-cellulose engeyona eye-ionic, ebonwa ngaphandle njenge-powder emhlophe, engenamzimba futhi engenamkhawulo, incibilika emanzini kanye namanzi apholile ukusula isixazululo se-colloidal. Isixazululo samanzi sinomsebenzi ongaphezulu, ukucaca okuphezulu nokusebenza okuzinzile. I-HPMC inempahla yejeli eshisayo. Ngemuva kokushisa, ikhambi lomkhiqizo elinamanzi amanzi liyakha imvula ye-gel, bese icwilisa ngemuva kokuphola. Izinga lokushisa le-gel lemininingwane ehlukile lihlukile. Ukushintshwa kwe-solubity nge-viscosity, i-viscuasity zhao ephansi, kukhudlwana i-solubity, imininingwane ehlukene yezakhiwo ze-HPMC inomehluko othile, i-HPMC ehlakazekile emanzini ayithintwa yinani le-PH.
Ukushisa okuzenzakalelayo kokushisa okuzenzakalelayo, ukushukunyiswa okuvumayo, ukulimala kweqiniso kanye nokushisa kwengilazi bekungama-360 ℃, 0.341G / CM3, 1.326G / CM3 no-170 ~ 180 ℃, ngokulandelana. Ngemuva kokushisa, kuphenduka nsundu ngo-190 ~ 200 ° C futhi kuvutha ngo-225 ~ 230 ° C.
I-HPMC icishe yangena ngaphakathi ku-chloroform, ethanol (95%), kanye ne-diethel ether, futhi incibilikisiwe emhlolweni we-ethanol ne-methylene chloride, i-methanol ne-methanol chlol, nengxube yamanzi ne-ethanol. Amanye amazinga we-HPMC ayanyibilika ekuxubeni i-acetone, i-methylene chloride, kanye ne-2-propapol, kanye nakwamanye ama-solvents ezi-organic.
Ithebula 1: Izinkomba zobuchwepheshe
umklamo
Gauge,
I-60 GD (2910).
I-65GD (2906)
I-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
I-Gel Temperature ℃
56-64.
62.0-68.0
70.0-90.0
I-Viscosity MPA s.
3,5,6,15,50,5000
50400 0
I-100400 0150 00100 000
Ukwehla kwesisindo esomile%
5.0 noma ngaphansi
I-Burning Residue%
1.5 noma ngaphansi
pH
4.0-8.0
Insimbi esindayo
20 noma ngaphansi
i-arsenic
2.0 noma ngaphansi
2. Izici zomkhiqizo
2.1 I-Hydroxypropyllylylyly ichithiwe emanzini abandayo ukwakha ikhambi le-colloidal ebonakalayo. Uma nje ingezwe emanzini abandayo futhi ivuswe kancane, ingachithwa kwikhambi elisobala. Ngokuphambene nalokho, ngokuyisisekelo kuncibilika emanzini ashisayo ngaphezulu kwama-60 ℃ futhi kungavuvukala kuphela. Ekulungiseleleni i-hydroxypropylllllylylylylyllose ikhambi lamanzi, kungcono ukwengeza ingxenye ye-hydroxypropylllylylylll ngenani elithile lamanzi, uvuse ngokuqinile, bese wengeza amanzi asele asele, bese wengeza amanzi abandayo ukwengeza kwinani elidingekayo.
2.2 hydroxypropyllylylyl i-ether ye-cellulose engekho, ikhambi layo ayiphathi ngemali ekhokhwayo ye-ionic, ayisebenzi ngosawoti wensimbi noma ama-onic arganic activations, ukuze iqinisekise ukuthi i-HPMC ayisebenzi nezinye izinto zokulungiselela ukukhiqiza.
2.3 I-Hydroxypropylllylylyl ine-anti-anti-sensitivity eqinile, futhi ngokwanda kokufakwa esikhundleni sesakhiwo samangqamuzana, ukuzwela okulwa nokulwa nakho kuyathuthukiswa. Izidakamizwa zisebenzisa i-HPMC njengoba ama-ExciPients anekhwalithi ezinzile esikhathini esisebenzayo kunezidakamizwa ezisebenzisa amanye ama-excipients (isitashi, i-dextrin, ushukela oluyimpuphu).
2.4 I-Hydroxypropyll methylcellulose i-metabolically indert. Njenge-Excipieint ye-Pharmaceutical, ayihlangene noma imunwe, ngakho-ke ayinikezi ukushisa ezidakamizweni nasekudla. Inokusebenza okuhlukile kwenani eliphansi le-calorific, izidakamizwa ezingenawo usawoti, ezingezona ze-allergenic nokudla kwabanesifo sikashukela.
I-2.5hpmc iqinile kuma-acid kanye nezisekelo, kepha uma i-PH idlula 2 ~ 11 futhi ithintwa ukushisa okuphezulu noma isikhathi eside sokugcina, kuzonciphisa izinga lokuvuthwa.
2.6 Ikhambi le-hydroxypropyllose linganikeza ikhambi elingaphezulu, elibonisa ingaphezulu elinganiselayo kanye namanani wokungezwani kwezingcingo. Ine-emulsation ephumelelayo kusistimu yesigaba ezimbili futhi ingasetshenziswa njenge-stabilizer esebenzayo ne-colloid evikelayo.
2.7 Isixazululo se-hydroxypropyllose i-methylcellulose sikhangise kahle izakhiwo ezakha amafilimu, futhi siyinto enhle yokuhlangana yamathebulethi namaphilisi. Ulwelwesi olusungulwe yilo alunamibala futhi lunzima. Uma kufakwa i-glycerol, ipulasitiki yayo ingandiswa. Ngemuva kokwelashwa komhlaba, umkhiqizo uhlakazeka emanzini abandayo, futhi izinga lokuchithwa lingalawulwa ngokushintsha imvelo ye-PH. Isetshenziswa kumalungiselelo wokukhulula kancane kanye namalungiselelo afakiwe angenayo.
3. Isicelo somkhiqizo
3.1. Isetshenziswa njenge-ejenti yokunamathela futhi ehlakazayo
I-HPMC isetshenziselwa ukukhuthaza ukubizelwa kwezidakamizwa kanye nezinga lezicelo zokukhishwa, kungachithwa ngokuqondile ku-solvive, ukubonakala okuphansi kwe-HPMC kuncibilikisiwe ngamanzi ukuze kuthathwe soludi onobala kakhulu ku-Iphory Sticky Colloid, amaphilisi, amaphilisi, amagremu ekunamathelayo nokuqhekeka Umenzeli, nokuvunywa okuphezulu kwe-glue, sebenzisa kuphela ngenxa yohlobo oluhlukile nezidingo ezihlukile, okujwayelekile kungu-2% ~ 5%.
Ikhambi le-HPMC elinamanzi kanye nokuhluzwa okuthile kwe-ethanol ukwenza i-binder composite; Isibonelo: 2% HPMC Aqualid Isixazululo esixutshwe nesixazululo esingama-55% e-Ethanol sasisetshenziselwa i-pelleting of amoxicillin caplules, ukuze ukuhlukaniswa okuphakathi kwama-amoxicillin capsule kukhuphuke ngama-38% kuya ku-90% ngaphandle kwe-HPMC.
I-HPMC ingenziwa ngokunamathela okuhlanganisiwe okunokuhlushwa okuhlukile kwesitashi se-starch ngemuva kokuchithwa; Ukuchithwa kwamathebulethi e-erythromycin angenayo akhuphuke kusuka ku-38.26% kuya ku-97.38% lapho u-2% hpmc kanye nesitashi esingu-8% sahlanganiswa.
2.2. Yenza izinto ze-film coating kanye nefilimu eyakha izinto ezibonakalayo
I-HPMC njengezinto ezihlanganisiwe zamanzi ezinamanzi inezici ezilandelayo: isixazululo esilinganiselayo solution; Inqubo yokuhlanganisa ilula; Ifilimu elihle kwakha impahla; Angagcina ukwakheka kwengcezu, ukubhala; Ingaba umswakama; Ungafaka umbala, ukunambitheka kokulungiswa. Lo mkhiqizo usetshenziselwa ukuhlanganiswa kwamafilimu amanzi amaphilisi kanye namaphilisi anokubonakala okuphansi, kanye nokukhomba kwamafilimu okungewona amanzi ngokubonakala okuphezulu, inani lokusebenzisa lingu-2% -5%.
2.3, njenge-ejenti yokuqina kanye ne-colloidal vitrop glue
I-HPMC esetshenziswa njenge-ejenti yokuqina ingu-0.45% ~ 1.0%, ingasetshenziswa njengamaconsi wamehlo kanye ne-ejenti yokuqina kwezinyembezi; Isetshenziselwa ukukhuphula ukuqina kwe-glue ye-hydrophobic, vimba izinhlayiyana zamalahle, ukuhanjiswa kwezulu, umthamo ojwayelekile ngu-0.5% ~ 1.5%.
2.4, njenge-blocker, ukukhishwa kancane kwento, i-ejenti yokukhishwa elawulwa kanye ne-ejenti ye-pore
Imodeli ye-HPMC ephezulu ye-Viscosity isetshenziselwa ukulungiselela ama-blockers kanye nama-ejenti wokukhishwa alawulwayo amathebhulethi ahlanganisiwe wokukhishwa kwamathebulethi asetshenzisiwe kanye namathebulethi okukhishwa kwe-hydrophilic gel Imodeli ye-Low-Viscosity iyi-ejenti evuthayo ye-pore-eduduzayo yamathebulethi okukhishwa okuqhubekayo noma okulawulwa kokukhishwa kwalezi zibhebhelo anjengamathebhulethi anjalo atholakala ngokushesha, alandelwe ukukhishwa okuqhubekayo noma okulawulwa ukuze alondoloze ukugxila okusebenzayo egazini.
2.5. Ijeli ne-matrix evamile
Ama-suppogel ama-suppogel kanye namalungiselelo anamathela esiswini angalungiswa ngokusebenzisa isimo sokwakheka kwe-hpdrogel okuvame ukusetshenziswa yi-HPMC emanzini.
2.6 Izinto zokunamathela eziphilayo
IMetronidazole yahlanganiswa ne-HPMC ne-Polycarboxylelene 934 ku-mixer ukwenza amaphilisi wokukhishwa alawulwa ngokulawulwa okungu-250mg. Ukuhlolwa kokuchithwa kwe-vitro kukhombisa ukuthi ukulungiselela ngokushesha okufuzeke emanzini, futhi ukukhululwa kwezidakamizwa kulawulwa yi-devil kanye nokuphumula kwe-carbon chain. Ukuqaliswa kwezilwane kukhombisa ukuthi uhlelo olusha lokukhishwa kwezidakamizwa lwalunezakhiwo ezibalulekile zokunamathela ezibhalini ze-BOVINE SUBLIDIAL Mucosa.
2.7, njengosizo lokumiswa
I-viscosity ephezulu yalo mkhiqizo ingusizo oluhle lokumiswa kwamalungiselelo awuketshezi, umthamo wayo ojwayelekile ngu-0.5% ~ 1.5%.
4. Izibonelo zohlelo lokusebenza
4.1 I-FIME COAIT Solution: I-HPMC 2KG, i-Talc 2kg, i-Castor Oil 1000ml, i-Twain -80 1000ml, i-plylene glycol, 95% ethanol 53000ml, amanzi afanele we-pig 47000ml, inani elifanele le-pig 47000ml, inani elifanele le-pig 47000ml, inani elifanele le-pig 47000ml, inani elifanele le-pig 47000ml, inani elifanele le-pig 47000ml, inani elifanele le-pig 47000ml, inani elifanele le-pig 47000ml, inani elifanele le-pig 47000ml, inani elifanele lezinhlamvu. Kunezindlela ezimbili zokukwenza.
4.1.1 Ukulungiswa kwe-boluble pigment izingubo izingubo zezingubo: Faka inani elinqunyelwe le-HPMC libe yi-95% ethanol, chombisa olunye i-vector ye-pigment emanzini (Hlola uma kunesidingo), hlanganisa izixazululo ezimbili futhi uvuse ngokulinganayo ukwakha isixazululo esibonakalayo . Hlanganisa i-80% yesisombululo (ama-20% okuphoqelela) ngenani elinqunyelwe lamafutha e-castor, ana-20-80, ne-plylene glycol.
4.1.2 Ukulungiswa kwe-insoluble pigment (efana ne-iron oxide) i-HPMC ye-coatiw HPMC yangezwa ngo-95% ethanol ubusuku bonke, futhi amanzi angezwa ukwenza ikhambi elingu-2% HPMC elibonakalayo. I-20% yalesi sixazululo yathathwa ukuze iphoqelele, futhi isixazululo esisele esingu-80% kanye ne-iron oxide yalungiswa yindlela yokugaya uketshezi, bese kufakwa inani lesinye izingxenye futhi lixutshwe ngokulinganayo ukuze lisetshenziswe. Inqubo yokuhlanganisa uketshezi lwe-coating Ngomoya oshisayo we-5 ~ 10min angaphuma ebhodweni, afaka esomile ukuze ame ngaphezulu kwe-8h.
I-4.2α-i-Interferon Eye Membrane 50 / I-Interferon ichithwe ku-10ml0.01ml hydrochloric acid, exutshwe ne-90ml hydrochloric kanye ne-0.5GHMC, ihlanganiswe ngenduku yengilazi ejikelezayo, ihlanganiswe ngo-60 ℃ futhi yomile emoyeni. Lo mkhiqizo wenziwa ngezinto zefilimu.
Amathebulethi we-COTRIMOXAZAZLE (0.4G ± 0.08g) I-SMZ (80 Mesh) 40kg, isitashi (30 Mesh) 8kg, 3% hpmc aqualu turlualu, TMP (80 Mearate 0.3kg, TMP (80 Mesh) 8KG, Indlela Yokulungiselela Hlanganisa i-SMZ ne-TMP, bese wengeza isitashi bese uxuba i-5min. Ngesisombululo se-3% HPMC esinamanzi, impahla ethambile, enotshani besikrini se-mesh, ukomisa, bese kuthi ngesikrini se-magnesium esigcwele okuphelele, engeza i-magnesium stearate amaphilisi. Lo mkhiqizo usetshenziswa ikakhulukazi njenge-binder. Ukuchithwa kwamathebulethi kwakungu-96% / 20min.
I-4.4 amaphilisi amapayipi (0.25g) Piperate 80 Mesh 25kg, isitashi (120 mesh) 2.1kg, inani le-magnesium elifanelekile. Indlela yayo yokukhiqiza ukuxuba i-acid ye-peiphoperic, isitashi, i-hpmc ngokulinganayo, nge-20% izinto ezithambile ze-ethanEL, i-16% ye-ethanol screen, i-vector magnesium stearate yonke, nge-100mm eyindilinga yeBelt (PPA0.25 ) ukucindezela amaphilisi. Nge-Starch njenge-ejenti ehlukanisayo, izinga lokuchithwa kwale thebulethi alikho ngaphansi kwama-80% / 2min, eliphakeme kunemikhiqizo efanayo eJapan.
4.5 Izinyembezi ze-artificial teere HPMC-4000, HPMC-4500 noma i-HPMC-5000 0.3G, Sodium Chloride 0.45g, i-10%, 10%, 10%, i-10%, amanzi angezwe ku-100ml. Indlela yayo yokukhiqiza yi-HPMC ebekwe emanzini ayi-15ml, ku-80 ~ 90 ~ 90 ~ 90 ~ 90 ~ 90 ~ 90 ~ 90 ~ 90 ~ 90 ~ 90 ~ 90 ~ 90 ~ 90 ~ 90 ~ 90 ~ 90 ~ 90 ~ 90 ~ 90 ~ 90 , ngomusa uthele i-filtration, filltrate esitsheni esivaliwe, inzalo ku-98 ~ 100 ℃ ye-30min, okungukuthi, i-PH REAnges kusuka ku-8.4 ° C kuya ku-8.6 ° C. Lo mkhiqizo ucelwe ukucisha izinyembezi, Lapho isetshenziselwa i-anterior Chamber Microscopy, ingakhuphuka ngokufanelekile umthamo walo mkhiqizo, u-0.7% ~ 1.5% kufanelekile.
4.6 I-MeteTHorphan Reconded Reserfes Amatafula we-Metitthorphan Resin Salt 187.5mg, Lactose 40.0mg, Vvp70.0mg, Vapor Silica 10mg, 40.0, 40.0MG ~ Ilungiselelwe njengamathebhulethi ngendlela ejwayelekile. Lo mkhiqizo usetshenziswa njengezinto ezilawulwa ukukhishwa.
I-4.7 yamathebhulethi e-avantomycin ⅳ, amaphilisi wamanzi angama-2149g avantomycin ⅳ monohydrate kanye ne-1000ml isohpropyl inhlanganisela ye-15% (ukugxilisa isisindo) eudragitl-100 (9: 1) avuswa, ahlanganiswa, futhi omiswe ngo-35 ℃. Ama-granules omisiwe angu-575g no-62.5g hydroxypropyloclellosellose e-50 ahlanganiswa, bese kuthi isitebhisi esingu-7.5g kanye ne-3.25g acid kanye ne-3.25g i-magnesium yengezwe kumathebulethi azothola ukukhishwa okuqhubekayo kwe-MyCuntiard MyCin ⅳ. Lo mkhiqizo usetshenziswa njengezinto zokukhishwa kancane.
4.8 I-NIFEDIPINIPIPIPIPIPIPE I-GRANLUSE ADUSTION-SUSKERULES 1 Ingxenye nifedipine, 3 izingxenye ze-hydroxypropyllyllylyllylyllylyllyllyllylyllylyllylylllyllyllyllylyllyllyllylyllyllyllyllyllylyllllylylllylylllyllylylllyllylyllylylllylylllylyllylylllllyllylllylyllllls methylllose kanye nezingxenye ezintathu ze-ethyl clullule indlela. Izinga lokukhishwa kwezidakamizwa lemifino alizange lithintwe ukuguqulwa kwezemvelo PH futhi sasihamba kancane kunaleyo yemidlalo etholakala kwezentengiselwano. Ngemuva kwamahora ayi-12 okuphatha ngomlomo, ukugxila kwegazi lomuntu kwakungu-12mg / ml, futhi kwakungekho mehluko umuntu ngamunye.
I-4.9 Propranhaol Hydrochloride eqhubekayo yokukhishwa kwe-capsule propranhaol hydrochloride 60kg, i-microcrystalline cellulose 40kg, engeza amanzi angama-50l ukwenza ama-granules. I-HPMC1KG ne-EC 9KG bahlanganiswa kwi-solvent exubile (Methylene Chloride: Methanol = 1: 1) 200l ukwenza isixazululo se-coating / ama-flow rainting / izinhlayiya ezihlanganisiwe ngosayizi we-1.4 Screen Screen Bonke izinhlayiya, bese ugcwala engxenyeni yamatshe enomshini wokugcwalisa ojwayelekile we-capsule. I-capsule ngayinye iqukethe ama-160mg we-propranolol hydrochloride spherical izinhlayiya.
4.10 Amacwecwe ama-NAPROL HCL Skeleton alungiswe ngokuxuba i-NAPROL HCL: I-HPMC: CMC-NE ngesilinganiso 1: 0.25: 2.25. Izinga lokukhishwa kwezidakamizwa lalisondele ku-zero oda ezingakapheli amahora ayi-12.
Ezinye izidakamizwa nazo zingenziwa ngezinto zokuxutshwa ezixubile, njenge-metoprolol: hpmc: cmc-na Ngokuya: 1: 1.25: 1.25; I-Allylprolol: HPMC ngokusho kwe-1: 2.8: 2.92 Ratio. Izinga lokukhishwa kwezidakamizwa lalisondele ku-zero oda ezingakapheli amahora ayi-12.
4.11 Amathebulethi ama-Skeleton wezinto ezihlanganisiwe zezinto ezihlanganisiwe ze-Ethalaminosives zalungiswa ngendlela ejwayelekile esebenzisa ingxube ye-Micro Pople Gel: CMC-NE: HPMC 1: 0.7: 4.4. Lesi sidakamizwa singadedelwa ngo-12h sobabili e-vitro naseVivo, futhi iphethini yokukhishwa eqondile yayinokuhlobana okuhle. Imiphumela yokuhlolwa kokuqina okusheshayo ngokuya ngemithetho ye-FDA ibikaza ukuthi impilo yokugcina yalo mkhiqizo ingafika eminyakeni emi-2.
I-4.12 HPMC (50MPA - S), i-HPMC (4000 MPA S) (izingxenye ezi-3) ne-HPC1 zichithwe izingxenye zamanzi, izingxenye ezingama-60 ze-acetamizen kanye nezingxenye eziyisithupha ze-silica gel, futhi isifutho somile. Lo mkhiqizo uqukethe ama-80% emithi eyinhloko.
4.13 I-theophylline hydrophilic gel amatafula amathafathi abalwa ngokuya ngesisindo sethebhulethi esiphelele, okungu-18% -35% i-theophylline, 7.5% -22.5% HPMC, 0.5% Gcina ukugxila kwegazi okusebenzayo komzimba womuntu we-12h ngemuva kokuphathwa ngomlomo.
Isikhathi sePosi: Feb-05-2024