1. Iimpawu ezisisiseko ze-HPMC
IHydroxypropyl methylcellulose, igama lesiNgesi yihydroxypropyl methylcellulose, ekwaziwa ngokuba yiHPMC.I-molecular formula yi-C8H15O8-(C10Hl8O6)N-C8HL5O8, kwaye ubunzima bayo be-molecular malunga ne-86,000.Imveliso i-semi-synthetic, equka inxalenye ye-methyl kunye nenxalenye ye-cellulose ye-polyhydroxypropyl ether.Inokwenziwa ngeendlela ezimbini: enye kukuphatha ibakala elifanelekileyo le-methyl cellulose kunye ne-NaOH, kwaye emva koko uphendule ngepropylene oxide phantsi kobushushu obuphezulu kunye noxinzelelo oluphezulu.Ixesha lokuphendula kufuneka ligcinwe ukwenzela ukuba amaqela e-methyl kunye ne-hydroxypropyl aguqulwe abe yi-ethers.Ifom ikhona kwaye idibaniswe ne-ring glucose dehydrated ye-cellulose ukuya kumlinganiselo ofunekayo;enye kukunyanga umqhaphu we-cotton lint okanye i-wood pulp fiber kunye ne-caustic soda ukusabela ukufumana i-methane chloride kunye ne-propylene oxide, enokuthi iphuculwe ngakumbi kwaye iphantsi.Yenze ibe ngumgubo ocolekileyo kunye nofanayo okanye iigranules.I-HPMC sisityalo se-cellulose sendalo kunye ne-excipient yamayeza egqwesileyo enoluhlu olubanzi lwemithombo.Okwangoku isetyenziswa kakhulu ekhaya nakwamanye amazwe kwaye yenye yezona zinto zixhaphakileyo zisetyenziselwa amayeza amayeza asetyenziswa ngomlomo.
Le mveliso imhlophe ukuya kumhlophe omhlophe, ayinayo ityhefu, ayinavumba, i-granular okanye i-fibrous, i-powder elula ehamba lula.Uzinzile phantsi kokukhanya kunye nokufuma.Yandisa emanzini abandayo ukwenza isisombululo se-milky colloidal kunye ne-viscosity ethile, kwaye i-sol-gel interconversion phenomenon iyenzeka ngenxa yokutshintsha kweqondo lokushisa kwesisombululo kunye noxinzelelo oluthile.Inyibilika kakhulu kwi-70% ye-ethanol okanye i-dimethyl ketone, kodwa ayinyibiliki kwi-ethanol epheleleyo, i-chloroform okanye i-ethoxyethane.
Ixabiso le-pH le-hydroxypropyl methylcellulose liphakathi kwe-4.0 kunye ne-8.0, kwaye inozinzo oluhle.Ixabiso le-pH lizinzile phakathi kwe-3.0 kunye ne-11.0.Ingagcinwa kwi-20°C kunye nokufuma okumalunga ne-80% kangangeentsuku ezili-10.I-coefficient yokufunxa ukufuma kwe-HPMC yi-6.2%.
I-Hydroxypropyl methylcellulose ineentlobo ezahlukeneyo zeemveliso ngenxa yemixholo eyahlukeneyo ye-methoxy kunye namaqela e-hydroxypropyl kwisakhiwo.Kwiindawo ezithile, iintlobo ezahlukeneyo zeemveliso zine-viscosity ethile kunye neempawu ze-thermal.Ukushisa kwe-gel kwaye ngoko ke baneempawu ezahlukeneyo ezingasetyenziselwa iinjongo ezahlukeneyo.I-pharmacopoeia yelizwe ngalinye ineemfuno ezahlukeneyo zemodeli kunye namazwi: i-European Pharmacopoeia isekelwe kwii-viscosities ezahlukeneyo, amanqanaba ahlukeneyo okutshintshwa, amanqanaba okusebenzisa kunye namanani amabakala ahlukeneyo emveliso ethengiswa kwimarike.Iyunithi ye-United States Pharmacopoeia yi-mPa · s, kwaye amagama aqhelekileyo alandelayo Sebenzisa amadijithi amane ukumela umxholo we-hydroxypropyl methylcellulose kunye neendawo ezahlukeneyo kunye neentlobo, ezifana ne-hydroxypropyl methylcellulose, 2208. Amadijithi amabini okuqala amele ipesenti eqikelelweyo yamaqela e-methoxy, kwaye amanani amabini okugqibela amele iqela le-hydroxyl.Ipesenti eqikelelweyo yepropyl.
2. I-HPMC inyibilikiswe kwindlela yamanzi
2.1 Indlela yamanzi ashushu
Ekubeni i-hydroxypropyl cellulose inganyibiliki emanzini ashushu, inokusasazeka ngokulinganayo emanzini ashushu kwaye ipholile.Iindlela ezimbini eziqhelekileyo ziyaziswa ngolu hlobo lulandelayo:
(1) Faka umlinganiselo ofunekayo wamanzi ashushu kwisikhongozelo uze usifudumeze ukuya kutsho kuma-70°C.Yongeza imveliso ngokuthe ngcembe ngelixa ushukumisa kancinane.Ekuqaleni, imveliso idada emanzini kwaye ngokuthe ngcembe yenza i-slurry.
(2) Yongeza i-1/3 okanye i-2/3 yomthamo ofunekayo wamanzi kwisikhongozelo kwaye uyifudumeze ukuya kuma-70°C ukusasaza imveliso, ulungise udaka lwamanzi ashushu, uze wongeze umlinganiselo oseleyo wamanzi abandayo okanye wongeze umkhenkce. amanzi kumanzi ashushu aludaka.i-slurry emanzini, ugxobhoze umxube emva kokupholisa.
2.2 Indlela yokuxuba umgubo
Iingqungquthela ze-powder zihlakazwe ngokucokisekileyo ngokuxuba okomileyo kunye nezixa ezilinganayo okanye ezinkulu zezinye izithako ezinomgubo kwaye zichithwe ngamanzi, apho i-HMCS ichitheka ngaphandle kwe-coagulation.
3. Izinto eziluncedo zeHPMC
3.1 Inyibilika emanzini abandayo
Iyanyibilika kumanzi abandayo angaphantsi kwe-40℃ okanye i-70% ye-ethanol, kwaye ayinyibiliki emanzini ashushu ngaphezulu kwe-60℃, kodwa iyakwazi ijeli.
3.2 Ukungangeni ngamachiza
I-HPMC yi-ether ye-cellulose engeyiyo ionic.Isisombululo sayo asinayo i-ionic kwaye ayisebenzisi kunye neetyuwa zetsimbi okanye i-ionic organic compounds.Ke ngoko, abanye abancedisi abasabelani nayo ngexesha lenkqubo yokuvelisa.
3.3 Uzinzo
Izinzile kwi-asidi kunye ne-alkali kwaye ingagcinwa ixesha elide phakathi kwe-pH 3 kunye ne-1l ngaphandle kokutshintsha okuphawulekayo kwi-viscosity.Izisombululo zamanzi ze-hydroxypropyl methylcellulose (HPMC) zi-antifungal kwaye zigcina uzinzo oluhle lwe-viscosity ngexesha lokugcinwa kwexesha elide.Uzinzo olusemgangathweni lwe-HPMC lungcono kunezincedisi zemveli (ezifana ne-dextrin, istatshi, njl.).
3.4 I-viscosity ehlengahlengiswayo
I-viscosity derivatives eyahlukeneyo ye-HPMC ingaba ngokwemilinganiselo eyahlukeneyo, kwaye i-viscosity yabo ingatshintshwa ngokweemfuno zokuthobela imithetho ethile kwaye ibe nobudlelwane obuhle bomgca, ngoko umlinganiselo unokukhethwa ngokweemfuno.
3.5 Ukungazinzi kweMetabolic
I-HPMC ayifunxanga okanye ixutywe emzimbeni kwaye ayiboneleli ngobushushu, ngoko ke iyindawo ekhuselekileyo yokulungiselela amayeza.
3.6 Ukhuseleko
I-HPMC ngokuqhelekileyo ithathwa njengento engeyiyo ityhefu, into engabonakaliyo, kunye ne-LD50 ye-5g / kg kwiigundane kunye ne-5.2g / kg kwiigundane.Iidosi zemihla ngemihla azinabungozi ebantwini.
4 Ukusetyenziswa kweHPMC kumalungiselelo
4.1 Izinto zokugquma ifilimu kunye nezixhobo zokwenza ifilimu
IHydroxypropyl methylcellulose (HPMC) isetyenziswa njengesixhobo sokugquma ifilimu.Iipilisi zayo ezigqunyiweyo azikho iingenelo ezicacileyo ngaphezu kweepilisi ezigqunywe ngokwesintu ezifana neepilisi ezifakwe iswekile ngokwemiqathango yokufihla incasa kunye nokubonakala kweziyobisi, kodwa ukuqina kwayo, ukunyanzeliswa, kunye ne-hygroscopicity, ukuchithwa kakubi., Ukufumana ubunzima bokugubungela kunye nezinye izikhombisi zekhwalithi zingcono.Ibakala eliphantsi le-viscosity yale mveliso lisetyenziswa njengento yokugubungela ifilimu e-soluble yamanzi kwiipilisi kunye neepilisi, kwaye ibakala eliphezulu le-viscosity lisetyenziswa njengento yokugubungela ifilimu kwiinkqubo ze-solvent ze-organic.Ukugxininiswa ngokuqhelekileyo yi-2.0% ~ 20%.
4.2 Njengomdibanisi kunye ne-disintegrant
Ibakala eliphantsi le-viscosity yale mveliso lingasetyenziselwa njenge-binder kunye ne-disintegrant yamacwecwe, iipilisi, kunye ne-granules, ngelixa ibakala eliphezulu le-viscosity lingasetyenziselwa kuphela njenge-binder.Idosi iyahluka ngokwemodeli kunye neemfuno, ngokubanzi i-5% yeetafile ezomileyo zegranulation kunye ne-2% yeetafile ezimanzi zegranulation.
4.3 Njengoncedo lokunqunyanyiswa
I-agent yokumisa i-gel i-viscous i-gel i-hydrophilic kwaye ingasetyenziselwa ukucotha isantya sokumisa i-particle kwaye ibambelele kumphezulu we-particle ukukhusela ama-particle ukuba adibanise kwiibhola.Izixhobo zokumisa zidlala indima ebalulekileyo ekuveliseni i-agent yokumiswa.HPMC is an best suspension additive.Isisombululo sayo se-colloidal esinyibilikisiweyo sinokunciphisa ukunyanzeliswa kwe-liquid-solid interfacial kunye namandla amahhala amancinci amancinci amancinci, ngaloo ndlela kuphuculwe ukuzinza kwenkqubo yokusabalalisa okungafaniyo.Le mveliso yi-high-viscosity ukumiswa kokulungiselela kunye nesiphumo esihle sokunqunyanyiswa, ukusabalalisa lula, udonga olunganamatheli, kunye namasuntswana amahle e-flocculation.Idosi yayo eqhelekileyo yi-0.5% ukuya kwi-1.5%.
4.4 Njenge-arhente eyekayo, ekhutshwa ngokuzinzileyo kunye ne-porogen
Ibanga eliphezulu le-viscosity yale mveliso lisetyenziselwa ukulungiselela i-hydrophilic gel matrix yokukhululwa okuqhubekayo, iipilisi zezinto ezixubileyo ze-matrix ezizinzileyo zokukhululwa kwee-retarders kunye nee-agent-release-release agents.Inesiphumo sokulibazisa ukukhutshwa kweziyobisi.Ukugxininiswa kokusetyenziswa kwayo yi-10% -80% (W / W).Amanqanaba e-viscosity aphantsi asetyenziswa njenge-pore inducers ekuqulunqweni kokukhululwa okuqhubekayo okanye okulawulwayo.Iipilisi ezinjalo zinokufikelela ngokukhawuleza idosi yokuqala efunekayo kwisiphumo sonyango, emva koko ivelise isiphumo sokukhululwa esizinzileyo okanye esilawulwayo, kunye nokugcina ukugxilwa kweyeza elisebenzayo emzimbeni.IHydroxypropyl methylcellulose i-hydrates emanzini ukwenza umaleko wejeli.Indlela yokukhutshwa kweziyobisi yamacwecwe e-matrix ikakhulu ibandakanya ukusasazwa komgangatho wejeli kunye nokuchithwa kwejeli.
4.5 Izinto ezityebisayo kunye nee-colloids ezikhuselayo
Xa le mveliso isetyenziswa njenge-thickener, i-concentration esetyenziswa ngokuqhelekileyo yi-0.45% ~ 1.0%.Le mveliso inokunyusa ukuzinza kweglue ye-hydrophobic, yenza i-colloid ekhuselayo, ithintele amaqhekeza kwi-agglomeration kunye ne-agglomeration, ngaloo ndlela inqanda ukubunjwa kwemvula.Ukugxininiswa kwayo okuqhelekileyo ngu-0.5% ~ 1.5%.
4.6 Sebenzisa njengesixhobo se-capsule
Ngokuqhelekileyo i-capsule shell material ye-capsules yi-gelatin.Inkqubo yokuveliswa kweegobolondo ze-gelatin capsule ilula, kodwa kukho iingxaki kunye neziganeko ezifana nokukhuselwa kakubi kumanzi kunye ne-oxygen-sensitive drugs, ukunciphisa ukuchithwa kweziyobisi, kunye nokulibaziseka ukuchithwa kweegobolondo ze-capsule ngexesha lokugcinwa.Ngoko ke, i-hydroxypropyl methylcellulose isetyenziselwa indawo yezixhobo ze-capsule ekulungiseleleni ii-capsules, eziphucula ukuveliswa, ukubumba kunye nokusetyenziswa kwemiphumo yee-capsules, kwaye iye yakhuthazwa ngokubanzi ekhaya nakwamanye amazwe.
4.7 Njenge-bioadhesive
I-teknoloji ye-Bioadhesion isebenzisa i-excipients kunye ne-polymers ye-bioadhesive ukunamathela kwi-mucosa yezinto eziphilayo kunye nokuphucula ukuhambelana kunye nokuqina koqhagamshelwano phakathi kokulungiswa kunye ne-mucosa, evumela ukuba ichiza likhutshwe ngokukhawuleza kwaye lifunnwe yi-mucosa ukufezekisa iinjongo zonyango.Ukufezekisa injongo yokonyango, okwangoku isetyenziselwa ukuphatha izifo kwi-nasal cavity, i-mucosa yomlomo kunye nezinye iindawo zomzimba.Itekhnoloji ye-bioadhesion ye-gastrointestinal luhlobo olutsha lwenkqubo yokuhanjiswa kweziyobisi ephuhliswe kwiminyaka yakutshanje.Ayinakwandisa nje ixesha lokuhlala lamalungiselelo eziyobisi kwindlela yesisu, kodwa iphucula ukusebenza koqhagamshelwano phakathi kwechiza kunye nesayithi lokufunxa inwebu yeseli kunye nokutshintsha isakhiwo senwebu yeseli.Ukushukuma, oko kukuthi, ukufikeleleka kwechiza kwiiseli ze-epithelial zamathumbu, ngaloo ndlela
Ixesha lokuposa: Feb-01-2024