1. Imvelo eyisisekelo ye-HPMC
IHypromellose, igama lesiNgisi elithi hydroxypropyl methylcellulose, alias HPMC. Ifomula yayo yamangqamuzana ithi C8H15O8-(C10Hl8O6)n-C8Hl5O8, futhi isisindo samangqamuzana cishe singama-86,000. Lo mkhiqizo uyi-semi-synthetic material, eyingxenye yeqembu le-methyl kanye nengxenye ye-polyhydroxypropyl ether ye-cellulose. Ingenziwa ngezindlela ezimbili: enye iwukwelapha i-methyl cellulose yebanga elifanele nge-NaOH, bese isabela nge-propylene oxide ngaphansi kwezinga lokushisa eliphezulu nokucindezela okukhulu. Isikhathi sokusabela kufanele sigcinwe ukuze kuvunyelwe amaqembu e-methyl kanye ne-hydroxypropyl ukuthi ahlangane ne-ether. Ifomu lixhunywe kwindandatho ye-anhydroglucose ye-cellulose, futhi ingafinyelela izinga elifunekayo; enye iwukwelapha i-linter kakotini noma i-wood pulp fiber nge-caustic soda, bese itholwa ngokusabela nge-chlorinated methane kanye ne-propylene oxide ngokulandelana, bese icwengisiswa ngokuqhubekayo, Phula, yenza ibe yimpushana ecolekile nefanayo noma imbudumbudu. I-HPMC iyinhlobonhlobo ye-cellulose yezitshalo zemvelo, futhi iyisakhi esihle kakhulu semithi, esinomthombo obanzi. Njengamanje, isetshenziswa kabanzi ekhaya naphesheya, futhi ingenye yezinsiza zemithi enezinga eliphezulu kakhulu lokusebenzisa phakathi kwezidakamizwa eziphuzwayo.
Umbala walo mkhiqizo umhlophe kuya komhlophe okubisi, awunabo ubuthi futhi awunambitheki, futhi uyimpushana noma i-fibrous, impushana egeleza kalula. Iyazinza ngaphansi kokuchayeka ekukhanyeni kanye nomswakama. Ikhukhumala emanzini abandayo ukuze yakhe isixazululo se-milky colloidal esinezinga elithile le-viscosity. I-sol-gel interconversion phenomenon ingenzeka ngenxa yokushintsha kwezinga lokushisa lokuhlushwa okuthile kwesisombululo. Kulula kakhulu ukuncibilika ku-70% wotshwala noma i-dimethyl ketone, futhi ngeke incibilike ku-anhydrous alcohol, i-chloroform noma i-ethoxyethane.
I-Hypromellose inokusimama okuhle lapho i-pH iphakathi kuka-4.0 no-8.0, futhi ingaba khona ngokuzinza phakathi kuka-3.0 no-11.0. Ngemva kokugcina izinsuku ezingu-10 ezingeni lokushisa elingu-20°C kanye nomswakama ohlobene no-80%, I-coefficient yokumunca umswakama ye-HPMC ingu-6.2%.
Ngenxa yomehluko kokuqukethwe kwezinto ezimbili ezingaphansi kwesakhiwo se-hypromellose, i-methoxy ne-hydroxypropyl, izinhlobo ezahlukene zemikhiqizo ziye zavela. Ekugxilweni okuthile, izinhlobo ezihlukahlukene zemikhiqizo zine-viscosity ethize kanye nezinga lokushisa le-Thermal gelation, ngakho-ke, linezici ezihlukene futhi zingasetshenziswa ngezinhloso ezahlukene. I-pharmacopoeias yamazwe ahlukahlukene inezincazelo ezihlukile nezinkulumo zemodeli: I-European Pharmacopoeia isuselwe kumabanga ahlukahlukene ama-viscosities ahlukene kanye namazinga ahlukene okushintsha imikhiqizo emakethe. Ivezwa yibanga kanye nenombolo. Iyunithi ngama-mPa•s. Ngemva kokwengeza amadijithi angu-4 ukukhombisa okuqukethwe kanye nohlobo lwengxenye ngayinye ye-hypromellose, isibonelo, i-hypromellose 2208, amadijithi amabili okuqala amelela isilinganiso sephesenti leqembu le-methoxy, amadijithi amabili okugcina amelela i-hydroxypropyl Iphesenti elilinganiselwe lamacala.
2.Indlela yokuncibilikisa i-HPMC emanzini
2.1 Indlela yamanzi ashisayo
Njengoba i-hypromellose ingancibiliki emanzini ashisayo, ingahlakazwa ngokufanayo emanzini ashisayo esigabeni sokuqala, bese kuthi lapho isipholile, izindlela ezimbili ezijwayelekile zichazwe kanje:
(1) Faka inani elidingekayo lamanzi ashisayo esitsheni bese ushisa kuze kufike ku-70℃. Yengeza kancane kancane umkhiqizo ngaphansi kokuvuselela kancane. Ekuqaleni, umkhiqizo untanta phezu kwamanzi, bese kancane kancane wenza i-slurry. Pholisa i-slurry.
(2) Faka u-1/3 noma u-2/3 wenani elidingekayo lamanzi esitsheni bese uwushisa ufike ku-70°C ukuze uhlakaze umkhiqizo ukuze ulungise udaka lwamanzi ashisayo, bese wengeza inani elisele lamanzi abandayo noma amanzi eqhwa. ukuya emanzini ashisayo slurry Ku-slurry, pholisa ingxube ngemva kokugqugquzela.
2.2 Indlela yokuxuba umpuphu
Izinhlayiya zempushana nezinye izithako eziyimpuphu zenani elilinganayo noma elikhulu zihlakazwa ngokugcwele ngokuxuba okomile, bese amanzi engezwa ukuze ancibilike. Ngalesi sikhathi, i-hypromellose ingancibilika ngaphandle kwe-agglomeration.
3. Izinzuzo ze-HPMC
3.1 Ukuncibilika kwamanzi abandayo
Incibilika emanzini abandayo angaphansi kuka-40°C noma i-ethanol engu-70%. Ayincibiliki emanzini ashisayo angaphezu kuka-60°C, kodwa ingafakwa i-gelled.
3.2 Ukungangeni ngamakhemikhali
IHypromellose (HPMC) iwuhlobo lwe-non-ionic cellulose ether. Isixazululo saso asinakho ukushaja kwe-ionic futhi asihlanganyeli nosawoti wensimbi noma izinhlanganisela eziphilayo ze-ionic. Ngakho-ke, amanye ama-excipients awaphenduli nawo phakathi nenqubo yokulungiselela.
3.3 Ukuzinza
Iqinile ngokuqhathaniswa kukho kokubili i-asidi ne-alkali, futhi ingagcinwa isikhathi eside phakathi kwe-pH 3 kuya ku-1l, futhi i-viscosity yayo ayinalo ushintsho olusobala. Isixazululo esinamanzi se-hypromellose (HPMC) sinomphumela wokulwa nesikhunta futhi singagcina ukuqina okuhle kwe-viscosity ngesikhathi sokugcina isikhathi eside. Izisetshenziswa zemithi ezisebenzisa i-HPMC zinokuzinza kwekhwalithi engcono kunalezo ezisebenzisa izinto ezisizayo zendabuko (ezifana ne-dextrin, isitashi, njll.).
3.4 Ukulungiswa kwe-viscosity
I-viscosity derivatives ehlukene ye-HPMC ingaxutshwa ngezilinganiso ezahlukene, futhi i-viscosity yayo ingashintsha ngokuvumelana nomthetho othile, futhi inobudlelwane obuhle bomugqa, ngakho-ke ingakhethwa ngokuvumelana nezidingo.
3.5 Inertia ye-Metabolic
I-HPMC ayimuncwe noma igaywe emzimbeni, futhi ayinikezi ama-calories, ngakho-ke iyisakhi esiphephile samalungiselelo okwelapha.
3.6 Ezokuphepha
Kukholelwa ukuthi i-HPMC iyimpahla engenabuthi futhi engacasuli. Umthamo obulalayo omaphakathi wamagundane ngu-5g/kg, kanti umthamo obulalayo omaphakathi wamagundane ngu-5.2g/kg. Umthamo wansuku zonke awunangozi emzimbeni womuntu.
4. Ukusetshenziswa kwe-HPMC emalungiselelweni
4.1 Isetshenziswa njengezinto zokumboza ifilimu nezinto zokwakha ifilimu
I-Hypromellose (HPMC) isetshenziswa njenge-tablet ehlanganiswe nefilimu. Uma kuqhathaniswa namaphilisi endabuko ahlanganiswe njengamaphilisi afakwe ushukela, amaphilisi ahlanganisiwe awanazo izinzuzo ezisobala ekufihleni ukunambitheka nokubukeka, kodwa ukuqina kwabo kanye nokuqina , Ukumuncwa komswakama, ukuhlakazeka, ukuzuza kwesisindo sokugqoka kanye nezinye izinkomba zekhwalithi zingcono. Ibanga eliphansi le-viscosity lalo mkhiqizo lisetshenziswa njengento yokumboza ifilimu encibilikayo emanzini kumaphilisi namaphilisi, futhi izinga le-viscosity ephezulu lisetshenziswa njengento yokumboza ifilimu yezinhlelo ze-organic solvent. Ukuhlushwa kokusetshenziswa kuvame ukuba ngu-2.0% -20%.
4.2 njengesibophezelo kanye nesihlukanisi
Ibanga le-viscosity eliphansi lalo mkhiqizo lingasetshenziswa njenge-binder kanye ne-disintegrant yamaphilisi, amaphilisi, nama-granules, futhi ibanga le-viscosity ephezulu lingasetshenziswa kuphela njenge-binder. Umthamo uyahlukahluka ngamamodeli ahlukene kanye nezidingo. Ngokuvamile, inani le-binder elisetshenziselwa amaphilisi e-granulation eyomile lingu-5%, kanti inani le-binder elisetshenziselwa amaphilisi e-granulation emanzi ngu-2%.
4.3 Njenge-ejenti elengayo
I-ejenti yokumisa ijeli ye-viscous ene-hydrophilicity. Ukusetshenziswa kwe-ejenti yokumisa i-ejenti elengayo kunganciphisa isivinini se-sedimentation yezinhlayiya, futhi ingaxhunyaniswa ebusweni bezinhlayiya ukuvimbela izinhlayiya ukuthi zingama-polymerizing futhi zijike zibe yinqwaba. Ama-ejenti amisiwe adlala indima ebalulekile ekukhiqizeni ukumiswa. I-HPMC iyinhlobonhlobo enhle kakhulu yama-ejenti amisiwe. Isixazululo se-colloidal esincibilikisiwe kuso singanciphisa ukushuba kwesixhumi esibonakalayo esiwuketshezi kanye namandla amahhala ezinhlayiyeni ezincane eziqinile, ngaleyo ndlela kuthuthukise ukuzinza kwesistimu yokuhlakazeka kwe-heterogeneous. Lo mkhiqizo uwukulungiswa koketshezi lokumiswa okuphezulu kwe-viscosity okulungiselelwe njenge-ejenti yokumisa. Inomphumela omuhle wokumisa, kulula ukuphinde uyihlakaze, inganamatheli, futhi izinhlayiya ezicolekile. Inani elijwayelekile lingu-0.5% kuya ku-1.5%.
4.4 Isetshenziswa njengesivimbeli, i-ejenti ekhulula kancane futhi elawulwayo kanye ne-ejenti eyenza izimbotshana
Ibanga le-viscosity ephezulu yalo mkhiqizo lisetshenziselwa ukulungisa amaphilisi e-hydrophilic gel matrix akhishwa ngokuqhubekayo, amaphilisi okubuyisela emuva kanye nama-ejenti akhipha okulawulwayo amaphilisi ezinto ezixubile ze-matrix akhululwa ngokuqhubekayo. Kunomphumela wokubambezela ukukhululwa kwezidakamizwa. Ukusetshenziswa kwayo ukugxila ku-10% ~ 80% (W / W). Ibanga eliphansi le-viscosity lisetshenziswa njenge-ejenti eyenza izimbotshana ekwakhiweni kokukhululwa okuqhubekayo noma okulawulwayo. Umthamo wokuqala odingekayo ukuze uthole umphumela wokwelapha walolu hlobo lwethebhulethi ungafinyelelwa ngokushesha, bese kuba umphumela wokukhululwa oqhubekayo noma olawulwayo, futhi ukugcwala kwesidakamizwa egazini okusebenzayo kugcinwa emzimbeni . I-Hypromellose hydrates ukwakha ungqimba lwejeli lapho ihlangana namanzi. Indlela yokukhishwa kwezidakamizwa kuthebhulethi ye-matrix ngokuyinhloko ukusakazeka kongqimba lwejeli kanye nokuguguleka kongqimba lwejeli.
4.5 Iglue evikelayo esetshenziswa njenge-thickener ne-colloid
Uma lo mkhiqizo usetshenziswa njenge-thickener, ukugxila okuvamile ngu-0.45% ~ 1.0%. Lo mkhiqizo ungase futhi ukwandise ukuzinza kweglue le-hydrophobic, yakha i-colloid evikelayo, ivimbele i-particle coalescence kanye ne-agglomeration, ngaleyo ndlela ivimbele ukwakheka kwama-sediments. Ukugxila kwayo okuvamile ngu-0.5% ~ 1.5%.
4.6 Isetshenziswa njenge-capsule material
Ngokuvamile, i-capsule shell material ye-capsule ngokuyinhloko i-gelatin. Inqubo yokukhiqiza igobolondo le-Ming capsule ilula, kodwa kunezinkinga ezithile nezimo ezifana nokuvikeleka kabi komswakama kanye nezidakamizwa ezizwela umoya-mpilo, ukunciphisa ukuchithwa kwezidakamizwa, nokubambezeleka kokuhlakazeka kwegobolondo le-capsule ngesikhathi sokugcinwa. Ngakho-ke, i-hypromellose isetshenziswa esikhundleni sezinto ze-capsule ekulungiseleleni ama-capsules, okuthuthukisa ukubunjwa nokusetshenziswa kwe-capsule, futhi iye yakhuthazwa kabanzi ekhaya nakwamanye amazwe.
4.7 Njenge-bioadhesive
Ubuchwepheshe be-Bioadhesive, ukusetshenziswa kwezinto ezisizayo ezinama-polymers we-bioadhesive, ngokunamathela ku-mucosa yezinto eziphilayo, kuthuthukisa ukuqhubeka nokuqina kokuxhumana phakathi kokulungiswa kanye ne-mucosa, ukuze umuthi ukhishwe kancane kancane futhi udonswe yi-mucosa ukufeza inhloso ukwelashwa. Isetshenziswa kabanzi manje Isetshenziselwa ukwelapha izifo ze-nasal cavity kanye ne-oral mucosa. Ubuchwepheshe be-gastrointestinal bioadhesion wuhlobo olusha lohlelo lokulethwa kwezidakamizwa olwakhiwe eminyakeni yamuva nje. Akugcini nje ukwandisa isikhathi sokuhlala kwamalungiselelo ezidakamizwa emgudwini wamathumbu, kodwa futhi kuthuthukisa ukusebenza kokuxhumana komuthi nge-membrane yeseli yesayithi lokumuncwa futhi ishintsha uketshezi lwe-membrane yeseli. Amandla angena omuthi kumaseli we-epithelial wamathumbu amancane ayathuthukiswa, ngaleyo ndlela athuthukise i-bioavailability yomuthi.
4.8 Njengejeli yesihloko
Njengokulungiswa okunamathelayo kwesikhumba, ijeli inochungechunge lwezinzuzo ezinjengokuphepha, ubuhle, ukuhlanza okulula, izindleko eziphansi, inqubo elula yokulungiselela, nokuhambisana okuhle nezidakamizwa. Eminyakeni yamuva, ithole ukunakwa okukhulu futhi isibe ukuthuthukiswa kwamalungiselelo angaphandle esikhumba. isiqondiso.
4.9 Njengesivimbeli semvula ohlelweni lwe-emulsification
Isikhathi sokuthumela: Dec-16-2021