1. Imvelo eyisisekelo ye-HPMC
I-Hypromellose, igama lesiNgisi igama hydroxyproppropyl methylcellulose, alias hpmc. Ifomula yayo yamangqamuzana yi-C8H15O8- (C10HL8O6) N-C8HL5O8, futhi isisindo samangqamuzana singaba ngu-86,000. Lo mkhiqizo yinto esetshenziswayo ye-semi-zokwenziwa, eyingxenye ye-methyl group nengxenye yePolyhydroxypropylylllllylylylylylylylylylylylylylylll ether of cellulose. Kungenziwa ngezindlela ezimbili: eyodwa ukwelapha i-methyl cellulose yebanga elifanele nge-naoh, bese usabela nge-oxylene oxide ngaphansi kokushisa okuphezulu kanye nengcindezi ephezulu. Isikhathi sokuphendula kumele sigcinwe ukuvumela amaqembu we-methylypropyl ahlanganise ne-ether. Uhlobo lokuxhumeka kwindandatho ye-anhydroglucose ye-cellulose, futhi ingafinyelela ngezinga elifunekayo; Okunye ukwelapha i-lictric yekotini noma i-file ye-solip ene-caustic soda, bese uthola ngokuphendula nge-methane e-cherleated ne-opylene oxide ngokulandelana, bese ucoca futhi, yenza i-powder noma umfaniswano noma umfaniswano noma umfaniswano noma umfaniswano noma umfaniswano noma umfaniswano. I-HPMC iyinqwaba yezitshalo zemvelo ze-cellulose yemvelo, futhi futhi iyi-excipieint enhle kakhulu yezemithi, enomthombo obanzi. Njengamanje, kusetshenziswa kabanzi ekhaya nakwamanye amazwe, futhi kungenye ye-Excipietietieticals yezemithi ngezinga eliphakeme kakhulu lokusetshenziswa phakathi kwezidakamizwa zomlomo.
Umbala walo mkhiqizo umhlophe ku-Milky White, ungeyena ubuthi futhi awunambitheki, futhi kuyimpuphu ye-granular noma ye-fibrous, egeleza kalula. Kuzinzile ngaphansi kokuvezwa kokukhanya kanye nomswakama. Kuyavuvukala emanzini abandayo ukwakha isixazululo esimhlophe se-milky emhlophe ngezinga elithile lokubonakala. I-Sol-Gel InterconVersion Penomenon ingenzeka ngenxa yokushintshwa kokushisa kwesixazululo esithile. Kulula kakhulu ukuncibilikisa ngo-70% utshwala noma i-dimethyl ketone, futhi ngeke ichithe e-anhydrove adhobal, chloroform noma e-ethoxosethane.
I-Hypromellose inokuqina okuhle lapho i-pH iphakathi kuka-4.0 no-8.0, futhi ingaba khona ngokungxekile phakathi kuka-3.0 no-11.0. Ngemuva kokugcina izinsuku eziyi-10 ekushiseni okungu-20 ° C kanye nomswakama ohlobene ka-80%, i-michitha amuncy coufficient ye-HPMC ingu-6.2%.
Ngenxa yomehluko kokuqukethwe kwabanye okufakwa esikhundleni kwesakhiwo se-hypromellose, i-methoxy ne-hydroxypropyl, kwavela izinhlobo ezahlukahlukene zemikhiqizo. Oqongweni oluthile, izinhlobo ezahlukahlukene zemikhiqizo zinokuvunywa okuthile nokushisa okushisayo okushisayo, inezindawo ezahlukahlukene futhi zingasetshenziselwa izinhloso ezihlukile. I-pharmacopoeis yamazwe ahlukahlukene inemininingwane ehlukile nezinkulumo zemodeli: I-European Pharmacopoeia isuselwe kumabanga ahlukahlukene we-viscosities ahlukene kanye namazinga ahlukene wokufaka esikhundleni semikhiqizo emakethe. Kuvezwa yibanga kanye nenombolo. Iyunithi yi-MPA • s. Ngemuva kokungeza amadijithi ama-4 ukukhombisa okuqukethwe nohlobo lwe-propromeent ngayinye ye-hypromellose, isibonelo, i-hypromeellose 2208, amadijithi amabili okuqala amelela amaphesenti alinganiselwane we-methoxy, amadijithi amabili okugcina amelela amaphesenti acishe alinganiselayo.
2.Indlela yokuqeda i-HPMC echithwa emanzini
2.1 Indlela Eshisayo Yamanzi
Njengoba i-Hypromellose ayichithi emanzini ashisayo, ingahlakazeka ngendlela efanayo emanzini ashisayo esiteji sokuqala, bese kuthi lapho sekupholile, izindlela ezimbili ezijwayelekile zichazwa ngale ndlela elandelayo:
(1) Beka inani elidingekayo lamanzi ashisayo esitsheni bese usishisa cishe ku-70 ℃. Kancane kancane engeza umkhiqizo ngaphansi kokuvuselelwa kancane. Ekuqaleni, umkhiqizo uyantanta ebusweni bamanzi, bese kancane kancane wakha i-slurry. Pholisa phansi i-slurry.
(2) engeza u-1/3 noma 2/3 wenani elidingekayo lamanzi esitsheni bese usishisa ku-70 ° C ukuhlakaza umkhiqizo ukuze uhambise i-slurry yamanzi eshisayo, bese wengeza inani elisele lamanzi abandayo noma amanzi eqhwa Kuya kuma-slurry amanzi ashisayo ku-slurry, upholise ingxube ngemuva kokuvusa.
2.2 Indlela yokuxuba nje ye-powder
Izinhlayiya ze-powder nezinye izithako eziyimpuphu zenani elilinganayo noma elikhudlwana zihlakazeka ngokugcwele ngokuxubana owomile, bese kufakwa amanzi ukuze ancibilike. Ngalesi sikhathi, i-Hypromellose ingachithwa ngaphandle kokuqothuka.
3. Izinzuzo ze-HPMC
3.1 I-SOLUBO YAMANZI
Kuyancibilika emanzini abandayo ngaphansi kwama-40 ° C noma 70% ethanol. Ngokuyisisekelo insoluble emanzini ashisayo ngenhla kwama-60 ° C, kepha ingagcinwa.
I-3.2 inertertness
I-Hypromellose (HPMC) uhlobo lwe-ether engeyona eye-cellulose. Isixazululo saso asinakho ukukhokhiswa kwe-ionic futhi akuhlangani nosawoti wensimbi noma amakhompiyutha we-onic arganic. Ngakho-ke, amanye ama-Excipients awaphenduli nakho ngesikhathi senqubo yokulungiselela.
3.3 Ukuqina
Kuzinzile ku-acid ne-alkali, futhi kungagcinwa isikhathi eside phakathi kwe-ph 3 kuya ku-1l, futhi ukubonakala kwayo akunalo ushintsho olusobala. Isixazululo samanzi se-hppromellose (HPMC) sinomphumela wokulwa nokulwa futhi sikwazi ukugcina ukuqina okuhle kwentokozo ngesikhathi sokugcina isikhathi eside. Ama-Executieints Ezemithi asebenzisa i-HPMC anokuqina okungcono kwekhwalithi kunaleyo esebenzisa ama-excipients wendabuko (njenge-dextrin, isitashi, njll.).
3.4 Ukuguqulwa kwe-viscosity
Ukutholwa okuhlukile kwe-viscosives ye-HPMC kungahlanganiswa ngezilinganiso ezihlukile, futhi ukubonakala kwayo kungashintsha ngokuya ngomthetho othile, futhi kunobudlelwano obuhle obuhle, ngakho-ke kungakhethwa ngokuya ngezidingo.
3.5 Metabolic inertia
I-HPMC ayimuzwanga noma i-metabolized emzimbeni, futhi ayinikezi amakhalori, ngakho-ke kuyinto ephephile ephephile yamalungiselelo okwelapha.
3.6 Ezokuphepha
Ngokuvamile kukholelwa ukuthi i-HPMC iyinto engeyona enobuthi futhi engacasuli. Umthamo obulala amagundane amagundane yi-5G / kg, kanti umthamo obulalayo obulalayo wamagundane ngu-5.2g / kg. Umthamo wansuku zonke awunangozi emzimbeni womuntu.
4. Ukusetshenziswa kwe-HPMC kumalungiselelo
I-4.1 isetshenziswe njengezinto zokuhlanganisa amafilimu kanye nefilimu eyakha izinto ezibonakalayo
I-Hypromellose (HPMC) isetshenziswa njengezinto zethebhulethi ezihlanganisiwe zefilimu. Uma kuqhathaniswa namathebhulethi ahlanganisiwe endabuko afana namathebhulethi anoshukela, amaphilisi ahlanganisiwe awanazo izinzuzo ezisobala ekufihleni ukunambitheka nokubukeka, kepha ubulukhuni bawo, ukukhishwa kwawo, ukuncishiswa, ukuhlukaniswa kwesisindo, ezinye izinkomba zekhwalithi zingcono. Ibanga eliphansi le-viscosity yalo mkhiqizo lisetshenziswa njengezinto ezisetshenziswayo zefilimu ezingenamanzi zamathebulethi kanye namaphilisi, futhi ibanga eliphakeme le-vivecosity lisetshenziswa njengezinto zokuhlanganisa amafilimu ze-Organic Solvent Systems. Ukuhlushwa ukusetshenziswa kuvame ukuba ngu-2.0% -20%.
4.2 Njenge-binder nokuqhekeka
Ibanga eliphansi le-viscosity alo mkhiqizo lingasetshenziswa njenge-binder nokuqhekeka kwamathebulethi, amaphilisi kanye nama-granule, kanye nebanga eliphakeme elivelayo lingasetshenziswa kuphela njenge-binder. Umthamo uyahlukahluka ngamamodeli ahlukile nezidingo. Ngokuvamile, inani le-binder elisetshenziselwe amaphilisi e-granung alomile lingama-5%, futhi inani le-binder elisetshenziselwa amaphilisi we-granung angu-2%.
I-4.3 njenge-ejenti yokumisa okwesikhashana
I-ejenti esomisayo iyinto ye-gel ye-viscous nge-hydrophility. Ukusetshenziswa kwe-ejenti okumisiwe kuma-ejenti okumisa ama-ejenti kunganciphisa ijubane ledimentation yezinhlayiya, futhi kungahle kufakwe ebusweni bezinhlayiya ukuvikela izinhlayiya kusuka ku-polymerizing kanye nokuguqula inqwaba. Ama-ejenti asolayo adlala indima ebalulekile ekukhiqizweni kokumihlela. I-HPMC iyizinhlobonhlobo ezinhle kakhulu zokumisa ama-ejenti. Isixazululo seColloidal sincibilike kuso singanciphisa ukungezwani kwesibonisi esiqinile se-liquid-solid kanye namandla amahhala ezinhlayiyeni ezincane eziqinile, ngaleyo ndlela uthuthukise ukuqina kohlelo lokuhlakazeka kwe-heterogeneous. Lo mkhiqizo ukumiswa okuphezulu kokumiswa koketshezi okulungiselelwe njenge-ejenti okumisiwe. Inokusamisa okuhle okulandelayo, kulula ukuhlela kabusha, izinhlayiya ezingenamkhawulo, nezinhlanzi ezinhle ze-Flecculated. Inani elijwayelekile lingu-0.5% kuye ku-1.5%.
I-4.4 isetshenziswe njenge-blocker, i-ejenti yokukhishwa ehamba kancane nelawulwa ne-alent ekwakhekeni
Ibanga eliphakeme le-viscosity kulo mkhiqizo lisetshenziselwa ukulungiselela amaphilisi we-hydrophilic gel matrix amathebulethi okukhishwa kwama-hydrophilic, ama-retaarders kanye nama-ejenti wokukhishwa alawulwayo amathebhulethi ahlanganisiwe asetshenzisiwe. Inomphumela wokubambezela ukukhishwa kwezidakamizwa. Ukuhlushwa kwayo ukusetshenziswa kwayo kungu-10% ~ 80% (W / W). Ibanga eliphansi le-viscosity lisetshenziswa njenge-ejenti eyakha ama-ajenti yokwakheka okuqhubekayo noma okulawulwayo. I-DOSE yokuqala edingekayo yezokwelapha yalolu hlobo lwethebhulethi ingafinyelelwa ngokushesha, bese kuba khona umphumela wokukhishwa oqinile noma olawulwayo, futhi okuhlushwa izidakamizwa ezisebenzayo zegazi kuyagcinwa emzimbeni. IHypromellose Hydrate ukwakha ungqimba lwejeli lapho ihlangana namanzi. Indlela yokukhishwa kwezidakamizwa kusuka kuthebhulethi ye-matrix ikakhulukazi ingukuphazamiseka kwe-gel ungqimba kanye nokuguguleka kwe-gel ungqimba.
4.5 I-glue evikela isetshenziswa njenge-reatriner ne-colloid
Lapho lo mkhiqizo usetshenziswa njengoqweqwe, okuhlushwa okujwayelekile kungu-0.45% ~ 1.0%. Lo mkhiqizo ungaphinde ukhuphule ukuqina kwe-hydrophobic glue, wakhe i-colloid evikelayo, ukuvimbela izinhlayiya zama-coalescence ne-agglomeration, ngaleyo ndlela kuvimbela ukwakheka kwama-sedimentnts. Ukuhlushwa kwayo okujwayelekile kungu-0.5% ~ 1.5%.
4.6 isetshenziswe njenge-capsule impahla
Imvamisa, i-capsule Shell impahla ye-capsule ikakhulukazi i-gelatin. Inqubo yokukhiqiza ye-Ming Capsule Shell ilula, kepha kukhona ezinye izinkinga nezimo ezinjengokuvikelwa kabi kwemithi yomswakama kanye nokuvikelwa kwezidakamizwa, nokuncipha kokuncishiswa kwezidakamizwa, nokubambezeleka kokuhlakazeka kwe-capsule Shell ngesikhathi sesitoreji. Ngakho-ke, i-Hypromellose isetshenziswa esikhundleni se-capsule impahla lapho kulungiswa ama-caplule, athuthukisa ukuphambana kanye nokusebenzisa umphumela we-capsule, futhi kukhushulwe kakhulu ekhaya nakwamanye amazwe.
4.7 njenge-bioaphesive
Ubuchwepheshe beBioasesive, ukusetshenziswa kwe-Excipients nge-Biodhesive Polymers, ngokunamathela ekuqhubekeni kwemvelo, ukuqina koxhumana naye phakathi kokulungiselela kanye ne-mucosa, ukuze umuthi yi-mucosa kancane futhi umunwe yi-mucosa ukufeza inhloso ye ukwelashwa. Kusetshenziswa kabanzi manje kusetshenziselwa ukwelapha izifo ze-nasal cavity kanye ne-mucosa yomlomo. Ubuchwepheshe be-Gettrointesinal Biofiosion ubuchwepheshe buhlobo olusha lohlelo lokulethwa kwezidakamizwa oluthuthukisiwe eminyakeni yamuva. Akugcini nje kuphela isikhathi sokuhlala samalungiselelo ezidakamizwa epheshana lesisu, kodwa futhi kuthuthukisa ukusebenza komuthi womuthi nolwelwesi lwamaseli wesayithi lokutholwa futhi kushintsha uketshezi lwe-fluane yeseli. Amandla angenayo wesidakamizwa kumaseli e-epithelial wesisu esincane ayathuthukiswa, ngaleyo ndlela athuthukise ukungatholakali kwe-bioavailability yomuthi.
4.8 njengejeli eliphakeme
Njengokulungiselela okunamathelayo kwesikhumba, i-gel inochungechunge lwezinzuzo ezinjengokuphepha, ubuhle, ukuhlanza okulula, izindleko eziphansi, inqubo elula yokulungiselela, kanye nokuhambisana okuhle nezidakamizwa. Eminyakeni yamuva, ithole ukunakwa kakhulu futhi sekuphenduke ukuthuthukiswa kwamalungiselelo angaphandle wesikhumba. ukuqondisa.
I-4.9 njenge-levilitor ye-Precipitation ohlelweni lwe-emulsification
Isikhathi sePosi: Dec-16-2021