Kumenyekanisha kumiterere yibanze no gukoresha imiti ya hypromellose (HPMC)

1. Imiterere shingiro ya HPMC
Hypromellose, izina ryicyongereza hydroxypropyl methylcellulose, alias HPMC. Inzira ya molekile yayo ni C8H15O8- (C10Hl8O6) n-C8Hl5O8, naho uburemere bwa molekile ni 86.000. Iki gicuruzwa nigice cya sintetike, igice cyitsinda rya methyl nigice cya polyhydroxypropyl ether ya selile. Irashobora gukorwa nuburyo bubiri: bumwe nukuvura methyl selulose yo murwego rwiza hamwe na NaOH, hanyuma ukitwara hamwe na okiside ya propylene munsi yubushyuhe bwinshi numuvuduko mwinshi. Igihe cyo kubyitwaramo kigomba gukomeza kugirango methyl na hydroxypropyl bihuze na ether. Imiterere ya ihujwe na anhydroglucose impeta ya selile, kandi irashobora kugera kurwego rwifuzwa; ikindi ni ukuvura ipamba cyangwa fibre fibre hamwe na soda ya caustic, hanyuma ukabona ukoresheje reaction ya metani ya chlorine metani na oxyde ya propylene ikurikiranye, hanyuma ukarushaho kunonosorwa, Pulverize, gukora ifu nziza kandi imwe cyangwa granule. HPMC ni selile zitandukanye ziterwa na selile, kandi nigikoresho cyiza cya farumasi, gifite isoko yagutse. Kugeza ubu, ikoreshwa henshi mu gihugu ndetse no hanze yarwo, kandi ni kimwe mu bikoresha imiti bifite umubare munini w’imiti ikoreshwa mu kanwa.

 

Ibara ryibicuruzwa byera kugeza amata yera, adafite uburozi kandi nta buryohe, kandi ni ifu ya granular cyangwa fibrous, ifu yoroshye. Irahagaze neza mugihe urumuri nubushuhe. Yabyimbye mumazi akonje kugirango ikore amata yera ya colloidal yumuti hamwe nurwego runaka rwubwiza. Ikibazo cya sol-gel gishobora kubaho bitewe nubushyuhe bwubushyuhe bwikibazo runaka. Biroroshye cyane gushonga muri 70% alcool cyangwa dimethyl ketone, kandi ntibizashonga muri alcool idasanzwe, chloroform cyangwa ethoxyethane.

Hypromellose ifite ituze ryiza mugihe pH iri hagati ya 4.0 na 8.0, kandi irashobora kubaho neza hagati ya 3.0 na 11.0. Nyuma yo kubika iminsi 10 ku bushyuhe bwa 20 ° C hamwe nubushyuhe bugereranije bwa 80%, Coefficient deux deux de HPMC ni 6.2%.

Bitewe no gutandukanya ibiri mubisimburwa byombi mumiterere ya hypromellose, mikorerexy na hydroxypropyl, ubwoko bwibicuruzwa byagaragaye. Muburyo bwihariye, ubwoko butandukanye bwibicuruzwa bifite ubukonje bwihariye nubushyuhe bwa Thermal gelation, kubwibyo, bifite ibintu bitandukanye kandi birashobora gukoreshwa mubikorwa bitandukanye. Imiti ya farumasi y’ibihugu bitandukanye ifite ibisobanuro bitandukanye n’imvugo byerekana icyitegererezo: Pharmacopoeia yu Burayi ishingiye ku byiciro bitandukanye by’imitsi itandukanye hamwe n’urwego rutandukanye rwo gusimbuza ibicuruzwa ku isoko. Byerekanwa n amanota wongeyeho umubare. Igice ni mPa • s. Nyuma yo kongeramo imibare 4 kugirango yerekane ibirimo nubwoko bwa buri kintu gisimbuza hypromellose, kurugero, hypromellose 2208, imibare ibiri yambere igereranya ijanisha ryagereranijwe ryitsinda ryimikorere, imibare ibiri yanyuma yerekana hydroxypropyl Ijanisha ryimanza.

2.Uburyo bwo gushonga HPMC mumazi

2.1 Uburyo bwamazi ashyushye

Kubera ko hypromellose idashonga mumazi ashyushye, irashobora gukwirakwizwa kimwe mumazi ashyushye mugihe cyambere, hanyuma iyo ikonje, uburyo bubiri busanzwe busobanurwa gutya:

(1) Shyira amazi asabwa muri kontineri hanyuma uyashyuhe kugeza kuri 70 ℃. Buhoro buhoro ongeramo ibicuruzwa munsi yo gukurura buhoro. Ku ikubitiro, ibicuruzwa bireremba hejuru y’amazi, hanyuma bigenda buhoro buhoro. Hisha hasi.

. kumazi ashyushye mumashanyarazi, shyira imvange nyuma yo gukurura.

2.2 Uburyo bwo kuvanga ifu
Ifu ya poro nibindi bikoresho byifu bingana cyangwa binini bikwirakwizwa rwose no kuvanga byumye, hanyuma amazi akongerwaho gushonga. Muri iki gihe, hypromellose irashobora gushonga nta agglomeration.

3. Ibyiza bya HPMC

3.1 Amazi akonje

Irashobora gushonga mumazi akonje munsi ya 40 ° C cyangwa Ethanol 70%. Ntishobora gushonga mumazi ashyushye hejuru ya 60 ° C, ariko irashobora gushonga.

3.2 Kutagira imiti

Hypromellose (HPMC) ni ubwoko bwa selile ya ionic selile. Igisubizo cyacyo ntigifite ionic kandi ntigikorana numunyu wicyuma cyangwa ibinyabuzima kama. Kubwibyo, ibindi bicuruzwa ntibabyitwaramo mugihe cyo kwitegura.

3.3 Guhagarara

Irahagaze neza kuri aside na alkali, kandi irashobora kubikwa igihe kirekire hagati ya pH 3 kugeza 1l, kandi ububobere bwayo nta mpinduka zigaragara. Igisubizo cyamazi ya hypromellose (HPMC) igira ingaruka zirwanya imiterere kandi irashobora kugumya kwihagararaho neza mugihe cyo kubika igihe kirekire. Ibikoresho bya farumasi bifashisha HPMC bifite ireme ryiza kuruta abakoresha ibicuruzwa gakondo (nka dextrin, krahisi, nibindi).

3.4 Guhindura ibishishwa

Ibikomoka kuri viscosity bitandukanye bya HPMC birashobora kuvangwa muburyo butandukanye, kandi ububobere bwayo burashobora guhinduka ukurikije amategeko runaka, kandi bukagira umubano mwiza, bityo birashobora gutoranywa ukurikije ibisabwa.

3.5 Inertia ya metabolike

HPMC ntabwo yinjizwa cyangwa ngo ihindurwe mu mubiri, kandi ntabwo itanga karori, bityo rero ni ikintu cyiza cyo gutegura imiti.

3.6 Umutekano

Muri rusange abantu bemeza ko HPMC ari ibintu bidafite uburozi kandi bidatera uburakari. Igipimo cyica hagati yimbeba ni 5g / kg, naho imiti yica imbeba ni 5.2g / kg. Igipimo cya buri munsi ntacyo cyangiza kumubiri wumuntu.

4. Gushyira mu bikorwa HPMC mu myiteguro

4.1 Ikoreshwa nkibikoresho byo gutwika firime nibikoresho byo gukora firime

Hypromellose (HPMC) ikoreshwa nkibikoresho byanditseho firime. Ugereranije n'ibinini bisanzwe bisize nk'isukari isize isukari, ibinini bisize nta nyungu zigaragara bifite mu guhisha uburyohe no kugaragara, ariko ubukana bwabyo no gukaranga, kwinjiza ibicu, gusenyuka, kwiyongera ibiro hamwe nibindi bipimo byiza ni byiza. Urwego rwo hasi-rwinshi rwibicuruzwa bikoreshwa nkibikoresho bifata amazi ya elegitoronike yifashisha ibinini n'ibinini, naho urwego rwo hejuru rwinshi rukoreshwa nkibikoresho byo gutwika firime kuri sisitemu yo gukemura ibibazo. Gukoresha kwibanda mubisanzwe ni 2.0% -20%.

4.2 nkuguhuza no gutandukana

Urwego ruto-rwinshi rwibicuruzwa rushobora gukoreshwa nkuguhuza no gutandukanya ibinini, ibinini, na granules, kandi urwego rwo hejuru rwinshi rushobora gukoreshwa gusa. Igipimo kiratandukanye nuburyo butandukanye nibisabwa. Mubisanzwe, ingano ya binder ikoreshwa kubinini byumye byumye ni 5%, naho ingano ya binder ikoreshwa kubinini bitose ni 2%.

4.3 Nkumukozi uhagarika

Guhagarika ibintu ni gel ya viscous gel ifite hydrophilicity. Gukoresha agent ihagarika muguhagarika agent birashobora kugabanya umuvuduko wimyuka yibice, kandi birashobora kwomekwa hejuru yibice kugirango birinde ibice kugirango polimerize kandi yegeranye muri misa. Guhagarika ibikorwa bigira uruhare runini mukubyara guhagarikwa. HPMC nuburyo bwiza cyane bwo guhagarika abakozi. Umuti wa colloidal ushonga muriwo urashobora kugabanya impagarara zamazi akomeye nimbaraga zidasanzwe kubice bito bito, bityo bikazamura ituze rya sisitemu yo gukwirakwiza heterogeneous. Iki gicuruzwa nigikorwa cyo guhagarika amazi menshi cyateguwe nkumukozi uhagarika. Ifite ingaruka nziza zo guhagarika, byoroshye gusubiramo, bidafatanye, nibice byiza bya flocculated. Amafaranga asanzwe ni 0.5% kugeza 1.5%.

4.4 Ikoreshwa nka blokeri, itinda kandi igenzurwa nogusohora no gukora pore

Urwego rwohejuru-rwinshi rwibicuruzwa bikoreshwa mugutegura hydrophilique gel matrix ikomeza-kurekura ibinini, retarders hamwe nigenzura-kurekura ibintu bivanze-matrike ivanze-ibisohoka. Ifite ingaruka zo gutinda kurekura ibiyobyabwenge. Ikoreshwa ryayo ni 10% ~ 80% (W / W). Urwego rwo hasi rwijimye rukoreshwa nkibikoresho byo gukora pore kugirango irekure cyangwa igenzurwa. Igipimo cyambere gisabwa kugirango ingaruka zokuvura ubu bwoko bwibinini zirashobora kugerwaho byihuse, hanyuma hagakorwa ingaruka zihoraho cyangwa zigenzurwa, kandi imiti igabanya ubukana bwamaraso ikaguma mumubiri. Hypromellose hydrates kugirango ikore geli iyo ihuye namazi. Uburyo bwo kurekura ibiyobyabwenge muri tablet ya matrix ahanini ni ikwirakwizwa rya gel hamwe nisuri ya gel.

4.5 Gukingira kole ikoreshwa nkibyimbye na colloid

Iyo ibicuruzwa bikoreshejwe nkibyimbye, ibisanzwe bisanzwe ni 0.45% ~ 1.0%. Iki gicuruzwa kirashobora kandi kongera ituze rya hydrophobe glue, gukora colloid ikingira, ikarinda uduce duto duto hamwe na agglomeration, bityo bikabuza gushinga imyanda. Ubusanzwe kwibanda kwayo ni 0.5% ~ 1.5%.

4.6 Byakoreshejwe nkibikoresho bya capsule

Mubisanzwe, capsule shell material ya capsule ahanini ni gelatine. Igikorwa cyo gukora ibishishwa bya Ming capsule biroroshye, ariko haribibazo bimwe na bimwe nko kurinda nabi ubushuhe n’ibiyobyabwenge byangiza ogisijeni, kugabanya ibiyobyabwenge, no gutinda gusenyuka kwa capsule mugihe cyo kubika. Kubwibyo, hypromellose ikoreshwa nkigisimbuza ibikoresho bya capsule mugutegura capsules, itezimbere imiterere nogukoresha ingaruka za capsule, kandi yazamuwe cyane mugihugu ndetse no mumahanga.

4.7 Nka bioadhesive

Ikoranabuhanga rya Bioadhesive, gukoresha ibibyimba hamwe na polyaderi ya bioadhesive, mugukurikiza mucosa yibinyabuzima, byongera ubudahwema nubukomezi bwimikoranire hagati yimyiteguro na mucosa, kuburyo imiti irekurwa buhoro buhoro kandi ikinjizwa na mucosa kugirango igere ku ntego yo kwivuza. Irakoreshwa cyane ubu Ikoreshwa mukuvura indwara zifata izuru na mucosa yo mu kanwa. Gastrointestinal bioadhesion tekinoroji ni ubwoko bushya bwa sisitemu yo gutanga ibiyobyabwenge byakozwe mumyaka yashize. Ntabwo yongerera igihe cyo gutura gusa imiti yo gutegura ibiyobyabwenge mu nzira ya gastrointestinal, ahubwo inatezimbere imikorere yimiti yibiyobyabwenge hamwe na selile ya selile yinjira kandi ihindura amazi ya membrane selile. Imbaraga zinjira mumiti kuri selitile epithelial selile y amara mato arongerwa, bityo bikazamura bioavailable yibiyobyabwenge.

4.8 Nka gele yibanze

Nukwifata neza kuruhu, gel ifite urukurikirane rwibyiza nkumutekano, ubwiza, isuku yoroshye, igiciro gito, inzira yoroshye yo gutegura, hamwe no guhuza neza nibiyobyabwenge. Mu myaka yashize, byitabweho cyane kandi byahindutse iterambere ryuruhu rwitegura hanze. icyerekezo.

4.9 Nka inhibitori yimvura muri sisitemu ya emulisation


Igihe cyo kohereza: Ukuboza-16-2021