1. Hunhu hwakakosha hweHPMC
Hypromellose, Chirungu zita hydroxypropyl methylcellulose, arias HPMC. Yayo molecular formula ndeye C8H15O8-(C10Hl8O6)n-C8Hl5O8, uye huremu hwemamorekuru hunosvika 86,000. Ichi chigadzirwa isemi-synthetic material, inova chikamu cheboka remethyl uye chikamu che polyhydroxypropyl ether ye cellulose. Inogona kugadzirwa nenzira mbiri: imwe ndeyekurapa methyl cellulose yegiredhi yakakodzera neNaOH, uyezve kuita nepropylene oxide pasi pekupisa kwakanyanya uye kudzvanywa kwakanyanya. Iyo nguva yekuita inofanirwa kutsigirwa kuti ibvumidze methyl uye hydroxypropyl mapoka kuti abatane ne ether. Iyo fomu ye yakabatana kune anhydroglucose mhete ye cellulose, uye inogona kusvika painodiwa dhigirii; imwe yacho kurapa donje linter kana huni pulp fiber ine caustic soda, uye wobva wawana nekuita neklorini methane uye propylene oxide zvakateerana, uye wozowedzera kunatswa, Pulverize, ita muhupfu hwakatsetseka uye hwakafanana kana granule. HPMC yakasiyana-siyana yechisikigo chirimwa cellulose, uye zvakare yakanakisa mishonga yemishonga, ine yakafara sosi. Parizvino, inoshandiswa zvakanyanya kumba nekune dzimwe nyika, uye ndeimwe yevabatsiri vemishonga ine chiyero chepamusoro chekushandisa pakati pemishonga yemuromo.
Rudzi rwechigadzirwa ichi rwakachena kune mukaka chena, rusina chepfu uye rusina kunaka, uye iine granular kana fibrous, nyore-kuyerera poda. Yakagadzikana pasi pechiedza uye hunyoro. Inoputika mumvura inotonhora kuti iite mukaka chena colloidal solution ine imwe dhigirii ye viscosity. Iyo sol-gel interconversion phenomenon inogona kuitika nekuda kwekushanduka kwekushisa kweimwe kusangana kwemhinduro. Zviri nyore kwazvo kunyungudika mu70% doro kana dimethyl ketone, uye haizonyungudika muanhydrous doro, chloroform kana ethoxyethane.
Hypromellose ine kugadzikana kwakanaka kana pH iri pakati pe4.0 ne8.0, uye inogona kuvapo yakagadzikana pakati pe3.0 ne11.0. Mushure mekuchengetedza kwemazuva gumi pane tembiricha ye20 ° C uye hunyoro hunoenderana ne80%, Hunyoro hwekunyudza coefficient yeHPMC i6.2%.
Nekuda kwekusiyana kwezviri mukati mezviviri zvinotsiva muchimiro che hypromellose, methoxy uye hydroxypropyl, marudzi akasiyana ezvigadzirwa akaonekwa. Mune yakatarwa, mhando dzakasiyana dzezvigadzirwa zvine chaiyo viscosity uye Thermal gelation tembiricha, saka, ine zvakasiyana zvivakwa uye inogona kushandiswa kune zvakasiyana zvinangwa. Iyo pharmacopoeias yenyika dzakasiyana siyana ine zvakatemerwa uye mataurirwo emuenzaniso: Iyo European Pharmacopoeia yakavakirwa pamagiredhi akasiyana eiyo akasiyana viscosities uye akasiyana madhigirii ekutsiva zvigadzirwa pamusika. Inoratidzwa negiredhi nenhamba. Iyo unit ndeye mPa•s. Mushure mekuwedzera manhamba ekuratidza zvirimo uye rudzi rwechimwe nechimwe chinotsiva hypromellose, semuenzaniso, hypromellose 2208, manhamba maviri ekutanga anomiririra inofungidzirwa muzana yeboka remethoxy, manhamba maviri ekupedzisira anomiririra hydroxypropyl Inosvika muzana yemakesi.
2.Nzira yekupedza HPMC mumvura
2.1 Mvura inopisa nzira
Sezvo hypromellose isinganyungudika mumvura inopisa, inogona kuparadzirwa zvakafanana mumvura inopisa padanho rekutanga, uyezve kana yatonhodzwa, nzira mbiri dzakajairwa dzinotsanangurwa seizvi:
(1) Isa huwandu hunodiwa hwemvura inopisa mumudziyo uye kupisa kusvika ku70 ℃. Zvishoma nezvishoma wedzera chigadzirwa pasi pekugadzirisa zvishoma nezvishoma. Pakutanga, chigadzirwa chinoyangarara pamusoro pemvura, uye zvishoma nezvishoma chinoumba slurry. Dzorera pasi slurry.
(2) Wedzera 1/3 kana 2/3 yehuwandu hunodiwa hwemvura mumudziyo uye kupisa kusvika 70 ° C kuparadzira chigadzirwa kugadzirira mvura inopisa slurry, uye wobva wawedzera huwandu hwasara hwemvura inotonhora kana mvura yechando. kumvura inopisa slurry Mu slurry, tonhorera musanganiswa mushure mekusimudzira.
2.2 Poda yekusanganisa nzira
Zvimedu zvehupfu uye zvimwe zvigadzirwa zvehupfu zvakaenzana kana zvakakura zvakaparadzirwa zvizere nekusanganiswa kwakaoma, uye ipapo mvura inowedzerwa kunyungudika. Panguva ino, iyo hypromellose inogona kunyungudika pasina agglomeration.
3. Zvakanakira HPMC
3.1 Kunyungudika kwemvura inotonhora
Inonyungudika mumvura inotonhora iri pasi pe40°C kana 70% ethanol. Iyo haina kunyungudika mumvura inopisa inopfuura 60 ° C, asi inogona kugadzirwa.
3.2 Kemikari inertness
Hypromellose (HPMC) imhando isiri-ionic cellulose ether. Mhinduro yayo haina ionic charge uye haidyidzane nesimbi yemunyu kana ionic organic compounds. Naizvozvo, zvimwe zvinokonzeresa hazviite nazvo panguva yekugadzirira.
3.3 Kugadzikana
Iyo yakanyatsogadzikana kune ese acid uye alkali, uye inogona kuchengetwa kwenguva yakareba pakati pepH 3 kusvika 1l, uye viscosity yayo haina shanduko yakajeka. Iyo aqueous solution ye hypromellose (HPMC) ine anti-mold effect uye inogona kuchengetedza yakanaka viscosity kugadzikana panguva yekuchengetedza kwenguva refu. Mishonga yemishonga inoshandisa HPMC ine kugadzikana kwemhando iri nani pane iyo inoshandisa zvechinyakare excipients (senge dextrin, starch, nezvimwewo).
3.4 Kugadziriswa kwe viscosity
Different viscosity derivatives yeHPMC inogona kusanganiswa muzvikamu zvakasiyana, uye viscosity yayo inogona kuchinja maererano nemumwe mutemo, uye ine hukama hwakanaka hwemutsara, saka inogona kusarudzwa maererano nezvinodiwa.
3.5 Metabolic inertia
HPMC haina kunyura kana metabolized mumuviri, uye haipi macalorie, saka yakachengeteka excipient yemishonga kugadzirira.
3.6 Chengetedzo
Zvinowanzotendwa kuti HPMC haisi-chepfu uye isingatsamwire zvinhu. Mushonga unouraya wepakati wemakonzo i5g/kg, uye muyero wepakati unouraya wemakonzo i5.2g/kg. Chiyero chezuva nezuva hachina ngozi kumuviri wemunhu.
4. Kushandiswa kweHPMC mukugadzirira
4.1 Inoshandiswa semafirimu ekuputira zvinhu uye firimu rekugadzira zvinhu
Hypromellose (HPMC) inoshandiswa sefirimu-yakavharwa piritsi zvinhu. Kuenzaniswa nemapiritsi echinyakare akavharidzirwa akadai semapiritsi akaputirwa neshuga, mahwendefa akaputirwa haana zvakanakira kuvharidzira kuravira uye chitarisiko, asi kuoma kwavo uye friability , Kunyura kwehunyoro, kuparara, kuvhara uremu kuwedzera uye zvimwe zviratidzo zvemhando zviri nani. Iyo yakaderera-viscosity giredhi yechigadzirwa ichi inoshandiswa semvura-inonyungudika firimu yekuputira zvinhu zvemapiritsi nemapiritsi, uye iyo yepamusoro-viscosity giredhi inoshandiswa seyakaputira firimu zvinhu zveorganic solvent masisitimu. Iko kushandiswa kusungirirwa kunowanzo 2.0% -20%.
4.2 sebhainda uye disintegrant
Iyo yakaderera-viscosity giredhi yechigadzirwa ichi inogona kushandiswa sebhainda uye disintegrant yemapiritsi, mapiritsi, uye granules, uye yakakwirira-viscosity giredhi inogona kungoshandiswa sebhainda. Chiyero chinosiyana nemhando dzakasiyana uye zvinodiwa. Kazhinji, huwandu hwebhainda hunoshandiswa pamahwendefa akaoma egranulation i5%, uye huwandu hwebinder hunoshandiswa kunyorova mahwendefa i2%.
4.3 Semumiriri wekumisa basa
Suspending agent is viscous gel substance ine hydrophilicity. Iko kushandiswa kwekumisa mumiriri mukumisa mumiriri kunogona kudzikamisa kukurumidza kwesedimentation yezvimedu, uye inogona kusungirirwa pamusoro pezvimedu kudzivirira zvimedu kubva ku polymerizing uye kunyungudika kuita misa. Kumisa maajenti anoita basa rakakosha mukugadzirwa kwekumiswa. HPMC yakanakisa siyana yekumisa vamiririri. Iyo colloidal solution yakanyungudutswa mairi inogona kuderedza tension ye-liquid-solid interface uye simba rekusununguka pane zviduku zvakasimba, zvichiita kuti kugadzikana kweiyo heterogeneous dispersion system. Ichi chigadzirwa chepamusoro-viscosity kumiswa kwemvura yekugadzirira yakagadzirirwa semumiriri wekumisa. Iyo ine yakanaka kumisa mhedzisiro, iri nyore kuparadzira, isina kunamira, uye yakanaka flocculated zvimedu. Mari yakajairika ndeye 0.5% kusvika 1.5%.
4.4 Inoshandiswa sevhavha, inononoka uye inodzorwa kuburitsa mumiririri uye pore-inogadzira agent
Iyo yepamusoro-viscosity giredhi yechigadzirwa ichi inoshandiswa kugadzirira hydrophilic gel matrix inosimudzira-kuburitswa mahwendefa, retarders uye inodzorwa-yekuburitsa maajenti eakasanganiswa-material matrix akatsigira-kuburitswa mahwendefa. Iine mhedzisiro yekunonoka kuburitswa kwezvinodhaka. Iko kushandiswa kwayo kwe10% ~ 80% (W / W). Iyo yakaderera viscosity giredhi inoshandiswa sepore-inogadzira mumiriri kune yakatsiga kana yakadzora kuburitsa maumbirwo. Mushonga wekutanga unodiwa pakurapa kwerudzi urwu rwepiritsi unogona kukurumidza kusvika, uye ipapo inotsigirwa kana inodzorwa kuburitsa mhedzisiro inoitwa, uye inoshanda yeropa zvinodhaka zvinochengetwa mumuviri. Hypromellose hydrates kuumba gel layer kana yasangana nemvura. Iyo nzira yekusunungurwa kwezvinodhaka kubva pahwendefa rematrix inonyanya kupararira kwejel layer uye kuputika kwejeri.
4.5 Inodzivirira glue inoshandiswa seyakakora uye colloid
Kana chigadzirwa ichi chikashandiswa seyakakora, iyo yakajairwa fungidziro ndeye 0.45% ~ 1.0%. Ichi chigadzirwa chinogona zvakare kuwedzera kugadzikana kweiyo hydrophobic glue, kuumba inodzivirira colloid, kudzivirira particle coalescence uye agglomeration, nekudaro ichitadzisa kuumbwa kwesediments. Yayo yakajairwa fungidziro ndeye 0.5% ~ 1.5%.
4.6 Inoshandiswa se capsule zvinhu
Kazhinji, iyo capsule shell zvinhu zve capsule inonyanya gelatin. Maitiro ekugadzirwa kweMing capsule shell ari nyore, asi kune mamwe matambudziko uye zviitiko senge kusachengetedzwa kwemwando uye mweya weokisijeni zvinodhaka, kuderedzwa kwekuparara kwezvinodhaka, uye kunonoka kuparara kwegomba recapsule panguva yekuchengetedza. Naizvozvo, hypromellose inoshandiswa sechinotsiva iyo capsule zvinhu mukugadzirira kwe capsules, iyo inovandudza kuumbwa uye kushandiswa kweiyo capsule, uye yakasimudzirwa zvakanyanya kumba nekune dzimwe nyika.
4.7 Se bioadhesive
Bioadhesive tekinoroji, kushandiswa kwezvinobatsira zvine bioadhesive polymers, nekunamatira kune biological mucosa, inosimudzira kuenderera uye kusimba kwekubatana pakati pekugadzirira uye mucosa, kuitira kuti mushonga usunungurwe zvishoma nezvishoma uye ubatwe nemucosa kuzadzisa chinangwa kurapwa. Inoshandiswa zvakanyanya ikozvino Inoshandiswa kurapa zvirwere zvemhino yemhino uye mucosa yemuromo. Gastrointestinal bioadhesion tekinoroji rudzi rutsva rwekuburitsa zvinodhaka system yakagadziriswa mumakore achangopfuura. Izvo hazvingorebesi nguva yekugara yekugadzirira kwezvinodhaka mudumbu remukati, asi zvakare inovandudza kusangana kwemushonga nesero membrane yenzvimbo yekunyura uye inoshandura kuyerera kwesero membrane. Simba rinopinda remushonga kune epithelial masero emudumbu muduku anowedzerwa, nokudaro achivandudza bioavailability yemushonga.
4.8 Sejeri remusoro
Segadziriro yekunamatira yeganda, gel ine nhevedzano yezvakanakira senge chengetedzo, runako, nyore kuchenesa, mutengo wakaderera, nyore kugadzirira maitiro, uye kuenderana kwakanaka nemishonga. Mumakore achangopfuura, yakagamuchira kutariswa kwakanyanya uye yakave kugadzirwa kweganda kunze kwekugadzirira. direction.
4.9 Semvura inhibitor mune emulsification system
Nguva yekutumira: Zvita-16-2021