1. Hunhu hweHPMC
Hypromellose, zita rechirungu rekuti hydroxypropyl methylcellulose, zita rekuti HPMC. Fomura yayo yemamorekuru iC8H15O8-(C10Hl8O6)n-C8Hl5O8, uye huremu hwemamorekuru hunosvika 86,000. Chigadzirwa ichi chinhu chinogadzirwa nesemi-synthetic, chiri chikamu cheboka remethyl uye chikamu chepolyhydroxypropyl ether yecellulose. Chinogona kugadzirwa nenzira mbiri: imwe ndeyekurapa methyl cellulose yemhando yakakodzera neNaOH, uye wobva waita nepropylene oxide pasi pekupisa kwakanyanya uye kumanikidzwa kwakanyanya. Nguva yekuita inofanira kuenderera mberi kuti mapoka emethyl nehydroxypropyl abatane ne ether. Chimiro chechinhu ichi chakabatana neanhydroglucose ring ye cellulose, uye chinogona kusvika padanho rinodiwa; imwe ndeyekurapa cotton linter kana wood pulp fiber ne caustic soda, uye wobva wawana nekuita ne chlorinated methane ne propylene oxide zvakateerana, wobva wanyatso gadziriswa, Pulverize, woita upfu hwakanaka kana humwechete. HPMC imhando ye cellulose yezvirimwa zvechisikigo, uye zvakare imushonga wakanaka kwazvo wemishonga, une tsime rakakura. Parizvino, inoshandiswa zvakanyanya kumba nekune dzimwe nyika, uye ndeimwe yemushonga unoshandiswa zvakanyanya pakati pemishonga inonwiwa.
Ruvara rwechigadzirwa ichi ruchena kusvika kuchena semukaka, haruna chepfu uye haruna kunaka, uye ihupfu hwakaita segranular kana fibrous, hunoyerera zviri nyore. Hunogara zvakanaka kana huchionekwa nechiedza uye hunyoro. Hunozvimba mumvura inotonhora kuti hugadzire mushonga wecolloidal wakachena semukaka une mwero wakati we viscosity. Chiitiko che sol-gel interconversion chinogona kuitika nekuda kwekuchinja kwekushisa kwehuwandu hwakati hwemushonga. Zviri nyore kwazvo kunyungudika mu 70% alcohol kana dimethyl ketone, uye hahunyungudike mu anhydrous alcohol, chloroform kana ethoxyethane.
Hypromellose ine kugadzikana kwakanaka kana pH iri pakati pe4.0 ne8.0, uye inogona kugara zvakanaka pakati pe3.0 ne11.0. Mushure mekuchengeta kwemazuva gumi patembiricha ye20°C uye hunyoro hwe80%, chiyero chekunwa hunyoro cheHPMC i6.2%.
Nekuda kwekusiyana kwezviri mukati mezvinhu zviviri zvinotsiva muchimiro chehypromellose, methoxy uye hydroxypropyl, mhando dzakasiyana dzezvigadzirwa dzakaonekwa. Mune huwandu hwakasiyana, mhando dzakasiyana dzezvigadzirwa dzine viscosity chaiyo uye tembiricha yekupisa, saka, ine hunhu hwakasiyana uye inogona kushandiswa kune zvinangwa zvakasiyana. Mishonga yenyika dzakasiyana ine zvirevo zvakasiyana uye matauriro emuenzaniso: European Pharmacopoeia yakavakirwa pamagiredhi akasiyana e viscosities akasiyana uye madhigirii akasiyana ekutsiva zvigadzirwa zviri pamusika. Inoratidzwa negiredhi pamwe nenhamba. Yuniti yacho i mPa•s. Mushure mekuwedzera manhamba mana kuratidza zviri mukati uye rudzi rwechimwe nechimwe chinotsiva hypromellose, semuenzaniso, hypromellose 2208, manhamba maviri ekutanga anomiririra chikamu chinofungidzirwa cheboka re methoxy, manhamba maviri ekupedzisira anomiririra hydroxypropyl. Inenge chikamu chezviitiko.
2. Nzira yekunyungudutsa HPMC mumvura
2.1 Nzira yemvura inopisa
Sezvo hypromellose isinganyungudike mumvura inopisa, inogona kuparadzirwa zvakaenzana mumvura inopisa pakutanga, uye kana yatonhodzwa, nzira mbiri dzakajairika dzinotsanangurwa seinotevera:
(1) Isa mvura inopisa inodiwa mumudziyo woipisa kusvika pa70℃. Wedzera zvishoma nezvishoma chigadzirwa uchikurunga zvishoma nezvishoma. Pakutanga, chigadzirwa chinoyangarara pamusoro pemvura, uye zvishoma nezvishoma chinoita slurry. Tonhodza slurry.
(2) Wedzera 1/3 kana 2/3 yehuwandu hwemvura hunodiwa mumudziyo woipisa kusvika 70°C kuti uparadzire chigadzirwa kuti ugadzire slurry yemvura inopisa, wobva wawedzera huwandu hwasara hwemvura inotonhora kana mvura yechando muslurry yemvura inopisa. Muslurry, tonhodza musanganiswa mushure mekukurunga.
2.2 Nzira yekusanganisa upfu
Zvidimbu zveupfu nezvimwe zvinhu zvakaita seupfu zvakaenzana kana kuti zvakakura zvinoparadzirwa zvizere nekusanganisa kwakaoma, uye mvura inowedzerwa kuti inyunguduke. Panguva iyi, hypromellose inogona kunyungudutswa pasina kuungana.
3. Mabhenefiti eHPMC
3.1 Kunyungudika kwemvura inotonhora
Inonyungudika mumvura inotonhora iri pasi pe40°C kana 70% ethanol. Hainyungudike mumvura inopisa iri pamusoro pe60°C, asi inogona kunyungudika.
3.2 Kusashanda kwemakemikari
Hypromellose (HPMC) imhando ye non-ionic cellulose ether. Mushonga wayo hauna ionic charge uye hausangani nemetal salts kana ionic organic compounds. Saka, zvimwe zvinhu zvinobatsira hazvisangani nayo panguva yekugadzirira.
3.3 Kugadzikana
Yakagadzikana zvakanyanya kune ese ari maviri acid nealkali, uye inogona kuchengetwa kwenguva yakareba pakati pe pH 3 kusvika 1l, uye viscosity yayo haina shanduko yakajeka. Mhinduro yemvura yehypromellose (HPMC) ine simba rekudzivirira mold uye inogona kuchengetedza viscosity yakanaka panguva yekuchengetwa kwenguva refu. Mishonga inoshandisa HPMC ine kugadzikana kwemhando yepamusoro kupfuura iyo inoshandisa mishonga yechinyakare (yakadai sedextrin, starch, nezvimwewo).
3.4 Kugadziriswa kwe viscosity
Zvigadzirwa zvakasiyana zveHPMC zvinogona kusanganiswa muzvikamu zvakasiyana, uye viscosity yayo inogona kuchinja zvichienderana nemutemo wakati, uye ine hukama hwakanaka hwemutsara, saka inogona kusarudzwa zvichienderana nezvinodiwa.
3.5 Kusashanda zvakanaka kwemuviri
HPMC hainyudzwe kana kugayiwa mumuviri, uye haipe macalorie, saka chinhu chakachengeteka chemishonga.
3.6 Kuchengetedzwa
Zvinotendwa kuti HPMC chinhu chisina chepfu uye hachitsamwisi. Chipimo chepakati chemushonga unouraya mbeva i5g/kg, uye chiyero chepakati chemushonga unouraya mbeva i5.2g/kg. Chipimo chezuva nezuva hachikuvadzi muviri wemunhu.
4. Kushandiswa kweHPMC mukugadzirira
4.1 Inoshandiswa sezvinhu zvekufukidza firimu uye zvinhu zvinogadzira firimu
Hypromellose (HPMC) inoshandiswa semapiritsi akaputirwa nefirimu. Kana tichienzanisa nemapiritsi echinyakare akaputirwa akadai semapiritsi akaputirwa neshuga, mapiritsi akaputirwa haana zvakanakira zviri pachena pakuvhara kuravira uye chitarisiko, asi kuomarara kwawo uye kupfava, kunyudzwa kwehunyoro, kuparara, kuwedzera huremu hwepurasitiki nezvimwe zviratidzo zvemhando zviri nani. Chikamu chepasi che viscosity chechigadzirwa ichi chinoshandiswa sechinoputirwa nefirimu chinonyungudika mumvura pamapiritsi nemapiritsi, uye chikamu chepamusoro che viscosity chinoshandiswa sechinoputirwa nefirimu kumasisitimu e organic solvent. Kuwanda kwekushandiswa kunowanzova 2.0%-20%.
4.2 sechinhu chinosunga uye chinoparadzana
Chiyero chekusimba kwakaderera kwechigadzirwa ichi chinogona kushandiswa sechinobatanidza uye chinoparadza mapiritsi, mapiritsi, uye granules, uye chiyero chekusimba kwakakwira chinogona kushandiswa chete sechinobatanidza. Chiyero chinosiyana zvichienderana nemamodeli akasiyana uye zvinodiwa. Kazhinji, huwandu hwechinobatanidza hunoshandiswa pamapiritsi akaoma egranulation i5%, uye huwandu hwechinobatanidza hunoshandiswa pamapiritsi egranulation akanyorova i2%.
4.3 Semumiriri anomisa basa
Mushonga unomisa chinhu chine ganda rakakora rine hydrophilicity. Kushandiswa kwemushonga unomisa mumushonga unomisa kunogona kuderedza kumhanya kwe sedimentation yezvikamu, uye unogona kunamirwa pamusoro pezvikamu kudzivirira zvikamu kuti zvisaite polymer uye zviite clamping. Mushonga unomisa une basa rakakosha mukugadzirwa kwe suspensions. HPMC imhando yakanaka yemushonga unomisa. Mushonga we colloidal wakanyungudutswa mairi unogona kuderedza kushushikana kwe liquid-solid interface uye simba rakasununguka pazvikamu zvidiki zvakasimba, nokudaro zvichiwedzera kugadzikana kwe heterogeneous dispersion system. Chigadzirwa ichi i high-viscosity suspension liquid preparation yakagadzirirwa semushonga unomisa. Chine simba rakanaka rekumisa, chiri nyore kudimbura, hachina kunamira, uye chakapfava flocculated particles. Huwandu hwakajairika i 0.5% kusvika 1.5%.
4.4 Inoshandiswa semushonga unovhara, unononoka uye unodzorwa uye unoumba maburi
Chiyero chepamusoro chemushonga uyu chinoshandiswa kugadzira mapiritsi e-hydrophilic gel matrix sustainable-release, retarders uye controlled-release agents emushonga we-mixed-matrix sustainable-release tablets. Chine simba rekunonoka kuburitswa kwemushonga. Kushandiswa kwaro kuri 10% ~ 80% (W /W). Chiyero che low viscosity chinoshandiswa semushonga unogadzira maburi emushonga we-sustainable kana controlled release formulations. Chiyero chekutanga chinodiwa kuti mushonga werudzi urwu wepiritsi ushande zvakanaka, uye ipapo mhedzisiro yekuburitswa kwemushonga weropa inogoneka, uye huwandu hwemushonga weropa hunoshanda hunochengetwa mumuviri. Hypromellose inonyungudutsa kuti igadzire gel layer kana yasangana nemvura. Maitiro ekuburitswa kwemushonga kubva mupiritsi rematrix kunyanya kupararira kwegel layer uye kuputsika kwegel layer.
4.5 Guruu rinodzivirira rinoshandiswa sechinokora uye sechinokora
Kana chigadzirwa ichi chikashandiswa sechinokora, huwandu hwakajairika hunosvika 0.45% ~ 1.0%. Chigadzirwa ichi chinogonawo kuwedzera kugadzikana kweglue rinonyungudika mumvura, kugadzira colloid inodzivirira, kudzivirira kubatana kwezvikamu uye kuungana, nokudaro zvichidzivisa kuumbwa kwemadhaka. Huwandu hwacho hwakajairika hunosvika 0.5% ~ 1.5%.
4.6 Inoshandiswa sechigadzirwa chekapisi
Kazhinji, zvinhu zviri muchikamu checapsule zvinonyanya kuve gelatin. Maitiro ekugadzira chikamu checapsule cheMing ari nyore, asi kune mamwe matambudziko nezvimwe zviitiko zvakaita sekusadzivirira mishonga inonzwa hunyoro uye oxygen, kuderedza kunyungudika kwemishonga, uye kunonoka kuputsika kwechikamu checapsule panguva yekuchengetwa. Saka, hypromellose inoshandiswa panzvimbo pechinhu chiri muchikamu checapsule mukugadzirira macapsule, izvo zvinovandudza kugona kwekugadzira uye kushandiswa kwechikamu, uye zvave zvichikurudzirwa zvakanyanya munyika nekune dzimwe nyika.
4.7 Sechinhu chinonamira zvinhu zvipenyu
Tekinoroji yeBioadhesive, kushandiswa kwezvinobatsira ne bioadhesive polymers, nekunamatira ku biological mucosa, kunowedzera kuenderera mberi nekusimba kwekubatana pakati pemushonga ne mucosa, kuitira kuti mushonga unoburitswa zvishoma nezvishoma uye unyudzwe ne mucosa kuti uwane chinangwa chekurapa. Unoshandiswa zvakanyanya ikozvino. Unoshandiswa kurapa zvirwere zvemhino nemuromo wemuromo. Tekinoroji yeBioadhesion yemudumbu rudzi rutsva rwenzira yekuendesa mishonga yakagadzirwa mumakore achangopfuura. Haingowedzere nguva yekugara kwemishonga mudumbu, asiwo inovandudza mashandiro emushonga ne cell membrane yenzvimbo yekunyudzwa uye inochinja kuyerera kwe cell membrane. Simba remushonga rinopinda mumasero e epithelial emudumbu diki rinowedzerwa, nokudaro zvichivandudza bioavailability yemushonga.
4.8 Segel yemushonga wepamusoro
Semushonga unonamira ganda, gel ine zvakanakira zvakawanda zvakaita sekuchengetedzeka, runako, kuchenesa kuri nyore, mutengo wakaderera, nzira iri nyore yekugadzirira, uye kushanda zvakanaka nemishonga. Mumakore achangopfuura, yave ichinyanya kutariswa uye yave kugadzirwa kwegadziriro yeganda yekunze.
4.9 Semushonga wekudzivirira kunaya kwemvura mu emulsification system
Nguva yekutumira: Zvita-16-2021