Chii chinonzi Hypromellose?

Hypromellose, inozivikanwa sehydroxypropyl methylcellulose, HPMC. Iro molecular formula ndeye C8H15O8-(C10Hl8O6)n-C8Hl5O8, uye uremu hwayo hwema molecular inenge 86000. Hypromellose is a semi-synthetic material, iyo chikamu che methyl uye chikamu che polyhydroxypropyl ether ye cellulose. Inogona kubudiswa nenzira mbiri: imwe ndeyokuti giredhi yakakodzera yemethyl cellulose inobatwa neNaOH, uye yobva yaita nepropylene oxide pasi pekushisa kwepamusoro uye kumanikidzwa. Iyo fomu yakabatanidzwa kune anhydroglucose mhete ye cellulose, uye inogona kusvika padanho rakanaka; imwe yacho kurapa donje linter kana huni pulp fiber ne caustic soda, uye kuita nemethyl chloride uye propylene oxide zvakatevedzana kuti uiwane, uye wozowedzera kunatsa, yakapwanyika kuita yakanaka uye yakafanana poda kana granules. HPMC yakasiyana-siyana yechisikigo chirimwa cellulose, uye zvakare yakanakisa mishonga yemishonga, iyo ine huwandu hwakasiyana hwezvinyorwa. Parizvino, inoshandiswa zvakanyanya kumba nekune dzimwe nyika, uye ndeimwe yevabatsiri vemishonga ine chiyero chepamusoro chekushandisa mumishonga yemuromo.

Hypromellose ichena kusvika kuchena mukaka muruvara, isina muchetura uye isinganakidze, uye iri muchimiro chegranular kana fibrous powder inoyerera nyore. Yakagadzikana pasi pechiedza uye hunyoro. Iyo inoputika mumvura inotonhora kuti igadzire mukaka chena colloidal solution, ine imwe dhigirii ye viscosity, uye chiitiko che sol-gel interconversion chinogona kuitika nekuda kwekushanduka kwekushisa kweimwe kusangana kwemhinduro. Inonyungudika mu70% doro kana dimethyl ketone, uye haizonyungudika mudoro rakazara, chloroform kana ethoxyethane.

Kana pH yehypromellose iri pakati pe4.0 ne8.0, ine kugadzikana kwakanaka, uye inogona kuvapo yakagadzikana kana pH iri pakati pe3.0 ne11.0. Kana tembiricha iri 20°C uye hunyoro huri 80%, inochengetwa kwemazuva gumi. Hunyoro hwekutora hunyoro hweHPMC i6.2%.

1. Izvo zvakakosha zveHypromellose HPMC

Nekuda kwezvakasiyana zvemukati methoxy uye hydroxypropyl muchimiro chehypromellose, marudzi akasiyana ezvigadzirwa akaonekwa. Mukutarisisa kwakasiyana, marudzi akasiyana ezvigadzirwa ane chaiwo viscosity uye Thermal gelation tembiricha, saka, ane akasiyana zvivakwa uye anogona kushandiswa kune zvakasiyana zvinangwa. Iyo pharmacopoeias yenyika dzakasiyana siyana ine mirau yakasiyana uye inomiririra pamhando: iyo European Pharmacopoeia, zvinoenderana neakasiyana mamakisi eeviscosities akasiyana uye madhigirii ekutsiviwa kwezvinhu zvinotengeswa mumusika, inomiririrwa nemagiredhi pamwe nenhamba, uye unit iri mPa. ·s; kuUnited States Pharmacopoeia, zita rinowanzozivikanwa Wedzera manhamba mana kumagumo kuratidza zvirimo uye rudzi rwechimwe nechimwe chinotsiva hypromellose, senge hypromellose 2208, manhamba maviri ekutanga anomiririra inenge muzana yemethoxy, uye manhamba maviri ekupedzisira anomiririra hydroxypropyl. Inenge muzana ye.

2. Nzira yekupedza Hypromellose HPMC mumvura

2.1 nzira yemvura inopisa
Sezvo hypromellose isinganyungudika mumvura inopisa, inogona kuparadzirwa zvakafanana mumvura inopisa pakutanga, uye yozotonhora. Nzira mbiri dzakajairika dzinotsanangurwa sezvizvi:
(1) Isa huwandu hunodiwa hwemvura inopisa mumudziyo, uye kupisa kusvika ku70 ° C, zvishoma nezvishoma uwedzere chigadzirwa ichi pasi pekugadzirisa zvishoma nezvishoma, pakutanga, chigadzirwa ichi chinoyangarara pamusoro pemvura, uye zvishoma nezvishoma chinogadzira slurry, inomutsa Kutonhodza slurry pasi.
(2) Wedzera 1/3 kana 2/3 yehuwandu hunodiwa hwemvura mumudziyo uye kupisa kusvika ku70 ° C kuti uparadzire chigadzirwa kugadzirira mvura inopisa inoputika, wobva wawedzera huwandu hwemvura inotonhora kana yechando. mvura inopisa silts Mu slurry, musanganiswa unotonhorera mushure mekusimudzira.

2.2 Poda yekusanganisa nzira
Zvimedu zvehupfu zvinoparadzirwa zvakakwana nekusanganiswa kwakaoma nechiyero chakaenzana kana chikuru chezvimwe zvinhu zvehupfu, uye zvino zvakanyungudutswa mumvura. Panguva ino, iyo hypromellose inogona kunyungudika pasina agglomeration.

3. Zvakanakira zveHypromellose HPMC

3.1 Kunyungudika kwemvura inotonhora
Soluble mumvura inotonhora iri pasi pe40°C kana 70% ethanol, isinganyungudike 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 inenge yakagadzikana kune asidhi uye alkali, uye inogona kuchengetwa kwenguva yakareba pakati pepH 3 ne1l pasina kuchinja kuri pachena mu viscosity. Iyo aqueous solution ye hypromellose (HPMC) ine anti-mildew effect uye inogona kuchengetedza yakanaka viscosity kugadzikana panguva yekuchengetedza kwenguva refu. Mishonga inoshandisa HPMC sezvishandiso ine kugadzikana kwemhando iri nani pane iyo inoshandisa zvechinyakare zvekushandisa (senge dextrin, starch, nezvimwewo).

3.4 Viscosity inogadziriswa
Different viscosity derivatives of HPMC inogona kusanganiswa maererano nereshiyo dzakasiyana, uye viscosity yayo inogona kuchinja maererano nemimwe mitemo, uye ine hukama hwakanaka hwemutsara, saka chiyero chinogona kusarudzwa maererano nezvinodiwa.

3.5 Metabolic inertia
HPMC haina kunyudzwa kana kugadzirwa mumuviri, uye haipi kupisa, saka yakachengeteka mishonga yekugadzirira excipient.

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. Mishonga yezuva nezuva haina ngozi kuvanhu.

4. Kushandiswa kweHypromellose HPMC mukugadzirira

4.1 Seye firimu yekuputira zvinhu uye firimu-kugadzira zvinhu
Uchishandisa hypromellose (HPMC) senge firimu-yakavharwa piritsi rekushandisa, kana ichienzaniswa neyakajairwa mahwendefa akadai seshuga-yakavharwa mapiritsi, iwo mahwendefa akaputirwa haana mabhenefiti ari pachena mukuvharisa kuravira kwemushonga uye chitarisiko, asi kuoma kwavo uye friability , kunyura munyoro, 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 senge firimu-kupfeka zvinhu zve organic solvent masisitimu. Iko kusungirirwa kunowanzo 2.0% kusvika 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, dosage yebinder yemapiritsi egranulation yakaoma i5%, uye dosage yebinder yemapiritsi ekunyorova i2%.

4.3 Semumiriri wekumisa basa
Iyo inomisa mumiriri iine viscous gel chinhu chine hydrophilicity, iyo inogona kudzikamisa sedimentation kumhanya kwezvimedu kana ichinge yashandiswa mune inomisa mumiriri, uye inogona kusungirirwa pamusoro pezvimedu kudzivirira zvimedu kuti zvisabatana uye kuderera kuita bhora. . Kumisa mabasa kunoita basa rakakosha pakuita kuti vanhu vamiswe. HPMC yakanakisa akasiyana ekumisa maajenti, uye yakanyungudika colloidal mhinduro inogona kuderedza kushushikana kweiyo liquid-solid interface uye yemahara simba pane madiki masisitimu, nekudaro ichiwedzera kugadzikana kweiyo heterogeneous dispersion system. Iyo yakakwira-viscosity giredhi yechigadzirwa ichi inoshandiswa seyekumiswa-mhando yegadziriro yemvura yakagadzirirwa semumiriri wekumisa. Iyo ine yakanaka kumisa mhedzisiro, iri nyore kuparadzirazve, haina kunamatira kumadziro, uye ine yakanaka flocculated particles. Iyo yakajairika dosage ndeye 0.5% kusvika 1.5%.

4.4 Sechivharo, inosimudzira-inoburitsa mumiririri uye pore-inokonzeresa agent
Iyo yepamusoro-viscosity giredhi yechigadzirwa ichi inoshandiswa kugadzirira hydrophilic gel matrix yakasimudzwa-kuburitswa mahwendefa, blockers uye inodzorwa-kuburitsa maajenti eakasanganiswa zvinhu matrix akatsigira-kuburitswa mahwendefa, uye ane mhedzisiro yekunonoka kuburitswa kwezvinodhaka. Iko kushandiswa kwayo kwe10% ~ 80% (W / W). Low-viscosity mamakisi anoshandiswa semapore-forming agents ekusimudzira-kuburitswa kana kudzorwa-kuburitsa gadziriro. Mushonga wekutanga unodiwa pakurapa kwerudzi urwu rwepiritsi unogona kuwanikwa nekukurumidza, uye wobva waita kusimudzira-kuburitswa kana kudzorwa-kuburitsa mhedzisiro, uye inoshanda yeropa zvinodhaka zvinochengetwa mumuviri. Kana hypromellose ikasangana nemvura, inoisa mvura kuti igadzire gel layer. Iyo nzira yekusunungurwa kwezvinodhaka kubva pahwendefa rematrix inonyanya kusanganisira kupararira kwejel layer uye kuputika kwejeri.

4.5 Inodzivirira guruu seyakakora uye colloid
Kana chigadzirwa ichi chikashandiswa seyakakora, iyo inowanzo shandiswa inosvika 0.45% ~ 1.0%. Ichi chigadzirwa chinogona zvakare kuwedzera kugadzikana kwe hydrophobic glue, kuumba inodzivirira colloid, kudzivirira zvimedu kubva kuagglomerating uye agglomerating, nekudaro zvichitadzisa kuumbwa kwe sediment, uye yakajairika kusungwa i 0.5% ~ 1.5%.

4.6 Capsule zvinhu zve capsules
Kazhinji iyo capsule shell capsule material ye capsule inobva pane gelatin. Nzira yekugadzirwa kwegelatin capsule shell iri nyore, asi kune mamwe matambudziko uye zviitiko zvakadai sekudzivirira kusina kunaka kubva kune unyoro uye zvinodhaka zvinonzwa oksijeni, kuderera kwezvinodhaka zvinodhaka, uye kunonoka kuparara kwegomba re capsule panguva yekuchengetedza. Nokudaro, hypromellose, sechinzvimbo chegelatin capsules, inoshandiswa mukugadzirira kwe capsules, iyo inovandudza kuumbwa uye kushandiswa kwemaitiro e capsules, uye yakakurudzirwa zvakanyanya kumba nekune dzimwe nyika.

4.7 sebioadhesive
Bioadhesion tekinoroji, kushandiswa kwezvinobatsira zvine bioadhesive polymers, kuburikidza nekunamatira kune biological mucosa, inosimudzira kuenderera uye kusimba kwekubatana pakati pekugadzirira uye mucosa, kuitira kuti mushonga wacho usunungurwe zvishoma nezvishoma uye unobatwa nemucosa kuti uwane zvinangwa zvekurapa. Iko ikozvino inoshandiswa zvakanyanya Inoshandiswa kurapa zvirwere zvemhino yemhino, mucosa yemuromo uye zvimwe zvikamu. Gastrointestinal bioadhesion tekinoroji inzira nyowani yekuunza zvinodhaka yakagadziriswa mumakore achangopfuura. Haisi kungorebesa nguva yekugara yemishonga yekugadzirira mudumbu, asi zvakare inovandudza kusangana kwekuita pakati pemushonga uye sero membrane panzvimbo yekunyura, kushandura kuyerera kwesero membrane, Kuwedzera kupinda kwemushonga kusvika mudumbu. epithelial masero, nokudaro achivandudza bioavailability yemushonga.

4.8 Setopical gel
Segadziriro yekunamatira yeganda, gel ine nhevedzano yezvakanakira senge chengetedzo, runako, nyore kuchenesa, mutengo wakaderera, nyore kugadzirira maitiro, uye kuenderana kwakanaka nemishonga. direction.

4.9 Semvura inhibitor mune emulsification system