1. Ubume obusisiseko be-HPMC
IHypromellose, igama lesiNgesi elithi hydroxypropyl methylcellulose, eligama linguHPMC.I-molecular formula yi-C8H15O8-(C10Hl8O6)n-C8Hl5O8, kwaye ubunzima be-molecular malunga ne-86,000.Le mveliso i-semi-synthetic material, eyinxalenye yeqela le-methyl kunye nenxalenye ye-polyhydroxypropyl ether ye-cellulose.Inokwenziwa ngeendlela ezimbini: enye kukuphatha i-methyl cellulose yebakala elifanelekileyo kunye ne-NaOH, kwaye emva koko iphendule ngepropylene oxide phantsi kobushushu obuphezulu kunye noxinzelelo oluphezulu.Ixesha lokuphendula kufuneka ligcinwe ukuvumela amaqela e-methyl kunye ne-hydroxypropyl ukuba ahlangane ne-ether.Ifom ye idityaniswe kwiringi ye-anhydroglucose ye-cellulose, kwaye inokufikelela kwinqanaba elifunekayo;enye kukunyanga i-cotton linter okanye i-wood pulp fiber nge-caustic soda, kwaye emva koko ufumane ngokusabela nge-chlorinated methane kunye ne-propylene oxide ngokulandelelana, kwaye emva koko icocwe ngakumbi, Pulverize, yenza ibe ngumgubo ococekileyo kunye nofanayo okanye igranule.I-HPMC yintlobo ngeentlobo zeselulosi yezityalo zendalo, kwaye ikwayi-excipient egqwesileyo yamayeza, enomthombo obanzi.Okwangoku, isetyenziswa kakhulu ekhaya nakwamanye amazwe, kwaye yenye yezinto ezincedisa amayeza ezinezinga eliphezulu lokusetyenziswa phakathi kwamachiza omlomo.
Umbala wale mveliso umhlophe kumhlophe we-milky, awunayo ityhefu kwaye awunayo incasa, kwaye i-granular okanye i-fibrous, i-powder elula ehamba lula.Izinzile phantsi kokukhanya kunye nokufuma.Idumba emanzini abandayo ukwenza isisombululo se-milky colloidal esineqondo elithile le-viscosity.I-sol-gel ye-interconversion phenomenon ingenzeka ngenxa yokutshintsha kweqondo lokushisa loxinzelelo oluthile lwesisombululo.Kulula kakhulu ukuchithwa kwi-70% yotywala okanye i-dimethyl ketone, kwaye ayiyi kuchithwa kwi-alcohol anhydrous, i-chloroform okanye i-ethoxyethane.
IHypromellose inozinzo oluhle xa i-pH iphakathi kwe-4.0 kunye ne-8.0, kwaye ingaba khona ngokuzinzileyo phakathi kwe-3.0 kunye ne-11.0.Emva kokugcina iintsuku ezili-10 kwiqondo lobushushu le-20 ° C kunye nokufuma okuhambelana ne-80%, I-coefficient yokufunxa ukufuma kwe-HPMC yi-6.2%.
Ngenxa yomahluko kumxholo wezinto ezimbini ezibambeleyo kwisakhiwo se-hypromellose, i-methoxy kunye ne-hydroxypropyl, iintlobo ezahlukeneyo zeemveliso ziye zavela.Kugxininiso oluthile, iintlobo ezahlukeneyo zeemveliso zine-viscosity ethile kunye nobushushu be-Thermal gelation, ngoko ke, zineepropati ezahlukeneyo kwaye zingasetyenziselwa iinjongo ezahlukeneyo.Ii-pharmacopoeias zamazwe ahlukeneyo zineenkcazo ezahlukeneyo kunye nokuchazwa kwemodeli: I-European Pharmacopoeia isekelwe kumanqanaba ahlukeneyo ee-viscosities ezahlukeneyo kunye namanqanaba ahlukeneyo okutshintshwa kweemveliso kwimarike.Ibonakaliswa libakala kunye nenani.Iyunithi zii-mPa•s.Emva kokongeza amadijithi ama-4 ukubonisa umxholo kunye nohlobo lwe-substituent nganye ye-hypromellose, umzekelo, i-hypromellose 2208, amadijithi amabini okuqala amele ipesenti eqikelelweyo yeqela le-methoxy, amadijithi amabini okugqibela amele i-hydroxypropyl Ipesenti eqikelelweyo yamatyala.
2.Indlela yokunyibilikisa i-HPMC emanzini
2.1 Indlela yamanzi ashushu
Ekubeni i-hypromellose inganyibiliki emanzini ashushu, inokuchithwa ngokufanayo kumanzi ashushu kwinqanaba lokuqala, kwaye emva kokuba ipholile, iindlela ezimbini eziqhelekileyo zichazwe ngolu hlobo lulandelayo:
(1) Beka umlinganiselo ofunekayo wamanzi ashushu kwisikhongozelo kwaye ufudumale ukuya kuma 70℃.Yongeza kancinci imveliso phantsi kokuvuselela kancinci.Ekuqaleni, imveliso idada phezu kwamanzi, kwaye ngokuthe ngcembe yenza i-slurry.Pholisa udaka.
(2) Yongeza i-1/3 okanye i-2/3 yomlinganiselo ofunekayo wamanzi kwisikhongozeli kwaye uyifudumeze ukuya kuma-70°C ukusasaza imveliso ukulungiselela udaka lwamanzi ashushu, uze wongeze umlinganiselo oseleyo wamanzi abandayo okanye amanzi omkhenkce. ukuya kwi-slurry yamanzi ashushu Kwi-slurry, pholisa umxube emva kokuvuselela.
2.2 Indlela yokuxuba umgubo
Iingqungquthela zepowder kunye nezinye izithako ze powdery zexabiso elilinganayo okanye elikhulu zichithwa ngokupheleleyo ngokuxuba okomileyo, kwaye emva koko amanzi adibaniswa ukuze adibanise.Ngeli xesha, i-hypromellose inokuchithwa ngaphandle kwe-agglomeration.
3. Izinto eziluncedo zeHPMC
3.1 Ukunyibilika kwamanzi abandayo
Inyibilika emanzini abandayo angaphantsi kwe-40 ° C okanye i-70% ye-ethanol.Ayinyibiliki kumanzi ashushu angaphezu kwama-60°C, kodwa inokufakwa ijeli.
3.2 Ukungangeni ngamachiza
IHypromellose (HPMC) luhlobo lwe-ether ye-cellulose engeyiyo ionic.Isisombululo sayo asinayo i-ionic kwaye ayisebenzisi kunye neetyuwa zetsimbi okanye i-ionic organic compounds.Ngoko ke, abanye abancedisi abaphenduli kunye nayo ngexesha lenkqubo yokulungiselela.
3.3 Uzinzo
Izinzile kwi-asidi kunye ne-alkali, kwaye inokugcinwa ixesha elide phakathi kwe-pH 3 ukuya kwi-1l, kwaye i-viscosity yayo ayinalo utshintsho olucacileyo.Isisombululo samanzi se-hypromellose (HPMC) sinomphumo ochasene nesikhunta kwaye sinokugcina uzinzo oluhle lwe-viscosity ngexesha lokugcinwa kwexesha elide.Abancedisi bamayeza abasebenzisa i-HPMC banozinzo olungcono lomgangatho kunezo zisebenzisa izixhobo zemveli (ezifana ne-dextrin, istatshi, njl.).
3.4 Ukulungelelaniswa kwe-viscosity
I-viscosity derivatives eyahlukeneyo ye-HPMC inokuxutywa ngokwemilinganiselo eyahlukeneyo, kwaye i-viscosity yayo inokutshintsha ngokomgaqo othile, kwaye inobudlelwane obuhle bomgca, ngoko inokukhethwa ngokweemfuno.
3.5 Inertia yeMetabolic
I-HPMC ayifunxanga okanye ifakwe emzimbeni, kwaye ayiboneleli ngeekhalori, ngoko ke i-excipient ekhuselekileyo yamalungiselelo amayeza.
3.6 Ukhuseleko
Ngokuqhelekileyo kukholelwa ukuba i-HPMC yinto engeyona ityhefu kwaye ayithukuthelisi.Idosi ebulalayo ephakathi kwiigundane yi-5g / kg, kwaye idosi ebulalayo ephakathi kwiigundane yi-5.2g / kg.Idosi yemihla ngemihla ayinabungozi kumzimba womntu.
4. Ukusetyenziswa kweHPMC kumalungiselelo
4.1 Isetyenziswe njengezinto zokugquma ifilimu kunye nemathiriyeli yokwenza ifilimu
IHypromellose (HPMC) isetyenziswa njengemathiriyeli yethebhulethi eqatywe ifilimu.Xa kuthelekiswa namacwecwe aqhelekileyo adityanisiweyo afana namacwecwe afakwe iswekile, iipilisi ezigqunyiweyo azikho iingenelo ezicacileyo zokufihla incasa kunye nokubonakala, kodwa ukuqina kwazo kunye nokuqina , Ukufunxa ukufuma, ukuchithwa, ukugqithiswa kobunzima kunye nezinye izikhombisi zekhwalithi zingcono.Ibanga eliphantsi le-viscosity yale mveliso lisetyenziswa njengento yokugubungela ifilimu e-soluble yamanzi kwiipilisi kunye neepilisi, kwaye i-high-viscosity grade isetyenziswe njengento yokugubungela ifilimu kwiinkqubo ze-solvent ze-organic.Ukugxininiswa kokusetyenziswa ngokuqhelekileyo yi-2.0% -20%.
4.2 njengomdibanisi kunye ne-disintegrant
Ibanga eliphantsi le-viscosity yale mveliso lingasetyenziselwa njenge-binder kunye ne-disintegrant yamacwecwe, iipilisi, kunye ne-granules, kwaye i-high-viscosity grade ingasetyenziswa kuphela njenge-binder.Idosi iyahluka ngeemodeli ezahlukeneyo kunye neemfuno.Ngokuqhelekileyo, inani le-binder elisetyenziselwa iipilisi ezomileyo ze-granulation yi-5%, kwaye inani le-binder elisetyenziselwa iipilisi ze-granulation ezimanzi yi-2%.
4.3 Njenge-arhente exhomayo
I-ejenti yokuxhoma yinto yejeli ye-viscous ene-hydrophilicity.Ukusetyenziswa kwe-ejenti yokumisa kwi-agent yokumisa kunokunciphisa isantya se-sedimentation yamaqhekeza, kwaye inokudityaniswa kumphezulu weengqungquthela zokukhusela iinqununu ezivela kwi-polymerizing kunye nokudibanisa kwi-mass mass.Ii-arhente zokuxhoma zidlala indima ebalulekileyo ekuveliseni ukumiswa.I-HPMC luhlobo olubalaseleyo lweearhente zokumisa.Isisombululo se-colloidal esichithwe kuyo sinokunciphisa ukunyanzeliswa kwe-liquid-solid interface kunye namandla akhululekile kwiincinci ezincinci eziqinileyo, ngaloo ndlela ziphucula ukuzinza kwenkqubo yokusabalalisa okungafaniyo.Le mveliso yi-high-viscosity ukumiswa kolwelo ukulungiswa okulungiselelwe njenge-arhente yokumisa.Inesiphumo esihle sokuxhoma, kulula ukuphinda uyisasaze, ayincangathi, kunye namasuntswana acolekileyo acolekileyo.Isixa esiqhelekileyo yi-0.5% ukuya kwi-1.5%.
4.4 Isetyenziswe njenge-blocker, i-arhente yokukhulula ecothayo kunye nelawulwayo kunye ne-pore-forming agent
Ibakala eliphezulu le-viscosity yale mveliso lisetyenziselwa ukulungiselela i-hydrophilic gel matrix yokukhululwa okuqhubekayo, i-retarders kunye nee-agent-release-release agents kwiipilisi ezixutywayo ze-matrix ezizinzileyo.Inesiphumo sokulibazisa ukukhutshwa kweziyobisi.Ukugxininiswa kokusetyenziswa kwayo yi-10% ~ 80% (W / W).Ibakala eliphantsi le-viscosity lisetyenziswa njenge-ejenti yokwenza i-pore kwimiqulu eqhubekayo okanye elawulwayo yokukhululwa.Idosi yokuqala efunekayo kwisiphumo sonyango solu hlobo lwethebhulethi inokufikelelwa ngokukhawuleza, kwaye emva koko isiphumo sokukhululwa esizinzileyo okanye esilawulwayo siyenziwa, kwaye ukugxininiswa kweziyobisi zegazi kugcinwa emzimbeni.I-Hypromellose hydrates ukwenza umaleko wejeli xa idibana namanzi.Indlela yokukhutshwa kweziyobisi kwi-tablet ye-matrix ikakhulu ukusasazwa komgangatho wejeli kunye nokukhukuliseka komgangatho wejeli.
4.5 Iglu ekhuselayo esetyenziswa njenge-thickener kunye ne-colloid
Xa le mveliso isetyenziswe njenge-thickener, i-concentration eqhelekileyo yi-0.45% ~ 1.0%.Le mveliso inokunyusa ukuzinza kweglue ye-hydrophobic, yenza i-colloid ekhuselayo, ithintele i-particle coalescence kunye ne-agglomeration, ngaloo ndlela inqanda ukubunjwa kwe-sediments.Ukugxininiswa kwayo okuqhelekileyo ngu-0.5% ~ 1.5%.
4.6 Isetyenziswe njengempahla ye-capsule
Ngokuqhelekileyo, i-capsule shell material ye-capsule ikakhulu yi-gelatin.Inkqubo yokuveliswa kwegobolondo le-Ming capsule ilula, kodwa kukho ezinye iingxaki kunye neziganeko ezifana nokukhuselwa kakubi komswakama kunye ne-oxygen amachiza abuthathaka, ukunciphisa ukuchithwa kweziyobisi, kunye nokulibaziseka kokuchithwa kwegobolondo le-capsule ngexesha lokugcinwa.Ngoko ke, i-hypromellose isetyenziselwa indawo yempahla ye-capsule ekulungiseleleni i-capsules, ephucula ukubunjwa kunye nokusetyenziswa kwempembelelo ye-capsule, kwaye iye yakhuthazwa ngokubanzi ekhaya nakwamanye amazwe.
4.7 Njenge-bioadhesive
Itekhnoloji ye-Bioadhesive, ukusetyenziswa kwezinto ezincedisayo kunye neepolymers ze-bioadhesive, ngokubambelela kwi-mucosa yebhayoloji, ukwandisa ukuqhubeka kunye nokuqina koqhagamshelwano phakathi kwamalungiselelo kunye ne-mucosa, ukuze ichiza likhutshwe ngokukhawuleza kwaye lifunxwe yi-mucosa ukufezekisa injongo unyango.Isetyenziswa ngokubanzi ngoku Isetyenziselwa ukunyanga izifo ze-nasal cavity kunye ne-mucosa yomlomo.Itekhnoloji ye-bioadhesion ye-gastrointestinal luhlobo olutsha lwenkqubo yokuhanjiswa kweziyobisi ephuhliswe kwiminyaka yakutshanje.Ayinakwandisa nje ixesha lokuhlala lamalungiselelo eziyobisi kwindlela yesisu, kodwa iphucula ukusebenza koqhagamshelwano lwechiza kunye nenwebu yeseli yendawo yokufunxa kunye nokutshintsha ubuninzi be-membrane yeseli.Amandla okungena kweyeza kwiiseli ze-epithelial zamathumbu amancinci aphuculwa, ngaloo ndlela kuphuculwe i-bioavailability yeyeza.
4.8 Njengejeli yezihloko
Njengokulungiselela ukunamathela kwesikhumba, i-gel inoluhlu lweenzuzo ezifana nokhuseleko, ubuhle, ukucocwa lula, ixabiso eliphantsi, inkqubo yokulungiselela elula, kunye nokuhambelana kakuhle neziyobisi.Kwiminyaka yakutshanje, ifumene ingqwalasela ebanzi kwaye ibe luphuhliso lwamalungiselelo angaphandle kwesikhumba.ulwalathiso.
4.9 Njenge-precipitation inhibitor kwinkqubo ye-emulsification
Ixesha lokuposa: Dec-16-2021