Uncwadi olunxulumeneyo ekhaya nakwamanye amazwe ekulungiseleleni amayeza e-hydroxypropyl methylcellulose (HPMC) kwiminyaka yakutshanje ahlaziywa, ahlalutywa kwaye ashwankathelwa, kunye nokusetyenziswa kwawo kumalungiselelo aqinileyo, amalungiselelo olwelo, amalungiselelo okukhululwa azinzileyo kunye nokulawulwa, amalungiselelo capsule, gelatin The latest izicelo kwintsimi yokuqulunqwa okutsha okufana ne-adhesive formulations kunye ne-bioadhesives. Ngenxa yomahluko kubunzima bemolekyuli kunye ne-viscosity ye-HPMC, ineempawu kunye nokusetyenziswa kwe-emulsification, i-adhesion, thickening, i-viscosity ekhulayo, ukumisa, i-gelling kunye nokwenza ifilimu. Isetyenziswa ngokubanzi kumalungiselelo amayeza kwaye iya kudlala indima enkulu kwintsimi yamalungiselelo. Ngophononongo olunzulu lweepropathi zayo kunye nokuphuculwa kobuchwephesha bokuqulunqa, i-HPMC iya kusetyenziswa ngokubanzi kuphando lweefom zedosi entsha kunye neenkqubo ezintsha zokuhanjiswa kwamachiza, ngaloo ndlela ikhuthaza uphuhliso oluqhubekayo lwemixube.
ihydroxypropyl methylcellulose; amalungiselelo amayeza; abancedisi bamayeza.
Abaxhamli bamachiza ayisiyiyo kuphela isiseko sezinto zokwenziwa kwamalungiselelo echiza ekrwada, kodwa ikwanxulumene nobunzima benkqubo yokulungiselela, umgangatho wamachiza, uzinzo, ukhuseleko, izinga lokukhululwa kweziyobisi, indlela yokwenza, ukusebenza ngempumelelo kwezonyango, kunye nophuhliso lweendlela ezintsha. iifom zedosi kunye neendlela ezintsha zolawulo. ezinxulumene ngokusondeleyo. Ukuvela kwezinto ezintsha ezincedisa amayeza kaninzi kukhuthaza ukuphuculwa komgangatho wamalungiselelo kunye nophuhliso lweefom zedosi entsha. IHydroxypropyl methylcellulose (HPMC) yenye yezona zinto zixhaphakileyo kumayeza asetyenziswa ekhaya naphesheya. Ngenxa yobunzima bayo obuhlukeneyo bemolekyuli kunye ne-viscosity, inemisebenzi ye-emulsifying, ukubopha, ukuqina, ukuqina, ukuxhoma kunye nokuncamathelisa. Iimpawu kunye nokusetyenziswa okunje nge-coagulation kunye nokwakheka kwefilimu zisetyenziswa kakhulu kwitekhnoloji yamayeza. Eli nqaku liphonononga ngokubanzi ukusetyenziswa kwe-hydroxypropyl methylcellulose (HPMC) ekuqulunqweni kwiminyaka yamuva.
1.Iimpawu eziphambili zeHPMC
I-Hydroxypropyl methyl cellulose (HPMC), i-formula ye-molecular yi-C8H15O8- (C10 H18O6) n- C8H15O8, kunye nobunzima be-molecular mass malunga ne-86 000. Le mveliso yinto ye-semi-synthetic, eyingxenye ye-methyl kunye nenxalenye ye-polyhydroxypropyl ether kwi-cellulose. Inokuveliswa ngeendlela ezimbini: Enye kukuba i-methyl cellulose yebakala elifanelekileyo iphathwa nge-NaOH kwaye emva koko iphendule ngepropylene oxide phantsi kobushushu obuphezulu kunye noxinzelelo oluphezulu. Ixesha lokuphendula kufuneka lihlale ixesha elide ngokwaneleyo ukuvumela i-methyl kunye ne-hydroxypropyl ukuba zenze iibhondi ze-ether Ixhunyiwe kwindandatho ye-anhydroglucose ye-cellulose ngendlela ye-cellulose, kwaye inokufikelela kwinqanaba elifunekayo; enye kukunyanga i-cotton linter okanye i-wood pulp fiber nge-caustic soda, kwaye emva koko usabele nge-chlorinated methane kunye ne-propylene oxide ngokulandelelana, kwaye emva koko uyicokise ngakumbi. , utyunyuzwe ube ngumgubo ococekileyo kunye nofanayo okanye iigranules.
Umbala wale mveliso umhlophe ukuya kumhlophe omhlophe, awunavumba kwaye awunancancisi, kwaye ifom i-granular okanye i-fibrous-powder elula ehamba lula. Le mveliso inokuchithwa emanzini ukwenza isisombululo esicacileyo se-milky white colloidal kunye ne-viscosity ethile. I-sol-gel interconversion phenomenon ingenzeka ngenxa yokutshintsha kweqondo lokushisa kwesisombululo kunye noxinzelelo oluthile.
Ngenxa yomahluko kumxholo wale mibini ibambeleyo kwisakhiwo se-methoxy kunye ne-hydroxypropyl, iintlobo ezahlukeneyo zeemveliso ziye zavela. Kwiimpawu ezithile, iintlobo ezahlukeneyo zeemveliso zineempawu ezithile. I-Viscosity kunye nokushisa kwe-thermal gelation, ngoko ke ineempawu ezahlukeneyo kwaye ingasetyenziselwa iinjongo ezahlukeneyo. I-Pharmacopoeia yamazwe ahlukeneyo inemimiselo eyahlukeneyo kunye nokumelwa kwimodeli: I-European Pharmacopoeia isekwe kumanqanaba ahlukeneyo ee-viscosities ezahlukeneyo kunye namanqanaba ahlukeneyo okutshintshwa kweemveliso ezithengiswa kwimarike, ezichazwe ngamabakala kunye namanani, kwaye iyunithi "mPa s. ”. Kwi-US Pharmacopoeia, iidijithi ze-4 zongezwa emva kwegama eliqhelekileyo ukubonisa umxholo kunye nohlobo lwe-substitute nganye ye-hydroxypropyl methylcellulose, njenge-hydroxypropyl methylcellulose 2208. Amanani amabini okuqala amele ixabiso elisondeleyo leqela le-methoxy. Ipesenti, amanani amabini okugqibela amele uqikelelo lwepesenti yehydroxypropyl.
I-Calocan's hydroxypropyl methylcellulose ine-3 series, ezizezi, uchungechunge lwe-E, uchungechunge lwe-F kunye nochungechunge lwe-K, uluhlu ngalunye luneemodeli ezahlukeneyo zokukhetha kuzo. Uchungechunge lwe-E lusetyenziswa kakhulu njengeengqungquthela zefilimu, ezisetyenziselwa ukugubungela ithebhulethi, i-tablet cores evaliweyo; I-E, F series zisetyenziswa njenge-viscosifiers kunye nokukhulula ii-agents ezibuyisela umva kumalungiselelo ophthalmic, i-agent e-suspending, i-thickeners yamalungiselelo olwelo, iipilisi kunye ne-Binders of granules; Uthotho lwe-K lusetyenziswa kakhulu njengezithinteli zokukhulula kunye nemathiriyeli yejeli ye-hydrophilic yolungiselelo olucothayo nolulawulwayo lokukhululwa.
Abavelisi basekhaya ikakhulu baquka iFuzhou No. 2 Chemical Factory, Huzhou Food and Chemical Co., Ltd., Sichuan Luzhou Pharmaceutical Accessories Factory, Hubei Jinxian Chemical Factory No. 1, Feicheng Ruitai Fine Chemical Co., Ltd., Shandong Liaocheng Ahua Pharmaceutical Co. ., Ltd., Xi'an Huian izityalo zekhemikhali, njl.
2.Izinto ezilungileyo zeHPMC
HPMC iye yaba yenye excipients amayeza asetyenziswa kakhulu ekhaya nakwamanye amazwe, kuba HPMC iingenelo ukuba ezinye excipients abanazo.
2.1 Ukunyibilika kwamanzi abandayo
Inyibilika kumanzi abandayo angaphantsi kwama-40 ℃ okanye 70% ethanol, ayinyibiliki kumanzi ashushu angaphezu kwama-60 ℃, kodwa iyakwazi ijeli.
2.2 Anert ngokwekhemikhali
I-HPMC luhlobo lwe-ether ye-cellulose engekho i-ionic, isisombululo sayo asinayo i-ionic intlawulo kwaye ayisebenzi kunye neetyuwa zetsimbi okanye i-ionic organic compounds, ngoko ke ezinye izinto ezincedisayo aziyi kusabela ngayo ngexesha lenkqubo yokuvelisa amalungiselelo.
2.3 Uzinzo
Izinzile kwi-asidi kunye ne-alkali, kwaye inokugcinwa ixesha elide phakathi kwe-pH 3 kunye ne-11 ngaphandle kotshintsho oluphawulekayo kwi-viscosity. Isisombululo se-aqueous se-HPMC sinomphumela wokulwa nomkhuhlane kwaye sigcina 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.).
2.4 I-Viscosity Adjustability
I-viscosity derivatives eyahlukeneyo ye-HPMC inokuxutywa ngokwemilinganiselo eyahlukeneyo, kwaye i-viscosity yayo ingatshintshwa ngokomthetho othile, kwaye inobudlelwane obuhle bomgca, ngoko ke umlinganiselo unokukhethwa ngokweemfuno.
2.5 Ukungazinzi kweMetabolic
I-HPMC ayifunxanga okanye ixutywe emzimbeni, kwaye ayiboneleli ngobushushu, ngoko ke iyindawo ekhuselekileyo yokulungiselela amayeza. 2.6 Ukhuseleko Ngokuqhelekileyo kuqwalaselwa ukuba i-HPMC yinto engabonakaliyo kwaye ingenabuhlungu, i-dose ebulalayo ephakathi kweegundane yi-5 g·kg - 1, kunye ne-median ebulalayo ye-rats yi-5. 2 g · kg - 1. Umthamo wemihla ngemihla awunabungozi kumzimba womntu.
3.Ukusetyenziswa kweHPMC kwimixube
3.1 Njengezinto zokugquma ifilimu kunye nezinto zokwenza ifilimu
Ukusebenzisa i-HPMC njengesixhobo sethebhulethi egqunywe ngefilimu, icwecwe eligqunyiweyo alinazo iingenelo ezicacileyo zokufihla incasa kunye nenkangeleko xa kuthelekiswa neetafile ezigqunywe ngokwesiko ezifana neetafile ezigqunywe ngeswekile, kodwa ukuqina kwayo, ukuqina kwayo, ukufunxa ukufuma, isidanga sokuqhekeka. , Ukufumana ubunzima bokugubungela kunye nezinye izikhombisi zekhwalithi zingcono. Ibakala eliphantsi le-viscosity yale mveliso lisetyenziswa njengento yokugubungela ifilimu e-soluble yamanzi kwiipilisi kunye neepilisi, kwaye ibakala eliphezulu le-viscosity lisetyenziswa njengento yokugubungela ifilimu kwiinkqubo ze-organic solvent, ngokuqhelekileyo kwi-concentration ye-2% ukuya kwi-20. %.
UZhang Jixing et al. isebenzise indlela yesiphumo somgangatho wokuphucula ukuqulunqwa kwe-premix kunye ne-HPMC njengotyatyazo lwefilimu. Ukuthatha ifilimu yokwenza ifilimu i-HPMC, isixa se-polyvinyl alcohol kunye ne-plasticizer polyethylene glycol njengezinto zophando, amandla okuqina kunye nokunyanzeliswa kwefilimu kunye ne-Viscosity yesisombululo sokugquma ifilimu yisalathiso sokuhlola, kunye nobudlelwane phakathi kokuhlolwa. isalathisi kunye nemiba yokuhlola ichazwa yimodeli yemathematika, kwaye inkqubo yokuqulunqa eyona nto ifunyenwe ekugqibeleni. Ukusetyenziswa kwayo yi-agent eyenza ifilimu ngokulandelelanayo i-hydroxypropyl methylcellulose (HPMCE5) 11.88 g, i-polyvinyl alcohol 24.12 g, i-plasticizer polyethylene glycol 13.00 g, kunye ne-viscosity yokumiswa kokugquma yi-20 mPa · s, ukunyanzeliswa kunye nokufikeleleka kwempembelelo yefilimu . Zhang Yuan yaphucula inkqubo yokulungiselela, wasebenzisa HPMC njengesibophelelo ukubuyisela istatshi slurry, kwaye watshintsha amacwecwe Jiahua ukuba amacwecwe film-coated ukuze kuphuculwe umgangatho amalungiselelo ayo, ukuphucula hygroscopicity yayo, lula ukucima, amacwecwe axengaxengayo, splintered kunye nezinye iingxaki, ukwandisa uzinzo lwethebhulethi. Inkqubo efanelekileyo yokuqulunqa igqitywe ngovavanyo lwe-orthogonal, oko kukuthi, i-slurry concentration yayiyi-2% HPMC kwi-70% yesisombululo se-ethanol ngexesha lokugqoka, kwaye ixesha lokuvuselela ngexesha le-granulation laliyi-15 min. Iziphumo I-Jiahua film-coated tablets ezilungiselelwe yinkqubo entsha kunye nomyalelo waphuculwa kakhulu kwinkangeleko, ixesha lokuhlukana kunye nobunzima obungundoqo kunezo ziveliswa yinkqubo yomyalelo wokuqala, kwaye izinga elifanelekileyo leepilisi ezifakwe kwifilimu liphuculwe kakhulu. ifikelele ngaphezu kwama-95%. U-Liang Meiyi, uLu Xiaohui, njl. njl kuchaphazela ukukhutshwa kweziyobisi. U-Huang Yunran ulungiselele i-Dragon's Blood Colon Positioning Tablets, kwaye wasebenzisa i-HPMC kwisisombululo sokugquma umaleko wokudumba, kwaye iqhezu layo lobunzima laliyi-5%. Ingabonwa ukuba i-HPMC ingasetyenziswa ngokubanzi kwinkqubo yonikezelo lwamachiza ekujoliswe kuyo kwikholoni.
I-Hydroxypropyl methylcellulose ayiyona nje into egqwesileyo yokugquma ifilimu, kodwa ingasetyenziselwa njengento yokwenza ifilimu ekuqulunqweni kwefilimu. Wang Tongshun njl. ziphuculwe kummiselo wekhompawundi zinc licorice kunye aminolexanol oral composite film, kunye bhetyebhetye, ukufana, ukugudiswa, elubala ye-arhente ifilimu njengesalathiso sophando, ukufumana amayeza elona liphezulu PVA 6.5 g, HPMC 0.1 g kunye 6.0 g ye ipropylene glycol iyahlangabezana neemfuno zokukhutshwa kancinci kunye nokhuseleko, kwaye ingasetyenziswa njengolungiselelo Ummiselo wefilimu edibeneyo.
3.2 njengesibophelelo kunye nesichithakeleyo
Ibakala eliphantsi le-viscosity yale mveliso lingasetyenziselwa njenge-binder kunye ne-disintegrant yamacwecwe, iipilisi kunye neegranules, kunye nebakala eliphezulu le-viscosity lingasetyenziselwa kuphela njenge-binder. Idosi iyahluka ngeemodeli ezahlukeneyo kunye neemfuno. Ngokuqhelekileyo, idosi ye-binder kwiipilisi ezomileyo ze-granulation yi-5%, kunye ne-dosage ye-binder kwiipilisi ezimanzi ze-granulation yi-2%.
U-Li Houtao et al uhlolisise i-binder yeepilisi ze-tinidazole. I-8% ye-polyvinylpyrrolidone (i-PVP-K30), i-40% isiraphu, i-10% ye-starch slurry, i-2.0% i-hydroxypropyl methylcellulose K4 (HPMCK4M), i-50% ye-ethanol yaphandwa njenge-adhesion yamacwecwe e-tinidazole ngokulandelelana. ukulungiswa kweepilisi ze-tinidazole. Ukutshintsha kwembonakalo yeepilisi ezicacileyo kunye nasemva kokugquma kwathelekiswa, kunye nokunyanzeliswa, ukuqina, umda wexesha lokuchithwa kunye nesantya sokuchithwa kwamacwecwe ahlukeneyo amiselweyo. Iziphumo Iipilisi ezilungiselelwe yi-2.0% ye-hydroxypropyl methylcellulose zazicwebezelisa, kwaye umlinganiselo wobunzima awufumananga i-edge chipping kunye ne-corning phenomenon, kwaye emva kokugquma, imilo yethebhulethi yayiphelele kwaye imbonakalo yayilungile. Ngoko ke, iipilisi ze-tinidazole ezilungiselelwe nge-2.0% HPMC-K4 kunye ne-50% ye-ethanol njengezibophelelo zisetyenzisiwe. UGuan Shihai wafunda inkqubo yokuqulunqa iiFuganning Tablets, wahlola i-adhesives, kwaye wahlola i-ethanol ye-50%, i-15% ye-starch paste, i-10% ye-PVP kunye ne-50% yezisombululo ze-ethanol kunye nokunyanzeliswa, ukuguda, kunye nokuqina njengezibonakaliso zokuvavanya. , 5% CMC-Na kunye ne-15% isisombululo se-HPMC (5 mPa s). Iziphumo Amaphepha alungiswe yi-50% ethanol, i-15% ye-starch paste, i-10% ye-PVP 50% isisombululo se-ethanol kunye ne-5% ye-CMC-Na yayinomgangatho ogudileyo, kodwa ukunyanzeliswa kakubi kunye nobunzima obuphantsi, obungenako ukuhlangabezana neemfuno zokugquma; Isisombululo se-15% se-HPMC ( 5 mPa · s), ubuso bethebhulethi buhamba kakuhle, i-friability ifanelekile, kwaye i-compressibility ilungile, enokuthi ihlangabezane neemfuno zokugqoka. Ngoko ke, i-HPMC (i-5 mPa s) yakhethwa njenge-adhesive.
3.3 njenge-arhente exhomayo
Umgangatho ophezulu we-viscosity wale mveliso usetyenziswa njenge-arhente yokumisa ukulungiselela ukulungiswa kolwelo lokumiswa. Inesiphumo esihle sokunqumamisa, kulula ukuphinda isasazeke, ayibambeleli eludongeni, kwaye inamasuntswana amahle e-flocculation. Idosi eqhelekileyo yi-0.5% ukuya kwi-1.5%. Ingoma uTian et al. esetyenziswa ngokuqhelekileyo izixhobo zepolymer (i-hydroxypropyl methylcellulose, i-sodium carboxymethylcellulose, i-povidone, i-xanthan gum, i-methylcellulose, njl.) njengee-arhente zokumisa ukulungiselela i-racecadotril. ukumiswa okomileyo. Ngokusebenzisa i-sedimentation volume ratio ye-suspensions eyahlukeneyo, i-redispersibility index, kunye ne-rheology, i-viscosity yokumiswa kunye ne-morphology ye-microscopic yabonwa, kunye nokuzinza kwamasuntswana eziyobisi phantsi kovavanyo olukhawulezileyo nalo lwaphandwa. Iziphumo Ukunqunyanyiswa okomileyo okulungiselelwe nge-2% HPMC njengoko i-arhente yokuxhoma yayinenkqubo elula kunye nokuzinza okulungileyo.
Xa kuthelekiswa ne-methyl cellulose, i-hydroxypropyl methyl cellulose ineempawu zokwenza isisombululo esicacileyo, kwaye kukho kuphela inani elincinci lezinto ezingenakusasazwa, ngoko ke i-HPMC isetyenziswa ngokuqhelekileyo njenge-arhente yokumisa kumalungiselelo e-ophthalmic. ULiu Jie et al. esetyenzisiweyo i-HPMC, i-hydroxypropyl cellulose (HPC), i-carbomer 940, i-polyethylene glycol (PEG), i-sodium hyaluronate (HA) kunye nokudityaniswa kwe-HA / HPMC njengee-agent zokumisa ukulungiselela ukucaciswa okungafaniyo kwe-Ciclovir ophthalmic suspension, i-sedimentation volume ratio, ubukhulu be-particle kunye ne-dispersibility zikhethwa njengezalathi zokuhlola ukuhluza eyona arhente ixhomileyo. Iziphumo zibonisa ukuba i-acyclovir ophthalmic suspension elungiselelwe yi-0.05% HA kunye ne-0.05% ye-HPMC njenge-arhente yokumisa, umlinganiselo we-sedimentation volume ngu-0.998, ubungakanani be-particle size, i-redispersibility ilungile, kwaye ukulungiswa kuzinzile ukwanda kwesondo.
3.4 Njenge-blocker, i-arhente yokukhulula ecothayo nelawulwayo kunye ne-pore-forming agent
Umgangatho ophezulu we-viscosity wale mveliso usetyenziselwa ukulungiswa kweepilisi ze-hydrophilic gel matrix ezihlala zikhutshwa, i-blockers kunye ne-controlled-release-release agents ye-mixed-matrix yokukhutshwa okuzinzileyo, kwaye inomphumela wokulibazisa ukukhutshwa kweziyobisi. Ukugxininiswa kwayo yi-10% ukuya kwi-80%. Amanqanaba e-low-viscosity asetyenziswa njenge-porogens yokukhululwa okuzinzileyo okanye ukukhutshwa okulawulwayo kwamalungiselelo. I-dose yokuqala efunekayo kwimpembelelo yonyango yaloo macwecwe inokufikelelwa ngokukhawuleza, kwaye emva koko ukukhutshwa okuzinzileyo okanye ukukhutshwa okulawulwayo kwenziwa, kwaye ugxininiso lweziyobisi lwegazi olusebenzayo lugcinwa emzimbeni. . IHydroxypropyl methylcellulose ifakwe emanzini ukwenza umaleko wejeli xa idibana namanzi. Indlela yokukhutshwa kweziyobisi kwithebhulethi ye-matrix ikakhulu ibandakanya ukusasazwa komgangatho wejeli kunye nokukhukuliseka komgangatho wejeli. UJung Bo Shim et al ulungiselele i-carvedilol iipilisi ezikhutshwa ngokuzinzileyo kunye ne-HPMC njengezinto ezikhutshwa ngokuzinzileyo.
IHydroxypropyl methylcellulose ikwasetyenziswa ngokubanzi kwiipilisi zematrix ezizinzileyo zamayeza esintu aseTshayina, kwaye uninzi lwezithako ezisebenzayo, iindawo ezisebenzayo kunye nolungiselelo olunye lwamayeza esintu aseTshayina asetyenziswa. U-Liu Wen et al. isebenzise i-15% ye-hydroxypropyl methylcellulose njengento ye-matrix, i-1% ye-lactose kunye ne-5% ye-microcrystalline cellulose njenge-fillers, kwaye ilungiselele i-Jingfang Taohe Chengqi Decoction kwi-matrix yomlomo iipilisi ezikhutshwa ngokuqhubekayo. Imodeli yi-equation ye-Higuchi. Inkqubo yokuqulunqa ifomyula ilula, ukulungiswa kulula, kwaye idatha yokukhulula izinzile, ehlangabezana neemfuno ze-Chinese Pharmacopoeia. Tang Guanguang et al. isebenzise i-saponins iyonke ye-Astragalus njengechiza eliyimodeli, yalungisa iipilisi zematriki ze-HPMC, kwaye yaphonononga izinto ezichaphazela ukukhutshwa kwechiza kwiindawo ezisebenzayo zamayeza emveli aseTshayina kwiipilisi zematrix zeHPMC. Iziphumo Njengoko idosi ye-HPMC isonyuka, ukukhutshwa kwe-astragaloside kwehlile, kwaye ipesenti yokukhutshwa kwechiza yayinobudlelwane obuphantse bube mgca kunye nezinga lokuchithwa kwe-matrix. Kwithebhulethi ye-matrix ye-hypromellose ye-HPMC, kukho ubudlelwane obuthile phakathi kokukhululwa kwenxalenye esebenzayo yeyeza lemveli laseTshayina kunye nedosi kunye nohlobo lwe-HPMC, kunye nenkqubo yokukhululwa kwe-hydrophilic chemical monomer iyafana nayo. I-Hydroxypropyl methylcellulose ayifanelekanga kuphela kwiikhompawundi ze-hydrophilic, kodwa nakwizinto ezingekho phantsi kwe-hydrophilic. U-Liu Guihua wasebenzisa i-17% ye-hydroxypropyl methylcellulose (HPMCK15M) njengento eqhubekayo yokukhupha i-matrix, kwaye ilungiselele iipilisi ze-matrix ze-Tianshan Xuelian eziqhubekayo ngokuxutywa kwe-granulation kunye ne-tableting. Ukukhutshwa okuzinzileyo kwakucacile, kwaye inkqubo yamalungiselelo yayizinzile kwaye inokwenzeka.
IHydroxypropyl methylcellulose ayisetyenziswanga kuphela kwiipilisi zematrix ezikhutshwa ngokuzinzileyo zezithako ezisebenzayo kunye neendawo ezisebenzayo zamayeza esintu aseTshayina, kodwa zisetyenziswa ngakumbi nangakumbi kumalungiselelo ekhompawundi yamayeza esintu. Wu Huichao et al. isebenzise i-20% ye-hydroxypropyl methyl cellulose (HPMCK4M) njengesixhobo se-matrix, kwaye yasebenzisa indlela yokunciphisa i-powder ngokuthe ngqo ukulungiselela i-Yizhi hydrophilic gel matrix tablet engakwazi ukukhulula iyeza ngokuqhubekayo kwaye ngokuzinzileyo kwiiyure ze-12. I-Saponin Rg1, i-ginsenoside Rb1 kunye ne-Panax notoginseng saponin R1 zisetyenziswe njengezalathisi zovavanyo ukuphanda ukukhutshwa kwe-vitro, kwaye i-equation yokukhutshwa kwechiza yafakelwe ukufunda indlela yokukhupha ichiza. Iziphumo Indlela yokukhutshwa kwechiza ihambelana ne-zero-order kinetic equation kunye ne-Ritger-Peppas equation, apho i-geniposide yakhululwa yi-non-Fick diffusion, kunye namacandelo amathathu e-Panax notoginseng akhutshwe ngokukhukuliseka kwamathambo.
3.5 Iglu ekhuselayo njenge-thickener kunye ne-colloid
Xa le mveliso isetyenziswa njenge-thickener, ipesenti yoxinaniso eqhelekileyo yi-0.45% ukuya kwi-1.0%. Iyakwazi nokwandisa ukuzinza kweglue ye-hydrophobic, yenza i-colloid ekhuselayo, ithintele amaqhekeza kwi-coalescing kunye ne-agglomerating, ngaloo ndlela inqanda ukubunjwa kwe-sediments. Ipesenti yayo yogxininiso oluqhelekileyo luyi-0.5% ukuya kwi-1.5%.
Wang Zhen et al. wasebenzisa i-L9 orthogonal yokuyila indlela yokuvavanya ukuphanda inkqubo yokulungiselela amayeza e-carbon enema esebenzayo. Iimeko zenkqubo efanelekileyo yokugqitywa kokugqibela kwe-carbon enema ye-carbon activated kukusebenzisa i-0.5% ye-sodium carboxymethyl cellulose kunye ne-2.0% ye-hydroxypropyl methylcellulose (i-HPMC iqulethe i-23.0% yeqela le-methoxyl, i-hydroxypropoxyl Base 11.6%) njenge-thickener, inkqubo inceda ukunyusa umgangatho. uzinzo lwekhabhoni esebenzayo yamayeza. UZhang Zhiqiang et al. iphuhlise i-pH-sensitive levofloxacin hydrochloride ijeli ye-ophthalmic ekulungele ukusetyenziswa kunye nesiphumo esiqhubekayo sokukhululwa, isebenzisa i-carbopol njenge-matrix yejel kunye ne-hydroxypropyl methylcellulose njenge-agent agent. Ummiselo ofanelekileyo ngovavanyo, ekugqibeleni ufumana umyalelo ochanekileyo yi-levofloxacin hydrochloride 0.1 g, carbopol (9400) 3 g, i-hydroxypropyl methylcellulose (E50 LV) 20 g, i-disodium hydrogen 0.35 g, i-phosphoric acid 0.45 g ye-sodium chloride engu-5 yesodium. , 0.03 I-g ye-ethyl paraben, kunye namanzi ongezwa ukwenza i-100 mL. Kuvavanyo, umbhali uhlolisise uchungechunge lwe-hydroxypropyl methylcellulose METHOCEL yeNkampani yeColorcon eneenkcukacha ezahlukeneyo (K4M, E4M, E15 LV, E50LV) ukulungiselela i-thickeners enemilinganiselo eyahlukeneyo, kwaye umphumo wakhetha i-HPMC E50 LV njenge-thickener. I-Thickener ye-pH-sensitive levofloxacin hydrochloride iijeli ezikhawulezayo.
3.6 njengempahla ye-capsule
Ngokuqhelekileyo, i-capsule shell material ye-capsules ikakhulu yi-gelatin. Inkqubo yokuveliswa kwegobolondo ye-capsule ilula, kodwa kukho ezinye iingxaki kunye neziganeko ezifana nokukhuselwa kakubi kumanzi kunye neziyobisi ezingenayo i-oxygen, ukunciphisa ukuchithwa kweziyobisi, kunye nokulibaziseka ukuchithwa kwegobolondo ye-capsule ngexesha lokugcinwa. Ngoko ke, i-hydroxypropyl methylcellulose isetyenziselwa indawo ye-gelatin capsules yokulungiswa kwee-capsules, eziphucula ukuveliswa kwe-capsule kunye nokusetyenziswa kwempembelelo, kwaye ikhuthazwe ngokubanzi ekhaya nakwamanye amazwe.
Ukusebenzisa i-theophylline njengeyeza lokulawula, uPodczeck et al. yafumanisa ukuba izinga lokuchithwa kwechiza lee-capsules ezinamaqokobhe e-hydroxypropyl methylcellulose lalilikhulu kunelo le-gelatin capsules. Isizathu sohlalutyo kukuba ukuchithwa kwe-HPMC kukuchithwa kwe-capsule yonke ngexesha elifanayo, ngelixa ukuchithwa kwe-gelatin capsule kukuchithwa kwesakhiwo senethiwekhi kuqala, kwaye emva koko ukuchithwa kwe-capsule yonke, I-capsule ye-HPMC ifaneleke ngakumbi kwi-Capsule shells ukwenzela ukukhutshwa ngokukhawuleza. Chiwele et al. kwakhona wafumana izigqibo ezifanayo kwaye wathelekisa ukuchithwa kwe-gelatin, i-gelatin / i-polyethylene glycol kunye neegobolondo ze-HPMC. Iziphumo zibonise ukuba iigobolondo ze-HPMC zachithwa ngokukhawuleza phantsi kweemeko ezahlukeneyo ze-pH, ngelixa i-gelatin capsules Ichaphazeleka kakhulu kwiimeko ze-pH ezahlukeneyo. Tang Yue et al. uvavanye uhlobo olutsha lweqokobhe le-capsule kwidosi ephantsi yedosi engenanto yenkqubo yokuthwala i-powder inhaler. Xa kuthelekiswa negobolondo ye-capsule ye-hydroxypropyl methylcellulose kunye negobolondo ye-capsule ye-gelatin, ukuzinza kwegobolondo ye-capsule kunye neempawu zepowder kwigobolondo phantsi kweemeko ezahlukeneyo zaphandwa, kwaye uvavanyo lwe-friability lwenziwa. Iziphumo zibonisa ukuba xa kuthelekiswa ne-gelatin capsules, iigobolondo ze-HPMC ze-capsule zingcono ekuzinzeni nasekukhuseleni umgubo, zinamandla okumelana nokufuma, kwaye zine-friability ephantsi kuneeqokobhe ze-capsule ze-gelatin, ngoko ke i-HPMC i-capsule shells ifaneleka ngakumbi kwii-Capsules zokuphefumula umgubo owomileyo.
3.7 njenge-bioadhesive
Itekhnoloji ye-Bioadhesion isebenzisa izinto ezincedisayo kunye neepolymers ze-bioadhesive. Ngokubambelela kwi-biological mucosa, iphakamisa ukuqhubeka kunye nokuqina koqhagamshelwano phakathi kokulungiswa kunye ne-mucosa, ukuze ichiza likhululwe ngokukhawuleza kwaye lifunxwe yi-mucosa ukufezekisa injongo yonyango. Isetyenziswa kakhulu ngoku. Ukunyangwa kwezifo zendlela yesisu, i-vagin, i-mucosa yomlomo kunye nezinye iindawo.
Itekhnoloji ye-bioadhesion ye-gastrointestinal yinkqubo entsha yokuhanjiswa kwechiza ephuhliswe kwiminyaka yakutshanje. Ayinakwandisa nje ixesha lokuhlala lamalungiselelo eziyobisi kwindlela yesisu, kodwa iphucula ukusebenza koqhagamshelwano phakathi kwechiza kunye nenwebu yeseli kwindawo yokufunxa, itshintsha ulwelo lwenwebu yeseli, kwaye yenza ukungenwa kwechiza kungene. iiseli ezincinci ze-epithelial zamathumbu ziyaphuculwa, ngaloo ndlela ziphucula i-bioavailability yechiza. Wei Keda et al. ihlolisise i-tablet core prescription kunye ne-dosage ye-HPMCK4M kunye ne-Carbomer 940 njengezinto zophando, kwaye yasebenzisa isixhobo sokuzenzela se-bioadhesion ukulinganisa amandla okuxobula phakathi kwethebhulethi kunye ne-biofilm eyenziwe ngomgangatho wamanzi kwingxowa yeplastiki. , kwaye ekugqibeleni ukhethe umxholo we-HPMCK40 kunye ne-carbomer 940 ukuba ibe yi-15 kunye ne-27.5 mg kwindawo efanelekileyo yomyalelo we-NCaEBT ye-tablet cores, ngokulandelanayo, ukulungiselela i-NCaEBT tablet cores, ebonisa ukuba izinto ze-bioadhesive (ezifana ne-hydroxypropyl methylcellulose) inokunciphisa kakhulu Ukuphucula ukunamathela kokulungiselela kwi-tissue.
Amalungiselelo e-oral bioadhesive nayo luhlobo olutsha lwenkqubo yokuhanjiswa kweziyobisi eye yaphononongwa ngakumbi kwiminyaka yakutshanje. Amalungiselelo e-oral bioadhesive angakwazi ukubambelela ichiza kwindawo echaphazelekayo yomlomo womlomo, engagcini nje ukwandisa ixesha lokuhlala kweziyobisi kwi-mucosa yomlomo, kodwa ikhusela i-mucosa yomlomo. Isiphumo esingcono sonyango kunye ne-bioavailability ephuculweyo yeziyobisi. Xue Xiaoyan et al. iphucule ukuqulunqwa kweepilisi ze-insulin ezinamathele ngomlomo, usebenzisa i-apple pectin, i-chitosan, i-carbomer 934P, i-hydroxypropyl methylcellulose (i-HPMC K392) kunye ne-sodium alginate njengezinto ze-bioadhesive, kunye ne-freeze-drying ukulungiselela i-insulin yomlomo. I-Adhesive double layer sheet. I-insulin elungiselelwe i-tablet ye-adhesive yomlomo ine-porous sponge-like structure, ekulungele ukukhutshwa kwe-insulin, kwaye inomaleko okhuselayo we-hydrophobic, onokuqinisekisa ukukhululwa kweyeza kunye nokuphepha ukulahlekelwa kweyeza. Hao Jifu et al. kwakhona walungisa amaso oral-mthubi bioadhesive patches usebenzisa iglu Baiji, HPMC kunye carbomer njengezinto bioadhesive.
Kwiinkqubo zokuziswa kweziyobisi kwilungu lobufazi, iteknoloji ye-bioadhesion nayo isetyenziswe ngokubanzi. Zhu Yuting et al. isetyenzisiwe i-carbomer (CP) kunye ne-HPMC njengezinto ezincamathelayo kunye ne-matrix yokukhululwa okuqhubekayo ukulungiselela iipilisi ze-clotrimazole ze-bioadhesive ze-vaginal ezineendlela ezahlukeneyo kunye nokulinganisa, kunye nokulinganisa ukunamathela kwazo, ixesha lokubambelela kunye nepesenti yokudumba kwimekobume ye-vaginal fluid. , i-prescription efanelekileyo ihlolwe njenge-CP-HPMC1: i-1, i-adhesive sheet elungiselelwe yayinokusebenza kakuhle kokubambelela, kwaye inkqubo yayilula kwaye inokwenzeka.
3.8 njengejeli yezihloko
Njengolungiselelo olunamathele, i-gel inoluhlu lweenzuzo ezifana nokhuseleko, ubuhle, ukucocwa lula, ixabiso eliphantsi, inkqubo yokulungiselela elula, kunye nokuhambelana kakuhle neziyobisi. Isikhokelo sophuhliso. Umzekelo, ijeli ye-transdermal yifomu entsha yedosi efundwe ngakumbi kwiminyaka yakutshanje. Ayinakuphepha kuphela ukutshatyalaliswa kwamachiza kwindlela yesisu kunye nokunciphisa i-peak-to-trough ye-concentration ye-concentration yeziyobisi zegazi, kodwa ibe yenye yeenkqubo ezisebenzayo zokukhupha ichiza ukoyisa iziphumo ebezingalindelekanga zeziyobisi. .
UZhu Jingjie et al. wafunda umphumo weematriki ezahlukeneyo ekukhutshweni kwe-scutellarin alcohol plastid gel in vitro, kwaye ihlolwe nge-carbomer (980NF) kunye ne-hydroxypropyl methylcellulose (HPMCK15M) njenge-matrices ye-gel, kwaye yafumana i-scutellarin efanelekileyo kwi-scutellarin. I-gel matrix ye-alcohol plastids. Iziphumo zovavanyo zibonisa ukuba 1. 0% carbomer, 1. 5% carbomer, 1. 0% carbomer + 1. 0% HPMC, 1. 5% carbomer + 1. 0% HPMC njengoko gel matrix Zombini zifanelekile scutellarin alcohol plastids . Ngexesha lovavanyo, kwafunyaniswa ukuba i-HPMC inokutshintsha indlela yokukhutshwa kwechiza ye-carbomer gel matrix ngokufaka i-kinetic equation yokukhutshwa kwechiza, kwaye i-1.0% ye-HPMC inokuphucula i-1.0% ye-carbomer matrix kunye ne-1.5% ye-carbomer matrix. Isizathu sinokuthi i-HPMC ikhula ngokukhawuleza, kwaye ukwanda ngokukhawuleza kwinqanaba lokuqala lovavanyo kwenza ukuba i-gap ye-molecular ye-carbomer gel imathiriyeli ibe nkulu, ngaloo ndlela isantya sokukhululwa kwechiza. UZhao Wencui et al. isebenzise i-carbomer-934 kunye ne-hydroxypropyl methylcellulose njengabathwali ukulungiselela i-norfloxacin ophthalmic gel. Inkqubo yokulungiselela ilula kwaye inokwenzeka, kwaye umgangatho uhambelana nejel ye-ophthalmic ye "Chinese Pharmacopoeia" (uhlelo lwe-2010) Iimfuno zomgangatho.
3.9 I-precipitation inhibitor ye-self-microemulsifying system
I-Self-microemulsifying drug delivery system (SMEDDS) luhlobo olutsha lwenkqubo yokuhanjiswa kweziyobisi ngomlomo, engumxube odibeneyo, ozinzileyo kunye ocacileyo owenziwe ngamachiza, isigaba seoli, i-emulsifier kunye ne-co-emulsifier. Ukuqulunqwa komyalelo ulula, kwaye ukhuseleko kunye nokuzinza kulungile. Amachiza anganyibiliki kakuhle, izixhobo zepolymer ezinyibilikayo emanzini, ezifana ne-HPMC, i-polyvinylpyrrolidone (PVP), njl. ukwandisa ukunyibilika kwechiza kunye nokuphucula i-bioavailability.
Peng Xuan et al. ilungise i-silibinin supersaturated self-emulsifying drug delivery system (S-SEDDS). I-Oxyethylene hydrogenated castor oil (Cremophor RH40), 12% caprylic capric acid polyethylene glycol glyceride (Labrasol) njenge-co-emulsifier, kunye ne-50 mg · g-1 HPMC. Ukongeza i-HPMC kwi-SSEDDS inokunyusa i-silibinin yasimahla ukuze inyibilike kwi-S-SEDDS kwaye ithintele i-silibinin ekuphumeni. Xa kuthelekiswa nokwenziwa kwe-self-microemulsion formulations, inani elikhulu le-surfactant lidla ngokudityaniswa ukunqanda ukugqunywa kwechiza okungaphelelanga. Ukongezwa kwe-HPMC kunokugcina ukunyibilika kwe-silibinin kwindawo yokuchithwa ngokuthe rhoqo, ukunciphisa i-emulsification kwi-self-microemulsion formulations. umthamo we-arhente.
4.Isiphelo
Ingabonwa ukuba i-HPMC isetyenziswe ngokubanzi kumalungiselelo ngenxa yeempawu zayo zomzimba, iikhemikhali kunye ne-biological, kodwa i-HPMC nayo ineziphene ezininzi kumalungiselelo, njengesiganeko sokukhululwa kwangaphambili kunye nasemva kokuqhuma. methyl methacrylate) ukuphucula. Kwangelo xesha, abanye abaphandi baphanda ngokusetyenziswa kwethiyori ye-osmotic kwi-HPMC ngokulungiselela iipilisi ezikhutshwa rhoqo ze-carbamazepine kunye ne-verapamil hydrochloride ekhupha iipilisi eziqhubekayo ukuze ziqhubeke nokufunda indlela yokukhululwa kwayo. Ngelizwi, ngakumbi nangakumbi abaphandi benza umsebenzi omninzi wokusetyenziswa okungcono kwe-HPMC kumalungiselelo, kunye nophando olunzulu lweempawu zayo kunye nokuphuculwa kobugcisa bokulungiselela, i-HPMC iya kusetyenziswa ngokubanzi kwiifom zedosi entsha. kunye neefom ezintsha zedosi. Kuphando lwenkqubo yamachiza, kwaye emva koko ukhuthaze uphuhliso oluqhubekayo lwekhemesti.
Ixesha lokuposa: Oct-08-2022