Iincwadi ezinxulumene noko ekhaya nakwamanye amazwe ekulungiseleleni izinto ezincedisayo zamayeza i-hydroxypropyl methylcellulose (HPMC) kwiminyaka yakutshanje zihlolwe, zahlalutywa zaza zashwankathelwa, kunye nokusetyenziswa kwayo kumalungiselelo aqinileyo, amalungiselelo olwelo, amalungiselelo okukhululwa ahlala ixesha elide nalawulwayo, amalungiselelo e-capsule, i-gelatin. Izicelo zamva nje kwicandelo leefomyula ezintsha ezifana neefomyula zokuncamathelisa kunye nee-bioadhesives. Ngenxa yomahluko kubunzima beemolekyuli kunye ne-viscosity ye-HPMC, ineempawu kunye nokusetyenziswa kwe-emulsification, ukunamathela, ukuqina, i-viscosity eyandayo, ukuxhoma, i-gelling kunye nokwenza ifilimu. Isetyenziswa kakhulu kumalungiselelo amachiza kwaye iya kudlala indima enkulu kwicandelo lamalungiselelo. Ngophando olunzulu lweempawu zayo kunye nokuphuculwa kwetekhnoloji yokwenza, i-HPMC iya kusetyenziswa kakhulu kuphando lweefom ezintsha zedosi kunye neenkqubo ezintsha zokuhambisa amayeza, ngaloo ndlela ikhuthaza uphuhliso oluqhubekayo lwefomyula.
i-hydroxypropyl methylcellulose; amalungiselelo amayeza; izinto ezincedisayo amayeza.
Izinto ezincedisayo kumayeza azisiso nje kuphela isiseko esibalulekileyo sokwenziwa kwamayeza aluhlaza, kodwa zikwanxulumene nobunzima benkqubo yokulungiselela, umgangatho wamayeza, uzinzo, ukhuseleko, izinga lokukhululwa kwamayeza, indlela yokusebenza, ukusebenza kakuhle kwezonyango, kunye nophuhliso lweefom ezintsha zedosi kunye neendlela ezintsha zolawulo. Ukuvela kwezinto ezincedayo kumayeza kudla ngokukhuthaza ukuphuculwa komgangatho wokulungiselela kunye nophuhliso lweefom ezintsha zedosi. I-Hydroxypropyl methylcellulose (HPMC) yenye yezona zinto zincedayo kumayeza ekhaya nakwamanye amazwe. Ngenxa yobunzima bayo obahlukeneyo beemolekyuli kunye ne-viscosity, inemisebenzi yokuxuba, ukubopha, ukuqina, ukuqina, ukuxhoma, kunye nokuncamathisela. Iimpawu kunye nokusetyenziswa okufana nokuxinana kunye nokwakheka kwefilimu kusetyenziswa kakhulu kubuchwepheshe bamayeza. Eli nqaku liphonononga ikakhulu ukusetyenziswa kwe-hydroxypropyl methylcellulose (HPMC) kwiifomyula kwiminyaka yakutshanje.
1.Iimpawu ezisisiseko ze-HPMC
I-Hydroxypropyl methyl cellulose (HPMC), ifomula yemolekyuli yi-C8H15O8-(C10 H18O6) n-C8H15O8, kwaye ubunzima bemolekyuli obuhambelanayo bumalunga ne-86 000. Le mveliso yinto eyenziwe ngokwe-semi-synthetic, eyinxalenye ye-methyl kunye nenxalenye ye-polyhydroxypropyl ether ye-cellulose. Ingaveliswa ngeendlela ezimbini: Enye kukuba i-methyl cellulose yodidi olufanelekileyo iphathwa nge-NaOH ize ixutywe ne-propylene 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. Iqhagamshelwe kwindandatho ye-anhydroglucose ye-cellulose ngendlela ye-cellulose, kwaye inokufikelela kwinqanaba elifunekayo; enye kukuphatha i-cotton linter okanye i-wood pulp fiber nge-caustic soda, ize ixutywe ne-chlorinated methane kunye ne-propylene oxide ngokulandelelana, ize emva koko icoceke ngakumbi. , icoliwe ibe ngumgubo okanye iigranules ezintle nezifanayo.
Umbala wale mveliso umhlophe ukuya kumhlophe okobisi, awunavumba kwaye awunancasa, kwaye imo yayo yi-granular okanye i-fibrous easy-flow powder. Le mveliso inokunyibilikiswa emanzini ukuze yenze isisombululo se-colloidal esicacileyo ukuya kumhlophe okobisi esine-viscosity ethile. Isiganeko sokuguqulwa kwe-sol-gel sinokwenzeka ngenxa yokutshintsha kobushushu besisombululo ngoxinzelelo oluthile.
Ngenxa yomahluko kumxholo wezi zinto zimbini ezithatha indawo kwisakhiwo se-methoxy kunye ne-hydroxypropyl, kuye kwavela iintlobo ezahlukeneyo zeemveliso. Kwizinga elithile, iintlobo ezahlukeneyo zeemveliso zineempawu ezithile. Ubushushu be-viscosity kunye ne-thermal gelation, ngoko ke zineempawu ezahlukeneyo kwaye zinokusetyenziselwa iinjongo ezahlukeneyo. I-Pharmacopoeia yamazwe ahlukeneyo inemigaqo eyahlukeneyo kunye neembonakaliso kwimodeli: I-European Pharmacopoeia isekelwe kwiindidi ezahlukeneyo ze-viscosities ezahlukeneyo kunye namanqanaba ahlukeneyo okutshintshwa kweemveliso ezithengiswa kwimarike, ezichazwe ngamabakala kunye namanani, kwaye iyunithi yi-"mPa s". Kwi-US Pharmacopoeia, amanani ama-4 ongezwe emva kwegama eliqhelekileyo ukubonisa umxholo kunye nohlobo lwe-substituent nganye ye-hydroxypropyl methylcellulose, efana ne-hydroxypropyl methylcellulose 2208. Amanani amabini okuqala amele ixabiso eliqikelelweyo leqela le-methoxy. Ipesenti, amanani amabini okugqibela amele ipesenti eqikelelweyo ye-hydroxypropyl.
I-hydroxypropyl methylcellulose kaCalocan ineentlobo ezintathu, ezizezi uthotho lwe-E, uthotho lwe-F kunye nothotho lwe-K, uthotho ngalunye luneemodeli ezahlukeneyo onokukhetha kuzo. Uthotho lwe-E lusetyenziswa kakhulu njengeengubo zefilimu, lusetyenziselwa ukugquma iithebhulethi, ii-cores zethebhulethi ezivaliweyo; Uthotho lwe-E, lwe-F lusetyenziswa njengee-viscosifiers kunye nee-release retarding agents kumalungiselelo amehlo, ii-suspending agents, ii-thickeners kumalungiselelo olwelo, iithebhulethi kunye nee-Binders ze-granules; Uthotho lwe-K lusetyenziswa kakhulu njengee-release inhibitors kunye nezixhobo ze-hydrophilic gel matrix kumalungiselelo okukhululwa acothayo nalawulwayo.
Abavelisi basekhaya ikakhulu baquka iFuzhou No. 2 Chemical Factory, iHuzhou Food and Chemical Co., Ltd., iSichuan Luzhou Pharmaceutical Accessories Factory, iHubei Jinxian Chemical Factory No. 1, iFeicheng Ruitai Fine Chemical Co., Ltd., iShandong Liaocheng Ahua Pharmaceutical Co., Ltd., izityalo zeekhemikhali zaseXi'an Huian, njl.
2.Iingenelo ze-HPMC
I-HPMC iye yaba yenye yezona zinto zisetyenziswa kakhulu ekuphekeni amayeza ekhaya nakwamanye amazwe, kuba i-HPMC inezibonelelo ezingenazo ezinye izinto ezincedayo.
2.1 Ukunyibilika kwamanzi abandayo
Inyibilika emanzini abandayo angaphantsi kwama-40 ℃ okanye ama-70% e-ethanol, ayinyibiliki emanzini ashushu angaphezu kwama-60 ℃, kodwa ingayigalela ijeli.
2.2 Ikhemikhali engasebenzi kakuhle
I-HPMC luhlobo lwe-non-ionic cellulose ether, isisombululo sayo asinayo i-ionic charge kwaye asidibani neetyuwa zesinyithi okanye ii-ionic organic compounds, ngoko ke ezinye izinto ezincedisayo azisabelani nayo ngexesha lenkqubo yokuvelisa amalungiselelo.
2.3 Uzinzo
Izinzile kwi-asidi kunye ne-alkali, kwaye ingagcinwa ixesha elide phakathi kwe-pH 3 kunye ne-11 ngaphandle kotshintsho olukhulu kwi-viscosity. Isisombululo samanzi se-HPMC sinefuthe lokulwa nokungunda kwaye sigcina uzinzo oluhle lwe-viscosity ngexesha lokugcina ixesha elide. Izinto ezisetyenziswa ngamayeza ezisebenzisa i-HPMC zinozinzo olungcono kunolo zisebenzisa izinto ezisetyenziswa ngamayeza zemveli (ezifana ne-dextrin, istarch, njl.njl.).
2.4 Ukulungelelaniswa kokubonakala kwe-viscosity
Ii-viscosity derivatives ezahlukeneyo ze-HPMC zinokuxutywa ngomlinganiselo owahlukileyo, kwaye i-viscosity yayo inokutshintshwa ngokomthetho othile, kwaye inobudlelwane obuhle obuchanekileyo, ngoko ke umlinganiselo unokukhethwa ngokweemfuno.
2.5 Ukungakwazi ukusebenza kwe-metabolic
I-HPMC ayifunxwa okanye ayigaywanga emzimbeni, kwaye ayiboneleli ngobushushu, ngoko ke ingumxumi okhuselekileyo wokulungiselela amayeza. 2.6 Ukhuseleko Ngokuqhelekileyo kuthathwa njenge-HPMC yinto engenabungozi kwaye engacaphukisiyo, idosi ephakathi ebulalayo kwiimpuku yi-5 g·kg – 1, kwaye idosi ephakathi ebulalayo kwiimpuku yi-5. 2 g · kg – 1. Idosi yemihla ngemihla ayinabungozi emzimbeni womntu.
3.Ukusetyenziswa kwe-HPMC kwiifomyula
3.1 Njengezinto zokugquma ifilimu kunye nezinto zokwenza ifilimu
Isebenzisa i-HPMC njengesixhobo sethebhulethi esigqunywe ngefilimu, ithebhulethi egqunywe ngefilimu ayinazo iingenelo ezicacileyo zokufihla incasa kunye nenkangeleko xa ithelekiswa neethebhulethi zemveli ezigqunywe ngeswekile, kodwa ubulukhuni bayo, ukugungqa kwayo, ukufunxwa komswakama, inqanaba lokuqhekeka, ukutyeba kobunzima kunye nezinye izalathisi zomgangatho zingcono. Umgangatho ophantsi wokuqina kwale mveliso usetyenziswa njengesixhobo sokugcoba ifilimu esinyibilikayo emanzini kwiithebhulethi kunye neepilisi, kwaye umgangatho ophezulu wokuqina usetyenziswa njengesixhobo sokugcoba ifilimu kwiinkqubo ze-organic solvent, ngokuqhelekileyo kuxinzelelo lwe-2% ukuya kwi-20%.
UZhang Jixing nabanye basebenzise indlela yomphezulu wesiphumo ukuphucula ukwakheka kwe-premix nge-HPMC njengombala wefilimu. Ukuthatha izinto zokwenza ifilimu i-HPMC, ubungakanani be-polyvinyl alcohol kunye ne-plasticizer polyethylene glycol njengezinto zophando, amandla okutsalwa kunye nokuphuma kwefilimu kunye ne-viscosity yesisombululo sokutsalwa kwefilimu yi-index yokuhlolwa, kwaye ubudlelwane phakathi kwe-index yokuhlolwa kunye nezinto zokuhlola buchazwa yimodeli yemathematika, kwaye inkqubo efanelekileyo yokwenziwa ekugqibeleni ifunyenwe. Ukusetyenziswa kwayo ngokulandelelanayo yi-arhente yokwenza ifilimu i-hydroxypropyl methylcellulose (HPMCE5) 11.88 g, i-polyvinyl alcohol 24.12 g, i-plasticizer polyethylene glycol 13.00 g, kwaye i-viscosity yokumiswa kwe-coating yi-20 mPa·s, ukutsalwa kunye namandla okutsalwa kwefilimu kufikelele kwisiphumo esingcono. UZhang Yuan uphucule inkqubo yokulungiselela, wasebenzisa i-HPMC njengesixhobo sokubopha endaweni yesitatshi, waza watshintsha iithebhulethi zeJiahua kwiithebhulethi ezigqunywe ngefilimu ukuphucula umgangatho wamalungiselelo azo, ukuphucula i-hygroscopicity yazo, ukufiphala lula, iithebhulethi ezikhululekileyo, iingxaki eziqhekekileyo nezinye, ukuphucula uzinzo lwethebhulethi. Inkqubo efanelekileyo yokwenza imiselwe ngovavanyo oluhambelanayo, oko kukuthi, uxinaniso lwe-slurry yayiyi-2% HPMC kwisisombululo se-ethanol esingu-70% ngexesha lokugquma, kwaye ixesha lokuxubha ngexesha lokuxutywa yayiyi-15 min. Iziphumo Iithebhulethi ezigqunywe ngefilimu zeJiahua ezilungiselelwe yinkqubo entsha kunye nomyalelo ziphuculwe kakhulu kwinkangeleko, ixesha lokuqhekeka kunye nobunzima obuphakathi kunezo zenziwe yinkqubo yokuqala yomyalelo, kwaye izinga elifanelekileyo leethebhulethi ezigqunywe ngefilimu liphuculwe kakhulu. zifikelele ngaphezulu kwe-95%. ULiang Meiyi, uLu Xiaohui, njl. njl. basebenzise i-hydroxypropyl methylcellulose njengezinto zokwenza ifilimu ukulungiselela ithebhulethi yokubeka ikholoni ye-patinae kunye nethebhulethi yokubeka ikholoni ye-matrine, ngokwahlukeneyo. zichaphazela ukukhululwa kweziyobisi. UHuang Yunran walungisa iipilisi zokubeka ikholoni yegazi leDragon's Blood Colon, waza wafaka iHPMC kwisisombululo sokugquma somaleko wokudumba, kwaye ubunzima bayo babuyi-5%. Kuyabonakala ukuba iHPMC ingasetyenziswa kakhulu kwinkqubo yokuhambisa amayeza ajoliswe kumathumbu amakhulu.
I-Hydroxypropyl methylcellulose ayisiyonto ibalaseleyo yokugquma ifilimu kuphela, kodwa ingasetyenziswa njengezinto zokwenza ifilimu kwiifomyula zefilimu. I-Wang Tongshun njl. zilungiselelwe ukumiselwa kwe-compound zinc licorice kunye ne-aminolexanol oral composite film, kunye nokuguquguquka, ukufana, ukugudileyo, ukucaca kwearhente yefilimu njengesalathisi sophando, ukufumana i-prescription efanelekileyo yi-PVA 6.5 g, i-HPMC 0.1 g kunye ne-6.0 g ye-propylene glycol ukuhlangabezana neemfuno zokukhululwa kancinci kunye nokhuseleko, kwaye zingasetyenziswa njengeprescription yokulungiselela ifilimu edibeneyo.
3.2 njenge-binder kunye ne-disintegrant
Umgangatho ophantsi we-viscosity wale mveliso ungasetyenziswa njenge-binder kunye ne-disintegrant kwiipilisi, iipilisi kunye nee-granules, kwaye umgangatho ophezulu we-viscosity ungasetyenziswa kuphela njenge-binder. Umthamo uyahluka ngokweemodeli kunye neemfuno ezahlukeneyo. Ngokubanzi, umthamo we-binder kwiipilisi ze-granulation ezomileyo yi-5%, kwaye umthamo we-binder kwiipilisi ze-granulation ezimanzi yi-2%.
ULi Houtao nabanye bahlolisise i-binder yeetablethi ze-tinidazole. I-8% ye-polyvinylpyrrolidone (PVP-K30), i-40% yesiraphu, i-10% yesitatshi esimdaka, i-2.0% ye-hydroxypropyl methylcellulose K4 (HPMCK4M), i-50% ye-ethanol ziphandwe njengokunamathela kweetablethi ze-tinidazole ngokulandelelana. Utshintsho lwembonakalo yeetablethi ezicacileyo kunye nokwaleka emva kokwaleka luthelekiswe, kwaye ukuqhekeka, ubunzima, umda wexesha lokuqhekeka kunye nesantya sokunyibilika kweetablethi ezahlukeneyo ezimiselweyo zilinganisiwe. Iziphumo Iitablethi ezilungiselelwe nge-2.0% ye-hydroxypropyl methylcellulose zazikhazimla, kwaye umlinganiselo wokuqhekeka awufumananga nto yokuqhekeka komphetho kunye nokugoba, kwaye emva kokwaleka, imo yethebhulethi yayiphelele kwaye imbonakalo yayilungile. Ke ngoko, iitablethi ze-tinidazole ezilungiselelwe nge-2.0% ye-HPMC-K4 kunye ne-50% ye-ethanol njengezihlanganisi zisetyenzisiwe. UGuan Shihai wafunda inkqubo yokwenziwa kweeFuganning Tablets, wavavanya izincamathelisi, waza wavavanya i-ethanol engama-50%, i-starch paste eyi-15%, i-PVP eyi-10% kunye ne-ethanol engama-50% ene-compressability, smoothness, kunye ne-friability njengezalathi zovavanyo. , Isisombululo se-5% CMC-Na kunye ne-15% HPMC (5 mPa s). Iziphumo Amaphepha alungiselelwe yi-ethanol engama-50%, i-starch paste eyi-15%, isisombululo se-ethanol esiyi-10% PVP eyi-50% kunye ne-5% CMC-Na ayenomphezulu ogudileyo, kodwa ucinezeleka kakubi kunye nobunzima obuphantsi, obungenakuhlangabezana neemfuno zokufaka; Isisombululo se-HPMC esiyi-15% (5 mPa·s), umphezulu wethebhulethi uthambile, i-friability iyafaneleka, kwaye i-compressability ilungile, enokuhlangabezana neemfuno zokufaka. Ke ngoko, i-HPMC (5 mPa s) yakhethwa njenge-glue.
3.3 njengearhente yokumisa
Umgangatho ophezulu we-viscosity wale mveliso usetyenziswa njenge-agent yokumisa ukulungiselela ulwelo olufana nokumiswa. Inesiphumo esihle sokumisa, kulula ukuyiphinda isasazeke, ayinamatheli eludongeni, kwaye inamasuntswana amancinci e-flocculation. Umthamo oqhelekileyo yi-0.5% ukuya kwi-1.5%. USong Tian nabanye basebenzise izixhobo zepolymer ezisetyenziswa rhoqo (i-hydroxypropyl methylcellulose, i-sodium carboxymethylcellulose, i-povidone, i-xanthan gum, i-methylcellulose, njl.njl.) njengee-agent zokumisa ukulungiselela i-racecadotril. Ukumiswa okomileyo. Ngokusebenzisa umlinganiselo wevolumu ye-sedimentation ye-suspensions ezahlukeneyo, i-redispersibility index, kunye ne-rheology, i-suspension viscosity kunye ne-microscopic morphology zabonwa, kwaye ukuzinza kwamasuntswana eziyobisi phantsi kovavanyo olukhawulezisiweyo nako kwaphandwa. Iziphumo Ukumiswa okomileyo okulungiselelwe nge-2% HPMC njenge-agent yokumisa kwakunenkqubo elula kunye nokuzinza okuhle.
Xa kuthelekiswa ne-methyl cellulose, i-hydroxypropyl methyl cellulose ineempawu zokwenza isisombululo esicacileyo, kwaye kukho inani elincinci kakhulu lezinto ezingenanto zisasazekileyo, ngoko ke i-HPMC ikwasetyenziswa njenge-agent yokumisa kumalungiselelo eliso. ULiu Jie nabanye basebenzise i-HPMC, i-hydroxypropyl cellulose (HPC), i-carbomer 940, i-polyethylene glycol (PEG), i-sodium hyaluronate (HA) kunye nokudibanisa i-HA/HPMC njengee-agent zokumisa ukulungiselela iinkcukacha ezahlukeneyo. Kwi-Ciclovir ophthalmic suspension, umlinganiselo we-sedimentation volume, ubungakanani be-particle kunye ne-redispersibility zikhethwa njengezalathisi zokuhlola ukuze kuhlolwe i-agent yokumisa engcono. Iziphumo zibonisa ukuba i-acyclovir ophthalmic suspension elungiselelwe yi-0.05% HA kunye ne-0.05% HPMC njenge-agent yokumisa, umlinganiselo we-sedimentation volume yi-0.998, ubungakanani be-particle buyafana, i-redispersibility ilungile, kwaye ukulungiswa kuzinzile. Ukwanda kwesondo.
3.4 Njenge-blocker, i-arhente yokukhulula ecothayo nelawulwayo kunye ne-arhente yokwenza iimbobo
Umgangatho ophezulu wokuqaqamba kwale mveliso usetyenziselwa ukulungiselela iipilisi ze-hydrophilic gel matrix sustainable-release, ii-blockers kunye nee-arhente ezilawulwayo zokukhululwa kweepilisi ze-matrix sustainable-release ezixutyiweyo, kwaye zinefuthe lokulibazisa ukukhululwa kwamayeza. Uxinzelelo lwayo yi-10% ukuya kwi-80%. Amanqanaba okuqaqamba aphantsi asetyenziswa njengee-porogens kumalungiselelo okukhululwa okuqhubekayo okanye okulawulwayo. Idosi yokuqala efunekayo kwisiphumo sonyango sale thebhulethi inokufikelelwa ngokukhawuleza, kwaye emva koko isiphumo sokukhululwa okuqhubekayo okanye okulawulwayo siyasebenza, kwaye uxinzelelo olusebenzayo lweziyobisi zegazi lugcinwa emzimbeni. . I-Hydroxypropyl methylcellulose iyamanziswa ukuze yenze umaleko wejeli xa idibana namanzi. Indlela yokukhululwa kwamayeza kwithebhulethi ye-matrix ibandakanya ikakhulu ukusasazwa komaleko wejeli kunye nokukhukuliseka komaleko wejeli. UJung Bo Shim nabanye balungiselele iipilisi ze-carvedilol sustainable-release ezine-HPMC njengezinto ezikhutshwa rhoqo.
I-Hydroxypropyl methylcellulose ikwasetyenziswa kakhulu kwiipilisi ze-matrix ezikhutshwa rhoqo zemithi yesintu yaseTshayina, kwaye uninzi lwezithako ezisebenzayo, iindawo ezisebenzayo kunye nokulungiswa okukodwa kwemithi yesintu yaseTshayina kuyasetyenziswa. ULiu Wen nabanye basebenzise i-15% ye-hydroxypropyl methylcellulose njengezinto ze-matrix, i-1% ye-lactose kunye ne-5% ye-microcrystalline cellulose njengezizalisi, kwaye balungiselela i-Jingfang Taohe Chengqi Decoction kwiipilisi ze-matrix ezikhutshwa rhoqo ze-matrix. Imodeli yi-equation ye-Higuchi. Inkqubo yokwakheka kwefomyula ilula, ukulungiswa kulula, kwaye idatha yokukhululwa izinzile, ehlangabezana neemfuno ze-Chinese Pharmacopoeia. UTang Guanguang nabanye basebenzise i-total saponins ye-Astragalus njengeyeza eliyimodeli, balungiselela iipilisi ze-matrix ze-HPMC, kwaye bahlola izinto ezichaphazela ukukhululwa kweyeza kwiindawo ezisebenzayo zemithi yesintu yaseTshayina kwiipilisi ze-matrix ze-HPMC. Iziphumo Njengoko umthamo we-HPMC usanda, ukukhululwa kwe-astragaloside kwehla, kwaye ipesenti yokukhululwa kweyeza yayinobudlelwane obuphantse bube ngqo kunye nezinga lokunyibilika kwe-matrix. Kwithebhulethi ye-hypromellose HPMC matrix, kukho ubudlelwane obuthile phakathi kokukhululwa kwenxalenye esebenzayo yeyeza lemveli laseTshayina kunye nomthamo kunye nohlobo lwe-HPMC, kwaye inkqubo yokukhululwa kwe-hydrophilic chemical monomer iyafana nayo. I-Hydroxypropyl methylcellulose ayifanelekanga kuphela kwiikhompawundi ze-hydrophilic, kodwa nakwizinto ezingezizo ze-hydrophilic. ULiu Guihua usebenzise i-17% ye-hydroxypropyl methylcellulose (HPMCK15M) njengezinto ze-sustained-release matrix, kwaye walungisa iithebhulethi ze-Tianshan Xuelian sustained-release matrix ngendlela ye-granulation emanzi kunye ne-tableting. Isiphumo sokukhululwa okuqhubekayo sasicacile, kwaye inkqubo yokulungiselela yayizinzile kwaye inokwenzeka.
I-hydroxypropyl methylcellulose ayisetyenziswa kuphela kwiipilisi ze-matrix ezikhutshwa rhoqo zezithako ezisebenzayo kunye neendawo ezisebenzayo zonyango lwendabuko lwaseTshayina, kodwa isetyenziswa ngakumbi nangakumbi kumalungiselelo e-compound amayeza endabuko aseTshayina. UWu Huichao nabanye basebenzise i-20% ye-hydroxypropyl methyl cellulose (HPMCK4M) njengezinto ze-matrix, kwaye basebenzise indlela yokucinezela i-powder direct ukulungiselela ithebhulethi ye-Yizhi hydrophilic gel matrix enokukhupha ichiza ngokuqhubekayo nangokuzinzileyo iiyure ezili-12. I-Saponin Rg1, i-ginsenoside Rb1 kunye ne-Panax notoginseng saponin R1 zisetyenziswe njengezalathi zovavanyo ukuphanda ukukhululwa kwi-vitro, kwaye i-equation yokukhululwa kweziyobisi yafakelwa ukufunda indlela yokukhululwa kweziyobisi. Iziphumo Indlela yokukhululwa kweziyobisi ihambelana ne-equation ye-zero-order kinetic kunye ne-Ritger-Peppas equation, apho i-geniposide yakhululwa yi-non-Fick diffusion, kwaye izinto ezintathu kwi-Panax notoginseng zakhutshwa yi-skeletal erosion.
3.5 Iglu ekhuselayo njenge-thickener kunye ne-colloid
Xa le mveliso isetyenziswa njengesithambisi-manzi, uxinaniso oluqhelekileyo lwepesenti yi-0.45% ukuya kwi-1.0%. Ingakwandisa uzinzo lweglue enganyangekiyo emanzini, yenze i-colloid ekhuselayo, ithintele amasuntswana ukuba angadibani kwaye ahlangane, ngaloo ndlela ithintele ukwakheka kwenkunkuma. Uxinaniso lwayo oluqhelekileyo lwepesenti yi-0.5% ukuya kwi-1.5%.
UWang Zhen nabanye basebenzise indlela yoyilo lwe-L9 orthogonal yokulinga ukuphanda inkqubo yokulungiselela i-enema ye-carbon esebenzayo yamayeza. Iimeko zenkqubo ezifanelekileyo zokumisela kokugqibela i-enema ye-carbon esebenzayo yamayeza kukusebenzisa i-0.5% ye-sodium carboxymethyl cellulose kunye ne-2.0% ye-hydroxypropyl methylcellulose (i-HPMC ineqela le-methoxyl eliyi-23.0%, i-hydroxypropoxyl Base 11.6%) njengesithambisi, iimeko zenkqubo zinceda ukuphucula uzinzo lwe-carbon esebenzayo yamayeza. UZhang Zhiqiang nabanye baphuhlise i-gel ye-levofloxacin hydrochloride ophthalmic ekulungele ukusetyenziswa ene-pH enomphumo wokukhululwa okuqhubekayo, besebenzisa i-carbopol njenge-matrix ye-gel kunye ne-hydroxypropyl methylcellulose njenge-arhente yokutyeba. Umyalelo ofanelekileyo ngovavanyo, ekugqibeleni ufumana umyalelo ofanelekileyo yi-levofloxacin hydrochloride 0.1 g, i-carbopol (9400) 3 g, i-hydroxypropyl methylcellulose (E50 LV) 20 g, i-disodium hydrogen phosphate 0.35 g, i-phosphoric acid 0.45 g ye-sodium dihydrogen, i-0.50 g ye-sodium chloride, i-0.03 g ye-ethyl paraben, kunye namanzi ongeziweyo ukwenza i-100 mL. Kolu vavanyo, umbhali uhlole uthotho lwe-hydroxypropyl methylcellulose METHOCEL lweColorcon Company oluneenkcukacha ezahlukeneyo (K4M, E4M, E15 LV, E50LV) ukulungiselela izithambisi ezinezinga ezahlukeneyo, kwaye isiphumo sikhethe i-HPMC E50 LV njenge-thickener. I-Thickener yee-gels ze-levofloxacin hydrochloride ezikhawulezayo ezinobungqingqwa be-pH.
3.6 njengesixhobo sekhaphu
Ngokwesiqhelo, izinto zegobolondo lekhaphu zekhaphu ikakhulu yigelatin. Inkqubo yokuvelisa igobolondo lekhaphu ilula, kodwa kukho iingxaki kunye neziganeko ezifana nokukhuselwa okungalunganga kumanzi kunye namayeza angena kwioksijini, ukunciphisa ukunyibilika kwamayeza, kunye nokudilizwa okulibazisekileyo kwegobolondo lekhaphu ngexesha lokugcinwa. Ke ngoko, i-hydroxypropyl methylcellulose isetyenziswa endaweni yeekhaphu zekhaphu zegelatin ukulungiselela iikhaphu, nto leyo ephucula ukwakheka kwekhaphu kunye nefuthe lokusetyenziswa, kwaye ikhuthazwe kakhulu ekhaya nakwamanye amazwe.
Esebenzisa i-theophylline njengeyeza lokulawula, uPodczeck nabanye bafumanise ukuba izinga lokunyibilika kwamayeza kwiikhaphu ezineegobolondo ze-hydroxypropyl methylcellulose likhulu kuneekhaphu ze-gelatin. Isizathu sohlalutyo kukuba ukuqhekeka kwe-HPMC kukuqhekeka kwekhaphu yonke ngaxeshanye, ngelixa ukuqhekeka kwekhaphu ye-gelatin kukuqhekeka kwesakhiwo senethiwekhi kuqala, kwaye emva koko kukuqhekeka kwekhaphu yonke, ngoko ke ikhaphu ye-HPMC ifanelekile ngakumbi kwiigobolondo zeCapsule kwiifomyula zokukhululwa kwangoko. UChiwele nabanye bafumene izigqibo ezifanayo kwaye bathelekisa ukunyibilika kwe-gelatin, i-gelatin/polyethylene glycol kunye neegobolondo ze-HPMC. Iziphumo zibonise ukuba iigobolondo ze-HPMC zanyibilika ngokukhawuleza phantsi kweemeko ezahlukeneyo ze-pH, ngelixa iikhaphu ze-gelatin zichaphazeleka kakhulu ziimeko ezahlukeneyo ze-pH. UTang Yue nabanye bahlole uhlobo olutsha lwegobolondo lekhaphu ye-capsule yenkqubo yokuthwala i-inhaler yedosi ephantsi. Xa kuthelekiswa neqokobhe le-capsule le-hydroxypropyl methylcellulose kunye neqokobhe le-capsule le-gelatin, kuphandwe uzinzo lweqokobhe le-capsule kunye neempawu zomgubo kwiqokobhe phantsi kweemeko ezahlukeneyo, kwaye kwenziwa uvavanyo lokuqhekeka. Iziphumo zibonisa ukuba xa kuthelekiswa ne-gelatin capsules, amaqokobhe e-HPMC capsule angcono ngokuqina nokukhusela i-powder, anokumelana nokufuma okunamandla, kwaye anokuqhekeka okuphantsi kunee-gelatin capsule shells, ngoko ke amaqokobhe e-HPMC capsule afanelekile ngakumbi kwi-Capsules zokuphefumla umgubo owomileyo.
3.7 njenge-bioadhesive
Itekhnoloji yokuncamathelisa i-bioadhesion isebenzisa izinto ezincedisayo ezinee-polymers ezincamathelisa i-bioadhesive. Ngokunamathela kwi-mucosa yebhayoloji, kuphucula ukuqhubeka nokuqina konxibelelwano phakathi kokulungiselela kunye ne-mucosa, ukuze iyeza likhutshwe kancinci kwaye lifunxwe yi-mucosa ukufezekisa injongo yonyango. Isetyenziswa kakhulu okwangoku. Unyango lwezifo zendlela yesisu, i-vagina, i-oral mucosa kunye nezinye iindawo.
Itekhnoloji yokuncamathelisa amathumbu yinkqubo entsha yokuhambisa amayeza ephuhliswe kwiminyaka yakutshanje. Ayigcini nje ngokwandisa ixesha lokuhlala kwamalungiselelo amayeza kwindlela yokugaya ukutya, kodwa ikwaphucula ukusebenza koqhagamshelwano phakathi kweyeza kunye ne-membrane yeseli kwindawo yokufunxa, itshintsha ukugeleza kwe-membrane yeseli, kwaye yenza ukuba ukungena kweyeza kwiiseli ze-epithelial zamathumbu amancinci kuphuculwe, ngaloo ndlela kuphucula ukufumaneka kweyeza. UWei Keda nabanye bahlolisise ummiselo wepilisi oyintloko ngedosi ye-HPMCK4M kunye neCarbomer 940 njengezinto zophando, kwaye basebenzise isixhobo sokuncamathelisa amathumbu esenziwe ngokwabo ukulinganisa amandla okuxobuka phakathi kwethebhulethi kunye ne-biofilm elinganisiweyo ngomgangatho wamanzi akwingxowa yeplastiki. , kwaye ekugqibeleni ndikhethe umxholo we-HPMCK40 kunye ne-carbomer 940 ukuba ube yi-15 kunye ne-27.5 mg kwindawo efanelekileyo yonyango lwee-tablet cores ze-NCaEBT, ngokulandelanayo, ukulungiselela ii-tablet cores ze-NCaEBT, nto leyo ebonisa ukuba izinto ezinamathelayo kwi-bioadhesive (ezifana ne-hydroxypropyl methylcellulose) zinokunciphisa kakhulu ukunamathela kokulungiselela kwizicubu.
Amalungiselelo okuncamathelisa ngomlomo nawo luhlobo olutsha lwenkqubo yokuhambisa amayeza oluye lwafundwa ngakumbi kwiminyaka yakutshanje. Amalungiselelo okuncamathelisa ngomlomo anokunamathela kwinxalenye echaphazelekayo yomlomo, nto leyo engagcini nje ngokwandisa ixesha lokuhlala kwesiyobisi kwi-mucosa yomlomo, kodwa ikwakhusela ne-mucosa yomlomo. Isiphumo esingcono sonyango kunye nokufumaneka kakuhle kwamayeza. UXue Xiaoyan nabanye baphucule ukwenziwa kweethebhulethi zokuncamathelisa ngomlomo ze-insulin, besebenzisa i-apple pectin, i-chitosan, i-carbomer 934P, i-hydroxypropyl methylcellulose (HPMC K392) kunye ne-sodium alginate njengezinto zokuncamathelisa emzimbeni, kunye nokomisa ngokukhenkceza ukulungiselela i-insulin yomlomo. Iphepha lokuncamathelisa eliphindwe kabini. Ithebhulethi yokuncamathelisa ngomlomo ye-insulin elungisiweyo inesakhiwo esifana nesiponji esinemingxuma, esilungele ukukhululwa kwe-insulin, kwaye inomaleko wokukhusela we-hydrophobic, onokuqinisekisa ukukhululwa kwesiyobisi kwicala elinye kwaye kuthintele ukulahleka kwesiyobisi. UHao Jifu nabanye balungiselele neepatches zokuncamathelisa ngomlomo ze-blue-yellow beads besebenzisa i-Baiji glue, i-HPMC kunye ne-carbomer njengezinto zokuncamathelisa emzimbeni.
Kwiinkqubo zokuhambisa amayeza kwi-vaginal, iteknoloji ye-bioadhesion nayo isetyenziswa kakhulu. UZhu Yuting nabanye basebenzise i-carbomer (CP) kunye ne-HPMC njengezinto zokuncamathelisa kunye ne-sustained-release matrix ukulungiselela iipilisi ze-clotrimazole bioadhesive vaginal ezineefomyula ezahlukeneyo kunye nemilinganiselo, kwaye balinganisa ukunamathela kwazo, ixesha lokunamathela kunye nepesenti yokudumba kwindawo yolwelo lwe-vaginal olwenziweyo. , iresiphi efanelekileyo yahlolwa njenge-CP-HPMC1: 1, iphepha lokuncamathelisa elilungisiweyo lalinokusebenza okuhle kokunamathela, kwaye inkqubo yayilula kwaye inokwenzeka.
3.8 njengejeli esetyenziswa phezulu
Njengolungiselelo lokuncamathelisa, ijeli ineenzuzo ezininzi ezifana nokhuseleko, ubuhle, ukucocwa okulula, iindleko eziphantsi, inkqubo yokulungiselela elula, kunye nokuhambelana kakuhle namayeza. Isikhokelo sophuhliso. Umzekelo, ijeli ye-transdermal luhlobo olutsha lwedosi oluye lwafundwa ngakumbi kwiminyaka yakutshanje. Ayinakuphepha kuphela ukutshatyalaliswa kwamayeza kwindlela yesisu kwaye inciphise ukutshintsha kwenani leziyobisi egazini ukuya ekutyeni, kodwa ikwayenye yeenkqubo ezisebenzayo zokukhupha amayeza ukuze yoyise iziphumo ebezingalindelekanga zamayeza.
UZhu Jingjie nabanye bafunde impembelelo yee-matrices ezahlukeneyo ekukhutshweni kwejeli yeplastid yotywala ye-scutellarin kwi-vitro, kwaye yahlolwa nge-carbomer (980NF) kunye ne-hydroxypropyl methylcellulose (HPMCK15M) njengee-matrices zejeli, kwaye bafumana i-scutellarin efanelekileyo kwi-scutellarin. I-matrix yejeli yeeplastid zotywala. Iziphumo zovavanyo zibonisa ukuba i-1.0% carbomer, i-1.5% carbomer, i-1.0% carbomer + 1.0% HPMC, i-1.5% carbomer + 1.0% HPMC njenge-matrix yejeli. Zombini zifanelekile kwiiplastid zotywala ze-scutellarin. Ngexesha lovavanyo, kwafunyaniswa ukuba i-HPMC inokutshintsha indlela yokukhululwa kwamayeza kwi-matrix yejeli ye-carbomer ngokufaka i-kinetic equation yokukhululwa kwamayeza, kwaye i-1.0% HPMC inokuphucula i-1.0% carbomer matrix kunye ne-1.5% carbomer matrix. Isizathu sisenokuba kukuba i-HPMC ikhula ngokukhawuleza, kwaye ukwanda ngokukhawuleza kwinqanaba lokuqala lovavanyo kwenza umsantsa weemolekyuli zezinto zejeli ye-carbomer ube mkhulu, ngaloo ndlela kukhawuleziswe izinga lokukhululwa kwamayeza. UZhao Wencui nabanye basebenzise i-carbomer-934 kunye ne-hydroxypropyl methylcellulose njengabathwali ukulungiselela ijeli ye-ophthalmic ye-norfloxacin. Inkqubo yokulungiselela ilula kwaye inokwenzeka, kwaye umgangatho uhambelana nejeli ye-ophthalmic ye-"Chinese Pharmacopoeia" (uhlelo luka-2010) Iimfuno zomgangatho.
3.9 Isithinteli sokuna kwemvula kwinkqubo yokuzixuba ngokwayo
Inkqubo yokuhambisa amayeza e-self-microemulsifying (SMEDDS) luhlobo olutsha lwenkqubo yokuhambisa amayeza ngomlomo, oluyingxubevange efanayo, ezinzileyo necacileyo eyenziwe ngamayeza, isigaba seoli, i-emulsifier kunye ne-co-emulsifier. Ulwakhiwo lweresiphi lulula, kwaye ukhuseleko kunye nozinzo zilungile. Kwiziyobisi ezinganyibilikiyo kakuhle, izinto zepolymer zefayibha ezinyibilikayo emanzini, ezifana ne-HPMC, i-polyvinylpyrrolidone (PVP), njl.njl., zihlala zongezwa ukwenza amayeza asimahla kunye namayeza afakwe kwi-microemulsion afikelele ekunyibilikeni okungaphezulu kwindlela yesisu, ukuze kwandiswe ukunyibilika kwamayeza kwaye kuphuculwe ukufumaneka kwawo.
UPeng Xuan nabanye balungiselele inkqubo yokuhanjiswa kweziyobisi ezizixubayo (S-SEDDS) ene-silicone supersaturated self-emulsifying drug delivery (S-SEDDS). Ioyile ye-castor ene-oxyethylene hydrogenated (Cremophor RH40), i-12% ye-caprylic capric acid polyethylene glycol glyceride (Labrasol) njenge-co-emulsifier, kunye ne-50 mg·g-1 HPMC. Ukongeza i-HPMC kwi-SSEDDS kunokunyusa i-silibinin yasimahla ukuze inyibilike kwi-S-SEDDS kwaye kuthintele ukuba i-silibinin ingangeni. Xa kuthelekiswa ne-self-microemulsion formulations zemveli, inani elikhulu le-surfactant lidla ngokufakwa ukuthintela ukufakwa kwamayeza angaphelelanga. Ukongezwa kwe-HPMC kunokugcina ukunyibilika kwe-silibinin kwindawo yokunyibilikisa kuhleli kungaguquki, kunciphisa i-emulsification kwi-self-microemulsion formulations.
4. Isiphelo
Kuyabonakala ukuba i-HPMC isetyenziswa kakhulu kumalungiselelo ngenxa yeempawu zayo zomzimba, iikhemikhali kunye nezebhayoloji, kodwa i-HPMC ikwanazo neziphene ezininzi kumalungiselelo, ezifana nemeko yokukhululwa ngaphambi nasemva kokuqhuma. Kwangaxeshanye, abanye abaphandi baphande ukusetyenziswa kwethiyori ye-osmotic kwi-HPMC ngokulungiselela iipilisi ze-carbamazepine ezikhutshwayo kunye neepilisi ze-verapamil hydrochloride ezikhutshwayo ukuze bafunde ngakumbi indlela yokukhululwa kwayo. Ngamafutshane, abaphandi abaninzi benza umsebenzi omninzi wokusetyenziswa ngcono kwe-HPMC kumalungiselelo, kwaye ngophando olunzulu lweempawu zayo kunye nokuphuculwa kwetekhnoloji yokulungiselela, i-HPMC iya kusetyenziswa kakhulu kwiifom ezintsha zedosi kunye neefom ezintsha zedosi. Kuphando lwenkqubo yamayeza, kwaye emva koko kukhuthazwe uphuhliso oluqhubekayo lwekhemesti.
Ixesha lokuthumela: Okthobha-08-2022