Mabuku okhudzana ndi izi kunyumba ndi kunja kwa dziko lapansi pakukonzekera zinthu zothandizira mankhwala monga hydroxypropyl methylcellulose (HPMC) m'zaka zaposachedwa adawunikidwanso, kufufuzidwa ndi kufotokozedwa mwachidule, komanso kugwiritsidwa ntchito kwake mu zokonzekera zolimba, kukonzekera madzi, kukonzekera kosasunthika komanso kolamulidwa, kukonzekera kapisozi, gelatin. Ntchito zaposachedwa kwambiri pakupanga zinthu zatsopano monga zomatira ndi zomatira. Chifukwa cha kusiyana kwa kulemera kwa mamolekyulu ndi kukhuthala kwa HPMC, ili ndi mawonekedwe ndi ntchito za emulsification, adhesion, thickening, viscosity increasing, suspensing, gelling ndi film-forming. Imagwiritsidwa ntchito kwambiri pakupanga mankhwala ndipo idzakhala ndi gawo lalikulu pakupanga mankhwala. Ndi kuphunzira mozama za makhalidwe ake komanso kusintha kwa ukadaulo wopanga, HPMC idzagwiritsidwa ntchito kwambiri pakufufuza mitundu yatsopano ya mlingo ndi njira zatsopano zoperekera mankhwala, potero ikulimbikitsa chitukuko chopitilira cha zopangira.
hydroxypropyl methylcellulose; mankhwala okonzekera; zinthu zowonjezera mankhwala.
Zinthu zothandizira mankhwala sizimangoyambira kupanga mankhwala osaphika, komanso zimakhudzana ndi kuvutika kwa njira yokonzekera, ubwino wa mankhwala, kukhazikika, chitetezo, kuchuluka kwa mankhwala otulutsidwa, momwe amagwirira ntchito, mphamvu yachipatala, komanso kupanga mitundu yatsopano ya mlingo ndi njira zatsopano zoperekera mankhwala. Kutuluka kwa zinthu zothandizira mankhwala atsopano nthawi zambiri kumalimbikitsa kusintha kwa ubwino wa kukonzekera ndi kupanga mitundu yatsopano ya mlingo. Hydroxypropyl methylcellulose (HPMC) ndi imodzi mwa zinthu zothandizira mankhwala zodziwika bwino kunyumba ndi kunja. Chifukwa cha kulemera kwake kosiyana kwa mamolekyulu ndi kukhuthala, ili ndi ntchito zophatikiza, kumangirira, kukhuthala, kukhuthala, kuyimitsa, ndi kumata. Zinthu ndi ntchito monga kuphatikizika ndi kupanga filimu zimagwiritsidwa ntchito kwambiri muukadaulo wamankhwala. Nkhaniyi ikuwunikanso makamaka kugwiritsa ntchito hydroxypropyl methylcellulose (HPMC) m'njira zopangira m'zaka zaposachedwa.
1.Makhalidwe oyambira a HPMC
Hydroxypropyl methyl cellulose (HPMC), fomula ya molekyulu ndi C8H15O8-(C10 H18O6) n-C8H15O8, ndipo kulemera kwa molekyulu ndi pafupifupi 86 000. Chogulitsachi ndi chinthu chopangidwa mwapadera, chomwe ndi gawo la methyl ndi gawo la polyhydroxypropyl ether ya cellulose. Chingapangidwe m'njira ziwiri: Choyamba ndi chakuti methyl cellulose ya mtundu woyenera imachiritsidwa ndi NaOH kenako imayanjanitsidwa ndi propylene oxide pansi pa kutentha kwakukulu ndi kupanikizika kwakukulu. Nthawi yochitira izi iyenera kukhala yayitali mokwanira kuti methyl ndi hydroxypropyl zipange ma ether bonds. Imalumikizidwa ku mphete ya anhydroglucose ya cellulose mu mawonekedwe a cellulose, ndipo imatha kufika pamlingo womwe mukufuna; china ndi kuchiza thonje kapena ulusi wa pulp wamatabwa ndi caustic soda, kenako nkuchita ndi chlorinated methane ndi propylene oxide motsatizana, kenako n’kuiyeretsanso. , kuphwanyidwa kukhala ufa wabwino komanso wofanana kapena granules.
Mtundu wa mankhwalawa ndi woyera mpaka woyera ngati mkaka, wopanda fungo komanso wopanda kukoma, ndipo mawonekedwe ake ndi ufa wosalala kapena wosalala. Mankhwalawa amatha kusungunuka m'madzi kuti apange yankho loyera la colloidal loyera mpaka mkaka wokhala ndi kukhuthala kwina. Chochitika cha interconversion cha sol-gel chingachitike chifukwa cha kusintha kwa kutentha kwa yankho ndi kuchuluka kwina.
Chifukwa cha kusiyana kwa zomwe zili m'malo awiriwa m'mapangidwe a methoxy ndi hydroxypropyl, mitundu yosiyanasiyana ya zinthu yawonekera. Pazinthu zinazake, mitundu yosiyanasiyana ya zinthu ili ndi makhalidwe akeake. Chifukwa chake, kukhuthala ndi kutentha kwa gelation zimakhala ndi makhalidwe osiyanasiyana ndipo zingagwiritsidwe ntchito pazinthu zosiyanasiyana. Pharmacopoeia ya mayiko osiyanasiyana ili ndi malamulo ndi ziwonetsero zosiyanasiyana pa chitsanzo: European Pharmacopoeia imachokera ku mitundu yosiyanasiyana ya kukhuthala kosiyanasiyana ndi madigiri osiyanasiyana osinthira zinthu zomwe zimagulitsidwa pamsika, zomwe zimafotokozedwa ndi magiredi kuphatikiza manambala, ndipo unit ndi "mPa s". Mu US Pharmacopoeia, manambala 4 amawonjezedwa pambuyo pa dzina lodziwika bwino kuti asonyeze zomwe zili ndi mtundu wa chosinthira chilichonse cha hydroxypropyl methylcellulose, monga hydroxypropyl methylcellulose 2208. Manambala awiri oyamba akuyimira mtengo woyerekeza wa gulu la methoxy. Peresenti, manambala awiri omaliza akuyimira peresenti yoyerekeza ya hydroxypropyl.
Hydroxypropyl methylcellulose ya Calocan ili ndi mitundu itatu, yomwe ndi mndandanda wa E, mndandanda wa F ndi mndandanda wa K, mndandanda uliwonse uli ndi mitundu yosiyanasiyana yosankha. Mitundu ya E imagwiritsidwa ntchito kwambiri ngati zokutira filimu, zomwe zimagwiritsidwa ntchito popanga zokutira mapiritsi, zotsekeka; Mitundu ya E, F imagwiritsidwa ntchito ngati zoteteza komanso zoletsa kutulutsa zinthu zokonzekera maso, zoyimitsa, zothina zopangira madzi, mapiritsi ndi zomangira za granules; Mitundu ya K imagwiritsidwa ntchito kwambiri ngati zoletsa kutulutsa zinthu ndi zinthu za hydrophilic gel matrix zopangira kutulutsa zinthu pang'onopang'ono komanso kolamulidwa.
Opanga zinthu zapakhomo makamaka ndi Fuzhou 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 chemical plants, ndi zina zotero.
2.Ubwino wa HPMC
HPMC yakhala imodzi mwa mankhwala ogwiritsidwa ntchito kwambiri m'nyumba ndi kunja, chifukwa HPMC ili ndi ubwino womwe mankhwala ena owonjezera alibe.
2.1 Kusungunuka kwa madzi ozizira
Amasungunuka m'madzi ozizira osakwana 40 ℃ kapena 70% ethanol, osasungunuka m'madzi otentha opitilira 60 ℃, koma amatha kusungunuka ndi gel.
2.2 Kupanda mankhwala
HPMC ndi mtundu wa ether ya cellulose yosakhala ionic, yankho lake lilibe mphamvu ya ionic ndipo siligwirizana ndi mchere wachitsulo kapena mankhwala a ionic organic, kotero zinthu zina zothandizira sizimachita nayo panthawi yopanga mankhwala.
2.3 Kukhazikika
Ndi yokhazikika bwino pa asidi ndi alkali, ndipo imatha kusungidwa kwa nthawi yayitali pakati pa pH 3 ndi 11 popanda kusintha kwakukulu kwa kukhuthala. Yankho lamadzi la HPMC limakhala ndi mphamvu yotsutsana ndi chimfine ndipo limasunga kukhuthala kwabwino pakusungidwa kwa nthawi yayitali. Zinthu zothandizira mankhwala zomwe zimagwiritsidwa ntchito pogwiritsa ntchito HPMC zimakhala ndi kukhazikika kwabwino kuposa zomwe zimagwiritsa ntchito zinthu zothandizira zachikhalidwe (monga dextrin, starch, ndi zina zotero).
2.4 Kusintha kwa kukhuthala
Zochokera ku kukhuthala kosiyanasiyana za HPMC zimatha kusakanikirana mosiyanasiyana, ndipo kukhuthala kwake kumatha kusinthidwa malinga ndi lamulo linalake, ndipo kumakhala ndi ubale wabwino wa mzere, kotero chiŵerengerocho chingasankhidwe malinga ndi zosowa.
2.5 Kulephera kwa kagayidwe kachakudya
HPMC siimayamwa kapena kusinthidwa kukhala kagayidwe m'thupi, ndipo sipereka kutentha, kotero ndi chinthu chotetezeka chopangira mankhwala. 2.6 Chitetezo Kawirikawiri amaganiziridwa kuti HPMC ndi chinthu chopanda poizoni komanso chosakwiyitsa, mlingo wapakati wakupha wa mbewa ndi 5 g·kg – 1, ndipo mlingo wapakati wakupha wa makoswe ndi 5. 2 g · kg – 1. Mlingo wa tsiku ndi tsiku ndi woopsa kwa thupi la munthu.
3.Kugwiritsa ntchito HPMC mu njira zopangira
3.1 Monga zinthu zopangira filimu ndi zinthu zopangira filimu
Pogwiritsa ntchito HPMC ngati piritsi lophimbidwa ndi filimu, piritsi lophimbidwalo silili ndi ubwino woonekeratu pakubisa kukoma ndi mawonekedwe poyerekeza ndi mapiritsi ophimbidwa ndi shuga, koma kuuma kwake, kusinthasintha, kuyamwa kwa chinyezi, kuchuluka kwa kusweka, kulemera kwa utoto ndi zizindikiro zina zabwino ndizabwino. Mlingo wotsika wa mankhwalawa umagwiritsidwa ntchito ngati chophimba cha filimu chosungunuka m'madzi cha mapiritsi ndi mapiritsi, ndipo mtundu wapamwamba wa kukhuthala umagwiritsidwa ntchito ngati chophimba cha filimu cha machitidwe osungunula achilengedwe, nthawi zambiri pamlingo wa 2% mpaka 20%.
Zhang Jixing ndi ena adagwiritsa ntchito njira yopangira pamwamba kuti akonze bwino kapangidwe ka premix ndi HPMC ngati chophimba cha filimu. Pogwiritsa ntchito zinthu zopangira filimu HPMC, kuchuluka kwa polyvinyl alcohol ndi plasticizer polyethylene glycol ngati zinthu zofufuzira, mphamvu yokoka ndi kutseguka kwa filimuyo ndi kukhuthala kwa yankho lophimba filimuyo ndiye chizindikiro chowunikira, ndipo ubale pakati pa index yowunikira ndi zinthu zowunikira umafotokozedwa ndi chitsanzo cha masamu, ndipo njira yabwino kwambiri yopangira imapezedwa. Kugwiritsa ntchito kwake ndi hydroxypropyl methylcellulose (HPMCE5) 11.88 g, polyvinyl alcohol 24.12 g, plasticizer polyethylene glycol 13.00 g, ndipo kukhuthala kwa kusungunuka kwa chophimba ndi 20 mPa·s, kukhuthala ndi kukhwima kwa filimuyo kunafika pamlingo wabwino kwambiri. Zhang Yuan adasintha njira yokonzekera, adagwiritsa ntchito HPMC ngati chomangira kuti alowe m'malo mwa slurry ya starch, ndipo adasintha mapiritsi a Jiahua kukhala mapiritsi okhala ndi filimu kuti akonze bwino kukonzekera kwake, akonze hygroscopicity yake, azitha kutha mosavuta, mapiritsi omasuka, osweka ndi mavuto ena, ndikuwonjezera kukhazikika kwa mapiritsi. Njira yabwino kwambiri yopangira idatsimikiziridwa ndi zoyeserera za orthogonal, zomwe zikutanthauza kuti kuchuluka kwa slurry kunali 2% HPMC mu 70% ethanol solution panthawi yopaka utoto, ndipo nthawi yosakaniza panthawi yopaka utoto inali mphindi 15. Zotsatira Mapiritsi okhala ndi filimu ya Jiahua okonzedwa ndi njira yatsopanoyi ndi mankhwala adasinthidwa kwambiri mawonekedwe, nthawi yosweka ndi kuuma kwapakati kuposa omwe adapangidwa ndi njira yoyambirira yopangira, ndipo kuchuluka koyenera kwa mapiritsi okhala ndi filimuyi kudakwera kwambiri. Adafika pa 95%. Liang Meiyi, Lu Xiaohui, ndi ena. adagwiritsanso ntchito hydroxypropyl methylcellulose ngati chinthu chopangira filimu kuti akonze piritsi loyika patinae colon ndi piritsi loyika pa matrine colon, motsatana. Izi zimakhudza kutulutsidwa kwa mankhwala. Huang Yunran adakonza Mapiritsi Oika Magazi a Dragon's Blood Colon, ndipo adayika HPMC pa yankho lophimba la chotupacho, ndipo gawo lake lalikulu linali 5%. Zikuoneka kuti HPMC ingagwiritsidwe ntchito kwambiri mu njira yoperekera mankhwala m'matumbo.
Hydroxypropyl methylcellulose si chinthu chabwino kwambiri chophikira filimu, komanso chingagwiritsidwe ntchito ngati chinthu chopangira filimu mu mapangidwe a filimu. Wang Tongshun etc. amakonzedwa kuti agwirizane ndi mankhwala a compound zinc licorice ndi aminolexanol oral composite film, ndi kusinthasintha, kufanana, kusalala, kuwonekera bwino kwa mankhwala a filimu ngati index yofufuzira, ndipo mankhwala abwino kwambiri ndi PVA 6.5 g, HPMC 0.1 g ndi 6.0 g ya propylene glycol ikukwaniritsa zofunikira za kutulutsidwa pang'onopang'ono komanso chitetezo, ndipo ingagwiritsidwe ntchito ngati mankhwala okonzekera filimu yophatikiza.
3.2 monga chomangira ndi chopatukana
Mlingo wotsika wa kukhuthala kwa mankhwalawa ungagwiritsidwe ntchito ngati chomangira ndi chosungunula mapiritsi, mapiritsi ndi tinthu tating'onoting'ono, ndipo kuchuluka kwa kukhuthala kwakukulu kungagwiritsidwe ntchito ngati chomangira. Mlingo umasiyana malinga ndi mitundu ndi zofunikira zosiyanasiyana. Kawirikawiri, mlingo wa chomangira mapiritsi ouma ndi 5%, ndipo mlingo wa chomangira mapiritsi onyowa ndi 2%.
Li Houtao ndi anzake adafufuza chomangira cha mapiritsi a tinidazole. 8% polyvinylpyrrolidone (PVP-K30), 40% madzi a syrup, 10% starch slurry, 2.0% hydroxypropyl methylcellulose K4 (HPMCK4M), 50% ethanol adafufuzidwa ngati kumatirira kwa mapiritsi a tinidazole motsatizana. Kusintha kwa mawonekedwe a mapiritsi osavuta komanso atapaka utoto kunayerekezeredwa, ndipo kufooka, kuuma, nthawi yotha kusweka ndi kuchuluka kwa kusungunuka kwa mapiritsi osiyanasiyana operekedwa ndi dokotala kunayesedwa. Zotsatira Mapiritsi okonzedwa ndi 2.0% hydroxypropyl methylcellulose anali owala, ndipo muyeso wa kufooka sunapeze vuto la kusweka kwa m'mphepete ndi m'makona, ndipo atapaka utoto, mawonekedwe a piritsi anali okwanira ndipo mawonekedwe ake anali abwino. Chifukwa chake, mapiritsi a tinidazole okonzedwa ndi 2.0% HPMC-K4 ndi 50% ethanol ngati zomangira adagwiritsidwa ntchito. Guan Shihai anaphunzira njira yopangira mapiritsi a Fuganning, anayang'ana zomatira, ndipo anayang'ana 50% ethanol, 15% starch phala, 10% PVP ndi 50% ethanol solutions ndi kukanikiza, kusalala, ndi kuphwanyika ngati zizindikiro zowunikira. , 5% CMC-Na ndi 15% HPMC solution (5 mPa s). Zotsatira Mapepala okonzedwa ndi 50% ethanol, 15% starch phala, 10% PVP 50% ethanol solution ndi 5% CMC-Na anali ndi malo osalala, koma osakanizika bwino komanso olimba pang'ono, omwe sangakwaniritse zosowa za kupaka; 15% HPMC solution (5 mPa·s), pamwamba pa piritsi ndi yosalala, kuphwanyika ndikoyenera, ndipo kuphwanyika ndi kwabwino, komwe kungakwaniritse zosowa za kupaka. Chifukwa chake, HPMC (5 mPa s) idasankhidwa kukhala guluu.
3.3 monga wothandizira woyimitsa
Mlingo wapamwamba wa mankhwalawa umagwiritsidwa ntchito ngati choyimitsa pokonzekera chokonzekera chamadzimadzi choyimitsa. Chili ndi mphamvu yabwino yoyimitsa, n'chosavuta kufalikira, sichimamatira pakhoma, ndipo chili ndi tinthu tating'onoting'ono tomwe timayamwa. Mlingo wamba ndi 0.5% mpaka 1.5%. Song Tian ndi anzake adagwiritsa ntchito zinthu zomwe zimagwiritsidwa ntchito kwambiri monga polymer (hydroxypropyl methylcellulose, sodium carboxymethylcellulose, povidone, xanthan gum, methylcellulose, ndi zina zotero) ngati zoyimitsa pokonzekera racecadotril. Kudzera mu sedimentation voliyumu ratio ya zoyimitsa zosiyanasiyana, redispersibility index, ndi rheology, suspension viscosity ndi microscopic morphology zinawonedwa, ndipo kukhazikika kwa tinthu ta mankhwala pansi pa kuyesa kofulumira kunafufuzidwanso. Zotsatira Kuyimitsa kouma kokonzedwa ndi 2% HPMC ngati choyimitsa kunali ndi njira yosavuta komanso kukhazikika bwino.
Poyerekeza ndi methyl cellulose, hydroxypropyl methyl cellulose ili ndi makhalidwe opangitsa kuti ikhale yomveka bwino, ndipo pali zinthu zochepa kwambiri zomwe sizimafalikira, kotero HPMC imagwiritsidwanso ntchito ngati choyimitsa pokonzekera maso. Liu Jie ndi anzake adagwiritsa ntchito HPMC, hydroxypropyl cellulose (HPC), carbomer 940, polyethylene glycol (PEG), sodium hyaluronate (HA) ndi kuphatikiza kwa HA/HPMC ngati zoyimitsa kuti akonze zinthu zosiyanasiyana. Pa Ciclovir ophthalmic suspension, sedimentation volume ratio, particle size ndi redispersibility zimasankhidwa ngati zizindikiro zowunikira kuti ziwonetse choyimitsa chabwino kwambiri. Zotsatira zake zikusonyeza kuti acyclovir ophthalmic suspension yokonzedwa ndi 0.05% HA ndi 0.05% HPMC ngati choyimitsa, sedimentation volume ratio ndi 0.998, kukula kwa tinthu ndi kofanana, redispersibility ndi yabwino, ndipo kukonzekerako ndi kokhazikika. Kuwonjezeka kwa kugonana.
3.4 Monga choletsa, chotulutsa pang'onopang'ono komanso chowongolera komanso chopanga ma pore
Mlingo wapamwamba wa mankhwalawa umagwiritsidwa ntchito pokonzekera mapiritsi osungunuka a gel matrix, zoletsa ndi zotulutsa zolamulidwa za mapiritsi osakanikirana a matrix, ndipo zimakhala ndi mphamvu yochedwetsa kutulutsidwa kwa mankhwala. Kuchuluka kwake ndi 10% mpaka 80%. Magawo otsika a kukhuthala amagwiritsidwa ntchito ngati ma porogens okonzekera kutulutsidwa kosatha kapena kolamulidwa. Mlingo woyamba wofunikira pakuthandizira kwa mapiritsi otere ukhoza kufikika mwachangu, kenako kutulutsidwa kosatha kapena kolamulidwa kumachitika, ndipo kuchuluka kwa mankhwala m'magazi kumasungidwa m'thupi. Hydroxypropyl methylcellulose imanyowa kuti ipange gawo la gel ikakumana ndi madzi. Njira yotulutsira mankhwala kuchokera pa piritsi la matrix imaphatikizapo kufalikira kwa gawo la gel ndi kuwonongeka kwa gawo la gel. Jung Bo Shim ndi ena adakonza mapiritsi a carvedilol okhazikika ndi HPMC ngati zinthu zotulutsira kosatha.
Hydroxypropyl methylcellulose imagwiritsidwanso ntchito kwambiri m'mapiritsi a matrix otulutsidwa nthawi zonse a mankhwala achikhalidwe aku China, ndipo zosakaniza zambiri zogwira ntchito, zigawo zogwira ntchito komanso zokonzekera kamodzi za mankhwala achikhalidwe aku China zimagwiritsidwa ntchito. Liu Wen ndi anzake adagwiritsa ntchito 15% hydroxypropyl methylcellulose ngati zinthu za matrix, 1% lactose ndi 5% microcrystalline cellulose ngati zodzaza, ndipo adakonza Jingfang Taohe Chengqi Decoction mu mapiritsi otulutsidwa nthawi zonse a matrix. Chitsanzocho ndi Higuchi equation. Dongosolo la kapangidwe ka formula ndi losavuta, kukonzekera ndikosavuta, ndipo deta yotulutsidwa ndi yokhazikika, yomwe ikukwaniritsa zofunikira za Chinese Pharmacopoeia. Tang Guanguang ndi anzake adagwiritsa ntchito ma saponins onse a Astragalus ngati mankhwala achitsanzo, adakonza mapiritsi a matrix a HPMC, ndipo adafufuza zinthu zomwe zimakhudza kutulutsidwa kwa mankhwala kuchokera kuzinthu zogwira ntchito za mankhwala achikhalidwe aku China m'mapiritsi a matrix a HPMC. Zotsatira Pamene mlingo wa HPMC ukuwonjezeka, kutulutsidwa kwa astragaloside kunachepa, ndipo kuchuluka kwa kutulutsidwa kwa mankhwalawa kunali ndi ubale wofanana ndi kuchuluka kwa kusungunuka kwa matrix. Mu piritsi la hypromellose HPMC matrix, pali ubale wina pakati pa kutulutsidwa kwa gawo logwira ntchito la mankhwala achikhalidwe aku China ndi mlingo ndi mtundu wa HPMC, ndipo njira yotulutsira hydrophilic chemical monomer ndi yofanana nayo. Hydroxypropyl methylcellulose si yoyenera kokha pazinthu za hydrophilic, komanso zinthu zomwe sizimalowa m'madzi. Liu Guihua adagwiritsa ntchito 17% hydroxypropyl methylcellulose (HPMCK15M) ngati zinthu zotulutsira sustained-release matrix, ndipo adakonza mapiritsi a Tianshan Xuelian suinged-release matrix pogwiritsa ntchito njira yonyowa ya granulation ndi tableting. Zotsatira zake zotulutsira sustained zinali zodziwikiratu, ndipo njira yokonzekera inali yokhazikika komanso yotheka.
Hydroxypropyl methylcellulose siigwiritsidwa ntchito kokha pa mapiritsi a matrix otulutsidwa nthawi zonse a zosakaniza zogwira ntchito komanso magawo ogwira ntchito a mankhwala achikhalidwe aku China, komanso imagwiritsidwa ntchito kwambiri popanga mankhwala achikhalidwe aku China. Wu Huichao ndi ena adagwiritsa ntchito 20% hydroxypropyl methyl cellulose (HPMCK4M) ngati zinthu za matrix, ndipo adagwiritsa ntchito njira yopondereza ufa mwachindunji kukonzekera piritsi la Yizhi hydrophilic gel matrix lomwe lingathe kutulutsa mankhwalawa mosalekeza komanso mokhazikika kwa maola 12. Saponin Rg1, ginsenoside Rb1 ndi Panax notoginseng saponin R1 zidagwiritsidwa ntchito ngati zizindikiro zowunikira kuti zifufuze kutulutsidwa mu vitro, ndipo equation yotulutsidwa kwa mankhwala idayikidwa kuti iphunzire njira yotulutsira mankhwala. Zotsatira Njira yotulutsira mankhwala idagwirizana ndi zero-order kinetic equation ndi Ritger-Peppas equation, momwe geniposide idatulutsidwa ndi non-Fick diffusion, ndipo zigawo zitatu mu Panax notoginseng zidatulutsidwa ndi kukokoloka kwa mafupa.
3.5 Guluu woteteza ngati chokhuthala ndi chokolera
Pamene mankhwalawa agwiritsidwa ntchito ngati chokhuthala, kuchuluka kwa nthawi zonse kumakhala pakati pa 0.45% mpaka 1.0%. Kungathenso kulimbitsa guluu wosagwirizana ndi madzi, kupanga colloid yoteteza, kuletsa tinthu tating'onoting'ono kuti tisagwirizane ndi kusonkhana, motero kuletsa mapangidwe a zinyalala. Kuchuluka kwake kofala ndi pakati pa 0.5% mpaka 1.5%.
Wang Zhen ndi anzake adagwiritsa ntchito njira yoyesera ya L9 orthogonal kuti afufuze njira yokonzekera enema ya carbon activated medical. Njira yabwino kwambiri yodziwira kuti enema ya carbon activated medical ndi kugwiritsa ntchito 0.5% sodium carboxymethyl cellulose ndi 2.0% hydroxypropyl methylcellulose (HPMC ili ndi gulu la methoxyl la 23.0%, hydroxypropoxyl Base 11.6%) ngati chokhuthala, njira yogwirira ntchito imathandizira kukhazikika kwa carbon activated medical. Zhang Zhiqiang ndi anzake adapanga gel yokonzeka kugwiritsidwa ntchito ya levofloxacin hydrochloride ophthalmic yokhala ndi pH yokhala ndi mphamvu yotulutsa mpweya, pogwiritsa ntchito carbopol ngati matrix ya gel ndi hydroxypropyl methylcellulose ngati chokhuthala. Mankhwala abwino kwambiri poyesa, pamapeto pake amapeza mankhwala abwino kwambiri ndi levofloxacin hydrochloride 0.1 g, carbopol (9400) 3 g, hydroxypropyl methylcellulose (E50 LV) 20 g, disodium hydrogen phosphate 0.35 g, phosphoric acid 0.45 g ya sodium dihydrogen, 0.50 g ya sodium chloride, 0.03 g ya ethyl paraben, ndi madzi zinawonjezedwa kuti apange 100 mL. Mu mayesowa, wolembayo adafufuza mndandanda wa hydroxypropyl methylcellulose METHOCEL wa Colorcon Company wokhala ndi mafotokozedwe osiyanasiyana (K4M, E4M, E15 LV, E50LV) kuti akonze zokhuthala zokhala ndi kuchuluka kosiyanasiyana, ndipo zotsatira zake zidasankha HPMC E50 LV ngati chokhuthala. Chokhuthala cha ma gels a levofloxacin hydrochloride instant sensitive pH.
3.6 ngati zinthu za kapisozi
Kawirikawiri, chipolopolo cha kapisozi cha makapisozi chimakhala ndi gelatin. Njira yopangira chipolopolo cha kapisozi ndi yosavuta, koma pali mavuto ndi zochitika zina monga chitetezo chochepa ku chinyezi ndi mankhwala omwe amakhudzidwa ndi mpweya, kuchepa kwa kusungunuka kwa mankhwala, komanso kusweka kwa chipolopolo cha kapisozi panthawi yosungira. Chifukwa chake, hydroxypropyl methylcellulose imagwiritsidwa ntchito m'malo mwa makapisozi a gelatin pokonzekera makapisozi, zomwe zimapangitsa kuti kapangidwe ka makapisozi kakhale koyenera komanso momwe amagwiritsidwira ntchito, ndipo yakhala ikulengezedwa kwambiri kunyumba ndi kunja.
Pogwiritsa ntchito theophylline ngati mankhwala owongolera, Podczeck ndi anzake adapeza kuti kuchuluka kwa kusungunuka kwa makapisozi okhala ndi zipolopolo za hydroxypropyl methylcellulose kunali kwakukulu kuposa kwa makapisozi a gelatin. Chifukwa cha kusanthulaku ndikuti kusungunuka kwa HPMC ndiko kusungunuka kwa kapisozi yonse nthawi imodzi, pomwe kusungunuka kwa kapisozi ya gelatin ndiko kusungunuka kwa kapangidwe ka netiweki poyamba, kenako kusungunuka kwa kapisozi yonse, kotero kapisozi ya HPMC ndiyoyenera kwambiri zipolopolo za Capsule kuti zitulutsidwe mwachangu. Chiwele ndi anzake adapezanso mfundo zofanana ndipo adayerekeza kusungunuka kwa gelatin, gelatin/polyethylene glycol ndi zipolopolo za HPMC. Zotsatira zake zidawonetsa kuti zipolopolo za HPMC zidasungunuka mwachangu pansi pa mikhalidwe yosiyanasiyana ya pH, pomwe makapisozi a gelatin Amakhudzidwa kwambiri ndi mikhalidwe yosiyanasiyana ya pH. Tang Yue ndi anzake adafufuza mtundu watsopano wa chipolopolo cha kapisozi cha dongosolo lonyamula mankhwala lopanda ufa wouma. Poyerekeza ndi chipolopolo cha kapisozi cha hydroxypropyl methylcellulose ndi chipolopolo cha kapisozi cha gelatin, kukhazikika kwa chipolopolo cha kapisozi ndi mawonekedwe a ufa womwe uli mu chipolopolocho m'mikhalidwe yosiyanasiyana kunafufuzidwa, ndipo mayeso a kufooka kwa chipolopolocho adachitika. Zotsatira zake zikusonyeza kuti poyerekeza ndi makapisozi a gelatin, zipolopolo za kapisozi za HPMC zimakhala bwino pakukhazikika komanso kuteteza ufa, zimakhala ndi kukana chinyezi kwambiri, komanso zimakhala ndi kufooka kochepa kuposa zipolopolo za kapisozi za gelatin, kotero zipolopolo za kapisozi za HPMC ndizoyenera kwambiri Makapisozi kuti apume ufa wouma.
3.7 ngati chomatira cha bioglue
Ukadaulo wa bioadhesion umagwiritsa ntchito zinthu zowonjezerera zinthu zokhala ndi ma polima omatira. Mwa kumamatira ku mucosa wachilengedwe, kumawonjezera kusagwirizana ndi kulimba kwa kukhudzana pakati pa mankhwala ndi mucosa, kotero kuti mankhwalawa amatulutsidwa pang'onopang'ono ndikulowetsedwa ndi mucosa kuti akwaniritse cholinga cha chithandizo. Amagwiritsidwa ntchito kwambiri pakadali pano. Kuchiza matenda am'mimba, nyini, mucosa wamlomo ndi ziwalo zina.
Ukadaulo wa bioadhesion m'mimba ndi njira yatsopano yoperekera mankhwala yomwe yapangidwa m'zaka zaposachedwa. Sikuti imangowonjezera nthawi yokhalamo kwa mankhwala m'mimba, komanso imapangitsa kuti kulumikizana pakati pa mankhwalawa ndi nembanemba ya selo pamalo omwe amayamwa, imasintha kusinthasintha kwa nembanemba ya selo, ndikupangitsa kuti kulowa kwa mankhwalawa m'maselo ang'onoang'ono a m'matumbo kukhale kowonjezereka, motero kumawonjezera bioavailability ya mankhwalawa. Wei Keda et al. adafufuza mankhwala a piritsi ndi mlingo wa HPMCK4M ndi Carbomer 940 ngati zinthu zofufuzira, ndipo adagwiritsa ntchito chipangizo chodzipangira bioadhesion kuti ayesere mphamvu yochotsa pakati pa piritsi ndi biofilm yoyerekezeredwa ndi mtundu wa madzi omwe ali mu thumba la pulasitiki. , ndipo potsiriza ndinasankha kuchuluka kwa HPMCK40 ndi carbomer 940 kukhala 15 ndi 27.5 mg m'dera labwino kwambiri la mapiritsi a NCaEBT, motsatana, kuti ndikonzekere mapiritsi a NCaEBT, zomwe zikusonyeza kuti zinthu zomatira (monga hydroxypropyl methylcellulose) zitha kuchepetsa kwambiri kumatirira kwa mankhwalawo ku minofu.
Mankhwala omatira pakamwa ndi mtundu watsopano wa njira yoperekera mankhwala yomwe yaphunziridwa kwambiri m'zaka zaposachedwa. Mankhwala omatira pakamwa amatha kumamatira mankhwalawa ku gawo lokhudzidwa la mkamwa, zomwe sizimangowonjezera nthawi yokhala kwa mankhwalawa mkamwa, komanso zimateteza mucosa wa mkamwa. Zotsatira zabwino zochiritsira komanso kupezeka kwa mankhwala bwino. Xue Xiaoyan et al. adakonza mapangidwe a mapiritsi omatira pakamwa a insulin, pogwiritsa ntchito apulo pectin, chitosan, carbomer 934P, hydroxypropyl methylcellulose (HPMC K392) ndi sodium alginate ngati zinthu zomatira pakamwa, komanso kuzizira kuti akonze insulin ya mkamwa. Pepala lomatira la magawo awiri. Piritsi lomatira pakamwa la insulin lokonzedwa lili ndi kapangidwe kofanana ndi siponji, komwe ndi kothandiza kutulutsa insulin, ndipo lili ndi gawo loteteza hydrophobic, lomwe lingatsimikizire kuti mankhwalawa amatulutsidwa mbali imodzi ndikupewa kutayika kwa mankhwalawa. Hao Jifu et al. adapanganso mapeyala abuluu-chikasu a mkamwa pogwiritsa ntchito guluu wa Baiji, HPMC ndi carbomer ngati zinthu zomatira pakamwa.
Mu njira zoperekera mankhwala kumaliseche, ukadaulo wa bioadhesion wagwiritsidwanso ntchito kwambiri. Zhu Yuting ndi anzake adagwiritsa ntchito carbomer (CP) ndi HPMC ngati zinthu zomatira komanso matrix yotulutsidwa mosalekeza kuti akonze mapiritsi a clotrimazole bioadhesive vagina okhala ndi mitundu yosiyanasiyana ndi ma ratios, ndipo anayeza kumatira kwawo, nthawi yomatira komanso kuchuluka kwa kutupa m'malo opangidwa ndi madzi a m'maliseche. , mankhwala oyenera adawonetsedwa ngati CP-HPMC1: 1, pepala lomatira lokonzedwa linali ndi magwiridwe antchito abwino omatira, ndipo njirayo inali yosavuta komanso yotheka.
3.8 ngati gel yopaka pamwamba
Monga chokonzekera chomatira, gel ili ndi zabwino zambiri monga chitetezo, kukongola, kuyeretsa kosavuta, mtengo wotsika, njira yosavuta yokonzekera, komanso kugwirizana bwino ndi mankhwala. Njira yopangira. Mwachitsanzo, gel yodutsa pakhungu ndi mtundu watsopano wa mlingo womwe waphunziridwa kwambiri m'zaka zaposachedwa. Sikuti imangopewa kuwonongeka kwa mankhwala m'mimba ndikuchepetsa kusinthasintha kwa kuchuluka kwa mankhwala m'magazi, komanso yakhala imodzi mwa njira zothandiza zotulutsira mankhwala kuti zithetse zotsatirapo zoyipa za mankhwala.
Zhu Jingjie ndi anzake adaphunzira za momwe ma matrices osiyanasiyana amakhudzira kutulutsa kwa scutellarin alcohol plastid gel mu vitro, ndipo adawunikidwa ndi carbomer (980NF) ndi hydroxypropyl methylcellulose (HPMCK15M) ngati ma matrices a gel, ndipo adapeza scutellarin yoyenera scutellarin. Gel matrix ya ma plastid a mowa. Zotsatira za kafukufuku zikuwonetsa kuti 1.0% carbomer, 1.5% carbomer, 1.0% carbomer + 1.0% HPMC, 1.5% carbomer + 1.0% HPMC ngati matrix a gel. Zonsezi ndi zoyenera ma plastid a mowa a scutellarin. Pa nthawi yoyesera, zidapezeka kuti HPMC ikhoza kusintha njira yotulutsira mankhwala ya carbomer gel matrix poyika kinetic equation ya kutulutsa mankhwala, ndipo 1.0% HPMC ikhoza kusintha 1.0% carbomer matrix ndi 1.5% carbomer matrix. Chifukwa chake chingakhale chakuti HPMC imakula mofulumira, ndipo kukula mofulumira kumayambiriro kwa kuyeseraku kumapangitsa kuti kusiyana kwa mamolekyu a zinthu za carbomer gel kukhale kwakukulu, motero kufulumizitsa kuchuluka kwa kutulutsa mankhwala. Zhao Wencui ndi anzake adagwiritsa ntchito carbomer-934 ndi hydroxypropyl methylcellulose ngati zonyamulira kuti akonze norfloxacin ophthalmic gel. Njira yokonzekerayi ndi yosavuta komanso yotheka, ndipo khalidwe lake likugwirizana ndi gel ya maso ya "Chinese Pharmacopoeia" (2010 edition) Zofunikira pa khalidwe.
3.9 Choletsa mvula cha dongosolo lodzipangira lokha
Dongosolo lodzipangira mankhwala lodzipangira lokha (SMEDDS) ndi mtundu watsopano wa njira yoperekera mankhwala opangidwa ndi munthu, womwe ndi wosakaniza wofanana, wokhazikika komanso wowonekera bwino wopangidwa ndi mankhwala, gawo la mafuta, emulsifier ndi co-emulsifier. Kapangidwe ka mankhwala ndi kosavuta, ndipo chitetezo ndi kukhazikika ndi zabwino. Pa mankhwala osasungunuka bwino, zinthu za polymer zosungunuka m'madzi, monga HPMC, polyvinylpyrrolidone (PVP), ndi zina zotero, nthawi zambiri zimawonjezedwa kuti mankhwala omasuka ndi mankhwala omwe ali mu microemulsion azitha kusungunuka kwambiri m'mimba, kuti awonjezere kusungunuka kwa mankhwala ndikuwonjezera kupezeka kwa bioavailability.
Peng Xuan ndi ena adapanga njira yodzipangira mankhwala yodzipangira yokha (S-SEDDS). Oxyethylene hydrogenated castor oil (Cremophor RH40), 12% caprylic capric acid polyethylene glycol glyceride (Labrasol) ngati co-emulsifier, ndi 50 mg·g-1 HPMC. Kuwonjezera HPMC ku SSEDDS kungapangitse silibinin yaulere kusungunuka mu S-SEDDS ndikuletsa silibinin kutuluka. Poyerekeza ndi njira zachikhalidwe zodzipangira zokha, kuchuluka kwa surfactant nthawi zambiri kumawonjezedwa kuti kupewe kusungunuka kwa mankhwala osakwanira. Kuwonjezera kwa HPMC kumatha kusunga kusungunuka kwa silibinin mu dissolving medium kukhala kofanana, kuchepetsa emulsification mu njira zodzipangira zokha. Mlingo wa mankhwalawa.
4. Mapeto
Zikuoneka kuti HPMC yagwiritsidwa ntchito kwambiri pokonzekera chifukwa cha mphamvu zake zakuthupi, zamankhwala komanso zamoyo, koma HPMC ilinso ndi zofooka zambiri pakukonzekera, monga momwe zimakhalira ndi kusintha kwa methyl methacrylate isanatuluke komanso itatha. Nthawi yomweyo, ofufuza ena adafufuza momwe chiphunzitso cha osmotic chimagwiritsidwira ntchito mu HPMC pokonzekera mapiritsi a carbamazepine otulutsidwa nthawi zonse ndi mapiritsi a verapamil hydrochloride otulutsidwa nthawi zonse kuti aphunzire momwe amatulutsira. Mwachidule, ofufuza ambiri akuchita ntchito yambiri kuti agwiritse ntchito bwino HPMC pokonzekera, ndipo ndi kuphunzira mozama za makhalidwe ake ndi kusintha kwa ukadaulo wokonzekera, HPMC idzagwiritsidwa ntchito kwambiri m'njira zatsopano zoyesera ndi mitundu yatsopano ya mankhwala. Mu kafukufuku wa mankhwala, kenako ndikulimbikitsa chitukuko chopitilira cha mankhwala.
Nthawi yotumizira: Okutobala-08-2022