Zolemba zokhudzana ndi kunyumba ndi kunja pokonzekera mankhwala opangira mankhwala a hydroxypropyl methylcellulose (HPMC) m'zaka zaposachedwa adawunikiridwa, kufufuzidwa ndi kufotokozedwa mwachidule, ndikugwiritsa ntchito pokonzekera zolimba, kukonzekera kwamadzimadzi, kukonzekera kosalekeza ndi kuwongolera kumasulidwa, kukonzekera kapisozi, gelatin The latest ntchito m'munda wa formulations latsopano monga zomatira formulations ndi bioadhesives. Chifukwa cha kusiyana wachibale maselo kulemera ndi mamasukidwe akayendedwe a HPMC, ali makhalidwe ndi ntchito emulsification, adhesion, thickening, mamasukidwe akayendedwe kuwonjezeka, kuyimitsa, gelling ndi filimu kupanga. Amagwiritsidwa ntchito kwambiri pokonzekera mankhwala ndipo adzakhala ndi gawo lalikulu pakukonzekera. Ndi kafukufuku wozama wa katundu wake ndi kupititsa patsogolo luso la kupanga, HPMC idzagwiritsidwa ntchito kwambiri pofufuza mitundu yatsopano ya mlingo ndi njira zatsopano zoperekera mankhwala, potero kulimbikitsa chitukuko chosalekeza cha mankhwala.
hydroxypropyl methylcellulose; kukonzekera mankhwala; excipients mankhwala.
Othandizira mankhwala sizinthu zokhazokha zopangira mankhwala opangira mankhwala, komanso zokhudzana ndi zovuta za kukonzekera, khalidwe la mankhwala, kukhazikika, chitetezo, mlingo wa kumasulidwa kwa mankhwala, machitidwe, mphamvu zachipatala, ndi chitukuko cha zatsopano. mafomu a mlingo ndi njira zatsopano zoyendetsera. zogwirizana kwambiri. Kutuluka kwa mankhwala atsopano opangira mankhwala nthawi zambiri kumalimbikitsa kuwongolera kwa kukonzekera bwino komanso kupanga mitundu yatsopano ya mlingo. Hydroxypropyl methylcellulose (HPMC) ndi imodzi mwazinthu zodziwika bwino za mankhwala kunyumba ndi kunja. Chifukwa cha kulemera kwake kwa maselo ndi kukhuthala kwake, ili ndi ntchito za emulsifying, kumanga, thickening, thickening, suspending, ndi glueing. Mawonekedwe ndi ntchito monga coagulation ndi kupanga mafilimu amagwiritsidwa ntchito kwambiri muukadaulo wamankhwala. Nkhaniyi imayang'ana kwambiri kagwiritsidwe ntchito ka hydroxypropyl methylcellulose (HPMC) m'mapangidwe azaka zaposachedwa.
1.Zinthu zoyambira za HPMC
Hydroxypropyl methyl cellulose (HPMC), mawonekedwe a molekyulu ndi C8H15O8-(C10 H18O6) n- C8H15O8, ndipo kuchuluka kwa maselo ndi pafupifupi 86 000. Izi ndi semi-synthetic zakuthupi, zomwe ndi gawo la methyl ndi gawo la polyhydroxypropyl ether wa cellulose. Ikhoza kupangidwa m'njira ziwiri: Imodzi ndi yakuti methyl cellulose ya giredi yoyenera imathandizidwa ndi NaOH kenako imachita ndi propylene oxide pansi pa kutentha kwambiri komanso kuthamanga kwambiri. Nthawi yochitapo iyenera kukhala nthawi yayitali kuti methyl ndi hydroxypropyl ipange zomangira za ether Imalumikizidwa ndi mphete ya anhydroglucose ya cellulose mu mawonekedwe a cellulose, ndipo imatha kufikira digiri yomwe mukufuna; china ndi kuchitira thonje linter kapena nkhuni zamkati ulusi ndi caustic soda, ndiyeno kuchita ndi chlorinated methane ndi propylene okusayidi motsatizana, ndiyeno kuonjezera kuyeretsa. , wophwanyidwa mu ufa wabwino ndi yunifolomu kapena granules.
Mtundu wa mankhwalawa ndi woyera mpaka woyera wamkaka, wopanda fungo komanso wosakoma, ndipo mawonekedwe ake ndi granular kapena fibrous ufa wosavuta kuyenda. Izi zitha kusungunuka m'madzi kuti zikhale zomveka bwino mpaka zamkaka zoyera za colloidal ndi kukhuthala kwina. The sol-gel osakaniza interconversion chodabwitsa akhoza kuchitika chifukwa cha kutentha kusintha kwa yankho ndi ndende inayake.
Chifukwa cha kusiyana kwa zomwe zili m'malo awiriwa mumapangidwe a methoxy ndi hydroxypropyl, mitundu yosiyanasiyana ya mankhwala yawonekera. M'malo ena, mitundu yosiyanasiyana yazinthu imakhala ndi mawonekedwe ake. Viscosity ndi kutentha kwa gelation kutentha, kotero zimakhala ndi katundu wosiyana ndipo zingagwiritsidwe ntchito pazifukwa zosiyanasiyana. Pharmacopoeia ya mayiko osiyanasiyana ili ndi malamulo osiyanasiyana ndi zowonetsera pa chitsanzo: European Pharmacopoeia imachokera pamagulu osiyanasiyana a ma viscosities osiyanasiyana ndi magawo osiyanasiyana olowa m'malo mwa zinthu zomwe zimagulitsidwa pamsika, zomwe zimafotokozedwa ndi magiredi kuphatikiza manambala, ndipo gawoli ndi "mPa s. ”. Ku US Pharmacopoeia, manambala a 4 amawonjezeredwa pambuyo pa dzina lachidziwitso kuti asonyeze zomwe zili ndi mtundu wa hydroxypropyl methylcellulose, monga hydroxypropyl methylcellulose 2208. Ziwerengero ziwiri zoyambirira zimayimira pafupifupi mtengo wa methoxy gulu. Peresenti, manambala awiri omaliza akuyimira pafupifupi peresenti ya hydroxypropyl.
Calocan's hydroxypropyl methylcellulose ili ndi mndandanda wa 3, womwe ndi mndandanda wa E, mndandanda wa F ndi mndandanda wa K, mndandanda uliwonse uli ndi mitundu yosiyanasiyana yosankha. Mndandanda wa E umagwiritsidwa ntchito kwambiri ngati zokutira zamafilimu, zomwe zimagwiritsidwa ntchito popaka piritsi, zida zotsekedwa zamapiritsi; E, F mndandanda ntchito ngati viscosifiers ndi kumasula wothandizila retarding mankhwala ophthalmic, suspending wothandizira, thickeners kwa madzi Kukonzekera, mapiritsi ndi Binders wa granules; K mndandanda umagwiritsidwa ntchito kwambiri ngati zoletsa kutulutsa ndi zida za hydrophilic gel matrix pokonzekera pang'onopang'ono komanso mowongolera.
Opanga apakhomo makamaka akuphatikizapo 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 mankhwala zomera, etc.
2.Ubwino wa HPMC
HPMC wakhala mmodzi wa anthu ambiri ntchito excipients mankhwala kunyumba ndi kunja, chifukwa HPMC ali ubwino kuti excipients ena alibe.
2.1 Kusungunuka kwamadzi ozizira
Kusungunuka m'madzi ozizira m'munsimu 40 ℃ kapena 70% Mowa, makamaka osasungunuka m'madzi otentha pamwamba pa 60 ℃, koma gel osakaniza.
2.2 Opanda mankhwala
HPMC ndi mtundu wa si-ionic mapadi efa, yankho alibe maayoni mlandu ndipo alibe kugwirizana ndi mchere zitsulo kapena ayoni organic mankhwala, kotero excipients ena sachita nawo popanga ndondomeko kukonzekera.
2.3 Kukhazikika
Ndiwokhazikika kwa asidi ndi zamchere, ndipo akhoza kusungidwa kwa nthawi yaitali pakati pa pH 3 ndi 11 popanda kusintha kwakukulu mu viscosity. Njira yamadzimadzi ya HPMC imakhala ndi anti-mildew ndipo imasunga kukhazikika kwa viscosity pakusungidwa kwanthawi yayitali. Zothandizira zamankhwala zomwe zimagwiritsa ntchito HPMC zimakhala ndi kukhazikika kwabwinoko kuposa zomwe zimagwiritsa ntchito zopangira zachikhalidwe (monga dextrin, wowuma, ndi zina).
2.4 Kusinthika kwa Viscosity
Osiyana mamasukidwe akayendedwe zotumphukira za HPMC akhoza kusakaniza mulingo wosiyana, ndi mamasukidwe akayendedwe ake akhoza kusinthidwa malinga ndi lamulo linalake, ndipo ali ndi ubale wabwino liniya, kotero gawo akhoza kusankhidwa malinga ndi zosowa.
2.5 Kulephera kwa metabolic
HPMC si odzipereka kapena zimapukusidwa mu thupi, ndipo sapereka kutentha, choncho ndi otetezeka mankhwala kukonzekera excipient. 2.6 Chitetezo Nthawi zambiri amaonedwa kuti HPMC ndi zinthu zopanda poizoni komanso zosakwiyitsa, mlingo wapakati wakupha mbewa ndi 5 g · kg - 1, ndipo mlingo wakupha wapakati pa makoswe ndi 5. 2 g · kg - 1. Mlingo watsiku ndi tsiku ndi wopanda vuto kwa thupi la munthu.
3.Kugwiritsa ntchito HPMC mu formulations
3.1 Monga zinthu zokutira filimu ndi zinthu zopangira mafilimu
Pogwiritsa ntchito HPMC ngati piritsi lophimbidwa ndi filimu, piritsi lophimbidwa liribe ubwino wodziwikiratu pobisa kukoma ndi maonekedwe poyerekeza ndi mapiritsi achikhalidwe monga mapiritsi okhala ndi shuga, koma kuuma kwake, friability, kuyamwa kwa chinyezi, digiri ya disintegration. , kupaka kulemera kwa kulemera ndi zizindikiro zina zabwinoko. Otsika mamasukidwe akayendedwe kalasi ya mankhwalawa amagwiritsidwa ntchito ngati madzi sungunuka filimu ❖ kuyanika zakuthupi pamapiritsi ndi mapiritsi, ndi mkulu mamasukidwe akayendedwe kalasi ntchito ngati filimu ❖ kuyanika zakuthupi organic zosungunulira kachitidwe, kawirikawiri pa ndende ya 2% mpaka 20. %.
Zhang Jixing et al. adagwiritsa ntchito njira yapamtunda kuti akwaniritse mapangidwe a premix ndi HPMC ngati zokutira filimu. Kutenga zinthu zopangira filimu HPMC, kuchuluka kwa mowa wa polyvinyl ndi plasticizer polyethylene glycol monga zinthu zofufuzira, kulimba kwamphamvu komanso kuthekera kwa filimuyo ndi The viscosity of the film coating solution ndi inspection index, ndi ubale pakati pa kuyendera. index ndi zinthu zowunikira zimafotokozedwa ndi masamu a masamu, ndipo njira yabwino yopangira zinthu imapezedwa. mowa wake ndi motero filimu kupanga wothandizira hydroxypropyl methylcellulose (HPMCE5) 11.88 g, polyvinyl mowa 24.12 g, plasticizer polyethylene glycol 13.00 g, ndi ❖ kuyanika kuyimitsidwa mamasukidwe akayendedwe kukhuthala ndi 20 mPa s, permeability ndi kumakoka mphamvu ya filimu . Zhang Yuan adakonza njira yokonzekera, adagwiritsa ntchito HPMC ngati chomangira m'malo mwa wowuma slurry, ndikusintha mapiritsi a Jiahua kukhala mapiritsi ophimbidwa ndi filimu kuti apititse patsogolo zokonzekera zake, apititse patsogolo hygroscopicity yake, yosavuta kuzimiririka, mapiritsi otayirira, ogawanika ndi zovuta zina, onjezerani kukhazikika kwa piritsi. The mulingo woyenera chiphunzitso ndondomeko anatsimikiza ndi orthogonal kuyesera, kutanthauza, slurry ndende anali 2% HPMC mu 70% Mowa njira pa ❖ kuyanika, ndi yolimbikitsa nthawi granulation anali 15 min. Zotsatira Mapiritsi opangidwa ndi filimu ya Jiahua okonzedwa ndi ndondomeko yatsopanoyi ndi mankhwala adasintha kwambiri maonekedwe, nthawi yowonongeka ndi kuuma kwapakati kusiyana ndi zomwe zinapangidwa ndi ndondomeko yoyambirira ya mankhwala, ndipo mlingo woyenerera wa mapiritsi ophimbidwa ndi filimuyo unasintha kwambiri. kufika pa 95%. Liang Meiyi, Lu Xiaohui, ndi zina zotero adagwiritsanso ntchito hydroxypropyl methylcellulose monga filimu yopangira filimu kukonzekera piritsi loyika patinae colon ndi matrine colon positioning tablet, motsatira. zimakhudza kutulutsidwa kwa mankhwala. Huang Yunran adakonza Mapiritsi a Dragon's Blood Colon Positioning, ndikuyika HPMC panjira yothetsera kutupa, ndipo gawo lake lalikulu linali 5%. Zitha kuwoneka kuti HPMC itha kugwiritsidwa ntchito kwambiri pamakina operekera mankhwala omwe amatsata m'matumbo.
Hydroxypropyl methylcellulose sizinthu zabwino kwambiri zokutira filimu, komanso zitha kugwiritsidwa ntchito ngati zinthu zopangira filimu popanga mafilimu. Wang Tongshun etc. ndi wokometsedwa kwa mankhwala a pawiri nthaka licorice ndi aminolexanol m`kamwa gulu gulu filimu, ndi kusinthasintha, kufanana, kusalala, mandala filimu wothandizila monga kafukufuku index, kupeza mulingo woyenera mankhwala ndi PVA 6.5 g, HPMC 0.1 g ndi 6.0 g wa propylene glycol amakwaniritsa zofunikira za kumasulidwa pang'onopang'ono ndi chitetezo, ndipo angagwiritsidwe ntchito monga kukonzekera mankhwala a kompositi filimu.
3.2 ngati chomangira komanso chosokoneza
Otsika mamasukidwe akayendedwe kalasi ya mankhwala angagwiritsidwe ntchito ngati binder ndi disintegrant kwa mapiritsi, mapiritsi ndi granules, ndi mkulu mamasukidwe akayendedwe kalasi angagwiritsidwe ntchito ngati binder. Mlingo umasiyanasiyana ndi mitundu yosiyanasiyana ndi zofunika. Nthawi zambiri, mlingo wa binder pamapiritsi owuma a granulation ndi 5%, ndipo mlingo wa binder pamapiritsi a granulation wonyowa ndi 2%.
Li Houtao et al adawunikira chophatikizira mapiritsi a tinidazole. 8% polyvinylpyrrolidone (PVP-K30), 40% madzi, 10% wowuma slurry, 2.0% hydroxypropyl methylcellulose K4 (HPMCK4M), 50% Mowa anafufuzidwa monga adhesion wa tinidazole mapiritsi motsatana. kukonzekera mapiritsi a tinidazole. Mawonekedwe akusintha kwamapiritsi osamveka bwino komanso atapaka utoto adafaniziridwa, ndipo kulimba, kuuma, malire a nthawi ya kupasuka komanso kusungunuka kwa mapiritsi osiyanasiyana adayesedwa. Zotsatira Mapiritsi opangidwa ndi 2.0% hydroxypropyl methylcellulose anali onyezimira, ndipo muyeso wa friability sunapeze chodabwitsa cham'mphepete ndi kumakona, ndipo atapaka, mawonekedwe a piritsi anali athunthu ndipo mawonekedwe ake anali abwino. Choncho, tinidazole mapiritsi okonzeka ndi 2.0% HPMC-K4 ndi 50% Mowa monga zomangira ntchito. Guan Shihai anaphunzira ndondomeko chiphunzitso cha Mapale Fuganning, kufufuzidwa zomatira, ndi kuwunika 50% Mowa, 15% wowuma phala, 10% PVP ndi 50% Mowa njira ndi compressibility, kusalala, ndi friability monga kuunika zizindikiro. , 5% CMC-Na ndi 15% HPMC yankho (5 mPa s). Zotsatira Mapepala okonzedwa ndi 50% Mowa, 15% wowuma phala, 10% PVP 50% Mowa njira ndi 5% CMC-Na anali pamwamba yosalala, koma compressibility osauka ndi otsika kuuma, amene sakanatha kukwaniritsa zosowa ❖ kuyanika; 15% HPMC yankho ( 5 mPa · s), pamwamba pa piritsi ndi yosalala, friability ndi oyenerera, ndipo compressibility ndi zabwino, amene angathe kukwaniritsa zofunika zokutira. Chifukwa chake, HPMC (5 mPa s) idasankhidwa kukhala zomatira.
3.3 ngati woyimitsa ntchito
Mkulu-makamaka mamasukidwe kalasi ya mankhwala ntchito ngati suspending wothandizira kukonzekera kuyimitsidwa-mtundu wa madzi kukonzekera. Zili ndi zotsatira zabwino zoyimitsa, ndizosavuta kufalitsanso, sizimamatira pakhoma, ndipo zimakhala ndi particles zabwino za flocculation. Mlingo wamba ndi 0.5% mpaka 1.5%. Song Tian et al. amagwiritsidwa ntchito polima zipangizo zambiri (hydroxypropyl methylcellulose, sodium carboxymethylcellulose, povidone, xanthan chingamu, methylcellulose, etc.) monga suspending wothandizira kukonzekera racecadotril. kuyimitsidwa youma. Kupyolera mu chiŵerengero cha sedimentation voliyumu ya kuyimitsidwa kosiyana, chiwerengero cha redispersibility index, ndi rheology, kuyimitsidwa mamasukidwe akayendedwe ndi kachitidwe kakang'ono kakang'ono kakuwoneka, ndipo kukhazikika kwa tinthu tating'onoting'ono ta mankhwala pansi pa kuyesera kofulumira kunafufuzidwanso. Zotsatira Kuyimitsidwa kowuma kokonzedwa ndi 2% HPMC monga wothandizira woyimitsa anali ndi njira yosavuta komanso yokhazikika bwino.
Poyerekeza ndi methyl cellulose, hydroxypropyl methyl cellulose ili ndi mawonekedwe opangira yankho lomveka bwino, ndipo pali zinthu zochepa chabe zomwe sizimabalalika, kotero HPMC imagwiritsidwanso ntchito ngati choyimitsa pokonzekera maso. Liu Jie et al. ntchito HPMC, hydroxypropyl mapadi (HPC), carbomer 940, polyethylene glycol (PEG), sodium hyaluronate (HA) ndi kuphatikiza HA/HPMC monga suspending wothandizira kukonzekera specifications osiyana Pakuti Ciclovir ophthalmic kuyimitsidwa, sedimentation voliyumu chiŵerengero, tinthu kukula ndi redispersibility amasankhidwa ngati zizindikiro zowunikira kuti awonetsere woyimitsa bwino kwambiri. Zotsatira zimasonyeza kuti acyclovir ophthalmic kuyimitsidwa anakonza 0,05% HA ndi 0,05% HPMC monga suspending wothandizira, ndi sedimentation buku chiŵerengero ndi 0,998, tinthu kukula ndi yunifolomu, ndi redispersibility zabwino, ndi kukonzekera khola Kugonana kumawonjezera.
3.4 Monga chotsekereza, chotulutsa pang'onopang'ono komanso chowongolera komanso chopanga pore
Mlingo wapamwamba kwambiri wa mankhwalawa umagwiritsidwa ntchito popanga mapiritsi otulutsidwa a hydrophilic gel matrix, otsekereza ndi owongolera omwe amatulutsidwa ndi mapiritsi osakanikirana a matrix okhazikika, ndipo amakhala ndi zotsatira zakuchedwetsa kutulutsidwa kwa mankhwala. Kukhazikika kwake ndi 10% mpaka 80%. Makalasi otsika amachulukidwe otsika amagwiritsidwa ntchito ngati ma porogens pokonzekera kumasulidwa kosalekeza kapena kukonzekera kumasulidwa. Mlingo woyambirira wofunikira pakuchiritsa mapiritsi oterowo utha kufikika mwachangu, ndiyeno kumasulidwa kosalekeza kapena kumasulidwa kokhazikika kumachitika, ndipo ndende yogwira ntchito yamagazi imasungidwa m'thupi. . Hydroxypropyl methylcellulose imathiridwa madzi kuti ipange gel wosanjikiza ikakumana ndi madzi. Njira yotulutsa mankhwala kuchokera papiritsi ya matrix makamaka imaphatikizapo kufalikira kwa gel osanjikiza ndi kukokoloka kwa gel osanjikiza. Jung Bo Shim et al anakonza mapiritsi a carvedilol otulutsidwa ndi HPMC ngati zinthu zotulutsidwa.
Hydroxypropyl methylcellulose imagwiritsidwanso ntchito kwambiri m'mapiritsi okhazikika amankhwala achi China, ndipo zinthu zambiri zomwe zimagwiritsidwa ntchito, zida zogwira mtima komanso zokonzekera limodzi zamankhwala achi China zimagwiritsidwa ntchito. Liu Wen et al. adagwiritsa ntchito 15% hydroxypropyl methylcellulose ngati matrix, 1% lactose ndi 5% microcrystalline cellulose ngati zodzaza, ndikukonza Decoction ya Jingfang Taohe Chengqi kukhala mapiritsi otulutsa pakamwa. Chitsanzo ndi equation ya Higuchi. Dongosolo lopanga ma fomula ndi losavuta, kukonzekera ndikosavuta, ndipo kutulutsidwa kwa data kumakhala kokhazikika, komwe kumakwaniritsa zofunikira za Chinese Pharmacopoeia. Tang Guanguang et al. adagwiritsa ntchito ma saponins okwana a Astragalus ngati mankhwala achitsanzo, adakonza mapiritsi a matrix a HPMC, ndikuwunika zomwe zimakhudza kutulutsidwa kwa mankhwalawa kuchokera kumadera ogwira mtima amankhwala achi China pamapiritsi a HPMC matrix. Zotsatira Pamene mlingo wa HPMC ukukwera, kutulutsidwa kwa astragaloside kunatsika, ndipo kuchuluka kwa mankhwalawo kunali ndi ubale wofanana ndi kusungunuka kwa matrix. Mu piritsi la hypromellose HPMC matrix, pali ubale wina pakati pa kutulutsidwa kwa gawo lothandiza la mankhwala achi China komanso mlingo ndi mtundu wa HPMC, komanso kutulutsidwa kwa hydrophilic chemical monomer ndikofanana. Hydroxypropyl methylcellulose siyoyenera kokha kwa mankhwala a hydrophilic, komanso zinthu zomwe si hydrophilic. Liu Guihua adagwiritsa ntchito 17% hydroxypropyl methylcellulose (HPMCK15M) ngati zinthu zomwe zimatulutsidwa mosalekeza, ndipo adakonza mapiritsi a Tianshan Xuelian osasunthika pogwiritsa ntchito granulation yonyowa komanso njira yolembera. Kutulutsa kosalekeza kunali koonekeratu, ndipo njira yokonzekera inali yokhazikika komanso yotheka.
Hydroxypropyl methylcellulose sikuti amangogwiritsidwa ntchito pamapiritsi a matrix okhazikika a zosakaniza zogwira ntchito komanso mbali zogwira mtima zamankhwala achi China, komanso amagwiritsidwa ntchito mochulukira pokonzekera mankhwala achikhalidwe achi China. Wu Huichao et al. adagwiritsa ntchito 20% hydroxypropyl methyl cellulose (HPMCK4M) ngati matrix, ndipo adagwiritsa ntchito njira yopondereza ya ufa mwachindunji kukonzekera Yizhi hydrophilic gel matrix piritsi yomwe imatha kumasula mankhwalawa mosalekeza komanso mokhazikika kwa maola 12. Saponin Rg1, ginsenoside Rb1 ndi Panax notoginseng saponin R1 adagwiritsidwa ntchito ngati zowunikira kuti afufuze kutulutsidwa kwa in vitro, ndipo equation yotulutsa mankhwala idayikidwa kuti iphunzire njira yotulutsira mankhwala. Zotsatira Njira yotulutsa mankhwala imayenderana ndi zero-order kinetic equation ndi Ritger-Peppas equation, momwe geniposide idatulutsidwa ndi kufalikira kwa non-Fick, ndipo zigawo zitatu za Panax notoginseng zidatulutsidwa ndi kukokoloka kwa chigoba.
3.5 Zomatira zodzitchinjiriza ngati thickener ndi colloid
Izi zikagwiritsidwa ntchito ngati thickener, kuchuluka kwanthawi zonse kumakhala 0.45% mpaka 1.0%. Komanso kuonjezera bata wa guluu hydrophobic, kupanga colloid zoteteza, kuteteza particles kuchokera coalescing ndi agglomerating, potero inhibiting mapangidwe matope. Kuphatikizika kwake kwakukulu ndi 0.5% mpaka 1.5%.
Wang Zhen et al. adagwiritsa ntchito njira yoyesera ya L9 orthogonal kuti afufuze njira yokonzekera mankhwala opangidwa ndi carbon enema. Njira yabwino kwambiri yodziwira mankhwala opangidwa ndi carbon enema ndi 0.5% sodium carboxymethyl cellulose ndi 2.0% hydroxypropyl methylcellulose (HPMC ili ndi 23.0% methoxyl gulu, hydroxypropoxyl Base 11.6%) monga thickener, ndondomeko yothandizira kukhazikika kwa mankhwala activated carbon. Zhang Zhiqiang et al. anapanga gel osakaniza pH-sensitive levofloxacin hydrochloride ophthalmic ophthalmic wokonzeka kugwiritsa ntchito, pogwiritsa ntchito carbopol monga gel matrix ndi hydroxypropyl methylcellulose monga thickening agent. Mulingo woyenera kwambiri wa mankhwala ndi kuyesera, potsiriza amapeza mulingo woyenera mankhwala ndi levofloxacin hydrochloride 0.1 g, carbopol (9400) 3 g, hydroxypropyl methylcellulose (E50 LV) 20 g, disodium hydrogen hydrogen 0.35 g, phosphoric acid 0.45 g wa sodium chloride 0.45 g wa sodium diphosphate. , 0.03 g wa ethyl paraben, ndi madzi adawonjezeredwa kuti apange 100 ml. M'mayesowa, wolemba adawonetsa mndandanda wa hydroxypropyl methylcellulose METHOCEL wa Colourcon Company wokhala ndi mawonekedwe osiyanasiyana (K4M, E4M, E15 LV, E50LV) kuti akonzekere zokhuthala mosiyanasiyana, ndipo zotsatira zake zidasankha HPMC E50 LV ngati chowonjezera. Thickener kwa pH-tcheru levofloxacin hydrochloride ma gel osakaniza.
3.6 ngati kapisozi zakuthupi
Nthawi zambiri, chipolopolo cha kapisozi cha makapisozi chimakhala ndi gelatin. Kapangidwe ka chipolopolo cha kapisozi ndi chosavuta, koma pali mavuto ndi zochitika zina monga chitetezo chosatetezeka ku chinyezi ndi mankhwala osokoneza okosijeni, kuchepetsa kusungunuka kwa mankhwala, ndi kuchedwa kutha kwa chipolopolo cha capsule panthawi yosungira. Choncho, hydroxypropyl methylcellulose ntchito m'malo mwa makapisozi gelatin pokonza makapisozi, amene bwino kapisozi kupanga formability ndi zotsatira ntchito, ndipo wakhala ankalimbikitsa kunyumba ndi kunja.
Kugwiritsa ntchito theophylline ngati mankhwala owongolera, Podczeck et al. anapeza kuti kusungunuka kwa mankhwala kwa makapisozi okhala ndi zipolopolo za hydroxypropyl methylcellulose kunali kwakukulu kuposa makapisozi a gelatin. Chifukwa cha kusanthula ndi kuti kupasuka kwa HPMC ndi kupasuka kwa kapisozi lonse pa nthawi yomweyo, pamene kupasuka kwa gelatin kapisozi ndi kupasuka kwa dongosolo maukonde poyamba, ndiyeno kupasuka kwa kapisozi lonse, kotero kuti kutha kwa kapisozi gelatin. Kapisozi wa HPMC ndi woyenera kwambiri ku zipolopolo za Capsule kuti atulutsidwe mwachangu. Chiwele et al. adapezanso malingaliro ofanana ndikuyerekeza kusungunuka kwa gelatin, gelatin / polyethylene glycol ndi zipolopolo za HPMC. Zotsatira zake zidawonetsa kuti zipolopolo za HPMC zidasungunuka mwachangu pansi pazikhalidwe zosiyanasiyana za pH, pomwe makapisozi a gelatin Zimakhudzidwa kwambiri ndi mitundu yosiyanasiyana ya pH. Tang Yue et al. anawonetsa mtundu watsopano wa kapisozi chipolopolo kwa otsika mlingo mankhwala akusowekapo ufa youma inhaler chonyamulira dongosolo. Poyerekeza ndi chipolopolo cha kapisozi cha hydroxypropyl methylcellulose ndi chipolopolo cha kapisozi cha gelatin, kukhazikika kwa chipolopolo cha kapisozi ndi katundu wa ufa mu chipolopolo pansi pazikhalidwe zosiyanasiyana adafufuzidwa, ndipo kuyesa kwa friability kunachitika. Zotsatira zimasonyeza kuti poyerekeza ndi makapisozi gelatin, HPMC kapisozi zipolopolo ndi bwino mu bata ndi chitetezo ufa, kukhala ndi mphamvu chinyezi kukana, ndi kukhala ndi friability m'munsi kuposa gelatin kapisozi zipolopolo, kotero HPMC kapisozi zipolopolo ndi oyenera Makapisozi kwa ufa youma inhalation.
3.7 ngati bioadhesive
Tekinoloje ya bioadhesion imagwiritsa ntchito zowonjezera ndi ma polima a bioadhesive. Mwa kutsatira kwachilengedwenso mucosa, kumawonjezera kupitiriza ndi zothina kukhudzana ndi kukonzekera ndi mucosa, kuti mankhwala pang`onopang`ono anamasulidwa ndi odzipereka ndi mucosa kukwaniritsa cholinga cha mankhwala. Amagwiritsidwa ntchito kwambiri masiku ano. Chithandizo cha matenda a m`mimba thirakiti, nyini, m`kamwa mucosa ndi mbali zina.
Tekinoloje ya m'mimba ya bioadhesion ndi njira yatsopano yoperekera mankhwala yomwe idapangidwa zaka zaposachedwa. Sikuti prolongs okhala nthawi ya mankhwala kukonzekera mu m`mimba thirakiti, komanso bwino kukhudzana ntchito pakati pa mankhwala ndi nembanemba selo pa mayamwidwe malo, kusintha fluidity wa selo nembanemba, ndi kupanga The malowedwe a mankhwala mu maselo ang'onoang'ono a m'matumbo a epithelial amalimbikitsidwa, potero kumapangitsa kuti mankhwalawa azikhala ndi bioavailability. Wei Keda et al. adaunika malangizo a piritsi limodzi ndi mlingo wa HPMCK4M ndi Carbomer 940 monga zinthu zofufuzira, ndipo adagwiritsa ntchito chipangizo chodzipangira chokha kuti apime mphamvu yapakati pa piritsilo ndi biofilm yofananira ndi mtundu wamadzi a m'thumba lapulasitiki. , ndipo potsirizira pake anasankha zomwe zili mu HPMCK40 ndi carbomer 940 kuti zikhale 15 ndi 27.5 mg m'malo abwino kwambiri a mapiritsi a NCaEBT mapiritsi, motero, kukonzekera mapiritsi a mapiritsi a NCaEBT, kusonyeza kuti zipangizo za bioadhesive (monga hydroxypropyl methylcellulose) zingachepetse kwambiri Kupititsa patsogolo kumamatira kwa kukonzekera kwa minofu.
Kukonzekera kwapakamwa kwa bioadhesive ndi mtundu watsopano wa njira yoperekera mankhwala yomwe yaphunziridwa kwambiri m'zaka zaposachedwa. Oral bioadhesive kukonzekera akhoza kutsatira mankhwala kukhudzidwa mbali ya m`kamwa patsekeke, amene osati prolongs okhala nthawi ya mankhwala mu m`kamwa mucosa, komanso kuteteza m`kamwa mucosa. Bwino achire zotsatira ndi bwino mankhwala bioavailability. Xue Xiaoyan et al. kukhathamiritsa mapangidwe a insulin oral zomatira mapiritsi, ntchito apple pectin, chitosan, carbomer 934P, hydroxypropyl methylcellulose (HPMC K392) ndi sodium alginate monga bioadhesive zipangizo, ndi kuzizira-kuyanika kukonzekera pakamwa insulin. Zomatira pawiri wosanjikiza pepala. Piritsi lokonzekera la insulin pakamwa lili ndi mawonekedwe a porous ngati siponji, omwe ndi abwino kutulutsa insulini, ndipo amakhala ndi hydrophobic protective layer, yomwe imatha kuwonetsetsa kutulutsidwa kwa mankhwalawo ndikupewa kutayika kwa mankhwalawa. Hao Jifu et al. Anakonzanso mikanda yabuluu-yellow pakamwa pogwiritsa ntchito guluu wa Baiji, HPMC ndi carbomer ngati zinthu zomatira.
M'njira zoperekera mankhwala kumaliseche, ukadaulo wa bioadhesion wagwiritsidwanso ntchito kwambiri. Zhu Yuting et al. ntchito carbomer (CP) ndi HPMC monga zomatira zipangizo ndi kupitiriza-kumasulidwa masanjidwewo kukonzekera clotrimazole bioadhesive nyini mapiritsi ndi formulations osiyana ndi ziŵerengero, ndipo anayeza awo adhesion, nthawi adhesion ndi kuchuluka kutupa mu chilengedwe cha yokumba madzimadzi kumaliseche. , mankhwala oyenera adawonetsedwa ngati CP-HPMC1: 1, pepala lomata lokonzekera linali ndi ntchito yabwino yomatira, ndipo njirayo inali yosavuta komanso yotheka.
3.8 ngati gel osakaniza
Monga kukonzekera zomatira, gel osakaniza ali ndi ubwino wambiri monga chitetezo, kukongola, kuyeretsa kosavuta, mtengo wotsika, njira yosavuta yokonzekera, komanso kugwirizanitsa bwino ndi mankhwala. Mayendedwe a chitukuko. Mwachitsanzo, gel transdermal ndi mawonekedwe atsopano a mlingo omwe adaphunziridwa kwambiri m'zaka zaposachedwa. Iwo sangakhoze kokha kupewa chiwonongeko cha mankhwala m`mimba thirakiti ndi kuchepetsa pachimake-ndi-m'mbewa kusiyanasiyana kwa magazi mankhwala ndende, komanso wakhala mmodzi wa ogwira mankhwala kumasulidwa kachitidwe kugonjetsa mankhwala mavuto. .
Zhu Jingjie et al. adaphunzira zotsatira za matrices osiyanasiyana pakutulutsa gel osakaniza a scutellarin alcohol plastid mu vitro, ndikuwunika ndi carbomer (980NF) ndi hydroxypropyl methylcellulose (HPMCK15M) ngati matrices a gel, ndipo adapeza scutellarin yoyenera scutellarin. Gel matrix a mowa plastids. Zotsatira zoyesera zimasonyeza kuti 1. 0% carbomer, 1. 5% carbomer, 1. 0% carbomer + 1. 0% HPMC, 1. 5% carbomer + 1. 0% HPMC monga gel matrix Onsewa ndi oyenera scutellarin mowa plastids . Panthawi yoyesera, zidapezeka kuti HPMC ikhoza kusintha njira yotulutsira mankhwala a carbomer gel matrix potengera kinetic equation ya kutulutsidwa kwa mankhwala, ndipo 1.0% HPMC imatha kusintha 1.0% carbomer matrix ndi 1.5% carbomer matrix. Chifukwa chingakhale chakuti HPMC ikukula mofulumira, ndipo kuwonjezereka kofulumira kumayambiriro kwa kuyesa kumapangitsa kusiyana kwa maselo a carbomer gel zinthu zazikulu, motero kufulumizitsa kutulutsa kwake mankhwala. Zhao Wencui et al. adagwiritsa ntchito carbomer-934 ndi hydroxypropyl methylcellulose ngati zonyamulira kukonza norfloxacin ophthalmic gel. Njira yokonzekera ndi yosavuta komanso yotheka, ndipo khalidweli likugwirizana ndi gel ophthalmic "Chinese Pharmacopoeia" (kope la 2010) Zofunikira za khalidwe.
3.9 Precipitation inhibitor for self-microemulsifying system
Self-microemulsifying drug delivery system (SMEDDS) ndi mtundu watsopano wa njira yoperekera mankhwala pakamwa, yomwe imakhala yosakanikirana, yokhazikika komanso yowonekera yopangidwa ndi mankhwala, gawo la mafuta, emulsifier ndi co-emulsifier. Mapangidwe a mankhwalawa ndi ophweka, ndipo chitetezo ndi bata ndi zabwino. Pakuti bwino sungunuka mankhwala, madzi sungunuka CHIKWANGWANI polima zipangizo, monga HPMC, polyvinylpyrrolidone (PVP), etc., nthawi zambiri anawonjezera kuti ufulu mankhwala ndi mankhwala encapsulated mu microemulsion kukwaniritsa supersaturated kuvunda mu m`mimba thirakiti, kuti kuonjezera kusungunuka kwa mankhwala ndikusintha bioavailability.
Peng Xuan et al. anakonza silibinin supersaturated self-emulsifying drug delivery system (S-SEDDS). Oxyethylene hydrogenated castor oil (Cremophor RH40), 12% caprylic capric acid polyethylene glycol glyceride (Labrasol) monga co-emulsifier, ndi 50 mg·g-1 HPMC. Kuonjezera HPMC ku SSEDDS kumatha kuchulukitsa silibinin yaulere kuti isungunuke mu S-SEDDS ndikuletsa silibinin kuti isatuluke. Poyerekeza ndi mapangidwe achikhalidwe a self-microemulsion formulations, kuchuluka kwa surfactant nthawi zambiri kumawonjezedwa kuti tipewe kutsekeka kosakwanira kwa mankhwala. Kuwonjezera HPMC akhoza kusunga solubility wa silibinin mu kuvunda sing'anga ndi zonse, kuchepetsa emulsification mu self-microemulsion formulations. Mlingo wa wothandizila.
4.Mapeto
Zitha kuwoneka kuti HPMC yakhala ikugwiritsidwa ntchito kwambiri pokonzekera chifukwa cha thupi, mankhwala ndi zamoyo, koma HPMC ilinso ndi zofooka zambiri pokonzekera, monga chodabwitsa cha kumasulidwa kusanachitike ndi pambuyo pake. methyl methacrylate) kuti musinthe. Nthawi yomweyo, ofufuza ena adafufuza zakugwiritsa ntchito chiphunzitso cha osmotic mu HPMC pokonzekera mapiritsi otulutsa carbamazepine ndi mapiritsi otulutsa a verapamil hydrochloride kuti apitirize kuphunzira momwe amatulutsira. Mwachidule, ofufuza ochulukirapo akugwira ntchito zambiri kuti agwiritse ntchito bwino HPMC pokonzekera, komanso pophunzira mozama za katundu wake ndi kupititsa patsogolo luso la kukonzekera, HPMC idzagwiritsidwa ntchito kwambiri mumitundu yatsopano ya mlingo. ndi mafomu atsopano a mlingo. Mu kafukufuku wa mankhwala dongosolo, ndiyeno kulimbikitsa mosalekeza chitukuko cha mankhwala.
Nthawi yotumiza: Oct-08-2022