Izincwadi ezihlobene ekhaya nakwamanye amazwe ekulungiseleleni izinto ezisiza ezenza imithi i-hydroxypropyl methylcellulose (HPMC) eminyakeni yamuva zibuyekeziwe, zahlaziywa futhi zafingqwa, futhi ukusetshenziswa kwazo emalungiselelweni aqinile, amalungiselelo oketshezi, amalungiselelo okukhululwa aqhubekayo futhi alawulwayo, amalungiselelo e-capsule, i-gelatin The latest izinhlelo zokusebenza emkhakheni wokwakheka okusha okufana ne-adhesive formulations nama-bioadhesives. Ngenxa yomehluko esisindweni samangqamuzana ahlobene kanye ne-viscosity ye-HPMC, inezici kanye nokusetshenziswa kwe-emulsification, ukunamathela, ukuqina, ukukhuphuka kwe-viscosity, ukumisa okwesikhashana, i-gelling kanye nokwenza ifilimu. Isetshenziswa kabanzi emalungiselelweni emithi futhi izodlala indima enkulu emkhakheni wamalungiselelo. Ngocwaningo olujulile lwezakhiwo zayo kanye nokuthuthukiswa kobuchwepheshe bokubunjwa, i-HPMC izosetshenziswa kabanzi ocwaningweni lwamafomu amasha omthamo kanye nezinhlelo ezintsha zokulethwa kwezidakamizwa, ngaleyo ndlela kuthuthukiswe ukuthuthukiswa okuqhubekayo kwezithako.
i-hydroxypropyl methylcellulose; amalungiselelo emithi; ama-excipients emithi.
Ama-excipients emithi akuzona nje isisekelo esibonakalayo sokwakhiwa kwamalungiselelo emithi eluhlaza, kodwa futhi ahlobene nobunzima benqubo yokulungisa, ikhwalithi yezidakamizwa, ukuzinza, ukuphepha, izinga lokukhululwa kwezidakamizwa, indlela yokwenza, ukusebenza kahle komtholampilo, kanye nokuthuthukiswa kwemishanguzo emisha. amafomu omthamo kanye nezindlela ezintsha zokuphatha. ehlobene eduze. Ukuvela kwezakhi ezintsha zemithi ngokuvamile kukhuthaza ukuthuthukiswa kwekhwalithi yokulungiselela kanye nokuthuthukiswa kwamafomu amasha omthamo. I-Hydroxypropyl methylcellulose (HPMC) ingesinye sezisiza ezidume kakhulu zemithi ekhaya naphesheya. Ngenxa yesisindo sayo samangqamuzana ahlukene kanye ne-viscosity, inemisebenzi yokuhlanganisa, ukubopha, ukuqina, ukuqina, ukumisa, nokunamathisela. Izici nokusetshenziswa okufana ne-coagulation kanye nokwakheka kwefilimu kusetshenziswa kakhulu kubuchwepheshe bezemithi. Lo mbhalo ikakhulukazi ubuyekeza ukusetshenziswa kwe-hydroxypropyl methylcellulose (HPMC) ekwenziweni eminyakeni yamuva nje.
1.Izakhiwo eziyisisekelo ze-HPMC
I-Hydroxypropyl methyl cellulose (HPMC), ifomula yamangqamuzana i-C8H15O8-(C10 H18O6) n- C8H15O8, futhi isisindo samangqamuzana esihlobene cishe singama-86 000. Lo mkhiqizo uyingxenye ye-semi-synthetic, eyingxenye ye-methyl nengxenye ye-polyhydroxypropyl ether i-cellulose. Ingakhiqizwa ngezindlela ezimbili: Eyodwa ukuthi i-methyl cellulose yebanga elifanele iphathwa nge-NaOH bese isabela nge-propylene oxide ngaphansi kwezinga lokushisa eliphezulu nokucindezela okukhulu. Isikhathi sokuphendula kufanele sithathe isikhathi eside ngokwanele ukuvumela i-methyl ne-hydroxypropyl ukuthi yakhe izibopho ze-ether Ixhunywe kwendandatho ye-anhydroglucose ye-cellulose ngendlela ye-cellulose, futhi ingafinyelela izinga elifunayo; enye iwukwelapha i-linter kakotini noma i-wood pulp fiber nge-caustic soda, bese isabela nge-chlorinated methane ne-propylene oxide ngokulandelana, bese iqhubeka nokuyicwenga. , ichotshozwe ibe yimpushana ecolekile futhi efanayo noma ama-granules.
Umbala walo mkhiqizo umhlophe kuya komhlophe omhlophe, awunaphunga futhi awunambitheki, futhi ifomu liyimpushana noma impushana egeleza kalula. Lo mkhiqizo ungancibilika emanzini ukuze wenze isisombululo se-colloidal esimhlophe esimhlophe esine-viscosity ethile. I-sol-gel interconversion phenomenon ingenzeka ngenxa yokushintsha kwezinga lokushisa kwesisombululo ngokugxila okuthile.
Ngenxa yomehluko kokuqukethwe kwalezi zingxenye ezimbili ezakhiweni ze-methoxy ne-hydroxypropyl, izinhlobo ezahlukene zemikhiqizo ziye zavela. Ekugxilweni okukhethekile, izinhlobo ezahlukene zemikhiqizo zinezici ezithile. I-viscosity kanye nokushisa kwe-gelation eshisayo, ngakho-ke kunezindawo ezihlukene futhi ingasetshenziswa ngezinhloso ezahlukene. I-Pharmacopoeia yamazwe ahlukahlukene inemithethonqubo ehlukene kanye nezethulo kumodeli: I-European Pharmacopoeia isekelwe emazingeni ahlukene e-viscosities ehlukene kanye namazinga ahlukene okushintshaniswa kwemikhiqizo ethengiswa emakethe, evezwe ngamamaki kanye nezinombolo, futhi iyunithi ithi “mPa s. ”. E-US Pharmacopoeia, amadijithi angu-4 angeziwe ngemva kwegama elijwayelekile ukukhombisa okuqukethwe kanye nohlobo lwe-hydroxypropyl methylcellulose ngayinye, njenge-hydroxypropyl methylcellulose 2208. Amadijithi amabili okuqala amelela inani elilinganiselwe leqembu le-methoxy. Amaphesenti, amadijithi amabili okugcina amelela cishe amaphesenti e-hydroxypropyl.
I-Calocan's hydroxypropyl methylcellulose inochungechunge olu-3, okungukuthi uchungechunge luka-E, uchungechunge luka-F nochungechunge lwe-K, uchungechunge ngalunye lunamamodeli ahlukahlukene ongakhetha kuwo. Uchungechunge lwe-E lusetshenziswa kakhulu njengezingubo zefilimu, ezisetshenziselwa ukugqoka ithebhulethi, izintambo zethebhulethi ezivaliwe; Uchungechunge lwe-E, F lusetshenziswa njengama-viscosifiers kanye nama-ejenti okubuyisela emuva ekulungiselelweni kwe-ophthalmic, ama-agent amisiwe, ama-thickeners okulungiselela uketshezi, amaphilisi kanye nama-Binders of granules; Uchungechunge lwe-K lusetshenziswa kakhulu njengama-release inhibitors kanye nezinto ze-hydrophilic gel matrix zokulungiselela ukukhululwa okunensayo nalawulwayo.
Abakhiqizi basekhaya ikakhulukazi bahlanganisa i-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., izitshalo zamakhemikhali ze-Xi'an Huian, njll.
2.Izinzuzo ze-HPMC
I-HPMC isibe ngomunye wabasizi bemithi abasetshenziswa kakhulu ekhaya naphesheya, ngoba i-HPMC inezinzuzo ezinye izihlanganisi ezingenazo.
2.1 Ukuncibilika kwamanzi abandayo
Incibilika emanzini abandayo angaphansi kuka-40 ℃ noma 70% ethanol, ngokuyisisekelo ayincibiliki emanzini ashisayo angaphezu kuka-60 ℃, kodwa ikwazi ukwenza ijeli.
2.2 I-inert ngamakhemikhali
I-HPMC iwuhlobo lwe-non-ionic cellulose ether, ikhambi layo alinayo i-ionic charge futhi ayihlangani nosawoti wensimbi noma ama-ionic organic compounds, ngakho-ke ezinye izinto ezisizayo azisabelani nazo ngesikhathi sokukhiqizwa kwamalungiselelo.
2.3 Ukuzinza
Iqinile ngokuqhathaniswa kukho kokubili i-asidi ne-alkali, futhi ingagcinwa isikhathi eside phakathi kwe-pH 3 kanye ne-11 ngaphandle koshintsho olubalulekile ku-viscosity. Isixazululo esinamanzi se-HPMC sinomphumela wokunqanda isikhutha futhi sigcina ukuqina okuhle kwe-viscosity ngesikhathi sokugcina isikhathi eside. Izisetshenziswa zemithi ezisebenzisa i-HPMC zinokuzinza kwekhwalithi engcono kunalezo ezisebenzisa izinto ezisizayo zendabuko (ezifana ne-dextrin, isitashi, njll.).
2.4 I-Viscosity Adjustability
I-viscosity derivatives ehlukene ye-HPMC ingaxutshwa ngezilinganiso ezahlukene, futhi i-viscosity yayo ingashintshwa ngokuvumelana nomthetho othile, futhi inobudlelwane obuhle bomugqa, ngakho-ke ingxenye ingakhethwa ngokuvumelana nezidingo.
2.5 Ukungasebenzi kahle kwe-metabolic
I-HPMC ayimuncwa noma igaywe emzimbeni, futhi ayinikezi ukushisa, ngakho-ke iyisisetshenziswa esiphephile sokulungiselela imithi. 2.6 Ukuphepha Ngokuvamile kucatshangelwa ukuthi i-HPMC iyinto engenabuthi futhi engacasuli, umthamo obulalayo omaphakathi wamagundane ngu-5 g·kg – 1, kanti umthamo obulalayo omaphakathi wamagundane ngu-5. 2 g · kg – 1. Umthamo wansuku zonke awunangozi emzimbeni womuntu.
3.Ukusetshenziswa kwe-HPMC ekwenziweni
3.1 Njengezinto zokumboza ifilimu nezinto zokwakha ifilimu
Isebenzisa i-HPMC njengendwangu yethebhulethi ehlanganiswe nefilimu, ithebhulethi enamathebulethi ayinazo izinzuzo ezisobala ekufihleni ukunambitheka nokubukeka uma iqhathaniswa namaphilisi endabuko ambozwe njengamaphilisi afakwe ushukela, kodwa ubulukhuni bayo, ukugoba, ukumuncwa komswakama, idigri yokuhlakazeka. , ukuzuza kwesisindo sokugqoka nezinye izinkomba zekhwalithi zingcono. Ibanga eliphansi le-viscosity lalo mkhiqizo lisetshenziswa njengento yokumboza ifilimu encibilika emanzini kumathebulethi namaphilisi, futhi ibanga le-viscosity ephezulu lisetshenziswa njengento yokumboza ifilimu yezinhlelo ze-organic solvent, imvamisa ekugxilweni kuka-2% kuya ku-20. %.
UZhang Jixing et al. isebenzise indlela yomphumela wokwenza ngcono ukwakheka kwe-premix nge-HPMC njengokwemboza kwefilimu. Ukuthatha izinto zokwakha ifilimu i-HPMC, inani le-polyvinyl alcohol ne-plasticizer polyethylene glycol njengezici zophenyo, amandla aqinile kanye nokungeneka kwefilimu kanye ne-Viscosity yesisombululo sokumboza ifilimu inkomba yokuhlola, kanye nobudlelwano phakathi kokuhlolwa. inkomba kanye nezici zokuhlola kuchazwa imodeli yezibalo, futhi inqubo yokwakheka efanele itholakala ekugcineni. Ukusetshenziswa kwayo ngokulandelana kuyi-ejenti eyenza ifilimu i-hydroxypropyl methylcellulose (HPMCE5) 11.88 g, i-polyvinyl alcohol 24.12 g, i-plasticizer polyethylene glycol 13.00 g, kanye ne-viscosity yokumiswa kokumbozayo ingu-20 mPa·s, ukunwebeka kanye namandla aqinile efilimu. . U-Zhang Yuan uthuthukise inqubo yokulungiselela, wasebenzisa i-HPMC njengesibophezelo sokuthatha indawo ye-starch slurry, futhi washintsha amaphilisi e-Jiahua aba amaphilisi anefilimu ukuze kuthuthukiswe ikhwalithi yamalungiselelo awo, athuthukise i-hygroscopicity yawo, ukufiphala kalula, amaphilisi axekethile, ahlukene kanye nezinye izinkinga, thuthukisa ukuzinza kwethebhulethi. Inqubo yokwakheka efanelekile yanqunywa ukuhlolwa kwe-orthogonal, okungukuthi, ukugxila kwe-slurry kwakungu-2% we-HPMC kusisombululo se-ethanol esingu-70% ngesikhathi sokumbozwa, futhi isikhathi sokunyakaza phakathi ne-granulation sasiyi-15 min. Imiphumela Amaphilisi anamekwe ngefilimu ye-Jiahua alungiselelwe inqubo entsha nencwadi kadokotela athuthukiswa kakhulu ekubukekeni, isikhathi sokuhlakazeka kanye nobulukhuni obuyinhloko kunalawo akhiqizwa inqubo yencwadi kadokotela yasekuqaleni, kanye nezinga elifanelekile lamaphilisi anamekwe ngefilimu lathuthukiswa kakhulu. ifinyelele ngaphezu kwama-95%. U-Liang Meiyi, uLu Xiaohui, njll. baphinde basebenzisa i-hydroxypropyl methylcellulose njengento yokwakha ifilimu ukuze balungise ithebhulethi yokubeka i-patinae colon kanye ne-matrine colon positioning tablet, ngokulandelana. kuthinte ukukhululwa kwezidakamizwa. U-Huang Yunran walungisa amaphilisi e-Dragon's Blood Colon Positioning, futhi wasebenzisa i-HPMC esixazululweni sokumboza ungqimba oluvuvukalayo, futhi ingxenyenamba yayo enkulu yayingu-5%. Kungabonakala ukuthi i-HPMC ingasetshenziswa kabanzi ohlelweni lokulethwa kwezidakamizwa oluqondiswe kukholoni.
I-Hydroxypropyl methylcellulose ayiyona nje into enhle kakhulu yokuhlanganisa ifilimu, kodwa futhi ingasetshenziswa njengezinto zokwakha ifilimu ekwakhiweni kwefilimu. I-Wang Tongshun njll. ithuthukiswe ekubhalweni kwe-compound zinc licorice kanye nefilimu eyinhlanganisela ye-aminolexanol yomlomo, enokuguquguquka, ukufana, ukushelela, ukucaca kwe-ejenti yefilimu njengenkomba yophenyo, thola incwadi kadokotela engu-PVA 6.5 g, HPMC 0.1 g kanye no-6.0 g we i-propylene glycol ihlangabezana nezidingo zokukhululwa kancane nokuphepha, futhi ingasetshenziswa njengendlela yokulungiselela ukubhaliswa kwefilimu ehlanganisiwe.
3.2 njenge-binder kanye ne-disintegrant
Ibanga eliphansi le-viscosity yalo mkhiqizo lingasetshenziswa njenge-binder kanye ne-disintegrant yamaphilisi, amaphilisi nama-granules, futhi izinga le-viscosity eliphezulu lingasetshenziswa kuphela njenge-binder. Umthamo uyahlukahluka ngamamodeli ahlukene kanye nezidingo. Ngokuvamile, umthamo we-binder wamaphilisi e-granulation owomile ngu-5%, kanti umthamo we-binder kumaphilisi we-granulation omanzi ngu-2%.
U-Li Houtao et al bahlole i-binder yamaphilisi e-tinidazole. I-8% polyvinylpyrrolidone (PVP-K30), 40% isiraphu, 10% isitashi slurry, 2.0% i-hydroxypropyl methylcellulose K4 (HPMCK4M), 50% ethanol yaphenywa njengokunamathela kwamaphilisi e-tinidazole ngokushintshana. ukulungiswa kwamaphilisi e-tinidazole. Ukushintsha kokubukeka kwamaphilisi angenalutho kanye nangemuva kokumbozwa kwaqhathaniswa, futhi ukuqina, ukuqina, umkhawulo wesikhathi sokuhlakazeka kanye nezinga lokuqedwa kwamaphilisi kadokotela ahlukene kukalwa. Imiphumela Amaphilisi alungiswe ngo-2.0% we-hydroxypropyl methylcellulose abecwebezela, futhi ukukalwa kokuqina kwe-friability akutholanga ukwenzeka kwe-cripping ne-corning, futhi ngemva kokumbozwa, umumo wethebhulethi wawuphelele futhi nokubukeka kwakukuhle. Ngakho-ke, amaphilisi e-tinidazole alungiswe ne-2.0% HPMC-K4 kanye ne-ethanol engu-50% njengezibophezelo asetshenzisiwe. U-Guan Shihai wafunda inqubo yokwenziwa kwama-Fuganning Tablets, wahlola izinto ezinamathelayo, futhi wahlola u-50% we-ethanol, u-15% wokunamathisela isitashi, u-10% we-PVP kanye no-50% wezixazululo ze-ethanol ezinokucindezelwa, ukushelela, kanye nokuqina njengezinkomba zokuhlola. , 5% CMC-Na kanye nesixazululo se-HPMC esingu-15% (5 mPa s). Imiphumela Amashidi alungiswe nge-ethanol engu-50%, 15% yokunamathisela isitashi, 10% i-PVP 50% isixazululo se-ethanol kanye no-5% we-CMC-Na ayenobuso obushelelezi, kodwa ukucindezelwa okubi kanye nobulukhuni obuphansi, obungakwazi ukuhlangabezana nezidingo zokumboza; Isixazululo se-HPMC esingu-15% ( 5 mPa·s), ingaphezulu lethebhulethi libushelelezi, i-friability ifanelekile, futhi ukucindezelwa kuhle, okungahlangabezana nezidingo zokugqoka. Ngakho-ke, i-HPMC ( 5 mPa s) yakhethwa njenge-adhesive.
3.3 njenge-ejenti emisiwe
Ibanga le-viscosity ephezulu yalo mkhiqizo lisetshenziswa njenge-ejenti yokumisa ukuze kulungiswe uketshezi lohlobo lokumiswa. Inomphumela omuhle wokumisa, kulula ukuyihlakaza, ayinamatheli odongeni, futhi inezinhlayiya ezinhle ze-flocculation. Umthamo ojwayelekile ngu-0.5% kuya ku-1.5%. Ingoma Tian et al. kusetshenziswa izinto ezisetshenziswa kakhulu ze-polymer (i-hydroxypropyl methylcellulose, i-sodium carboxymethylcellulose, i-povidone, i-xanthan gum, i-methylcellulose, njll.) njengama-ejenti amisiwe ukuze alungiselele i-racecadotril. ukumiswa okomile. Ngokusebenzisa isilinganiso sevolumu ye-sedimentation yokumiswa okuhlukene, inkomba ye-redispersibility, kanye ne-rheology, i-viscosity yokumiswa kanye ne-microscopic morphology yabonwa, kanye nokuzinza kwezinhlayiya zezidakamizwa ngaphansi kokuhlolwa okusheshisa futhi kwaphenywa. Imiphumela Ukumiswa okomile okulungiselelwe nge-2% HPMC njengoba i-ejenti elengayo ibe nenqubo elula nokuzinza okuhle.
Uma kuqhathaniswa ne-methyl cellulose, i-hydroxypropyl methyl cellulose inezici zokwenza isixazululo esicacile, futhi kukhona kuphela inani elincane kakhulu lezinto ezingahlakazekile ze-fibrous, ngakho-ke i-HPMC nayo ivame ukusetshenziswa njenge-ejenti yokumisa ekulungiseleleni amehlo. U-Liu Jie et al. kusetshenziswe i-HPMC, i-hydroxypropyl cellulose (HPC), i-carbomer 940, i-polyethylene glycol (PEG), i-sodium hyaluronate (HA) kanye nenhlanganisela ye-HA/HPMC njengama-ejenti amisiwe ukuze kulungiswe imininingwane ehlukene Ye-Ciclovir ophthalmic suspension, i-sedimentation volume ratio, usayizi wezinhlayiyana kanye nokuhlakazeka kabusha. zikhethwa njengezinkomba zokuhlola ukuze kuhlolwe i-ejenti yokumisa isikhashana engcono kakhulu. Imiphumela ibonisa ukuthi i-acyclovir ophthalmic suspension elungiselelwe ngu-0.05% HA kanye no-0.05% HPMC njenge-ejenti yokumisa, isilinganiso sevolumu ye-sedimentation singu-0.998, usayizi wezinhlayiyana ufana, i-redispersibility yinhle, futhi ukulungiswa kuzinzile Ubulili buyanda.
3.4 Njengesivimbeli, i-ejenti ekhulula kancane futhi elawulwayo kanye ne-ejenti eyenza izimbotshana
Ibanga le-viscosity ephezulu yalo mkhiqizo lisetshenziselwa ukulungiswa kwamaphilisi e-hydrophilic gel matrix akhishwa ngokuqhubekayo, ama-blockers nama-ejenti akhishwa okulawulwayo amaphilisi e-mixed-material matrix akhululwa ngokuqhubekayo, futhi anomphumela wokubambezela ukukhululwa kwezidakamizwa. Ukugxila kwayo ku-10% kuya ku-80%. Amabanga ane-viscosity ephansi asetshenziswa njengama-porogens okulungiselelwa ukukhishwa okuqhubekayo noma ukukhishwa okulawulwayo. Umthamo wokuqala odingekayo ukuze uthole umphumela wokwelapha wamaphilisi anjalo ungafinyelelwa ngokushesha, bese kuba umphumela wokukhululwa okuqhubekayo noma olawulwayo, futhi ukugxila kwezidakamizwa egazini kugcinwa emzimbeni. . IHydroxypropyl methylcellulose ifakwa emanzini ukuze yakhe ungqimba lwejeli lapho ihlangana namanzi. Indlela yokukhishwa kwezidakamizwa kuthebhulethi ye-matrix ikakhulukazi ihlanganisa ukusakazeka kongqimba lwejeli kanye nokuguguleka kongqimba lwejeli. U-Jung Bo Shim et al ulungiselele amaphilisi e-carvedilol akhishwa ngokuqhubekayo nge-HPMC njengento ekhishwa njalo.
IHydroxypropyl methylcellulose iphinde isetshenziswe kabanzi kumaphilisi e-matrix akhishwa njalo emithi yendabuko yamaShayina, futhi iningi lezithako ezisebenzayo, izingxenye ezisebenzayo kanye namalungiselelo okukodwa omuthi wendabuko waseShayina asetshenziswa. U-Liu Wen et al. wasebenzisa u-15% we-hydroxypropyl methylcellulose njengento ye-matrix, u-1% we-lactose kanye no-5% we-microcrystalline cellulose njengezigcwalisi, futhi walungisa I-Jingfang Taohe Chengqi Decoction ibe amaphilisi omlomo we-matrix akhishwa okuqhubekayo. Imodeli yi-equation ye-Higuchi. Isistimu yokuqamba ifomula ilula, ukulungiswa kulula, futhi idatha yokukhishwa izinzile, ehlangabezana nezidingo ze-Chinese Pharmacopoeia. Tang Guanguang et al. wasebenzisa ama-saponins aphelele e-Astragalus njengesidakamizwa esiyimodeli, walungisa amaphilisi e-matrix e-HPMC, futhi wahlola izici ezithinta ukukhishwa kwezidakamizwa ezingxenyeni ezisebenzayo zomuthi wendabuko waseShayina kumaphilisi e-matrix e-HPMC. Imiphumela Njengoba umthamo we-HPMC ukhula, ukukhishwa kwe-astragaloside kwehla, futhi iphesenti lokukhululwa lomuthi lalinobudlelwano obucishe bube bomugqa nezinga lokuqedwa kwe-matrix. Kuthebulethi ye-matrix ye-hypromellose HPMC, kunobudlelwano obuthile phakathi kokukhishwa kwengxenye esebenzayo yomuthi wendabuko waseShayina kanye nomthamo nohlobo lwe-HPMC, futhi inqubo yokukhishwa kwe-hydrophilic chemical monomer iyafana nayo. IHydroxypropyl methylcellulose ayifanele nje kuphela izinhlanganisela ze-hydrophilic, kodwa futhi nezinto ezingezona i-hydrophilic. U-Liu Guihua usebenzise u-17% we-hydroxypropyl methylcellulose (HPMCK15M) njengento ye-matrix ekhishwa njalo, futhi walungisa amaphilisi e-matrix e-Tianshan Xuelian akhishwa ngokuqhubekayo ngendlela ye-granulation emanzi kanye nethebhulethi. Umphumela wokukhishwa okuqhubekayo wawusobala, futhi inqubo yokulungiselela yayizinzile futhi ingenzeka.
IHydroxypropyl methylcellulose ayisetshenziswa kuphela kumathebulethi e-matrix akhishwa okuqhubekayo ezithako ezisebenzayo nezingxenye ezisebenzayo zomuthi wendabuko wamaShayina, kodwa futhi asetshenziswa kakhulu nangokwengeziwe emalungiselelweni enhlanganisela yemithi yesiShayina. Wu Huichao et al. wasebenzisa i-20% ye-hydroxypropyl methyl cellulose (HPMCK4M) njengento ye-matrix, futhi wasebenzisa indlela yokucindezela eqondile ye-powder ukuze alungiselele ithebhulethi ye-Yizhi hydrophilic gel matrix engakhulula umuthi ngokuqhubekayo nangokuzinza amahora angu-12. I-Saponin Rg1, i-ginsenoside Rb1 kanye ne-Panax notoginseng saponin R1 zisetshenziswe njengezinkomba zokuhlola ukuze kuphenywe ukukhululwa kwe-in vitro, futhi isibalo sokukhishwa kwesidakamizwa safakwa ukuze kufundwe indlela yokukhishwa kwezidakamizwa. Imiphumela Indlela yokukhishwa kwezidakamizwa ihambisane nezibalo ze-kinetic ezi-oda uziro kanye nezibalo ze-Ritger-Peppas, lapho i-geniposide yakhululwa khona ngokusabalaliswa okungeyona i-Fick, kanye nezingxenye ezintathu ku-Panax notoginseng zakhishwa ukuguguleka kwamathambo.
3.5 Ingcina ye-Protective njenge-thickener ne-colloid
Uma lo mkhiqizo usetshenziswa njenge-thickener, ukugxila kwamaphesenti ajwayelekile ngu-0.45% kuya ku-1.0%. Kungase futhi kwandise ukuzinza kwe-glue ye-hydrophobic, yakha i-colloid evikelayo, ivimbele izinhlayiya ezivela ku-coalescing kanye ne-agglomerating, ngaleyo ndlela ivimbele ukwakheka kwe-sediments. Ukugxila kwayo kwamaphesenti ajwayelekile ngu-0.5% kuya ku-1.5%.
Wang Zhen et al. wasebenzisa indlela ye-L9 orthogonal yokuhlola yokuhlola ukuze aphenye inqubo yokulungiselela ikhabhoni enema ecushiwe. Izimo ezinhle kakhulu zenqubo yokunqunywa kokugcina kwekhabhoni enema ecushiwe ukusebenzisa u-0.5% we-sodium carboxymethyl cellulose kanye no-2.0% we-hydroxypropyl methylcellulose (i-HPMC iqukethe u-23.0% weqembu le-methoxyl, i-hydroxypropoxyl Base 11.6%) njenge-thickener, inqubo isiza ukuthuthukisa. ukuzinza kwekhabhoni ecushiwe yomuthi. UZhang Zhiqiang et al. yakha ijeli ye-pH ezwela i-levofloxacin hydrochloride ophthalmic elungele ukusetshenziswa enomphumela wokukhululwa okuqhubekayo, isebenzisa i-carbopol njenge-matrix yejeli kanye ne-hydroxypropyl methylcellulose njenge-ejenti ejiya. Imithi kadokotela ngokuhlola, ekugcineni ithola incwadi kadokotela i-levofloxacin hydrochloride 0.1 g, carbopol (9400) 3 g, hydroxypropyl methylcellulose (E50 LV) 20 g, i-disodium hydrogen 0.35 g, phosphoric acid 0.45 g ye-sodium chloride engu-5 ye-sodium chloride engu-5. , 0.03 g ye-ethyl paraben, namanzi engeziwe ukwenza i-100 ml. Esivivinyweni, umbhali uhlole uchungechunge lwe-hydroxypropyl methylcellulose METHOCEL lwe-Colorcon Company ngezicaciso ezihlukene (K4M, E4M, E15 LV, E50LV) ukuze kulungiswe izingqimba ezinokuqina okuhlukile, futhi umphumela wakhetha i-HPMC E50 LV njengesishuqululi. I-Thickener ye-pH-sensitive levofloxacin hydrochloride amajeli asheshayo.
3.6 njengempahla ye-capsule
Ngokuvamile, igobolondo legobolondo le-capsule lama-capsules ikakhulukazi i-gelatin. Inqubo yokukhiqiza igobolondo le-capsule ilula, kodwa kunezinkinga ezithile kanye nezimo ezifana nokuvikeleka okungalungile ngokumelene nomswakama kanye nezidakamizwa ezizwela umoya-mpilo, ukunciphisa ukuchithwa kwezidakamizwa, kanye nokulibaziseka kokuhlakazeka kwegobolondo le-capsule ngesikhathi sokugcinwa. Ngakho-ke, i-hydroxypropyl methylcellulose isetshenziswa esikhundleni se-gelatin capsules ukulungiswa kwama-capsules, okuthuthukisa ukwakheka kwe-capsule yokukhiqiza kanye nomphumela wokusetshenziswa, futhi iye yakhuthazwa kabanzi ekhaya nakwamanye amazwe.
Ukusebenzisa i-theophylline njengesidakamizwa esilawulayo, uPodczeck et al. ithole ukuthi izinga lokuqedwa kwezidakamizwa lama-capsules anamagobolondo e-hydroxypropyl methylcellulose lalilikhulu kunele-gelatin capsules. Isizathu sokuhlaziywa ukuthi ukuhlakazeka kwe-HPMC ukuhlakazeka kwayo yonke i-capsule ngesikhathi esifanayo, kuyilapho ukuhlakazeka kwe-gelatin capsule kungukuhlakazeka kwesakhiwo senethiwekhi kuqala, bese kuba ukuhlakazeka kwayo yonke i-capsule, ngakho-ke I-HPMC capsule ifaneleka kakhulu amagobolondo e-Capsule ekwakhiweni kokukhishwa ngokushesha. Chiwele et al. waphinde wathola iziphetho ezifanayo futhi waqhathanisa ukuchithwa kwe-gelatin, i-gelatin/polyethylene glycol namagobolondo e-HPMC. Imiphumela ibonise ukuthi amagobolondo e-HPMC ahlakazwa ngokushesha ngaphansi kwezimo ze-pH ezihlukene, kuyilapho ama-gelatin capsules Ithinteka kakhulu izimo ze-pH ezihlukene. Tang Yue et al. ihlole uhlobo olusha lwegobolondo le-capsule lomthamo ophansi wesidakamizwa esingenalutho esingenalutho sesistimu ye-inhaler ye-powder. Uma kuqhathaniswa negobolondo le-capsule ye-hydroxypropyl methylcellulose kanye negobolondo le-capsule ye-gelatin, ukuzinza kwegobolondo le-capsule kanye nezakhiwo ze-powder egobolondweni ngaphansi kwezimo ezihlukene zaphenywa, futhi ukuhlolwa kwe-friability kwenziwa. Imiphumela ibonisa ukuthi uma kuqhathaniswa nama-gelatin capsules, amagobolondo e-HPMC capsule angcono ekuzinzeni nasekuvikelweni kwempushana, anokumelana nomswakama okuqinile, futhi ane-friability ephansi kunamagobolondo e-gelatin capsule, ngakho-ke amagobolondo e-HPMC capsule afaneleka kakhulu kuma-Capsules for dry powder inhalation.
3.7 njenge-bioadhesive
Ubuchwepheshe be-Bioadhesion busebenzisa ama-excipient anama-polymers e-bioadhesive. Ngokunamathela ku-mucosa yezinto eziphilayo, kuthuthukisa ukuqhubeka nokuqina kokuxhumana phakathi kokulungiswa kanye ne-mucosa, ukuze umuthi ukhululwe kancane futhi uthathwe yi-mucosa ukufeza injongo yokwelashwa. Isetshenziswa kabanzi njengamanje. Ukwelashwa kwezifo ze-gastrointestinal tract, i-vagin, i-mucosa yomlomo nezinye izingxenye.
Ubuchwepheshe be-gastrointestinal bioadhesion wuhlelo olusha lokulethwa kwezidakamizwa olwakhiwe eminyakeni yamuva nje. Akwandisi nje kuphela isikhathi sokuhlala samalungiselelo ezidakamizwa emgudwini wesisu, kodwa futhi kuthuthukisa ukusebenza kokuxhumana phakathi komuthi kanye nolwelwesi lwamaseli endaweni yokumuncwa, kuguqule ukugcwala kwe-membrane yeseli, futhi kwenze ukungena komuthi kungene. amangqamuzana amancane e-epithelial emathunjini ayathuthukiswa, ngaleyo ndlela athuthukise i-bioavailability yomuthi. Wei Keda et al. ihlole incwadi kadokotela ewumgogodla wethebhulethi ngomthamo we-HPMCK4M kanye ne-Carbomer 940 njengezici zophenyo, futhi yasebenzisa idivayisi yokuzakhela yona ye-bioadhesion ukuze ikale amandla okuxebuka phakathi kwethebhulethi kanye ne-biofilm elingisiwe ngekhwalithi yamanzi esikhwameni sepulasitiki. , futhi ekugcineni ukhethe okuqukethwe kwe-HPMCK40 kanye ne-carbomer 940 ukuze kube yi-15 kanye ne-27.5 mg endaweni efanelekile kadokotela ye-NCaEBT tablet cores, ngokulandelanayo, ukulungisa ama-tablet cores e-NCaEBT, okubonisa ukuthi izinto ze-bioadhesive (njenge-hydroxypropyl methylcellulose) zinganciphisa kakhulu Ukuthuthukisa ukunamathela kokulungiswa kwezicubu.
Amalungiselelo e-oral bioadhesive nawo awuhlobo olusha lohlelo lokulethwa kwezidakamizwa olufundwe kabanzi eminyakeni yamuva. Amalungiselelo e-oral bioadhesive angakwazi ukunamathela umuthi engxenyeni ethintekile yomlomo womlomo, okungagcini nje ukwandisa isikhathi sokuhlala kwesidakamizwa ku-mucosa yomlomo, kodwa futhi ivikela i-mucosa yomlomo. Umphumela ongcono wokwelapha kanye ne-bioavailability yezidakamizwa ethuthukisiwe. UXue Xiaoyan et al. yenze kahle ukwakhiwa kwamaphilisi okunamathela omlomo we-insulin, kusetshenziswa i-apula pectin, i-chitosan, i-carbomer 934P, i-hydroxypropyl methylcellulose (HPMC K392) kanye ne-sodium alginate njengezinto ezinamathelayo ze-bioadhesive, kanye nokomisa iqhwa ukuze kulungiswe i-insulin yomlomo. Ishidi lesendlalelo esinamathelisa kabili. Ithebhulethi enamathiselwe ngomlomo ye-insulin elungiselelwe inesakhiwo esifana nesiponji esinezimbotshana, esilungele ukukhululwa kwe-insulin, futhi inesendlalelo sokuvikela se-hydrophobic, esingaqinisekisa ukukhululwa komuthi ngendlela eyodwa nokugwema ukulahleka komuthi. Hao Jifu et al. futhi yalungisa ubuhlalu obuluhlaza okwesibhakabhaka nokuphuzi okunamathelayo oral usebenzisa iglue ye-Baiji, i-HPMC kanye ne-carbomer njengezinto ezinamathelayo ze-bioadhesive.
Ezinhlelweni zokulethwa kwezidakamizwa zesitho sangasese sowesifazane, ubuchwepheshe be-bioadhesion nabo busetshenziswe kabanzi. UZhu Yuting et al. isebenzise i-carbomer (CP) ne-HPMC njengezinto zokunamathisela kanye ne-matrix ekhishwa okuqhubekayo ukuze kulungiswe amaphilisi e-clotrimazole bioadhesive ye-vaginal anezinhlanganisela ezahlukene kanye nezilinganiso, futhi akala ukunamathela kwawo, isikhathi sokunamathela kanye namaphesenti okuvuvukala endaweni yoketshezi lokwenziwa kwe-vaginal. , incwadi kadokotela efanelekile yahlolwa njenge-CP-HPMC1: 1, ishidi lokunamathisela elilungisiwe lalinokusebenza okuhle kokunamathela, futhi inqubo yayilula futhi ingenzeka.
3.8 njengejeli yesihloko
Njengokulungiswa kwe-adhesive, ijeli inochungechunge lwezinzuzo ezifana nokuphepha, ubuhle, ukuhlanza okulula, izindleko eziphansi, inqubo elula yokulungiselela, nokuhambisana okuhle nezidakamizwa. Inkomba yentuthuko. Isibonelo, ijeli ye-transdermal iyifomu elisha lomthamo elifundwe kakhulu eminyakeni yamuva. Akukwazi nje ukugwema ukucekelwa phansi kwezidakamizwa emgudwini wamathumbu futhi kunciphise ukuhlukahluka kwezidakamizwa egazini, kodwa futhi isibe enye yezinhlelo ezisebenzayo zokukhulula izidakamizwa ukunqoba imiphumela emibi yezidakamizwa. .
UZhu Jingjie et al. yafunda umphumela wamatrices ahlukene ekukhishweni kwejeli ye-scutellarin alcohol plastid in vitro, futhi yahlolwa nge-carbomer (980NF) ne-hydroxypropyl methylcellulose (HPMCK15M) njengamatrices ejeli, futhi yathola i-scutellarin elungele i-scutellarin. I-gel matrix ye-alcohol plastids. Imiphumela yokuhlola ibonisa ukuthi 1. 0% carbomer, 1. 5% carbomer, 1. 0% carbomer + 1. 0% HPMC, 1. 5% carbomer + 1. 0% HPMC as gel matrix Kokubili kufanelekile i-scutellarin alcohol plastids . Ngesikhathi sokuhlolwa, kutholwe ukuthi i-HPMC ingashintsha imodi yokukhishwa kwezidakamizwa ye-carbomer gel matrix ngokufaka i-kinetic equation yokukhululwa kwezidakamizwa, futhi i-1.0% HPMC ingathuthukisa i-matrix ye-carbomer engu-1.0% kanye ne-1.5% ye-carbomer matrix. Isizathu singase sibe ukuthi i-HPMC ikhula ngokushesha, futhi ukwanda okusheshayo esigabeni sokuqala sokuhlola kwenza igebe lamangqamuzana ejeli ye-carbomer libe likhulu, ngaleyo ndlela kusheshise izinga lokukhululwa kwezidakamizwa. UZhao Wencui et al. wasebenzisa i-carbomer-934 kanye ne-hydroxypropyl methylcellulose njengabathwali ukuze balungiselele ijeli ye-norfloxacin yamehlo. Inqubo yokulungiselela ilula futhi ingenzeka, futhi ikhwalithi ihambisana nejeli ye-ophthalmic ye-"Chinese Pharmacopoeia" (uhlelo luka-2010) Izidingo zekhwalithi.
3.9 I-precipitation inhibitor ye-self-microemulsifying system
I-Self-microemulsifying drug delivery system (SMEDDS) wuhlobo olusha lwesistimu yokulethwa kwezidakamizwa ngomlomo, okuyingxube efanayo, ezinzile futhi esobala eyakhiwe izidakamizwa, isigaba sikawoyela, i-emulsifier kanye ne-co-emulsifier. Ukwakheka kwencwadi kadokotela kulula, futhi ukuphepha nokuzinza kuhle. Ezidakamizweni ezingancibiliki kahle, izinto zokwakha ze-fiber polymer ezincibilika emanzini, njenge-HPMC, i-polyvinylpyrrolidone (PVP), njll., zivame ukungezwa ukwenza izidakamizwa zamahhala kanye nezidakamizwa ezifakwe ku-microemulsion zizuze ukuchithwa kwe-supersaturated emgudwini wesisu, ukuze ukwandisa ukunyibilika kwezidakamizwa futhi kuthuthukise i-bioavailability.
Peng Xuan et al. walungisa i-silibinin supersaturated self-emulsifying drug delivery system (S-SEDDS). I-Oxyethylene hydrogenated castor oil (Cremophor RH40), 12% caprylic capric acid polyethylene glycol glyceride (Labrasol) njenge-co-emulsifier, kanye ne-50 mg·g-1 HPMC. Ukwengeza i-HPMC ku-SSEDDS kungagcwalisa i-silibinin yamahhala ukuze incibilike ku-S-SEDDS futhi kuvimbele i-silibinin ekuqhumeni. Uma kuqhathaniswa nokwakhiwa kwe-self-microemulsion yendabuko, inani elikhulu le-surfactant livamise ukungezwa ukuze kuvinjelwe ukugoqa kwezidakamizwa okungaphelele. Ukwengezwa kwe-HPMC kungagcina ukuncibilika kwe-silibinin endaweni yokuncibilika kungashintshi, kunciphisa i-emulsification ekwakhekeni kwe-self-microemulsion. umthamo we-ejenti.
4.Isiphetho
Kungabonakala ukuthi i-HPMC isetshenziswe kabanzi ekulungiseleleni ngenxa yezakhiwo zayo ezingokomzimba, zamakhemikhali nezebhayoloji, kodwa i-HPMC iphinde ibe nokushiyeka okuningi emalungiselelweni, okufana nokwenzeka kokukhululwa kwangaphambi nangemuva kokuqhuma. methyl methacrylate) ukuthuthukisa. Ngasikhathi sinye, abanye abacwaningi baphenya ukusetshenziswa kwethiyori ye-osmotic ku-HPMC ngokulungiselela amaphilisi akhishwa njalo e-carbamazepine kanye namaphilisi okukhishwa okuqhubekayo kwe-verapamil hydrochloride ukuze aqhubeke nokutadisha indlela yawo yokukhululwa. Ngamafuphi, abacwaningi abaningi ngokwengeziwe benza umsebenzi omningi wokusetshenziswa okungcono kwe-HPMC emalungiselelweni, futhi ngokucwaninga okujulile kwezakhiwo zayo kanye nokuthuthukiswa kobuchwepheshe bokulungiselela, i-HPMC izosetshenziswa kabanzi kumafomu amasha wemithamo. kanye namafomu amasha omthamo. Ocwaningweni lwesistimu yezemithi, bese ukhuthaza ukuthuthukiswa okuqhubekayo kwekhemisi.
Isikhathi sokuthumela: Oct-08-2022