Izincwadi ezihlobene ekhaya nakwamanye amazwe ekulungiseleleni izinto ezisizayo zemithi i-hydroxypropyl methylcellulose (HPMC) eminyakeni yamuva nje zibuyekezwe, zahlaziywa futhi zafingqwa, kanye nokusetshenziswa kwayo ekulungiseleleni okuqinile, ekulungiseleleni uketshezi, ekulungiseleleni ukukhululwa okuqhubekayo nokulawulwayo, ekulungiseleleni i-capsule, e-gelatin. Izicelo zakamuva emkhakheni wezindlela ezintsha ezifana nezindlela zokunamathela kanye ne-bioadhesives. Ngenxa yomehluko wesisindo sama-molecule kanye ne-viscosity ye-HPMC, inezici kanye nokusetshenziswa kwe-emulsification, ukunamathela, ukuqina, i-viscosity ekhulayo, ukumisa, i-gelling kanye nokwenza ifilimu. Isetshenziswa kabanzi ekulungiseleleni imithi futhi izodlala indima enkulu emkhakheni wezindlela zokulungiselela. Ngocwaningo olujulile lwezakhiwo zayo kanye nokuthuthukiswa kobuchwepheshe bokwenza, i-HPMC izosetshenziswa kabanzi ocwaningweni lwezinhlobo ezintsha zemithamo kanye nezinhlelo ezintsha zokulethwa kwemithi, ngaleyo ndlela ikhuthaze ukuthuthukiswa okuqhubekayo kwezindlela.
i-hydroxypropyl methylcellulose; amalungiselelo emithi; izinto ezisizayo zemithi.
Izinto ezisetshenziswa ekhemisi azizona nje isisekelo esibalulekile sokwakheka kwamalungiselelo emithi eluhlaza, kodwa futhi zihlobene nobunzima benqubo yokulungiselela, ikhwalithi yemithi, ukuzinza, ukuphepha, izinga lokukhishwa kwemithi, indlela yokusebenza, ukusebenza kahle kwezokwelapha, kanye nokuthuthukiswa kwamafomu amasha omthamo kanye nezindlela ezintsha zokuphatha. Ukuvela kwezinto ezisetshenziswa ekhemisi ezintsha kuvame ukukhuthaza ukuthuthukiswa kwekhwalithi yokulungiselela kanye nokuthuthukiswa kwamafomu amasha omthamo. I-Hydroxypropyl methylcellulose (HPMC) ingenye yezinto ezisetshenziswa ekhemisi ezithandwa kakhulu ekhaya nakwamanye amazwe. Ngenxa yesisindo sayo sama-molecule kanye ne-viscosity yayo ehlukene, inemisebenzi yokuhlanganisa, ukubopha, ukuqina, ukuqina, ukumiswa, kanye nokunamathelisa. Izici kanye nokusetshenziswa okufana nokujiya kanye nokwakheka kwefilimu kusetshenziswa kabanzi kubuchwepheshe bemithi. Lesi sihloko sibukeza kakhulu ukusetshenziswa kwe-hydroxypropyl methylcellulose (HPMC) ekwakhiweni eminyakeni yamuva.
1.Izakhiwo eziyisisekelo ze-HPMC
I-Hydroxypropyl methyl cellulose (HPMC), ifomula yama-molecule yi-C8H15O8-(C10 H18O6) n-C8H15O8, kanti isisindo sama-molecule esihlobene singaba ngu-86 000. Lo mkhiqizo uyinto eyenziwe ngokwengxenye, eyingxenye ye-methyl kanye nengxenye ye-polyhydroxypropyl ether ye-cellulose. Ingakhiqizwa ngezindlela ezimbili: Enye ukuthi i-methyl cellulose yebanga elifanele iphathwa nge-NaOH bese isabela nge-propylene oxide ngaphansi kokushisa okuphezulu kanye nokucindezela okuphezulu. Isikhathi sokuphendula kumele sithathe isikhathi eside ngokwanele ukuvumela i-methyl kanye ne-hydroxypropyl ukuthi zakhe izibopho ze-ether. Ixhunywe endandatho ye-anhydroglucose ye-cellulose ngesimo se-cellulose, futhi ingafinyelela izinga elifunekayo; enye ukwelapha i-cotton linter noma i-wood pulp fiber nge-caustic soda, bese isabela nge-chlorinated methane kanye ne-propylene oxide ngokulandelana, bese iwucwengisisa ngokwengeziwe. , ichotshozwa ibe yimpuphu noma ama-granule amahle futhi afanayo.
Umbala walo mkhiqizo umhlophe kuya komhlophe njengobisi, awunaphunga futhi awunambitheki, futhi isimo sawo siyimpuphu egeleza kalula noma enemicu. Lo mkhiqizo ungancibilikiswa emanzini ukuze wakhe isixazululo se-colloidal esicacile kuya komhlophe njengobisi esinobuthi obuthile. Isenzakalo sokuguqulwa kwe-sol-gel singenzeka ngenxa yokushintsha kwezinga lokushisa kwesisombululo ngokugxila okuthile.
Ngenxa yomehluko kokuqukethwe kwalezi zinto ezimbili ezithatha indawo esakhiweni se-methoxy kanye ne-hydroxypropyl, kuye kwavela izinhlobo ezahlukene zemikhiqizo. Ekugxilweni okuthile, izinhlobo ezahlukene zemikhiqizo zinezici ezithile. Ngakho-ke, izinga lokushisa le-viscosity kanye ne-thermal gelation, zinezakhiwo ezahlukene futhi zingasetshenziswa ngezinhloso ezahlukene. I-Pharmacopoeia yamazwe ahlukahlukene inemithethonqubo kanye nezethulo ezahlukene kumodeli: I-European Pharmacopoeia isekelwe kumazinga ahlukahlukene e-viscosities ahlukene kanye namazinga ahlukene okushintshaniswa kwemikhiqizo ethengiswa emakethe, evezwa ngamabanga kanye nezinombolo, futhi iyunithi "yi-mPa s". E-US Pharmacopoeia, kunezinombolo ezi-4 ezingeziwe ngemuva kwegama elijwayelekile ukukhombisa okuqukethwe kanye nohlobo lwe-substituent ngayinye ye-hydroxypropyl methylcellulose, njenge-hydroxypropyl methylcellulose 2208. Izinombolo ezimbili zokuqala zimelela inani elilinganiselwe leqembu le-methoxy. Iphesenti, izinombolo ezimbili zokugcina zimelela iphesenti elilinganiselwe le-hydroxypropyl.
I-hydroxypropyl methylcellulose kaCalocan inochungechunge olu-3, okungukuthi uchungechunge lwe-E, uchungechunge lwe-F kanye nochungechunge lwe-K, uchungechunge ngalunye lunamamodeli ahlukahlukene ongakhetha kuwo. Uchungechunge lwe-E lusetshenziswa kakhulu njengezembozo zefilimu, olusetshenziselwa ukumboza ithebhulethi, ama-core ethebhulethi avaliwe; uchungechunge lwe-E, lwe-F lusetshenziswa njenge-viscosifiers kanye nama-release retarding agents okulungiselela amehlo, ama-suspending agents, ama-thickeners okulungiselela uketshezi, amaphilisi kanye nama-Binders of granules; uchungechunge lwe-K lusetshenziswa kakhulu njenge-release inhibitors kanye nezinto ze-hydrophilic gel matrix zokulungiselela ukukhululwa okuhamba kancane nokulawulwayo.
Abakhiqizi basekhaya bahlanganisa iFuzhou No. 2 Chemical Factory, iHuzhou Food and Chemical Co., Ltd., iSichuan Luzhou Pharmaceutical Accessories Factory, iHubei Jinxian Chemical Factory No. 1, iFeicheng Ruitai Fine Chemical Co., Ltd., iShandong Liaocheng Ahua Pharmaceutical Co., Ltd., izitshalo zamakhemikhali zaseXi'an Huian, njll.
2.Izinzuzo ze-HPMC
I-HPMC isibe ngesinye sezithako zemithi ezisetshenziswa kakhulu ekhaya nakwamanye amazwe, ngoba i-HPMC inezinzuzo ezinye izithako ezingenazo.
2.1 Ukuncibilika kwamanzi abandayo
Incibilika emanzini abandayo angaphansi kuka-40 ℃ noma u-70% we-ethanol, empeleni ayincibiliki emanzini ashisayo angaphezu kuka-60 ℃, kodwa ingafakwa ijeli.
2.2 Ukungasebenzi kahle kwamakhemikhali
I-HPMC uhlobo lwe-non-ionic cellulose ether, isixazululo sayo asinayo i-ionic charge futhi asihlangani nosawoti wensimbi noma ama-ionic organic compounds, ngakho-ke ezinye izinto ezisizayo azisabelani nayo ngesikhathi senqubo yokukhiqiza amalungiselelo.
2.3 Ukuqina
Izinzile kakhulu kokubili ku-acid kanye ne-alkali, futhi ingagcinwa isikhathi eside phakathi kwe-pH 3 kanye ne-11 ngaphandle kokushintsha okukhulu kwe-viscosity. Isixazululo samanzi se-HPMC sinomphumela wokulwa nokukhunta futhi sigcina ukuzinza okuhle kwe-viscosity ngesikhathi sokugcina isikhathi eside. Izinto ezisetshenziswa emithini ezisebenzisa i-HPMC zinokuqina okungcono kunezo ezisebenzisa izinto ezisetshenziswayo zendabuko (njenge-dextrin, isitashi, njll.).
2.4 Ukulungiswa Kokugoba
Izinhlobo ezahlukene ze-viscosity derivatives ze-HPMC zingaxutshwa ngezilinganiso ezahlukene, futhi i-viscosity yayo ingashintshwa ngokomthetho othile, futhi inobuhlobo obuhle obuqondile, ngakho-ke isilinganiso singakhethwa ngokwezidingo.
2.5 Ukungakwazi ukusebenza kwe-metabolic
I-HPMC ayimuncwa noma ayigaywa emzimbeni, futhi ayinikezi ukushisa, ngakho-ke iyisithako esiphephile sokulungiselela imithi. 2.6 Ukuphepha Ngokuvamile kubhekwa ukuthi i-HPMC iyinto engenabo ubuthi futhi engacasuli, isilinganiso esiphakathi esibulalayo samagundane singu-5 g·kg – 1, kanti isilinganiso esiphakathi esibulalayo samagundane singu-5. 2 g · kg – 1. Isilinganiso sansuku zonke asiyona ingozi emzimbeni womuntu.
3.Ukusetshenziswa kwe-HPMC ekwakhiweni
3.1 Njengezinto zokumboza ifilimu kanye nezinto zokwakha ifilimu
Isebenzisa i-HPMC njengento yethebhulethi embozwe ngefilimu, ithebhulethi embozwe ayinazo izinzuzo ezicacile zokufihla ukunambitheka nokubukeka uma kuqhathaniswa namathebhulethi ambozwe ngendabuko njengamathebhulethi ambozwe ngoshukela, kodwa ubulukhuni bayo, ukugoba kwayo, ukumuncwa komswakama, izinga lokuqhekeka. , ukukhuluphala kwesisindo kanye nezinye izinkomba zekhwalithi kungcono. Izinga lokuqina okuphansi kwalo mkhiqizo lisetshenziswa njengento yokugqoka ifilimu encibilikayo emanzini yamathebhulethi namaphilisi, kanti izinga lokuqina okuphezulu lisetshenziswa njengento yokugqoka ifilimu yezinhlelo ze-organic solvent, ngokuvamile ekugxilweni okungu-2% kuya ku-20%.
UZhang Jixing nabanye basebenzise indlela yobuso bomphumela ukuze bathuthukise ukwakheka kwe-premix nge-HPMC njengokugqoka ifilimu. Uma kuthathwa izinto zokwakha ifilimu i-HPMC, inani le-polyvinyl alcohol kanye ne-plasticizer polyethylene glycol njengezici zokuphenya, amandla okudonsa kanye nokuvuleka kwefilimu kanye ne-viscosity yesisombululo sokumboza ifilimu yinkomba yokuhlola, futhi ubudlelwano phakathi kwenkomba yokuhlola kanye nezici zokuhlola buchazwa yimodeli yezibalo, futhi inqubo yokwenza efanele ekugcineni iyatholakala. Ukusetshenziswa kwayo ngokulandelana yi-ejenti yokwakha 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 kwe-coating ingu-20 mPa·s, ukuvuleka kanye namandla okudonsa efilimu kufinyelele umphumela omuhle kakhulu. UZhang Yuan uthuthukise inqubo yokulungiselela, wasebenzisa i-HPMC njengesihlanganisi sokufaka esikhundleni se-starch slurry, futhi washintsha amaphilisi e-Jiahua aba amaphilisi ambozwe ngefilimu ukuze athuthukise ikhwalithi yamalungiselelo awo, athuthukise i-hygroscopicity yawo, alula ukuwafiphaza, amaphilisi axegayo, izinkinga eziqhekekile nezinye, athuthukise ukuzinza kwethebhulethi. Inqubo yokwakheka efanele yanqunywa ngokuhlolwa kwe-orthogonal, okungukuthi, ukuhlushwa kwe-slurry kwakungu-2% HPMC kusisombululo se-ethanol esingu-70% ngesikhathi sokumboza, kanti isikhathi sokuxubha ngesikhathi sokubumbana kwakungu-15 min. Imiphumela Amaphilisi ambozwe ngefilimu e-Jiahua alungiselelwe yinqubo entsha kanye nodokotela athuthukiswe kakhulu ekubukekeni, isikhathi sokuqhekeka kanye nobunzima obuphakathi kunalawo akhiqizwe yinqubo yokuqala kadokotela, futhi izinga elifanelekile lamaphilisi ambozwe ngefilimu lathuthukiswa kakhulu. Afinyelele ngaphezu kuka-95%. ULiang Meiyi, uLu Xiaohui, njll. basebenzise ne-hydroxypropyl methylcellulose njengento yokwakha ifilimu ukulungiselela ithebhulethi yokubeka ikholoni ye-patinae kanye nethebhulethi yokubeka ikholoni ye-matrine, ngokulandelana. UHuang Yunran walungisa amaphilisi okuma kwe-Dragon's Blood Colon, wabe esefaka i-HPMC esixazululweni sokumboza ungqimba lokuvuvukala, futhi ingxenye yayo yobukhulu yayingu-5%. Kungabonakala ukuthi i-HPMC ingasetshenziswa kabanzi ohlelweni lokulethwa kwemithi oluqondiswe kumathumbu amakhulu.
I-Hydroxypropyl methylcellulose akuyona nje into enhle kakhulu yokumboza ifilimu, kodwa futhi ingasetshenziswa njengento yokwakha ifilimu ekwakhiweni kwefilimu. I-Wang Tongshun njll. ilungiselelwe ngokwemiyalelo ye-compound zinc licorice kanye ne-aminolexanol oral composite film, enokuguquguquka, ukufana, ukushelela, ukucaca kwe-ejenti yefilimu njengenkomba yophenyo, ithola i-prescription engcono kakhulu yi-PVA 6.5 g, i-HPMC 0.1 g kanye ne-6.0 g ye-propylene glycol ehlangabezana nezidingo zokukhululwa kancane nokuphepha, futhi ingasetshenziswa njengemiyalelo yokulungiselela ifilimu ehlanganisiwe.
3.2 njenge-binder kanye ne-disintegrant
Izinga eliphansi le-viscosity lalo mkhiqizo lingasetshenziswa njenge-binder kanye ne-disintegrant yamaphilisi, amaphilisi kanye nama-granule, kanti izinga eliphezulu le-viscosity lingasetshenziswa kuphela njenge-binder. Umthamo uyahlukahluka kuye ngamamodeli ahlukene kanye nezidingo. Ngokuvamile, umthamo we-binder wamaphilisi e-granulation owomile ungu-5%, kanti umthamo we-binder wamaphilisi e-granulation amanzi ungu-2%.
ULi Houtao nabanye bahlole i-binder yamaphilisi e-tinidazole. I-8% polyvinylpyrrolidone (PVP-K30), isiraphu engu-40%, i-10% starch slurry, i-2.0% hydroxypropyl methylcellulose K4 (HPMCK4M), i-50% ethanol kuhlolwe njengokunamathela kwamaphilisi e-tinidazole ngokulandelana. Ukulungiswa kwamaphilisi e-tinidazole kuqhathaniswe izinguquko zokubukeka kwamaphilisi alula kanye nokugqoka ngemva kokugqoka, futhi izinga lokuqhekeka, ubulukhuni, umkhawulo wesikhathi sokuqhekeka kanye nezinga lokuqhekeka kwamaphilisi ahlukene kadokotela kwalinganiswa. Imiphumela Amaphilisi alungiselelwe nge-2.0% hydroxypropyl methylcellulose ayecwebezela, futhi ukulinganiswa kokuqhekeka akutholanga lutho oluvela emphethweni kanye nokugoba, futhi ngemva kokugqoka, isimo sethebhulethi sasiphelele futhi ukubukeka kwakukuhle. Ngakho-ke, kwasetshenziswa amaphilisi e-tinidazole alungiselelwe nge-2.0% HPMC-K4 kanye ne-50% ethanol njengezihlanganisi. UGuan Shihai wafunda inqubo yokwakheka kwamaThebhulethi e-Fuganning, wahlola izinamathiseli, wahlola izixazululo ze-ethanol ezingama-50%, i-starch paste engu-15%, i-PVP engu-10% kanye ne-ethanol engama-50% ngokucindezelwa, ukushelela, kanye nokugobeka njengezinkomba zokuhlola. , Isixazululo se-5% CMC-Na kanye ne-15% HPMC (5 mPa s). Imiphumela Amashidi alungiselelwe yi-ethanol engama-50%, i-starch paste engu-15%, isixazululo se-ethanol esingu-10% PVP esingu-50% kanye ne-5% CMC-Na ayenobuso obubushelelezi, kodwa obungacindezelwa kahle kanye nobunzima obuphansi, obungenakuhlangabezana nezidingo zokugqoka; Isixazululo se-HPMC esingu-15% (5 mPa·s), ubuso bethebhulethi bubushelelezi, ukugobeka kuyafaneleka, futhi ukugobeka kuhle, okungahlangabezana nezidingo zokugqoka. Ngakho-ke, i-HPMC (5 mPa s) yakhethwa njenge-glue.
3.3 njenge-ejenti yokumisa okwesikhashana
Izinga eliphezulu lokuthamba kwalo mkhiqizo lisetshenziswa njenge-ejenti yokumisa ukuze kulungiselelwe ukulungiswa koketshezi olufana nokumiswa. Linomphumela omuhle wokumisa, kulula ukulihlakaza kabusha, alinamatheli odongeni, futhi linezinhlayiya ezincane ze-flocculation. Umthamo ojwayelekile u-0.5% kuya ku-1.5%. USong Tian nabanye basebenzise izinto ze-polymer ezisetshenziswa kakhulu (i-hydroxypropyl methylcellulose, i-sodium carboxymethylcellulose, i-povidone, i-xanthan gum, i-methylcellulose, njll.) njengezinto zokumisa ukuze kulungiselelwe i-racecadotril. I-dry suspension. Ngesilinganiso sevolumu ye-sedimentation yokumiswa okuhlukene, inkomba yokuhlakazeka kabusha, kanye ne-rheology, i-suspension viscosity kanye ne-microscopic morphology kwabonwa, futhi ukuzinza kwezinhlayiya zemithi ngaphansi kokuhlolwa okusheshisiwe nakho kwahlolwa. Imiphumela I-dry suspension elungiselelwe nge-2% HPMC njenge-ejenti yokumisa yayinenqubo elula kanye nokuzinza okuhle.
Uma kuqhathaniswa ne-methyl cellulose, i-hydroxypropyl methyl cellulose inezici zokwakha ikhambi elicacile, futhi inani elincane kakhulu lezinto ezi-fibrous ezingahlakazeki ezikhona, ngakho-ke i-HPMC isetshenziswa kakhulu njenge-ejenti yokumisa emalungiselelweni amehlo. ULiu Jie nabanye basebenzise i-HPMC, i-hydroxypropyl cellulose (HPC), i-carbomer 940, i-polyethylene glycol (PEG), i-sodium hyaluronate (HA) kanye nokuhlanganiswa kwe-HA/HPMC njenge-ejenti yokumisa ukuze kulungiselelwe imininingwane ehlukene. Ukuze kumiswe i-Ciclovir ophthalmic, isilinganiso sevolumu ye-sedimentation, usayizi wezinhlayiya kanye nokuhlakazeka kabusha kukhethwa njengezinkomba zokuhlola ukuze kuhlolwe i-ejenti yokumisa engcono kakhulu. Imiphumela ikhombisa ukuthi ukumiswa kwe-acyclovir ophthalmic okulungiselelwe yi-0.05% HA kanye ne-0.05% HPMC njenge-ejenti yokumisa, isilinganiso sevolumu ye-sedimentation singu-0.998, usayizi wezinhlayiya uyafana, ukuhlakazeka kabusha kuhle, futhi ukulungiselela kuzinzile. Ukwanda kobulili.
3.4 Njengesivimbeli, i-ejenti yokukhulula ehamba kancane futhi elawulwayo kanye ne-ejenti yokwakha ama-pore
Izinga eliphezulu lokuthamba kwalo mkhiqizo lisetshenziselwa ukulungiselela amaphilisi e-hydrophilic gel matrix sustainable-release, ama-blocker kanye nama-controlled-release agents amaphilisi e-mixed-matrix sustainable-release, futhi anomphumela wokulibazisa ukukhishwa kwemithi. Ukuhlushwa kwawo kungu-10% kuya ku-80%. Amazinga aphansi okuthamba asetshenziswa njenge-porogens kumalungiselelo okukhululwa okuqhubekayo noma okulawulwayo. Umthamo wokuqala odingekayo kumphumela wokwelapha wamaphilisi anjalo ungafinyelelwa ngokushesha, bese kuba nomphumela wokukhululwa okuqhubekayo noma okulawulwayo, futhi ukuhlushwa kwemithi yegazi okusebenzayo kugcinwa emzimbeni. . I-Hydroxypropyl methylcellulose iyamanziswa ukuze yakhe ungqimba lwejeli lapho ihlangana namanzi. Indlela yokukhululwa kwemithi kuthebhulethi ye-matrix ihlanganisa kakhulu ukusabalala kongqimba lwejeli kanye nokuguguleka kongqimba lwejeli. UJung Bo Shim nabanye balungiselele amaphilisi e-carvedilol sustainable-release ane-HPMC njengezinto zokukhululwa okuqhubekayo.
I-Hydroxypropyl methylcellulose isetshenziswa kabanzi kumathebulethi e-matrix akhishwa njalo emithini yendabuko yaseShayina, futhi iningi lezithako ezisebenzayo, izingxenye ezisebenzayo kanye nokulungiselela okukodwa kwemithi yendabuko yaseShayina kuyasetshenziswa. ULiu Wen nabanye basebenzise i-15% hydroxypropyl methylcellulose njengento ye-matrix, i-1% lactose kanye ne-5% microcrystalline cellulose njengezigcwalisi, futhi balungisa i-Jingfang Taohe Chengqi Decoction kumathebulethi e-matrix akhishwa njalo emithini yendabuko. Imodeli iyi-equation ye-Higuchi. Uhlelo lokwakheka kwefomula lulula, ukulungiselela kulula, futhi idatha yokukhululwa izinzile, ehlangabezana nezidingo ze-Chinese Pharmacopoeia. UTang Guanguang nabanye basebenzise ama-saponins aphelele e-Astragalus njengomuthi oyisibonelo, balungisa amathebulethi e-matrix e-HPMC, futhi bahlola izici ezithinta ukukhishwa kwemithi ezingxenyeni ezisebenzayo zokwelapha zendabuko zaseShayina kumathebulethi e-matrix e-HPMC. Imiphumela Njengoba umthamo we-HPMC wanda, ukukhishwa kwe-astragaloside kwehla, futhi iphesenti lokukhululwa kwemithi lalinobuhlobo obucishe bube bushelelezi nesilinganiso sokuncibilika kwe-matrix. Kuthebhulethi ye-hypromellose HPMC matrix, kukhona ubudlelwano obuthile phakathi kokukhishwa kwengxenye esebenzayo yemithi yendabuko yaseShayina kanye nomthamo nohlobo lwe-HPMC, futhi inqubo yokukhululwa kwe-monomer yamakhemikhali e-hydrophilic ifana nayo. I-Hydroxypropyl methylcellulose ayifanele kuphela amakhemikhali e-hydrophilic, kodwa futhi nezinto ezingezona ezi-hydrophilic. ULiu Guihua usebenzise i-17% hydroxypropyl methylcellulose (HPMCK15M) njengezinto ze-matrix ezikhishwa njalo, futhi walungisa amaphilisi e-matrix ekhishwa njalo e-Tianshan Xuelian ngendlela ye-granulation emanzi kanye ne-tableting. Umphumela wokukhululwa okuqhubekayo wawusobala, futhi inqubo yokulungiselela yayizinzile futhi ingenzeka.
I-hydroxypropyl methylcellulose ayisetshenziswa kuphela kumathebulethi e-matrix akhishwa njalo ezithako ezisebenzayo kanye nezingxenye ezisebenzayo zokwelapha zendabuko zaseShayina, kodwa futhi isetshenziswa kakhulu emalungiselelweni emithi yendabuko yaseShayina. UWu Huichao nabanye basebenzise i-20% hydroxypropyl methyl cellulose (HPMCK4M) njengezinto ze-matrix, futhi basebenzise indlela yokucindezela i-powder direct ukulungisa ithebhulethi ye-Yizhi hydrophilic gel matrix engakhipha umuthi njalo nangokuzinzile amahora ayi-12. I-Saponin Rg1, i-ginsenoside Rb1 kanye ne-Panax notoginseng saponin R1 zasetshenziswa njengezinkomba zokuhlola ukuphenya ukukhishwa kwe-in vitro, futhi i-equation yokukhishwa kwemithi yafakwa ukuze kufundwe indlela yokukhishwa kwemithi. Imiphumela Indlela yokukhishwa kwemithi ivumelane ne-equation kinetic ye-zero-order kanye ne-equation ye-Ritger-Peppas, lapho i-geniposide yakhishwa khona ngokusakazwa okungeyona i-Fick, kanti izingxenye ezintathu ku-Panax notoginseng zakhishwa ngokuguguleka kwamathambo.
3.5 Iglue evikelayo njenge-thickener kanye ne-colloid
Uma lo mkhiqizo usetshenziswa njengesithambisi, ukuhlushwa okujwayelekile kwephesenti kungu-0.45% kuya ku-1.0%. Kungakhulisa futhi ukuzinza kweglue engangenisi amanzi, kwakha i-colloid evikelayo, kuvimbele izinhlayiya ukuthi zingahlangani futhi zihlangane, ngaleyo ndlela kuvimbele ukwakheka kwezinsalela. Ukuhlushwa kwayo okujwayelekile kwephesenti kungu-0.5% kuya ku-1.5%.
UWang Zhen nabanye basebenzise indlela yokuklama yokuhlola ye-L9 orthogonal ukuze bahlole inqubo yokulungiselela i-enema ye-carbon activated medical. Izimo zenqubo ezifanele kakhulu zokunqunywa kokugcina kwe-enema ye-carbon activated medical ukusebenzisa i-0.5% sodium carboxymethyl cellulose kanye ne-2.0% hydroxypropyl methylcellulose (i-HPMC iqukethe iqembu le-methoxyl elingu-23.0%, i-hydroxypropoxyl Base 11.6%) njengesithako esijiyile, izimo zenqubo zisiza ukuthuthukisa ukuzinza kwe-carbon activated medical. UZhang Zhiqiang nabanye bathuthukise ijeli ye-levofloxacin hydrochloride ophthalmic ekulungele ukusetshenziswa ene-pH enomphumela wokukhululwa okuqhubekayo, besebenzisa i-carbopol njenge-gel matrix kanye ne-hydroxypropyl methylcellulose njenge-ejenti yokujiyile. Ukuhlolwa okuhle kakhulu, ekugcineni kuthola ukunikezwa okungcono kakhulu yi-levofloxacin hydrochloride 0.1 g, i-carbopol (9400) 3 g, i-hydroxypropyl methylcellulose (E50 LV) 20 g, i-disodium hydrogen phosphate 0.35 g, i-phosphoric acid 0.45 g ye-sodium dihydrogen, i-0.50 g ye-sodium chloride, i-0.03 g ye-ethyl paraben, kanye namanzi angeziwe ukwenza i-100 mL. Ekuhlolweni, umbhali uhlole uchungechunge lwe-hydroxypropyl methylcellulose METHOCEL lwe-Colorcon Company ngezincazelo ezahlukene (K4M, E4M, E15 LV, E50LV) ukulungiselela izithisi ezinamazinga ahlukene, futhi umphumela wakhetha i-HPMC E50 LV njengesithisi. Isithisi samajeli asheshayo e-levofloxacin hydrochloride azwela i-pH.
3.6 njengezinto ze-capsule
Ngokuvamile, izinto zegobolondo le-capsule zama-capsule ziyi-gelatin ikakhulukazi. Inqubo yokukhiqiza igobolondo le-capsule ilula, kodwa kunezinkinga ezithile kanye nezimo ezifana nokuvikelwa okungekuhle emithini yomswakama kanye nemithi ezwela umoya-mpilo, ukunciphisa ukuncibilika kwemithi, kanye nokuwohloka okulibazisekile kwegobolondo le-capsule ngesikhathi sokugcina. Ngakho-ke, i-hydroxypropyl methylcellulose isetshenziswa esikhundleni sama-capsule e-gelatin ekulungiseleleni ama-capsule, okuthuthukisa ukwakheka kokukhiqiza i-capsule kanye nomphumela wokusetshenziswa, futhi ikhuthazwe kabanzi ekhaya nakwamanye amazwe.
Besebenzisa i-theophylline njengomuthi wokulawula, uPodczeck nabanye bathole ukuthi izinga lokuncibilika komuthi wama-capsule anamagobolondo e-hydroxypropyl methylcellulose lalilikhulu kunelama-capsule e-gelatin. Isizathu sokuhlaziywa ukuthi ukuncibilika kwe-HPMC kuwukuncibilika kwe-capsule yonke ngesikhathi esisodwa, kuyilapho ukuncibilika kwe-capsule ye-gelatin kuwukuncibilika kwesakhiwo senethiwekhi kuqala, bese kuba ukuncibilika kwe-capsule yonke, ngakho-ke i-capsule ye-HPMC ifaneleka kakhulu kumagobolondo e-Capsule ukuze kukhiqizwe ngokushesha. UChiwele nabanye bathole neziphetho ezifanayo futhi baqhathanisa ukuncibilika kwe-gelatin, i-gelatin/polyethylene glycol namagobolondo e-HPMC. Imiphumela ikhombisile ukuthi amagobolondo e-HPMC ancibilika ngokushesha ngaphansi kwezimo ezahlukene ze-pH, kuyilapho ama-capsule e-gelatin ethintwa kakhulu yizimo ezahlukene ze-pH. UTang Yue nabanye bahlole uhlobo olusha lwegobolondo le-capsule lohlelo lokuthwala i-inhaler yesidakamizwa esingenalutho oluphansi. Uma kuqhathaniswa negobolondo le-capsule le-hydroxypropyl methylcellulose kanye negobolondo le-capsule le-gelatin, kuhlolwe ukuqina kwegobolondo le-capsule kanye nezakhiwo zempuphu egobolondo ngaphansi kwezimo ezahlukene, futhi kwenziwa ukuhlolwa kokugobeka. Imiphumela ikhombisa ukuthi uma kuqhathaniswa nama-capsule e-gelatin, amagobolondo e-capsule e-HPMC angcono ekuqineni nasekuvikeleni i-powder, anokumelana okunamandla komswakama, futhi anokugobeka okuphansi kunemagobolondo e-capsule e-gelatin, ngakho-ke amagobolondo e-capsule e-HPMC afaneleka kakhulu kuma-Capsule ukuze kuhogelwe i-dry powder.
3.7 njengesinamathelisi sezinto eziphilayo
Ubuchwepheshe bokunamathela kwe-bioadhesion busebenzisa izinto ezisizayo ezinama-polymers anamathelayo. Ngokunamathela ku-mucosa yezinto eziphilayo, kuthuthukisa ukuqhubeka nokuqina kokuxhumana phakathi kokulungiselela kanye ne-mucosa, ukuze umuthi ukhishwe kancane kancane futhi umuncwe yi-mucosa ukuze kufezwe injongo yokwelashwa. Usetshenziswa kabanzi njengamanje. Ukwelashwa kwezifo zomgudu wokugaya ukudla, isitho sangasese sowesifazane, i-mucosa yomlomo nezinye izingxenye.
Ubuchwepheshe bokunamathela esiswini buyindlela entsha yokulethwa kwemithi ethuthukiswe eminyakeni yamuva nje. Akugcini nje ngokwandisa isikhathi sokuhlala kwamalungiselelo emithi endleleni yokugaya ukudla, kodwa futhi kuthuthukisa ukusebenza kokuxhumana phakathi komuthi kanye nolwelwesi lweseli endaweni yokumunca, kushintsha ukugeleza kolwelwesi lweseli, futhi kwenza ukungena komuthi kumaseli amancane e-epithelial emathunjini kuthuthukiswe, ngaleyo ndlela kuthuthukiswe ukutholakala komuthi. UWei Keda nabanye bahlole umuthi oyinhloko wethebhulethi ngomthamo we-HPMCK4M kanye ne-Carbomer 940 njengezinto zokucwaninga, futhi basebenzise idivayisi yokunamathela eyenziwe ngokwabo ukukala amandla okuxebuka phakathi kwethebhulethi kanye ne-biofilm elingisiwe ngekhwalithi yamanzi esikhwameni sepulasitiki. , futhi ekugcineni ngikhethe okuqukethwe yi-HPMCK40 kanye ne-carbomer 940 ukuthi kube yi-15 kanye ne-27.5 mg endaweni efanele yokunikezwa kwemithi yama-tablet cores e-NCaEBT, ngokulandelana, ukuze ngilungiselele ama-tablet cores e-NCaEBT, okubonisa ukuthi izinto ezinamathelayo (njenge-hydroxypropyl methylcellulose) zinganciphisa kakhulu ukunamathela komuthi ezicutshini.
Amalungiselelo okunamathela ngomlomo nawo awuhlobo olusha lohlelo lokulethwa kwemithi oluye lwafundwa kakhulu eminyakeni yamuva. Amalungiselelo okunamathela ngomlomo anganamathela umuthi engxenyeni ethintekile yomlomo, okungagcini nje ngokwandisa isikhathi sokuhlala komuthi ku-mucosa yomlomo, kodwa futhi kuvikela i-mucosa yomlomo. Umphumela ongcono wokwelapha kanye nokutholakala kwemithi okuthuthukisiwe. UXue Xiaoyan nabanye. bathuthukise ukwakheka kwamaphilisi okunamathela ngomlomo e-insulin, besebenzisa i-apple pectin, i-chitosan, i-carbomer 934P, i-hydroxypropyl methylcellulose (HPMC K392) kanye ne-sodium alginate njengezinto zokunamathela ezinamathelayo, kanye nokomisa ngeqhwa ukulungiselela i-insulin yomlomo. Ishidi lokunamathela eliphindwe kabili elinamathelayo. Ithebhulethi lokunamathela ngomlomo le-insulin elilungiselelwe linesakhiwo esifana nesiponji esinezimbobo, esilungele ukukhishwa kwe-insulin, futhi linesendlalelo sokuvikela esingapholi, esingaqinisekisa ukukhishwa komuthi ohlangothini olulodwa futhi sigweme ukulahleka komuthi. UHao Jifu nabanye. Baphinde balungisa ama-patches okunamathela ngomlomo aluhlaza okwesibhakabhaka-ophuzi besebenzisa i-glue ye-Baiji, i-HPMC kanye ne-carbomer njengezinto zokunamathela ezinamathelayo.
Ezinhlelweni zokulethwa kwezidakamizwa zesitho sangasese sowesifazane, ubuchwepheshe bokunamathela kwe-bioadhesion busetshenziswe kabanzi. UZhu Yuting nabanye basebenzise i-carbomer (CP) kanye ne-HPMC njengezinto zokunamathela kanye ne-sustained-release matrix ukulungiselela amaphilisi esitho sangasese sowesifazane e-clotrimazole anamafomula nezilinganiso ezahlukene, futhi balinganisa ukunamathela kwawo, isikhathi sokunamathela kanye nephesenti lokuvuvukala endaweni yoketshezi lwesitho sangasese sowesifazane okwenziwa. , umuthi ofanele wahlolwa njenge-CP-HPMC1: 1, ishidi lokunamathela elilungisiwe lalinokusebenza okuhle kokunamathela, futhi inqubo yayilula futhi ingenzeka.
3.8 njengejeli yokugcoba
Njengomuthi wokunamathisela, ijeli inezinzuzo eziningi ezifana nokuphepha, ubuhle, ukuhlanza okulula, izindleko eziphansi, inqubo yokulungiselela elula, kanye nokuhambisana kahle nemithi. Isiqondiso sentuthuko. Isibonelo, ijeli ye-transdermal iyindlela entsha yokulinganisa eye yafundwa kakhulu eminyakeni yamuva nje. Ayikwazi nje ukugwema ukubhujiswa kwemithi endleleni yokugaya ukudla futhi inciphise ukuhlukahluka kokuhlushwa kwemithi egazini kusukela phezulu kuya emgudwini, kodwa futhi ibe enye yezinhlelo zokukhishwa kwemithi ezisebenzayo zokunqoba imiphumela emibi yemithi.
UZhu Jingjie nabanye bafunde umphumela wama-matrices ahlukene ekukhishweni kwejeli ye-scutellarin alcohol plastid in vitro, futhi bahlolwa nge-carbomer (980NF) kanye ne-hydroxypropyl methylcellulose (HPMCK15M) njenge-matrices yejeli, futhi bathola i-scutellarin efanele i-scutellarin. I-matrix yejeli yama-plastid otshwala. Imiphumela yokuhlola ikhombisa ukuthi i-1.0% carbomer, i-1.5% carbomer, i-1.0% carbomer + 1.0% HPMC, i-1.5% carbomer + 1.0% HPMC njenge-matrix yejeli. Zombili zifanele ama-plastid otshwala e-scutellarin. Ngesikhathi sokuhlola, kwatholakala ukuthi i-HPMC ingashintsha indlela yokukhishwa kwemithi ye-matrix yejeli ye-carbomer ngokufaka i-kinetic equation yokukhishwa kwemithi, kanti i-1.0% HPMC ingathuthukisa i-1.0% carbomer matrix kanye ne-1.5% carbomer matrix. Isizathu kungaba ukuthi i-HPMC ikhula ngokushesha, futhi ukwanda okusheshayo esigabeni sokuqala sokuhlola kwenza igebe lama-molecule lezinto zejeli ye-carbomer libe likhulu, ngaleyo ndlela kusheshiswe izinga lokukhishwa kwemithi. UZhao Wencui nabanye basebenzise i-carbomer-934 kanye ne-hydroxypropyl methylcellulose njengabathwali ukulungiselela ijeli ye-ophthalmic ye-norfloxacin. Inqubo yokulungiselela ilula futhi iyenzeka, futhi ikhwalithi ihambisana nejeli ye-ophthalmic ye-“Chinese Pharmacopoeia” (uhlelo luka-2010) Izidingo zekhwalithi.
3.9 Isithiyo sokuna kwemvula sesistimu yokuzihlanganisa
Uhlelo lokulethwa kwezidakamizwa oluzisebenzisayo (i-SMEDDS) luhlobo olusha lohlelo lokulethwa kwezidakamizwa ngomlomo, oluyingxube efanayo, ezinzile futhi esobala eyakhiwe umuthi, isigaba samafutha, i-emulsifier kanye ne-co-emulsifier. Ukwakheka komuthi kulula, futhi ukuphepha nokuzinza kuhle. Emithini engancibiliki kahle, izinto ze-polymer ze-fiber ezincibilika emanzini, njenge-HPMC, i-polyvinylpyrrolidone (PVP), njll., zivame ukungezwa ukuze kwenziwe imithi yamahhala kanye nemithi efakwe ku-microemulsion ifinyelele ukuncibilika okugcwele emgodini wokugaya ukudla, ukuze kwandiswe ukuncibilika komuthi futhi kuthuthukiswe ukutholakala kwawo.
UPeng Xuan nabanye balungiselele uhlelo lokulethwa kwezidakamizwa oluzihlanganisayo oluyi-silibinin supersaturated self-emulsifying (S-SEDDS). Uwoyela we-castor o-oxyethylene hydrogenated (Cremophor RH40), i-caprylic capric acid polyethylene glycol glyceride (Labrasol) engu-12% 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 ukuthi ingangeni. Uma kuqhathaniswa nezindlela zendabuko zokuzihlanganisa, inani elikhulu le-surfactant livame ukungezwa ukuvimbela ukufakwa kwezidakamizwa okungaphelele. Ukwengezwa kwe-HPMC kungagcina ukuncibilika kwe-silibinin endaweni yokuncibilika kungaguquguquki, kunciphisa i-emulsification kuzindlela zokuzihlanganisa ezizihlanganisayo.
4. Isiphetho
Kungabonakala ukuthi i-HPMC isetshenziswe kabanzi ekulungiseleleni ngenxa yezakhiwo zayo zomzimba, zamakhemikhali kanye nezasebhayoloji, kodwa i-HPMC inezinkinga eziningi ekulungiseleleni, njengokwenzeka kokukhululwa kwangaphambi nangemuva kokuqhuma. Ngesikhathi esifanayo, abanye abacwaningi baphenye ukusetshenziswa kwethiyori ye-osmotic ku-HPMC ngokulungiselela amaphilisi e-carbamazepine akhululwayo kanye namaphilisi e-verapamil hydrochloride akhululwayo ukuze baqhubeke nokufunda indlela yayo yokukhululwa. Ngamafuphi, abacwaningi abaningi benza umsebenzi omningi wokusetshenziswa okungcono kwe-HPMC ekulungiseleleni, futhi ngokutadisha okujulile kwezakhiwo zayo kanye nokuthuthukiswa kobuchwepheshe bokulungiselela, i-HPMC izosetshenziswa kabanzi ezinhlotsheni ezintsha zemithamo kanye namafomu amasha emithamo. Ocwaningweni lwesistimu yemithi, bese kuthuthukiswa intuthuko eqhubekayo yekhemisi.
Isikhathi sokuthunyelwe: Okthoba-08-2022