Littattafan da suka danganci gida da waje a cikin shirye-shiryen magunguna na hydroxypropyl methylcellulose (HPMC) a cikin 'yan shekarun nan an sake nazarin su, an bincika su kuma an taƙaita su, da aikace-aikacen sa a cikin shirye-shirye masu ƙarfi, shirye-shiryen ruwa, ci gaba da sarrafa shirye-shiryen saki, shirye-shiryen capsule, gelatin The latest aikace-aikace a cikin filin na sabon formulations kamar biodhesive formulations. Saboda da bambanci a cikin zumunta kwayoyin nauyi da danko na HPMC, yana da halaye da kuma amfani da emulsification, mannewa, thickening, danko karuwa, suspending, gelling da kuma film-forming. Ana amfani da shi sosai a cikin shirye-shiryen magunguna kuma zai taka rawa sosai a fagen shirye-shirye. Tare da zurfin binciken kadarorinta da haɓaka fasahar samarwa, za a yi amfani da HPMC sosai a cikin binciken sabbin abubuwa masu magani, don inganta cigaban ci gaba na tsari.
hydroxypropyl methylcellulose; shirye-shiryen magunguna; magungunan magunguna.
Pharmaceutical excipients ne ba kawai kayan tushe ga samuwar raw miyagun ƙwayoyi shirye-shirye, amma kuma alaka da wahala daga cikin shiri tsari, miyagun ƙwayoyi ingancin, da kwanciyar hankali, aminci, miyagun ƙwayoyi saki kudi, yanayin aiki, asibiti inganci, da kuma ci gaban da sabon sashi siffofin da kuma sabon hanyoyin da gudanarwa. dangantaka ta kusa. Fitowar sabbin kayan aikin magunguna sau da yawa yana haɓaka haɓaka ingancin shirye-shiryen da haɓaka sabbin nau'ikan nau'ikan. Hydroxypropyl methylcellulose (HPMC) yana ɗaya daga cikin mashahuran kayan aikin magunguna a gida da waje. Saboda nau'in nau'in kwayoyin halitta daban-daban da danko, yana da ayyuka na emulsifying, dauri, kauri, kauri, dakatarwa, da mannawa. Abubuwan da ake amfani da su kamar su coagulation da ƙirƙirar fim ana amfani da su sosai a cikin fasahar magunguna. Wannan labarin yafi yin bitar aikace-aikacen hydroxypropyl methylcellulose (HPMC) a cikin ƙira a cikin 'yan shekarun nan.
1.Abubuwan asali na HPMC
Hydroxypropyl methyl cellulose (HPMC), da kwayoyin dabara ne C8H15O8-(C10 H18O6) n-C8H15O8, da kuma zumunta kwayoyin taro ne game da 86 000. Wannan samfurin ne Semi-Synthetic abu, wanda shi ne wani ɓangare na methyl da wani ɓangare na polyhydroxypropyl ether na cellulose. Ana iya samar da shi ta hanyoyi biyu: Daya shine methyl cellulose na matsayi mai dacewa ana bi da shi tare da NaOH sannan kuma a mayar da shi tare da propylene oxide a ƙarƙashin matsanancin zafi da matsa lamba. Dole ne lokacin amsawa ya daɗe don ba da damar methyl da hydroxypropyl su samar da ether bonds An haɗa shi da zoben anhydroglucose na cellulose a cikin nau'in cellulose, kuma zai iya kaiwa matakin da ake so; ɗayan kuma shine a yi maganin linter ɗin auduga ko itacen ɓangarorin itace tare da caustic soda, sannan a mayar da martani da methane mai chlorinated da propylene oxide a jere, sannan a ƙara tace shi. , niƙa a cikin lafiya da kuma uniform foda ko granules.
Launin wannan samfurin fari ne zuwa fari mai madara, mara wari kuma maras ɗanɗano ne, kuma sigar ta granular ko fibrous foda mai sauƙin gudu. Ana iya narkar da wannan samfurin a cikin ruwa don samar da bayani mai haske zuwa farin colloidal tare da wani ɗanko. Alamar sol-gel interconversion na iya faruwa saboda canjin yanayin zafi na maganin tare da wani taro.
Saboda bambancin abun ciki na waɗannan maye biyu a cikin tsarin methoxy da hydroxypropyl, nau'ikan samfurori sun bayyana. A cikin ƙayyadaddun ƙididdiga, nau'ikan samfuran daban-daban suna da takamaiman halaye. Danko da zafin jiki na thermal, don haka suna da kaddarorin daban-daban kuma ana iya amfani da su don dalilai daban-daban. Pharmacopoeia na kasashe daban-daban yana da ka'idoji daban-daban da wakilci akan samfurin: Pharmacopoeia na Turai yana dogara ne akan nau'ikan nau'ikan nau'ikan viscosities daban-daban da digiri daban-daban na maye gurbin samfuran da aka sayar a kasuwa, wanda aka bayyana ta maki da lambobi, kuma sashin shine "mPa s". A cikin Pharmacopoeia na Amurka, ana ƙara lambobi 4 bayan sunan gabaɗaya don nuna abun ciki da nau'in kowane madadin hydroxypropyl methylcellulose, kamar hydroxypropyl methylcellulose 2208. Lambobi biyu na farko suna wakiltar ƙimar ƙimar ƙungiyar methoxy. Kashi, lambobi biyu na ƙarshe suna wakiltar kusan kashi na hydroxypropyl.
Calocan's hydroxypropyl methylcellulose yana da jerin 3, wato jerin E, jerin F da jerin K, kowane jerin yana da nau'ikan nau'ikan da za a zaɓa daga. E jerin galibi ana amfani da su azaman suturar fina-finai, ana amfani da su don suturar kwamfutar hannu, rufaffiyar kwamfutar hannu; E, F jerin ana amfani da su a matsayin viscosifiers da saki retarding jamiái don ophthalmic shirye-shirye, suspending jamiái, thickeners ga ruwa shirye-shirye, Allunan da Binders na granules; Ana amfani da jerin K galibi azaman masu hanawa saki da kayan gel matrix na hydrophilic don jinkirin shirye-shiryen sakin sarrafawa.
Masana'antun cikin gida sun hada da Fuzhou No. 2 Chemical Factory, Huzhou Food and Chemical Co., Ltd., Sichuan Luzhou Pharmaceutical Na'urorin haɗi Factory, Hubei Jinxian Chemical Factory No. 1, Feicheng Ruitai Fine Chemical Co., Ltd., Shandong Liaocheng Ahua Co., Ltd. sinadaran da sauransu.
2.Amfanin HPMC
HPMC ya zama daya daga cikin abubuwan da aka fi amfani da su a cikin gida da waje, saboda HPMC yana da fa'idar da sauran kayan aikin ba su da shi.
2.1 Ruwa mai sanyi
Mai narkewa a cikin ruwan sanyi ƙasa 40 ℃ ko 70% ethanol, m insoluble a cikin ruwan zafi sama da 60 ℃, amma iya gel.
2.2 Kemikal rashin aiki
HPMC wani nau'in ether ne wanda ba shi da ionic cellulose, maganinsa ba shi da cajin ionic kuma baya hulɗa tare da gishiri na ƙarfe ko mahaɗin kwayoyin ionic, don haka sauran abubuwan haɓaka ba sa amsawa tare da shi yayin aiwatar da shirye-shirye.
2.3 Kwanciyar hankali
Yana da ingantacciyar kwanciyar hankali ga duka acid da alkali, kuma ana iya adana shi na dogon lokaci tsakanin pH 3 da 11 ba tare da babban canji a cikin danko ba. Maganin ruwa mai ruwa na HPMC yana da tasirin anti-mildew kuma yana kula da kwanciyar hankali mai kyau yayin ajiya na dogon lokaci. Abubuwan da ake amfani da magunguna masu amfani da HPMC suna da ingantacciyar kwanciyar hankali fiye da waɗanda ke amfani da abubuwan haɓaka na gargajiya (kamar dextrin, sitaci, da sauransu).
2.4 Daidaitawar Danko
Ana iya haɗa nau'o'in danko daban-daban na HPMC a cikin nau'i daban-daban, kuma ana iya canza danko bisa ga wata doka, kuma yana da dangantaka mai kyau na linzamin kwamfuta, don haka za'a iya zaɓar rabo bisa ga bukatun.
2.5 Rashin rashin kuzari
HPMC ba a tunawa ko metabolized a cikin jiki, kuma baya samar da zafi, don haka yana da aminci shirye-shiryen magunguna. 2.6 Tsaro An yi la'akari da cewa HPMC abu ne marar guba kuma maras ban sha'awa, matsakaicin kisa ga mice shine 5 g · kg - 1 , kuma matsakaicin matsakaici na berayen shine 5. 2 g · kg - 1 . Adadin yau da kullun ba shi da lahani ga jikin ɗan adam.
3.Aikace-aikacen HPMC a cikin tsari
3.1 Kamar yadda kayan shafa fim da kayan aikin fim
Yin amfani da HPMC azaman kayan kwamfutar hannu mai rufi na fim, kwamfutar hannu mai rufi ba ta da fa'ida a bayyane wajen rufe dandano da bayyanar idan aka kwatanta da allunan da aka lulluɓe na gargajiya kamar allunan da aka yi da sukari, amma taurin sa, friability, ɗaukar danshi, digiri na tarwatsewa. , Rufe nauyi riba da sauran ingancin Manuniya ne mafi alhẽri. Ana amfani da ƙananan ƙarancin danko na wannan samfurin azaman kayan shafa na ruwa mai narkewa don allunan da kwayoyi, kuma ana amfani da madaidaicin madaidaicin azaman kayan shafa na fim don tsarin narkewar ƙwayoyin cuta, yawanci a matakin 2% zuwa 20%.
Zhang Jixing et al. yayi amfani da hanyar tasirin tasiri don haɓaka ƙirar ƙira tare da HPMC azaman murfin fim. Ɗaukar da fim-kafa abu HPMC, adadin polyvinyl barasa da kuma plasticizer polyethylene glycol a matsayin bincike dalilai, da tensile ƙarfi da permeability na fim da The danko na fim shafi bayani ne dubawa index, da kuma dangantaka tsakanin dubawa index da dubawa dalilai aka bayyana ta hanyar wani ilmin lissafi model, da kuma a karshe samu tsari. Its amfani ne bi da bi film-forming wakili hydroxypropyl methylcellulose (HPMCE5) 11.88 g, polyvinyl barasa 24.12 g, plasticizer polyethylene glycol 13.00 g, da shafi dakatar danko ne 20 mPa · s, da permeability da tensile mafi kyaun sakamako na fim. Zhang Yuan ya inganta tsarin shirye-shiryen, ya yi amfani da HPMC a matsayin mai ɗaure don maye gurbin slurry na sitaci, kuma ya canza allunan Jiahua zuwa allunan da aka rufe da fim don inganta ingancin shirye-shiryensa, inganta yanayin tsafta, mai sauƙin bushewa, allunan sako-sako, rarrabuwa da sauran matsaloli, haɓaka kwanciyar hankali na kwamfutar hannu. Mafi kyawun tsarin ƙira an ƙaddara ta gwaje-gwajen orthogonal, wato, ƙaddamarwar slurry shine 2% HPMC a cikin maganin ethanol na 70% yayin sutura, kuma lokacin motsawa yayin granulation shine 15 min. Sakamako Allunan masu rufaffiyar fim ɗin Jiahua da sabon tsari da takardar sayan magani suka shirya sun inganta sosai a bayyanar, lokacin rarrabuwar kawuna da taurin asali fiye da waɗanda aka samar ta hanyar rubutun asali, kuma ƙimar cancantar allunan masu rufin fim ɗin sun inganta sosai. ya kai fiye da 95%. Liang Meiyi, Lu Xiaohui, da dai sauransu kuma sun yi amfani da hydroxypropyl methylcellulose a matsayin kayan shirya fim don shirya kwamfutar hannu na patinae da kuma kwamfutar hannu na matatrine, bi da bi. shafi sakin miyagun ƙwayoyi. Huang Yunran ya shirya Allunan Matsayin Jini na Macijin, kuma ya yi amfani da HPMC zuwa maganin kumburin kumburin, kuma yawan juzu'insa ya kai kashi 5%. Ana iya ganin cewa ana iya amfani da HPMC sosai a cikin tsarin isar da magunguna da aka yi niyya ga hanji.
Hydroxypropyl methylcellulose ba kawai kayan shafan fim ne mai kyau ba, amma kuma ana iya amfani da shi azaman kayan ƙirƙirar fim a cikin ƙirar fim. Wang Tongshun da dai sauransu an inganta su zuwa takardar sayan magani na fili zinc licorice da aminolexanol na baka composite film, tare da sassauci, uniformity, santsi, nuna gaskiya na fim wakili kamar yadda bincike index, samun mafi kyau duka takardar sayan magani ne PVA 6.5 g, HPMC 0.1 g da 6.0 g na propylene glycol, sadu da aminci da prescription da ake amfani da propylene glycol. na fim ɗin da aka haɗa.
3.2 a matsayin mai ɗaure da tarwatsewa
Za'a iya amfani da ƙaramin ɗanƙoƙi na wannan samfur azaman ɗaure da rarrabuwa don allunan, kwaya da granules, kuma babban ƙimar danko za'a iya amfani dashi azaman ɗaure kawai. Matsakaicin ya bambanta da samfura da buƙatu daban-daban. Gabaɗaya, adadin abin ɗaure don busassun busassun granulation shine 5%, kuma sashi na ɗaure don allunan granulation shine 2%.
Li Houtao et al sun bincika abin daure na tinidazole. 8% polyvinylpyrrolidone (PVP-K30), 40% syrup, 10% sitaci slurry, 2.0% hydroxypropyl methylcellulose K4 (HPMCK4M), 50% ethanol an bincika a matsayin manne na tinidazole Allunan bi da bi. shirye-shiryen tinidazole Allunan. Canje-canje na bayyanar allunan da aka kwatanta da kuma bayan rufewa an kwatanta, kuma an auna friability, taurin, iyakar lokacin rarrabuwar kawuna da narkar da nau'ikan allunan kwaya daban-daban. Sakamako Allunan da aka shirya ta 2.0% hydroxypropyl methylcellulose sun kasance masu sheki, kuma ma'aunin friability ɗin bai sami wani abu ba game da tsinkewa da kusurwa, kuma bayan shafi, siffar kwamfutar hannu ya cika kuma bayyanar yana da kyau. Saboda haka, allunan tinidazole da aka shirya tare da 2.0% HPMC-K4 da 50% ethanol kamar yadda aka yi amfani da su. Guan Shihai ya yi nazarin tsarin samar da allunan Fuganning, ya duba abubuwan da ake amfani da su, kuma ya duba 50% ethanol, 15% sitaci manna, 10% PVP da 50% ethanol mafita tare da matsawa, santsi, da friability a matsayin alamomin kimantawa. , 5% CMC-Na da 15% HPMC bayani (5mPa s). Sakamako A zanen gado shirya da 50% ethanol, 15% sitaci manna, 10% PVP 50% ethanol bayani da 5% CMC-Na da m surface, amma matalauta compressibility da low taurin, wanda ba zai iya saduwa da bukatun da shafi; 15% HPMC bayani (5 mPa · s), saman kwamfutar hannu yana da santsi, friability ya cancanta, kuma matsawa yana da kyau, wanda zai iya saduwa da bukatun shafi. Saboda haka, an zaɓi HPMC (5mPa s) azaman mannewa.
3.3 a matsayin wakili mai dakatarwa
Ana amfani da babban darajar wannan samfurin azaman wakili mai dakatarwa don shirya wani shiri na ruwa nau'in dakatarwa. Yana da sakamako mai kyau na dakatarwa, yana da sauƙin sakewa, baya tsayawa a bango, kuma yana da ƙwayoyin flocculation masu kyau. Matsakaicin adadin yau da kullun shine 0.5% zuwa 1.5%. Song Tian et al. ana amfani da kayan polymer da aka saba amfani da su (hydroxypropyl methylcellulose, sodium carboxymethylcellulose, povidone, xanthan danko, methylcellulose, da sauransu) azaman wakilai masu dakatarwa don shirya racecadotril. bushewar dakatarwa. Ta hanyar daɗaɗɗen ƙarar ƙwayar cuta na daban-daban suspensions, da redispersibility index, da kuma rheology, dakatar danko da microscopic ilimin halittar jiki da aka lura, da kuma kwanciyar hankali na miyagun ƙwayoyi barbashi karkashin hanzari gwaji da aka kuma bincika. Sakamakon busassun dakatarwa da aka shirya tare da 2% HPMC a matsayin wakilin dakatarwa yana da tsari mai sauƙi da kwanciyar hankali mai kyau.
Idan aka kwatanta da methyl cellulose, hydroxypropyl methyl cellulose yana da halaye na samar da mafi bayyana bayani, kuma kawai kadan adadin da ba tarwatsa fibrous abubuwa wanzu, don haka HPMC kuma yawanci amfani da suspending wakili a ido shirye-shirye. Liu Jie et al. yi amfani da HPMC, hydroxypropyl cellulose (HPC), carbomer 940, polyethylene glycol (PEG), sodium hyaluronate (HA) da kuma hade da HA / HPMC a matsayin dakatar jamiái shirya daban-daban bayani dalla-dalla Ga Ciclovir ophthalmic dakatar, sedimentation girma rabo, barbashi size da redispersibility da ake zažužžukan a matsayin mai nuna alama mafi kyau a cikin tuhuma. Sakamakon ya nuna cewa dakatarwar ophthalmic acyclovir da aka shirya ta 0.05% HA da 0.05% HPMC a matsayin wakili mai dakatarwa, ƙwayar ƙwayar cuta shine 0.998, girman ƙwayar ƙwayar cuta shine uniform, redispersibility yana da kyau, kuma shirye-shiryen shine barga jima'i yana ƙaruwa.
3.4 A matsayin mai katange, jinkirin da sarrafawa mai sarrafawa da wakili mai haifar da pore
Ana amfani da babban darajar danko na wannan samfurin don shirye-shiryen hydrophilic gel matrix dorewa-saki Allunan, blockers da sarrafawa-saki jamiái na gauraye-material matrix dore-saki Allunan, kuma yana da sakamako na jinkirta saki miyagun ƙwayoyi. Matsayinta shine 10% zuwa 80%. Ana amfani da ma'auni mai ƙarancin danko azaman porogens don dorewa-saki ko shirye-shiryen sakin sarrafawa. Matsakaicin farko da ake buƙata don tasirin warkewar irin waɗannan allunan za a iya isa da sauri, sa'an nan kuma ana aiwatar da ci gaba-saki-saki-saki-saki, kuma ana kiyaye tasirin magungunan jini mai inganci a cikin jiki. . Hydroxypropyl methylcellulose yana da ruwa don samar da gel Layer lokacin da ya hadu da ruwa. Tsarin sakin miyagun ƙwayoyi daga kwamfutar hannu na matrix ya haɗa da yaduwa na gel Layer da yashwar gel Layer. Jung Bo Shim et al da aka shirya carvedilol allunan ci gaba-saki tare da HPMC azaman kayan ci gaba mai dorewa.
Hydroxypropyl methylcellulose kuma ana amfani da shi sosai a cikin dorewa-saki matrix allunan maganin gargajiya na kasar Sin, kuma ana amfani da yawancin sinadaran aiki, sassa masu tasiri da shirye-shirye guda na magungunan gargajiya na kasar Sin. Liu Wen et al. An yi amfani da 15% hydroxypropyl methylcellulose a matsayin kayan matrix, 1% lactose da 5% microcrystalline cellulose a matsayin masu cikawa, kuma an shirya Jingfang Taohe Chengqi Decoction a cikin matrix na baka na ci gaba da sakin allunan. Samfurin shine lissafin Higuchi. Tsarin tsari na tsari yana da sauƙi, shirye-shiryen yana da sauƙi, kuma bayanan da aka saki suna da kwanciyar hankali, wanda ya dace da bukatun Pharmacopoeia na kasar Sin. Tang Guanguang et al. ya yi amfani da jimlar saponins na Astragalus a matsayin samfurin samfurin, shirya allunan matrix na HPMC, kuma sun bincika abubuwan da suka shafi sakin miyagun ƙwayoyi daga sassa masu tasiri na magungunan gargajiya na kasar Sin a cikin allunan matrix na HPMC. Sakamako Yayin da adadin HPMC ya karu, sakin astragaloside ya ragu, kuma adadin sakin maganin yana da kusan alaƙar layi tare da adadin rushewar matrix. A cikin kwamfutar hannu na hypromellose HPMC, akwai wata alaƙa tsakanin sakin ingantaccen ɓangaren magungunan gargajiya na kasar Sin da sashi da nau'in HPMC, kuma tsarin sakin nau'in sinadarai na hydrophilic monomer yana kama da shi. Hydroxypropyl methylcellulose ba kawai dace da hydrophilic mahadi, amma kuma ga wadanda ba hydrophilic abubuwa. Liu Guihua ya yi amfani da 17% hydroxypropyl methylcellulose (HPMCK15M) a matsayin kayan matrix mai dorewa, kuma ya shirya Tianshan Xuelian dorewar-saki matrix Allunan ta rigar granulation da hanyar tableting. Sakamakon ci gaba-saki a bayyane yake, kuma tsarin shirye-shiryen ya kasance karko kuma mai yuwuwa.
Hydroxypropyl methylcellulose ba wai kawai ana amfani da shi a kan allunan matrix mai dorewa na kayan aiki masu aiki da sassa masu tasiri na maganin gargajiya na kasar Sin ba, har ma ana amfani da su sosai a cikin shirye-shiryen magungunan gargajiya na kasar Sin. Wu Huichao et al. ya yi amfani da 20% hydroxypropyl methyl cellulose (HPMCK4M) a matsayin kayan matrix, kuma ya yi amfani da hanyar haɗin foda kai tsaye don shirya kwamfutar hannu na Yizhi hydrophilic gel matrix wanda zai iya sakin miyagun ƙwayoyi ci gaba da tsayayye na 12 hours. Saponin Rg1, ginsenoside Rb1 da Panax notoginseng saponin R1 an yi amfani da su azaman alamun ƙima don bincika sakin a cikin vitro, kuma an daidaita ma'auni na sakin miyagun ƙwayoyi don nazarin tsarin sakin miyagun ƙwayoyi. Sakamako Tsarin sakin miyagun ƙwayoyi ya dace da sifili-oda kinetic equation da kuma Ritger-Peppas equation, a cikin abin da geniposide aka saki da ba Fick diffusion, da uku sassa a Panax notoginseng aka saki ta kwarangwal yashwa.
3.5 Manne mai karewa azaman thickener da colloid
Lokacin da aka yi amfani da wannan samfurin azaman mai kauri, yawan adadin da aka saba shine 0.45% zuwa 1.0%. Hakanan zai iya ƙara kwanciyar hankali na manne hydrophobic, samar da colloid mai karewa, hana barbashi daga coalescing da agglomerating, don haka hana samuwar sediments. Matsakaicin kaso na gama gari shine 0.5% zuwa 1.5%.
Wang Zhen et al. ya yi amfani da hanyar ƙirar gwaji ta L9 orthogonal don bincika tsarin shirye-shiryen na maganin da ke kunna carbon enema. A ganiya tsari yanayi na karshe kayyade magani kunna carbon enema ne don amfani da 0.5% sodium carboxymethyl cellulose da 2.0% hydroxypropyl methylcellulose (HPMC ya ƙunshi 23.0% methoxyl kungiyar, hydroxypropoxyl Base 11.6%) a matsayin thickener carbon, da aiki da kwanciyar hankali da makamashi yanayi taimako. Zhang Zhiqiang et al. ɓullo da pH-m levofloxacin hydrochloride ophthalmic shirye-don-amfani gel tare da ci gaba-saki sakamako, ta amfani da carbopol a matsayin gel matrix da hydroxypropyl methylcellulose a matsayin thickening wakili. Mafi kyawun takardar sayan magani ta gwaji, a ƙarshe ya sami takardar sayan magani mafi kyau shine levofloxacin hydrochloride 0.1 g, carbopol (9400) 3 g, hydroxypropyl methylcellulose (E50 LV) 20 g, disodium hydrogen phosphate 0.35 g, phosphoric acid 0.45 g na sodium chloride 0.05 g na sodium dihydrogede. g na ethyl paraben, kuma an ƙara ruwa don yin 100 ml. A cikin gwajin, marubucin ya bincika jerin hydroxypropyl methylcellulose METHOCEL na Kamfanin Colorcon tare da ƙayyadaddun ƙayyadaddun bayanai (K4M, E4M, E15 LV, E50LV) don shirya masu kauri da yawa daban-daban, kuma sakamakon ya zaɓi HPMC E50 LV a matsayin mai kauri. Thickener don pH-m levofloxacin hydrochloride gels nan take.
3.6 a matsayin capsule abu
Yawancin lokaci, capsule harsashi abu na capsules ne yafi gelatin. Tsarin samar da harsashi na capsule abu ne mai sauki, amma akwai wasu matsaloli da al'amura kamar rashin kariya daga danshi da magungunan da ke da iskar oxygen, rage narkar da kwayoyi, da jinkirta wargajewar harsashin capsule yayin ajiya. Sabili da haka, ana amfani da hydroxypropyl methylcellulose a matsayin madadin gelatin capsules don shirye-shiryen capsules, wanda ke inganta tsarin samar da capsule da tasirin amfani, kuma an inganta shi sosai a gida da waje.
Yin amfani da theophylline azaman magani mai sarrafawa, Podczeck et al. ya gano cewa adadin narkar da miyagun ƙwayoyi na capsules tare da bawoyin hydroxypropyl methylcellulose ya fi na gelatin capsules. Dalilin binciken shi ne cewa rarrabuwar HPMC ita ce rushewar gaba ɗaya capsule a lokaci guda, yayin da rarrabuwa na capsule gelatin shine rushewar tsarin cibiyar sadarwa da farko, sannan kuma rushewar gaba ɗaya capsule, don haka capsule na HPMC ya fi dacewa da harsashi na Capsule don samar da tsari na gaggawa. Chiwele et al. Hakanan ya sami irin wannan shawarar kuma idan aka kwatanta da narkar da gelatin, gelatin/polyethylene glycol da harsashi na HPMC. Sakamakon ya nuna cewa an narkar da harsashi na HPMC da sauri a ƙarƙashin yanayi daban-daban na pH, yayin da gelatin capsules Yana da matukar tasiri ga yanayin pH daban-daban. Tang Yue et al. an duba wani sabon nau'in harsashi na capsule don ƙananan ƙwayar magani mara bushewar foda mai ɗaukar hoto. Idan aka kwatanta da harsashi na capsule na hydroxypropyl methylcellulose da capsule na gelatin, an bincika kwanciyar hankali na kwandon capsule da kaddarorin foda a cikin harsashi a ƙarƙashin yanayi daban-daban, kuma an gudanar da gwajin friability. Sakamakon ya nuna cewa idan aka kwatanta da gelatin capsules, HPMC capsule bawo sun fi kyau a cikin kwanciyar hankali da kariyar foda, suna da ƙarfin juriya na danshi, kuma suna da ƙananan friability fiye da gelatin capsule bawo, don haka HPMC capsule bawo sun fi dacewa da Capsules don bushe foda inhalation.
3.7 a matsayin bioadhesive
Fasahar bioadhesion tana amfani da abubuwan haɓakawa tare da polymers masu haɓakawa. Ta hanyar yin amfani da ƙwayar ƙwayar ƙwayar cuta, yana haɓaka ci gaba da haɗin gwiwa tsakanin shirye-shiryen da mucosa, don haka an saki miyagun ƙwayoyi a hankali kuma a shayar da mucosa don cimma manufar magani. Ana amfani da shi sosai a halin yanzu. Maganin cututtuka na gastrointestinal tract, farji, mucosa na baki da sauran sassa.
Fasahar bioadhesion na hanji wani sabon tsarin isar da magunguna ne da aka haɓaka a cikin 'yan shekarun nan. Yana ba kawai tsawaita lokacin zama na shirye-shiryen miyagun ƙwayoyi a cikin ƙwayar gastrointestinal ba, amma kuma yana inganta aikin hulɗar tsakanin miyagun ƙwayoyi da membrane na sel a wurin sha, yana canza canjin ƙwayar sel, kuma yana sa shigar da miyagun ƙwayoyi a cikin ƙananan ƙwayoyin epithelial na hanji yana inganta, don haka inganta bioavailability na miyagun ƙwayoyi. Wei Keda et al. sun tantance ainihin rubutun kwamfutar hannu tare da adadin HPMCK4M da Carbomer 940 a matsayin abubuwan bincike, kuma sun yi amfani da na'urar bioadhesion da kanta don auna ƙarfin kwasfa tsakanin kwamfutar hannu da simintin biofilm ta ingancin ruwan da ke cikin jakar filastik. , kuma a ƙarshe ya zaɓi abun ciki na HPMCK40 da carbomer 940 don zama 15 da 27.5 MG a cikin mafi kyawun yanki na takardar sayan magani na NCaEBT kwamfutar hannu, bi da bi, don shirya kayan kwalliyar kwamfutar hannu na NCaEBT, yana nuna cewa kayan bioadhesive (kamar hydroxypropyl methylcellulose) na iya rage haɓakar nama don haɓaka haɓakar nama.
Shirye-shiryen bioadhesive na baka kuma sabon nau'in tsarin isar da magunguna ne wanda aka yi nazari sosai a cikin 'yan shekarun nan. Shirye-shiryen bioadhesive na baka na iya manne da miyagun ƙwayoyi zuwa ɓangaren da abin ya shafa na rami na baka, wanda ba kawai tsawaita lokacin zama na miyagun ƙwayoyi a cikin mucosa na baka ba, har ma yana kare mucosa na baka. Ingantacciyar sakamako na warkewa da ingantacciyar ƙwayar ƙwayar cuta. Xue Xiaoyan et al. An inganta samar da allunan manne na baka na insulin, ta amfani da apple pectin, chitosan, carbomer 934P, hydroxypropyl methylcellulose (HPMC K392) da sodium alginate azaman kayan bioadhesive, da daskare-bushe don shirya insulin na baka. M takarda Layer biyu. Kwamfutar manne na baka da aka shirya yana da tsari mai kama da soso, wanda ya dace da sakin insulin, kuma yana da Layer na kariya na hydrophobic, wanda zai iya tabbatar da sakin maganin ba tare da izini ba kuma ya guje wa asarar magungunan. Hao Jifu et al. Har ila yau, an shirya beads masu launin shuɗi-yellow na baka ta amfani da manne Baiji, HPMC da carbomer a matsayin kayan aikin bioadhesive.
A cikin tsarin isar da magungunan farji, fasahar bioadhesion kuma an yi amfani da ita sosai. Zhu Yuting et al. amfani da carbomer (CP) da HPMC a matsayin m kayan da kuma ci gaba-saki matrix don shirya clotrimazole bioadhesive farji Allunan tare da daban-daban formulations da rabo, da kuma auna su adhesion, manne lokaci da kumburi kashi a cikin muhalli na wucin gadi ruwa ruwa. , An duba takardar sayan magani da ta dace kamar CP-HPMC1: 1, takardar manne da aka shirya yana da kyakkyawan aikin mannewa, kuma tsarin yana da sauƙi kuma mai yiwuwa.
3.8 a matsayin Topical gel
A matsayin shiri na m, gel yana da jerin fa'idodi kamar aminci, kyakkyawa, tsaftacewa mai sauƙi, ƙananan farashi, tsari mai sauƙi, da kuma dacewa mai kyau tare da kwayoyi. Hanyar ci gaba. Misali, gel transdermal wani sabon nau'in sashi ne wanda aka yi nazari sosai a cikin 'yan shekarun nan. Ba zai iya kawai kauce wa lalata kwayoyi a cikin gastrointestinal fili da kuma rage ganiya-to-trough bambancin da jini magani maida hankali ne akan, amma kuma ya zama daya daga cikin m miyagun ƙwayoyi saki tsarin don shawo kan miyagun ƙwayoyi illa. .
Zhu Jingjie et al. yayi nazarin tasirin matrices daban-daban akan sakin sutellarin barasa plastid gel a cikin vitro, kuma an gwada shi tare da carbomer (980NF) da hydroxypropyl methylcellulose (HPMCK15M) azaman gel matrices, kuma ya sami sutellarin dace da sutellarin. Gel matrix na barasa plastids. Sakamakon gwaji ya nuna cewa 1. 0% carbomer, 1. 5% carbomer, 1. 0% carbomer + 1. 0% HPMC, 1. 5% carbomer + 1. 0% HPMC a matsayin gel matrix Dukansu sun dace da plastids barasa na scutellarin. A lokacin gwajin, an gano cewa HPMC na iya canza yanayin sakin miyagun ƙwayoyi na matrix gel matrix ta hanyar dacewa da ma'auni na kinetic na sakin miyagun ƙwayoyi, kuma 1.0% HPMC na iya inganta 1.0% carbomer matrix da 1.5% carbomer matrix. Dalili na iya zama cewa HPMC yana faɗaɗa da sauri, kuma saurin haɓakawa a farkon matakin gwaji ya sa ratar kwayoyin halitta na kayan gel carbomer ya fi girma, ta haka yana haɓaka ƙimar sakin miyagun ƙwayoyi. Zhao Wencui et al. An yi amfani da carbomer-934 da hydroxypropyl methylcellulose a matsayin masu ɗaukar kaya don shirya gel na ophthalmic na norfloxacin. Tsarin shirye-shiryen yana da sauƙi kuma mai yiwuwa, kuma ingancin ya dace da gel na ophthalmic na "Pharmacopoeia na kasar Sin" (2010 edition) Bukatun ingancin.
3.9 Mai hana hazo don tsarin kai-microemulsifying
Tsarin isar da magunguna na kai-microemulsifying (SMEDDS) sabon nau'in tsarin isar da magunguna ne na baka, wanda shine gauraya mai kama da juna, barga da gaskiya wanda ya hada da magani, lokacin mai, emulsifier da co-emulsifier. Abun da ke cikin takardar sayan magani yana da sauƙi, kuma aminci da kwanciyar hankali suna da kyau. Don magungunan da ba su da ƙarfi, kayan polymer mai narkewa na ruwa, irin su HPMC, polyvinylpyrrolidone (PVP), da sauransu, ana ƙara su sau da yawa don yin magungunan kyauta da magungunan da ke cikin microemulsion sun sami rarrabuwar kawuna a cikin ƙwayar gastrointestinal, don haɓaka solubility na miyagun ƙwayoyi da haɓaka bioavailability.
Peng Xuan et al. shirya silibinin supersaturated kai-emulsifying tsarin isar da ƙwayoyi (S-SEDDS). Oxyethylene hydrogenated Castor oil (Cremophor RH40), 12% caprylic capric acid polyethylene glycol glyceride (Labrasol) a matsayin co-emulsifier, da 50 mg · g-1 HPMC. Ƙara HPMC zuwa SSEDDS na iya haɓaka silibinin kyauta don narke a cikin S-SEDDS kuma ya hana silibinin daga hazo. Idan aka kwatanta da na al'ada kai-microemulsion formulations, mafi girma adadin surfactant yawanci ƙara don hana rashin cikar miyagun ƙwayoyi encapsulation. Bugu da kari na HPMC iya ci gaba da solubility na silibinin a cikin rushe matsakaici in mun gwada da m, rage emulsification a kai-microemulsion formulations. sashi na wakili.
4.Kammalawa
Ana iya ganin HPMC an yi amfani da shi sosai a cikin shirye-shirye saboda abubuwan da ke tattare da shi na zahiri, sinadarai da halittu, amma HPMC kuma tana da nakasu da yawa a cikin shirye-shirye, kamar al'amarin fitowar gaba da bayan fashe. methyl methacrylate) don ingantawa. A lokaci guda, wasu masu bincike sun binciki aikace-aikacen ka'idar osmotic a cikin HPMC ta hanyar shirya allunan ci gaba na carbamazepine da allunan ci gaba da sakin verapamil hydrochloride don ƙarin nazarin tsarin sakin sa. A cikin kalma ɗaya, ƙarin masu bincike suna yin aiki mai yawa don ingantaccen aikace-aikacen HPMC a cikin shirye-shirye, kuma tare da zurfin nazarin kaddarorin sa da haɓaka fasahar shirye-shirye, HPMC za ta fi amfani da ita a cikin sabbin nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan nau'ikan suna yin amfani da su. A cikin bincike na tsarin magunguna, sa'an nan kuma inganta ci gaba da ci gaban kantin magani.
Lokacin aikawa: Oktoba-08-2022