An sake duba, an yi nazari da taƙaita rubuce-rubucen da suka shafi wannan a cikin gida da waje wajen shirya sinadaran magunguna hydroxypropyl methylcellulose (HPMC) a cikin 'yan shekarun nan, kuma an yi amfani da shi a cikin shirye-shiryen da suka yi ƙarfi, shirye-shiryen ruwa, shirye-shiryen saki mai ɗorewa da sarrafawa, shirye-shiryen capsules, gelatin Sabbin aikace-aikacen a fagen sabbin dabaru kamar su manne da bioadhesives. Saboda bambancin nauyin kwayoyin halitta da danko na HPMC, yana da halaye da amfani da emulsification, mannewa, kauri, ƙaruwar danko, dakatarwa, gelling da kuma samar da fim. Ana amfani da shi sosai a shirye-shiryen magunguna kuma zai taka rawa mafi girma a fagen shirye-shirye. Tare da zurfafa bincike kan kaddarorinsa da kuma inganta fasahar hada magunguna, HPMC za a fi amfani da shi sosai a binciken sabbin nau'ikan magunguna da sabbin tsarin isar da magunguna, ta haka ne za a haɓaka ci gaba da haɓaka hada magunguna.
hydroxypropyl methylcellulose; shirye-shiryen magunguna; abubuwan da ke ƙara wa magunguna.
Abubuwan da ke cikin magunguna ba wai kawai su ne tushen samar da shirye-shiryen magunguna na ɗanye ba, har ma suna da alaƙa da wahalar tsarin shiri, ingancin magani, kwanciyar hankali, aminci, saurin sakin magani, yanayin aiki, ingancin asibiti, da haɓaka sabbin nau'ikan magunguna da sabbin hanyoyin gudanarwa. suna da alaƙa da juna. Fitowar sabbin abubuwan da ke cikin magunguna sau da yawa yana haɓaka ingancin shiri da haɓaka sabbin nau'ikan magunguna. Hydroxypropyl methylcellulose (HPMC) yana ɗaya daga cikin shahararrun abubuwan da ke cikin magunguna a gida da waje. Saboda bambancin nauyin kwayoyin halitta da ɗanko, yana da ayyukan emulsifying, ɗaurewa, kauri, kauri, dakatarwa, da mannewa. Siffofi da amfani kamar coagulation da samar da fim ana amfani da su sosai a fasahar magunguna. Wannan labarin galibi yana sake duba aikace-aikacen hydroxypropyl methylcellulose (HPMC) a cikin tsari a cikin 'yan shekarun nan.
1.Babban kaddarorin HPMC
Hydroxypropyl methyl cellulose (HPMC), tsarin kwayoyin halitta shine C8H15O8-(C10 H18O6) n-C8H15O8, kuma nauyin kwayoyin halitta shine kimanin 86 000. Wannan samfurin abu ne mai kama da na roba, wanda yake ɓangare na methyl kuma wani ɓangare na polyhydroxypropyl ether na cellulose. Ana iya samar da shi ta hanyoyi biyu: Na farko shine cewa ana kula da methyl cellulose na matakin da ya dace da NaOH sannan a mayar da martani da propylene oxide a ƙarƙashin zafin jiki mai yawa da matsin lamba mai yawa. Lokacin amsawa dole ne ya daɗe don barin methyl da hydroxypropyl su samar da haɗin ether. An haɗa shi da zoben anhydroglucose na cellulose a cikin nau'in cellulose, kuma yana iya kaiwa matakin da ake so; ɗayan kuma shine a shafa auduga ko zare na itace da caustic soda, sannan a mayar da martani da methane da propylene oxide da aka yi chlorine a jere, sannan a ƙara tace shi. , a niƙa shi zuwa foda ko granules mai kyau da daidaito.
Launin wannan samfurin fari ne zuwa fari mai kama da madara, ba shi da ƙamshi kuma ba shi da ɗanɗano, kuma siffar foda ce mai laushi ko mai laushi mai sauƙin gudana. Ana iya narkar da wannan samfurin a cikin ruwa don samar da ruwan colloidal mai haske zuwa mai kama da madara tare da ɗanɗano mai kama da madara. Lamarin canzawar sol-gel na iya faruwa saboda canjin zafin maganin tare da wani takamaiman yawan amfani.
Saboda bambancin da ke cikin abubuwan da ke cikin waɗannan maye biyu a cikin tsarin methoxy da hydroxypropyl, nau'ikan samfura daban-daban sun bayyana. A cikin takamaiman yawan samfura, nau'ikan samfura daban-daban suna da takamaiman halaye. Danko da zafin jiki na gelation na thermal, saboda haka suna da halaye daban-daban kuma ana iya amfani da su don dalilai daban-daban. Pharmacopoeia na ƙasashe daban-daban yana da ƙa'idodi da wakilci daban-daban akan samfurin: European Pharmacopoeia ya dogara ne akan nau'ikan ...
Calocan's hydroxypropyl methylcellulose yana da jerin 3, wato jerin E, jerin F da jerin K, kowanne jerin yana da nau'ikan samfura iri-iri da za a zaɓa daga ciki. Ana amfani da jerin E galibi azaman murfin fim, ana amfani da shi don murfin kwamfutar hannu, ƙwayayen kwamfutar hannu da aka rufe; ana amfani da jerin E, F azaman viscosifiers da magungunan hana sakin jiki don shirye-shiryen ido, wakilai masu dakatarwa, masu kauri don shirye-shiryen ruwa, allunan da kuma abubuwan da ke ɗaure granules; Ana amfani da jerin K galibi azaman masu hana sakin jiki da kayan matrix na hydrophilic don shirye-shiryen sakin jiki masu jinkiri da sarrafawa.
Masana'antun cikin gida galibi sun haɗa da Fuzhou No. 2 Chemical Factory, Huzhou Food and Chemical Co., Ltd., Sichuan Luzhou Pharmaceutical Accessories Factory, Hubei Jinxian Chemical Factory No. 1, Feicheng Ruitai Fine Chemical Co., Ltd., Shandong Liaocheng Ahua Pharmaceutical Co., Ltd., Xi'an Huian chemical plants, da sauransu.
2.Abũbuwan amfãni daga HPMC
HPMC ta zama ɗaya daga cikin magungunan da aka fi amfani da su a gida da waje, domin HPMC tana da fa'idodi da sauran magungunan da ba su da su.
2.1 Ruwan sanyi yana narkewa
Yana narkewa a cikin ruwan sanyi ƙasa da 40 ℃ ko 70% ethanol, ba ya narkewa a cikin ruwan zafi sama da 60 ℃, amma ana iya yin gel.
2.2 Ba ya aiki a sinadarai
HPMC wani nau'in cellulose ether ne wanda ba ionic ba, maganin sa ba shi da cajin ionic kuma baya hulɗa da gishirin ƙarfe ko mahaɗan ionic na halitta, don haka sauran abubuwan da ke taimakawa ba sa amsawa da shi yayin aikin samar da shirye-shirye.
2.3 Kwanciyar hankali
Yana da daidaito idan aka kwatanta da acid da alkali, kuma ana iya adana shi na dogon lokaci tsakanin pH 3 da 11 ba tare da wani canji mai mahimmanci a cikin danko ba. Maganin ruwa na HPMC yana da tasirin hana mildew kuma yana kiyaye kyakkyawan kwanciyar hankali yayin ajiya na dogon lokaci. Magungunan da ke amfani da HPMC suna da ingantaccen kwanciyar hankali fiye da waɗanda ke amfani da sinadaran gargajiya (kamar dextrin, sitaci, da sauransu).
2.4 Daidaita Danko
Ana iya haɗa nau'ikan danko daban-daban na HPMC a cikin rabo daban-daban, kuma ana iya canza dankonsa bisa ga wani takamaiman doka, kuma yana da kyakkyawar alaƙar layi, don haka ana iya zaɓar rabon bisa ga buƙatun.
2.5 Rashin ƙarfin metabolism
Ba a shan HPMC ko kuma a narkar da shi a jiki, kuma ba ya samar da zafi, don haka magani ne mai aminci. 2.6 Tsaro Gabaɗaya ana ɗaukar cewa HPMC abu ne da ba shi da guba kuma ba ya haifar da haushi, matsakaicin adadin da ake buƙata don beraye shine 5 g·kg – 1, kuma matsakaicin adadin da ake buƙata don beraye shine 5.2 g · kg – 1. Yawan da ake buƙata a kowace rana ba shi da lahani ga jikin ɗan adam.
3.Amfani da HPMC a cikin tsari
3.1 A matsayin kayan shafa fim da kayan samar da fim
Ta amfani da HPMC a matsayin kayan kwamfutar hannu mai rufi da fim, kwamfutar hannu mai rufi ba ta da wata fa'ida a bayyane wajen ɓoye ɗanɗano da kamanni idan aka kwatanta da allunan da aka rufe da sukari, amma taurinsa, saurinsa, sha danshi, matakin wargajewa, ƙaruwar nauyin rufi da sauran alamun inganci sun fi kyau. Ana amfani da ƙarancin ɗanɗano na wannan samfurin azaman kayan shafa fim mai narkewa cikin ruwa don allunan da allunan, kuma ana amfani da babban ɗanɗano azaman kayan shafa fim don tsarin narkewar halitta, yawanci a cikin taro na 2% zuwa 20%.
Zhang Jixing da abokan aikinsa sun yi amfani da hanyar saman tasirin don inganta tsarin haɗin premix tare da HPMC a matsayin murfin fim. Sun ɗauki kayan da ke samar da fim ɗin HPMC, adadin polyvinyl alcohol da plasticizer polyethylene glycol a matsayin abubuwan bincike, ƙarfin tensile da permeability na fim ɗin da kuma danko na maganin rufe fim ɗin shine ma'aunin dubawa, kuma an bayyana alaƙar da ke tsakanin ma'aunin dubawa da abubuwan dubawa ta hanyar samfurin lissafi, kuma an sami mafi kyawun tsarin tsari. Amfani da shi bi da bi shine wakilin samar da fim hydroxypropyl methylcellulose (HPMCE5) 11.88 g, polyvinyl alcohol 24.12 g, plasticizer polyethylene glycol 13.00 g, kuma danko na dakatar da rufewa shine 20 mPa·s, ƙarfin permeability da tensile na fim ɗin ya kai mafi kyawun sakamako. Zhang Yuan ya inganta tsarin shiryawa, ya yi amfani da HPMC a matsayin abin ɗaurewa don maye gurbin sitaci slurry, kuma ya canza allunan Jiahua zuwa allunan da aka shafa musu fim don inganta ingancin shirye-shiryensa, inganta hygroscopicity, sauƙin ɓacewa, allunan da aka sassauta, da sauran matsaloli, da haɓaka daidaiton allunan. An ƙayyade mafi kyawun tsarin hadawa ta hanyar gwaje-gwajen orthogonal, wato, yawan sinadarin slurry shine 2% HPMC a cikin maganin ethanol 70% yayin shafa, kuma lokacin juyawa yayin tattara allunan shine mintuna 15. Sakamako Allunan da aka shafa wa fim ɗin Jiahua da aka shirya ta sabon tsari da takardar sayan magani sun inganta sosai a cikin kamanni, lokacin wargajewa da taurin zuciyar fiye da waɗanda aka samar ta hanyar asali na takardar sayan magani, kuma ƙimar da aka cancanta na allunan da aka shafa wa fim ɗin ta inganta sosai. Ya kai fiye da 95%. Liang Meiyi, Lu Xiaohui, da sauransu sun kuma yi amfani da hydroxypropyl methylcellulose a matsayin kayan samar da fim don shirya allunan sanya patinae colon da allunan sanya patinae colon, bi da bi. Suna shafar sakin magani. Huang Yunran ya shirya Allunan Sanya Maganin Ciwon Jini na Dragon, sannan ya shafa HPMC a kan maganin shafawa na Layer na kumburi, kuma kashi 5% na nauyinsa ya kasance. Ana iya ganin cewa ana iya amfani da HPMC sosai a tsarin isar da magunguna ga hanji.
Hydroxypropyl methylcellulose ba wai kawai kayan shafa fim ne mai kyau ba, har ma ana iya amfani da shi azaman kayan samar da fim a cikin tsarin fim. An inganta Wang Tongshun da sauransu zuwa ga takardar maganin sinadarin zinc licorice da kuma fim ɗin aminolexanol na baki, tare da sassauci, daidaito, santsi, da kuma bayyana wakilin fim a matsayin ma'aunin bincike, samun takardar maganin da ya fi dacewa shine PVA 6.5 g, HPMC 0.1 g da 6.0 g na propylene glycol sun cika buƙatun sakin jiki a hankali da aminci, kuma ana iya amfani da su azaman takardar maganin shirya fim ɗin.
3.2 a matsayin abin ɗaurewa da kuma mai wargazawa
Ana iya amfani da ƙarancin ƙarfin wannan samfurin a matsayin abin ɗaurewa da kuma narkar da shi ga allunan, kwayoyi da granules, kuma babban ƙarfin ƙarfin za a iya amfani da shi ne kawai a matsayin abin ɗaurewa. Yawan da za a ɗauka ya bambanta dangane da samfura da buƙatu daban-daban. Gabaɗaya, yawan ƙarfin haɗin don allunan granulation busasshe shine 5%, kuma yawan ƙarfin haɗin don allunan granulation da aka yi da ruwa shine 2%.
Li Houtao da abokan aikinsa sun duba abin ɗaure allunan tinidazole. An binciki kashi 8% na polyvinylpyrrolidone (PVP-K30), syrup 40%, sitaci slurry 10%, 2.0% hydroxypropyl methylcellulose K4 (HPMCK4M), 50% ethanol yayin da ake manne allunan tinidazole. Shirya allunan tinidazole. An kwatanta canje-canjen bayyanar allunan da aka yi amfani da su bayan an shafa su, kuma an auna ƙarfinsu, tauri, lokacin wargajewa da kuma yawan narkewar allunan magani daban-daban. Sakamako Allunan da 2.0% hydroxypropyl methylcellulose suka shirya sun yi sheƙi, kuma ma'aunin friability bai sami wani abin da ke haifar da guntuwar gefuna da kuma kusurwoyi ba, kuma bayan an shafa su, siffar allunan ta cika kuma kamannin ya yi kyau. Saboda haka, an yi amfani da allunan tinidazole da aka shirya da 2.0% HPMC-K4 da 50% ethanol a matsayin abin ɗaurewa. Guan Shihai ya yi nazarin tsarin samar da Allunan Fuganning, ya tantance manne-manne, sannan ya tantance kashi 50% na ethanol, kashi 15% na manne sitaci, kashi 10% na PVP da kashi 50% na ethanol tare da matsewa, laushi, da kuma friability a matsayin alamun kimantawa. , kashi 5% na CMC-Na da kashi 15% na HPMC (5 mPa s). Sakamako Takardun da aka shirya ta hanyar ethanol 50%, kashi 15% na manne sitaci, kashi 10% na PVP 50% na ethanol da kashi 5% na CMC-Na suna da santsi, amma rashin matsewa da ƙarancin tauri, wanda bai iya biyan buƙatun shafi ba; kashi 15% na maganin HPMC (5 mPa·s), saman kwamfutar hannu yana da santsi, an cancanta da friability, kuma freability yana da kyau, wanda zai iya biyan buƙatun shafi. Saboda haka, an zaɓi HPMC (5 mPa s) a matsayin manne.
3.3 a matsayin wakilin dakatarwa
Ana amfani da wannan samfurin mai girman ɗanko a matsayin wakili mai dakatarwa don shirya shiri na ruwa mai nau'in dakatarwa. Yana da kyakkyawan tasirin dakatarwa, yana da sauƙin sake wargazawa, baya mannewa a bango, kuma yana da ƙananan ƙwayoyin flocculation. Yawan da aka saba amfani da shi shine 0.5% zuwa 1.5%. Song Tian et al. sun yi amfani da kayan polymer da aka saba amfani da su (hydroxypropyl methylcellulose, sodium carboxymethylcellulose, povidone, xanthan gum, methylcellulose, da sauransu) azaman wakilai masu dakatarwa don shirya dakatarwar busasshe ta racecadotril. Ta hanyar rabon ƙarar sedimentation na dakatarwa daban-daban, an lura da ma'aunin redispersibility, da rheology, viscosity na dakatarwa da yanayin microscopic, kuma an binciki kwanciyar hankali na ƙwayoyin magani a ƙarƙashin gwajin da aka hanzarta. Sakamako An kuma binciki dakatarwar busasshe da aka shirya tare da 2% HPMC azaman 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 mafita mafi haske, kuma ƙaramin adadin abubuwan fibrous marasa warwatse ne kawai ke wanzuwa, don haka ana amfani da HPMC a matsayin maganin dakatarwa a cikin shirye-shiryen ido. Liu Jie da abokan aikinsa sun yi amfani da HPMC, hydroxypropyl cellulose (HPC), carbomer 940, polyethylene glycol (PEG), sodium hyaluronate (HA) da haɗin HA/HPMC a matsayin masu dakatarwa don shirya takamaiman bayanai daban-daban. An zaɓi dakatarwar ido ta Ciclovir, rabon ƙarar sedimentation, girman barbashi da sake warwatsewa a matsayin alamun dubawa don tantance mafi kyawun wakilin dakatarwa. Sakamakon ya nuna cewa dakatarwar ido ta acyclovir da 0.05% HA da 0.05% HPMC suka shirya a matsayin wakilin dakatarwa, rabon ƙarar sedimentation shine 0.998, girman barbashi iri ɗaya ne, sake warwatsewa yana da kyau, kuma shiri yana da karko Jima'i yana ƙaruwa.
3.4 A matsayin mai toshewa, wakili mai sakin jiki a hankali kuma mai sarrafawa da kuma wakili mai samar da ramuka
Ana amfani da wannan samfurin mai girman gaske wajen shirya allunan gel matrix masu dorewa, masu toshewa da kuma wakilai masu sarrafawa na allunan matrix masu dorewa, kuma yana da tasirin jinkirta sakin magani. Yawansa yana tsakanin kashi 10% zuwa 80%. Ana amfani da ƙananan matakan raguwa a matsayin porogens don shirye-shiryen saki mai dorewa ko na sarrafawa. Ana iya isa ga allurar farko da ake buƙata don tasirin magani na irin waɗannan allunan cikin sauri, sannan ana yin tasirin sakin da ya daɗe ko na sarrafawa, kuma ana kiyaye ingantaccen yawan magungunan jini a jiki. Ana shayar da Hydroxypropyl methylcellulose don samar da layin gel lokacin da ya haɗu da ruwa. Hanyar sakin magani daga allunan matrix galibi ya haɗa da yaɗuwar layin gel da ya lalace na layin gel. Jung Bo Shim et al sun shirya allunan sakin da ya daɗe tare da HPMC azaman kayan sakin da ya daɗe.
Ana kuma amfani da Hydroxypropyl methylcellulose sosai a cikin allunan matrix masu dorewa na maganin gargajiya na kasar Sin, kuma ana amfani da yawancin sinadaran aiki, sassan da suka dace da shirye-shiryen maganin gargajiya na kasar Sin guda ɗaya. Liu Wen da abokan aikinsa sun yi amfani da kashi 15% na hydroxypropyl methylcellulose a matsayin kayan matrix, kashi 1% na lactose da kashi 5% na microcrystalline cellulose a matsayin abubuwan cikawa, kuma sun shirya Jingfang Taohe Chengqi Decoction a cikin allunan matrix masu dorewa. Tsarin shine lissafin Higuchi. Tsarin hadadden tsari yana da sauƙi, shiri yana da sauƙi, kuma bayanan fitarwa suna da kwanciyar hankali, wanda ya cika buƙatun Pharmacopoeia na kasar Sin. Tang Guanguang da abokan aikinsa sun yi amfani da jimillar saponins na Astragalus a matsayin maganin samfuri, sun shirya allunan matrix na HPMC, kuma sun binciki abubuwan da ke shafar sakin magani daga ingantattun sassan maganin gargajiya na kasar Sin a cikin allunan matrix na HPMC. Sakamako Yayin da yawan HPMC ya karu, sakin astragaloside ya ragu, kuma kashi na sakin maganin yana da alaƙa kusan layi tare da ƙimar narkewar matrix. A cikin kwamfutar matrix ta hypromellose HPMC, akwai wata alaƙa tsakanin sakin ɓangaren maganin gargajiya na kasar Sin mai tasiri da kuma yawan da nau'in HPMC, kuma tsarin sakin monomer na sinadarai mai hydrophilic yayi kama da shi. Hydroxypropyl methylcellulose ba wai kawai ya dace da mahaɗan hydrophilic ba, har ma da abubuwan da ba su da hydrophilic. Liu Guihua ya yi amfani da kashi 17% na hydroxypropyl methylcellulose (HPMCK15M) a matsayin kayan matrix mai dorewa, kuma ya shirya allunan matrix mai dorewa na Tianshan Xuelian ta hanyar amfani da granulation da tableting. Tasirin sakin mai dorewa a bayyane yake, kuma tsarin shiri ya kasance mai karko kuma mai yiwuwa.
Ba wai kawai ana amfani da Hydroxypropyl methylcellulose a kan allunan matrix masu dorewa na sinadaran aiki da kuma ingantattun sassan maganin gargajiya na kasar Sin ba, har ma ana amfani da su sosai a cikin shirye-shiryen hadadden maganin gargajiya na kasar Sin. Wu Huichao da abokan aikinsa sun yi amfani da kashi 20% na hydroxypropyl methyl cellulose (HPMCK4M) a matsayin kayan matrix, kuma sun yi amfani da hanyar matsa foda kai tsaye don shirya allunan matrix na Yizhi hydrophilic wanda zai iya sakin maganin a hankali kuma a hankali na tsawon awanni 12. An yi amfani da Saponin Rg1, ginsenoside Rb1 da Panax notoginseng saponin R1 a matsayin alamun kimantawa don bincika sakin a cikin vitro, kuma an sanya lissafin sakin magani don nazarin tsarin sakin magani. Sakamako Tsarin sakin magani ya yi daidai da lissafin kinetic sifili da lissafin Ritger-Peppas, wanda aka saki geniposide ta hanyar yaduwar da ba ta Fick ba, kuma an saki sassa uku a cikin Panax notoginseng ta hanyar yashewar kwarangwal.
3.5 Manna mai kariya a matsayin mai kauri da kuma colloid
Idan aka yi amfani da wannan samfurin a matsayin mai kauri, yawan kashi da aka saba samu shine 0.45% zuwa 1.0%. Hakanan zai iya ƙara kwanciyar hankali na manne mai kama da hydrophobic, samar da colloid mai kariya, hana barbashi haɗuwa da haɗuwa, ta haka yana hana samuwar laka. Yawan kashi da aka saba samu shine 0.5% zuwa 1.5%.
Wang Zhen da abokan aikinsa sun yi amfani da hanyar gwaji ta L9 orthogonal don bincika tsarin shirya maganin carbon enema mai kunnawa ta magani. Mafi kyawun yanayin tsari don tantance ƙarshe na maganin carbon enema mai kunnawa ta magani shine amfani da 0.5% sodium carboxymethyl cellulose da 2.0% hydroxypropyl methylcellulose (HPMC ya ƙunshi 23.0% methoxyl group, hydroxypropoxyl Base 11.6%) a matsayin mai kauri, yanayin aikin yana taimakawa wajen haɓaka kwanciyar hankali na maganin carbon mai kunnawa. Zhang Zhiqiang da abokan aikinsa sun haɓaka gel ɗin levofloxacin hydrochloride mai shirye don amfani da ido wanda ke da tasirin sakin jiki mai ɗorewa, suna amfani da carbopol azaman matrix na gel da hydroxypropyl methylcellulose azaman maganin kauri. Mafi kyawun maganin da aka yi ta gwaji, a ƙarshe an sami mafi kyawun maganin da aka rubuta 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 dihydrogen, 0.50 g na sodium chloride, 0.03 g na ethyl paraben, sannan aka ƙara ruwa don yin 100 mL. A cikin gwajin, marubucin ya tantance jerin hydroxypropyl methylcellulose METHOCEL na Kamfanin Colorcon tare da takamaiman bayanai daban-daban (K4M, E4M, E15 LV, E50LV) don shirya masu kauri tare da yawan da ya bambanta, kuma sakamakon ya zaɓi HPMC E50 LV a matsayin mai kauri. Mai kauri don gels na nan take na levofloxacin hydrochloride masu amsawa ga pH.
3.6 a matsayin kayan capsule
Yawanci, sinadarin harsashin capsules galibi gelatin ne. Tsarin samar da harsashin capsule abu ne mai sauƙi, amma akwai wasu matsaloli da abubuwan da suka faru kamar rashin kariya daga danshi da magungunan da ke da alaƙa da iskar oxygen, rage narkewar magani, da jinkirin wargajewar harsashin capsule yayin ajiya. Saboda haka, ana amfani da hydroxypropyl methylcellulose a madadin gelatin capsules don shirya capsules, wanda ke inganta yanayin samar da capsules da tasirin amfani, kuma an tallata shi sosai a gida da waje.
Ta amfani da theophylline a matsayin maganin sarrafawa, Podczeck da sauransu sun gano cewa yawan narkewar maganin capsules tare da harsashin hydroxypropyl methylcellulose ya fi na capsules na gelatin girma. Dalilin binciken shine cewa rushewar HPMC shine rushewar dukkan capsule a lokaci guda, yayin da rushewar capsule na gelatin shine rushewar tsarin hanyar sadarwa da farko, sannan rushewar dukkan capsule, don haka capsule na HPMC ya fi dacewa da harsashin Capsule don samar da tsari nan take. Chiwele da sauransu sun sami irin wannan ƙarshe kuma sun kwatanta rushewar gelatin, gelatin/polyethylene glycol da harsashin HPMC. Sakamakon ya nuna cewa harsashin HPMC ya narke cikin sauri a ƙarƙashin yanayi daban-daban na pH, yayin da capsules na gelatin Yana shafar yanayin pH daban-daban. Tang Yue da sauransu sun duba wani sabon nau'in harsashin capsule don tsarin ɗaukar iskar shaƙa mai ƙarancin magani. Idan aka kwatanta da harsashin capsule na hydroxypropyl methylcellulose da harsashin capsule na gelatin, an binciki kwanciyar hankalin harsashin capsule da halayen foda a cikin harsashi a ƙarƙashin yanayi daban-daban, kuma an gudanar da gwajin friability. Sakamakon ya nuna cewa idan aka kwatanta da ƙwayoyin gelatin, ƙwayoyin HPMC sun fi ƙarfi a cikin kwanciyar hankali da kariyar foda, suna da ƙarfi wajen jure danshi, kuma suna da ƙarancin jurewar gelatin fiye da ƙwayoyin gelatin, don haka ƙwayoyin HPMC sun fi dacewa da ƙwayoyin don shaƙa busasshen foda.
3.7 a matsayin biomandhesive
Fasahar bioadhesion tana amfani da sinadaran da ke ɗauke da sinadarai masu ɗaurewa. Ta hanyar mannewa da ƙwayoyin halitta, tana ƙara ci gaba da matsewa tsakanin shirye-shiryen da mucosa, ta yadda maganin zai saki sannu a hankali kuma mucosa ta sha shi don cimma manufar magani. Ana amfani da shi sosai a halin yanzu. Maganin cututtukan hanji, farji, mucosa ta baki da sauran sassa.
Fasahar bioadhesion ta hanji sabuwar hanyar isar da magunguna ce da aka haɓaka a cikin 'yan shekarun nan. Ba wai kawai tana tsawaita lokacin da ake amfani da shirye-shiryen magunguna a cikin hanyar narkewar abinci ba, har ma tana inganta aikin hulɗa tsakanin maganin da membrane na tantanin halitta a wurin shan ƙwayoyi, tana canza ruwan membrane na tantanin halitta, kuma tana sa shigar maganin cikin ƙananan ƙwayoyin epithelial na hanji ya ƙaru, ta haka ne inganta samuwar maganin. Wei Keda da abokan aikinsa sun tantance takardar maganin da ke cikin kwamfutar hannu tare da adadin HPMCK4M da Carbomer 940 a matsayin abubuwan bincike, kuma sun yi amfani da na'urar bioadhesion da aka yi da kansu don auna ƙarfin barewa tsakanin kwamfutar hannu da biofilm ɗin da aka kwaikwayi ta hanyar ingancin ruwan da ke cikin jakar filastik. , kuma a ƙarshe sun zaɓi abun ciki na HPMCK40 da carbomer 940 don zama 15 da 27.5 MG a cikin mafi kyawun wurin rubutaccen magani na ƙwayoyin NCaEBT, bi da bi, don shirya ƙwayoyin NCaEBT, wanda ke nuna cewa kayan bioadhesive (kamar hydroxypropyl methylcellulose) na iya rage mahimmancin Inganta mannewar shiri zuwa kyallen.
Shirye-shiryen biomandhesive na baki suma wani sabon nau'in tsarin isar da magani ne wanda aka yi nazari sosai a cikin 'yan shekarun nan. Shirye-shiryen biomandhesive na baki na iya manne maganin zuwa ga ɓangaren da abin ya shafa na bakin, wanda ba wai kawai yana tsawaita lokacin zama na maganin a cikin mucosa na baki ba, har ma yana kare mucosa na baki. Ingancin tasirin magani da inganta samuwar magani. Xue Xiaoyan et al. sun inganta tsarin allurar insulin ta baki, ta amfani da pectin apple, chitosan, carbomer 934P, hydroxypropyl methylcellulose (HPMC K392) da sodium alginate a matsayin kayan biomandhesive, da kuma busar da su don shirya insulin ta baki. Takardar manne mai layi biyu. Kwamfutar mannewa ta baki da aka shirya tana da tsari mai kama da soso mai ramuka, wanda yake da kyau don sakin insulin, kuma yana da layin kariya mai kama da hydrophobic, wanda zai iya tabbatar da sakin maganin a gefe ɗaya kuma ya guji asarar maganin. Hao Jifu et al. sun kuma shirya facin biomandhesive na baki mai launin shuɗi-rawaya ta amfani da manne na Baiji, HPMC da carbomer azaman kayan biomandhesive.
A cikin tsarin isar da magunguna ta farji, an kuma yi amfani da fasahar bioadhesion sosai. Zhu Yuting da abokan aikinsa sun yi amfani da carbomer (CP) da HPMC a matsayin kayan manne da kuma matrix mai dorewa don shirya ƙwayoyin clotrimazole bioadhesive farji tare da tsari da rabo daban-daban, kuma sun auna mannewarsu, lokacin mannewa da kashi na kumburi a cikin yanayin ruwan farji na wucin gadi. An tantance takardar da ta dace kamar CP-HPMC1: 1, takardar manne da aka shirya tana da kyakkyawan aikin mannewa, kuma tsarin ya kasance mai sauƙi kuma mai yiwuwa.
3.8 a matsayin gel na waje
A matsayin wani shiri na manne, gel yana da fa'idodi da yawa kamar aminci, kyau, tsaftacewa mai sauƙi, araha, tsarin shiri mai sauƙi, da kuma dacewa mai kyau da magunguna. Hanyar haɓakawa. Misali, gel ɗin transdermal sabon nau'in magani ne wanda aka yi nazari sosai a cikin 'yan shekarun nan. Ba wai kawai zai iya guje wa lalata magunguna a cikin hanji da rage bambancin yawan magungunan jini ba, har ma ya zama ɗaya daga cikin ingantattun tsarin sakin magunguna don shawo kan illolin magunguna.
Zhu Jingjie da abokan aikinsa sun yi nazarin tasirin matrices daban-daban akan sakin gel ɗin plastid na scutellarin a cikin vitro, kuma an tantance su da carbomer (980NF) da hydroxypropyl methylcellulose (HPMCK15M) a matsayin gel matrices, kuma sun sami scutellarin wanda ya dace da scutellarin. Gel matrix na alkalami 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 scutellarin alcohol plastids. A lokacin gwajin, an gano cewa HPMC na iya canza yanayin sakin magani na matrix ɗin gel na carbomer ta hanyar daidaita daidaiton motsi na sakin magani, kuma 1.0% HPMC na iya inganta matrix 1.0% carbomer da matrix 1.5%. Dalilin na iya zama cewa HPMC yana faɗaɗa da sauri, kuma faɗaɗawa cikin sauri a farkon matakin gwajin yana sa gibin ƙwayoyin halitta na kayan gel ɗin carbomer ya fi girma, ta haka ne yake hanzarta fitar da maganin. Zhao Wencui da abokan aikinsa sun yi amfani da carbomer-934 da hydroxypropyl methylcellulose a matsayin masu ɗaukar magani don shirya gel ɗin ido na norfloxacin. Tsarin shiri yana da sauƙi kuma mai yiwuwa, kuma ingancin ya yi daidai da gel ɗin ido na "Chinese Pharmacopoeia" (bugun 2010).
3.9 Mai hana ruwa shiga tsarin microemulsifying kai tsaye
Tsarin isar da magunguna kai-tsaye (SMEDDS) wani sabon nau'in tsarin isar da magunguna ta baki ne, wanda cakuda ne mai kama da juna, mai karko kuma mai haske wanda ya ƙunshi magani, matakin mai, emulsifier da co-emulsifier. Tsarin maganin yana da sauƙi, kuma aminci da kwanciyar hankali suna da kyau. Ga magungunan da ba sa narkewa da kyau, ana ƙara kayan polymer na fiber mai narkewa da ruwa, kamar HPMC, polyvinylpyrrolidone (PVP), da sauransu, don sa magungunan kyauta da magungunan da aka lulluɓe a cikin microemulsion su sami narkewar da ta cika a cikin hanyar narkewar abinci, don ƙara narkewar maganin da inganta samuwarsa.
Peng Xuan da abokan aikinsa sun shirya tsarin isar da magunguna na silibinin mai cike da sinadarin hydrogenated self-emulsifying (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 ƙara silibinin kyauta don narkewa a cikin S-SEDDS kuma hana silibinin fitowa daga ruwa. Idan aka kwatanta da tsarin microemulsion na gargajiya, yawanci ana ƙara yawan surfactant don hana cikar ƙwayoyin cuta. Ƙara HPMC na iya kiyaye narkewar silibinin a cikin matsakaicin narkewar ya zama daidai, yana rage emulsification a cikin tsarin microemulsion kai. Yawan maganin.
4. Kammalawa
Za a iya ganin cewa HPMC an yi amfani da shi sosai a shirye-shirye saboda halayensa na zahiri, sinadarai da kuma na halitta, amma HPMC kuma yana da gazawa da yawa a shirye-shirye, kamar abin da ke faruwa kafin da bayan fashewar. methyl methacrylate) don ingantawa. A lokaci guda, wasu masu bincike sun binciki amfani da ka'idar osmotic a cikin HPMC ta hanyar shirya allunan carbamazepine masu dorewa da allunan verapamil hydrochloride masu dorewa don ƙara nazarin tsarin sakin sa. A takaice dai, ƙarin masu bincike suna yin aiki mai yawa don ingantaccen amfani da HPMC a cikin shirye-shirye, kuma tare da zurfafa bincike kan kaddarorin sa da haɓaka fasahar shiri, HPMC za a yi amfani da shi sosai a cikin sabbin nau'ikan allurai da sabbin nau'ikan allurai. A cikin binciken tsarin magunguna, sannan kuma haɓaka ci gaba da haɓaka kantin magani.
Lokacin Saƙo: Oktoba-08-2022