Hydroxypropyl methylcellulose (HPMC)
Category: kayan shafa; Abun ƙwayar cuta; Abubuwan polymer mai sarrafa sauri don shirye-shiryen jinkirin sakin; Wakilin daidaitawa; Taimakon dakatarwa, mannen kwamfutar hannu; Ƙarfafa mannewa wakili.
1. Gabatarwar samfur
Wannan KYAUTA BA IONIC CELLULOSE ETHER bane, a waje ana lura dashi azaman farin foda, mara wari kuma mara ɗanɗano, mai narkewa cikin ruwa da mafi yawan abubuwan kaushi na kwayoyin halitta, kumburi a cikin ruwan sanyi don share ko ɗan turBIdized colloidal bayani. Maganin ruwa mai ruwa yana da aiki na saman, babban nuna gaskiya da aikin barga. HPMC yana da dukiyar gel mai zafi. Bayan dumama, samfurin aqueous bayani yana haifar da hazo gel, sannan ya narke bayan sanyaya. Gel zafin jiki na daban-daban bayani dalla-dalla ne daban-daban. Solubility canje-canje tare da danko, danko zhao low, mafi girma da solubility, daban-daban bayani dalla-dalla na HPMC Properties da wasu bambance-bambance, HPMC narkar da ruwa ba ya shafi pH darajar.
The m konewa zafin jiki, sako-sako da yawa, gaskiya yawa da gilashin miƙa mulki zafin jiki kasance 360 ℃, 0.341g / cm3, 1.326g / cm3 da 170 ~ 180 ℃, bi da bi. Bayan dumama, yana juya launin ruwan kasa a 190 ~ 200 ° C kuma yana ƙonewa a 225 ~ 230 ° C.
HPMC kusan ba zai iya narkewa a cikin chloroform, ethanol (95%), da diethyl ether, kuma an narkar da shi a cikin cakuda ethanol da methylene chloride, cakuda methanol da methylene chloride, da cakuda ruwa da ethanol. Wasu matakan HPMC suna narkewa cikin gaurayawan acetone, methylene chloride, da 2-propanol, da kuma a cikin sauran kaushi na halitta.
Tebur 1: Alamomin fasaha
aikin
Ma'auni,
60 gd (2910).
65GD (2906)
75GD (2208)
Methoxy%
28.0-32.0
27.0-30.0
19.0-24.0
Hydroxypropoxy %
7.0-12.0
4.0-7.5
4.0-12.0
Gel zafin jiki ℃
56-64.
62.0-68.0
70.0-90.0
Viscosity mpa s.
3,5,6,15,50,4000
Farashin 504000
100400 0150 00100 000
Rashin nauyi mai bushe%
5.0 ko fiye
Rago mai ƙonewa %
1.5 ko fiye
pH
4.0-8.0
Karfe mai nauyi
20 ko kasa da haka
arsenic
2.0 ko fiye
2. Siffofin samfur
2.1 Hydroxypropyl methylcellulose an narkar da shi a cikin ruwan sanyi don samar da maganin colloidal danko. Idan dai an ƙara shi a cikin ruwan sanyi kuma an motsa shi kadan, ana iya narkar da shi a cikin bayani mai haske. A akasin wannan, shi ne m insoluble a cikin ruwan zafi sama da 60 ℃ kuma zai iya kawai kumbura. A cikin shiri na maganin ruwa na hydroxypropyl methicellulose, yana da kyau a ƙara wani ɓangare na hydroxypropyl methicellulose a cikin wani adadin ruwa, motsawa da ƙarfi, mai tsanani zuwa 80 ~ 90 ℃, sa'an nan kuma ƙara sauran hydroxypropyl methicellulose, kuma a karshe amfani da ruwan sanyi don kari. zuwa adadin da ake buƙata.
2.2 Hydroxypropyl methylcellulose shine ether wanda ba na ionic cellulose ba, maganinsa baya ɗaukar cajin ionic, baya hulɗa tare da salts na ƙarfe ko mahaɗin kwayoyin ionic, don tabbatar da cewa HPMC baya amsawa tare da sauran albarkatun ƙasa da abubuwan haɓakawa a cikin aiwatar da shirye-shiryen. samarwa.
2.3 Hydroxypropyl methylcellulose yana da ƙarfi anti-hankali, kuma tare da karuwar digiri na maye gurbin a cikin tsarin kwayoyin halitta, an kuma inganta anti-sensitivity. Magungunan da ke amfani da HPMC azaman abubuwan haɓakawa suna da ingantaccen inganci a cikin ingantaccen lokacin fiye da kwayoyi masu amfani da sauran abubuwan haɓaka na gargajiya (sitaci, dextrin, sukari mai foda).
2.4 Hydroxypropyl methylcellulose ba shi da kuzari. A matsayin mai maganin magunguna, ba a daidaita shi ko shayarwa, don haka ba ya samar da zafi a cikin magunguna da abinci. Yana da ƙayyadaddun zartarwa ga ƙarancin calorific, marasa gishiri, magungunan marasa allergenic da abinci ga masu ciwon sukari.
2.5HPMC yana da kwanciyar hankali ga acid da tushe, amma idan pH ya wuce 2 ~ 11 kuma zafin jiki mafi girma ko lokacin ajiya ya shafe shi, zai rage girman ripenness.
2.6 Hydroxypropyl methylcellulose bayani mai ruwa-ruwa na iya samar da aikin saman, yana nuna matsakaicin matsakaici da ƙimar tashin hankali na tsaka-tsakin. Yana da ingantaccen emulsification a cikin tsarin tsari guda biyu kuma ana iya amfani dashi azaman ingantaccen stabilizer da colloid mai kariya.
2.7 Hydroxypropyl methylcellulose aqueous bayani yana da kyau kwarai film-forming Properties, kuma shi ne mai kyau shafi abu ga Allunan da kwayoyi. Membran da aka yi da shi ba shi da launi kuma mai tauri. Idan an ƙara glycerol, ana iya ƙara yawan filastik. Bayan jiyya na saman, samfurin yana tarwatsewa a cikin ruwan sanyi, kuma ana iya sarrafa ƙimar rushewar ta canza yanayin pH. Ana amfani da shi a cikin shirye-shiryen jinkirin sakewa da shirye-shirye masu rufi.
3. Aikace-aikacen samfur
3.1. An yi amfani da shi azaman manne da wakili mai tarwatsewa
HPMC da ake amfani da su inganta da miyagun ƙwayoyi rushewa da mataki na saki aikace-aikace, za a iya kai tsaye narkar da a cikin sauran ƙarfi kamar m, low danko na HPMC narkar da cikin ruwa don samar da m zuwa hauren giwa m colloid bayani, Allunan, kwayoyi, granules a kan m da disintegrating. wakili, da babban danko don manne, kawai amfani da su saboda nau'ikan daban-daban da buƙatu daban-daban, babban shine 2% ~ 5%.
Maganin ruwa mai ruwa na HPMC da wani ƙayyadadden ƙwayar ethanol don yin ɗaure mai haɗawa; Misali: 2% HPMC Maganin ruwa mai gauraye da 55% ethanol bayani an yi amfani dashi don pelleting na amoxicillin capsules, ta yadda matsakaicin narkar da amoxicillin capsules ya karu daga 38% zuwa 90% ba tare da HPMC ba.
Ana iya yin HPMC da manne mai hade tare da maida hankali daban-daban na sitaci slurry bayan rushewa; Narkar da allunan masu rufin erythromycin sun karu daga 38.26% zuwa 97.38% lokacin da aka haɗa 2% HPMC da sitaci 8%.
2.2. Yi kayan shafa fim da kayan aikin fim
HPMC a matsayin kayan shafa mai ruwa mai narkewa yana da halaye masu zuwa: matsakaicin bayani danko; Tsarin sutura yana da sauƙi; Kyakkyawan kayan ƙirƙirar fim; Zai iya kiyaye siffar yanki, rubutu; Zai iya zama mai hana danshi; Iya launi, dandanon gyara. ANA AMFANI DA WANNAN KAYAN A MATSAYIN RUFE FILM RUWAN RUWAN KWALLIYA DA KWALLIYA MAI KYAU, KUMA GA RUFIN FIM BA RUWA BA MAI KYAU, ADADIN AMFANIN 2% -5%.
2.3, azaman wakili mai kauri da manne kariyar colloidal
HPMC da aka yi amfani da shi azaman wakili mai kauri shine 0.45% ~ 1.0%, ana iya amfani dashi azaman digon ido da wakili mai kauri na wucin gadi; Ana amfani da shi don haɓaka kwanciyar hankali na manne hydrophobic, hana haɓakar ƙwayoyin cuta, hazo, adadin da aka saba shine 0.5% ~ 1.5%.
2.4, a matsayin mai toshewa, jinkirin sakin kayan aiki, mai sarrafawa mai sarrafawa da wakili na pore
Ana amfani da samfurin danko mai girma na HPMC don shirya masu toshewa da wakilai masu sarrafawa na gaurayawar kayan kwarangwal masu dorewa da allunan kwarangwal na hydrophilic gel kwarangwal. Samfurin ƙarancin danko shine wakili mai haifar da pore don ci gaba-saki-saki ko sarrafawa-saki allunan don haka ana samun kashi na farko na warkewar irin waɗannan allunan cikin sauri, biye da ci gaba-saki-saki ko sarrafawa-saki don kiyaye tasiri mai yawa a cikin jini.
2.5. Gel da suppository matrix
Ana iya shirya suppositories na hydrogel da shirye-shiryen mannewa na ciki ta hanyar amfani da halayen haɓakar hydrogel wanda HPMC ke amfani da shi a cikin ruwa.
2.6 Abubuwan liƙa na halitta
An gauraya Metronidazole da HPMC da polycarboxylethylene 934 a cikin mahaɗa don yin allunan sakin da aka sarrafa bioadhesive mai ɗauke da 250mg. Gwajin rushewar in vitro ya nuna cewa shirye-shiryen da sauri ya kumbura cikin ruwa, kuma ana sarrafa sakin miyagun ƙwayoyi ta hanyar watsawa da shakatawar sarkar carbon. Aiwatar da dabba ya nuna cewa sabon tsarin sakin miyagun ƙwayoyi yana da mahimman kaddarorin mannewar halittu ga mucosa sublingual na bovine.
2.7, a matsayin taimakon dakatarwa
Babban danko na wannan samfurin shine taimako na dakatarwa mai kyau don shirye-shiryen dakatarwar ruwa, adadin sa na yau da kullun shine 0.5% ~ 1.5%.
4. Misalai na aikace-aikace
4.1 Film shafi bayani: HPMC 2kg, talc 2kg, Castor man 1000ml, Twain -80 1000ml, propylene glycol 1000ml, 95% ethanol 53000ml, ruwa 47000ml, pigment dace adadin. Akwai hanyoyi guda biyu don yin shi.
4.1.1 Shiri na ruwa mai narkewa mai rufaffiyar tufafi: Ƙara adadin da aka tsara na HPMC cikin 95% ethanol, jiƙa shi dare ɗaya, narkar da wani vector na pigment a cikin ruwa (tace idan ya cancanta), haɗa mafita guda biyu kuma a motsa a ko'ina don samar da mafita mai haske. . Mix 80% na maganin (20% don gogewa) tare da adadin da aka tsara na man Castor, Tween-80, da propylene glycol.
4.1.2 Shiri na insoluble pigment (kamar baƙin ƙarfe oxide) shafi ruwa HPMC aka jika a 95% ethanol na dare, da kuma ruwa da aka kara don yin 2% HPMC m bayani. An fitar da kashi 20% na wannan maganin don gogewa, sauran 80% na maganin da ƙarfe oxide an shirya su ta hanyar niƙa ruwa, sa'an nan kuma an ƙara adadin adadin wasu abubuwan da aka ba da izini kuma a gauraya su daidai don amfani. A shafi aiwatar da shafi ruwa: zuba da hatsi takardar a cikin sugar shafi tukunya, bayan juyawa, da zafi iska preheats zuwa 45 ℃, za ka iya fesa ciyar shafi, ya kwarara iko a 10 ~ 15ml / min, bayan spraying, ci gaba da bushe. tare da iska mai zafi na 5 ~ 10min zai iya fita daga cikin tukunya, saka a cikin bushewa don bushe fiye da 8h.
4.2a-interferon ido membrane 50μg na α-interferon aka narkar da a 10ml0.01ml hydrochloric acid, gauraye da 90ml ethanol da 0.5GHPMC, tace, mai rufi a kan wani juyi gilashin sanda, haifuwa a 60 ℃ da bushe a cikin iska. An yi wannan samfurin zuwa kayan fim.
4.3 Cotrimoxazole Allunan (0.4g± 0.08g) SMZ (80 raga) 40kg, sitaci (120 raga) 8kg, 3% HPMC ruwa bayani 18-20kg, magnesium stearate 0.3kg, TMP (80 raga) 8kg, da shirye-shiryen. Mix SMZ da TMP, sa'an nan kuma ƙara sitaci da Mix don 5 min. Tare da prefabricated 3% HPMC ruwa bayani, taushi abu, tare da 16 raga allon granulation, bushewa, sa'an nan tare da 14 raga allon dukan hatsi, ƙara magnesium stearate mix, tare da 12mm zagaye tare da kalmar (SMZco) stamping Allunan. Ana amfani da wannan samfurin musamman azaman ɗaure. Narkar da allunan shine 96%/20min.
4.4 Piperate Allunan (0.25g) piperate 80 raga 25kg, sitaci (120 raga) 2.1kg, magnesium stearate dace adadin. Hanyar samar da ita ita ce haxa acidic acid, sitaci, HPMC a ko'ina, tare da 20% ethanol taushi abu, 16 raga allo granulate, bushe, sa'an nan 14 raga allon dukan hatsi, da vector magnesium stearate, tare da 100mm madauwari bel kalma (PPA0.25). ) allunan stamping. Tare da sitaci azaman wakili mai tarwatsewa, adadin narkar da wannan kwamfutar hannu bai wuce 80%/2min ba, wanda ya fi irin wannan samfura a Japan.
4.5 Artificial hawaye HPMC-4000, HPMC-4500 ko HPMC-5000 0.3g, sodium chloride 0.45g, potassium chloride 0.37g, borax 0.19g, 10% ammonium chlorbenzylammonium bayani 0.02ml, ruwa ƙara zuwa 100ml. Hanyar samar da ita ana sanyawa HPMC a cikin ruwa 15ml, a 80 ~ 90 ℃ cikakkar ruwa a dauki a, ƙara 35ml ruwa, sa'an nan dauke da sauran sinadaran 40ml aqueous bayani gauraye ko'ina, sa'an nan kuma ƙara ruwa zuwa cikakken adadin, sa'an nan kuma gauraye daidai, tsaya dare. , a hankali zuba tacewa, tace a cikin akwati shãfe haske, haifuwa a 98 ~ 100 ℃ na 30min, wato, The pH ya tashi daga 8.4 ° C zuwa 8.6 ° C. Ana amfani da wannan samfurin don RASHIN HAWAYE, YANA DA KYAU GA HAWAYE, Lokacin amfani da microscopy na gida na baya, ana iya ƙara ƙimar wannan samfurin, 0.5% KYAUTA shine 0.5% KYAUTA. .
4.6 Meththorphan sarrafawa saki Allunan meththorphan resin gishiri 187.5mg, lactose 40.0mg, PVP70.0mg, tururi silica 10mg, 40.0 mGHPMC-603, 40.0mg ~ microcrystalline cellulose phthalate-102. An shirya shi azaman allunan ta hanyar al'ada. Ana amfani da wannan samfurin azaman kayan fitarwa mai sarrafawa.
4.7 Domin avantomycin ⅳ allunan, 2149g avantomycin ⅳ monohydrate da 1000ml isopropyl cakuda ruwa na 15% (mass maida hankali) eudragitL-100 (9: 1) aka zuga, gauraye, granulated, da kuma bushe a 35 ℃. Busashen granules 575g da 62.5g hydroxypropylocellulose E-50 an gauraye su sosai, sannan aka saka 7.5g stearic acid da 3.25g magnesium stearate a cikin allunan don samun ci gaba da sakin vanguard mycinⅳ allunan. Ana amfani da wannan samfurin azaman kayan sakin jinkirin.
4.8 Nifedipine ci gaba-release granules 1 part nifedipine, 3 sassa hydroxypropyl methyl cellulose da 3 sassa ethyl cellulose aka gauraye da gauraye sauran ƙarfi (ethanol: methylene chloride = 1: 1), da kuma 8 sassa masara sitaci aka kara don samar da granules ta matsakaici-soluble. hanya. Matsakaicin sakin miyagun ƙwayoyi na granules bai shafi canjin yanayin pH ba kuma ya kasance a hankali fiye da na granules na kasuwanci. Bayan sa'o'i 12 na maganin baka, ƙwayar jinin ɗan adam ya kasance 12mg/ml, kuma babu wani bambanci na mutum.
4.9 Propranhaol hydrochloride ci gaba da saki capsule Propranhaol hydrochloride 60kg, microcrystalline cellulose 40kg, ƙara 50L ruwa don yin granules. HPMC1kg da EC 9kg aka gauraye a cikin gauraye sauran ƙarfi (methylene chloride: methanol = 1: 1) 200L don yin shafi bayani, tare da kwarara kudi na 750ml / min fesa a kan mirgina mai siffar zobe barbashi, mai rufi barbashi ta cikin pore size of 1.4. mm allon gabaɗayan barbashi, sannan a cika su cikin capsule na dutse tare da na'ura mai cika capsule na yau da kullun. Kowane capsule ya ƙunshi 160mg na propranolol hydrochloride spherical particles.
4.10 Naprolol HCL skeleton Allunan an shirya su ta hanyar haɗuwa da naprolol HCL: HPMC: CMC-NA a cikin rabo na 1: 0.25: 2.25. Adadin sakin magungunan ya kusan kusan odar sifili a cikin sa'o'i 12.
Hakanan ana iya yin wasu magunguna da kayan kwarangwal masu gauraya, kamar su metoprolol: HPMC: CMC-NA bisa ga: 1:1.25:1.25; Allylprolol: HPMC daidai da 1: 2.8: 2.92 rabo. Adadin sakin magungunan ya kusan kusan odar sifili a cikin sa'o'i 12.
4.11 Allunan kwarangwal na kayan gauraye na abubuwan da suka samo asali na ethylaminosine an shirya su ta hanyar al'ada ta hanyar amfani da cakuda micro foda silica gel: CMC-NA: HPMC 1: 0.7: 4.4. Ana iya fitar da miyagun ƙwayoyi na 12h duka a cikin vitro da a cikin vivo, kuma tsarin sakin layi yana da kyakkyawar alaƙa. Sakamakon ingantaccen gwajin kwanciyar hankali bisa ga dokokin FDA sun yi hasashen cewa rayuwar ajiyar wannan samfurin ya kai shekaru 2.
4.12 HPMC (50mPa·s) (5 sassa), HPMC (4000 mPa·s) (3 sassa) da HPC1 aka narkar da a cikin 1000 sassa na ruwa, 60 sassa acetaminophen da 6 sassa silica gel aka kara, zuga tare da homogenizer, da kuma fesa bushewa. Wannan samfurin ya ƙunshi kashi 80% na babban magani.
4.13 Theophylline hydrophilic gel kwarangwal Allunan aka lissafta bisa ga jimlar nauyin kwamfutar hannu, 18% -35% theophylline, 7.5% -22.5% HPMC, 0.5% lactose, da kuma adadin da ya dace na hydrophobic lubricant aka kullum shirya a cikin sarrafawa saki Allunan, wanda zai iya. kula da ingantaccen taro na jini na jikin mutum na awanni 12 bayan gudanar da baki.
Lokacin aikawa: Satumba-20-2022