Nau'i: kayan shafa; Kayan membrane; Kayan polymer masu sarrafa sauri don shirye-shiryen sakin a hankali; Wakilin daidaitawa; Taimakon dakatarwa, manne kwamfutar hannu; Wakilin mannewa mai ƙarfafawa.
1. Gabatar da samfur
Wannan KAYAYYAKI AN SAMU CEWA BA TA ILON-IONIC CELLULOSE ETHER BA, ana iya gani a waje a matsayin farin foda, mara ƙamshi da ɗanɗano, yana narkewa a cikin ruwa da yawancin sinadarai masu narkewa na halitta, yana kumbura a cikin ruwan sanyi don sharewa ko kuma ɗan turbidBIDized colloidal. Maganin ruwa yana da aikin saman, babban bayyananne da aiki mai karko. HPMC yana da mallakar gel mai zafi. Bayan dumama, maganin ruwa na samfurin yana samar da ruwan gel, sannan yana narkewa bayan sanyaya. Zafin gel na takamaiman bayanai daban-daban ya bambanta. Narkewa yana canzawa tare da danko, danko yana raguwa, mafi girman narkewa, ƙayyadaddun bayanai daban-daban na kaddarorin HPMC suna da wasu bambance-bambance, ƙimar pH ba ta shafar HPMC.
Zafin ƙonewa na bazata, yawan da ba shi da yawa, yawan gaske da kuma zafin canjin gilashi sun kasance 360℃, 0.341g/cm3, 1.326g/cm3 da 170 ~ 180℃, bi da bi. Bayan dumamawa, sai ya yi launin ruwan kasa a 190 ~ 200°C kuma ya ƙone a 225 ~ 230°C.
HPMC kusan ba ya narkewa a cikin chloroform, ethanol (95%), da diethyl ether, kuma yana narkewa a cikin cakuda ethanol da methylene chloride, cakuda methanol da methylene chloride, da cakuda ruwa da ethanol. Wasu matakan HPMC suna narkewa a cikin cakuda acetone, methylene chloride, da 2-propanol, da kuma a cikin sauran sinadaran sinadarai na halitta.
Tebur 1: Alamun fasaha
aikin
Ma'auni,
60 gd (2910).
65GD(2906)
75GD(2208)
% na Metoxy
28.0-32.0
27.0-30.0
19.0-24.0
% na Hydroxypropoxy
7.0-12.0
4.0-7.5
4.0-12.0
Zafin gel ℃
56-64.
62.0-68.0
70.0-90.0
Danko mai kama da na'urar aunawa (mpa).
3,5,6,15,50,4000
50400 0
100400 0150 00100 000
Rage nauyi mai bushewa %
5.0 ko ƙasa da haka
Ragowar ƙonawa %
1.5 ko ƙasa da haka
pH
4.0-8.0
Karfe mai nauyi
20 ko ƙasa da haka
arsenic
2.0 ko ƙasa da haka
2. Siffofin samfur
2.1 Ana narkar da Hydroxypropyl methylcellulose a cikin ruwan sanyi don samar da ruwan colloidal mai ƙauri. Muddin an ƙara shi a cikin ruwan sanyi kuma an ɗan juya shi kaɗan, ana iya narkar da shi zuwa ruwan haske. Akasin haka, ba ya narkewa a cikin ruwan zafi sama da 60℃ kuma yana iya kumbura kawai. A cikin shirya ruwan hydroxypropyl methicellulose, ya fi kyau a ƙara wani ɓangare na hydroxypropyl methicellulose a cikin wani adadin ruwa, a juya sosai, a dumama shi zuwa 80 ~ 90℃, sannan a ƙara sauran hydroxypropyl methicellulose, sannan a ƙarshe a yi amfani da ruwan sanyi don ƙara yawan da ake buƙata.
2.2 Hydroxypropyl methylcellulose wani sinadari ne na cellulose wanda ba ionic ba, ruwansa baya ɗauke da cajin ionic, baya hulɗa da gishirin ƙarfe ko mahaɗan ionic na halitta, don tabbatar da cewa HPMC ba ta amsawa da wasu kayan aiki da abubuwan da suka dace yayin samar da shiri ba.
2.3 Hydroxypropyl methylcellulose yana da ƙarfin hana jin zafi, kuma tare da ƙaruwar matakin maye gurbin tsarin kwayoyin halitta, ana kuma ƙara ƙarfin hana jin zafi. Magungunan da ke amfani da HPMC a matsayin abubuwan taimako suna da inganci mafi kyau a cikin lokacin tasiri fiye da magunguna da ke amfani da wasu abubuwan taimako na gargajiya (sitaci, dextrin, sukari foda).
2.4 Hydroxypropyl methylcellulose ba ya aiki yadda ya kamata a cikin metabolism. A matsayinsa na maganin magunguna, ba ya narkewa ko sha, don haka baya samar da zafi a cikin magunguna da abinci. Yana da amfani na musamman ga ƙananan kalori, marasa gishiri, marasa alerji da abinci ga masu ciwon sukari.
2.5HPMC yana da daidaito idan aka kwatanta da acid da tushe, amma idan pH ya wuce 2 ~ 11 kuma yanayin zafi mafi girma ko tsawon lokacin ajiya ya shafi shi, zai rage matakin nunarsa.
2.6 Maganin ruwa na Hydroxypropyl methylcellulose na iya samar da aikin saman, yana nuna matsakaicin matsin lamba a saman da kuma tsakanin fuskoki. Yana da ingantaccen emulsification a cikin tsarin matakai biyu kuma ana iya amfani da shi azaman mai daidaita aiki da kuma colloid mai kariya.
2.7 Maganin ruwa mai suna Hydroxypropyl methylcellulose yana da kyawawan halaye na samar da fim, kuma abu ne mai kyau na shafa allunan da kwayoyi. Famfon da aka samar ba shi da launi kuma yana da tauri. Idan aka ƙara glycerol, ana iya ƙara ƙarfinsa. Bayan an yi maganin saman, ana watsa samfurin a cikin ruwan sanyi, kuma ana iya sarrafa ƙimar narkewar ta hanyar canza yanayin pH. Ana amfani da shi a cikin shirye-shiryen sakin jiki a hankali da shirye-shiryen da aka shafa a cikin enteric.
3. Aikace-aikacen samfur
3.1. Ana amfani da shi azaman manne da kuma abin da ke wargazawa
Ana amfani da HPMC don haɓaka narkewar maganin da matakin aikace-aikacen fitarwa, ana iya narkar da shi kai tsaye a cikin ruwan narkewa azaman manne, ƙarancin ɗanɗano na HPMC da aka narkar a cikin ruwa don samar da mafita mai santsi zuwa ga hauren giwa, allunan, kwayoyi, granules akan manne da wakilin wargazawa, da kuma babban ɗanɗano na manne, ana amfani da shi ne kawai saboda nau'in da buƙatu daban-daban, gabaɗaya shine 2% ~ 5%.
Maganin ruwa na HPMC da wani yawan ethanol don yin mahaɗin haɗaka; Misali: An yi amfani da maganin ruwa na HPMC 2% da aka haɗa da maganin ethanol 55% don cire ƙwayoyin amoxicillin, ta yadda matsakaicin narkewar ƙwayoyin amoxicillin ya ƙaru daga 38% zuwa 90% ba tare da HPMC ba.
Ana iya yin HPMC da manne mai hadewa tare da yawan sinadarin sitaci daban-daban bayan narkewa; Narkewar ƙwayoyin erythromycin masu rufi a cikin enteric ya ƙaru daga 38.26% zuwa 97.38% lokacin da aka haɗa 2% HPMC da 8% sitaci.
2.2. Yi kayan shafa fim da kayan samar da fim
HPMC a matsayin kayan shafa mai narkewar ruwa yana da halaye masu zuwa: matsakaicin dankowar mafita; Tsarin shafa mai sauƙi ne; Kyakkyawan siffa ta samar da fim; Zai iya kiyaye siffar kayan, rubutu; Zai iya zama mai hana danshi; Zai iya yin launi, ɗanɗanon gyara. Ana amfani da wannan samfurin azaman shafa fim mai narkewar ruwa ga Allunan da ƙwayoyin cuta masu ƙarancin danko, kuma ga shafa fim ɗin da ba ya tushen ruwa mai yawan danko, adadin amfani shine 2%-5%.
2.3, a matsayin wakili mai kauri da kuma manne mai kariya daga colloidal
Ana amfani da HPMC azaman wakili mai kauri shine 0.45% ~ 1.0%, ana iya amfani dashi azaman digo na ido da wakili mai kauri na wucin gadi; Ana amfani dashi don ƙara kwanciyar hankali na manne mai hana ruwa, hana haɗuwa da barbashi, ruwan sama, yawan da aka saba amfani dashi shine 0.5% ~ 1.5%.
2.4, a matsayin mai toshewa, kayan sakin jiki a hankali, wakilin sakin jiki mai sarrafawa da kuma wakilin rami
Ana amfani da samfurin HPMC mai yawan viscosity don shirya masu toshewa da kuma wakilan sakin da aka sarrafa na allunan sakin kwarangwal masu gauraye da allunan sakin kwarangwal masu hydrophilic. Tsarin ƙarancin viscosity wakili ne mai haifar da ramuka don allunan sakin da aka ci gaba ko kuma waɗanda aka sarrafa don a sami maganin farko na irin waɗannan allunan cikin sauri, sannan a biyo baya da sakin da aka ci gaba ko sakin da aka sarrafa don kiyaye yawan da ke cikin jini.
2.5. Gel da matrix na suppository
Ana iya shirya maganin Hydrogel da shirye-shiryen manne na ciki ta hanyar amfani da halayyar samuwar hydrogel da HPMC ke amfani da shi a cikin ruwa.
2.6 Kayan manne na halitta
An haɗa Metronidazole da HPMC da polycarboxyethylene 934 a cikin mahaɗi don yin ƙwayoyin saki masu sarrafa biomandhesive waɗanda ke ɗauke da 250mg. Gwajin narkewar in vitro ya nuna cewa maganin ya kumbura cikin sauri cikin ruwa, kuma sakin maganin ya kasance ƙarƙashin tasirin yaɗuwa da sassauta sarkar carbon. Aiwatar da dabbobi ya nuna cewa sabon tsarin sakin magani yana da mahimman kaddarorin mannewa ga mucosa na ƙarƙashin harshe na shanu.
2.7, a matsayin taimakon dakatarwa
Babban danko na wannan samfurin yana da kyau wajen taimakawa wajen dakatar da ruwa, yawan maganin da aka saba amfani da shi shine 0.5% ~ 1.5%.
4. Misalan aikace-aikace
4.1 Maganin rufe fuska: HPMC 2kg, talc 2kg, man castor 1000ml, Twain -80 1000ml, propylene glycol 1000ml, 95% ethanol 53000ml, ruwa 47000ml, adadin da ya dace da launin. Akwai hanyoyi guda biyu don yin sa.
4.1.1 Shirya ruwan tufafi mai rufi da launin ruwan kasa: A zuba adadin HPMC da aka tsara a cikin kashi 95% na ethanol, a jiƙa shi cikin dare, a narkar da wani sinadarin launin ruwan kasa a cikin ruwa (idan ya cancanta), a haɗa ruwan biyu a gauraya daidai gwargwado don samar da ruwan da ya dace. A haɗa kashi 80% na ruwan (20% don gogewa) da adadin man castor, Tween-80, da propylene glycol da aka tsara.
4.1.2 An jiƙa ruwan shafa mai na HPMC wanda ba ya narkewa (kamar ƙarfe oxide) a cikin ruwan ethanol 95 cikin dare, sannan aka ƙara ruwa don yin maganin HPMC mai haske 2%. An cire kashi 20% na wannan maganin don gogewa, kuma an shirya sauran maganin 80% da ƙarfe oxide ta hanyar niƙa ruwa, sannan aka ƙara adadin sauran abubuwan da aka rubuta kuma aka gauraya daidai gwargwado don amfani. Tsarin shafa ruwan shafa: zuba takardar hatsi a cikin tukunyar shafa sukari, bayan juyawa, iskar zafi tana dumama zuwa 45℃, zaku iya fesa murfin ciyarwa, sarrafa kwararar ruwa cikin 10 ~ 15ml/min, bayan fesawa, ci gaba da bushewa da iska mai zafi na tsawon minti 5 ~ 10 ana iya cirewa daga tukunya, a saka a cikin na'urar busarwa don bushewa na tsawon awanni 8.
An narkar da membrane na ido mai siffar 4.2α-interferon mai girman 50μg na α-interferon a cikin 10ml0.01ml hydrochloric acid, an gauraya shi da ethanol 90ml da 0.5GHPMC, an tace shi, an shafa shi a kan sandar gilashi mai juyawa, an yi masa maganin kashe ƙwayoyin cuta a zafin 60℃ sannan aka busar da shi a iska. An yi wannan samfurin a cikin fim.
Allunan Cotrimoxazole 4.3 (0.4g±0.08g) SMZ (raga 80) 40kg, sitaci (raga 120) 8kg, 3% maganin ruwa na HPMC 18-20kg, magnesium stearate 0.3kg, TMP (raga 80) 8kg, hanyar shiryawa ita ce a haɗa SMZ da TMP, sannan a ƙara sitaci a gauraya na tsawon minti 5. Tare da maganin ruwa na HPMC 3% da aka riga aka shirya, abu mai laushi, tare da granulation na allo na raga 16, bushewa, sannan tare da allo na raga 14 na gaba ɗaya, a ƙara cakuda magnesium stearate, tare da zagaye na 12mm tare da allunan stamping na word (SMZco). Ana amfani da wannan samfurin galibi azaman manne. Narkewar allunan shine 96%/minti 20.
Allunan Piperate 4.4 (0.25g) piperate raga 80 25kg, sitaci (raga 120) 2.1kg, magnesium stearate gwargwadon adadin da ya dace. Hanyar samar da ita ita ce a haɗa pipeoperic acid, sitaci, HPMC daidai gwargwado, tare da kayan laushi na ethanol 20%, granulate mai allo 16, busasshe, sannan a sami allo mai allo 14 na dukkan hatsi, tare da vector magnesium stearate, tare da allunan tambarin bel mai zagaye 100mm (PPA0.25). Tare da sitaci a matsayin wakili mai wargazawa, ƙimar narkewar wannan allunan ba ta ƙasa da 80%/minti 2 ba, wanda ya fi girma fiye da samfuran makamantan su a Japan.
4.5 Tage na wucin gadi HPMC-4000, HPMC-4500 ko HPMC-5000 0.3g, sodium chloride 0.45g, potassium chloride 0.37g, borax 0.19g, 10% maganin ammonium chlorbenzylammonium 0.02ml, an ƙara ruwa a cikin 100ml. Hanyar samar da shi ita ce a sanya HPMC a cikin ruwa 15ml, a zafin jiki na 80 ~ 90℃, a zuba ruwa 35ml, sannan a dauke sauran sinadaran ruwan 40ml da aka gauraya daidai gwargwado, a zuba ruwa a daidai gwargwado, sannan a gauraya daidai gwargwado, a tsaya a cikin dare, a zuba tacewa a hankali, a tace a cikin akwati da aka rufe, a yi masa tsafta a zafin jiki na 98 ~ 100℃ na tsawon minti 30, wato, pH yana tsakanin 8.4 ° C zuwa 8.6 ° C. Ana amfani da wannan samfurin don ƙarancin yayyagewa, yana da kyau a maye gurbinsa da yayyagewa, idan aka yi amfani da shi don na'urar duba na'urar a baya, ana iya ƙara shi yadda ya kamata. YADDA AKE AMFANI DA WANNAN KAYAN, 0.7% ~ 1.5% ya dace.
4.6 Allunan da aka sarrafa na Meththorphan gishirin resin meththorphan 187.5mg, lactose 40.0mg, PVP70.0mg, silica tururi 10mg, 40.0 mGHPMC-603, 40.0mg ~ microcrystalline cellulose phthalate-102 da magnesium stearate 2.5mg. Ana shirya shi azaman allunan ta hanyar da aka saba. Ana amfani da wannan samfurin azaman kayan fitarwa mai sarrafawa.
4.7 Ga allunan avantomycin ⅳ, an juya 2149g avantomycin ⅳ monohydrate da cakuda ruwa isopropyl 1000ml na 15% (yawan taro) eudragitL-100 (9:1) a hankali, an gauraya, an yi masa granulated, sannan aka busar da su a zafin 35℃. An gauraya busassun granules 575g da 62.5g hydroxypropyloculose E-50 sosai, sannan aka ƙara stearic acid 7.5g da magnesium stearate 3.25g a cikin allunan don samun ci gaba da sakin allunan vanguard mycin ⅳ. Ana amfani da wannan samfurin azaman kayan fitarwa a hankali.
4.8 An haɗa ƙwayoyin Nifedipine masu jure sakin jiki kashi 1 na nifedipine, sassa 3 na hydroxypropyl methyl cellulose da sassa 3 na ethyl cellulose da gaurayen mai (ethanol: methylene chloride = 1:1), kuma an ƙara sassa 8 na sitaci masara don samar da ƙwayoyin ta hanyar matsakaici mai narkewa. Yawan sakin ƙwayoyin magani na ƙwayoyin bai shafi canjin pH na muhalli ba kuma ya yi ƙasa da na ƙwayoyin da ake samu a kasuwa. Bayan awanni 12 na shan magani ta baki, yawan jinin ɗan adam ya kai 12mg/ml, kuma babu wani bambanci na mutum ɗaya.
4.9 Propranhaol hydrochloride ya sami damar sakin ƙwayoyin Propranhaol hydrochloride 60kg, microcrystalline cellulose 40kg, ya ƙara ruwa 50L don yin granules. An haɗa HPMC1kg da EC 9kg a cikin ruwan da aka haɗa (methylene chloride: methanol = 1:1) 200L don yin maganin shafawa, tare da feshi na 750ml/min a kan ƙwayoyin da ke birgima, an shafa ƙwayoyin da aka shafa ta cikin girman ramin allon 1.4mm gaba ɗaya, sannan a cika su cikin ruwan dutse tare da injin cika ƙwayoyin. Kowane ƙwayar tana ɗauke da 160mg na ƙwayoyin propranolol hydrochloride masu siffar zobe.
An shirya allunan kwarangwal na Naprolol HCL guda 4.10 ta hanyar haɗa naprolol HCL :HPMC: CMC-NA a rabo na 1:0.25:2.25. Yawan sakin maganin ya kusa zama sifili cikin awanni 12.
Ana iya yin wasu magunguna da kayan kwarangwal iri-iri, kamar su metoprolol: HPMC: CMC-NA bisa ga: 1:1.25:1.25; Allylprolol:HPMC bisa ga rabon 1:2.8:2.92. Yawan sakin maganin ya kusa zama sifili cikin awanni 12.
4.11 An shirya allunan kwarangwal na kayan gauraye na ethylaminosine ta hanyar da aka saba amfani da ita ta amfani da cakuda ƙaramin foda na silica: CMC-NA :HPMC 1:0.7:4.4. Ana iya sakin maganin na tsawon awanni 12 duka a cikin vitro da kuma a cikin jiki, kuma tsarin sakin layi yana da kyakkyawar alaƙa. Sakamakon gwajin kwanciyar hankali mai sauri bisa ga ƙa'idodin FDA ya annabta cewa tsawon lokacin adana wannan samfurin zai kai har zuwa shekaru 2.
4.12 HPMC (50mPa·s) (sassa 5), HPMC (4000 mPa·s) (sassa 3) da HPC1 an narkar da su a cikin sassa 1000 na ruwa, an ƙara sassa 60 na acetaminophen da sassa 6 na silica gel, an juya su da homogenizer, sannan aka fesa su a busasshe. Wannan samfurin ya ƙunshi kashi 80% na babban magani.
4.13 An ƙididdige allunan kwarangwal na Theophylline hydrophilic bisa ga jimlar nauyin allunan, an shirya 18%-35% theophylline, 7.5%-22.5% HPMC, 0.5% lactose, da kuma adadin man shafawa mai kama da hydrophobic yawanci a cikin allunan da aka sarrafa, waɗanda za su iya kiyaye yawan jinin jikin ɗan adam na tsawon awanni 12 bayan shan magani ta baki.
Lokacin Saƙo: Fabrairu-05-2024