1. Asalin yanayin HPMC
Hypromellose, sunan Ingilishi hydroxypropyl methylcellulose, wanda aka fi sani da HPMC. Tsarin kwayoyin halittarsa shine C8H15O8-(C10Hl8O6)n-C8Hl5O8, kuma nauyin kwayoyin halittar shine kimanin 86,000. Wannan samfurin kayan haɗin kai ne, wanda yake ɓangare na ƙungiyar methyl kuma wani ɓangare na polyhydroxypropyl ether na cellulose. Ana iya ƙera shi ta hanyoyi biyu: ɗaya shine a magance methyl cellulose na matakin da ya dace tare da NaOH, sannan a yi aiki da propylene oxide a ƙarƙashin zafin jiki mai yawa da matsin lamba mai yawa. Dole ne a dage lokacin amsawa don ba da damar ƙungiyoyin methyl da hydroxypropyl su haɗu da ether. Siffar tana da alaƙa da zoben anhydroglucose na cellulose, kuma tana iya kaiwa matakin da ake so; ɗayan kuma shine a yi amfani da auduga ko zare na itace da caustic soda, sannan a samu ta hanyar yin aiki da methane da propylene oxide da aka yi da chlorine a jere, sannan a ƙara tacewa, a yi shi da foda ko granule mai kyau da daidaito. HPMC nau'in cellulose ne na tsirrai na halitta, kuma yana da kyau wajen samar da sinadarai masu amfani da magunguna, wanda ke da tushe mai faɗi. A halin yanzu, ana amfani da shi sosai a gida da waje, kuma yana ɗaya daga cikin sinadaran da ke samar da sinadarai masu amfani da magunguna mafi girma a tsakanin magungunan da ake sha.
Launin wannan samfurin fari ne zuwa fari mai kama da madara, ba shi da guba kuma ba shi da ɗanɗano, kuma foda ne mai laushi ko mai laushi, mai sauƙin gudana. Yana da ƙarfi idan aka fallasa shi ga haske da danshi. Yana kumbura a cikin ruwan sanyi don samar da ruwan colloidal mai launin madara mai ɗanɗano tare da ɗanɗano mai yawa. Lamarin canzawar sol-gel na iya faruwa saboda canjin zafin jiki na wani yawan maganin. Yana da sauƙin narkewa a cikin kashi 70% na barasa ko dimethyl ketone, kuma ba zai narke a cikin anhydrous alcohol, chloroform ko ethoxyethane ba.
Hypromellose yana da kyakkyawan kwanciyar hankali lokacin da pH ɗin yake tsakanin 4.0 da 8.0, kuma yana iya wanzuwa daidai tsakanin 3.0 da 11.0. Bayan adanawa na tsawon kwanaki 10 a zafin jiki na 20°C da kuma ɗanɗanon da ya kai 80%, ƙimar sha danshi na HPMC shine 6.2%.
Saboda bambancin da ke cikin abubuwan da ke cikin maye biyu a cikin tsarin hypromellose, methoxy da hydroxypropyl, nau'ikan samfura daban-daban sun bayyana. A cikin takamaiman yawan samfura, nau'ikan samfura daban-daban suna da takamaiman danko kuma zafin jiki na thermal gelation, saboda haka, yana da halaye daban-daban kuma ana iya amfani da shi don dalilai daban-daban. Magungunan magunguna na ƙasashe daban-daban suna da ƙayyadaddun bayanai da maganganu daban-daban na samfurin: European Pharmacopoeia ya dogara ne akan nau'ikan nau'ikan danko daban-daban da matakai daban-daban na maye gurbin samfuran da ke kasuwa. Ana bayyana shi ta hanyar daraja da lamba. Naúrar ita ce mPa•s. Bayan ƙara lambobi 4 don nuna abun ciki da nau'in kowane maye gurbin hypromellose, misali, hypromellose 2208, lambobi biyu na farko suna wakiltar kimanin kashi na ƙungiyar methoxy, lambobi biyu na ƙarshe suna wakiltar hydroxypropyl Kimanin kashi na lokuta.
2. Hanyar narkar da HPMC a cikin ruwa
2.1 Hanyar ruwan zafi
Tunda hypromellose baya narkewa a cikin ruwan zafi, ana iya watsa shi a cikin ruwan zafi a matakin farko, sannan idan ya sanyaya, an bayyana hanyoyi guda biyu na yau da kullun kamar haka:
(1) Sanya ruwan zafi da ake buƙata a cikin akwati sannan a dafa shi zuwa kimanin digiri 70 na Celsius. A hankali a zuba samfurin a hankali ana juyawa. Da farko, samfurin yana shawagi a saman ruwan, sannan a hankali ya samar da slurry. A kwantar da slurry ɗin.
(2) A zuba 1/3 ko 2/3 na adadin ruwan da ake buƙata a cikin akwati a dumama shi zuwa 70°C don watsa ruwan don shirya ruwan zafi, sannan a ƙara sauran ruwan sanyi ko ruwan ƙanƙara a cikin ruwan zafi. A cikin slurry, a sanyaya cakuda bayan an gauraya.
2.2 Hanyar haɗa foda
Ana watsa barbashin foda da sauran sinadaran foda iri ɗaya ko mafi girma gaba ɗaya ta hanyar busasshiyar gauraya, sannan a ƙara ruwa don narkewa. A wannan lokacin, ana iya narkar da hypromellose ba tare da haɗa shi ba.
3. Fa'idodin HPMC
3.1 Ruwan sanyi yana narkewa
Yana narkewa a cikin ruwan sanyi ƙasa da 40°C ko kuma kashi 70% na ethanol. Ba ya narkewa a cikin ruwan zafi sama da 60°C, amma ana iya yin gelled.
3.2 Rashin daidaiton sinadarai
Hypromellose (HPMC) wani nau'in cellulose ether ne wanda ba ionic ba. Maganinsa ba shi da cajin ionic kuma baya hulɗa da gishirin ƙarfe ko mahaɗan ionic na halitta. Saboda haka, sauran abubuwan da ke taimakawa ba sa amsawa da shi yayin shirye-shiryen.
3.3 Kwanciyar hankali
Yana da daidaito idan aka kwatanta da acid da alkali, kuma ana iya adana shi na dogon lokaci tsakanin pH 3 zuwa 1l, kuma dankonsa ba shi da wani canji a bayyane. Maganin ruwa na hypromellose (HPMC) yana da tasirin hana mold kuma yana iya kiyaye kwanciyar hankali mai kyau yayin ajiya na dogon lokaci. Magungunan da ke amfani da HPMC suna da kwanciyar hankali mafi kyau fiye da waɗanda ke amfani da sinadaran gargajiya (kamar dextrin, sitaci, da sauransu).
3.4 Daidaita danko
Ana iya haɗa nau'ikan danko daban-daban na HPMC a cikin rabo daban-daban, kuma dankonsa na iya canzawa bisa ga wani ƙa'ida, kuma yana da kyakkyawar alaƙar layi, don haka ana iya zaɓarsa bisa ga buƙatun.
3.5 Rashin kuzarin rayuwa
Ba a sha ko kuma a narkar da HPMC a cikin jiki, kuma ba ya samar da adadin kuzari, don haka yana da aminci ga magungunan magani.
3.6 Tsaro
Gabaɗaya ana kyautata zaton cewa HPMC abu ne da ba shi da guba kuma ba ya haifar da haushi. Matsakaicin maganin da ake buƙata don kashe beraye shine 5g/kg, kuma matsakaicin maganin da ake buƙata don kashe beraye shine 5.2g/kg. Yawan da ake buƙata a kowace rana ba shi da lahani ga jikin ɗan adam.
4. Amfani da HPMC a cikin shirye-shirye
4.1 Ana amfani da shi azaman kayan shafa fim da kayan samar da fim
Ana amfani da Hypromellose (HPMC) a matsayin kayan kwamfutar hannu mai rufi da fim. Idan aka kwatanta da allunan da aka rufe da fata na gargajiya kamar allunan da aka rufe da sukari, allunan da aka rufe ba su da wata fa'ida a bayyane wajen ɓoye ɗanɗano da kamanninsu, amma taurinsu da ɗanɗanonsu, sha danshi, wargajewa, ƙaruwar nauyi a fuska da sauran alamun inganci sun fi kyau. Ana amfani da ƙarancin ɗanɗanon wannan samfurin a matsayin kayan shafa fim mai narkewa a ruwa don allunan da allunan, kuma ana amfani da babban ɗanɗanon azaman kayan shafa fim don tsarin narkewar halitta. Yawan amfani yawanci shine 2.0%-20%.
4.2 a matsayin abin ɗaurewa da kuma mai wargazawa
Ana iya amfani da ƙarancin ɗanɗano na wannan samfurin a matsayin abin ɗaurewa da kuma narkar da shi ga allunan, kwayoyi, da granules, kuma ana iya amfani da babban ɗanɗano a matsayin abin ɗaurewa kawai. Yawan da ake buƙata ya bambanta dangane da samfura da buƙatu daban-daban. Gabaɗaya, adadin abin ɗaurewa da ake amfani da shi don allunan granulation busasshe shine 5%, kuma adadin abin ɗaurewa da ake amfani da shi don allunan granulation da aka jika shine 2%.
4.3 A matsayin wakilin dakatarwa
Maganin dakatarwa wani sinadari ne mai kama da gel mai kama da ruwa. Amfani da maganin dakatarwa a cikin maganin dakatarwa na iya rage saurin narkewar ƙwayoyin cuta, kuma ana iya haɗa shi da saman ƙwayoyin cuta don hana ƙwayoyin cuta su zama polymer da taruwa zuwa taro. Maganin dakatarwa yana taka muhimmiyar rawa wajen samar da dakatarwa. HPMC nau'in maganin dakatarwa ne mai kyau. Maganin colloidal da aka narkar a cikinsa zai iya rage tashin hankali na haɗin gwiwa mai ƙarfi da ruwa da kuma kuzarin kyauta akan ƙananan ƙwayoyin cuta masu ƙarfi, ta haka yana haɓaka kwanciyar hankali na tsarin watsawa iri-iri. Wannan samfurin shiri ne na ruwa mai ƙarfi wanda aka shirya azaman maganin dakatarwa. Yana da kyakkyawan tasirin dakatarwa, mai sauƙin sake wargajewa, ba ya mannewa, kuma ƙananan ƙwayoyin cuta masu laushi. Adadin da aka saba shine 0.5% zuwa 1.5%.
4.4 Ana amfani da shi azaman 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 don shirya allunan gel matrix mai dorewa, masu hana ruwa gudu da kuma wakilai masu sarrafawa don allunan matrix masu dorewa. Yana da tasirin jinkirta sakin magani. Yawan amfani da shi shine 10% ~ 80% (W / W). Ana amfani da ƙarancin matakin danko a matsayin wakili mai samar da ramuka don samar da tsari mai dorewa ko mai sarrafawa. Ana iya isa ga allurar farko da ake buƙata don tasirin magani na wannan nau'in allunan cikin sauri, sannan ana yin tasirin sakin da ya ci gaba ko kuma mai sarrafawa, kuma ana kiyaye ingantaccen yawan magungunan jini a jiki. Hypromellose hydrates don samar da layin gel lokacin da ya haɗu da ruwa. Hanyar sakin magani daga allunan matrix galibi shine yaduwar layin gel da lalata layin gel.
4.5 Manna mai kariya da ake amfani da shi azaman mai kauri da kuma colloid
Idan aka yi amfani da wannan samfurin a matsayin mai kauri, yawan da aka saba samu shine 0.45% ~ 1.0%. Wannan samfurin kuma zai iya ƙara kwanciyar hankali na manne mai kama da hydrophobic, samar da colloid mai kariya, hana haɗuwar ƙwayoyin cuta da haɗuwa, ta haka yana hana samuwar laka. Yawan da aka saba samu shine 0.5% ~ 1.5%.
4.6 Ana amfani da shi azaman kayan capsules
Yawanci, sinadarin harsashin capsule na capsule galibi gelatin ne. Tsarin samar da harsashin capsule na Ming abu ne mai sauƙi, amma akwai wasu matsaloli da abubuwan da suka faru kamar rashin kariyar danshi da magungunan da ke da alaƙa da iskar oxygen, rage narkewar magani, da kuma jinkirin wargajewar harsashin capsule yayin ajiya. Saboda haka, ana amfani da hypromellose a madadin kayan capsule a cikin shirya capsules, wanda ke inganta yadda ake mold da tasirin amfani da capsule, kuma an yaɗa shi sosai a gida da waje.
4.7 A matsayin mai ɗaurewa
Fasaha ta biomadhesive, amfani da sinadaran da ke ɗauke da sinadarai masu ɗaurewa, ta hanyar mannewa da mucosa na halitta, yana ƙara ci gaba da matsewa tsakanin shirye-shiryen da mucosa, ta yadda maganin zai saki a hankali kuma mucosa ta shanye shi don cimma manufar magani. Ana amfani da shi sosai yanzu. Ana amfani da shi don magance cututtukan hanci da mucosa na baki. Fasaha ta bioadhesion ta hanji sabuwar nau'in tsarin isar da magunguna ce da aka haɓaka a cikin 'yan shekarun nan. Ba wai kawai yana tsawaita lokacin zama na shirye-shiryen magunguna a cikin hanyar hanji ba, har ma yana inganta aikin hulɗar maganin tare da membrane na tantanin halitta na wurin sha kuma yana canza ruwan membrane na tantanin halitta. Ƙarfin shiga na maganin zuwa ƙwayoyin epithelial na ƙaramin hanji yana ƙaruwa, ta haka yana inganta bioavailability na maganin.
4.8 A matsayin gel na shafawa
A matsayin wani shiri na mannewa ga fata, gel yana da fa'idodi da dama kamar aminci, kyau, sauƙin tsaftacewa, ƙarancin farashi, tsarin shiri mai sauƙi, da kuma kyakkyawan jituwa da magunguna. A cikin 'yan shekarun nan, ya sami kulawa sosai kuma ya zama ci gaban shirye-shiryen fata na waje.
4.9 A matsayin mai hana hazo a cikin tsarin emulsification
Lokacin Saƙo: Disamba-16-2021