Emlandweni weminyaka eyikhulu wama-capsules, i-gelatin ibilokhu igcina isimo sezinto ezijwayelekile ze-capsule ngenxa yemithombo yayo ebanzi, izici ezinzile zomzimba namakhemikhali kanye nezakhiwo ezinhle kakhulu zokucubungula.Ngokukhula kokuthandwa kwabantu ngamaphilisi, amaphilisi angenalutho asetshenziswa kabanzi emkhakheni wokudla, umuthi kanye nemikhiqizo yezempilo.
Kodwa-ke, ukwenzeka nokusabalala kwesifo sohlanya lwezinkomo nesifo samatele kwenza abantu baqale ukukhathazeka ngemikhiqizo ephuma ezilwaneni.Izinto zokusetshenziswa ezivame ukusetshenziswa zegelatin ithambo nesikhumba sezinkomo nezingulube, futhi ingozi yayo iye yadonsa ukunaka kwabantu kancane kancane.Ukuze kuncishiswe ubungozi bokuphepha bezinto zokusetshenziswa ze-capsule ezingenalutho, ochwepheshe bezimboni bayaqhubeka nokucwaninga futhi bathuthukise izinto ezifanele ze-capsule ezithathwe esitshalweni.
Ngaphezu kwalokho, ngokwanda kwezinhlobonhlobo zama-capsules, ukuhlukahluka kokuqukethwe kwawo kancane kancane kwenza abantu babone ukuthi kunezinkinga zokuhambisana phakathi kwama-capsules angenalutho we-gelatin nokunye okuqukethwe okunezici ezikhethekile.Isibonelo, okuqukethwe okuqukethe amaqembu e-aldehyde noma okusabela ukukhiqiza amaqembu e-aldehyde ngaphansi kwezimo ezithile kungase kuholele ekuxhumaneni kwe-gelatin;Okuqukethwe okunokuncipha okuqinile kungase kube nokusabela kwe-Maillard nge-gelatin;Okuqukethwe okune-hygroscopicity eqinile kuzokwenza igobolondo le-Ming capsule lilahlekelwe amanzi futhi lilahlekelwe ukuqina kwalo kwasekuqaleni.Ukuzinza kwe-gelatin hollow capsule kwenza ukwakhiwa kwezinto ezintsha ze-capsule kudonse ukunaka okwengeziwe.
Yiziphi izinto ezithathwe esitshalweni ezifanele ukukhiqizwa kwama-capsules aqinile angenalutho?Abantu sebezame kaningi.Isicelo sedokhumenti yelungelo lobunikazi baseShayina: 200810061238 X isicelo sokuthatha i-cellulose sodium sulfate njengento eyinhloko ye-capsule;200510013285.3 isicelo sokuthatha isitashi noma ukwakheka kwesitashi njengento eyinhloko ye-capsule;U-Wang GM [1] ubike ukuthi ama-capsules angenalutho enziwe ngama-capsules e-chitosan;UZhang Xiaoju et al.[2] kubika imikhiqizo enephrotheni yesoya ye-Konjac njengento eyinhloko ye-capsule.Yiqiniso, izinto ezifundwa kakhulu yizinto ze-cellulose.Phakathi kwawo, amaphilisi angenalutho enziwe nge-hydroxypropyl methylcellulose (HPMC) enze ukukhiqizwa okukhulu.
I-HPMC isetshenziswa kabanzi emkhakheni wokudla nemithi.Kuyi-excipient yemithi evame ukusetshenziswa, efakwe ku-Pharmacopoeia yamazwe ahlukahlukene;I-FDA kanye ne-EU igunyaza i-HPMC njengesengezo sokudla esiqondile noma esingaqondile;Utshani buyinto ephephile, No. GRN 000213;Ngokusho kwedathabheyisi ye-JECFA, i-INS no.464, awukho umkhawulo kumthamo omkhulu wansuku zonke we-HPMC;Ngo-1997, kugunyazwe uMnyango Wezempilo waseChina njengesengezo sokudla kanye ne-thickener (No. 20), esebenza kuzo zonke izinhlobo zokudla futhi yengezwe ngokuvumelana nezidingo zokukhiqiza [2-9].Ngenxa yomehluko wezakhiwo phakathi kwe-HPMC ne-gelatin, incwadi kadokotela ye-HPMC i-hollow capsule iyinkimbinkimbi kakhulu, futhi amanye ama-gelling agents adinga ukungezwa, njenge-Arabic gum, i-carrageenan (i-seaweed gum), isitashi, njll.
I-HPMC capsule engenalutho iwumkhiqizo onomqondo wemvelo.Ubuchwepheshe bayo bezinto ezibonakalayo nokukhiqiza baqashelwa izinhlangano zamaJuda, zamaSulumane kanye nezitshalo.Ingakwazi ukuhlangabezana nezidingo zabantu abanezinkolo ezihlukahlukene kanye nemikhuba yokudla, futhi yamukeleka kakhulu.Ngaphezu kwalokho, amaphilisi angenalutho e-HPMC anezindawo ezilandelayo ezihlukile:
1.Okuqukethwe kwamanzi aphansi - cishe ngama-60% aphansi kune-gelatin engenalutho capsule
Okuqukethwe kwamanzi amaphilisi angenalutho we-gelatin ngokuvamile ku-12.5% - 17.5% [10].Izinga lokushisa kanye nomswakama wendawo kufanele kulawulwe ngaphakathi kwebanga elifanele ngesikhathi sokukhiqiza, ukuthuthwa, ukusetshenziswa kanye nokugcinwa kwamaphilisi angenalutho.Izinga lokushisa elifanele liyi-15-25 ℃ futhi umswakama ohlobene ngu-35% - 65%, ukuze ukusebenza komkhiqizo kugcinwe isikhathi eside.Okuqukethwe kwamanzi kwe-membrane ye-HPMC kuphansi kakhulu, ngokuvamile ku-4% - 5%, okucishe kube ngama-60% aphansi kunalelo le-gelatin capsule engenalutho (Fig. 1).Ukushintshisana kwamanzi nemvelo ngesikhathi sokugcinwa kwesikhathi eside kuzokhuphula okuqukethwe kwamanzi kwe-HPMC capsule engenalutho emaphaketheni ashiwo, kodwa ngeke kudlule u-9% phakathi neminyaka engu-5.
Umdwebo1.Ukuqhathaniswa kwe-LOD kwe-HMPC namagobolondo eGelatin ngaphansi kwe-RH ehlukile
Isici sokuqukethwe kwamanzi aphansi senza i-HPMC capsule engenalutho ifanele ukugcwalisa okuqukethwe okune-hygroscopic noma okuzwelayo emanzini ukuze kunwetshwe impilo yeshalofu yomkhiqizo.
2.Ukuqina okuphezulu, akukho brittleness
Njengoba kushiwo ngenhla, ifilimu ye-gelatin inomswakama othize.Uma ingaphansi kwalo mkhawulo, ifilimu ye-gelatin izoba brittle kakhulu.Ama-capsules avamile we-gelatin angenalutho ngaphandle kwanoma yiziphi izithasiselo anengozi yokuba brittleness engaphezu kuka-10% lapho okuqukethwe komswakama kungu-10%;Lapho okuqukethwe kwamanzi kuqhubeka nokwehla kuya ku-5%, 100% brittleness izokwenzeka.Ngokuphambene, ukuqina kwama-capsules angenalutho we-HPMC kungcono kakhulu, futhi agcina ukusebenza kahle ngisho noma umswakama wemvelo uphansi (Fig. 3).Kunjalo, izinga lokuthomba lamaphilisi angenalutho e-HPMC anemiyalelo ehlukene ngaphansi komswakamo ophansi lizokhombisa umehluko omkhulu.
Ngokuphambene nalokho, amaphilisi angenalutho e-gelatin abekwe endaweni enomswakama ophezulu azothamba, akhubazeke noma aze awe ngemva kokumunca amanzi.I-HPMC capsule engenalutho ingagcina isimo esihle nokusebenza ngisho nangaphansi kwesimo somswakama ophezulu.Ngakho-ke, i-HPMC capsule engenalutho inokuvumelana nezimo okuqinile emvelweni.Uma indawo yokuthengisa yomkhiqizo ihlanganisa izindawo zezulu ezihlukahlukene noma izimo zokulondoloza zingezinhle uma kuqhathaniswa, le nzuzo ye-HMPC capsule engenalutho ibaluleke kakhulu.
3.Ukuzinza kwamakhemikhali okuqinile
I-crosslinking reaction of gelatin capsules iyinkinga enameva ehlangatshezwana namalungiselelo e-capsule.Ngenxa yokuthi iqembu le-aldehyde lokuqukethwe lisabela neqembu le-amino lama-amino acid ku-gelatin ukwakha isakhiwo senethiwekhi, igobolondo le-capsule linzima ukuhlakazeka ngaphansi kwesimo sokuchithwa kwe-in vitro, esithinta ukukhululwa kwezidakamizwa.IHydroxypropyl methylcellulose iphuma ku-cellulose, engasebenzi ngamakhemikhali futhi inokuhambisana okuhle kakhulu nezinto eziningi.Ngakho-ke, i-HPMC capsule engenalutho ayinayo ingozi yokusabela kokuxhumanisa kanye nokuzinza okuphezulu kwamakhemikhali
4.Good enamathela ukusebenza
Ama-capsules ahlanganiswe ne-Enteric asetshenziselwa izidakamizwa okulula ukulinyazwa yi-asidi yesisu, ecasulayo ku-mucosa yesisu noma edinga ukuphathwa okuhlosiwe.Ubuchwepheshe obamukelekayo emhlabeni wonke bama-capsules ahlanganiswe ne-enteric yikona okuphelele kwama-pellets nama-capsules ahlanganiswe ne-enteric.I-HPMC i-capsule engenalutho ibonisa izinzuzo eziyingqayizivele ekunambeni okuphelele kwe-capsule.
Ucwaningo lubonisa ukuthi ngenxa yobuso obuqinile be-HPMC capsule engenalutho, ukuhlobana nezinto eziningi zokugqoka ze-enteric kuphakeme kakhulu kune-gelatin, futhi isivinini sokunamathela kanye nokufana kwezinto zokumboza kungcono kakhulu kune-gelatin, ikakhulukazi ukwethembeka kwe-coating of the body cap junction. ithuthukiswa kakhulu.Ukuhlolwa kwe-in vitro dissolution kubonise ukuthi ukungena kwe-HPMC capsule esiswini kwakuphansi futhi kwakukhona ukukhululwa okuhle emathunjini[
Isiphetho
Izici ze-HPMC capsule engenalutho ziye zandisa inkambu yokusetshenziswa kwayo.Kusukela kuyo yonke imikhiqizo yemvelo kuya kokuzwela umswakama noma okuqukethwe kwe-hygroscopic, futhi inezinhlelo zokusebenza eziyingqayizivele emkhakheni we-powder eyomile inhalants kanye ne-enteric coating.Kufanele kuqashelwe ukuthi amaphilisi angenalutho e-HPMC njengamanje emakethe ekhaya naphesheya anokungena komoyampilo okuphezulu futhi ahlakazeka kancane kunamakhepsuli angenalutho we-gelatin, kepha ukutholakala kwawo kwe-bioavailability ku-vivo kuyafana [11], okufanele kubhekwe ocwaningweni nasekuthuthukisweni.
Njengoba sonke sazi, kunendlela ende okufanele ihanjwe kusukela ocwaningweni lwaselabhorethri, ukuhlola ngezinga elikhulu, ukukhiqizwa kwezimboni kuya ekuthuthukisweni kwemakethe.Yingakho, ngemva kweminyaka yocwaningo nokuthuthukiswa, imikhiqizo embalwa yama-capsules angenalutho eyenziwe ngezinto ezithathwe ezitshalweni ifakwe ohlwini ngempumelelo.Ngo-1997, i-capsugel yahola ekufakweni kuhlu kwe-HPMC hollow capsule vcapstm e-United States, ihlinzeka ngokukhetha okusha kwe-oral capsule.Njengamanje, umthamo wokuthengisa wonyaka wama-capsules angenalutho we-HPMC emhlabeni usudlule izigidi eziyizinkulungwane ezingu-20, futhi ukhula ngenani lama-25% ngonyaka.
Isikhathi sokuthumela: May-06-2022