Kwimbali yekhulu leminyaka yee-capsules, i-gelatin isoloko igcina isimo sezinto eziqhelekileyo ze-capsule ngenxa yemithombo yayo ebanzi, iipropati ezizinzileyo zomzimba kunye neekhemikhali kunye neempawu ezibalaseleyo zokucubungula.Ngokunyuka kokuthandwa ngabantu kwii-capsules, ii-capsules ezingenanto zisetyenziswa ngokubanzi kwiindawo zokutya, amayeza kunye neemveliso zempilo.
Nangona kunjalo, ukwenzeka kunye nokusasazeka kwesifo se-mad cow kunye nesifo sonyawo kunye nomlomo kwenza abantu baqalise ukuxhalaba malunga neemveliso zezilwanyana.Izinto ezisetyenziswa ngokuqhelekileyo zegelatin lithambo kunye nolusu lwenkomo neehagu, kwaye umngcipheko wayo uthe ngokuthe ngcembe watsala ingqalelo yabantu.Ukuze kuncitshiswe umngcipheko wokhuseleko lwezixhobo eziluhlaza ze-capsule, iingcali zoshishino ziyaqhubeka nokuphanda kunye nokuphuhlisa izinto ezifanelekileyo ze-capsule ezivela kwisityalo.
Ukongezelela, ngokunyuka kweendidi ze-capsules, ukuhlukahluka komxholo wabo ngokuthe ngcembe kwenza abantu baqonde ukuba kukho iingxaki zokuhambelana phakathi kwee-capsules ze-gelatin ezingenanto kunye nezinye iziqulatho ezineempawu ezizodwa.Ngokomzekelo, iziqulatho eziqulethe amaqela e-aldehyde okanye ukusabela ukuvelisa amaqela e-aldehyde phantsi kweemeko ezithile kunokukhokelela ekudibaniseni i-gelatin;Imixholo enokunciphisa okunamandla ingaba ne-Maillard reaction kunye ne-gelatin;Umxholo one-hygroscopicity eqinile uya kwenza igobolondo ye-Ming capsule ilahlekelwe ngamanzi kwaye ilahlekelwe ubunzima bayo bokuqala.Ukuzinza kwe-gelatin hollow capsule kwenza ukuphuhliswa kwezinto ezintsha ze-capsule kutsale ingqalelo ngakumbi.
Ziziphi izinto ezithathwe kwisityalo ezifanelekileyo ukuveliswa kwee-capsules ezinzima ezingenanto?Abantu bazamile kakhulu.Isicelo soxwebhu lwelungelo elilodwa lomenzi waseTshayina No.: 200810061238 X isicelo sokuthatha i-cellulose sodium sulfate njengeyona nto ingundoqo ye-capsule;I-200510013285.3 isicelo sokuthatha isitashi okanye ukubunjwa kwesitashi njengento ephambili ye-capsule;U-Wang GM [1] wabika ukuba ii-capsules ezingenanto zenziwe kwii-capsules ze-chitosan;UZhang Xiaoju et al.[2] ingxelo yeemveliso ezineprotheni yesoya ye-Konjac njengeyona nto iphambili ye-capsule.Kakade ke, ezona zinto zifundiswayo zizixhobo zeselulosi.Phakathi kwazo, ii-capsules ezingenanto ezenziwe nge-hydroxypropyl methylcellulose (HPMC) zenze imveliso enkulu.
I-HPMC isetyenziswa kakhulu kwindawo yokutya kunye namayeza.Yinto esetyenziswa ngokuqhelekileyo i-pharmaceutical excipient, efakwe kwi-Pharmacopoeia yamazwe ahlukeneyo;I-FDA kunye ne-EU ivuma i-HPMC njengesongezo sokutya ngokuthe ngqo okanye esingathanga ngqo;I-Gras yinto ekhuselekileyo, No. GRN 000213;Ngokutsho kwedatha ye-JECFA, i-INS no.464, akukho mda kwi-dose ephezulu yemihla ngemihla ye-HPMC;Kwi-1997, yavunywa nguMphathiswa wezempilo waseTshayina njengento yokongeza ukutya kunye ne-thickener (No. 20), esebenzayo kuzo zonke iintlobo zokutya kwaye yongezwa ngokweemfuno zemveliso [2-9].Ngenxa yomahluko wezakhiwo phakathi kwe-HPMC kunye ne-gelatin, i-prescription ye-HPMC i-capsule engenanto inzima ngakumbi, kwaye ezinye ii-gelling agents kufuneka zongezwe, ezifana ne-Arabic gum, i-carrageenan (i-seaweed gum), isitashi, njl.
I-HPMC capsule ehollow yimveliso enengqiqo yendalo.Ithekhnoloji yayo yezinto eziphathekayo kunye nemveliso ibonwa ngamaYuda, amaSilamsi kunye nemibutho yemifuno.Inokwanelisa iimfuno zabantu abaneenkolo ezahlukeneyo kunye nemikhwa yokutya, kwaye yamkelwa kakhulu.Ukongeza, ii-capsules ezingenanto ze-HPMC zineempawu ezizodwa zilandelayo:
1.Umthamo wamanzi aphantsi - malunga ne-60% ngaphantsi kwe-gelatin hollow capsule
Isiqulatho samanzi se-gelatin ye-capsules engenanto ngokuqhelekileyo yi-12.5% - 17.5% [10].Ubushushu kunye nokufuma kokusingqongileyo kufuneka kulawulwe kuluhlu olufanelekileyo ngexesha lemveliso, ukuthuthwa, ukusetyenziswa kunye nokugcinwa kwee-capsules ezingenanto.Ubushushu obufanelekileyo yi-15-25 ℃ kunye nomswakama ohambelanayo ngu-35% - 65%, ukwenzela ukuba ukusebenza kwemveliso kunokugcinwa ixesha elide.Umxholo wamanzi we-membrane we-HPMC uphantsi kakhulu, ngokubanzi i-4% - i-5%, emalunga ne-60% engaphantsi kune-gelatin capsule engenanto (Umfanekiso 1).Ukutshintshana kwamanzi kunye nokusingqongileyo ngexesha lokugcinwa kwexesha elide kuya kwandisa umthamo wamanzi we-HPMC i-capsule engenanto kwi-packaging echaziweyo, kodwa ayiyi kudlula i-9% kwiminyaka eyi-5.
Isazobe soku1.Uthelekiso lwe-LOD lwe-HMPC kunye namaqokobhe eGelatin phantsi kwe-RH eyahlukileyo
Uphawu lwesiqulatho samanzi aphantsi senza i-HPMC i-capsule engenanto ifanele ukuzaliswa kwe-hygroscopic okanye imixholo ebuthathaka yamanzi ukwandisa ixesha leshelufu yemveliso.
2.Ukuqina okuphezulu, akukho brittleness
Njengoko kukhankanyiwe ngasentla, ifilimu ye-gelatin inomswakama ochaziweyo.Ukuba iphantsi kulo mda, ifilimu ye-gelatin iya kuba yi-brittle kakhulu.Iipilisi eziqhelekileyo ze-gelatin ezingenazo izongezo zinomngcipheko wobunzima obungaphezulu kwe-10% xa umxholo wokufuma uyi-10%;Xa umthamo wamanzi uqhubeka ukuhla ukuya kwi-5%, i-100% ye-brittleness iya kwenzeka.Ngokwahlukileyo, ukuqina kwee-capsules ezingenanto ze-HPMC zingcono kakhulu, kwaye zigcina ukusebenza kakuhle nokuba ukufuma kwendalo kuphantsi (Umfanekiso 3).Ewe kunjalo, ireyithi ye-embrittlement yee-capsules ezingenanto ze-HPMC ezinemigqaliselo eyahlukeneyo phantsi kokufuma okuphantsi kuya kubonisa umahluko omkhulu.
Ngokuchasene noko, iipilisi ze-gelatin ezingenanto ezibekwe kwindawo yokufuma okuphezulu ziya kuthamba, zikhubazeke okanye ziwe emva kokufunxa amanzi.I-HPMC capsule ehollow inokugcina imilo elungileyo kunye nokusebenza naphantsi kwemeko yokufuma okuphezulu.Ke ngoko, i-HPMC ihollow capsule inokuguquguquka okuqinileyo kokusingqongileyo.Xa indawo yokuthengisa yemveliso igubungela iindawo ezahlukeneyo zemozulu okanye iimeko zogcino zimbi kakhulu, olu ncedo lwe-HMPC ihollow capsule lubaluleke kakhulu.
3.Uzinzo oluqinileyo lweekhemikhali
I-crosslinking reaction of gelatin capsules yingxaki enameva edibana namalungiselelo e-capsule.Ngenxa yokuba iqela le-aldehyde lomxholo liphendula kunye neqela le-amino le-amino acids kwi-gelatin ukwenza isakhiwo sothungelwano, igobolondo le-capsule linzima ukunyibilika phantsi kwemeko yokuchithwa kwe-vitro, echaphazela ukukhutshwa kweziyobisi.IHydroxypropyl methylcellulose iphuma kwi cellulose, engasebenzi ngokwekhemikhali kwaye inohambelana kakuhle nezinto ezininzi.Ke ngoko, i-HPMC ye-capsule engenanto ayinamngcipheko wokusabela okunqamlezayo kunye nokuzinza okuphezulu kweekhemikhali
4.Ukusebenza kakuhle kokugquma
Iicapsules ezifakwe kwi-Enteric zisetyenziselwa iziyobisi ezilula ukonakalisa nge-asidi yesisu, ezicasulayo kwi-gastric mucosa okanye zifuna ulawulo olujoliswe kuyo.Itekhnoloji eyamkelwe kwihlabathi jikelele yee-enteric coated capsules yiyo yonke i-enteric coated pellets kunye ne-capsules.I-HPMC ihollow capsule ibonisa iingenelo ezizodwa kwi-coating jikelele ye-capsule.
Uphando lubonisa ukuba ngenxa yobuso oburhabaxa be-HPMC ehollow capsule, ukunxulumana nezona zinto zininzi zokugquma i-enteric ziphezulu kakhulu kunegelatin, kwaye isantya sokuncamathela kunye nokufana kwezinto zokugquma zingcono kakhulu kunegelatin, ngakumbi ukuthembeka kokugquma kwe-body cap junction. iphuculwe kakhulu.Uvavanyo lokuchithwa kwe-in vitro lubonise ukuba ukunyanzeliswa kwe-capsule ye-HPMC esiswini kwakusezantsi kwaye kwakukho ukukhululwa okulungileyo emathunjini.
Ukuqukumbela
Iimpawu zeHPMC capsule ehollow ziye zandisa indawo yesicelo.Ukusuka kuzo zonke iimveliso zendalo ukuya kwiziqulatho ezinochuku okanye i-hygroscopic, ikwanezicelo ezizodwa kwintsimi ye-powder inhalants eyomileyo kunye ne-enteric coating.Kufuneka kuqatshelwe ukuba ii-capsules ezingenanto ze-HPMC okwangoku kwimarike ekhaya nakwamanye amazwe zinokungena kweoksijini ephezulu kunye nokuqhekeka okucothayo kunee-gelatin ezingenanto, kodwa i-bioavailability yazo kwi-vivo iyafana [11], ekufuneka ithathelwe ingqalelo kuphando nakuphuhliso.
Njengoko sonke sisazi, kukho indlela ende yokuhamba ukusuka kuphando lwebhubhoratri, umfuniselo omkhulu, ukuveliswa kwemveliso ukuya ekukhuthazeni imarike.Yiyo loo nto, emva kweminyaka yophando kunye nophuhliso, zimbalwa kuphela iimveliso ze-capsules ezingenanto ezenziwe ngezinto ezithathwe kwizityalo ezidweliswe ngempumelelo.Kwi-1997, i-capsugel yakhokela ekudwelisweni kwe-HPMC i-hollow capsule vcapstm e-United States, inika ukhetho olutsha lwe-capsule yomlomo.Okwangoku, umthamo wokuthengisa wonyaka wee-capsules ezingenanto ze-HPMC kwihlabathi udlule kwi-20 yezigidigidi, kwaye ukhula ngesantya se-25% ngonyaka.
Ixesha lokuposa: May-06-2022