Iicapsules eziqinileyo/HPMC iicapsules ezingenanto/iicapsules zemifuno/high-efficiency API kunye nezithako ezingevani nokufuma/inzululwazi yefilimu/ulawulo lokukhululwa oluzinzileyo/iteknoloji yobunjineli yeOSD….
Ukusebenza kweendleko okugqwesileyo, ukuveliswa ngokulula, kunye nokulula kolawulo lwesigulana somthamo, iimveliso zedosi yomlomo eqinileyo (OSD) zihlala ziluhlobo olukhethwayo lolawulo kubaphuhlisi bamachiza.
Kumaqumrhu angama-38 amatsha emolekyuli amancinci (ii-NME) avunywe yi-US Food and Drug Administration ngo-2019, angama-26 ayeyi-OSD1.Ngo-2018, ingeniso yemarike yeemveliso ezinophawu lwe-OSD kunye nokuqhutyelwa kwesibini kwe-CMOs kwimarike yaseMntla Melika yayimalunga ne-$ 7.2 yezigidigidi ze-USD 2. Imarike encinci ye-molecule ye-outsourcing kulindeleke ukuba idlule i-USD 69 billion ngo-20243. Zonke ezi datha zibonisa ukuba ngomlomo. Iifom zedosi eqinileyo (OSDs) ziya kuqhubeka zisebenza.
Iipilisi zisalawula kwimakethi ye-OSD, kodwa ii-capsules ezinzima ziya ziba yinto enomdla ngakumbi.Oku kuyingxenye ngenxa yokuthembeka kwee-capsules njengendlela yokulawula, ngakumbi abo bane-APIs ephezulu ye-antitumor.Iicapsules zisondele kakhulu kwizigulana, zifihla amavumba angathandekiyo kunye neencasa, kwaye kulula ukuziginya, zingcono kakhulu kunezinye iifom zedosi.
UJulien Lamps, uMphathi weMveliso kwiLonza Capsules kunye neziThako zeMpilo, uxoxa ngeenzuzo ezahlukeneyo zee-capsules ezinzima kwiipilisi.Wabelana ngezimvo zakhe kwi-hydroxypropyl methylcellulose (HPMC) ye-capsules engenanto kunye nendlela abanokunceda ngayo abaphuhlisi bamachiza ukuba baphucule iimveliso zabo ngelixa behlangabezana nemfuno yabathengi yamayeza enziwe kwizityalo.
Iicapsules ezinzima: Ukuphucula ukuthotyelwa kwesigulane kunye nokwandisa ukusebenza
Izigulana zihlala zisokola ngamayeza anencasa okanye anevumba elibi, kunzima ukuwaginya, okanye anokuba neziphumo ezibi.Ngoku engqondweni, ukuphuhlisa iifom zedosi ekulula ukuyisebenzisa kunokuphucula ukuthotyelwa kwesigulane kwiirejimeni zonyango.Iipilisi ezinzima ziyindlela ekhangayo kwizigulane ngenxa yokuba, ngaphezu kwe-masking incasa kunye nevumba, zinokuthi zithathwe ngokuphindaphindiweyo, zinciphise umthwalo wethebhulethi, kwaye zibe namaxesha angcono okukhululwa, ngokusetyenziswa kokukhululwa ngokukhawuleza, ukukhutshwa okulawulwayo kunye nokukhululwa ngokukhawuleza ukuya. zuza.
Ulawulo olungcono malunga nokuziphatha kokukhululwa kwechiza, umzekelo nge-micropelletizing i-API, inokuthintela ukulahlwa kwedosi kunye nokunciphisa imiphumo emibi.Abaphuhlisi beziyobisi bafumanisa ukuba ukudibanisa itekhnoloji ye-multiparticulate kunye nee-capsules kwandisa ukuguquguquka kunye nokusebenza kokulawulwa kokukhutshwa kwe-API.Iyakwazi ukuxhasa iipellets eziqulethe ii-APIs ezahlukeneyo kwi-capsule efanayo, oku kuthetha ukuba izidakamizwa ezininzi zinokulawulwa ngaxeshanye kwiidosi ezahlukeneyo, ngakumbi ukunciphisa ukuphindaphinda kwe-dosing.
Ukuziphatha kwe-pharmacokinetic kunye ne-pharmacodynamic yale miqulu, kubandakanywa ne-multiparticulate system4, i-extrusion spheronization API3, kunye ne-fixed-dose combination system5, nayo ibonise ukuveliswa kwakhona okungcono xa kuthelekiswa nokuqulunqwa okuqhelekileyo.
Kungenxa yolu phuculo olunokwenzeka ekuthotyelweni kwesigulane kunye nokusebenza kakuhle ukuba imfuno yemarike yee-APIs zegranular ezifakwe kwii-capsules ezinzima ziqhubeka zikhula.
Ukhetho lwePolymer:
Isidingo se-capsules yemifuno yokubuyisela i-gelatin capsules enzima
Iipilisi ezinzima zendabuko zenziwe nge-gelatin, nangona kunjalo, i-gelatin i-capsules enzima inokuzisa imingeni xa idibana ne-hygroscopic okanye iziqulatho ezinobumanzi.I-Gelatin yimveliso ephuma kwisilwanyana esixhomekeke kwiimpendulo ezinqamlezayo ezichaphazela ukuziphatha kokutshatyalaliswa, kwaye inomxholo ophezulu wamanzi ukugcina ukuguquguquka kwayo, kodwa inokutshintshisa amanzi kunye ne-API kunye nabancedisi.
Ukongeza kwimpembelelo yempahla ye-capsule ekusebenzeni kwemveliso, izigulane ezininzi ziyathandabuza ukutya iimveliso zezilwanyana ngenxa yezizathu zentlalo okanye zenkcubeko kwaye zifuna amayeza avela kwisityalo okanye i-vegan.Ukuhlangabezana nale mfuno, iinkampani ezixuba amayeza zikwaqhubeleka nokutyala imali kwiirejimeni zokudoba ezintsha ukuphuhlisa ezinye iindlela ezisekwe kwizityalo ezikhuselekileyo nezisebenzayo.Ukuqhubela phambili kwisayensi yezinto eziphathekayo kwenze ukuba ii-capsules ezingenanto eziphuma kwizityalo ezithathwe kwizityalo zinokwenzeka, zinika izigulane inketho engeyiyo yezilwanyana ngaphandle kwezibonelelo ze-gelatin capsules-ukugwinya, ukukhululeka kokuveliswa, kunye neendleko ezifanelekileyo.
Ukupheliswa okungcono kunye nokuhambelana:
Ukusetyenziswa kwe-HPMC
Okwangoku, enye yezona ndlela zingcono kwi-gelatin yi-hydroxypropyl methylcellulose (HPMC), i-polymer ephuma kwimicu yomthi.
I-HPMC ayisebenzi kangako ngokwekhemikhali kunegelatin kwaye ikwafunxa amanzi amancinci kunegelatin6.Umxholo wamanzi aphantsi we-capsules we-HPMC unciphisa ukutshintshiselana kwamanzi phakathi kwe-capsule kunye neziqulatho, ezinokuthi kwezinye iimeko ziphucule iikhemikhali kunye nokuzinza komzimba wokuqulunqwa, ukwandisa ubomi beshelufu, kwaye kulula ukuhlangabezana nemingeni ye-hygroscopic APIs kunye ne-excipients.I-HPMC ihollow capsules ayinaluvelwano kubushushu kwaye kulula ukuyigcina nokuthutha.
Ngokunyuka kwe-APIs ephezulu, iimfuno zokuqulunqa ziba nzima ngakumbi.Ukuza kuthi ga ngoku, abaphuhlisi bamachiza baphumelele iziphumo ezilungileyo kakhulu kwinkqubo yokuhlola ukusetyenziswa kwee-capsules ze-HPMC ukubuyisela ii-capsules ze-gelatin.Enyanisweni, ii-capsules ze-HPMC okwangoku zikhethwa ngokubanzi kulingo lwezonyango ngenxa yokuhambelana kwazo kakuhle namachiza amaninzi kunye nabancedisi7.
Ukuphuculwa okuqhubekayo kwiteknoloji ye-capsule ye-HPMC kukwathetha ukuba abaphuhlisi bamachiza banokukwazi ngcono ukusebenzisa iiparamitha zayo zokuchithwa kunye nokuhambelana noluhlu olubanzi lwee-NME, kubandakanywa iikhompawundi ezinamandla kakhulu.
Iipilisi ze-HPMC ngaphandle kwe-ejenti ye-gelling zineepropati ezibalaseleyo zokuchithwa ngaphandle kwe-ion kunye ne-pH yokuxhomekeka, ukuze izigulane ziya kufumana umphumo ofanayo wonyango xa uthatha ichiza kwisisu esingenalutho okanye ngokutya.Njengoko kubonisiwe kuMfanekiso 1. 8
Ngenxa yoko, ukuphuculwa kokuchithwa kunokuvumela izigulane ukuba zingabi nangxaki malunga nokucwangcisa iidosi zazo, ngaloo ndlela zandisa ukuthotyelwa.
Ukongeza, ukuqhubeka nokutsha kwizisombululo ze-capsule ye-HPMC ye-membrane ye-capsule inokwenza ukuba kukhuselwe intestinal kunye nokukhululwa ngokukhawuleza kwiindawo ezithile zendlela yokugaya, ukuhanjiswa kweziyobisi ezijoliswe kuzo kwezinye iindlela zonyango, kunye nokuphucula ngakumbi ukusetyenziswa kwee-capsules ze-HPMC.
Olunye ulwalathiso lwesicelo kwii-capsules ze-HPMC kwizixhobo zokuphefumla zolawulo lwemiphunga.Imfuno yemarike iyaqhubeka ikhula ngenxa yokuphuculwa kwe-bioavailability ngokuphepha i-hepatic first-pass effect kunye nokubonelela ngendlela ethe ngqo yokulawula xa kujoliswe kwizifo ezifana ne-asthma kunye nesifo esingapheliyo se-pulmonary (COPD) ngolu hlobo lolawulo .
Abavelisi bamachiza bahlala bejonge ukuphuhlisa unyango olungabizi kakhulu, olunobuhlobo kwisigulana, kunye nolusebenzayo lwezifo zokuphefumla, kunye nokuphonononga unyango lokuhanjiswa kwechiza lokuphefumlelwa kwezinye izifo zenkqubo yemithambo-luvo (CNS).imfuno iyanda.
Isiqulatho samanzi esisezantsi se-HPMC capsules sizenza zilungele i-hygroscopic okanye ii-APIs ezingevani namanzi, nangona iimpawu ze-electrostatic phakathi kokwenziwa kunye ne-hollow capsules kufuneka ziqwalaselwe kulo lonke uphuhliso8.
iingcinga zokugqibela
Uphuhliso lwenzululwazi ye-membrane kunye ne-OSD yobunjineli beteknoloji iye yabeka isiseko kwii-capsules ze-HPMC zokutshintsha ii-capsules ze-gelatin kwezinye iifomyula, ukubonelela ngeendlela ezininzi zokuphucula ukusebenza kwemveliso.Ukongeza, ukonyuka kogxininiso kwizinto ezikhethwa ngabathengi kunye nokunyuka kwemfuno yamachiza angabizi kakhulu aphefumleyo kuye kwanyusa imfuno yee-capsules ezingenanto kunye nokuhambelana okungcono kunye neemolekyuli ezingevani nokufuma.
Nangona kunjalo, ukhetho lwempahla ye-membrane lungundoqo ekuqinisekiseni impumelelo yemveliso, kwaye ukhetho olufanelekileyo phakathi kwe-gelatin kunye ne-HPMC lunokwenziwa kuphela ngobuchule obufanelekileyo.Ukhetho oluchanekileyo lwezinto ze-membrane alukwazi nje ukuphucula ukusebenza kunye nokunciphisa ukusabela okubi, kodwa lunokunceda ukunqoba imingeni ethile yokuqulunqa.
Ixesha lokuposa: Sep-23-2022