Li-capsules tse thata / li-capsules tse sekoti tsa HPMC / li-capsules tsa meroho / API e sebetsang hantle haholo le metsoako e sa ameheng mongobo / saense ea lifilimi / taolo e tsitsitseng ea tokollo / theknoloji ea boenjiniere ea OSD….
Ts'ebeliso e ntle ea litšenyehelo, bonolo ba ho e etsa, le boiketlo ba taolo ea mokuli ea litekanyetso, lihlahisoa tsa Oral solid dosage (OSD) e ntse e le mokhoa o ratoang oa tsamaiso bakeng sa baetsi ba lithethefatsi.
Ho mekhatlo e 38 e mecha ea limolek'hule (li-NME) e amohetsoeng ke Tsamaiso ea Lijo le Lithethefatsi ea US ka 2019, ba 26 e ne e le OSD1. Ka 2018, chelete ea 'maraka ea lihlahisoa tsa OSD tse nang le ts'ebetso ea bobeli ke CMOs' marakeng oa Amerika Leboea e ne e ka ba $ 7.2 bilione USD 2. Mmaraka o monyenyane oa ho ntša limolek'hule o lebelletsoe ho feta USD 69 bilione ka 20243. Lintlha tsena kaofela li fana ka maikutlo a hore molomo. liforomo tse tiileng tsa litekanyetso (li-OSD) li tla tsoelapele ho ba teng.
Matlapa a ntse a laola 'maraka oa OSD, empa li-capsules tse thata li fetoha mokhoa o mong o hohelang. Sena se bakoa ke ho tšepahala ha li-capsules e le mokhoa oa tsamaiso, haholo-holo ba nang le matla a phahameng a antitumor APIs. Li-capsules li haufi haholo le bakuli, li pata monko o sa thabiseng le litatso, 'me li bonolo ho li koenya, haholo ho feta mefuta e meng ea litekanyetso.
Julien Lamps, Mookameli oa Sehlahisoa ho Lonza Capsules le Health Ingredients, o tšohla melemo e sa tšoaneng ea li-capsules tse thata holim'a matlapa. O arolelana leseli la hae ka li-capsules tse se nang letho tsa hydroxypropyl methylcellulose (HPMC) le kamoo li ka thusang baetsi ba lithethefatsi ho ntlafatsa lihlahisoa tsa bona ha ba ntse ba fihlela tlhoko ea bareki ea meriana e tsoang limela.
Li-capsules tse thata: Ntlafatsa ho latela mamello le ho ntlafatsa ts'ebetso
Hangata bakuli ba loana le meriana e latsoang kapa e nkhang hampe, e thata ho e koenya, kapa e ka bang le litlamorao tse mpe. Ho nahanoa ka sena, ho etsa liforomo tsa litekanyetso tse bonolo tsa basebelisi ho ka ntlafatsa ho latela mekhoa ea kalafo. Li-capsules tse thata ke khetho e khahlehang bakeng sa bakuli hobane, ntle le ho masking tatso le monko, li ka nkoa hangata, li fokotsa moroalo oa letlapa, 'me li na le linako tse ntle tsa ho lokolloa, ka tšebeliso ea ho lokolloa hang-hang, ho lokolloa ho laoloang le ho lokolloa butle-butle. finyella.
Taolo e betere holim'a boitšoaro ba ho lokolloa ha lithethefatsi, mohlala ka micropelletizing API, e ka thibela ho lahla lethal dose le ho fokotsa litla-morao. Bahlahisi ba lithethefatsi ba fumana hore ho kopanya theknoloji ea multiparticulate le li-capsules ho eketsa bonolo le katleho ea ts'ebetso ea API e laoloang. E ka ba ea ts'ehetsa li-pellets tse nang le li-API tse fapaneng ka har'a capsule e le 'ngoe, ho bolelang hore lithethefatsi tse ngata li ka tsamaisoa ka nako e le ngoe ka litekanyetso tse fapaneng, ho fokotsa khafetsa ea dosing.
Boitšoaro ba pharmacokinetic le pharmacodynamic tsa mekhoa ena, ho kenyelletsa le multiparticulate system4, extrusion spheronization API3, le mokhoa o tsitsitseng oa motsoako oa tsamaiso5, le oona o bontšitse ho ikatisa hamolemo ha ho bapisoa le mekhoa e tloaelehileng.
Ke ka lebaka la ntlafatso ena e ka bang teng ea ho latela mamello le katleho moo tlhoko ea 'maraka ea li-API tsa granular tse kentsoeng ka har'a li-capsules tse thata e ntse e hola.
Khetho ea polymer:
Tlhokahalo ea li-capsules tsa meroho ho nkela li-capsules tsa gelatin tse thata
Li-capsules tse thata tsa setso li entsoe ka gelatin, leha ho le joalo, li-capsules tse thata tsa gelatin li ka hlahisa mathata ha li kopana le litaba tsa hygroscopic kapa tse sa utloeleng mongobo. Gelatin ke sehlahisoa se entsoeng ke liphoofolo se atisang ho ba le liketso tse amanang le li-cross-link tse amang boitšoaro ba ho qhibiliha, 'me e na le metsi a batlang a le holimo ho boloka ho fetoha ha eona, empa e ka boela ea fapanyetsana metsi le li-API le li-excipients.
Ntle le tšusumetso ea thepa ea capsule ts'ebetsong ea sehlahisoa, bakuli ba ntseng ba eketseha ba leqe ho ja lihlahisoa tsa liphoofolo ka mabaka a sechaba kapa a setso 'me ba batla meriana e nkiloeng ke limela kapa vegan. Ho fihlela tlhoko ena, lik'hamphani tse etsang meriana le tsona li ntse li tsoela pele ho tsetela mekhoeng e mecha ea ho noa meriana ho hlahisa mekhoa e meng e thehiloeng limela e bolokehileng le e sebetsang hantle. Tsoelo-pele ea saense ea thepa e entse hore li-capsules tse sekoti tse entsoeng ke limela li khonehe, li fa bakuli khetho e sa hlahisoang ke liphoofolo ho phaella melemo ea li-capsules tsa gelatin-ho metsa, ho etsa bonolo, le ho boloka litšenyehelo.
Bakeng sa ho qhibiliha hantle le ho lumellana:
Tšebeliso ea HPMC
Hajoale, e 'ngoe ea mekhoa e metle ka ho fetisisa ea gelatin ke hydroxypropyl methylcellulose (HPMC), polymer e tsoang likhoeleng tsa lifate.
HPMC ha e kenelle ka lik'hemik'hale ho feta gelatin hape e monya metsi a fokolang ho feta gelatin6. Metsi a tlaase a li-capsules tsa HPMC a fokotsa phapanyetsano ea metsi pakeng tsa capsule le likahare, tseo ka linako tse ling li ka ntlafatsang botsitso ba lik'hemik'hale le 'meleng oa sebopeho, ho lelefatsa bophelo ba sethala, le ho tobana le mathata a hygroscopic APIs le li-excipients. Li-capsules tse sekoti tsa HPMC ha li utloe mocheso 'me ho bonolo ho li boloka le ho li tsamaisa.
Ka keketseho ea li-API tse sebetsang hantle haholo, litlhoko tsa ho etsoa li ntse li e-ba thata le ho feta. Ho fihlela joale, baetsi ba lithethefatsi ba fumane liphello tse ntle haholo ts'ebetsong ea ho hlahloba tšebeliso ea li-capsules tsa HPMC ho nkela li-capsules tsa gelatin sebaka sa setso. Ebile, li-capsules tsa HPMC hajoale li ratoa litekong tsa bongaka ka lebaka la ho lumellana ha tsona hantle le litlhare tse ngata le li-excipient7.
Lintlafatso tse tsoelang pele ho theknoloji ea capsule ea HPMC e boetse e bolela hore baetsi ba lithethefatsi ba khona ho sebelisa monyetla oa ho qhibiliha ha eona le ho lumellana le mefuta e mengata ea li-NME, ho kenyelletsa le metsoako e matla haholo.
Li-capsules tsa HPMC ntle le gelling agent li na le thepa e ntle ea ho qhibiliha ntle le ho itšetleha ka ion le pH, e le hore bakuli ba tla fumana phello e tšoanang ea phekolo ha ba noa moriana ka mpeng e se nang letho kapa ka lijo. Joalokaha ho bontšitsoe setšoantšong sa 1.8
Ka lebaka leo, ntlafatso ea ho qhibiliha e ka lumella bakuli hore ba se ke ba tšoenyeha ka ho hlophisa litekanyetso tsa bona, kahoo ba eketsa ho latela melao.
Ho phaella moo, ts'ebetso e tsoelang pele ea HPMC capsule membrane solutions e ka boela ea thusa ho sireletsa mala le ho lokolloa ka potlako libakeng tse itseng tsa tšilo ea lijo, ho fana ka lithethefatsi tse lebisitsoeng bakeng sa mekhoa e meng ea phekolo, le ho ntlafatsa ts'ebeliso ea li-capsules tsa HPMC.
Tataiso e 'ngoe ea ts'ebeliso ea li-capsules tsa HPMC ke lisebelisoa tsa ho hema bakeng sa tsamaiso ea matšoafo. Tlhokahalo ea 'maraka e ntse e hola ka lebaka la ntlafatso ea bioavailability ka ho qoba phello ea hepatic first pass le ho fana ka tsela e tobileng ea tsamaiso ha e tobane le mafu a kang asthma le chronic obstructive pulmonary disease (COPD) ka mokhoa ona oa tsamaiso.
Baetsi ba lithethefatsi ba lula ba batla ho hlahisa liphekolo tse baballang chelete e ngata, tse bonolo ho mokuli, le tse sebetsang hantle bakeng sa mafu a ho hema, le ho hlahloba liphekolo tsa phepelo ea lithethefatsi tse hulelitsoeng bakeng sa mafu a mang a methapo ea kutlo (CNS). tlhokeho ea eketseha.
Likahare tse tlase tsa metsi tsa li-capsules tsa HPMC li li etsa hore e be tse loketseng bakeng sa li-API tsa hygroscopic kapa tse sa utloeleng metsi, leha thepa ea electrostatic lipakeng tsa sebopeho le li-capsules tse sekoti le tsona li tlameha ho nahanoa ho pholletsa le nts'etsopele8.
mehopolo ea ho qetela
Nts'etsopele ea mahlale a membrane le theknoloji ea boenjiniere ea OSD e ralile motheo bakeng sa li-capsules tsa HPMC ho nkela li-capsules tsa gelatin mefuteng e meng, ho fana ka likhetho tse ling tsa ho ntlafatsa ts'ebetso ea sehlahisoa. Ntle le moo, khatello e ntseng e eketseha ea lintho tseo bareki ba li ratang le tlhokahalo e ntseng e eketseha ea litlhare tse huloang ka theko e tlase li ekelitse tlhoko ea li-capsules tse se nang letho tse tsamaisanang hantle le limolek'hule tse sa utloeleng mongobo.
Leha ho le joalo, khetho ea lisebelisoa tsa membrane ke senotlolo sa ho netefatsa katleho ea sehlahisoa, 'me khetho e nepahetseng pakeng tsa gelatin le HPMC e ka etsoa feela ka tsebo e nepahetseng. Khetho e nepahetseng ea li-membrane e ke ke ea ntlafatsa feela ts'ebetso le ho fokotsa litlamorao tse mpe, empa hape e thusa ho hlola mathata a itseng a sebopeho.
Nako ea poso: Sep-23-2022