Li-excipients tse tloaelehileng tsa mefuta ea litekanyetso tse tiileng tsa molomo

Litokisetso tse tiileng hajoale ke liforomo tsa litekanyetso tse ajoang ka ho fetesisa le tse sebelisoang ka ho fetesisa 'marakeng,' me hangata li na le lintho tse peli tse kholo le li-excipients.Li-excipients, tse tsejoang hape e le li-excipients, li bua ka lentsoe le akaretsang bakeng sa lisebelisoa tsohle tse eketsehileng ka litokisetso tse tiileng ntle le moriana o ka sehloohong.Ho ea ka thepa le mesebetsi e fapaneng ea li-excipients, li-excipients tsa litokisetso tse tiileng li atisa ho aroloa ka: li-filler, li-binders, disintegrants, lubricant, li-regulator tsa tokollo, 'me ka linako tse ling li-agent tsa mebala le li-flavor li ka eketsoa ho latela litlhoko tsa tokiso. ho ntlafatsa Kapa ho lokisa chebahalo le tatso ya sebopeho.
Li-excipients tsa litokisetso tse tiileng li lokela ho finyella litlhoko tsa tšebeliso ea meriana, 'me li be le litšobotsi tse latelang: ①E lokela ho ba le botsitso bo phahameng ba lik'hemik'hale' me e se ke ea e-ba le liphetoho tsa 'mele le lik'hemik'hale ka moriana o moholo;②Ha ea lokela ho ama phello ea phekolo le boikemisetso ba litaba tsa moriana o moholo;③ Ha ho kotsi 'meleng oa motho Ho kotsi, chefo e mehlano, ha ho na maikutlo a mabe.
1. Motlatsi (o mosesaane)
Ka lebaka la tekanyo e tlase ea moriana o ka sehloohong, tekanyo ea lithethefatsi tse ling ka linako tse ling ke limiligrama tse seng kae feela kapa ka tlaase ho moo, e sa lokelang ho etsoa ha letlapa kapa tsamaiso ea meriana.Ka hona, ha litaba tsa mantlha tsa lithethefatsi li le ka tlase ho 50mg, tekanyo e itseng ea ho tlatsa, e tsejoang hape e le diluent, e hloka ho eketsoa.
Sehlahisoa se loketseng se lokela ho ba se sa sebetseng hantle 'meleng le ka lik'hemik'hale mme se se ke sa ama bioavailability ea motsoako o sebetsang oa moriana.Li-filler tse sebelisoang hangata li kenyelletsa: ① Setache, ho kenyeletsoa setache sa koro, setache sa poone, le litapole, tseo har'a tsona setache sa poone se sebelisoang haholo;e tsitsitseng ka tlhaho, e tlaase ka hygroscopicity, empa e futsanehile ka ho hatella;② Lactose, e ntle ka thepa le ho hatelloa, metsi a matle;③ sucrose, e na le hygroscopicity e matla;④ pregelatinized starch, eo hape e tsejoang e le compressible starch, e na le compressibility e ntle, fluidity le self-lubricity;⑤ cellulose ea microcrystalline, e bitsoang MCC, e na le bokhoni bo matla ba ho tlama le ho hatelloa hantle;e tsejoang e le "dry binder";⑥Mannitol, ha e bapisoa le li-fillers tse ka holimo, e theko e boima hanyane, 'me hangata e sebelisoa matlapeng a hlafunoang, a nang le tatso e bobebe;⑦ Matsoai a inorganic, haholo-holo a kenyelletsang calcium sulfate, calcium phosphate, calcium carbonate, joalo-joalo, a nang le thepa ea 'mele le ea lik'hemik'hale e batlang e tsitsitse.
2. Mokelikeli oa metsi le sekhomaretsi
Lisebelisoa tsa ho kolobisa le li-binders ke li-excipients tse kenyelletsoeng nakong ea mohato oa granulation.Mokelikeli oa metsi ka boeona ha o na viscous, empa ke mokelikeli o susumetsang viscosity ea thepa ka ho kolobisa thepa.Lisebelisoa tse sebelisoang ka tloaelo haholo-holo li kenyelletsa metsi a hloekisitsoeng le ethanol, tseo har'a tsona metsi a hloekisitsoeng e leng khetho ea pele.
Li-adhesives li bua ka lisebelisoa tse thusang tse itšetlehileng ka viscosity ea tsona ho fana ka lisebelisoa tse se nang li-viscous kapa tse sa lekaneng tse nang le viscosity e loketseng.Likhomaretsi tse sebelisoang hangata li kenyelletsa: ① Starch slurry, e leng e 'ngoe ea likhomaretsi tse sebelisoang hangata, e theko e tlase, ebile e na le ts'ebetso e ntle,' me mohopolo o sebelisoang hangata ke 8% -15%;②Methylcellulose, e bitsoang MC, e na le ho qhibiliha ha metsi hantle;③Hydroxypropylcellulose, eo ho thoeng ke HPC, e ka sebelisoa e le phofo e tobileng ea tableting binder;④Hydroxypropylmethylcellulose, e bitsoang HPMC, thepa e qhibiliha ka metsing a batang;⑤Carboxymethylcellulose sodium, e bitsoang CMC-Na, e loketse lithethefatsi tse nang le khatello e fokolang;⑥Ethylcellulose, e bitsoang EC, thepa ha e qhibilihe ka metsing, empa e qhibiliha ka ethanol;⑦ Povidone, e bitsoang PVP, thepa e na le hygroscopic e feteletseng, e qhibilihang ka metsing le ethanol;⑧Ho feta moo, ho na le polyethylene glycol (e bitsoang PEG), Lisebelisoa tse kang gelatin.
3. Mokhelohi
Li-disintegrants li bua ka li-excipient tse khothalletsang ho senyeha ha matlapa ka potlako hore e be likaroloana tse ntle tsa maro a ka mpeng.Ntle le matlapa a molomo a nang le litlhoko tse khethehileng tse kang matlapa a lokolotsoeng ka nako e telele, matlapa a lokolotsoeng a laoloang, le matlapa a chewable, hangata li-disintegrants li hloka ho kenyelletsoa.Li-disintegrants tse sebelisoang ka tloaelo ke: ① setache se ommeng, se loketseng litlhare tse sa qhibiliheng kapa tse qhibilihang hanyane;② carboxymethyl starch sodium, e bitsoang CMS-Na, thepa ena ke disintegrant e sebetsang hantle haholo;③ cellulose ea hydroxypropyl e tlaase, e bitsoang L -HPC, e ka ruruhang kapele ka mor'a ho monya metsi;④Cross-linked methyl cellulose sodium, e bitsoang CCMC-Na;thepa e ruruha pele ka metsing ebe e qhibiliha, 'me ha e qhibilihe ka ethanol;Phoso ke hore e na le hygroscopicity e matla 'me e atisa ho sebelisoa ho granulation ea matlapa a matla kapa matlapa a chewable;⑥Disintegrants tse sebetsang haholo li kenyelletsa motsoako oa sodium bicarbonate le citric acid, le citric acid, fumaric acid, le sodium carbonate le tsona li ka sebelisoa, Potassium Carbonate le Potassium Bicarbonate joalo-joalo.
4. Setlolo
Lisebelisoa li ka aroloa ka bophara ka mekhahlelo e meraro, ho kenyeletsoa li-glidants, li-anti-sticing agents, le mafura ka mokhoa o moqotetsane.① Glidant: mosebetsi oa eona o ka sehloohong ke ho fokotsa likhohlano pakeng tsa likaroloana, ho ntlafatsa metsi a phofo, le ho thusa ho fokotsa phapang ea boima ba letlapa;② anti-sticking agent: mosebetsi oa eona o ka sehloohong ke ho thibela ho khomarela nakong ea khatello ea letlapa, E le ho netefatsa ts'ebetso e boreleli ea khatello ea letlapa, e ka boela ea ntlafatsa ponahalo ea matlapa;③ Chivalrous lubricant: fokotsa likhohlano lipakeng tsa thepa le lebota la hlobo, e le ho netefatsa ts'ebetso e boreleli ea khatello ea letlapa le ho sututsa.Lisebelisoa tse sebelisoang hangata (ka kutloisiso e pharaletseng) li kenyelletsa phofo ea talc, magnesium stearate (MS), gel ea silika e nang le micronized, polyethylene glycols, sodium lauryl sulfate, oli ea meroho ea hydrogenated, joalo-joalo.
5. Ho lokolla modulator
Litaolo tsa tokollo ka matlapa a molomo li loketse ho laola lebelo le tekanyo ea ho lokolloa ha lithethefatsi ka litokisetso tsa ho lokolloa ka molomo, e le ho etsa bonnete ba hore sethethefatsi se fetisetsoa sebakeng sa mokuli ka lebelo le itseng mme se boloka mohopolo o itseng ka har'a lisele kapa maro a 'mele. , ka hona Fumana phello e lebelletsoeng ea kalafo le ho fokotsa chefo le litla-morao.Li-regulators tse sebelisoang ka tloaelo li arotsoe haholo ka mofuta oa matrix, polymer e tlotsitsoeng butle-butle le e teteaneng.
(1) Modulator ea tokollo ea mofuta oa matrix
① Hydrophilic gel skeleton material: e kokomoha ha e pepesetsoa metsing ho etsa thibelo ea gel ho laola ho lokolloa ha lithethefatsi, tse sebelisoang hangata ke methyl cellulose, carboxymethyl cellulose, hydroxypropyl cellulose, povidone, carbomer, alginic acid Letsoai, chitosan, joalo-joalo.
② Lintho tse sa keneng tsa marapo: Thepa e sa keneng ea marapo e bua ka polymer e phahameng ea molek'hule e ke keng ea qhibiliha ka metsing kapa e nang le metsi a fokolang haholo.Tse sebelisoang haholo-holo ke ethyl cellulose, polyethylene, polyethylene e chefo e mehlano, polymethacrylic acid, ethylene-vinyl acetate copolymer, rabara ea silicone, joalo-joalo.
③ Lisebelisoa tsa moralo oa li-bioerodible: Lisebelisoa tse sebelisoang ka mokhoa o tloaelehileng haholo li kenyelletsa mafura a liphoofolo, oli ea meroho ea hydrogenated, boka ba linotsi, joala ea stearyl, boka ba carnauba, glyceryl monostearate, joalo-joalo.
(2) Mofetoleli oa ho lokolloa o koahetsoeng
① Lisebelisoa tsa polymer tse sa keneng: lisebelisoa tse tloaelehileng tse sa keneng tsa masapo tse kang EC.
②Enteric polymer thepa: thepa e tloaelehileng ea enteric polymer haholo-holo e kenyelletsa resin ea acrylic, mofuta oa L le mofuta oa S, hydroxypropylmethylcellulose acetate succinate (HPMCAS), cellulose acetate phthalate (CAP), hydroxypropylmethylcellulose phthalate (HPMCP), joalo-joalo. ka holim'a lisebelisoa ka lero la mala, 'me e qhibiliha likarolong tse itseng ho phetha karolo.
6. Lisebelisoa tse ling
Ho phaella ho li-excipients tse ka holimo tse sebelisoang ka tloaelo, ka linako tse ling li-excipients li eketsoa e le ho finyella litlhoko tsa tsamaiso ea lithethefatsi hantle, ho ntlafatsa temoho ea lithethefatsi kapa ho ntlafatsa ho latela melao.Ka mohlala, li-coloring, flavoring le sweetening agents.
①Moetsi oa mebala: Sepheo se seholo sa ho eketsa lisebelisoa tsena ke ho ntlafatsa ponahalo ea letlapa le ho etsa hore ho be bonolo ho khetholla le ho khetholla.Li-pigments tse sebelisoang ka tloaelo li lokela ho kopana le litlhaloso tsa meriana, 'me chelete e kenyelletsoeng hangata ha ea lokela ho feta 0.05%.
②Li-aromatics le li-sweeteners: Morero oa mantlha oa li-aromatics le li-sweeteners ke ho ntlafatsa tatso ea meriana, joalo ka matlapa a hlafunoang le matlapa a qhekellang ka molomo.Monko o monate o sebelisoang hangata o kenyelletsa li-essence, lioli tse fapaneng tse nkhang hamonate, joalo-joalo;Li-sweeteners tse sebelisoang hangata li kenyelletsa sucrose, aspartame, joalo-joalo.