I-excipients eziqhelekileyo zomlomo iifom zedosi eqinileyo

Amalungiselelo aqinileyo okwangoku awona mafomu asasazwa kakhulu kwaye asetyenziswa kakhulu kwimarike, kwaye ahlala equlathe izinto ezimbini eziphambili kunye nezinto ezincedisayo. Abancedisi, abakwabizwa ngokuba ngabancedisi, babhekisa kwigama eliqhelekileyo kuzo zonke izinto ezongezelelweyo kumalungiselelo aqinileyo ngaphandle kweyeza eliphambili. Ngokweepropati ezahlukeneyo kunye nemisebenzi ye-excipients, abancedisi bamalungiselelo aqinileyo bahlala behlulwe babe: izigcwalisi, izibophelelo, i-disintegrants, i-lubricant, izilawuli zokukhulula, kwaye ngamanye amaxesha ii-agent zemibala kunye nee-agent ze-flavoring nazo zinokongezwa ngokweemfuno zamalungiselelo. ukuphucula Okanye ukulungelelanisa imbonakalo kunye nencasa yokwakheka.
Abancedisi bamalungiselelo aqinileyo kufuneka bahlangabezane neemfuno zokusetyenziswa kweyeza, kwaye babe nezi mpawu zilandelayo: ① Kufuneka ibe nozinzo oluphezulu lwekhemikhali kwaye ingabi nakuphi na ukushukuma komzimba kunye nemichiza kunye nechiza eliphambili; ②Akufunekanga ichaphazele umphumo wonyango kunye nokuzimisela komxholo weyeza eliphambili; ③Akukho bungozi kumzimba womntu Ubungozi, iityhefu ezintlanu, akukho ziphumo zibi.
1. Isifaki (ebhityileyo)
Ngenxa yedosi ephantsi yechiza eliphambili, idosi yamanye amachiza ngamanye amaxesha i-milligrams ezimbalwa okanye ngaphantsi, engenzi kakuhle ekwenzeni ithebhulethi okanye ulawulo lweklinikhi. Ngoko ke, xa umxholo wechiza oyintloko ungaphantsi kwe-50mg, idosi ethile yokuzalisa, eyaziwa ngokuba yi-diluent, kufuneka ifakwe.
Isigcwalisi esifanelekileyo kufuneka sibe ne-physiologically kunye nekhemikhali inert kwaye ingachaphazeli i-bioavailability yesithako esisebenzayo sechiza. Izihluzi ezisetyenziswa ngokuxhaphakileyo ziquka: ① istatshi, kuquka istatshi sengqolowa, istatshi sombona, kunye netapile, apho isitatshi sombona sesona sisetyenziswa kakhulu; izinzile ngokwendalo, iphantsi kwi-hygroscopicity, kodwa ihlwempuzekile ekunyanzelweni; ② iLactose, igqwesileyo kwiipropathi kunye nokucinezeleka, ulwelo oluhle; ③ i-sucrose, ine-hygroscopicity eyomeleleyo; ④ isitashi esandulela igelatinized, esaziwa ngokuba sistatshi esicinezelekayo, sinokucinezeleka kakuhle, ulwelo kunye nokuzithambisa; ⑤ i-microcrystalline cellulose, ebizwa ngokuba yi-MCC, inamandla okubopha kunye nokunyanzeliswa okulungileyo; eyaziwa ngokuba yi "dry binder"; ⑥Mannitol, xa kuthelekiswa nezi zigcwali zingentla, ibiza kakhulu, kwaye ihlala isetyenziswa kwiitafile ezihlafunwayo, ezikwanoncasa obuthathaka; ⑦ Iityuwa ze-Inorganic, ingakumbi i-calcium sulfate, i-calcium phosphate, i-calcium carbonate, njl., ezineempawu ezizinzileyo zomzimba kunye neekhemikhali.
2. I-arhente yokumanzisa kunye ne-adhesive
Ii-agent zokumanzisa kunye nezibophelelo zi-excipients zongezwa ngexesha lenyathelo le-granulation. I-agent emanzi ngokwayo ayinayo i-viscous, kodwa i-liquid eyenza i-viscosity yezinto eziphathekayo ngokumanzisa izinto. Iiarhente zokumanzisa ezisetyenziswa ngokuqhelekileyo ziquka amanzi adibeneyo kunye ne-ethanol, phakathi kwayo amanzi adibeneyo akhethwa kuqala.
I-Adhesives ibhekisela kwizinto ezincedisayo ezixhomekeke kwi-viscosity yazo ukuze zinike izinto ezingabonakaliyo okanye ezingafanelekanga kunye ne-viscosity efanelekileyo. Izinto zokuncamathelisa ezisetyenziswa ngokuqhelekileyo ziquka: ① Udaka lwesitatshi, yenye yezinto ezincamathelayo ezisetyenziswa ngokuxhaphakileyo, sixabiso eliphantsi, kwaye sisebenza kakuhle, kwaye ugxininiso oluqhele ukusetyenziswa yi-8% -15%; ②Methylcellulose, ekubhekiselwa kuyo njenge-MC, inonyibiliko olulungileyo lwamanzi; ③I-Hydroxypropylcellulose, ekubhekiselwa kuyo njenge-HPC, ingasetyenziswa njenge-powder tableting binder ngqo; ④I-Hydroxypropylmethylcellulose, ebizwa ngokuba yi-HPMC, izinto eziphathekayo zinyibilika emanzini abandayo; ⑤Carboxymethylcellulose sodium, ekubhekiselwa kuyo njenge-CMC-Na, ilungele iziyobisi ezinokucinezeleka kakubi; ⑥Ethylcellulose, ekubhekiselwa kuyo ngokuba yi-EC, izinto eziphathekayo azinakunyibilika emanzini, kodwa zinyibilika kwi-ethanol; ⑦ I-Povidone, ebizwa ngokuba yi-PVP, i-material i-hygroscopic kakhulu, i-soluble emanzini kunye ne-ethanol; ⑧ Ukongezelela, kukho i-polyethylene glycol (ebizwa ngokuba yi-PEG), Izinto ezifana ne-gelatin.
3. Ukungavumelani
I-Disintegrants ibhekisela kwii-excipients ezikhuthaza ukuphuka ngokukhawuleza kweepilisi kwiincinci ezincinci kwi-gastrointestinal fluids. Ngaphandle kwamacwecwe omlomo aneemfuno ezikhethekileyo ezifana neepilisi ezikhutshwa ngokuqhubekayo, iipilisi ezikhutshwayo ezilawulwayo, kunye neepilisi ezihlafunwayo, i-disintegrants ngokubanzi kufuneka yongezwe. Iidisintegrants ezidla ngokusetyenziswa zezi: ① istatshi esomileyo, esilungele amachiza anganyibilikiyo okanye anyibilikayo kancinane; ② i-carboxymethyl starch sodium, ebizwa ngokuba yi-CMS-Na, le nto i-disintegrant ephezulu yokusebenza kakuhle; ③ i-cellulose ye-hydroxypropyl ephantsi, ebizwa ngokuba yi-L -HPC, enokuthi idumbe ngokukhawuleza emva kokufunxa amanzi; ④I-Methyl cellulose sodium edityaniswe ngokunqamlezileyo, ekubhekiselwa kuyo njenge-CCMC-Na; i-material idumba kuqala emanzini ize inyibilike, kwaye ayinyibiliki kwi-ethanol; Ukungalungi kukuba ine-hygroscopicity enamandla kwaye isetyenziswa ngokuqhelekileyo kwi-granulation yamacwecwe asebenzayo okanye amacwecwe ahlaziywayo; ⑥Izihluzi ezisebenzayo ziquka umxube wesodium bicarbonate kunye necitric acid, kunye necitric acid, fumaric acid, kunye nesodium carbonate nazo zingasetyenziswa, iPotassium Carbonate kunye nePotassium Bicarbonate njl.njl.
4. Isithambiso
Izithambisi zinokwahlulwa ngokubanzi zibe ngamacandelo amathathu, kubandakanywa ii-glidants, ii-anti- sticking agents, kunye nezithambiso ngengqiqo emxinwa. ① I-Glidant: umsebenzi wayo ophambili kukunciphisa ukungqubuzana phakathi kwamasuntswana, ukuphucula ulwelo lwepowder, kunye nokunceda ukunciphisa umahluko kubunzima bethebhulethi; ② i-agent echasayo: umsebenzi wayo oyintloko kukuthintela ukunamathela ngexesha lokunyanzeliswa kwethebhulethi, Ukuze kuqinisekiswe ukusebenza kakuhle kwe-tablet compression, kunokuphucula ukubonakala kwamacwecwe; ③ i-lubricant ye-chivalrous: nciphisa ingxabano phakathi kwezinto kunye nodonga lokubumba, ukuze kuqinisekiswe ukusebenza kakuhle kwe-tablet compression kunye nokutyhala. Izithambiso ezisetyenziswa ngokuqhelekileyo (ngengqiqo ebanzi) ziquka i-talc powder, i-magnesium stearate (MS), i-silica gel micronized, i-polyethylene glycols, i-sodium lauryl sulfate, i-oyile yemifuno ye-hydrogenated, njl.
5. Khupha imodyuli
Ukukhutshwa kwabalawuli kwiipilisi zomlomo zifanelekile ukulawula isantya kunye neqondo lokukhutshwa kweziyobisi kumalungiselelo okukhululwa okuzinzileyo ngomlomo, ukwenzela ukuba kuqinisekiswe ukuba ichiza linikezelwa kwindawo yesigulane ngesantya esithile kwaye igcina ugxininiso oluthile kwizicubu okanye ulwelo lomzimba. , ngaloo ndlela Fumana isiphumo esilindelekileyo sonyango kwaye unciphise ityhefu kunye neziphumo ebezingalindelekanga. Izilawuli zokukhulula ezisetyenziswa ngokuqhelekileyo zahlulwe zibe luhlobo lwe-matrix, ifilimu efakwe kwipolymer ecothayo kunye ne-thickener.
(1) Imodyuli yokukhulula yohlobo lweMatrix
①I-Hydrophilic gel skeleton material: iyadumba xa ibonakaliswe emanzini ukuze yenze umqobo wejeli ukulawula ukukhutshwa kweziyobisi, ngokuqhelekileyo isetyenziswa yi-methyl cellulose, carboxymethyl cellulose, hydroxypropyl cellulose, povidone, carbomer, alginic acid Ityuwa, chitosan, njl.
② Izinto zamathambo ezinganyibilikiyo: Izinto ezinganyibilikiyo zamathambo zibhekisa kwipolymer ephezulu yemolekyuli enganyibilikiyo emanzini okanye enonyibiliko oluncinci lwamanzi. Ngokuqhelekileyo isetyenziswa kakhulu yi-ethyl cellulose, i-polyethylene, i-polyethylene enetyhefu emihlanu, i-polymethacrylic acid, i-ethylene-vinyl acetate copolymer, irabha ye-silicone, njl.
③ Izinto zesakhelo se-Bioerodible: Izixhobo zesakhelo se-bioerodible ezisetyenziswa ngokuqhelekileyo zibandakanya amafutha ezilwanyana, i-hydrogenated oil oil, i-bewax, i-stearyl alcohol, i-carnauba wax, i-glyceryl monostearate, njl.
(2) Isilungisi sokukhulula esigqunyiweyo
① Izinto zepolymer ezinganyibilikiyo: izixhobo eziqhelekileyo ezinganyibilikiyo zamathambo ezifana ne-EC.
②Imathiriyeli ye-polymer ye-Enteric: izinto eziqhelekileyo ze-polymer ze-enteric ziquka ikakhulu i-acrylic resin, uhlobo lwe-L kunye nohlobo lwe-S, i-hydroxypropylmethylcellulose acetate succinate (HPMCAS), i-cellulose acetate phthalate (CAP), i-hydroxypropylmethylcellulose phthalate (HPMCP), njl njl. ngaphezulu kwezixhobo kwijusi yamathumbu, kwaye inyibilika kwiindawo ezithile ukuze idlale indima.
6. Ezinye izincedisi
Ukongeza kwezi zixhasi zisetyenziswa ngentla apha, abanye abancedisi bayongezwa ngamanye amaxesha ukuze kuhlangatyezwane neemfuno zolawulo lwamachiza, kuphuculwe ukuqondwa kweziyobisi okanye ukuphucula ukuthotyelwa. Umzekelo, imibala, i-flavoring kunye ne-sweetening agents.
①I-ejenti yombala: Injongo ephambili yokongeza le nto kukuphucula ukubonakala kwethebhulethi kwaye kube lula ukuchonga nokwahlula. I-pigments esetyenziswa ngokuqhelekileyo kufuneka ihlangabezane neenkcukacha zamachiza, kwaye imali eyongeziweyo akufanele idlule i-0.05%.
②Aromatics kunye ne-sweeteners: Eyona njongo iphambili yearomatics kunye ne-sweeteners kukuphucula incasa yamayeza, anje ngeepilisi ezihlafunwayo kunye neepilisi ezichithwa ngomlomo. Iziqholo ezisetyenziswa ngokuqhelekileyo ziquka i-essces, ii-oyile ezahlukeneyo ezivumbayo, njl.; iiswiti ezisetyenziswa ngokuqhelekileyo ziquka i-sucrose, i-aspartame, njl.