Izvo zvakajairika zvekushandisa zveoral solid dosage mafomu

Kugadzirira kwakasimba pari zvino ndiyo inonyanya kutenderedzwa uye inonyanya kushandiswa mafomu emushonga pamusika, uye anowanzo kuve nezvinhu zviviri zvikuru uye zvinobatsira. Maexcipients, anozivikanwawo seanobatsira, anoreva izwi rakajairwa kune ese ekuwedzera zvinhu mugadziriro yakasimba kunze kwemushonga mukuru. Zvinoenderana neakasiyana ezvivakwa uye mabasa ezvinobatsira, izvo zvinokonzeresa zvekugadzirira kwakasimba zvinowanzo kupatsanurwa kuita: mafirita, mabhainda, disintegrants, mafuta ekuzora, anoburitsa regi, uye dzimwe nguva maejenti emavara uye zvinonhuhwira zvinogona kuwedzerwa zvinoenderana nezvinodiwa zvegadziriro. kuvandudza Kana kugadzirisa chitarisiko uye kuravira kwekuumbwa.
Izvo zvinobatsira zvekugadzirira kwakasimba zvinofanirwa kusangana nezvinodiwa zvekushandiswa kwemushonga, uye kuve neanotevera maitiro: ①Inofanirwa kuve neyakagadzikana kemikari yakagadzikana uye isina chero yemuviri nemakemikari maitiro nemushonga mukuru; ②Haifanire kukanganisa maitiro ekurapa uye kugadzwa kwemukati kwemushonga mukuru; ③Hapana kukuvadza kumuviri wemunhu Kukuvadza, chepfu shanu, hapana maitiro akashata.
1. Filler (mutete)
Nekuda kwekuderera kwemushonga mukuru, muyero weimwe mishonga dzimwe nguva unongova mamirigiramu mashoma kana mashoma, izvo zvisingakodzeri kuumbwa kwehwendefa kana kutungamira kwekiriniki. Naizvozvo, kana iyo huru yemushonga yemukati iri pasi pe50mg, imwe dosi yekuzadza, inozivikanwawo sekuti diluent, inoda kuwedzerwa.
Iyo yakanaka yekuzadza inofanirwa kuve ye physiologically uye makemikari inert uye isingakanganise bioavailability yeinoshanda chemushonga. Mafirita anowanzo shandiswa anosanganisira: ① Sitachi, inosanganisira gorosi sitachi, chibage sitachi, uye mbatatisi, pakati peiyo chibage starch ndiyo inonyanya kushandiswa; yakagadzikana muzvisikwa, yakaderera mu hygroscopicity, asi yakashata mukumanikidzika; ② Lactose, yakanakisa mune zvivakwa uye compressible, yakanaka fluidity; ③ sucrose, ine yakasimba hygroscopicity; ④ pregelatinized starch, inozivikanwawo secompressible starch, ine yakanaka compressibility, fluidity uye self-lubricity; ⑤ microcrystalline cellulose, inonzi MCC, ine simba rakasimba rekusunga uye kugadzikana kwakanaka; inozivikanwa se "dry binder"; ⑥Mannitol, ichienzaniswa nemafirita ari pamusoro, inodhura zvishoma, uye inowanzoshandiswa mumapiritsi anotsenga, anewo kuravira kwakapfava; ⑦ Inorganic salts, kunyanya kusanganisira calcium sulfate, calcium phosphate, calcium carbonate, nezvimwewo, ine zvinhu zvakagadzikana zvemuviri nemakemikari.
2. Wetting agent uye adhesive
Wetting agents uye binders zvinhu zvinowedzerwa panguva ye granulation nhanho. Iyo yekunyorova iyo pachayo haisi viscous, asi imvura inokonzera viscosity yezvinhu nekunyorovesa zvinhu. Inowanzo shandiswa wetting agents inonyanya kusanganisira mvura yakasvibiswa uye ethanol, pakati pemvura yakasvibiswa ndiyo yekutanga sarudzo.
Adhesives anoreva izvo zvekubatsira izvo zvinotsamira kune yavo viscosity kupa isiri-viscous kana insufficiently viscous zvinhu zvine viscosity yakakodzera. Zvinamira zvinonyanya kushandiswa zvinonyanya kusanganisira: ① Starch slurry, inova imwe yeanonyanya kushandiswa adhesives, yakachipa, uye ine mashandiro akanaka, uye iyo inowanzo shandiswa inosvika 8% -15%; ②Methylcellulose, inonzi MC, ine mvura yakanaka yekunyungudika; ③Hydroxypropylcellulose, inonzi HPC, inogona kushandiswa sehupfu yakananga tableting binder; ④Hydroxypropylmethylcellulose, inonzi HPMC, zvinhu zvacho zvinonyungudika mumvura inotonhora; ⑤Carboxymethylcellulose sodium, inonzi CMC-Na, inokodzera zvinodhaka zvisina kusimba; ⑥Ethylcellulose, inonzi EC , zvinhu zvacho hazvigadziriswi mumvura, asi zvinonyunguduka mu ethanol; ⑦Povidone, inonzi PVP, iyo yakanyanyisa hygroscopic, inonyungudika mumvura uye ethanol; ⑧Kuwedzera, kune polyethylene glycol (inonzi PEG), Zvinhu zvakadai segelatin.
3. Disintegrant
Disintegrants zvinoreva zvinhu zvinobatsira zvinokurudzira kukurumidza kuparara kwemapiritsi kuita zvidimbu zvinyoro mumvura yemudumbu. Kunze kwemapiritsi emuromo ane zvinodiwa zvakakosha senge mahwendefa anoburitswa, anodzorwa-anoburitswa mahwendefa, uye anotsenga mahwendefa, disintegrants kazhinji inoda kuwedzerwa. Zvinowanzo shandiswa disintegrants ndezvi: ① starch yakaoma, yakakodzera kusanyungudika kana kunyungudika zvishoma mishonga; ② carboxymethyl starch sodium, inonzi CMS-Na, chinyorwa ichi ndeyepamusoro-inoshanda disintegrant; ③ yakaderera-inotsiva hydroxypropyl cellulose, inonzi L -HPC, inogona kuzvimba nekukurumidza mushure mekutora mvura; ④Cross-linked methyl cellulose sodium, inonzi CCMC-Na; zvinhu zvacho zvinotanga kuzvimba mumvura zvozonyungudika, uye hazvinyungudike mu ethanol; Izvo zvisingabatsiri ndezvokuti ine hygroscopicity yakasimba uye inowanzoshandiswa mu granulation yemapiritsi eeffervescent kana chewable tablets; ⑥Effervescent disintegrants inonyanya kusanganisira musanganiswa wesodium bicarbonate uye citric acid, uye citric acid, fumaric acid, uye sodium carbonate inogona zvakare kushandiswa, Potassium Carbonate uye Potassium Bicarbonate nezvimwe.
4. Mafuta
Mafuta ekuzora anogona kukamurwa zvakafara kuita mapoka matatu, anosanganisira glidants, anti-sticking agents, uye mafuta ekuzora nenzira nhete. ① Glidant: basa rayo guru nderokudzikisa kupokana pakati pezvimedu, kuvandudza kuyerera kwehupfu, uye kubatsira kuderedza mutsauko mukurema kwehwendefa; ② anti-sticking agent: basa rayo guru nderokudzivirira kunamatira panguva yekumanikidzika kwepiritsi, Kuti ive nechokwadi chekushanda kwakanaka kwepiritsi yekumanikidza, inogonawo kuvandudza kutaridzika kwemapiritsi; ③ chivalrous lubricant: kuderedza kupokana pakati pezvinhu uye madziro ekuumbwa, kuitira kuti uve nechokwadi chekushanda kwakanaka kwekumanikidza piritsi uye kusundira. Mafuta anowanzo shandiswa (mupfungwa yakafara) anosanganisira talc poda, magnesium stearate (MS), micronized silica gel, polyethylene glycols, sodium lauryl sulfate, hydrogenated muriwo mafuta, nezvimwe.
5. Kusunungura modulator
Release regulators mumapiritsi emuromo akakodzera kudzora kumhanya uye dhigirii rekuburitswa kwezvinodhaka mumuromo wakaramba-kuburitswa gadziriro, kuitira kuti ive nechokwadi chekuti mushonga unounzwa kunzvimbo yemurwere pane imwe kukurumidza uye unochengetedza imwe fungidziro mumatishu kana mvura yemuviri. , nokudaro Tora inotarisirwa kurapwa maitiro uye kuderedza chepfu uye mhedzisiro. Anowanzo shandiswa kuburitsa regulators anonyanya kukamurwa kuita matrix mhando, firimu-yakavharidzirwa inononoka-kuburitsa polymer uye thickener.
(1) Matrix-mhando yekuburitsa modulator
①Hydrophilic gel skeleton material: inozvimba kana yaiswa mumvura kuita chivharo chejeri chekudzora kuburitswa kwezvinodhaka, chinowanzoshandiswa methyl cellulose, carboxymethyl cellulose, hydroxypropyl cellulose, povidone, carbomer, alginic acid Munyu, chitosan, nezvimwe.
② Insoluble skeleton material: Insoluble skeleton material inoreva high molecular polymer isinganyunguriki mumvura kana kuti ine mvura shoma. Inonyanya kushandiswa ndeye ethyl cellulose, polyethylene, shanu-chepfu polyethylene, polymethacrylic acid, ethylene-vinyl acetate copolymer, silicone rabha, nezvimwe.
③ Bioerodible framework materials: Inowanzo shandiswa bioerodible framework zvinhu zvinonyanya kusanganisira mafuta emhuka, hydrogenated mafuta emuriwo, wakisi, stearyl doro, carnauba wax, glyceryl monostearate, nezvimwewo. Inogona kunonoka kunyungudutswa uye kuburitsa maitiro emishonga inonyungudika mumvura.
(2) Coated kusunungurwa modifier
① Insoluble polymer zvinhu: zvakajairika zvisinganyunguriki skeleton zvinhu seEC.
②Enteric polymer zvinhu: zvakajairika enteric polymer zvinhu zvinonyanya zvinosanganisira acrylic resin, L-mhando uye S-mhando, hydroxypropylmethylcellulose acetate succinate (HPMCAS), cellulose acetate phthalate (CAP), hydroxypropylmethylcellulose phthalate (HPMCP), nezvimwewo. pamusoro pezvinhu mujusi yemudumbu, uye inonyungudika muzvikamu zvakati kuti iite basa.
6. Zvimwe zvinhu
Pamusoro pezvishandiso zviri pamusoro apa zvinowanzoshandiswa, zvimwe zvinowedzerwa dzimwe nguva zvinowedzerwa kuitira kuti zvizadzise zvirinani zvinodikanwa zvekutonga zvinodhaka, kuvandudza kuzivikanwa kwezvinodhaka kana kuvandudza kutevedza. Semuyenzaniso, coloring, flavoring uye sweetening agents.
①Coloring agent: Chinangwa chikuru chekuwedzera chinyorwa ichi ndechekuvandudza kutaridzika kwehwendefa uye kuita kuti zvive nyore kuziva uye kusiyanisa. Inowanzo shandiswa pigment inofanira kusangana nemishonga yemishonga, uye mari yakawedzerwa haifaniri kudarika 0.05%.
②Aromatics uye sweeteners: Chinangwa chikuru chekunhuhwirira uye zvinotapira ndechekuvandudza kuravira kwemishonga, senge mahwendefa anotsenga uye mahwendefa anopwanya nemuromo. Zvinowanzo shandiswa zvinonhuhwirira zvinonyanya zvinosanganisira essences, akasiyana mafuta anonhuhwirira, nezvimwewo; anowanzo shandiswa zvinotapira anonyanya kusanganisira sucrose, aspartame, nezvimwe.