Feem ntau excipients ntawm qhov ncauj khoom noj cov ntaub ntawv

Cov khoom npaj tam sim no yog cov khoom siv dav dav thiab feem ntau siv cov ntaub ntawv hauv khw, thiab lawv feem ntau muaj ob yam khoom tseem ceeb thiab excipients. Excipients, tseem hu ua excipients, xa mus rau lub ntsiab lus dav dav rau tag nrho cov ntaub ntawv ntxiv hauv cov khoom npaj tshwj tsis yog cov tshuaj tseem ceeb. Raws li cov khoom sib txawv thiab kev ua haujlwm ntawm excipients, excipients ntawm cov khoom npaj feem ntau muab faib ua: fillers, binders, disintegrants, lubricants, tso regulators, thiab qee zaum cov xim thiab cov tshuaj tsw qab tuaj yeem muab ntxiv raws li qhov xav tau ntawm kev npaj. los txhim kho Los yog kho cov tsos thiab saj ntawm formulation.
Cov excipients ntawm cov khoom npaj yuav tsum ua raws li cov kev cai rau kev siv tshuaj, thiab muaj cov yam ntxwv hauv qab no: ①Nws yuav tsum muaj tshuaj lom neeg ruaj khov thiab tsis muaj kev cuam tshuam lub cev thiab tshuaj lom neeg nrog cov tshuaj tseem ceeb; ②Nws yuav tsum tsis txhob cuam tshuam rau kev kho mob thiab kev txiav txim siab cov ntsiab lus ntawm cov tshuaj tseem ceeb; ③ Tsis muaj kev puas tsuaj rau tib neeg lub cev Kev puas tsuaj, tsib yam tshuaj lom, tsis muaj kev phiv tshuaj.
1. Filler (thinner)
Vim tias qhov koob tshuaj tsawg ntawm cov tshuaj tseem ceeb, koob tshuaj ntawm qee cov tshuaj yog qee zaum tsuas yog ob peb milligrams lossis tsawg dua, uas tsis tsim nyog rau kev tsim cov ntsiav tshuaj lossis kev tswj hwm kev kho mob. Yog li ntawd, thaum cov ntsiab lus tseem ceeb ntawm cov tshuaj yog tsawg dua 50mg, ib qho tshuaj ntawm cov muab tub lim, tseem hu ua diluent, yuav tsum tau ntxiv.
Ib tug zoo tagnrho muab tub lim yuav tsum physiologically thiab chemically inert thiab tsis cuam tshuam rau bioavailability ntawm lub active ingredient ntawm cov tshuaj. Feem ntau siv cov fillers feem ntau muaj xws li: ① Starch, nrog rau cov hmoov txhuv nplej siab, pob kws hmoov txhuv nplej siab, thiab qos yaj ywm starch, uas feem ntau siv cov hmoov txhuv nplej siab; ruaj khov nyob rau hauv qhov, tsis tshua muaj hygroscopicity, tab sis tsis zoo nyob rau hauv compressibility; ② Lactose, zoo heev hauv cov khoom thiab compressible, fluidity zoo; ③ sucrose, muaj zog hygroscopicity; ④ pregelatinized starch, tseem hu ua compressible starch, muaj compressibility zoo, fluidity thiab nws tus kheej-lubricity; ⑤ microcrystalline cellulose, hu ua MCC, muaj zog binding muaj peev xwm thiab zoo compressibility; hu ua "dry binder"; ⑥Mannitol, piv nrog cov sau saum toj no, yog me ntsis kim dua, thiab feem ntau yog siv rau hauv cov ntsiav tshuaj chewable, uas kuj muaj ib tug ilv saj; ⑦ Inorganic ntsev, feem ntau suav nrog calcium sulfate, calcium phosphate, calcium carbonate, thiab lwm yam, nrog rau lub cev thiab tshuaj lom neeg ruaj khov.
2. Tus neeg sawv cev ntub dej thiab nplaum
Cov tshuaj ntub dej thiab cov ntawv khi yog cov khoom ntxiv ntxiv thaum lub sij hawm granulation. Tus neeg sawv cev ntub dej nws tus kheej tsis yog khov, tab sis yog cov kua uas ua rau cov viscosity ntawm cov khoom los ntawm ntub cov khoom. Feem ntau siv cov khoom ntub dej feem ntau suav nrog cov dej distilled thiab ethanol, cov dej distilled yog thawj qhov kev xaiv.
Adhesives xa mus rau cov ntaub ntawv pabcuam uas tso siab rau lawv tus kheej viscosity los ua kom tsis muaj kuab paug lossis tsis txaus cov ntaub ntawv nrog cov viscosity tsim nyog. Kev siv cov nplaum nplaum feem ntau suav nrog: ① Starch slurry, uas yog ib qho ntawm cov nplaum nplaum uas siv ntau tshaj plaws, yog pheej yig, thiab muaj kev ua tau zoo, thiab kev siv cov concentration yog 8% -15%; ②Methylcellulose, hu ua MC, muaj dej solubility zoo; ③Hydroxypropylcellulose, hu ua HPC, tuaj yeem siv los ua cov hmoov nplej ncaj qha; ④Hydroxypropylmethylcellulose, hu ua HPMC, cov khoom yog soluble hauv dej txias; ⑤Carboxymethylcellulose sodium, hu ua CMC-Na, haum rau cov tshuaj uas tsis zoo compressibility; ⑥Ethylcellulose, hu ua EC, cov khoom yog insoluble hauv dej, tab sis soluble hauv ethanol; ⑦ Povidone, hu ua PVP, cov khoom siv tsis tshua muaj hygroscopic, soluble hauv dej thiab ethanol; ⑧ Tsis tas li ntawd, muaj polyethylene glycol (hu ua PEG), Cov ntaub ntawv xws li gelatin.
3. Disintegrant
Disintegrants xa mus rau excipients uas txhawb kev tawg sai ntawm cov ntsiav tshuaj mus rau hauv cov khoom zoo hauv cov kua hauv plab. Tsuas yog cov ntsiav tshuaj ntawm qhov ncauj nrog cov kev cai tshwj xeeb xws li cov ntsiav tshuaj uas tau tso tawm, cov ntsiav tshuaj tswj-tso tawm, thiab cov ntsiav tshuaj chewable, feem ntau yuav tsum tau ntxiv cov tshuaj disintegrants. Feem ntau siv disintegrants yog: ① qhuav starch, haum rau insoluble los yog me ntsis soluble tshuaj; ② carboxymethyl starch sodium, hu ua CMS-Na, cov khoom siv no yog cov tshuaj tua kab mob siab; ③ qis-hloov hydroxypropyl cellulose, hu ua L-HPC, uas tuaj yeem o sai sai tom qab nqus dej; ④Cross-linked methyl cellulose sodium, hu ua CCMC-Na; cov khoom swells ua ntej nyob rau hauv dej thiab ces dissolves, thiab yog insoluble nyob rau hauv ethanol; Qhov tsis zoo yog tias nws muaj zog hygroscopicity thiab feem ntau yog siv rau hauv granulation ntawm effervescent ntsiav tshuaj los yog chewable ntsiav tshuaj; ⑥ Effervescent disintegrants feem ntau suav nrog kev sib xyaw ntawm sodium bicarbonate thiab citric acid, thiab citric acid, fumaric acid, thiab sodium carbonate kuj siv tau, Potassium Carbonate thiab Potassium Bicarbonate thiab lwm yam.
4. Lubricant
Lubricants tuaj yeem muab faib ua peb pawg, suav nrog glidants, anti-sticking agents, thiab lubricants hauv qhov nqaim. ① Glidant: nws lub luag haujlwm tseem ceeb yog txhawm rau txo qhov kev sib txhuam ntawm cov khoom, txhim kho cov kua dej ntawm cov hmoov, thiab pab txo qhov sib txawv ntawm cov ntsiav tshuaj hnyav; ② anti-sticking tus neeg saib xyuas: nws lub luag haujlwm tseem ceeb yog los tiv thaiv kev ua kom zoo thaum lub ntsiav tshuaj compression, txhawm rau kom ntseeg tau tias kev ua haujlwm zoo ntawm cov ntsiav tshuaj compression, nws tuaj yeem txhim kho cov tsos ntawm cov ntsiav tshuaj; ③ chivalrous lubricant: txo cov kev sib txhuam ntawm cov khoom thiab cov pwm phab ntsa, thiaj li ua kom lub lag luam du ntawm cov ntsiav tshuaj compression thiab thawb. Feem ntau siv cov roj nplua nyeem (hauv kev nkag siab dav) suav nrog talc hmoov, magnesium stearate (MS), micronized silica gel, polyethylene glycols, sodium lauryl sulfate, hydrogenated zaub roj, thiab lwm yam.
5. Tso tawm modulator
Kev tso tawm regulators nyob rau hauv lub qhov ncauj ntsiav tshuaj yog tsim rau kev tswj qhov ceev thiab degree ntawm cov tshuaj tso tawm nyob rau hauv lub qhov ncauj sustained-tso npaj, thiaj li yuav xyuas kom meej tias cov tshuaj xa mus rau tus neeg mob qhov chaw ntawm ib tug tej yam ceev thiab tswj ib tug tej yam concentration nyob rau hauv cov ntaub so ntswg los yog lub cev kua. , yog li Tau txais cov txiaj ntsig kho mob thiab txo cov tshuaj lom thiab cov kev mob tshwm sim. Feem ntau siv tso tawm regulators feem ntau muab faib ua hom matrix, zaj duab xis-coated qeeb-tso polymer thiab thickener.
(1) Matrix hom tso tawm modulator
①Hydrophilic gel skeleton khoom: nws swells thaum raug dej los tsim gel barrier los tswj cov tshuaj tso tawm, feem ntau siv yog methyl cellulose, carboxymethyl cellulose, hydroxypropyl cellulose, povidone, carbomer, alginic acid ntsev, chitosan, thiab lwm yam.
② Insoluble skeleton material: Insoluble skeleton material yog hais txog lub siab molecular polymer uas yog insoluble hauv dej los yog muaj dej solubility tsawg. Feem ntau siv yog ethyl cellulose, polyethylene, tsib-toxic polyethylene, polymethacrylic acid, ethylene-vinyl acetate copolymer, silicone roj hmab, thiab lwm yam.
③ Bioerodible moj khaum cov ntaub ntawv: Feem ntau siv bioerodible moj khaum cov ntaub ntawv feem ntau suav nrog tsiaj rog, hydrogenated zaub roj, beeswax, stearyl cawv, carnauba wax, glyceryl monostearate, thiab lwm yam.
(2) Coated tso tawm modifier
① Insoluble polymer cov ntaub ntawv: cov khoom siv pob txha tsis zoo xws li EC.
②Enteric polymer cov ntaub ntawv: cov ntaub ntawv enteric polymer feem ntau suav nrog acrylic resin, L-type thiab S-type, hydroxypropylmethylcellulose acetate succinate (HPMCAS), cellulose acetate phthalate (CAP), hydroxypropylmethylcellulose phthalate (HPMCP), thiab lwm yam. Nws siv cov yam ntxwv ntawm dissol saum toj no cov ntaub ntawv nyob rau hauv plab hnyuv kua txiv, thiab dissolves nyob rau hauv tej qhov chaw los ua ib tug luag hauj lwm.
6. Lwm yam khoom siv
Ntxiv nrog rau cov khoom siv saum toj no feem ntau siv, qee zaum lwm cov excipients raug ntxiv kom ua tau raws li cov kev xav tau ntawm kev tswj hwm tshuaj, txhim kho kev paub txog tshuaj lossis txhim kho kev ua raws cai. Piv txwv li, colouring, flavoring thiab sweetening agents.
①Coloring agent: Lub hom phiaj tseem ceeb ntawm kev ntxiv cov khoom no yog txhawm rau txhim kho cov tsos ntawm cov ntsiav tshuaj thiab ua kom yooj yim rau kev txheeb xyuas thiab paub qhov txawv. Feem ntau siv pigments yuav tsum tau raws li cov kws kho mob specifications, thiab tus nqi ntxiv yuav tsum tsis pub tshaj 0.05%.
②Aromatics thiab sweeteners: Lub hom phiaj tseem ceeb ntawm aromatics thiab sweeteners yog los txhim kho cov saj ntawm cov tshuaj, xws li chewable ntsiav tshuaj thiab hais lus disintegrating ntsiav tshuaj. Feem ntau siv cov tshuaj tsw qab feem ntau suav nrog cov essences, ntau yam roj tsw qab, thiab lwm yam.; Feem ntau siv cov khoom qab zib feem ntau suav nrog sucrose, aspartame, thiab lwm yam.