Pharmaceutical excipients vabatsiri uye vabatsiri vanoshandiswa mukugadzirwa kwemishonga uye kugadzira zvinyorwa, uye chikamu chakakosha chemishonga yekugadzirira. Sechisikigo chinobva papolymer zvinhu, cellulose ether ine hunhu hwe biodegradability, isiri-chepfu, uye yakaderera mutengo, senge sodium carboxymethyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl cellulose,Cellulose etherssenge hydroxyethyl cellulose uye ethyl cellulose zvine kukosha kwakakosha kwekushandisa mune zvemishonga excipients. Parizvino, zvigadzirwa zvemazhinji edzimba cellulose ether mabhizinesi anonyanya kushandiswa pakati uye yakaderera-yekupedzisira minda yeindasitiri, uye iyo yakawedzerwa kukosha haina kukwirira. Iyo indasitiri inoda nekuchimbidza kushandura uye kukwidziridza nekuvandudza epamusoro-magumo ekushandisa ezvigadzirwa.
Pharmaceutical excipients inoita basa rakakosha mukuvandudza nekugadzirwa kwezvakagadzirwa. Semuenzaniso, mukugadzirisa-kusunungurwa kwekugadzirira, zvinhu zvepolymer zvakadai se cellulose ethers zvinoshandiswa semishonga yemishonga mumapellets anoramba achibudiswa, matrix akasiyana-siyana anobudiswa-kusunungurwa maumbirwo, akavharidzirwa-akasunungurwa-kusunungurwa maumbirwo, akarembera-kusunungurwa macapsules, anoramba achibudiswa-kusunungurwa zvinodhaka zvinodhaka, uye kusunungurwa-kusunungurwa kwemishonga. Kugadzirira uye gadziriro yemvura inosimudzira-kuburitswa yakashandiswa zvakanyanya. Mune ino system, mapolymers akadai se cellulose ethers anowanzo shandiswa sevatakuri vezvinodhaka kudzora kuburitswa kwezvinodhaka mumuviri wemunhu, ndiko kuti, ivo vanofanirwa kuburitswa zvishoma nezvishoma mumuviri pamwero wakatarwa mukati meimwe nguva yenguva kuti uwane chinangwa chekurapa kunoshanda.
Zvinoenderana nehuwandu hweConsulting and Research department, pane mazana mashanu emhando dzevabatsiri pamusika munyika yangu, asi zvichienzaniswa neUnited States (inopfuura 1500 marudzi) neEuropean Union (inopfuura zviuru mazana matatu emarudzi), pane musiyano mukuru, uye mhando dzichiri diki. nyika yangu inopa mishonga yemishonga. Zvinonzwisiswa kuti gumi epamusoro emishonga ekuwedzera mumusika wemusika chiyero chemishonga gelatin capsules, sucrose, starch, film coating powder, 1,2-propylene glycol, PVP, hydroxypropyl methylcellulose (HPMC), uye microcrystalline fibers. Vegetarian, HPC, lactose.
"Natural cellulose ether ndiyo izwi rinowanzoreva mutsara wezvinyorwa zve cellulose zvinogadzirwa nekuita kwealkali cellulose uye etherifying agent pasi pemamwe mamiriro ezvinhu, uye chigadzirwa umo mapoka e hydroxyl pa cellulose macromolecule anotsiviwa zvishoma kana zvachose nemapoka ether. Cellulose ethers inoshandiswa zvakanyanya muminda yezuva nezuva, minda yekugadzira makemikari, mishonga yekudya, petroleum, mishonga yekudya, petroleum. minda, mishonga-giredhi zvigadzirwa zviri pakati uye yepamusoro-soro nzvimbo indasitiri uye ane yakakwirira akawedzera kukosha Nekuda kwemhando dzakasimba zvinodiwa, kugadzirwa kwemishonga-giredhi cellulose ethers zvakare kwakaoma yakasimudzwa-yakaburitswa matrix mahwendefa, gastric-soluble coating materials, yakaramba ichiburitswa microcapsule packaging materials, yakaramba ichiburitswa zvinodhaka firimu zvinhu, nezvimwe.
Sodium carboxymethyl cellulose (CMC-Na) ndiyo cellulose ether ine hombe kubuda uye kushandiswa kumba nekune dzimwe nyika. Iyo ionic cellulose ether yakagadzirwa kubva mudonje nehuni kuburikidza nealkalization uye etherification ine chloroacetic acid. CMC-Na inowanzoshandiswa mishonga yemishonga. Inowanzo shandiswa sebhainda rekugadzirira kwakasimba uye seyakakora, kukora uye kumisa mumiriri wegadziriro yemvura. Inogona zvakare kushandiswa semvura-inonyungudika matrix uye firimu-kugadzira zvinhu. Inowanzo shandiswa seyakagadziriswa-yakaburitswa zvinodhaka firimu zvinhu uye yakatsiga-kuburitsa matrix piritsi mune yakatsigirwa (inodzorwa) yekuburitsa maumbirwo.
Pamusoro pe sodium carboxymethyl cellulose semishonga yekubatsira, croscarmellose sodium inogona zvakare kushandiswa semishonga excipients. Cross-linked carboxymethyl cellulose sodium (CCMC-Na) chinhu chisina kunyungudika nemvura icho carboxymethyl cellulose inobata ne-cross-linking agent pane imwe tembiricha (40-80°C) pasi pekuita kweinorganic acid catalyst uye inocheneswa. Iyo crosslinking agent inogona kuve propylene glycol, succinic anhydride, maleic anhydride, adipic anhydride, nezvimwe. Croscarmellose sodium inoshandiswa se disintegrant yemapiritsi, capsules uye granules mumuromo kugadzirira. Inovimba necapillary uye kuzvimba mhedzisiro kuti iwane kuparara. Iyo ine yakanaka compressibility uye yakasimba kuparara. Zvidzidzo zvakaratidza kuti dhigirii rekuzvimba re croscarmellose sodium mumvura rakakura kupfuura iro rezvinozivikanwa disintegrants senge yakaderera-inotsiva sodium carboxymethyl cellulose uye hydrated microcrystalline cellulose.
Methyl cellulose (MC) isiri-ionic cellulose monoether yakagadzirwa kubva mudonje nehuni kuburikidza nealkalization uye methyl chloride etherification. Methyl cellulose ine yakanakisa solubility yemvura uye yakagadzikana mupH renji re2.0 kusvika 13.0. Inoshandiswa zvakanyanya mumishonga yemishonga, uye inoshandiswa mumapiritsi emitauro, intramuscular jekiseni, ophthalmic kugadzirira, oral capsules, oral suspensions, oral tablets uye topical kugadzirira. Uye zvakare, mukusimudzira-kuburitswa maumbirwo, MC inogona kushandiswa senge hydrophilic gel matrix yakasimudzira-kuburitswa, gastric-soluble coating material, inosimudzira-kusunungurwa microcapsule packaging material, inosimudzira-kuburitswa zvinodhaka firimu zvinhu, nezvimwe.
Hydroxypropyl methylcellulose (HPMC) isiri-ionic cellulose yakasanganiswa ether yakagadzirwa kubva mudonje nehuni kuburikidza nealkalization uye etherification yepropylene oxide uye methyl chloride. Haina hwema, haina kunaka, haina chepfu, inonyungudika mumvura inotonhora, uye gels mumvura inopisa. Hydroxypropyl methylcellulose is a cellulose yakasanganiswa ether akasiyana ayo anga achikurumidza kuwedzera mukugadzirwa, kushandiswa uye kunaka mumakore gumi nemashanu apfuura. Icho zvakare chimwe chezvikuru zvemishonga excipients inoshandiswa kumba nekune dzimwe nyika. Yakave ichishandiswa semushonga wemishonga kweanoda kusvika makore makumi mashanu. Makore enhoroondo. Parizvino, kushandiswa kweHPMC kunonyanya kuratidzwa mune zvinotevera zvishanu zvinhu:
Imwe yakaita sebhainda uye disintegrant. HPMC sebhainda inogona kuita kuti mushonga uve nyore kunyorova, uye inogona kuwedzera mazana enguva mushure mekutora mvura, saka inogona kuvandudza zvakanyanya kuparara kana kuburitswa kwehwendefa. HPMC ine viscosity yakasimba, uye inogona kukwidziridza iyo particle viscosity uye kuvandudza kusungirirwa kwezvinhu zvakabikwa zvine crisp kana kuomarara magadzirirwo. HPMC ine yakaderera viscosity inogona kushandiswa sebhainda uye disintegrant, uye HPMC ine high viscosity inogona chete kushandiswa sebhainda.
Chechipiri, inoshandiswa seyakagadziriswa uye inodzorwa yekuburitsa zvinhu zvekugadzirira nemuromo. HPMC inowanzoshandiswa hydrogel matrix zvinhu mukuchengetedza-kuburitswa gadziriro. HPMC yegiredhi yakaderera viscosity giredhi (5～50mPa·s) inogona kushandiswa sebhainda, viscosity inowedzera mumiriri uye inomisa mumiriri, uye HPMC yegiredhi yepamusoro viscosity giredhi (4000 ~100000mPa·s) inogona kushandiswa kugadzirira yakasanganiswa zvinhu matrix matrix inoburitswa-inoburitsa mahwendefa uye inoenderera-inoburitsa hydrophilic mahwendefa. mahwendefa akasununguka. HPMC inonyungudika mugastrointestinal fluid, ine zvakanakira compressibility yakanaka, fluidity yakanaka, simba rekurodha zvinodhaka uye hunhu hwekuburitsa zvinodhaka husina kukanganiswa nepH. Iyo yakakosha zvakanyanya hydrophilic inotakura zvinhu mune inosimudzira-kuburitswa gadziriro masisitimu uye inowanzoshandiswa seIyo hydrophilic gel matrix uye coating zvinhu zvekugara-kuburitswa gadziriro, uye inoshandiswa mugastric inoyangarara gadziriro uye inosimudzira-kuburitsa zvinodhaka membrane ebetsero zvinhu.
Yechitatu ndeyekupfekedza firimu-inogadzira agent.HPMCine maitiro akanaka ekugadzira firimu. Firimu rakaumbwa naro rakafanana, rakajeka, uye rakaoma, uye hazvisi nyore kutevedzera panguva yekugadzira. Kunyanya kumishonga iyo iri nyore kutora unyoro uye isina kugadzikana, kuishandisa sechinhu chekuzviparadzanisa kunogona kuvandudza zvakanyanya kugadzikana kwemishonga uye kudzivirira Iyo firimu inoshandura ruvara. HPMC ine akasiyana e viscosity yakatarwa. Kana yakasarudzwa zvakanaka, kunaka uye kutaridzika kwemapiritsi akaputirwa zviri nani pane zvimwe zvinhu, uye chiyero chayo chakajairika 2% kusvika 10%.
Ina inoshandiswa se capsule material. Mumakore achangopfuura, nekubuda kwezvirwere zvemhuka zvepasi rose, zvichienzaniswa negelatin capsules, zvidyarwa zvave zvitsva zveindasitiri yemishonga neyekudya. Pfizer yakabudirira kubvisa HPMC kubva mumiti yepanyama uye yakagadzirira VcapTM yemiriwo capsules. Kuenzaniswa neyechinyakare gelatin hollow capsules, yemiriwo capsules ine zvakanakira kuchinjika kwakafara, hapana njodzi yekuyambuka-inobatanidza kuita, uye kugadzikana kwakanyanya. Mutengo wekuburitsa zvinodhaka wakanyanya kugadzikana, uye misiyano yemunhu idiki. Mushure mekuparara kwemuviri wemunhu, haipindi uye inogona kubudiswa. Yakabviswa kubva mumuviri. Panyaya yemamiriro ekuchengetedza, mushure mekuedzwa kwakawanda, inenge isina brittle pasi pemvura yakadzika, uye zvimiro zvekapule shell zvichiri kugadzikana pasi pehunyoro hwepamusoro, uye zvinyorwa zvakasiyana-siyana zvemiti capsules pasi pemamiriro ekuchengetedza zvakanyanya hazvikanganisi. Nekunzwisisa kwevanhu kwemakapisi echirimwa uye shanduko yepfungwa dzemishonga yeruzhinji kumba nekune dzimwe nyika, kudiwa kwemusika kwemakapisi echirimwa kuchakura nekukurumidza.
Yechishanu yakaita semumiririri wekumisa. Suspension type liquid gadziriro inowanzoshandiswa kukiriniki dosage fomu, inova heterogeneous dispersion system umo isinganyungudika yakasimba mishonga inoparadzirwa mumvura yekuparadzira svikiro. Kugadzikana kwegadziriro inogadzirisa hutano hwekumisa kugadzirira kwemvura. HPMC colloidal mhinduro inogona kuderedza iyo yakasimba-yemvura yepakati tension, kuderedza pamusoro pemahara simba rezvimedu zvakasimba, uye kudzikamisa iyo heterogeneous dispersion system. Iyo yakanakisa suspending agent. HPMC inoshandiswa semukobvu wemadonhwe emeso, ine zvinyorwa zve 0.45% kusvika 1.0%.
Hydroxypropyl cellulose (HPC) isiri-ionic cellulose monoether yakagadzirwa kubva mudonje nehuni kuburikidza nealkalization uye propylene oxide etherification. HPC inowanzonyungudika mumvura iri pasi pe40 ° C uye yakawanda ye polar solvents, uye kushanda kwayo kunoenderana nemukati we hydroxypropyl uye chiyero chepolymerization. HPC inogona kuenderana nemishonga yakasiyana-siyana uye ine inertness yakanaka.
Yakaderera-inotsiva hydroxypropyl cellulose(L-HPC)inonyanya kushandiswa sepiritsi disintegrant uye binder. Maitiro ayo ndeaya: nyore kudzvanya uye kuumba, kushanda kwakasimba, kunyanya kuoma kuumba, epurasitiki uye brittle mahwendefa, wedzera L-HPC inogona kuvandudza kuoma kwehwendefa uye kupenya kwechimiro, uye inogonawo kuita kuti piritsi racho riparare nekukurumidza, kuvandudza kunaka kwemukati kwehwendefa, uye kuvandudza maitiro ekurapa.
High substituted hydroxypropyl cellulose (H-HPC) inogona kushandiswa sechinhu chinosunga mahwendefa, magranules uye magranules akanaka mumunda wemishonga. H-HPC ine yakanakisa firimu-inogadzira zvimiro, uye inoguma firimu yakaoma uye elastic, iyo inogona kufananidzwa nemapurasitiki. Nekusanganiswa nemamwe anti-wet coating agents, kushanda kwefirimu kunogona kuwedzera kuvandudzwa, uye inowanzoshandiswa semafirimu ekuputira mahwendefa. H-HPC inogona zvakare kushandiswa sematrix zvinhu kugadzirira matrix akasimudzira-kuburitswa mahwendefa, anoramba achiburitswa-kuburitswa mapellets uye maviri-layer akatsigira-kuburitswa mahwendefa.
Hydroxyethyl cellulose (HEC) isiri-ionic cellulose monoether yakagadzirwa kubva mudonje nehuni kuburikidza nealkalization uye ethylene oxide etherification. HEC inonyanya kushandiswa seyakakora, colloidal inodzivirira agent, adhesive, dispersant, stabilizer, suspending agent, film-forming agent uye inononoka-kuburitsa zvinhu mumunda wekurapa. Inogona kuiswa kune emulsions, mafuta ekuzora, uye madonhwe emeso emishonga yemusoro. Oral liquid, mahwendefa akasimba, capsules uye mamwe mafomu emushonga. Hydroxyethyl cellulose yakaverengerwa muUS Pharmacopoeia/US National Formulary uye European Pharmacopoeia.
Ethyl cellulose (EC) ndeimwe yeanonyanya kushandiswa mvura-insoluble cellulose derivatives. EC haina muchetura, yakagadzikana, isinganyungudika mumvura, asidhi kana alkaline mhinduro, uye inonyungudika muorganic solvents senge ethanol uye methanol. Mushonga unowanzoshandiswa musanganiswa we toluene/ethanol 4/1 (huremu). EC ine zvakawanda zvekushandisa mumishonga inosimudzira-kusunungurwa gadziriro, uye inoshandiswa zvakanyanya semutakuri uye microcapsules, kuvhara firimu-kugadzira zvinhu, nezvimwewo zvekugadzirisa-kusunungurwa kugadzirira, zvakadai semapiritsi ekugadzirisa mahwendefa, adhesives, film coating materials, etc. Inoshandiswa sematrix zvinhu firimu kugadzirira marudzi akasiyana-siyana ematrix akasimbiswa-akasunungurwa kugadzirira-kusunungura mahwendefa ekugadzirisa-kusunungurwa-kusunungura mahwendefa akasanganiswa, inosimudzira-kuburitswa pellets, seyakavharirwa zvinhu zvekubatsira kugadzirira yakaramba-yakasunungurwa microcapsules; inogonawo kushandiswa zvakanyanya sechinhu chinotakura Inoshandiswa kugadzirira kupararira kwakasimba; inogona kushandiswa zvakanyanya mune tekinoroji yemishonga sechinhu chekugadzira firimu uye chivharo chekudzivirira, uye chinogona zvakare kushandiswa sebhainda uye kuzadza. Sechidziviriro chekudzivirira chemapiritsi, chinogona kuderedza kunzwisiswa kwemapiritsi kune hunyoro uye kudzivirira mishonga kubva pakusvibiswa uye kusvibiswa nehunyoro; inogona zvakare kugadzira inononoka-kuburitsa glue layer uye microencapsulate iyo polymer kuti irambe ichiburitsa iyo mushonga mhedzisiro.
Muchidimbu, mvura-soluble sodium carboxymethyl cellulose, methyl cellulose, hydroxypropyl methyl cellulose, hydroxypropyl cellulose, hydroxyethyl cellulose uye oiri-soluble ethyl cellulose zvese zvinoenderana nekusiyana kwavo Hunhu hwechigadzirwa hunoshandiswa mune zvemishonga excipients, disinteral materials, disinteral materials, disinteral materials. kugadzirira, kupfekedza firimu-kuumba vamiririri, capsule zvinhu uye suspending agents. Tichitarisa pasirese, makambani akawanda ekunze kwenyika dzakawanda (Shin-Etsu Japan, Dow Wolff neAshland) akaziva musika mukuru wemishonga cellulose muChina mune ramangwana, uye pamwe nekuwedzera kugadzirwa kana kubatanidzwa, ivo vakawedzera kuvepo kwavo mumunda uyu. Investment mukati mekushandisa. Dow Wolff yakazivisa kuti ichawedzera kutarisisa kwayo kuumbwa, zvinongedzo uye zvinodiwa zvemusika weChina wekugadzira mishonga, uye tsvakiridzo yekushandiswa kwayo ichaedzawo kuswedera pedyo nemusika. The Wolff Cellulose Division yeDow Chemical uye Colorcon Corporation yeUnited States yakagadzira mubatanidzwa wakasimba uye unodzorwa wekugadzirira kuburitswa pasi rose. Iine vanopfuura 1,200 vashandi mumaguta mapfumbamwe, 15 asset institution uye 6 GMP makambani. Vashandi vekutsvagisa vakashandiswa vanopa masevhisi kune vatengi munyika dzinosvika zana nemakumi matanhatu. Ashland ine mabhesi ekugadzira muBeijing, Tianjin, Shanghai, Nanjing, Changzhou, Kunshan neJiangmen, uye yakaisa mari munzvimbo nhatu dzekutsvagisa tekinoroji muShanghai neNanjing.
Zvinoenderana nenhamba kubva pawebhusaiti yeChina Cellulose Association, muna 2017, kugadzirwa kwemukati kweselulosi ether kwaive 373,000 matani uye huwandu hwekutengesa hwaive zviuru mazana matatu nemakumi matanhatu ematani. Muna 2017, iyo chaiyo yekutengesa ionicCMCyaiva 234,000 matani, kuwedzera kwe18.61% gore negore, uye kutengesa kwehuwandu hweCMC isiri-ionic yaiva 126,000 matani, kuwedzera kwe8,2% gore negore. Kuwedzera kune HPMC (yekuvaka zvinhu giredhi) zvisiri-ionic zvigadzirwa,HPMC(giredhi remishonga), HPMC (giredhi rekudya), HEC, HPC, MC, HEMC, nezvimwewo zvese zvakasimuka zvinopesana nemaitiro, uye kugadzirwa uye kutengesa kwakaramba kuchiwedzera. Ether dzemumba cellulose ether dzave dzichikura nekukurumidza kweanopfuura makore gumi, uye kubuda kwave kuri kutanga munyika. Zvisinei, zvizhinji zvezvigadzirwa zvemakambani e-cellulose ether zvinonyanya kushandiswa pakati nepakati pekupedzisira kwemhizha, uye iyo yakawedzerwa kukosha haisi yakakwirira.
Parizvino, mazhinji emabhizinesi emumba cellulose ether ari munguva yakaoma yekushandura uye kusimudzira. Vanofanira kuramba vachiwedzera tsvakiridzo yechigadzirwa nekuedza kwekusimudzira, kuramba vachipfumisa mhando dzezvigadzirwa, kushandisa zvizere China, musika mukuru pasi rose, uye kuwedzera kuedza kusimudzira misika yekunze kuitira kuti mabhizinesi akwanise kukura nekukurumidza. Pedzisa shanduko uye kukwidziridza, pinda yepakati-kusvika-yepamusoro yekupedzisira yeindasitiri, uye uwane benign uye girinhi kukura.
Nguva yekutumira: Kubvumbi-25-2024