Makapisozi olimba/Makapisozi opanda kanthu a HPMC/makapisozi amasamba/API yogwira ntchito kwambiri komanso zosakaniza zosamva chinyezi/sayansi yamafilimu/kuwongolera kutulutsa kosalekeza/ukadaulo waukadaulo wa OSD….
Kuchita bwino kwambiri, kupanga kosavuta, komanso kuwongolera kwa odwala, zinthu za Oral Solid Dosage (OSD) zimakhalabe njira yomwe anthu opanga mankhwala amawakonda.
Mwa mabungwe 38 ang'onoang'ono a mamolekyu (NMEs) omwe adavomerezedwa ndi US Food and Drug Administration mu 2019, 26 anali OSD1.Mu 2018, msika wazinthu zodziwika bwino za OSD zomwe zidapangidwa ndi CMOs pamsika waku North America zinali pafupifupi $ 7.2 biliyoni USD 2. Msika waung'ono wotulutsa ma molekyulu akuyembekezeka kupitilira USD 69 biliyoni mu 20243. Deta yonseyi ikuwonetsa kuti pakamwa mafomu olimba a mlingo (OSDs) adzapitilirabe.
Mapiritsi amalamulirabe msika wa OSD, koma makapisozi olimba akukhala njira yowoneka bwino.Izi ndi zina chifukwa cha kudalirika kwa makapisozi monga njira yoyendetsera, makamaka omwe ali ndi APIs potency antitumor.Makapisozi ndi oyandikana kwambiri ndi odwala, amabisa fungo losasangalatsa komanso zokonda, ndipo ndi osavuta kumeza, kuposa mitundu ina ya mlingo.
Julien Lamps, Product Manager ku Lonza Capsules and Health Ingredients, akukambirana za ubwino wosiyanasiyana wa makapisozi olimba pamapiritsi.Amagawana nzeru zake za makapisozi opanda kanthu a hydroxypropyl methylcellulose (HPMC) ndi momwe angathandizire opanga mankhwalawo kukhathamiritsa malonda awo pomwe akukwaniritsa zofuna za ogula za mankhwala opangidwa kuchokera ku mbewu.
Makapisozi olimba: Sinthani kutsata kwa odwala ndikuwongolera magwiridwe antchito
Odwala nthawi zambiri amavutika ndi mankhwala omwe amalawa kapena kununkhiza, ovuta kuwameza, kapena omwe angakhale ndi zotsatira zoyipa.Poganizira izi, kupanga mafomu a mlingo wosavuta kugwiritsa ntchito kungathandize kuti odwala azitsatira njira zachipatala.Makapisozi olimba ndi njira yabwino kwa odwala chifukwa, kuwonjezera pa kukoma kwa masking ndi fungo, amatha kutengedwa mobwerezabwereza, kuchepetsa kulemedwa kwa piritsi, komanso kukhala ndi nthawi yabwino yotulutsa, pogwiritsa ntchito kumasulidwa kwachangu, kumasulidwa koyendetsedwa ndi kumasulidwa pang'onopang'ono. kukwaniritsa.
Kuwongolera bwino pamachitidwe otulutsa mankhwala, mwachitsanzo pogwiritsa ntchito micropelletizing API, kumatha kuletsa kutaya kwa mlingo ndikuchepetsa zotsatira zoyipa.Opanga mankhwala akuwona kuti kuphatikiza ukadaulo wa multiparticulate ndi makapisozi kumawonjezera kusinthasintha komanso kuchita bwino kwa API yoyendetsedwa yotulutsidwa.Ikhoza kuthandizira ma pellets omwe ali ndi ma API osiyanasiyana mu capsule yomweyi, zomwe zikutanthauza kuti mankhwala ambiri amatha kuperekedwa nthawi imodzi mumagulu osiyanasiyana, kuchepetsanso kuchuluka kwa dosing.
Makhalidwe a pharmacokinetic ndi pharmacodynamic a mapangidwe awa, kuphatikizapo multiparticulate system4, extrusion spheronization API3, ndi kusakanikirana kwa mlingo wokhazikika system5, adawonetsanso kuberekana bwino poyerekeza ndi machitidwe ochiritsira.
Ndi chifukwa cha kusintha komwe kungathe kuchitika pakutsata odwala komanso kuchita bwino komwe kufunikira kwa msika kwa ma API a granular omwe ali mu makapisozi olimba kukukulirakulira.
Zokonda polima:
Kufunika kwa makapisozi amasamba m'malo mwa makapisozi olimba a gelatin
Makapisozi olimba achikhalidwe amapangidwa ndi gelatin, komabe, makapisozi olimba a gelatin amatha kubweretsa zovuta mukakumana ndi hygroscopic kapena chinyezi.Gelatin ndi nyama yomwe imachokera ku nyama yomwe imakonda kugwirizanitsa zomwe zimakhudza khalidwe la kusungunuka, ndipo zimakhala ndi madzi ochulukirapo kuti zisunge kusinthasintha kwake, komanso zimatha kusinthanitsa madzi ndi APIs ndi zowonjezera.
Kuphatikiza pa kukhudzidwa kwa zinthu za kapisozi pakuchita kwazinthu, odwala ochulukirachulukira safuna kudya nyama pazifukwa za chikhalidwe kapena chikhalidwe ndipo akufunafuna mankhwala opangidwa ndi zomera kapena vegan.Kuti akwaniritse chosowachi, makampani opanga mankhwala akupitilizabe kugwiritsa ntchito njira zatsopano zopangira mankhwala kuti apange njira zina zopangira mbewu zomwe zili zotetezeka komanso zothandiza.Kupita patsogolo kwa sayansi yazinthu kwapangitsa kuti makapulisi opangidwa ndi zomera azitha kukhala otheka, kupereka odwala njira yosachokera ku zinyama kuwonjezera pa ubwino wa makapisozi a gelatin - kumeza, kupanga mosavuta, komanso kutsika mtengo.
Kuti zithetsedwe bwino komanso zogwirizana:
Kugwiritsa ntchito HPMC
Pakali pano, imodzi mwa njira zabwino zopangira gelatin ndi hydroxypropyl methylcellulose (HPMC), polima yochokera ku ulusi wamtengo.
HPMC imakhala yochepa kwambiri pamankhwala kuposa gelatin komanso imamwa madzi ochepa kuposa gelatin6.Madzi otsika a makapisozi a HPMC amachepetsa kusinthana kwa madzi pakati pa kapisozi ndi zomwe zili mkati, zomwe nthawi zina zimatha kupititsa patsogolo kukhazikika kwa mankhwala ndi thupi lachipangidwe, kuwonjezera moyo wa alumali, komanso kuthana ndi zovuta za hygroscopic APIs ndi zowonjezera.Makapisozi opanda kanthu a HPMC samva kutentha komanso osavuta kusunga ndi kunyamula.
Ndi kuwonjezeka kwa ma API apamwamba kwambiri, zofunikira zopangira mapangidwe zimakhala zovuta kwambiri.Pakadali pano, opanga mankhwala apeza zotsatira zabwino kwambiri pofufuza kugwiritsa ntchito makapisozi a HPMC m'malo mwa makapisozi achikhalidwe a gelatin.M'malo mwake, makapisozi a HPMC pakadali pano amakondedwa pamayesero azachipatala chifukwa chogwirizana bwino ndi mankhwala ambiri komanso othandizira7.
Kupititsa patsogolo teknoloji ya capsule ya HPMC kumatanthauzanso kuti opanga mankhwala osokoneza bongo amatha kugwiritsa ntchito bwino magawo ake osungunuka ndikugwirizana ndi ma NME osiyanasiyana, kuphatikizapo mankhwala amphamvu kwambiri.
Makapisozi a HPMC opanda gel osakaniza amakhala ndi zinthu zabwino kwambiri zosungunula popanda ion ndi pH kudalira, kotero kuti odwala adzalandira chimodzimodzi achire akamamwa mankhwalawa pamimba yopanda kanthu kapena chakudya.Monga momwe chithunzi 1.8 chikusonyezera
Zotsatira zake, kusintha kwa kusungunuka kungalole odwala kuti asakhale ndi nkhawa pakukonzekera Mlingo wawo, potero akuwonjezera kutsata.
Kuonjezera apo, kupitiriza kwatsopano mu HPMC capsule membrane solutions kungathandizenso chitetezo cha m'mimba ndi kumasulidwa mofulumira m'madera ena a m'mimba, kupititsa patsogolo mankhwala okhudzana ndi njira zina zothandizira, komanso kupititsa patsogolo kugwiritsa ntchito makapisozi a HPMC.
Njira ina yogwiritsira ntchito makapisozi a HPMC ndi pazida zopumira pamapapo.Kufuna kwa msika kukukulirakulirabe chifukwa chakukula kwa bioavailability popewa kuphatikizika koyamba kwa chiwindi komanso kupereka njira yolunjika yoyang'anira matenda monga mphumu ndi matenda osachiritsika a m'mapapo (COPD) ndi makonzedwe awa.
Opanga mankhwala nthawi zonse amayang'ana kupanga njira zochiritsira zotsika mtengo, zochezeka kwa odwala, komanso zogwira mtima pamatenda opumira, ndikuwunikanso njira zoperekera mankhwala opumira pamatenda ena apakati pa mitsempha (CNS).zofuna zikuwonjezeka.
Madzi otsika a makapisozi a HPMC amawapangitsa kukhala abwino kwa ma API a hygroscopic kapena osamva madzi, ngakhale ma electrostatic properties pakati pa mapangidwe ndi makapisozi opanda kanthu ayeneranso kuganiziridwa panthawi yonse ya chitukuko8.
maganizo omaliza
Kukula kwa sayansi ya membrane ndi ukadaulo waukadaulo wa OSD kwayala maziko a makapisozi a HPMC kuti alowe m'malo mwa makapisozi a gelatin m'mapangidwe ena, ndikupereka zosankha zambiri pakuwongolera magwiridwe antchito azinthu.Kuphatikiza apo, kugogomezera zomwe ogula amakonda komanso kukwera kwa kufunikira kwamankhwala otsika mtengo omwe amakokedwa kwalimbikitsa kufunikira kwa makapisozi opanda kanthu omwe amagwirizana bwino ndi mamolekyu omwe samva chinyezi.
Komabe, kusankha kwa nembanemba ndikofunikira pakuwonetsetsa kuti chinthucho chikuyenda bwino, ndipo kusankha koyenera pakati pa gelatin ndi HPMC kumatha kupangidwa ndi ukatswiri woyenera.Kusankha koyenera kwa nembanemba sikungangowonjezera mphamvu komanso kuchepetsa zotsatira zoyipa, komanso kumathandizira kuthana ndi zovuta zina.
Nthawi yotumiza: Sep-23-2022