1. Chikhalidwe cha HPMC
Hypromellose, dzina la Chingerezi hydroxypropyl methylcellulose, alias HPMC.Mapangidwe ake a molekyulu ndi C8H15O8-(C10Hl8O6)n-C8Hl5O8, ndipo kulemera kwa maselo ndi pafupifupi 86,000.Izi ndi semi-synthetic zakuthupi, zomwe ndi gawo la gulu la methyl komanso gawo la polyhydroxypropyl ether ya cellulose.Ikhoza kupangidwa ndi njira ziwiri: imodzi ndiyo kuchitira methyl cellulose ya kalasi yoyenera ndi NaOH, kenako ndikuchitapo kanthu ndi propylene oxide pansi pa kutentha kwambiri komanso kuthamanga kwambiri.Nthawi yochitapo iyenera kukhazikika kuti magulu a methyl ndi hydroxypropyl agwirizane ndi ether.Mawonekedwe a cholumikizidwa ndi mphete ya anhydroglucose ya cellulose, ndipo imatha kufikira digiri yomwe mukufuna;china ndi kuchitira thonje linter kapena nkhuni zamkati CHIKWANGWANI ndi caustic koloko, ndiyeno kupeza pochita ndi chlorinated methane ndi propylene okusayidi motsatizanatsatizana, ndiyeno zina woyengedwa , Pulverize, kupanga zabwino ndi yunifolomu ufa kapena granule.HPMC ndi mitundu yosiyanasiyana ya cellulose yachilengedwe, komanso ndi mankhwala abwino kwambiri opangira mankhwala, omwe ali ndi gwero lalikulu.Pakalipano, amagwiritsidwa ntchito kwambiri kunyumba ndi kunja, ndipo ndi imodzi mwazinthu zothandizira mankhwala zomwe zimagwiritsidwa ntchito kwambiri pakati pa mankhwala apakamwa.
Mtundu wa mankhwalawa ndi woyera mpaka woyera wamkaka, wopanda poizoni komanso wopanda kukoma, ndipo ndi granular kapena fibrous, ufa wosavuta kuyenda.Ndiwokhazikika pansi pa kuwunikira komanso chinyezi.Imafufuma m'madzi ozizira kuti ipange njira yoyera yoyera yamkaka yokhala ndi kukhuthala kwake.The Sol-gel osakaniza interconversion chodabwitsa akhoza kuchitika chifukwa cha kutentha kusintha kwa ndende ya njira.Ndizosavuta kusungunuka mu 70% mowa kapena dimethyl ketone, ndipo sizingasungunuke mu mowa wa anhydrous, chloroform kapena ethoxyethane.
Hypromellose imakhala yokhazikika pamene pH ili pakati pa 4.0 ndi 8.0, ndipo ikhoza kukhalapo mokhazikika pakati pa 3.0 ndi 11.0.Pambuyo posungira kwa masiku 10 pa kutentha kwa 20 ° C ndi chinyezi chachibale cha 80%, Kuchuluka kwa chinyezi kwa HPMC ndi 6.2%.
Chifukwa cha kusiyana kwa zomwe zili m'malo awiriwa m'mapangidwe a hypromellose, methoxy ndi hydroxypropyl, mitundu yosiyanasiyana ya mankhwala yawonekera.Pazigawo zina, mitundu yosiyanasiyana yazinthu imakhala ndi kukhuthala kwake komanso kutentha kwa Thermal gelation, chifukwa chake, imakhala ndi zinthu zosiyanasiyana ndipo imatha kugwiritsidwa ntchito pazifukwa zosiyanasiyana.Ma pharmacopoeias akumayiko osiyanasiyana ali ndi mawonekedwe ndi mafotokozedwe osiyanasiyana: European Pharmacopoeia imachokera pamagulu osiyanasiyana a ma viscosities osiyanasiyana komanso magawo osiyanasiyana osinthira zinthu pamsika.Imawonetsedwa ndi giredi kuphatikiza nambala.Chigawochi ndi mPa•s.Mukawonjezera manambala 4 kuti muwonetse zomwe zili ndi mtundu wa cholowa chilichonse cha hypromellose, mwachitsanzo, hypromellose 2208, manambala awiri oyamba amayimira pafupifupi kuchuluka kwa gulu la methoxy, manambala awiri omaliza amayimira hydroxypropyl Pafupifupi peresenti ya milandu.
2.Njira yosungunula HPMC m'madzi
2.1 Njira yamadzi otentha
Popeza hypromellose sisungunuka m'madzi otentha, imatha kumwazikana m'madzi otentha koyambirira, ndipo ikakhazikika, njira ziwiri zodziwika bwino zimafotokozedwa motere:
(1) Ikani madzi otentha ofunikira mumtsuko ndikutenthetsa mpaka pafupifupi 70 ℃.Pang'onopang'ono yonjezerani mankhwalawa pansi pa kuyambitsa pang'onopang'ono.Pachiyambi, mankhwalawa amayandama pamwamba pa madzi, ndiyeno pang'onopang'ono amapanga slurry.Kuziziritsa slurry.
(2) Onjezani 1/3 kapena 2/3 ya kuchuluka kwa madzi ofunikira mumtsuko ndikuwotchera mpaka 70 ° C kuti mumwaze mankhwalawo kuti mukonzekere slurry yamadzi otentha, ndikuwonjezera madzi otsalawo kapena madzi oundana. kwa madzi otentha slurry Mu slurry, ozizira kusakaniza mutatha kuyambitsa.
2.2 Njira yosakaniza ufa
Tinthu tating'onoting'ono ta ufa ndi zosakaniza zina za ufa wofanana kapena wokulirapo zimamwazikana ndi kusakaniza kowuma, kenako madzi amawonjezedwa kuti asungunuke.Panthawi imeneyi, hypromellose imatha kusungunuka popanda kuphatikiza.
3. Ubwino wa HPMC
3.1 Kusungunuka kwamadzi ozizira
Imasungunuka m'madzi ozizira pansi pa 40 ° C kapena 70% ethanol.Sipasungunuke m'madzi otentha kuposa 60 ° C, koma imatha kupangidwanso.
3.2 Kusakhazikika kwa Chemical
Hypromellose (HPMC) ndi mtundu wa ether wopanda ionic cellulose.Yankho lake lilibe mtengo wa ionic ndipo silimalumikizana ndi mchere wachitsulo kapena ma ionic organic compounds.Choncho, ena excipients sachita nawo pa kukonzekera ndondomeko.
3.3 Kukhazikika
Zimakhala zokhazikika kwa asidi ndi zamchere, ndipo zimatha kusungidwa kwa nthawi yaitali pakati pa pH 3 mpaka 1l, ndipo kukhuthala kwake kulibe kusintha koonekeratu.The aqueous solution of hypromellose (HPMC) imakhala ndi anti-mold effect ndipo imatha kusunga kukhazikika kwa mamasukidwe abwino pakasungidwe kwa nthawi yayitali.Zothandizira zamankhwala zomwe zimagwiritsa ntchito HPMC zimakhala ndi kukhazikika kwabwinoko kuposa zomwe zimagwiritsa ntchito zopangira zachikhalidwe (monga dextrin, wowuma, ndi zina).
3.4 Kusintha kwa mamasukidwe akayendedwe
Osiyana mamasukidwe akayendedwe zotumphukira za HPMC akhoza wothira mu magawo osiyanasiyana, ndi mamasukidwe akayendedwe ake akhoza kusintha malinga ndi lamulo linalake, ndipo ali ndi ubale wabwino liniya, kotero izo zikhoza kusankhidwa malinga ndi zofunika.
3.5 Metabolic inertia
HPMC si odzipereka kapena zimapukusidwa mu thupi, ndipo sapereka zopatsa mphamvu, choncho ndi otetezeka excipient kwa mankhwala.
3.6 Chitetezo
Nthawi zambiri amakhulupirira kuti HPMC ndi zinthu zopanda poizoni komanso zosakwiyitsa.Mlingo wakupha wapakati wa mbewa ndi 5g/kg, ndipo mlingo wapakati wakupha makoswe ndi 5.2g/kg.Mlingo watsiku ndi tsiku ndi wopanda vuto m'thupi la munthu.
4. Kugwiritsa ntchito HPMC pokonzekera
4.1 Imagwiritsidwa ntchito ngati zinthu zokutira filimu komanso kupanga filimu
Hypromellose (HPMC) imagwiritsidwa ntchito ngati mapiritsi okhala ndi filimu.Poyerekeza ndi mapiritsi ophimbidwa achikhalidwe monga mapiritsi okhala ndi shuga, mapiritsi ophimbidwa alibe ubwino wodziwikiratu pobisa kukoma ndi maonekedwe, koma kuuma kwawo ndi friability , Kutsekemera kwachinyezi, kupasuka, kupaka kulemera kwa kulemera ndi zizindikiro zina zabwinoko.Kalasi yotsika kwambiri ya mankhwalawa imagwiritsidwa ntchito ngati filimu yosungunuka yamadzi yosungunuka pamapiritsi ndi mapiritsi, ndipo kalasi yapamwamba kwambiri imagwiritsidwa ntchito ngati filimu yophimba filimu yazinthu zosungunulira za organic.Kugwiritsa ntchito ndende nthawi zambiri 2.0% -20%.
4.2 ngati chomangira komanso chosokoneza
Kalasi yotsika kwambiri ya mankhwalawa imatha kugwiritsidwa ntchito ngati chomangira komanso chosokoneza pamapiritsi, mapiritsi, ndi ma granules, ndipo kalasi yapamwamba kwambiri ingagwiritsidwe ntchito ngati chomangira.Mlingo umasiyanasiyana ndi mitundu yosiyanasiyana ndi zofunika.Nthawi zambiri, kuchuluka kwa zomangira zomwe zimagwiritsidwa ntchito pamapiritsi owuma ndi 5%, ndipo kuchuluka kwa zomangira zomwe zimagwiritsidwa ntchito pamapiritsi onyowa ndi 2%.
4.3 Monga woyimitsa ntchito
Kuyimitsa wothandizila ndi viscous gel osakaniza ndi hydrophilicity.Ntchito suspending wothandizira mu suspending wothandizira akhoza m'mbuyo sedimentation liwiro la particles, ndipo akhoza Ufumuyo pamwamba particles kuteteza particles ku polymerizing ndi condensing mu misa.Oyimitsa ntchito amagwira ntchito yofunika kwambiri popanga kuyimitsidwa.HPMC ndi mitundu yosiyanasiyana yoyimitsa.The colloidal njira kusungunuka mu izo akhoza kuchepetsa mavuto a madzi olimba mawonekedwe ndi ufulu mphamvu pa yaing'ono olimba particles, potero utithandize bata la sakanikira kubalalitsidwa dongosolo.Izi ndi mkulu-kukhuthala kwamakayendedwe kuyimitsidwa madzi kukonzekera wokonzeka ngati suspending wothandizira.Iwo ali wabwino suspending tingati, zosavuta kufalitsanso, sanali zomata, ndi zabwino flocculated particles.Kuchuluka kwanthawi zonse ndi 0.5% mpaka 1.5%.
4.4 Imagwiritsidwa ntchito ngati chotchinga, chotsitsa pang'onopang'ono komanso chowongolera komanso chopanga pore
Mlingo wapamwamba kwambiri wa mankhwalawa umagwiritsidwa ntchito pokonzekera mapiritsi otulutsidwa a hydrophilic gel matrix, retarders ndi othandizira kutulutsa owongolera amapiritsi osakanikirana a matrix okhazikika.Zimakhala ndi zotsatira zochedwetsa kutulutsidwa kwa mankhwala.Kugwiritsa ntchito kwake ndi 10% ~ 80% (W / W).Otsika mamasukidwe kalasi kalasi ntchito ngati pore-kupanga wothandizila kuti mosalekeza kapena ankalamulira kumasulidwa formulations.The koyamba mlingo chofunika achire zotsatira za mtundu uwu wa piritsi akhoza mwamsanga anafika, ndiyeno kupitiriza kapena ankalamulira kumasulidwa tingati, ndi ogwira magazi mankhwala ndende anakhalabe mu thupi .Hypromellose hydrates kupanga gel wosanjikiza akakumana ndi madzi.Njira yotulutsa mankhwala kuchokera papiritsi ya matrix makamaka kufalikira kwa gel osanjikiza ndi kukokoloka kwa gel osanjikiza.
4.5 Guluu woteteza amagwiritsidwa ntchito ngati thickener ndi colloid
Izi zikagwiritsidwa ntchito ngati thickener, ndende wamba ndi 0.45% ~ 1.0%.Izi mankhwala akhoza kuonjezera bata wa guluu hydrophobic, kupanga colloid zoteteza, kupewa tinthu coalescence ndi agglomeration, potero inhibiting mapangidwe matope.Kukhazikika kwake mwachizolowezi ndi 0.5% ~ 1.5%.
4.6 Amagwiritsidwa ntchito ngati zinthu za capsule
Nthawi zambiri, chipolopolo cha kapisozi cha kapisozi chimakhala ndi gelatin.Kapangidwe ka chipolopolo cha kapisozi cha Ming ndi chosavuta, koma pali zovuta ndi zochitika zina monga kusatetezedwa kwa chinyezi ndi mankhwala okhudzidwa ndi okosijeni, kuchepetsa kutha kwa mankhwala, komanso kuchedwa kwa kutha kwa chipolopolo cha kapisozi panthawi yosungira.Chifukwa chake, hypromellose imagwiritsidwa ntchito ngati choloweza m'malo mwa kapisozi pokonzekera makapisozi, omwe amathandizira kuumbika komanso kugwiritsa ntchito kapisozi, ndipo adalimbikitsidwa kwambiri kunyumba ndi kunja.
4.7 Monga bioadhesive
Ukadaulo wa bioadhesive, kugwiritsa ntchito ma polima okhala ndi ma polima a bioadhesive, potsatira mucosa yachilengedwe, kupititsa patsogolo kupitiliza ndi kulimba kwa kulumikizana pakati pa kukonzekera ndi mucous membrane, kotero kuti mankhwalawa amamasulidwa pang'onopang'ono ndikumwedwa ndi mucosa kuti akwaniritse cholinga. chithandizo.Amagwiritsidwa ntchito kwambiri tsopano Amagwiritsidwa ntchito pochiza matenda a m'mphuno ndi m'kamwa mucosa.Tekinoloje ya m'mimba ya bioadhesion ndi njira yatsopano yoperekera mankhwala yomwe idapangidwa zaka zaposachedwa.Sikuti prolongs okhala nthawi ya mankhwala kukonzekera mu m`mimba thirakiti, komanso bwino kukhudzana ntchito ya mankhwala ndi selo nembanemba wa mayamwidwe malo ndi kusintha fluidity wa selo nembanemba.Mphamvu yolowera ya mankhwala ku maselo a epithelial a intestine yaing'ono imakula, potero kumapangitsa kuti mankhwalawa akhale ndi bioavailability.
4.8 Ngati gel osakaniza
Monga zomatira zokonzekera khungu, gel osakaniza ali ndi mndandanda wa ubwino monga chitetezo, kukongola, kuyeretsa kosavuta, mtengo wotsika, njira yosavuta yokonzekera, komanso kugwirizana bwino ndi mankhwala.M'zaka zaposachedwapa, walandira chidwi kwambiri ndipo wakhala chitukuko cha khungu kunja kukonzekera.malangizo.
4.9 Monga choletsa mpweya mu dongosolo emulsification
Nthawi yotumiza: Dec-16-2021