Ngokunzulu kophando lwenkqubo yokuhanjiswa kweziyobisi kunye neemfuno ezingqongqo, abancedisi abatsha bamayeza bavela, phakathi kwayo i-hydroxypropyl methylcellulose isetyenziswa kakhulu. Eli phepha liphonononga izicelo zasekhaya nezangaphandle ze-hydroxypropyl methylcellulose. Indlela yokuvelisa kunye neenzuzo zayo kunye nokungonakali, iteknoloji yezixhobo kunye nethemba lokuphucula ekhaya, kunye nokusetyenziswa kwayo kwintsimi ye-excipients yamachiza.
Amagama angundoqo: abancedisi bamayeza; i-hydroxypropyl methylcellulose; imveliso isicelo
1. Intshayelelo
I-excipients yamachiza ibhekisela kwixesha eliqhelekileyo kuzo zonke ezinye izinto zonyango ezongeziweyo ekulungiseleleni ngaphandle kweyeza eliphambili ukwenzela ukusombulula ukwakheka, ukufumaneka kunye nokhuseleko lokulungiselela kwinkqubo yokuvelisa kunye nokuyila ukulungiswa. Abancedisi bamachiza babaluleke kakhulu kumalungiselelo amayeza. Kukho iintlobo ezininzi ze-excipients zamayeza kumalungiselelo asekhaya nakwamanye amazwe, kodwa kwiminyaka yakutshanje, iimfuno zokucoceka, ukutshatyalaliswa, ukuzinza, i-bioavailability kwi-vivo, ukuphuculwa kwempembelelo yonyango kunye nokunciphisa imiphumo emibi yamachiza iya phezulu kwaye iphezulu. , ukwenza ukuvela ngokukhawuleza kwabancedisi abatsha kunye neenkqubo zophando ukwenzela ukuba kuphuculwe ukusebenza kakuhle kokulungiswa kweziyobisi kunye nomgangatho wokusetyenziswa. Inani elikhulu lomzekelo wedatha libonisa ukuba i-hydroxypropyl methylcellulose inokuhlangabezana nezi mfuno zingentla njenge-excipient ye-pharmaceutical ephezulu. Imeko yangoku yophando kunye nemveliso yangaphandle kunye nokusetyenziswa kwayo kwintsimi yamalungiselelo amayeza iphinde ishwankathelwe.
2 Isishwankathelo seepropati ze-HPMC
I-HPMC ngumgubo omhlophe okanye otyheli kancinane, ongenavumba, ongenavumba, ongeyotyhefu ofunyenwe nge-etherification yealkali cellulose, ipropylene oxide kunye nealkyl chloride. Inyibilika ngokulula emanzini angaphantsi kwe-60 ° C kunye ne-70% ye-ethanol kunye ne-acetone, i-isoacetone, kunye ne-dichloromethane exutywe i-solvent; I-HPMC inozinzo olomeleleyo, ibonakaliswe ngokukodwa: okokuqala, isisombululo sayo samanzi asinayo intlawulo kwaye ayiphenduli ngeetyuwa zetsimbi okanye i-ionic organic compounds; okwesibini, nayo iyamelana neeasidi okanye iziseko. Uzinzile ngokwentelekiso. Ziimpawu zozinzo ze-HPMC ezenza umgangatho wamayeza ane-HPMC njengezincedisi uzinze ngakumbi kunalawo anezinto zemveli. Kuphononongo toxicology of HPMC njengoko excipients, kuboniswa ukuba HPMC akayi metabolized emzimbeni, kwaye akathabathi nxaxheba umzimba womntu. Unikezelo lwamandla, akukho tyhefu kunye nemiphumo emibi kumachiza, i-excipients zamachiza ezikhuselekileyo.
3 Uphando ngemveliso yangaphakathi neyangaphandle yeHPMC
3.1 Isishwankathelo sobugcisa bemveliso ye-HPMC ekhaya nakwamanye amazwe
Ukuze uhlangabezane ngcono neemfuno ezikhulayo kunye nezikhulayo zamalungiselelo amayeza ekhaya nakwamanye amazwe, iteknoloji yemveliso kunye nenkqubo ye-HPMC nazo zihlala zikhula kwindlela enzima kunye nende. Inkqubo yemveliso ye-HPMC inokohlulwa ibe yindlela yebhetshi kunye nendlela eqhubekayo. Iindidi eziphambili. Inkqubo eqhubekayo isetyenziswa ngokubanzi kumazwe angaphandle, ngelixa inkqubo yebhetshi isetyenziswa kakhulu eTshayina. Ukulungiswa kwe-HPMC kubandakanya amanyathelo okulungisa i-alkali cellulose, ukusabela kwe-etherification, unyango lokucoca, kunye nonyango olugqityiweyo lwemveliso. Phakathi kwazo, kukho iintlobo ezimbini zeendlela zenkqubo yokusabela kwe-etherification. : Indlela yesigaba segesi kunye nendlela yesigaba solwelo. Ukuthetha ngokuthelekisayo, indlela yesigaba segesi ineengenelo zomthamo omkhulu wemveliso, ubushushu obuphantsi bokusabela, ixesha elifutshane lokuphendula, kunye nolawulo lokusabela oluchanekileyo, kodwa uxinzelelo lokusabela lukhulu, utyalo-mali lukhulu, kwaye xa ingxaki isenzeka, kulula ukuyifumana. bangela iingozi ezinkulu. Indlela yesigaba solwelo ngokubanzi ineengenelo zoxinzelelo oluphantsi lokusabela, umngcipheko ophantsi, ixabiso eliphantsi lotyalo-mali, ulawulo olulula lomgangatho, kunye nokutshintshwa ngokulula kweentlobo; kodwa kwangaxeshanye, i-reactor efunwa yindlela yesigaba solwelo ayinakuba nkulu kakhulu, ekwanciphisa umthamo wokusabela. Xa kuthelekiswa nendlela yesigaba segesi, ixesha lokuphendula lide, amandla okuvelisa ancinci, izixhobo ezifunekayo zininzi, umsebenzi unzima, kwaye ulawulo oluzenzekelayo kunye nokuchaneka kuphantsi kunendlela yesigaba segesi. Okwangoku, amazwe aphuhlileyo anjengeYurophu kunye neUnited States ikakhulu asebenzisa indlela yesigaba segesi. Kukho iimfuno eziphezulu malunga neteknoloji kunye notyalo-mali. Ukuqwalasela imeko yelizwe lethu, inkqubo yesigaba solwelo ixhaphake kakhulu. Nangona kunjalo, kukho iindawo ezininzi e-China eziqhubekayo nokuhlaziya kunye nokuvuselela itekhnoloji, ukufunda kumanqanaba angaphandle angaphandle, kwaye baqalise iinkqubo eziqhubekayo. Okanye indlela yokwazisa indlela yegesi yangaphandle.
3.2 Uphuculo lobuchwephesha bemveliso yeHPMC yasekhaya
I-HPMC kwilizwe lam inamandla amakhulu ophuhliso. Phantsi kwamathuba alungileyo anjalo, yinjongo yomphandi ngamnye ukuqhubeka nokuphucula iteknoloji yemveliso ye-HPMC kunye nokunciphisa umsantsa phakathi koshishino lwasekhaya lwe-HPMC kunye namazwe angaphandle aphambili. Inkqubo ye-HPMC Lonke ikhonkco kwinkqubo yodibaniso lubaluleke kakhulu kwimveliso yokugqibela, phakathi kwayo i-alkalization kunye ne-etherification reactions [6] zezona zibalulekileyo. Ke ngoko, iteknoloji yemveliso yasekhaya ye-HPMC ekhoyo inokuqhutywa ukusuka kula macala mabini. Inguqu. Okokuqala, ukulungiswa kwe-alkali cellulose kufuneka kuqhutywe kwiqondo lokushisa eliphantsi. Ukuba imveliso ye-viscosity ephantsi ilungiselelwe, ezinye i-oxidants zingongezwa; ukuba imveliso ye-viscosity ephezulu ilungiselelwe, indlela yokukhusela igesi ye-inert ingasetyenziswa. Okwesibini, ukusabela kwe-etherification kuqhutyelwa kwiqondo lokushisa eliphezulu. Beka i-toluene kwisixhobo se-etherification kwangaphambili, thumela i-alkali cellulose kwisixhobo ngepompo, kwaye ungeze inani elithile le-isopropanol ngokweemfuno. Nciphisa umlinganiselo oqinileyo wolwelo. Kwaye sebenzisa inkqubo yokulawula ikhompyuter, enokukhawuleza ubushushu bengxelo, Iiparamitha zeNkqubo ezifana noxinzelelo kunye ne-pH zihlengahlengiswa ngokuzenzekelayo. Ewe, ukuphuculwa kweteknoloji yemveliso ye-HPMC nako kungaphuculwa ukusuka kwindlela yenkqubo, ukusetyenziswa kwezinto ezikrwada, ukucokisa unyango kunye neminye imiba.
4 Ukusetyenziswa kweHPMC kwicandelo lamayeza
4.1 Ukusetyenziswa kwe-HPMC kulungiselelo lweepilisi ezikhutshwa ngokuqhubekayo
Kwiminyaka yakutshanje, kunye nokuqhubeka nzulu kophando lwenkqubo yokuhanjiswa kweziyobisi, uphuhliso lwe-HPMC ye-viscosity ephezulu ekusetyenzisweni kwamalungiselelo okukhutshwa okuzinzileyo kuye kwatsala ingqalelo enkulu, kwaye umphumo wokukhutshwa okuzinzileyo kulungile. Xa kuthelekiswa, kusekho umsantsa omkhulu ekusetyenzisweni kweetafile zematrix ezikhutshwa ngokuzinzileyo. Ngokomzekelo, xa kuthelekiswa i-HPMC yasekhaya nakwamanye amazwe ye-nifedipine iipilisi zokukhululwa okuqhubekayo kunye ne-matrix ye-propranolol hydrochloride i-matrix ekhutshwe ngokuqhubekayo iipilisi, kufunyaniswa ukuba Ukusetyenziswa kwe-HPMC yasekhaya kumalungiselelo okukhululwa okuzinzileyo kufuna ukuphuculwa okuqhubekayo ukuphucula ngokuqhubekayo. inqanaba lamalungiselelo asekhaya.
4.2 Ukusetyenziswa kweHPMC ekutyebeni kwezithambisi zonyango
Ngenxa yeemfuno zokuhlolwa okanye unyango lwezinye izixhobo zonyango namhlanje, xa ungena okanye ushiya amalungu omntu kunye nezicubu, umphezulu wesixhobo kufuneka ube neempawu ezithile zokuthambisa, kwaye i-HPMC ineempawu ezithile zokuthambisa. Xa kuthelekiswa nezinye izithambiso zeoli, i-HPMC ingasetyenziswa njengento yokuthambisa yonyango , engakwazi ukunciphisa kuphela ukunxiba kwezixhobo, kodwa ihlangabezane neemfuno zokuthanjiswa kwezonyango kunye nokunciphisa iindleko.
4.3 Ukusetyenziswa kwe-HPMC njengefilimu yokupakisha yendalo ye-antioxidant enyibilikayo emanzini kunye nemathiriyeli yokugquma ifilimu kunye nemathiriyeli yokwenza ifilimu.
Xa kuthelekiswa nezinye izixhobo tablet ezigqunywe zemveli, HPMC iingenelo ezicacileyo ngokobulukhuni, friability kunye nokufunxa ukufuma. I-HPMC yamabanga ahlukeneyo e-viscosity ingasetyenziswa njengepakethe enyibilikayo yamanzi kwiipilisi kunye neepilisi. Isenokusetyenziswa njengefilimu yokupakisha kwiinkqubo ze-organic solvent. Kunokuthiwa i-HPMC yeyona nto isetyenziswa kakhulu kwifilimu yokugquma ifilimu kwilizwe lam. Ukongeza, i-HPMC ingasetyenziselwa njengezinto zokwenza ifilimu kwi-ejenti yefilimu, kunye nefilimu yokupakisha i-anti-oxidative yamanzi e-soluble esekelwe kwi-HPMC isetyenziswa ngokubanzi ekugcinweni kokutya, ngakumbi iziqhamo.
4.4 Ukusetyenziswa kwe-HPMC njengemathiriyeli yeqokobhe le-capsule
I-HPMC ingasetyenziswa njengesixhobo sokulungiselela amaqokobhe e-capsule. Izinto eziluncedo kwii-capsules ze-HPMC zezokuba zoyisa i-cross-linking effect ye-gelatin capsules, zihambelana kakuhle neziyobisi, zinozinzo oluphezulu, ziyakwazi ukulungelelanisa nokulawula ukukhutshwa kweziyobisi, ziphucule umgangatho weziyobisi, zineenzuzo zokukhululwa kweziyobisi ezizinzileyo. inkqubo. Ngokusebenzayo, ii-capsules ze-HPMC zinokutshintsha ngokupheleleyo ii-capsules ze-gelatin ezikhoyo, ezimele uphuhliso lwexesha elizayo lwee-capsules ezinzima.
4.5 Ukusetyenziswa kwe-HPMC njenge-arhente exhomayo
I-HPMC isetyenziswa njenge-arhente yokunqumamisa, kwaye isiphumo sayo sokuxhoma silungile. Kwaye imifuniselo ibonisa ukuba ukusebenzisa ezinye izinto eziqhelekileyo zepolymer njenge-arhente yokuxhoma ukulungiselela ukunqunyanyiswa okomileyo kuthelekiswa ne-HPMC njenge-arhente yokuxhoma ukulungiselela ukumiswa okomileyo. Ukumiswa okomileyo kulula ukuyilungisa kwaye kunozinzo oluhle, kwaye ukumiswa okubunjiweyo kuhlangabezana neemfuno zeempawu ezahlukeneyo zomgangatho wokumisa okomileyo. Ngoko ke, i-HPMC isoloko isetyenziswa njenge-arhente yokuxhoma kumalungiselelo e-ophthalmic.
4.6 Ukusetyenziswa kwe-HPMC njenge-blocker, i-arhente yokukhulula ngokukhawuleza kunye ne-porogen
I-HPMC ingasetyenziswa njenge-ejenti evalelayo, i-arhente yokukhululwa ezinzileyo kunye ne-ejenti eyenza i-pore ukulibaziseka nokulawula ukukhutshwa kweziyobisi. Kule mihla, i-HPMC ikwasetyenziswa ngokubanzi kumalungiselelo akhutshiweyo azinzileyo kunye namalungiselelo adibeneyo amayeza emveli aseTshayina, anje ngeTianshan Snow Lotus ekhutshwa ngokuzinzileyo iipilisi zematrix. Isicelo, isiphumo saso sokukhululwa esizinzileyo silungile, kwaye inkqubo yokulungiselela ilula kwaye izinzile.
4.7 Ukusetyenziswa kwe-HPMC njengeglue etyebileyo kunye ne-colloid ekhuselayo
I-HPMC ingasetyenziswa njenge-thickener [9] ukwenza ii-colloids ezikhuselayo, kunye nezifundo zovavanyo ezifanelekileyo zibonise ukuba ukusebenzisa i-HPMC njenge-thickener kunokuphucula uzinzo lwekhabhoni esebenzayo yamayeza. Ngokomzekelo, isetyenziswa ngokuqhelekileyo ekulungiseleleni i-pH-sensitive levofloxacin hydrochloride ijeli ye-ophthalmic ekulungele ukusetyenziswa. I-HPMC isetyenziswa njenge-thickener.
4.8 Ukusetyenziswa kwe-HPMC njenge-bioadhesive
I-adhesives esetyenziselwa iteknoloji ye-bioadhesion yi-macromolecular compounds kunye neempawu ze-bioadhesive. Ngokubambelela kwi-gastrointestinal mucosa, i-mucosa yomlomo kunye nezinye iindawo, ukuqhubeka kunye nokuqina koqhagamshelwano phakathi kweziyobisi kunye ne-mucosa kuqiniswa ukufezekisa iziphumo ezingcono zonyango. . Inani elikhulu lemizekelo yesicelo libonisa ukuba i-HPMC inokuhlangabezana kakuhle nezi mfuno zingasentla njenge-bioadhesive.
Ukongeza, i-HPMC inokusetyenziswa njenge-precipitation inhibitor ye-topical gels kunye ne-self-microemulsifying systems, kwaye kwishishini le-PVC, i-HPMC ingasetyenziswa njengesikhuseli sokusasazeka kwi-polymerization ye-VCM.
5 Isiphelo
Ngelizwi, i-HPMC isetyenziswe ngokubanzi kumalungiselelo amayeza kunye neminye imiba ngenxa yeempawu zayo ezizodwa ze-physicochemical kunye ne-biological. Nangona kunjalo, i-HPMC iseneengxaki ezininzi kumalungiselelo amayeza. Ithini indima ethile ye-HPMC kwisicelo; indlela yokufumanisa ukuba ingaba nefuthe le-pharmacological; ziziphi iimpawu enazo kwindlela yokukhululwa, njl. njl. Ingabonwa ukuba ngelixa i-HPMC isetyenziswa ngokubanzi, iingxaki ezininzi kufuneka zisonjululwe ngokukhawuleza. Kwaye ngakumbi nangakumbi abaphandi benza umsebenzi omninzi wosetyenziso olungcono lwe-HPMC kwezamayeza, ngaloo ndlela bekhuthaza ngokuqhubekayo uphuhliso lwe-HPMC kwicandelo labancedisi bamayeza.
Ixesha lokuposa: Nov-02-2022