Atiri: ihe mkpuchi; Ihe membrane; Ngwa polymer na-achịkwa ngwa ngwa maka nkwadebe nkwụsị ngwa ngwa; Onye na-eme ka ọ kwụsie ike; Enyemaka nkwusioru, nrapado mbadamba; Ihe nchikota adhesion siri ike.
1. Ntinye ngwaahịa
Ngwaahịa a bụ ETHER na-abụghị ionIC cellulose, nke a na-ahụ anya dị ka ntụ ntụ ọcha, enweghị isi na enweghị ụtọ, soluble na mmiri na ọtụtụ ihe ndị na-eme ihe na-edozi ahụ, ọzịza na mmiri oyi iji kpochapụ ma ọ bụ ntakịrị turBIdized colloidal solution. Ihe ngwọta mmiri nwere ọrụ elu, nghọta dị elu na arụmọrụ kwụsiri ike. HPMC nwere ihe onwunwe nke gel na-ekpo ọkụ. Mgbe kpochara, ngwaahịa aqueous ngwọta na-etolite gel mmiri ozuzo, wee gbazee mgbe jụrụ oyi. Okpomọkụ gel nke nkọwa dị iche iche dị iche. Solubility mgbanwe na viscosity, viscosity zhao ala, ukwuu na solubility, dị iche iche nkọwa nke HPMC Njirimara nwere ụfọdụ iche, HPMC etisasịwo na mmiri adịghị emetụta pH uru.
The spontaneous combustion okpomọkụ, rụrụ njupụta, ezi njupụta na iko mgbanwe okpomọkụ bụ 360 ℃, 0.341g / cm3, 1.326g / cm3 na 170 ~ 180 ℃, karị. Mgbe kpochara, ọ na-atụgharị agba aja aja na 190 ~ 200 Celsius C wee gbaa ọkụ na 225 ~ 230 Celsius.
HPMC fọrọ nke nta ka ọ ghara ịsacha na chloroform, ethanol (95%), na diethyl ether, wee gbazee na ngwakọta nke ethanol na methylene chloride, ngwakọta nke methanol na methylene chloride, na ngwakọta nke mmiri na ethanol. Ụfọdụ ọkwa HPMC na-agbaze na ngwakọta nke acetone, methylene chloride, na 2-propanol, yana na ihe mgbaze ndị ọzọ.
Tebụl 1: Ngosipụta teknụzụ
oru ngo
nlele,
60 gd (2910).
65GD (2906)
75GD (2208)
Methoxy%
28.0-32.0
27.0-30.0
19.0-24.0
Hydroxypropoxy%
7.0-12.0
4.0-7.5
4.0-12.0
Gel okpomọkụ ℃
56-64.
62.0-68.0
70.0-90.0
Viscosity mpa s.
3,5,6,15,50,4000
50400 0
100400 0150 00100 000
Mbelata arọ akọrọ%
5.0 ma ọ bụ obere
Ihe fọdụrụ na-ere ọkụ%
1.5 ma ọ bụ obere
pH
4.0-8.0
Igwe dị arọ
20 ma ọ bụ obere
arsenic
2.0 ma ọ bụ obere
2. Njirimara ngwaahịa
2.1 Hydroxypropyl methylcellulose na-agbaze na mmiri oyi iji mepụta ngwọta colloidal viscous. Ọ bụrụhaala na a na-agbakwunye ya na mmiri oyi ma kpalie ya ntakịrị, enwere ike ịgbaze ya n'ime ngwọta na-enweghị atụ. N'ụzọ megidere nke ahụ, ọ bụ ihu ọma insoluble na mmiri ọkụ n'elu 60 ℃ na ike zaa naanị. N'ime nkwadebe nke hydroxypropyl methicellulose aqueous solution, ọ kacha mma ịgbakwunye akụkụ nke hydroxypropyl methicellulose n'ime mmiri ụfọdụ, kpalie ike, kpoo ọkụ ruo 80 ~ 90 ℃, wee gbakwunye ihe fọdụrụ na hydroxypropyl methicellulose, n'ikpeazụkwa, jiri mmiri oyi gbakwunye. ruo ego achọrọ.
2.2 Hydroxypropyl methylcellulose bụ ihe na-abụghị ionic cellulose ether, ngwọta ya adịghị ebu ionic ụgwọ, adịghị emekọrịta na metal salts ma ọ bụ ionic organic ogige, nke mere na HPMC adịghị emeghachi omume na ndị ọzọ akụrụngwa na excipients na usoro nkwadebe. mmepụta.
2.3 Hydroxypropyl methylcellulose nwere mmetụta mgbochi siri ike, yana mmụba nke ogo nnọchi n'ụdị molekụla, a na-akwalitekwa mmetụta mgbochi ahụ. Ọgwụ ndị na-eji HPMC eme ihe dị ka ihe mgbakwunye nwere mma kwụsiri ike n'ime oge dị irè karịa ọgwụ na-eji ihe mgbakwunye ọdịnala ndị ọzọ (starch, dextrin, sugar powdered).
2.4 Hydroxypropyl methylcellulose bụ metabolically inert. Dị ka onye na-emepụta ọgwụ na-emepụta ọgwụ, ọ dịghị metabolized ma ọ bụ na-etinye uche ya, ya mere ọ naghị enye okpomọkụ na ọgwụ na nri. Ọ nwere ihe pụrụ iche maka uru calorific dị ala, enweghị nnu, ọgwụ na-adịghị ahụ maka ahụ na nri maka ndị ọrịa mamịrị.
2.5HPMC kwụsiri ike na acids na bases, mana ọ bụrụ na pH gafere 2 ~ 11 ma na-emetụta oke okpomọkụ ma ọ bụ ogologo oge nchekwa, ọ ga-ebelata ogo nke chara n'onwe.
2.6 Hydroxypropyl methylcellulose ngwọta nwere ike inye ọrụ elu, na-egosi oke elu na ụkpụrụ esemokwu interfacial. Ọ nwere emulsification dị irè na usoro nke abụọ ma nwee ike iji ya dị ka onye na-eme ka ọ dị mma na colloid nchebe.
2.7 Hydroxypropyl methylcellulose aqueous ngwọta nwere magburu onwe film-akpụ Njirimara, na bụ ezigbo mkpuchi ihe maka mbadamba nkume na ọgwụ. Akpụkpọ ahụ e ji mee ya enweghị agba ma sie ike. Ọ bụrụ na agbakwunyere glycerol, enwere ike ịbawanye ike ya. Mgbe ọgwụgwọ elu gasịrị, a na-agbasasị ngwaahịa ahụ na mmiri oyi, a pụkwara ịchịkwa ọnụego mgbasa site n'ịgbanwe gburugburu pH. A na-eji ya na nkwadebe ngwa ngwa na-emepụta ihe na ntinye ntinye.
3. Ngwa ngwaahịa
3.1. A na-eji ya dị ka ihe nrapado na nke na-agbasa
HPMC na-eji na-akwalite ọgwụ mgbasa na ogo ntọhapụ ngwa, nwere ike ozugbo etisasịwo na ihe mgbaze dị ka nrapado, ala viscosity nke HPMC etisasịwo na mmiri na-etolite transperent ka ọdụ́ nnyapade colloid ngwọta, mbadamba, ọgwụ, granules na nrapado na disintegrating. onye nnọchi anya, yana viscosity dị elu maka gluu, naanị iji ụdị dị iche iche na ihe dị iche iche chọrọ, izugbe bụ 2% ~ 5%.
HPMC aqueous ngwọta na a ụfọdụ ịta nke ethanol ime ihe mejupụtara ihe nkedo; Ọmụmaatụ: 2%HPMC mmiri mmiri agwakọta na 55% ethanol ngwọta e ji mee ihe maka pelleting nke amoxicillin capsules, nke mere na nkezi mgbasa nke amoxicillin capsules mụbara site na 38% ruo 90% na-enweghị HPMC.
HPMC nwere ike mere nke mejupụtara nrapado na dị iche iche ịta nke starch slurry mgbe mgbasa; Mgbasa nke mbadamba ụrọ erythromycin gbagoro site na 38.26% ruo 97.38% mgbe ejikọtara 2% HPMC na 8% starch.
2.2. Mee ihe mkpuchi ihe nkiri na ihe na-emepụta ihe nkiri
HPMC dị ka ihe mkpuchi mmiri na-agbaze mmiri nwere njirimara ndị a: viscosity ngwọta na-agafeghị oke; Usoro mkpuchi dị mfe; Ezigbo ihe na-emepụta ihe nkiri; Nwere ike idobe udi nke ibe, ide; Nwere ike ghara iru mmiri; Nwere ike agba, ụtọ mgbazi. A na-eji ngwaahịa a dị ka mkpuchi ihe nkiri na-edozi mmiri maka mbadamba nkume na ọgwụ ndị nwere obere viscosity, na maka ihe nkiri na-abụghị nke mmiri na-ekpuchi elu, ọnụ ọgụgụ ojiji bụ 2%-5%.
2.3, dị ka ihe na-eme ka ọ dị arọ na gluu nchebe colloidal
A na-eji HPMC eme ihe dị ka onye na-amụba ihe bụ 0.45% ~ 1.0%, enwere ike iji ya mee ihe dị ka anya mmiri na onye na-akwa akwa akwa; A na-eji ya mee ka nkwụsi ike nke gluu hydrophobic dịkwuo elu, na-egbochi ikuku coalescence, mmiri ozuzo, usoro ọgwụgwọ mbụ bụ 0.5% ~ 1.5%.
2.4, dị ka ihe mgbochi, ihe ntọhapụ ngwa ngwa, ihe ntọhapụ na-achịkwa na onye na-ahụ maka pore
A na-eji ụdị viscosity dị elu nke HPMC na-akwado ndị na-egbochi ndị na-egbochi ya na ndị ọrụ ntọhapụ a na-achịkwa nke mbadamba ihe ntọhapụ agwakọtara na ọkpụkpụ hydrophilic gel skeleton kwadoro ntọhapụ. Ụdị viscosity dị ala bụ ihe na-eme ka ọ bụrụ ihe na-eme ka ọ bụrụ ihe na-eme ka ọkpụkpụ na-adịgide adịgide ma ọ bụ nke a na-achịkwa ka e wee nweta ọgwụ ọgwụgwọ mbụ nke mbadamba nkume ndị dị otú ahụ ngwa ngwa, na-esote nkwụsị-ntọhapụ ma ọ bụ na-achịkwa-ntọhapụ iji nọgide na-enwe mmetụta dị irè n'ime ọbara.
2.5. Gel na suppository matrix
Enwere ike ịkwadebe suppositories hydrogel na nrapado gastric site na iji njirimara nke nhazi hydrogel nke HPMC na-ejikarị na mmiri.
2.6 Ihe nrapado ndu
Ejikọtara Metronidazole na HPMC na polycarboxylethylene 934 n'ime igwekota iji mee mbadamba ihe ntọhapụ nke bioadhesive nke nwere 250mg. Nnwale mgbasa nke in vitro gosiri na nkwadebe ahụ na-agba ọsọ ngwa ngwa na mmiri, a na-achịkwa ntọhapụ ọgwụ ahụ site na mgbasa ozi na ntụrụndụ carbon. Mmejuputa anụmanụ gosiri na usoro mwepụta ọgwụ ọhụrụ ahụ nwere ezigbo ihe nrapagide nke ndu na mucosa sublingual bovine.
2.7, dị ka enyemaka nkwusioru
HIGH viscosity nke ngwaahịa a bụ ezigbo nkwusioru enyemaka maka nkwusioru mmiri mmiri nkwadebe, ya na-emekarị usoro bụ 0.5% ~ 1.5%.
4. Ihe atụ ngwa
4.1 Ihe mkpuchi ihe nkiri: HPMC 2kg, talc 2kg, mmanụ castor 1000ml, Twain -80 1000ml, propylene glycol 1000ml, 95% ethanol 53000ml, mmiri 47000ml, pigmenti kwesịrị ekwesị ego. Enwere ụzọ abụọ iji mee ya.
4.1.1 Nkwadebe nke mmiri mmiri kpuchiri pigmenti soluble: Tinye ego nke HPMC edepụtara n'ime 95% ethanol, gbanye ya n'otu abalị, gbarie vector pigmenti ọzọ n'ime mmiri (nyochaa ma ọ bụrụ na ọ dị mkpa), jikọta ngwọta abụọ ahụ ma kpalie nke ọma iji mepụta ngwọta doro anya. . Gwakọta 80% nke ngwọta (20% maka polishing) na ego nke mmanụ castor, Tween-80, na propylene glycol.
4.1.2 Nkwadebe nke insoluble pigmenti (dị ka ígwè oxide) mkpuchi mmiri mmiri HPMC etinyere na 95% ethanol n'otu ntabi anya, na mmiri na-agbakwunyere na-eme ka 2% HPMC uzo ngwọta. A na-ewepụta 20% nke ngwọta a maka polishing, na ihe fọdụrụ 80% ngwọta na ígwè oxide kwadebere site na mmiri mmiri na-egweri usoro, na mgbe ahụ, ego ndenye nke ihe ndị ọzọ na-agbakwunyere na gwakọtara ọbụna maka ojiji. Usoro mkpuchi nke mmiri mmiri mkpuchi: wụsa mpempe ọka n'ime ite mkpuchi shuga, mgbe ntụgharị, ikuku na-ekpo ọkụ na-ekpo ọkụ ruo 45 ℃, ị nwere ike ịgbasa mkpuchi nri, njikwa na-eruba na 10 ~ 15ml / min, mgbe ịgbasachara, nọgide na-akpọnwụ. na ikuku na-ekpo ọkụ maka 5 ~ 10min nwere ike ịpụ na ite ahụ, tinye n'ime igwe nkụ ka ọ kpọọ nkụ maka ihe karịrị 8h.
A na-agbaze 4.2a-interferon anya akpụkpọ anụ 50μg nke α-interferon na 10ml0.01ml hydrochloric acid, jikọtara ya na 90ml ethanol na 0.5GHPMC, nchara, kpuchie na mkpanaka iko na-atụgharị, igba ogwu na 60 ℃ na akpọnwụwo na ikuku. A na-eme ngwaahịa a ka ọ bụrụ ihe nkiri.
4.3 Cotrimoxazole mbadamba (0.4g± 0.08g) SMZ (80 ntupu) 40kg, starch (120 ntupu) 8kg, 3% HPMC aqueous ngwọta 18-20kg, magnesium stearate 0.3kg, TMP (80 ntupu) 8kg. mix SMZ na TMP, wee tinye starch na mix maka 5min. Na prefabricated 3% HPMC aqueous ngwọta, nro ihe, na 16 mesh ihuenyo granulation, ihicha, na mgbe ahụ na 14 mesh ihuenyo dum ọka, tinye magnesium stearate mix, na 12mm gburugburu na okwu (SMZco) stamping mbadamba. A na-ejikarị ngwaahịa a dị ka ihe nkedo. Mgbasa nke mbadamba nkume ahụ bụ 96%/20min.
4.4 Piperate mbadamba (0.25g) piperate 80 ntupu 25kg, starch (120 ntupu) 2.1kg, magnesium stearate kwesịrị ekwesị ego. Usoro mmepụta ya bụ ịgwakọta pipeoperic acid, starch, HPMC n'otu n'otu, na 20% ethanol soft material, 16 mesh screen granulate, dry, and then 14 mesh screen whole grain, plus vector magnesium stearate, with 100mm belt word (PPA0.25) ) mbadamba stamping. Site na starch dị ka ihe na-agbasasị, ọnụego mgbasa nke mbadamba nkume a erughị 80%/2min, nke dị elu karịa ngwaahịa ndị yiri ya na Japan.
4.5 Artificial akwa HPMC-4000, HPMC-4500 ma ọ bụ HPMC-5000 0.3g, sodium chloride 0.45g, potassium chloride 0.37g, borax 0.19g, 10% ammonium chlorbenzylammonium ngwọta 0.02ml, mmiri tinye na 100ml. Ya mmepụta usoro bụ HPMC etinye na 15ml mmiri, na 80 ~ 90 ℃ zuru mmiri were a, tinye 35ml mmiri, na mgbe ahụ nwere ndị fọdụrụ components nke 40ml aqueous ngwọta gwakọtara evenly, tinye mmiri n'uju ego, wee gwakọta evenly, guzoro n'otu abalị. , jiri nwayọọ wunye filtration, iyo n'ime akpa akara, igba ogwu na 98 ~ 100 ℃ maka 30min, ya bụ, The pH sitere na 8.4 ° C ruo 8.6 Celsius C. A na-eji ngwaahịa a eme ihe maka erughị eru anya mmiri, bụ ihe dị mma dochie anya mmiri, mgbe a na-eji ya maka microscopy ụlọ dị n'ihu, enwere ike ịbawanye dose nke ngwaahịa a, 0.5% 0.5% .
4.6 Meththorphan na-achịkwa ntọhapụ mbadamba meththorphan resin nnu 187.5mg, lactose 40.0mg, PVP70.0mg, vapor silica 10mg, 40.0 mGHPMC-603, 40.0mg ~ microcrystalline cellulose phthalate-102.2 na magnesium. A na-akwado ya dị ka mbadamba nkume site na usoro nkịtị. A na-eji ngwaahịa a dị ka ihe ntọhapụ a na-achịkwa.
4.7 N'ihi na avantomycin ⅳ mbadamba nkume, 2149g avantomycin ⅳ monohydrate na 1000ml isopropyl mmiri ngwakọta nke 15% (oke mkpokọta) eudragitL-100 (9: 1) kpaliri, agwakọta, granulated, na akpọnwụwo na 35 ℃. A gwakọtara granules a mịrị amị 575g na 62.5g hydroxypropylocellulose E-50 nke ọma, wee tinye 7.5g stearic acid na 3.25g magnesium stearate na mbadamba nkume ahụ iji nweta ntọhapụ nke vanguard mycinⅳ mbadamba nkume na-aga n'ihu. A na-eji ngwaahịa a dị ka ihe ntọhapụ nwayọ.
4.8 Nifedipine kwadoro-release granules 1 akụkụ nifedipine, 3 akụkụ hydroxypropyl methyl cellulose na 3 akụkụ ethyl cellulose na ngwakọta agwakọta (ethanol: methylene chloride = 1: 1), na 8 akụkụ ọka starch na-agbakwunyere na-emepụta granules site ọkara-soluble. usoro. Mgbanwe nke pH gburugburu ebe obibi emetụtaghị ọnụego mwepụta ọgwụ ọjọọ nke granules ma jiri nwayọọ karịa nke granules dị na ahịa. Mgbe awa 12 nke nchịkwa ọnụ gasịrị, ntinye ọbara mmadụ bụ 12mg / ml, ọ dịghịkwa ọdịiche dị n'otu n'otu.
4.9 Propranhaol hydrochloride kwadoro ntọhapụ capsule Propranhaol hydrochloride 60kg, microcrystalline cellulose 40kg, na-agbakwunye mmiri 50L iji mee granules. A na-agwakọta HPMC1kg na EC 9kg n'ime ihe mgbaze agwakọta (methylene chloride: methanol = 1: 1) 200L iji mee ka ngwọta mkpuchi, na-agba ọsọ nke 750ml / min na ihe ndị na-agbagharị agbagharị, ihe ndị a na-ekpuchi anya site na pore size nke 1.4. mm na-ekpuchi ihe niile, wee jupụta n'ime capsule nkume nke nwere igwe na-ejuputa capsule nkịtị. Capsule ọ bụla nwere 160mg nke propranolol hydrochloride spherical particles.
4.10 Naprolol HCL skeleton mbadamba nkume kwadoro site na ịgwakọta naprolol HCL: HPMC: CMC-NA na nha nke 1: 0.25: 2.25. Ọnụego mwepụta ọgwụ dị nso n'usoro efu n'ime awa 12.
A pụkwara iji ihe ọkpụkpụ agwakọta ọgwụ ndị ọzọ, dị ka metoprolol: HPMC: CMC-NA dịka: 1:1.25:1.25; Allylprolol:HPMC dabere na nha 1:2.8:2.92. Ọnụego mwepụta ọgwụ dị nso n'usoro efu n'ime awa 12.
4.11 Mbadamba ụrọ skeleton nke ihe agwakọta nke ethylaminosine sitere na usoro nkịtị na-eji ngwakọta nke micro powder silica gel: CMC-NA: HPMC 1: 0.7: 4.4. Enwere ike ịhapụ ọgwụ ahụ maka awa 12 ma in vitro na in vivo, na usoro ntọhapụ linear nwere njikọ dị mma. Nsonaazụ nke nnwale nkwụsi ike accelerated dị ka iwu FDA siri kwuo amụma na ndụ nchekwa ngwaahịa a ruru afọ 2.
4.12 HPMC (50mPa·s) (akụkụ 5), HPMC (4000 mPa·s) (akụkụ 3) na HPC1 gbazere na akụkụ 1000 mmiri, 60 akụkụ acetaminophen na 6 akụkụ silica gel agbakwunyere, kpalitere ya na homogenizer, na fesa akpọnwụwo. Ngwaahịa a nwere 80% nke ọgwụ isi.
4.13 Theophylline hydrophilic gel skeleton mbadamba gbakọrọ dị ka ngụkọta mbadamba arọ, 18% -35% theophylline, 7.5% -22.5% HPMC, 0.5% lactose, na ihe kwesịrị ekwesị ego nke hydrophobic lubricant na-ejikarị kwadebere n'ime mbadamba ntọhapụ na-achịkwa, nke nwere ike. nọgide na-enwe mmetụta ọbara dị irè nke ahụ mmadụ maka awa 12 mgbe nchịkwa ọnụ gasịrị.
Oge nzipu: Feb-05-2024