Nkeji: ihe mkpuchi; Ihe mkpuchi akpụkpọ ahụ; Ihe polymer a na-achịkwa ọsọ ọsọ maka nkwadebe mwepụ nwayọ; Ihe na-eme ka ọ kwụsie ike; Ihe enyemaka nkwụsịtụ, ihe na-arapara mbadamba; Ihe na-arapara agbakwunyere.
1. Okwu mmeghe ngwaahịa
NGWAAHỊA a BỤ ETHER CELLULOSE NA-EMEGHỊ IONIC, a na-ahụ ya n'èzí dị ka ntụ ntụ ọcha, enweghị isi na uto, a na-agbaze na mmiri na ọtụtụ ihe mgbaze organic polar, na-aza n'ime mmiri oyi iji mee ka ọ dị ọcha ma ọ bụ dị ntakịrị turBIdized colloidal solution. Mmiri mmiri ahụ nwere ọrụ elu, nghọta dị elu na arụmọrụ kwụsiri ike. HPMC nwere ihe onwunwe nke jel ọkụ. Mgbe ọ kpochara ọkụ, mmiri mmiri ngwaahịa ahụ na-emepụta mmiri ozuzo jel, wee gbazee mgbe ọ jụrụ oyi. Okpomọkụ jel nke nkọwapụta dị iche iche dị iche. Mmiri mmiri na-agbanwe site na viscosity, viscosity zhao dị ala, mmiri mmiri ka ukwuu, nkọwapụta dị iche iche nke ihe onwunwe HPMC nwere ụfọdụ ọdịiche, uru pH anaghị emetụta HPMC.
Okpomọkụ ọkụ na-apụtaghị ìhè, njupụta dị nro, njupụta ezigbo na okpomọkụ mgbanwe iko bụ 360℃, 0.341g/cm3, 1.326g/cm3 na 170 ~ 180℃, n'otu n'otu. Mgbe ọ kpochara ọkụ, ọ na-acha aja aja na 190 ~ 200°C ma na-agba ọkụ na 225 ~ 230°C.
HPMC fọrọ nke nta ka ọ ghara ịgbaze na chloroform, ethanol (95%), na diethyl ether, ma gbazee na ngwakọta ethanol na methylene chloride, ngwakọta methanol na methylene chloride, na ngwakọta mmiri na ethanol. Ụfọdụ ọkwa nke HPMC na-agbaze na ngwakọta nke acetone, methylene chloride, na 2-propanol, yana na ihe mgbaze organic ndị ọzọ.
Tebụl 1: Ihe ngosi teknụzụ
ọrụ
Ihe nlele,
60 gd (2910).
65GD(2906)
75GD(2208)
Usoro pasentị
28.0-32.0
27.0-30.0
19.0-24.0
% nke Hydroxypropoxy
7.0-12.0
4.0-7.5
4.0-12.0
Okpomọkụ jel ℃
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 ibu akọrọ%
5.0 ma ọ bụ ihe na-erughị
Ihe fọdụrụ n'ọkụ%
1.5 ma ọ bụ ihe na-erughị
pH
4.0-8.0
Ígwè dị arọ
20 ma ọ bụ ihe na-erughị
arsenik
2.0 ma ọ bụ ihe na-erughị
2. Atụmatụ ngwaahịa
2.1 A na-agbaze Hydroxypropyl methylcellulose n'ime mmiri oyi iji mepụta mmiri colloidal viscous. Ọ bụrụhaala na etinyere ya na mmiri oyi ma kpalite ntakịrị, enwere ike ịgbaze ya ka ọ bụrụ mmiri doro anya. N'ụzọ megidere nke ahụ, ọ naghị agbaze na mmiri ọkụ karịa 60℃ ma ọ nwere ike ịgbaze naanị. N'ịkwadebe mmiri hydroxypropyl methicellulose, ọ kacha mma itinye akụkụ nke hydroxypropyl methicellulose n'ime mmiri ụfọdụ, gwakọta nke ọma, kpoo ya ọkụ ruo 80 ~ 90℃, wee tinye hydroxypropyl methicellulose fọdụrụ, wee mechaa jiri mmiri oyi mee ihe iji tinye ya na oke achọrọ.
2.2 Hydroxypropyl methylcellulose bụ cellulose ether nke na-abụghị ionic, ihe ngwọta ya anaghị ebu ibu ionic, ọ naghị ejikọta ya na nnu ígwè ma ọ bụ ihe ndị dị ndụ ionic, iji hụ na HPMC anaghị emeghachi omume na ihe ndị ọzọ e ji emepụta ihe na ihe ndị ọzọ na-enyere aka n'oge mmepụta nkwadebe.
2.3 Hydroxypropyl methylcellulose nwere ike igbochi mmetụta uche siri ike, yana mmụba nke ọkwa nnọchi anya na nhazi molekul, a na-emekwa ka mmetụta uche dịkwuo mma. Ọgwụ ndị na-eji HPMC dị ka ihe mgbakwunye na-enwe àgwà kwụsiri ike n'ime oge dị irè karịa ọgwụ ndị na-eji ihe mgbakwunye ọdịnala ndị ọzọ (starch, dextrin, shuga ntụ ntụ).
2.4 Hydroxypropyl methylcellulose anaghị arụ ọrụ nke ọma n'ụzọ metabolic. Dịka ihe na-enye ọgwụ, ọ naghị arụ ọrụ nke ọma ma ọ bụ na-amịkọrọ ya, yabụ ọ naghị enye okpomọkụ na ọgwụ na nri. O nwere ike itinye ya n'ọrụ pụrụ iche maka obere kalori, enweghị nnu, ọgwụ ndị na-anaghị akpata ahụ erughị ala na nri maka ndị ọrịa shuga.
2.5HPMC anaghị eguzogide asịd na ntọala, mana ọ bụrụ na pH ahụ gafere 2 ~ 11 ma okpomọkụ dị elu ma ọ bụ oge nchekwa dị ogologo emetụta ya, ọ ga-ebelata oke ntozu okè.
2.6 Mmiri Hydroxypropyl methylcellulose nwere ike ime ka elu rụọ ọrụ nke ọma, na-egosi oke nrụgide dị n'elu na nke dị n'etiti ihu. Ọ nwere emulsification dị irè na sistemụ nkebi abụọ ma enwere ike iji ya dị ka ihe na-eme ka ọ kwụsie ike ma na-echebe ya.
2.7 Mmiri Hydroxypropyl methylcellulose nwere ezigbo ihe mkpuchi maka mbadamba na mkpụrụ ọgwụ. Akpụkpọ ahụ nke ọ mepụtara enweghị agba ma sie ike. Ọ bụrụ na etinyere glycerol, enwere ike ịbawanye ike ya. Mgbe a gwọchara ya n'elu, a na-agbasa ngwaahịa ahụ na mmiri oyi, a pụkwara ijikwa ọnụego mgbaze site na ịgbanwe gburugburu pH. A na-eji ya na nkwadebe ndị na-ewepụta nwayọ nwayọ na nkwadebe ndị a kpuchiri enteric.
3. Ngwa ngwaahịa
3.1. Ejiri ya mee ihe dịka ihe na-arapara ma na-agbaze agbaze
A na-eji HPMC akwalite mgbasa ọgwụ na ọkwa nke ngwa ntọhapụ, enwere ike ịgbaze ozugbo na ihe mgbaze dị ka ihe na-arapara, obere viscosity nke HPMC agbazere na mmiri iji mepụta ngwọta colloid nke ọdụdụ, mbadamba, mkpụrụ ọgwụ, granules na ihe na-agbaze na ihe na-agbaze, yana nnukwu viscosity maka gluu, ejiri naanị n'ihi ụdị dị iche iche na ihe dị iche iche achọrọ, izugbe bụ 2% ~ 5%.
Mmiri HPMC na oke ethanol iji mee ihe njikọta; Ọmụmaatụ: E jiri mmiri HPMC 2% gwakọtara ya na mmiri ethanol 55% mee ka mkpụrụ ọgwụ amoxicillin dị nro, nke mere na nkezi mmiri nke mkpụrụ ọgwụ amoxicillin gbasaa site na 38% ruo 90% na-enweghị HPMC.
Enwere ike iji ihe nrapado mejupụtara HPMC mee ya na njupụta dị iche iche nke starch slurry mgbe agbazechara ya; Mgbaze nke mbadamba erythromycin nke a kpụchara n'ime enteric mụbara site na 38.26% ruo 97.38% mgbe ejikọtara 2% HPMC na 8% starch.
2.2. Mee ihe mkpuchi fim na ihe e ji akpụ ihe nkiri
HPMC dị ka ihe mkpuchi mmiri na-agbaze agbaze nwere njirimara ndị a: oke mmiri ngwọta; Usoro mkpuchi ahụ dị mfe; Ezigbo ihe okike nke imepụta ihe nkiri; Nwere ike idobe ọdịdị nke ihe ahụ, ide ihe; Ọ nwere ike iguzogide mmiri; Nwere ike agba agba, na ụtọ ndozi. A na-eji ngwaahịa a dị ka mkpuchi ihe nkiri mmiri na-agbaze agbaze maka mbadamba na mkpụrụ ọgwụ nwere obere viscosity, na maka mkpuchi ihe nkiri na-abụghị mmiri nwere nnukwu viscosity, ego ojiji ya bụ 2%-5%.
2.3, dị ka ihe na-eme ka ihe sie ike na gluu nchedo colloidal
A na-eji HPMC dị ka ihe na-eme ka ihe sie ike bụ 0.45% ~ 1.0%, enwere ike iji ya dị ka mmiri anya na ihe na-eme ka mmiri dị nkọ; A na-eji ya eme ka gluu hydrophobic dịkwuo mma, gbochie njikọ ihe, mmiri ozuzo, usoro a na-ejikarị eme ihe bụ 0.5% ~ 1.5%.
2.4, dịka ihe mgbochi, ihe mwepụta nwayọ nwayọ, ihe mwepụta a na-achịkwa na ihe nnọchi oghere
A na-eji ụdị HPMC dị elu viscosity eme ihe iji kwadebe ihe mgbochi na ihe ndị na-ewepụta ihe ndị a na-achịkwa nke mbadamba ihe ndị a na-agbakọta na mbadamba ihe ndị a na-agbakọta na gel hydrophilic. Ụdị obere viscosity bụ ihe na-akpali oghere maka mbadamba ihe ndị a na-agbapụta ma ọ bụ ndị a na-achịkwa ka e wee nweta ọgwụ mbụ nke mbadamba ndị dị otú ahụ ngwa ngwa, wee soro ya na mwepụta na-adịgide adịgide ma ọ bụ ntọhapụ a na-achịkwa iji nọgide na-enwe oke dị irè n'ọbara.
2.5. Gel na suppository matrix
Enwere ike ịkwadebe ihe ndị na-eme ka mmiri dị n'ime mmiri na ihe ndị na-eme ka afọ dị n'ime ya site n'iji njirimara nke mmepụta hydrogel nke HPMC na-ejikarị eme ihe.
2.6 Ihe ndị na-arapara ihe ndị dị ndụ
E tinyere Metronidazole na HPMC na polycarboxyethylene 934 n'ime igwekota iji mepụta mbadamba ihe eji emegharị ihe nke nwere 250mg. Nnwale ịgbaze n'ime vitro gosiri na nkwadebe ahụ gbasaara ngwa ngwa na mmiri, a na-ejikwa mgbasa na nkwụsịtụ nke carbon chain achịkwa mwepụta ọgwụ ahụ. Mmejuputa anụmanụ gosiri na usoro mwepụta ọgwụ ọhụrụ ahụ nwere nnukwu ihe ndị dị ndụ na mucosa sublingual ehi.
2.7, dị ka ihe enyemaka nkwụsịtụ
Oke viscosity nke ngwaahịa a bụ ezigbo ihe enyemaka nkwụsịtụ maka nkwadebe mmiri nkwụsịtụ, usoro ọgwụgwọ ya bụ 0.5% ~ 1.5%.
4. Ihe atụ nke ngwa
4.1 Ngwọta mkpuchi ihe nkiri: HPMC 2kg, talc 2kg, mmanụ castor 1000ml, Twain -80 1000ml, propylene glycol 1000ml, 95% ethanol 53000ml, mmiri 47000ml, agba kwesịrị ekwesị. E nwere ụzọ abụọ isi mee ya.
4.1.1 Nkwadebe nke mmiri mmiri ákwà e ji agba ...
4.1.2 Nkwadebe nke agba anaghị agbaze agbaze (dịka ígwè oxide) mmiri mkpuchi HPMC gbanyere n'ime ethanol 95% n'abalị, tinyekwa mmiri iji mee ka ọ bụrụ 2% HPMC ngwọta doro anya. E wepụtara 20% nke mmiri a maka ịchacha, e jikwa usoro egweri mmiri kwadebe ihe fọdụrụ 80% mmiri na oxide ígwè, wee tinye ọnụọgụ ọgwụ ndị ọzọ e nyere ma gwakọta ha nke ọma maka ojiji. Usoro mkpuchi nke mmiri mkpuchi: wụsa mpempe ọka n'ime ite mkpuchi shuga, mgbe ọ tụgharịrị, ikuku ọkụ na-ekpo ọkụ ruo 45℃, ị nwere ike fesa mkpuchi nri, njikwa mmiri n'ime 10 ~ 15ml/min, mgbe ị fesasịrị ya, nọgide na-akpọ nkụ na ikuku ọkụ maka nkeji 5 ~ 10, enwere ike ịpụ na ite ahụ, tinye ya na igwe nkụ ka ọ kpọọ nkụ ruo ihe karịrị awa 8.
A gbazere akpụkpọ anya 4.2α-interferon 50μg nke α-interferon na 10ml0.01ml hydrochloric acid, gwakọta ya na ethanol 90ml na 0.5GHPMC, a sachara ya, kpuchie ya na mkpanaka iko na-agbagharị agbagharị, gbazee ya na okpomọkụ 60℃ ma kpọọ nkụ n'ikuku. A na-emepụta ngwaahịa a ka ọ bụrụ ihe nkiri.
Mbadamba Cotrimoxazole 4.3 (0.4g±0.08g) SMZ (ntụpọ 80) 40kg, starch (ntụpọ 120) 8kg, 3% HPMC mmiri mmiri 18-20kg, magnesium stearate 0.3kg, TMP (ntụpọ 80) 8kg, ụzọ nkwadebe bụ ịgwakọta SMZ na TMP, wee tinye starch ma gwakọta ya maka nkeji 5. Site na mmiri mmiri 3% HPMC nke e mere tupu oge eruo, ihe dị nro, yana ihe mkpuchi 16 mesh, kpọọ nkụ, wee jiri ihe mkpuchi 14 mesh screen dum grain, tinye ngwakọta magnesium stearate, yana gburugburu 12mm yana mbadamba stamping word (SMZco). A na-ejikarị ngwaahịa a eme ihe dị ka ihe na-ejikọ ọnụ. Mgbaze nke mbadamba ahụ bụ 96%/20min.
Mbadamba Piperate 4.4 (0.25g) piperate 80 mesh 25kg, starch (120 mesh) 2.1kg, magnesium stearate nke kwesịrị ekwesị. Ụzọ mmepụta ya bụ ịgwakọta pipeoperic acid, starch, HPMC n'otu aka ahụ, na ihe dị nro ethanol 20%, granulate 16 mesh, kpọrọ nkụ, wee jiri mpempe 14 mesh screen wrench screen, tinyere vector magnesium stearate, na mbadamba 100mm gburugburu belt word (PPA0.25). Site na starch dị ka ihe na-agbawa agbawa, ọnụego mgbaze nke mbadamba a abụghị ihe na-erughị 80%/2 nkeji, nke dị elu karịa ngwaahịa ndị yiri ya na Japan.
4.5 Adọka e ji aka mee 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 solution 0.02ml, a na-etinye mmiri na 100ml. Usoro mmepụta ya bụ itinye HPMC na mmiri 15ml, na mmiri 80 ~ 90℃ zuru oke, were, tinye mmiri 35ml, wee nwee ihe ndị fọdụrụ na mmiri 40ml agwakọtara nke ọma, tinye mmiri ruo na oke zuru oke, wee gwakọta ya nke ọma, guzoro n'otu abalị, wụsa nzacha ahụ nwayọ, tinye ya n'ime akpa ahụ e mechiri emechi, gbazee ya na okpomọkụ 98 ~ 100℃ maka nkeji 30, ya bụ, pH sitere na 8.4 ° C ruo 8.6 ° C. A NA-EJI NGWA AHỊA A MEE KA Ọ DỊ MFE ỊDỌCHI, Ọ BỤ NTỤKWASỊ AKA, Ọ BỤ MGBE E JIRI YA MEE KA Ọ DỊ MFE ỊDỌCHI, Ọ BỤ MGBE E JIRI YA MEE KA Ọ DỊ MFE ỊDỌCHI, Ọ BỤ MGBE E JIRI YA MEE KA Ọ DỊ MFE ỊDỌCHI. Ọ BỤRỤ NA E JIRI YA MEE KA Ọ DỊ MFE ỊDỌCHI, E NWERE IKE ỊBỤ NTỤKWASỊ AKA. ỌNỤỌGỤGỤ NGWA AHỊA A, 0.7% ~ 1.5% kwesịrị ekwesị.
4.6 Mbadamba ihe eji emegharị Meththorphan nke nwere nnu resin meththorphan 187.5mg, lactose 40.0mg, PVP70.0mg, vapor silica 10mg, 40.0 mGHPMC-603, 40.0mg ~ microcrystalline cellulose phthalate-102 na magnesium stearate 2.5mg. A na-akwadebe ya dị ka mbadamba dịka usoro nkịtị si dị. A na-eji ngwaahịa a dị ka ihe eji emegharị achịkwa.
4.7 Maka mbadamba avantomycin ⅳ, a na-agwakọta 2149g avantomycin ⅳ monohydrate na ngwakọta mmiri isopropyl 1000ml nke 15% (njupụta oke) eudragitL-100 (9:1) ma kpọọ nkụ na okpomọkụ 35℃. A na-agwakọta granules kpọrọ nkụ 575g na 62.5g hydroxypropyloculose E-50 nke ọma, e mesịa tinye 7.5g stearic acid na 3.25g magnesium stearate na mbadamba ndị ahụ iji nweta ntọhapụ na-aga n'ihu nke mbadamba vanguard mycin ⅳ. A na-eji ngwaahịa a dị ka ihe na-ewepụta nwayọ nwayọ.
4.8 A gwakọtara mkpụrụ Nifedipine na-adịgide adịgide, otu akụkụ nifedipine, akụkụ atọ hydroxypropyl methyl cellulose na akụkụ atọ ethyl cellulose na ihe mgbaze agwakọtara (ethanol: methylene chloride = 1:1), a gbakwụnyekwara akụkụ asatọ nke starch ọka iji mepụta mkpụrụ granules site na usoro mmiri na-agbaze ọkara. Mgbanwe nke pH gburugburu ebe obibi emetụtaghị ọnụego mwepụta ọgwụ nke mkpụrụ granules ahụ ma dị nwayọ karịa nke mkpụrụ granules dị n'ahịa. Mgbe awa iri na abụọ nke ịṅụ ọgwụ ọnụ gasịrị, ọnụọgụ ọbara mmadụ bụ 12mg/ml, ọ dịghịkwa ọdịiche dị n'etiti onwe ya.
4.9 Propranhaol hydrochloride nwere ike iwepụ ihe mkpofu Propranhaol hydrochloride 60kg, microcrystalline cellulose 40kg, na-agbakwunye mmiri 50L iji mepụta granules. E tinyere HPMC1kg na EC 9kg n'ime ihe mgbaze agwakọtara (methylene chloride: methanol = 1:1) 200L iji mepụta ihe ngwọta mkpuchi ahụ, na-agba ọsọ nke 750ml/min na ihe mkpuchi gburugburu na-atụgharị, na-ekpuchi ihe mkpofu site na nha oghere nke ihe mkpuchi dum nke 1.4mm, wee tinye ya na kapsụl nkume ahụ na igwe ihe eji emeju kapsụl nkịtị. Kapsụl ọ bụla nwere 160mg nke ihe mkpuchi gburugburu propranolol hydrochloride.
E ji ngwakọta naprolol HCL :HPMC: CMC-NA mee mbadamba ọkpụkpụ 4.10. Ọnụọgụ ọgwụ ahụ fọrọ nke nta ka ọ bụrụ ihe efu n'ime awa iri na abụọ.
Enwere ike iji ihe ndị e ji ọkpụkpụ gwakọta mee ọgwụ ndị ọzọ, dịka metoprolol: HPMC: CMC-NA dịka: 1:1.25:1.25; Allylprolol:HPMC dịka nha 1:2.8:2.92 si dị. Ọnụego mwepụta ọgwụ ahụ fọrọ nke nta ka ọ bụrụ enweghị iwu n'ime awa iri na abụọ.
4.11 E ji usoro nkịtị kwadebe mbadamba ọkpụkpụ nke ihe ndị e ji ethylaminosine mee ihe: CMC-NA :HPMC 1:0.7:4.4. A pụrụ ịhapụ ọgwụ ahụ ruo awa iri na abụọ ma n'ime vitro ma n'ime vivo, usoro ntọhapụ ahịrị ahụ nwekwara ezigbo njikọ. Nsonaazụ nke nnwale nkwụsi ike ngwa ngwa dịka iwu FDA si dị na-egosi na ndụ nchekwa nke ngwaahịa a ruru afọ abụọ.
4.12 A gbazere HPMC (50mPa·s) (akụkụ ise), HPMC (4000 mPa·s) (akụkụ atọ) na HPC1 n'ime akụkụ mmiri 1000, tinye akụkụ 60 nke acetaminophen na akụkụ 6 nke silica gel, gwakọta ya na ihe na-eme ka ọ dị nro, ma fesa ya. Ngwaahịa a nwere 80% nke ọgwụ bụ isi.
4.13 A gbakọrọ mbadamba ọkpụkpụ Theophylline hydrophilic dịka mkpokọta ibu mbadamba si dị, a na-akwadebekarị 18%-35% theophylline, 7.5%-22.5% HPMC, 0.5% lactose, na oke mmanụ hydrophobic kwesịrị ekwesị n'ime mbadamba ntọhapụ a na-achịkwa, nke nwere ike ịnọgide na-enwe mmụba ọbara dị irè n'ahụ mmadụ ruo awa 12 mgbe ejiri ọnụ ṅụọ ya.
Oge ozi: Feb-05-2024