A na-enyocha akwụkwọ ndị metụtara ya n'ụlọ na ná mba ọzọ na nkwadebe nke ọgwụ excipients hydroxypropyl methylcellulose (HPMC) n'afọ ndị na-adịbeghị anya, nyochaa ma chịkọta ya, na ngwa ya na nkwadebe siri ike, nkwadebe mmiri mmiri, nkwadebe ntọhapụ na-achịkwa, nkwadebe capsule, gelatin kacha ọhụrụ. ngwa na ngalaba nke ọhụrụ usoro dị ka adhesive formulations na bioadhesives. N'ihi ihe dị iche na ikwu molekụla arọ na viscosity nke HPMC, o nwere àgwà na ojiji nke emulsification, adhesion, ndim, viscosity na-abawanye, suspending, gelling na film-akpụ. A na-eji ya eme ihe n'ọtụtụ ebe na nkwadebe ọgwụ na ọ ga-ekere òkè dị ukwuu na mpaghara nkwadebe. Na omimi ọmụmụ nke ya Njirimara na mma nke formulations technology, HPMC ga-ọzọ n'ọtụtụ ebe na nnyocha nke ọhụrụ onunu ogwu ụdị na ọhụrụ ọgwụ nnyefe usoro, si otú na-akwalite na-aga n'ihu mmepe nke formulations.
hydroxypropyl methylcellulose; nkwadebe ọgwụ; ọgwụ excipients.
Ọgwụ excipients abụghị nanị ihe ndabere ihe ndabere maka guzobe nke raw ọgwụ nkwadebe, kamakwa metụtara ihe isi ike nke usoro nkwadebe, ọgwụ àgwà, nkwụsi ike, nchekwa, ọgwụ ntọhapụ ọnụego, mode nke edinam, clinical nrụpụta, na mmepe nke ọhụrụ. ụdị onunu ogwu na ụzọ nchịkwa ọhụrụ. njikọ chiri anya. Mwepụta nke ihe mgbakwunye ọgwụ ọhụrụ na-akwalitekarị nkwalite ogo nkwadebe na mmepe nke ụdị usoro onunu ogwu ọhụrụ. Hydroxypropyl methylcellulose (HPMC) bụ otu n'ime ngwa ahịa ọgwụ kachasị ewu ewu n'ụlọ na ná mba ọzọ. N'ihi ịdị arọ molekụla ya dị iche iche na viscosity ya, ọ nwere ọrụ nke emulsifying, njide, ịgbatị, ịgbatị, na-akwụsịtụ, na gluing. A na-eji atụmatụ na ojiji dị ka coagulation na imepụta ihe nkiri na teknụzụ ọgwụ. Edemede a na-enyochakarị ngwa hydroxypropyl methylcellulose (HPMC) na usoro n'ime afọ ndị na-adịbeghị anya.
1.Njirimara ndị bụ isi nke HPMC
Hydroxypropyl methyl cellulose (HPMC), usoro molekụla bụ C8H15O8- (C10 H18O6) n-C8H15O8, na ihe gbasara molecular mass bụ ihe dịka 86 000. Ngwaahịa a bụ ihe na-emepụta ihe, nke bụ akụkụ nke methyl na akụkụ nke polyhydroxypropyl ether. nke cellulose. Enwere ike ịmepụta ya n'ụzọ abụọ: Otu bụ na a na-emeso methyl cellulose nke ọkwa kwesịrị ekwesị na NaOH wee meghachi omume na propylene oxide n'okpuru nnukwu okpomọkụ na nrụgide dị elu. Oge mmeghachi omume ga-adịru ogologo oge iji kwe ka methyl na hydroxypropyl mepụta njikọ ether Ọ jikọtara ya na mgbanaka anhydroglucose nke cellulose n'ụdị cellulose, ma nwee ike iru ogo achọrọ; nke ọzọ bụ iji caustic soda na-agwọ linter owu ma ọ bụ osisi pulp fiber, wee jiri methane chlorinated na propylene oxide meghachi omume n'otu n'otu, wee nụchaa ya ọzọ. , gwepịara ya ka ọ bụrụ ezigbo ntụ ntụ ma ọ bụ granules.
Agba nke ngwaahịa a na-acha ọcha ka mmiri ara ehi na-acha ọcha, enweghị isi na enweghị ụtọ, na ụdị ya bụ granular ma ọ bụ fibrous ntụ ntụ dị mfe na-eru. Enwere ike igbari ngwaahịa a n'ime mmiri ka ọ bụrụ ihe ngwọta colloidal na-acha ọcha doro anya na nke nwere ụfọdụ viscosity. Ihe mgbagwoju anya nke sol-gel nwere ike ime n'ihi mgbanwe okpomọkụ nke ngwọta na ụfọdụ ntinye uche.
N'ihi ọdịiche dị na ọdịnaya nke ihe abụọ a na-anọchi anya na nhazi nke methoxy na hydroxypropyl, ụdị ngwaahịa dị iche iche apụtala. N'ihe dị iche iche akọwapụtara, ụdị ngwaahịa dị iche iche nwere njirimara akọwapụtara. Viscosity na thermal gelation okpomọkụ, ya mere nwere ihe dị iche iche nwere ike iji mee ihe dị iche iche. Pharmacopoeia nke mba dị iche iche nwere ụkpụrụ dị iche iche na ihe nnọchianya na ihe nlereanya: European Pharmacopoeia dabeere na ọkwa dị iche iche nke viscosities dị iche iche na ọkwa dị iche iche nke nnọchi nke ngwaahịa ndị a na-ere n'ahịa, gosipụtara site na akara ule gbakwunyere nọmba, na unit bụ "mPa s". ". Na US Pharmacopoeia, 4 digits na-agbakwunyere mgbe aha jeneriki na-egosi ọdịnaya na ụdị nke ọ bụla nnọchi nke hydroxypropyl methylcellulose, dị ka hydroxypropyl methylcellulose 2208. Nke mbụ abụọ digits na-anọchi anya ihe dị ka uru nke methoxy otu. Pasent, ọnụọgụ abụọ ikpeazụ na-anọchi anya pasentị hydroxypropyl dị nso.
Calocan's hydroxypropyl methylcellulose nwere usoro 3, ya bụ usoro E, usoro F na usoro K, usoro nke ọ bụla nwere ụdị dị iche iche ịhọrọ. A na-ejikarị usoro E mee ihe dị ka mkpuchi ihe nkiri, nke a na-eji maka mkpuchi mbadamba nkume, ihe mkpuchi mbadamba nkume mechiri emechi; E, F usoro na-eji dị ka viscosifiers na hapụ retarding agents maka ophthalmic preparations, suspending agents, thickeners for water preparations, tablets and Binders of granules; A na-ejikarị usoro K dị ka ihe mgbochi ntọhapụ na ihe hydrophilic gel matrix maka nkwadebe ntọhapụ ngwa ngwa na njikwa.
Ndị na-emepụta ụlọ na-agụnye Fuzhou No. 2 Chemical Factory, Huzhou Food and Chemical Co., Ltd., Sichuan Luzhou Pharmaceutical Ngwa Factory, Hubei Jinxian Chemical Factory No. 1, Feicheng Ruitai Fine Chemical Co., Ltd., Shandong Liaocheng Ahua ụlọ ahịa ọgwụ. ., Ltd., Xi'an Huian chemical osisi, wdg.
2.Uru nke HPMC
HPMC abụrụla otu n'ime ihe ndị a na-eji ọgwụ eme ihe n'ụlọ na mba ofesi, n'ihi na HPMC nwere uru ndị ọzọ na-enwetaghị.
2.1 Mmiri oyi solubility
Soluble na mmiri oyi n'okpuru 40 ℃ ma ọ bụ 70% ethanol, bụ isi insoluble na mmiri ọkụ n'elu 60 ℃, ma ike gel.
2.2 kemịkalụ inert
HPMC bụ ụdị ether cellulose na-abụghị ionic, ihe ngwọta ya enweghị ụgwọ ionic na ọ dịghị emekọrịta ihe na nnu metal ma ọ bụ ogige ionic organic, ya mere ihe ndị ọzọ na-eme ka ọ ghara imeghachi omume na ya n'oge mmepụta nke nkwadebe.
2.3 Nkwụsi ike
Ọ kwụsiri ike ma acid na alkali, enwere ike ịchekwa ya ogologo oge n'etiti pH 3 na 11 na-enweghị mgbanwe dị ukwuu na viscosity. The aqueous ngwọta nke HPMC nwere mgbochi mildew mmetụta na-ejigide ezi viscosity kwụsie ike n'oge ogologo oge nchekwa. Ihe mgbakwunye ọgwụ na-eji HPMC nwere nkwụsi ike ka mma karịa ndị na-eji ihe mgbakwunye ọdịnala (dị ka dextrin, starch, wdg).
2.4 Mmezi viscosity
Enwere ike ịgwakọta viscosity dị iche iche nke HPMC n'ụzọ dị iche iche, enwere ike gbanwee viscosity ya dịka otu iwu siri dị, ma nwee mmekọrịta dị mma na linear, yabụ enwere ike họrọ oke dị ka mkpa.
2.5 Metabolic inertness
HPMC anaghị etinye aka na ya ma ọ bụ metabolized n'ime ahụ, ọ naghị enye ọkụ, yabụ ọ bụ ihe mgbakwunye nkwadebe ọgwụ dị mma. 2.6 Nchekwa A na-ewerekarị na HPMC bụ ihe na-adịghị egbu egbu na nke na-adịghị akpasu iwe, ọnụọgụ egbu egbu maka ụmụ oke bụ 5 g·kg - 1, na ọnụọgụ egbu egbu maka oke bụ 5. 2 g · kg - 1 . Ọgwụ kwa ụbọchị adịghị emerụ ahụ mmadụ.
3.Ngwa nke HPMC na usoro
3.1 Dị ka ihe mkpuchi ihe nkiri na ihe na-emepụta ihe nkiri
Iji HPMC dị ka ihe mbadamba ihe mkpuchi ihe nkiri, mbadamba ihe mkpuchi ahụ enweghị uru doro anya n'ikpuchi uto na ọdịdị ma e jiri ya tụnyere mbadamba nkume ndị nwere mkpuchi ọdịnala dịka mbadamba shuga, mana ike ya, friability, mmịpụta mmiri, ogo mgbasa. , mkpuchi ibu ibu na ihe ngosi ndị ọzọ dị mma ka mma. A na-eji ọkwa dị ala viscosity nke ngwaahịa a dị ka ihe mkpuchi ihe nkiri na-edozi mmiri maka mbadamba nkume na ọgwụ, na ọkwa dị elu na-eji ihe mkpuchi ihe nkiri maka usoro ihe mgbaze organic, na-emekarị na ntinye nke 2% ruo 20. %
Zhang Jixing et al. jiri usoro mmetụta dị elu na-ebuli usoro premix na HPMC dị ka mkpuchi ihe nkiri. Na-ewere HPMC nke na-emepụta ihe nkiri, ọnụ ọgụgụ nke mmanya polyvinyl na plasticizer polyethylene glycol dị ka ihe nyocha, ike ike na permeability nke ihe nkiri ahụ na viscosity nke ngwọta mkpuchi ihe nkiri bụ nchịkọta nyocha, na mmekọrịta dị n'etiti nyocha. A na-akọwa index na ihe nyocha site na usoro mgbakọ na mwepụ, na usoro nhazi kachasị mma na-emesị nweta. Ihe oriri ya bụ onye na-emepụta ihe nkiri hydroxypropyl methylcellulose (HPMCE5) 11.88 g, mmanya polyvinyl 24.12 g, plasticizer polyethylene glycol 13.00 g, na mkpuchi nkwusioru bụ 20 mPa·s, permeability na ike ike nke ihe nkiri ahụ ruru ike kachasị mma nke ihe nkiri ahụ. . Zhang Yuan kwalitere usoro nkwadebe ahụ, jiri HPMC mee ihe dị ka onye na-ekekọta iji dochie starch slurry, ma gbanwee mbadamba Jiahua ka ọ bụrụ mbadamba ihe nkiri na-eme ka ọ dịkwuo mma nke nkwadebe ya, meziwanye hygroscopicity ya, ọ dị mfe ịnwụ, mbadamba nkume rụrụ arụ, gbawara agbawa na nsogbu ndị ọzọ. welie mbadamba nkume kwụsie ike. Ekpebiri usoro nhazi kachasị mma site na nyocha orthogonal, ya bụ, ntinye uche nke slurry bụ 2% HPMC na 70% ethanol ngwọta n'oge mkpuchi, na oge mkpali n'oge granulation bụ 15 min. Nsonaazụ The Jiahua film ntekwasa mbadamba nkume ndị a kwadebere site na usoro ọhụrụ na ndenye ọgwụ na-eme ka ọ dịkwuo mma n'ọdịdị, oge nkwụsịtụ na isi ike karịa nke a na-emepụta site na usoro ndenye mbụ, na ọnụego ruru eru nke mbadamba ihe nkiri ahụ na-eme ka ọ dịkwuo mma. ruru ihe karịrị 95%. Liang Meiyi, Lu Xiaohui, wdg jikwa hydroxypropyl methylcellulose dị ka ihe na-emepụta ihe nkiri iji dozie mbadamba nkume patinae colon na mbadamba nkume matrine, n'otu n'otu. na-emetụta ntọhapụ ọgwụ. Huang Yunran kwadebere mbadamba nkume Dragọn's Blood Colon, ma tinye HPMC na mkpuchi mkpuchi nke oyi akwa ọzịza, akụkụ ya dị 5%. Enwere ike ịhụ na enwere ike iji HPMC mee ihe n'ọtụtụ ebe na usoro nnyefe ọgwụ ezubere iche maka eriri afọ.
Hydroxypropyl methylcellulose abụghị naanị ihe mkpuchi ihe nkiri magburu onwe ya, kamakwa enwere ike iji ya dị ka ihe na-emepụta ihe nkiri na usoro ihe nkiri. Wang Tongshun wdg na-kachasị ka ndenye ọgwụ nke compound zinc licorice na aminolexanol ọnụ mejupụtara film, na mgbanwe, uniformity, ire ụtọ, nghọta nke film gị n'ụlọnga dị ka nnyocha index, nweta ezigbo ndenye ọgwụ bụ PVA 6.5 g, HPMC 0.1 g na 6.0 g nke ihe nkiri. propylene glycol na-ezute ihe achọrọ maka ịhapụ ngwa ngwa na nchekwa, enwere ike iji ya dị ka ndenye nkwadebe nke ihe nkiri mejupụtara.
3.2 dị ka ihe nkedo na disintegrant
Enwere ike iji ọkwa viscosity dị ala nke ngwaahịa a dị ka ihe nkedo na disintegrant maka mbadamba nkume, mkpụrụ ọgwụ na granules, na ọkwa viscosity dị elu nwere ike iji naanị dị ka ihe nkedo. Usoro onunu ogwu dịgasị iche iche na ụdị na ihe achọrọ. N'ozuzu, usoro onunu ogwu maka mbadamba granulation akọrọ bụ 5%, yana usoro onunu ogwu maka mbadamba ụrọ mmiri bụ 2%.
Li Houtao et al nyochara ihe nkedo nke mbadamba tinidazole. 8% polyvinylpyrrolidone (PVP-K30), 40% sirop, 10% starch slurry, 2.0% hydroxypropyl methylcellulose K4 (HPMCK4M), 50% ethanol dị ka adhesion nke tinidazole mbadamba n'aka. nkwadebe nke tinidazole mbadamba. Mgbanwe ọdịdị nke mbadamba nkume dị larịị na mgbe mkpuchi gasịrị ka atụnyere, na friability, ike ike, oge nkwụsịtụ na ọnụego mgbasa nke mbadamba ọgwụ dị iche iche ka a tụrụ atụ. Nsonaazụ Mbadamba ụrọ nke 2.0% hydroxypropyl methylcellulose kwadebere bụ ihe na-egbukepụ egbukepụ, na nha friability ahụghị ihe ọ bụla na-eme mkpọtụ na nkuku, na mgbe mkpuchi, ụdị mbadamba ahụ zuru oke na ọdịdị dị mma. Ya mere, a na-eji mbadamba tinidazole kwadebere na 2.0% HPMC-K4 na 50% ethanol dị ka ihe nkedo. Guan Shihai mụrụ usoro nhazi nke Fuganning Tablets, nyochaa adhesives, wee nyochaa 50% ethanol, 15% starch paste, 10% PVP na 50% ethanol ngwọta na mkpakọ, ire ụtọ, na friability dị ka nyocha nyocha. , 5% CMC-Na na 15% HPMC ngwọta (5 mPa s). Nsonaazụ The Ibé akwụkwọ kwadebere 50% ethanol, 15% starch tapawa, 10% PVP 50% ethanol ngwọta na 5% CMC-Na nwere ezigbo elu, ma ogbenye compressibility na ala siri ike, nke na-enweghị ike izute mkpa nke mkpuchi; 15% HPMC ngwọta (5 mPa·s), elu nke mbadamba nkume dị mma, friability ruru eru, na mkpakọ dị mma, nke nwere ike izute mkpa mkpuchi. Ya mere, a họọrọ HPMC (5 mPa s) dị ka nrapado.
3.3 dị ka onye na-akwụsịtụ
A na-eji ọkwa viscosity dị elu nke ngwaahịa a dị ka onye na-akwụsịtụ iji dozie nkwadebe mmiri mmiri nkwusioru. Ọ nwere mmetụta nkwụsịtụ dị mma, ọ dị mfe ịgbasa, ọ dịghị arapara na mgbidi, ma nwee ezigbo flocculation ahụ. Usoro ọgwụgwọ mbụ bụ 0.5% ruo 1.5%. Song Tian et al. A na-ejikarị ihe polymer eme ihe (hydroxypropyl methylcellulose, sodium carboxymethylcellulose, povidone, xanthan gum, methylcellulose, wdg) dị ka ndị na-akwụsịtụ iji kwadebe racecadotril. akọrọ nkwusioru. Site na sedimentation olu ratio nke dị iche iche suspensions, redispersibility index, na rheology, nkwusioru viscosity na microscopic morphology hụrụ, na nkwụsi ike nke ọgwụ irighiri n'okpuru accelerated nnwale e nyochakwara. Nsonaazụ The akọrọ nkwusioru nke a kwadebere na 2% HPMC dị ka onye nkwusioru nwere usoro dị mfe na ezigbo nkwụsi ike.
Tụnyere methyl cellulose, hydroxypropyl methyl cellulose nwere àgwà nke na-akpụ a doro anya ngwọta, na naanị a nnọọ obere ego nke na-abụghị achụsasị fibrous bekee dị, otú HPMC na-ejikarị dị ka a suspending gị n'ụlọnga na ophthalmic preparations. Liu Jie et al. eji HPMC, hydroxypropyl cellulose (HPC), carbomer 940, polyethylene glycol (PEG), sodium hyaluronate (HA) na Nchikota HA / HPMC dị ka suspending elekọta mmadụ iji kwadebe dị iche iche nkọwa Maka Ciclovir ophthalmic nkwusioru, sedimentation olu ratio, urughuru size na redispersibility. A na-ahọrọ dị ka ihe nleba anya nyocha iji nyochaa onye ọrụ nkwụsịtụ kacha mma. Nsonaazụ na-egosi na acyclovir ophthalmic nkwusioru nke a kwadebere site na 0.05% HA na 0.05% HPMC dị ka onye na-ahụ maka nkwụsịtụ, oke nha nke sedimentation bụ 0.998, nha nha ahụ bụ edo, redispersibility dị mma, na nkwadebe kwụsiri ike Mmekọahụ na-abawanye.
3.4 Dị ka ihe mgbochi, onye na-ahapụ ngwa ngwa ma na-achịkwa ya na onye na-emepụta pore
A na-eji ọkwa viscosity dị elu nke ngwaahịa a maka nkwadebe nke hydrophilic gel matrix na-adịgide adịgide-ntọhapụ mbadamba nkume, blockers na ndị na-achịkwa-ntọhapụ nke ngwakọta-ihe matrix mbadamba kwadoro-wepụta mbadamba, na nwere mmetụta nke igbu oge ntọhapụ ọgwụ. Ntinye ya bụ 10% ruo 80%. A na-eji akara ngosi viscosity dị ala dị ka porogens maka nkwado ntọhapụ na-adịgide adịgide ma ọ bụ njikwa ntọhapụ. Enwere ike iru dose nke mbụ achọrọ maka mmetụta ọgwụgwọ nke mbadamba nkume ndị dị otú ahụ ngwa ngwa, mgbe ahụ, a na-eme ka ntọhapụ ma ọ bụ nkwụsị na-achịkwa, ma na-edobe ntinye ọgwụ ọbara dị irè n'ime ahụ. . Hydroxypropyl methylcellulose na-agba mmiri ka ọ bụrụ akwa gel mgbe ọ zutere mmiri. Usoro ntọhapụ ọgwụ site na mbadamba ihe matriks na-agụnyekarị mgbasa nke oyi akwa gel na mmebi nke oyi akwa gel. Jung Bo Shim et al kwadoro mbadamba ihe ntọhapụ carvedilol nwere HPMC dị ka ihe ntọhapụ.
A na-ejikwa hydroxypropyl methylcellulose mee ihe n'ọtụtụ mbadamba mbadamba matrix nke ọgwụ ọdịnala ndị China, na ọtụtụ n'ime ihe ndị na-arụ ọrụ, akụkụ ndị dị irè na otu nkwadebe nke ọgwụ ndị China ọdịnala na-eji. Liu Wen et al. ejiri 15% hydroxypropyl methylcellulose mee ihe dị ka ihe matrix, 1% lactose na 5% microcrystalline cellulose dị ka ndị na-ejuputa, ma kwadebere Jingfang Taohe Chengqi Decoction n'ime ọnụ matriks na-ahapụ mbadamba nkume. Ihe nlereanya bụ nha Higuchi. Usoro nhazi usoro dị mfe, nkwadebe dị mfe, na data ntọhapụ dị ntakịrị, nke na-emezu ihe ndị China Pharmacopoeia chọrọ. Tang Guanguang et al. jiri ngụkọta saponins nke Astragalus mee ihe dị ka ọgwụ nlereanya, kwadebere mbadamba ihe matrix HPMC, wee nyochaa ihe ndị na-emetụta ntọhapụ ọgwụ site na akụkụ dị irè nke ọgwụ ndị China ọdịnala na mbadamba HPMC matrix. Nsonaazụ Ka usoro onunu ogwu nke HPMC na-abawanye, ntọhapụ nke astragaloside na-ebelata, na pasent ntọhapụ nke ọgwụ ahụ nwere ihe fọrọ nke nta ka ọ bụrụ njikọ dị n'ahịrị na ọnụego mgbasa nke matriks. Na mbadamba nkume hypromellose HPMC, enwere njikọ dị n'etiti ntọhapụ nke akụkụ dị irè nke ọgwụ ndị China ọdịnala na usoro onunu ogwu na ụdị HPMC, na ntọhapụ nke hydrophilic chemical monomer yiri ya. Hydroxypropyl methylcellulose abụghị naanị maka ogige hydrophilic, kamakwa maka ihe ndị na-abụghị hydrophilic. Liu Guihua jiri 17% hydroxypropyl methylcellulose (HPMCK15M) dị ka ihe matrix na-adịgide adịgide, ma kwadebere Tianshan Xuelian mbadamba ụgbụ a na-ahapụ matrix site na mmiri granulation na usoro mbadamba. Mmetụta ntọhapụ na-adịgide adịgide pụtara ìhè, na usoro nkwadebe ahụ kwụsiri ike ma nwee ike ime ya.
Hydroxypropyl methylcellulose abụghị naanị etinyere ya na mbadamba matriks a na-ahapụ akwadoro nke ihe ndị na-arụ ọrụ yana akụkụ dị mma nke ọgwụ ndị China ọdịnala, mana a na-ejikwa ya na nkwadebe ngwakọta ọgwụ ndị China. Wu Huichao et al. jiri 20% hydroxypropyl methyl cellulose (HPMCK4M) dị ka ihe matriks, ma jiri usoro nchịkọta ntụ ntụ mee ihe iji dozie mbadamba nkume Yizhi hydrophilic gel matrix nke nwere ike ịhapụ ọgwụ ahụ na-aga n'ihu na nkwụsi ike maka awa 12. A na-eji Saponin Rg1, ginsenoside Rb1 na Panax notoginseng saponin R1 mee ihe dị ka nyocha nyocha iji nyochaa ntọhapụ na vitro, na nhazi ntọhapụ ọgwụ ahụ dabara adaba iji mụọ usoro ntọhapụ ọgwụ. Nsonaazụ Usoro ntọhapụ ọgwụ ahụ kwekọrọ na nha nha nha nke efu na nha Ritger-Peppas, bụ nke ewepụtara geniposide site na mgbasa ozi na-abụghị Fick, na akụkụ atọ dị na Panax notoginseng ka ewepụtara site na mbuze ọkpụkpụ.
3.5 Gluo nchekwa dị ka thickener na colloid
Mgbe a na-eji ngwaahịa a dị ka thickener, ntinye pasent nke mbụ bụ 0.45% ruo 1.0%. Ọ nwekwara ike ime ka nkwụsi ike nke gluu hydrophobic dịkwuo elu, na-emepụta colloid nchebe, na-egbochi ihe ndị dị na coalescing na agglomerating, si otú ahụ na-egbochi nhazi nke sediments. Ọnụ ọgụgụ ya na-emekarị bụ 0.5% ruo 1.5%.
Wang Zhen et al. jiri usoro nnwale L9 orthogonal iji nyochaa usoro nkwadebe nke carbon enema na-arụ ọrụ ọgwụ. Kacha mma usoro ọnọdụ maka ikpeazụ mkpebi siri ike nke ọgwụ na-arụ ọrụ carbon enema bụ iji 0,5% sodium carboxymethyl cellulose na 2.0% hydroxypropyl methylcellulose (HPMC nwere 23.0% methoxyl otu, hydroxypropoxyl Base 11.6%) dị ka a thickener, usoro ọnọdụ na-enyere aka. nkwụsi ike nke carbon na-arụ ọrụ ọgwụ. Zhang Zhiqiang et al. mebere pH-sensitive levofloxacin hydrochloride ophthalmic jel dị njikere iji ya na nsonaazụ ntọhapụ na-adịgide adịgide, na-eji carbopol dị ka gel matrix na hydroxypropyl methylcellulose dị ka onye na-eme ihe. Ezigbo ndenye ọgwụ site na nnwale, n'ikpeazụ nweta ezigbo ndenye ọgwụ bụ levofloxacin hydrochloride 0.1 g, carbopol (9400) 3 g, hydroxypropyl methylcellulose (E50 LV) 20 g, disodium hydrogen phosphate 0.35 g, phosphoric acid 0.45 g sodium dihydrogede. , 0.03 g nke ethyl paraben, na mmiri na-agbakwunyere 100 ml. N'ime ule ahụ, onye edemede ahụ kpuchiri hydroxypropyl methylcellulose METHOCEL usoro nke Colorcon Company na nkọwa dị iche iche (K4M, E4M, E15 LV, E50LV) iji kwadebe thickeners na iche iche iche, na n'ihi na-ahọrọ HPMC E50 LV dị ka thickener. Thickener maka pH-sensitive levofloxacin hydrochloride gels ozugbo.
3.6 dị ka capsule ihe
Ọtụtụ mgbe, ihe mkpuchi capsule nke capsules na-abụkarị gelatin. Usoro mmepụta nke shei capsule dị mfe, ma enwere ụfọdụ nsogbu na ihe ndị dị ka nchebe na-adịghị mma megide mmiri mmiri na ọgwụ ndị na-emetụta ikuku oxygen, mbelata mgbasa ọgwụ ọgwụ, na nkwụsịtụ nke shea capsule na-egbu oge n'oge nchekwa. Ya mere, a na-eji hydroxypropyl methylcellulose dochie anya capsules gelatin maka nkwadebe nke capsules, nke na-eme ka mmepụta capsule dị mma na mmetụta ojiji, ma kwalitere ya n'ụlọ na ná mba ọzọ.
Iji theophylline dị ka ọgwụ nchịkwa, Podczeck et al. chọpụtara na ọnụego mgbasa ọgwụ nke capsules nwere shei hydroxypropyl methylcellulose karịrị nke capsules gelatin. Ihe kpatara nyocha ahụ bụ na nbibi nke HPMC bụ nkwụsị nke capsule dum n'otu oge ahụ, ebe mgbawa nke capsule gelatin bụ nkewa nke usoro netwọk mbụ, wee gbasaa nke capsule dum, ya mere, Capsule HPMC dabara adaba maka shells Capsule maka usoro mwepụta ozugbo. Chiwele et al. nwetakwara nkwubi okwu yiri nke ahụ ma tụnyere mgbasa nke gelatin, gelatin/polyethylene glycol na shells HPMC. Nsonaazụ gosiri na a na-agbaze shells HPMC ngwa ngwa n'okpuru ọnọdụ pH dị iche iche, ebe gelatin capsules Ọ na-emetụta ọnọdụ pH dị iche iche nke ukwuu. Tang Yue et al. enyochara ụdị shei capsule ọhụrụ maka sistemu ihe na-ebu ihe na-ebu ọgwụ na-enweghị ntụ ntụ ntụ. E jiri ya tụnyere shei capsule nke hydroxypropyl methylcellulose na capsule shei nke gelatin, a na-enyocha nkwụsi ike nke shea capsule na njirimara nke ntụ ntụ na shea n'okpuru ọnọdụ dị iche iche, na nyocha nke friability. Nsonaazụ na-egosi na e jiri ya tụnyere gelatin capsules, HPMC capsule shells dị mma na nkwụsi ike na nchebe ntụ ntụ, nwere nguzogide mmiri siri ike, ma nwee obere friability karịa gelatin capsule shells, ya mere HPMC capsule shells dị mma maka Capsules maka ikpo ọkụ ntụ ntụ.
3.7 dị ka bioadhesive
Teknụzụ bioadhesion na-eji ihe ndị nwere polymers bioadhesive. Site na ịrapagidesi ike na mucosa ndu, ọ na-eme ka ọganihu na nkwụsị nke kọntaktị dị n'etiti nkwadebe na mucosa, nke mere na a na-eji nwayọọ nwayọọ na-ahapụ ọgwụ ahụ ma tinye ya n'ime mucosa iji nweta nzube nke ọgwụgwọ. A na-ejikarị ya eme ihe ugbu a. Ọgwụgwọ nke ọrịa nke eriri afọ tract, ikpu, onu mucosa na akụkụ ndị ọzọ.
Teknụzụ bioadhesion nke eriri afọ bụ usoro nnyefe ọgwụ ọhụrụ emepụtara n'afọ ndị na-adịbeghị anya. Ọ bụghị naanị na ọ na-agbatị oge obibi nke nkwadebe ọgwụ na tract gastrointestinal, kamakwa na-eme ka arụmọrụ kọntaktị dị n'etiti ọgwụ na akpụkpọ ahụ cell na saịtị absorption, na-agbanwe mmiri nke akpụkpọ ahụ cell, ma na-eme ka ntinye nke ọgwụ ahụ banye. A na-eme ka mkpụrụ ndụ epithelial nke obere eriri afọ dịkwuo mma, si otú a na-eme ka bioavailability nke ọgwụ ahụ dịkwuo mma. Wei Keda et al. jiri usoro ọgwụgwọ HPMCK4M na Carbomer 940 kpuchie mbadamba nkume ahụ dị ka ihe nyocha, wee jiri ngwaọrụ bioadhesion nke mere onwe ya iji tụọ ike peeling n'etiti mbadamba nkume na biofilm simulated site na ịdị mma nke mmiri dị na akpa rọba. , n'ikpeazụ họrọ ọdịnaya nke HPMCK40 na carbomer 940 ka ọ bụrụ 15 na 27.5 mg na mpaghara ọgwụ kacha mma nke NCaEBT mbadamba nkume cores, n'otu n'otu, iji kwadebe NCaEBT mbadamba nkume cores, na-egosi na ihe bioadhesive (dị ka hydroxypropyl methylcellulose) nwere ike belata nke ukwuu. adhesion nke nkwadebe na anụ ahụ.
Nkwadebe bioadhesive nke ọnụ bụkwa ụdị usoro nnyefe ọgwụ ọhụrụ nke a mụọla nke ọma n'afọ ndị na-adịbeghị anya. Nkwadebe bioadhesive nke ọnụ nwere ike ịrapagidesi ike na ọgwụ ahụ na akụkụ emetụtara nke oghere ọnụ, nke ọ bụghị naanị na-agbatị oge obibi nke ọgwụ ahụ na mucosa ọnụ, kamakwa na-echebe mucosa ọnụ. Mmetụta ọgwụgwọ ka mma yana nwelite bioavailability ọgwụ. Xue Xiaoyan et al. Haziri nhazi nke mbadamba ihe nrapado ọnụ nke insulin, na-eji apple pectin, chitosan, carbomer 934P, hydroxypropyl methylcellulose (HPMC K392) na sodium alginate dị ka ihe bioadhesive, na ifriizi-ihicha iji kwadebe insulin ọnụ. Mpempe akwụkwọ oyi akwa abụọ nrapado. Mbadamba ụrọ nke insulin a kwadebere nke ọma nwere ihe owuwu nwere oghere dị ka sponge, nke dị mma maka mwepụta insulin, ma nwee oyi akwa nchekwa hydrophobic, nke nwere ike hụ na mwepụta nke ọgwụ na-enweghị isi wee zere ịnwụ ọgwụ ahụ. Hao Jifu et al. kwadokwara beads na-acha anụnụ anụnụ-edo edo ọnụ ọnụ bioadhesive patches na-eji Baiji gluu, HPMC na carbomer dị ka ihe bioadhesive.
N'ime usoro nnyefe ọgwụ ikpu, teknụzụ bioadhesion ejiriwokwa nke ọma. Zhu Yuting et al. ejiri carbomer (CP) na HPMC mee ihe dị ka ihe nrapado na matrix na-adịgide adịgide iji kwadebe mbadamba nkume clotrimazole bioadhesive vaginal nwere usoro dị iche iche na oke dị iche iche, wee tụọ nrapanye ha, oge nrapanye na pasent ọzịza na gburugburu ebe mmiri ara ehi arụrụ arụ. , A na-enyocha ndenye ọgwụ kwesịrị ekwesị dị ka CP-HPMC1: 1, mpempe akwụkwọ ntanye a kwadebere na-arụ ọrụ nke ọma, na usoro ahụ dị mfe ma kwe omume.
3.8 dị ka Gel
Dị ka nkwadebe nrapado, gel nwere usoro uru dị ka nchekwa, ịma mma, nhicha dị mfe, ọnụ ala dị ala, usoro nkwadebe dị mfe, yana ezigbo ndakọrịta na ọgwụ. Ntuziaka nke mmepe. Dịka ọmụmaatụ, gel transdermal bụ ụdị usoro onunu ogwu ọhụrụ nke a na-amụ karịa n'afọ ndị na-adịbeghị anya. Ọ nwere ike ọ bụghị nanị na-ezere mbibi nke ọgwụ ọjọọ n'ime eriri afọ tract na ibelata ọnụ ọgụgụ kasị elu-na-trough mgbanwe nke ọbara ọgwụ ịta, ma bụrụkwa otu n'ime irè ntọhapụ ọgwụ na usoro iji merie ọgwụ ọjọọ mmetụta. .
Zhu Jingjie et al. mụọ mmetụta nke matrices dị iche iche na ntọhapụ nke scutellarin alcohol plastid gel in vitro, ma kpuchie ya na carbomer (980NF) na hydroxypropyl methylcellulose (HPMCK15M) dị ka gel matrices, wee nweta sutellarin kwesịrị ekwesị maka sutellarin. Gel matrix nke plastids mmanya. Nsonaazụ nnwale na-egosi na 1. 0% carbomer, 1. 5% carbomer, 1. 0% carbomer + 1. 0% HPMC, 1. 5% carbomer + 1. 0% HPMC dị ka gel matrix Ha abụọ dabara adaba maka plastids mmanya sutellarin. . N'oge nnwale ahụ, achọpụtara na HPMC nwere ike ịgbanwe usoro ntọhapụ ọgwụ nke carbomer gel matrix site na itinye nha nha nke ntọhapụ ọgwụ, yana 1.0% HPMC nwere ike melite 1.0% carbomer matrix na 1.5% carbomer matrix. Ihe kpatara ya nwere ike ịbụ na HPMC na-amụba ngwa ngwa, na mgbasawanye ngwa ngwa na mmalite nke nnwale ahụ na-eme ka ọdịiche dị na molekụla nke carbomer gel dị ukwuu, si otú a na-eme ka ọnụọgụ ọgwụ ya dịkwuo elu. Zhao Wencui et al. ejiri carbomer-934 na hydroxypropyl methylcellulose mee ihe dị ka ndị na-ebu iji dozie gel norfloxacin ophthalmic gel. Usoro nkwadebe dị mfe ma kwe omume, na àgwà kwekọrọ na gel ophthalmic nke "Chinese Pharmacopoeia" (mbipụta 2010) chọrọ mma.
3.9 Ihe mgbochi mmiri ozuzo maka sistemu microemulsifying onwe
Usoro nnyefe ọgwụ nke onwe-microemulsifying (SMEDDS) bụ ụdị ọhụrụ nke usoro nnyefe ọgwụ ọnụ, nke bụ ngwakọta, kwụsiri ike na nke doro anya nke mejupụtara ọgwụ, oge mmanụ, emulsifier na co-emulsifier. Ngwakọta nke ndenye ọgwụ dị mfe, na nchekwa na nkwụsi ike dị mma. Maka ọgwụ ndị na-adịghị mma soluble, a na-agbakwunye ihe ndị na-eme ka mmiri na-edozi mmiri, dị ka HPMC, polyvinylpyrrolidone (PVP), na ihe ndị ọzọ, iji mee ka free ọgwụ na ọgwụ ndị na-ekpuchi microemulsion na-enweta mgbasa nke supersaturated na eriri afọ, nke mere na mụbaa solubility ọgwụ ma melite bioavailability.
Peng Xuan et al. kwadebere silibinin supersaturated onwe-emulsifying usoro nnyefe ọgwụ (S-SEDDS). Oxyethylene hydrogenated castor mmanụ (Cremophor RH40), 12% caprylic capric acid polyethylene glycol glyceride (Labrasol) dị ka co-emulsifier, na 50 mg·g-1 HPMC. Ịtinye HPMC na SSEDDS nwere ike imeju silibinin efu ka ọ gbazee na S-SEDDS ma gbochie silibinin ịwụsa. E jiri ya tụnyere omenala onwe-microemulsion formulations, a nnukwu ego nke surfactant na-emekarị na-agbakwunyere iji gbochie ezughị ezu encapsulation ọgwụ. Mgbakwunye nke HPMC nwere ike idobe solubility nke silibinin na mgbasa ozi dịtụ ala, na-ebelata emulsification na usoro microemulsion nke onwe. onunu ogwu nke onye nnọchi anya.
4.Mkpebi
Enwere ike ịhụ na a na-eji HPMC eme ihe n'ọtụtụ ebe na nkwadebe n'ihi njirimara anụ ahụ, kemịkalụ na nke ndu, mana HPMC nwekwara ọtụtụ adịghị ike na nkwadebe, dị ka ihe ọhụrụ nke ntọhapụ tupu na mgbe ọ gasịrị. methyl methacrylate) iji meziwanye. N'otu oge ahụ, ụfọdụ ndị nchọpụta nyochara ngwa nke osmotic theory na HPMC site n'ịkwado mbadamba ụrọ nke carbamazepine na mbadamba verapamil hydrochloride na-adịgide adịgide iji mụọ usoro ntọhapụ ya ọzọ. N'okwu, ọtụtụ ndị na-eme nchọpụta na-arụ ọrụ dị ukwuu maka ngwa kachasị mma nke HPMC na nkwadebe, yana site na nyocha miri emi nke ihe onwunwe ya na mmelite nke nkà na ụzụ nkwadebe, HPMC ga-eji ya mee ihe na ụdị usoro onunu ogwu ọhụrụ. na ụdị usoro onunu ogwu ọhụrụ. Na nyocha nke usoro ọgwụ, wee kwalite mmepe nke ụlọ ahịa ọgwụ na-aga n'ihu.
Oge nzipu: Ọktoba 08-2022