1. The isi ọdịdị nke HPMC
Hypromellose, aha Bekee hydroxypropyl methylcellulose, utu aha HPMC.Usoro ihe omimi ya bụ C8H15O8-(C10Hl8O6)n-C8Hl5O8, na arọ molekụla dị ihe dịka 86,000.Ngwaahịa a bụ ihe ọkara synthetic, nke bụ akụkụ nke otu methyl na akụkụ nke polyhydroxypropyl ether nke cellulose.Enwere ike ịmepụta ya site na ụzọ abụọ: otu bụ ịgwọ methyl cellulose nke ọkwa kwesịrị ekwesị na NaOH, wee meghachi omume na propylene oxide n'okpuru nnukwu okpomọkụ na nrụgide dị elu.A ghaghị ịkwado oge mmeghachi omume iji kwe ka otu methyl na hydroxypropyl jikọọ na ether.Ụdị nke jikọtara ya na mgbanaka anhydroglucose nke cellulose, ma nwee ike iru ogo achọrọ;nke ọzọ bụ na-emeso owu linter ma ọ bụ osisi pulp eriri na caustic soda, wee nweta site na-emeghachi omume na chlorinated methane na propylene oxide na-aga nke ọma, na mgbe ọzọ nụchara anụcha , Pulverize, mee ka n'ime ezi na edo ntụ ntụ ma ọ bụ granule.HPMC bụ cellulose dị iche iche sitere n'okike, ma ọ bụkwa ihe magburu onwe ya na-emepụta ọgwụ, nke nwere nnukwu isi iyi.Ka ọ dị ugbu a, a na-ejikarị ya eme ihe n'ụlọ na ná mba ọzọ, ọ bụkwa otu n'ime ihe ndị na-emepụta ọgwụ nwere ọnụ ọgụgụ kachasị elu n'etiti ọgwụ ọnụ.
Agba nke ngwaahịa a na-acha ọcha na-acha ọcha na-acha ọcha, na-adịghị egbu egbu na enweghị ụtọ, ọ bụkwa granular ma ọ bụ fibrous, ntụ ntụ na-adị mfe.Ọ kwụsiri ike n'okpuru mkpughe ọkụ na iru mmiri.Ọ na-aza na mmiri oyi ka ọ bụrụ ngwọta colloidal na-acha ọcha na-acha ọcha nke nwere ogo viscosity ụfọdụ.Ihe ngbanwe nke sol-gel nwere ike ime n'ihi mgbanwe okpomọkụ nke ụfọdụ ntinye ngwọta.Ọ dị mfe igbari na mmanya 70% ma ọ bụ dimethyl ketone, ọ gaghị agbaze na mmanya na-egbu egbu, chloroform ma ọ bụ ethoxyethane.
Hypromellose nwere ezigbo nkwụsi ike mgbe pH dị n'etiti 4.0 na 8.0, ọ nwere ike ịdị n'etiti 3.0 na 11.0.Mgbe echekwabara maka ụbọchị 10 na okpomọkụ nke 20 Celsius C yana iru mmiri nke 80%, ọnụọgụ nnabata mmiri nke HPMC bụ 6.2%.
N'ihi ọdịiche dị na ọdịnaya nke ihe abụọ na-anọchi anya na nhazi nke hypromellose, methoxy na hydroxypropyl, ụdị ngwaahịa dị iche iche apụtala.N'ime otu ntinye uche, ụdị ngwaahịa dị iche iche nwere kpọmkwem viscosity na Thermal gelation okpomọkụ, ya mere, nwere ihe dị iche iche ma nwee ike iji ya mee ihe dị iche iche.The pharmacopoeias nke mba dị iche iche nwere dị iche iche nkọwa na okwu maka ihe nlereanya: The European Pharmacopoeia dabeere na ọkwa dị iche iche nke dị iche iche viscosities na dị iche iche nke nnọchi nke ngwaahịa na ahịa.A na-egosipụta ya site na ọkwa gbakwunyere nọmba.Nkeji a bụ mPa•s.Mgbe gbakwunyere ọnụọgụ 4 iji gosi ọdịnaya na ụdị nke ọ bụla nọchiri anya hypromellose, dịka ọmụmaatụ, hypromellose 2208, ọnụọgụ abụọ nke mbụ na-anọchite anya pasentị nke methoxy, ọnụọgụ abụọ ikpeazụ na-anọchi anya hydroxypropyl Odika pasent nke ikpe.
2.The usoro nke igbari HPMC na mmiri
2.1 Usoro mmiri ọkụ
Ebe ọ bụ na hypromellose anaghị agbaze na mmiri ọkụ, enwere ike ịgbasa ya na mmiri ọkụ na mbido mbụ, mgbe ahụ, ọ bụrụ na ọ dị mma, a na-akọwa ụzọ abụọ a na-ahụkarị dị ka ndị a:
(1) Tinye mmiri ọkụ achọrọ n'ime akpa ahụ wee kpoo ya ihe dịka 70 ℃.Jiri nwayọ tinye ngwaahịa ahụ n'okpuru edemede nwayọ.Na mbido, ngwaahịa ahụ na-ese n'elu mmiri, wee jiri nwayọọ nwayọọ na-emepụta slurry.Mee ka slurry dị jụụ.
(2) Tinye 1/3 ma ọ bụ 2/3 nke mmiri achọrọ n'ime akpa ahụ wee kpoo ya na 70 Celsius C iji chụsasịa ngwaahịa ahụ iji kwadebe mmiri ọkụ na-ekpo ọkụ, wee gbakwunye ihe fọdụrụ nke mmiri oyi ma ọ bụ mmiri ice. na mmiri ọkụ slurry Na slurry, dị jụụ ngwakọta mgbe edemede.
2.2 Usoro ngwakọta ntụ ntụ
A na-agbasasị akụkụ ntụ ntụ na ihe ndị ọzọ powdery nke nha ma ọ bụ buru ibu site na ngwakọta akọrọ, wee tinye mmiri ka ọ gbazee.N'oge a, hypromellose nwere ike ịgbaze n'enweghị agglomeration.
3. Uru nke HPMC
3.1 Mmiri oyi solubility
Ọ na-agbaze na mmiri oyi n'okpuru 40 Celsius C ma ọ bụ 70% ethanol.Ọ bụ isi ihe na-esighi ike na mmiri ọkụ karịa 60 Celsius C, mana enwere ike ịme ya.
3.2 Chemical inertness
Hypromellose (HPMC) bụ ụdị ether cellulose na-abụghị ionic.Ngwọta ya enweghị ụgwọ ionic na anaghị emekọ ya na nnu ígwè ma ọ bụ ogige ionic organic.Ya mere, ndị ọzọ excipients adịghị emeghachi omume na ya n'oge usoro nkwadebe.
3.3 Nkwụsi ike
Ọ dịtụ mma ma acid na alkali, enwere ike ịchekwa ya ogologo oge n'etiti pH 3 ruo 1l, na viscosity ya enweghị mgbanwe doro anya.Ngwọta mmiri nke hypromellose (HPMC) nwere mmetụta mgbochi ebu ma nwee ike idowe nkwụsi ike viscosity dị mma n'oge nchekwa ogologo oge.Ihe mgbakwunye ọgwụ na-eji HPMC nwere nkwụsi ike ka mma karịa ndị na-eji ihe mgbakwunye ọdịnala (dị ka dextrin, starch, wdg).
3.4 Mgbanwe nke viscosity
Enwere ike ịgwakọta viscosity dị iche iche nke HPMC n'ụzọ dị iche iche, na viscosity ya nwere ike ịgbanwe dịka otu iwu siri dị, ma nwee mmekọrịta dị mma na linear, yabụ enwere ike họrọ ya dịka ihe achọrọ.
3.5 Metabolic inertia
HPMC anaghị etinye uche ma ọ bụ metabolized n'ime ahụ, ọ naghị enye calorie, ya mere ọ bụ ihe dị mma maka nkwadebe ọgwụ.
3.6 Nchekwa
A na-ekwenyekarị na HPMC bụ ihe na-adịghị egbu egbu na nke na-adịghị ewe iwe.Ọnụọgụ ọnwụ nke etiti maka ụmụ oke bụ 5g/kg, yana oke egbu egbu maka oke bụ 5.2g/kg.Usoro onunu ogwu kwa ụbọchị adịghị emerụ ahụ mmadụ.
4. Ngwa nke HPMC na nkwadebe
4.1 Ejiri ya dị ka ihe mkpuchi ihe nkiri na ihe na-emepụta ihe nkiri
A na-eji Hypromellose (HPMC) mee ihe dị ka mbadamba ihe mkpuchi ihe nkiri.E jiri ya tụnyere mbadamba nkume ndị a na-ekpuchi omenala dịka mbadamba shuga, mbadamba nkume ndị a na-ekpuchi enweghị uru doro anya na-ekpuchi uto na ọdịdị ahụ, ma ha siri ike na friability , Mwepu mmiri mmiri, nkwụsịtụ, mkpuchi mkpuchi ibu na ihe ngosi ndị ọzọ dị 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.Ntinye uche ojiji na-abụkarị 2.0% -20%.
4.2 dị ka onye na-ekekọta na disintegrant
Enwere ike iji ọkwa nke viscosity dị ala nke ngwaahịa a dị ka ihe nkedo na nkesa maka mbadamba nkume, mkpụrụ ọgwụ na granules, na ọkwa viscosity dị elu nwere ike iji mee ihe dị ka ihe nkedo.Usoro onunu ogwu dịgasị iche iche na ụdị na ihe achọrọ.N'ozuzu, ọnụ ọgụgụ nke ihe nkedo eji maka mbadamba ụrọ akọrọ bụ 5%, na ọnụọgụ nke ejiri maka mbadamba mmiri granulation bụ 2%.
4.3 Dị ka onye na-akwụsịtụ
Ihe nkwusioru bụ ihe gel viscous nwere hydrophilicity.The ojiji nke suspending gị n'ụlọnga na suspending gị n'ụlọnga nwere ike ebelata sedimentation ọsọ nke irighiri, na ọ nwere ike na-agbakwunyere n'elu nke ahụ iji gbochie ahụ si polymerizing na condensing n'ime a uka.Ndị ọrụ nkwụsịtụ na-ekere òkè dị mkpa na mmepụta nke nkwusioru.HPMC bụ ezigbo ndị nnọchi anya nkwusioru dị iche iche.Ngwọta colloidal gbazere n'ime ya nwere ike ibelata esemokwu nke interface mmiri siri ike na ike efu na obere ihe siri ike, si otú a na-eme ka nkwụsi ike nke usoro mgbasa ozi dị iche iche.Ngwaahịa a bụ nkwadebe mmiri nkwusioru viscosity dị elu nke a kwadebere dị ka onye na-akwụsịtụ.Ọ nwere mmetụta nkwusioru dị mma, dị mfe ịgbasa, anaghị arapara n'ahụ, na ezigbo flocculated.Ọnụ ego a na-emekarị bụ 0.5% ruo 1.5%.
4.4 A na-eji ya 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 iji kwadebe mbadamba ihe ntọhapụ hydrophilic gel matrix, ndị na-azụ azụ na ihe ntọhapụ a na-achịkwa maka mbadamba ihe ntọhapụ agwakọta.Ọ nwere mmetụta nke igbu oge ntọhapụ ọgwụ.Nleta ojiji ya bụ 10% ~ 80% (W / W).A na-eji akara viscosity dị ala dị ka ihe na-emepụta pore maka nhazi ntọhapụ na-adịgide adịgide ma ọ bụ na-achịkwa.Enwere ike iru dose nke mbụ achọrọ maka mmetụta ọgwụgwọ nke ụdị mbadamba nkume a ngwa ngwa, wee nwee mmetụta ntọhapụ na-akwado ma ọ bụ na-achịkwa, ma na-edobe itinye uche ọgwụ ọbara dị irè n'ime ahụ.Hypromellose hydrates na-etolite akwa gel mgbe ọ zutere mmiri.Usoro nke ntọhapụ ọgwụ site na mbadamba ihe matriks bụ tumadi mgbasa nke oyi akwa gel na mmebi nke oyi akwa gel.
4.5 Gluo nchekwa eji dị ka thickener na colloid
Mgbe ngwaahịa a na-eji dị ka a thickener, mbụ ịta bụ 0.45% ~ 1.0%.Ngwaahịa a nwekwara ike ịbawanye nkwụsi ike nke gluu hydrophobic, na-etolite colloid na-echebe, gbochie urughuru coalescence na agglomeration, si otú na-egbochi guzobe sediments.Ntinye uche ya na-emekarị bụ 0.5% ~ 1.5%.
4.6 Ejiri ya dị ka ihe capsule
Ọtụtụ mgbe, ihe mkpuchi capsule nke capsule bụ nke kachasị gelatin.Usoro mmepụta nke shei capsule Ming dị mfe, mana enwere ụfọdụ nsogbu na ihe ndị dị ka nchebe na-adịghị mma nke mmiri mmiri na ọgwụ ndị na-enwe mmetụta oxygen, mbelata mgbasa ọgwụ ọgwụ, na igbu oge nke mgbasa nke capsule n'oge nchekwa.Ya mere, a na-eji hypromellose dochie ihe capsule na nkwadebe nke capsules, nke na-eme ka moldability na mmetụta nke capsule dịkwuo mma, ma kwalitere ya n'ụlọ na ná mba ọzọ.
4.7 Dị ka bioadhesive
Nkà na ụzụ bioadhesive, ngwa nke ihe ndị na-emepụta ihe na ihe ndị na-emepụta ihe na-emepụta ihe na-emepụta ihe na-emepụta ihe na-emepụta ihe na-emepụta ihe na-emepụta ihe, site n'ịrapara na mucosa ndu, na-eme ka ọganihu na njigide nke kọntaktị dị n'etiti nkwadebe na mucosa, nke mere na a na-eji nwayọọ nwayọọ na-ahapụ ọgwụ ahụ ma na-etinye uche ya na mucosa iji nweta nzube. ọgwụgwọ.A na-ejikarị ya eme ihe ugbu a A na-eji ya agwọ ọrịa nke oghere imi na mucosa ọnụ.Teknụzụ bioadhesion nke eriri afọ bụ ụdị 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 ọrụ kọntaktị nke ọgwụ ahụ dịkwuo mma na akpụkpọ ahụ cell nke ebe absorption na-agbanwe ma gbanwee mmiri mmiri nke akpụkpọ ahụ.A na-akwalite ike ntinye ọgwụ na sel epithelial nke obere eriri afọ, si otú ahụ na-eme ka bioavailability nke ọgwụ ahụ dịkwuo mma.
4.8 Dị ka ihe mgbakwasị ụkwụ
Dị ka nkwadebe nrapado maka akpụkpọ anụ, 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.N'ime afọ ndị na-adịbeghị anya, ọ natara nlebara anya dị ukwuu ma ghọọ mmepe nke nkwadebe mpụga akpụkpọ anụ.uzo.
4.9 Dị ka ihe mgbochi mmiri ozuzo na usoro emulsification
Oge nzipu: Dec-16-2021