1. The isi Njirimara nke HPMC
Hypromellose, aha zuru oke hydroxypropyl methylcellulose, utu aha HPMC. Usoro ihe omimi ya bụ C8H15O8- (C10Hl8O6) n-C8Hl5O8, na ịdị arọ ya dị ihe dị ka 86000. Ngwaahịa a bụ ihe eji eme ihe na-emepụta ihe, nke bụ akụkụ nke methyl na akụkụ nke polyhydroxypropyl ether nke cellulose. Enwere ike ịmepụta ya site na ụzọ abụọ: otu bụ na a na-emeso ọkwa kwesịrị ekwesị nke methyl cellulose na NaOH, wee meghachi omume na propylene oxide n'okpuru nnukwu okpomọkụ na nrụgide. Ụdị ahụ jikọtara ya na mgbanaka anhydroglucose nke cellulose, ma nwee ike iru ọkwa dị mma; nke ọzọ bụ na-emeso owu linter ma ọ bụ osisi pulp eriri na caustic soda, na-emeghachi omume na methyl chloride na propylene oxide n'otu n'otu iji nweta ya, na mgbe ọzọ nụchaa, gwepịara egweri na-eme ka mma na edo edo ntụ ntụ ma ọ bụ granules. HPMC bụ cellulose dị iche iche sitere n'okike, ma ọ bụkwa ihe magburu onwe ya na-emepụta ọgwụ, nke nwere ọtụtụ isi mmalite. 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 kasị elu na-eji ọgwụ ọnụ.
Ngwaahịa a na-acha ọcha na-acha ọcha na-acha ọcha na agba, anaghị egbu egbu na enweghị ụtọ, ọ dịkwa n'ụdị ntụ ntụ granular ma ọ bụ fibrous nke na-asọpụta ngwa ngwa. Ọ kwụsiri ike n'okpuru mkpughe ọkụ na iru mmiri. Ọ na-aza na mmiri oyi ka ọ bụrụ mmiri ara ehi colloidal ngwọta, nke nwere ogo nke viscosity, na ihe omume nke sol-gel interconversion nwere ike ime n'ihi mgbanwe okpomọkụ nke ụfọdụ ntinye nke ngwọta. Ọ na-agbaze nke ukwuu na mmanya 70% ma ọ bụ dimethyl ketone, ọ gaghị agbaze na mmanya zuru oke, chloroform ma ọ bụ ethoxyethane.
Mgbe pH nke hypromellose dị n'etiti 4.0 na 8.0, ọ nwere ezigbo nkwụsi ike, ọ pụkwara ịdị na-eguzosi ike mgbe pH dị n'etiti 3.0 na 11.0. Mgbe okpomọkụ dị 20 Celsius C na iru mmiri dị 80%, a na-echekwa ya maka ụbọchị 10. Ọnụego nnabata mmiri nke HPMC bụ 6.2%.
N'ihi ọdịnaya dị iche iche nke methoxy na hydroxypropyl na nhazi nke hypromellose, ụdị ngwaahịa dị iche iche apụtala. N'ihe dị iche iche dị iche iche, 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. Ndị pharmacopoeias nke mba dị iche iche nwere ụkpụrụ dị iche iche na ihe nnọchianya na ụdị: European Pharmacopoeia, dị ka ọkwa dị iche iche nke viscosities dị iche iche na ogo nke nnọchi nke ngwaahịa ndị a na-ere n'ahịa, na-anọchi anya akara ule gbakwunyere nọmba, na unit bụ mPa. · s; na United States Pharmacopoeia, aha a na-akpọkarị Tinye ọnụọgụ 4 na njedebe iji gosi ọdịnaya na ụdị nke ọ bụla n'ime hypromellose, dị ka hypromellose 2208, ọnụọgụ abụọ mbụ na-anọchi anya pasent nke methoxy, na ọnụọgụ abụọ ikpeazụ na-anọchi anya hydroxypropyl. Odika pasenti.
2. Usoro nke igbari HPMC na mmiri
2.1 usoro mmiri ọkụ
Ebe ọ bụ na hypromellose adịghị agbaze na mmiri ọkụ, enwere ike ịgbasa ya n'otu n'otu na mmiri ọkụ na mmalite, wee mee ka ọ dị jụụ. A na-akọwa ụzọ abụọ ahụkarị dị ka ndị a:
(1) Tinye mmiri ọkụ achọrọ n'ime akpa ahụ, ma kpoo ya ihe dị ka 70 Celsius C, jiri nwayọọ nwayọọ tinye ngwaahịa a n'okpuru nwayọọ nwayọọ, na mmalite, ngwaahịa a na-ese n'elu mmiri ahụ, wee jiri nwayọọ nwayọọ na-etolite. slurry, na-akpali Jụụ slurry ahụ.
(2) Tinye 1/3 ma ọ bụ 2/3 nke mmiri achọrọ n'ime akpa ahụ wee kpoo ya na 70 Celsius C iji gbasaa ngwaahịa ahụ iji kwadebe mmiri ọkụ na-ekpo ọkụ, wee tinye ihe fọdụrụ nke mmiri oyi ma ọ bụ mmiri ice ruo mgbe. silts mmiri ọkụ Na slurry, ngwakọta na-adị mma mgbe ọ kpalitere.
2.2 Usoro ngwakọta ntụ ntụ
A na-agbasasị ihe ndị ahụ ntụ ntụ n'ụzọ zuru ezu site na ịgwakọta akọrọ na nha ma ọ bụ karịa nke ihe ndị ọzọ powdery, wee gbazee na mmiri. N'oge a, hypromellose nwere ike ịgbaze n'enweghị agglomeration.
3. Uru nke HPMC
3.1 Mmiri oyi solubility
Soluble na mmiri oyi dị n'okpuru 40 Celsius ma ọ bụ 70% ethanol, nke a na-apụghị ịsacha na mmiri ọkụ n'elu 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 kwụsiri ike na acid na alkali, enwere ike ịchekwa ya ogologo oge n'etiti pH 3 na 1l na-enweghị mgbanwe doro anya na viscosity. Ngwọta mmiri nke hypromellose (HPMC) nwere mmetụta mgbochi mildew ma nwee ike idowe nkwụsi ike viscosity dị mma n'oge nchekwa ogologo oge. Pharmaceuticals na-eji HPMC dị ka ihe mgbakwunye nwere nkwụsi ike dị mma karịa ndị na-eji ihe mgbakwunye ọdịnala (dị ka dextrin, starch, wdg).
3.4 Viscosity mmezi
Enwere ike ịgwakọta viscosity dị iche iche nke HPMC dị ka oke dị iche iche si dị, na viscosity ya nwere ike ịgbanwe dịka iwu ụfọdụ siri dị, ma nwee mmekọrịta dị mma na linear, yabụ enwere ike họrọ oke dị ka achọrọ.
3.5 Metabolic inertia
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.
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 ubochi enweghi ihe ojoo nye mmadu.
4. Ngwa nke HPMC na nkwadebe
4.1 Dị ka ihe mkpuchi ihe nkiri na ihe na-emepụta ihe nkiri
N'iji hypromellose (HPMC) dị ka ihe mbadamba ihe nkiri na-ekpuchi ihe nkiri, ma e jiri ya tụnyere mbadamba omenala ndị dị ka mbadamba shuga, mbadamba nkume ndị a na-ekpuchi enweghị uru doro anya n'ikpuchi uto nke ọgwụ na ọdịdị ahụ, ma ha siri ike na friability , mmiri absorption. nkwụsịtụ, mkpuchi ibu ibu na ihe ngosi ndị ọzọ dị mma ka mma. A na-eji ọkwa dị ala 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 na-abụkarị 2.0% ruo 20%.
4.2 Dị ka ihe na-ekekọta ma na-agbasa
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, usoro onunu ogwu maka mbadamba granulation akọrọ bụ 5%, yana usoro onunu ogwu maka mbadamba ụrọ mmiri bụ 2%.
4.3 Dị ka onye na-akwụsịtụ
Onye na-ahụ maka nkwụsịtụ bụ ihe gel viscous nke nwere hydrophilicity, nke nwere ike belata ọsọ ọsọ nke sedimentation nke ihe ndị ahụ mgbe ejiri ya mee ihe na-eme ka ọ bụrụ ihe na-eme ka ọ dị n'elu ihe ahụ iji gbochie ihe ndị ahụ na-agbakọta ma na-adaba na bọlbụ. . Ndị ọrụ nkwụsịtụ na-ekere òkè dị mkpa n'ime nkwusioru. HPMC bụ ihe magburu onwe iche nke suspending elekọta mmadụ, na ya etisasịwo colloidal ngwọta nwere ike ibelata erughị ala nke mmiri mmiri siri ike interface na free ike na obere siri ike irighiri, si otú eme nkwụsi ike nke heterogeneous dispersion usoro. A na-eji ọkwa viscosity dị elu nke ngwaahịa a dị ka nkwadebe mmiri nkwusioru nke a kwadebere dị ka ihe nkwụsịtụ. Ọ nwere mmetụta nkwụsịtụ dị mma, ọ dị mfe ịgbasa, ọ naghị arapara n'ahụ mgbidi ahụ, ma nwee ezigbo flocculated particles. Usoro ọgwụgwọ mbụ bụ 0.5% ruo 1.5%.
4.4 Dị ka onye na-egbochi, onye na-ahapụ ya na onye na-akpata pore
A na-eji ọkwa viscosity dị elu nke ngwaahịa a iji kwadebe mbadamba nkume hydrophilic gel matrix na-adịgide adịgide, ndị na-egbochi ihe na-achịkwa maka mbadamba ihe matriks kwadoro-mwepu, ma nwee mmetụta nke igbu oge ntọhapụ ọgwụ. Nleta ojiji ya bụ 10% ~ 80% (W / W). A na-eji akara ngosi viscosity dị ala dị ka ihe na-emepụta pore maka nkwado ntọhapụ-adịgide ma ọ bụ njikwa-mwepu. Usoro mbụ achọrọ maka mmetụta ọgwụgwọ nke ụdị mbadamba nkume a nwere ike nweta ngwa ngwa, wee mee ka ntọhapụ na-adịgide adịgide ma ọ bụ na-achịkwa-ntọhapụ, na-anọgide na-ejigide ọgwụ ọgwụ ọbara dị irè n'ime ahụ. Mgbe hypromellose na-ezute mmiri, ọ na-eme ka ọ bụrụ oyi akwa gel. Usoro ntọhapụ ọgwụ sitere na mbadamba ihe matriks na-agụnyekarị mgbasa nke oyi akwa gel na mmebi nke oyi akwa gel.
4.5 Gluo nchekwa dị ka thickener na colloid
Mgbe ngwaahịa a na-eji dị ka a thickener, a na-ejikarị ịta bụ 0.45% ~ 1.0%. Ngwaahịa a nwekwara ike ịbawanye nkwụsi ike nke gluu hydrophobic, na-etolite colloid na-echebe, na-egbochi ụmụ irighiri ihe site na agglomerating na agglomerating, si otú a na-egbochi nhazi nke sedimenti, na ntinye ya na-emekarị bụ 0.5% ~ 1.5%.
4.6 Capsule ihe maka capsules
Ọtụtụ mgbe, ihe capsule shei capsule nke capsule na-adabere na gelatin. Usoro mmepụta nke shei capsule gelatin dị mfe, ma enwere ụfọdụ nsogbu na ihe ndị dị ka nchebe na-adịghị mma megide mmiri mmiri na ọgwụ ndị na-emetụ n'ahụ oxygen, ọnụego mgbasa ọgwụ dị ala, na nkwụsịtụ nke shea capsule na-egbu oge n'oge nchekwa. Ya mere, a na-eji hypromellose dochie anya capsules gelatin na nkwadebe nke capsules, nke na-eme ka nhazi na ojiji nke capsules dịkwuo mma, ma kwalitere ya n'ụlọ na ná mba ọzọ.
4.7 dị ka bioadhesive
Nkà na ụzụ bioadhesion, iji ihe ndị na-emepụta ihe na-emepụta ihe na-emepụta ihe na-emepụta ihe na-emepụta ihe na-emepụta ihe na-emepụta ihe na-emepụta ihe, site na ntinye aka na mucosa nke ndu, 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 ọgwụgwọ. A na-eji ya ugbu a n'ọtụtụ ebe A na-eji ya agwọ ọrịa nke oghere imi, ọnụ 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 eriri afọ, kamakwa na-eme ka arụ ọrụ kọntaktị dị n'etiti ọgwụ na akpụkpọ anụ ahụ na saịtị absorption, na-agbanwe mmiri nke akpụkpọ ahụ cell, mee ka ntinye nke ọgwụ ahụ dịkwuo mma na eriri afọ. sel epithelial, si otú a na-eme ka bioavailability nke ọgwụ ahụ dịkwuo mma.
4.8 Dị ka Gel
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. uzo.
Oge nzipu: Dec-15-2022