Ihe ọmụma
Trimethoprim ntụ ntụ bụ ọgwụ nje a na-ejikarị agwọ ọrịa nje dị iche iche. Ya lipophilicity, ma ọ bụ ikike igbari na abụba na mmanụ, bụ ihe dị mkpa e ji mara na-emetụta otú ọgwụ na-akpa àgwà n'ime ahụ. Ịghọta ọdịdị lipophilic nke trimethoprim ntụ ntụ nwere ike inye nghọta na ntinye ya, nkesa, na n'ozuzu ya dị ka ọgwụ. Ka anyị nyochaa isiokwu a nke ọma ma zaa ajụjụ ụfọdụ metụtara ya.
Kedu ihe na-emetụta trimethoprim ntụ ntụ solubility?
Trimethoprim powder's solubility na-emetụta ọtụtụ ihe, nke n'aka nke ya na-emetụta lipophilicity ya na omume zuru ezu na usoro ọgwụ na ahụ mmadụ. Ịghọta ihe ndị a dị oke mkpa maka ịkwalite nnyefe ọgwụ na ịdị irè.
Otu n'ime isi ihe na-emetụta trimethoprim ntụ ntụ solubility bụ pH. Trimethoprim bụ ntọala adịghị ike nke nwere pKa nke ihe dịka 7.2. Nke a pụtara na solubility ya na-adabere na pH, nke nwere oke solubility na gburugburu acidic na ala solubility na ọnọdụ alkaline. Na gburugburu acidic nke afọ (pH 1-3), trimethoprim na-agbaze karịa ma na-etinye ya ngwa ngwa. Otú ọ dị, ka ọ na-esi na tract gastrointestinal na-aga n'ihu na mpaghara alkaline, ike ya na-ebelata.
Okpomọkụ na-ekerekwa òkè na trimethoprim ntụ ntụ solubility. N'ozuzu, ka okpomọkụ na-abawanye, solubility nke ọtụtụ ihe siri ike na ihe mgbaze mmiri na-abawanye. Ụkpụrụ a na-emetụtakwa trimethoprim, ọ bụ ezie na mmetụta ahụ nwere ike ịdị ntakịrị ma e jiri ya tụnyere ụfọdụ ogige ndị ọzọ. Ịghọta mmekọrịta okpomọkụ-solubility dị mkpa maka ndị ọkà mmụta sayensị mmepụta ihe mgbe ha na-emepụta ụdị usoro ọgwụgwọ mmiri ma ọ bụ na-atụle ọnọdụ nchekwa maka ngwaahịa nwere trimethoprim.
Ọnụnọ nke ihe ndị ọzọ ma ọ bụ ihe mgbakwunye na nhazi nwere ike imetụta nke ukwuu trimethoprim ntụ ntụ solubility. Dịka ọmụmaatụ, enwere ike iji ụfọdụ ihe na-eme ka ahụ sie ike ma ọ bụ surfactants iji kwalite solubility nke trimethoprim na mgbasa ozi mmiri. N'aka nke ọzọ, ọnụnọ nke ion ma ọ bụ ogige ndị ọzọ nwere ike iduga n'ịmepụta ogige ma ọ bụ nnu nke nwere ike gbanwee profaịlụ solubility trimethoprim.
Oke urughuru bụ ihe ọzọ dị oke egwu na-emetụta solubility. Nta urughuru nha n'ozuzu na-eduga na ụba elu ebe, nke nwere ike welie mgbasa udu na mkpokọta solubility. Nke a dị mkpa karịsịa maka ọgwụ ndị na-adịghị mma sobe ya dị ka trimethoprim, ebe enwere ike iji micronization ma ọ bụ usoro mbelata nha nha nha ndị ọzọ iji melite bioavailability.
Nhọrọ nke usoro ihe mgbaze na-emetụtakwa trimethoprim ntụ ntụ solubility. Ọ bụ ezie na trimethoprim nwere oke solubility na mmiri (ihe dị ka 400 mg / L na 25 Celsius C), ọ na-agbaze karịa na ihe mgbaze organic dị ka ethanol ma ọ bụ dimethyl sulfoxide (DMSO). Ihe onwunwe a metụtara ọdịdị lipophilic ya ma nwee ike itinye ya na ngwa ọgwụ dị iche iche.
Ịghọta ihe ndị a na mmekọrịta ha dị oke mkpa maka ndị ọkà mmụta sayensị ọgwụ na ndị na-ahụ maka ụlọ ọgwụ. Site n'ịgbanwe mgbanwe ndị a, ọ ga-ekwe omume ịkwalite usoro trimethoprim maka nkwalite solubility, nkwụsi ike, na n'ikpeazụ, nrụpụta ọgwụgwọ.
Kedu ka trimethoprim ntụ ntụ lipophilicity si emetụta nnabata ya?
The lipophilicity nke trimethoprim ntụ ntụ na-arụ ọrụ dị oke mkpa na nnabata ya na ọgwụ ọgwụ n'ozuzu ya. Lipophilicity na-ezo aka n'ikike nke ngwakọta ịgbaze na abụba, mmanụ, na ihe mgbaze na-abụghị polar. N'ihe banyere trimethoprim, lipophilicity ya na-agafeghị oke na-emetụta nke ọma ka o si emekọrịta ihe na akpụkpọ anụ dị ndụ ma kesaa n'ime ahụ dum.
Ọdịdị lipophilic nke Trimethoprim na-enye ya ohere ịgafe ngwa ngwa nke akpụkpọ anụ dị ndụ, gụnyere epithelium eriri afọ. Ngwongwo a na-enye aka na bioavailability ọnụ ya dị elu, nke na-adịkarị gburugburu 60-80%. Mgbe a na-ekwu okwu, trimethoprim nwere ike ịgafe n'ụzọ dị mfe site na lipid bilayers nke sel eriri afọ, na-eme ka ọ banye n'ọbara. Mmụba nke ọma a bụ otu n'ime ihe kpatara trimethoprim ji arụ ọrụ dị ka ọgwụ mgbochi ọnụ.
lipophilicity nke trimethoprim na-emetụtakwa nkesa ya na ahụ. Ozugbo etinyere ya, trimethoprim nwere ike banye n'ime anụ ahụ dị iche iche na mmiri nke anụ ahụ n'ihi ikike ọ nwere ịgafe akpụkpọ anụ. Nkesa sara mbara a bara uru karịsịa maka ịgwọ ọrịa n'akụkụ dị iche iche nke ahụ, gụnyere urinary tract, akụkụ iku ume, na ọbụna usoro nhụjuanya etiti ruo n'ókè ụfọdụ.
Otú ọ dị, ọ dị mkpa iburu n'obi na ebe lipophilicity na-eme ka mmịnye na ntinye anụ ahụ dịkwuo elu, ọ pụkwara iduga n'ịba ụba protein. Trimethoprim bụ ihe dịka 40-70% jikọtara ya na protein plasma, nke nwere ike imetụta itinye uche ya n'efu n'ime ọbara yana, ya mere, ọrụ antimicrobial.
Nhazi n'etiti hydrophilicity na lipophilicity dị oke mkpa maka ịrụ ọrụ ọgwụ kacha mma. lipophilicity na-agafeghị oke nke Trimethoprim na-enye ya ohere idobe nguzozi n'etiti nnabata dị mma na solubility mmiri zuru oke, nke dị mkpa maka ikesa n'ime mmiri mmiri na-ekpo ọkụ na n'ikpeazụ.
Ịghọta mmekọrịta dị n'etiti trimethoprim's lipophilicity na nnabata ya dị mkpa maka ndị dọkịta mgbe ị na-atụle usoro doses na mmekọrịta ọgwụ nwere ike. Dịka ọmụmaatụ, ọgwụ lipophilic nke ukwuu nwere ike ịsọ mpi trimethoprim maka saịtị njikọ protein, nwere ike gbanwee itinye uche ya na arụmọrụ ya n'efu.
Ndị ọkà mmụta sayensị na-emepụta ọgwụ na-etinyekwa ihe ọmụma a iji mepụta usoro trimethoprim ka mma. Site n'iji lipophilicity nke ọgwụ ahụ eme ihe site na usoro nhazi dị iche iche, ọ ga-ekwe omume ịkwalite nnabata ya ma ọ bụ gbanwee profaịlụ ntọhapụ ya. Dịka ọmụmaatụ, sistemụ nnyefe ọgwụ ma ọ bụ nanoformulation nwere ike inyocha lipid iji kwalite bioavailability trimethoprim ma ọ bụ lekwasịrị anya n'anụ ahụ.
Ọzọkwa, lipophilicity nke trimethoprim na-emetụta ikike ya ịgafe mgbochi ụbụrụ ọbara. Ebe trimethoprim na-abanye n'ime sistemu ụjọ nke etiti ruo n'ókè ụfọdụ, itinye uche ya na mmiri cerebrospinal na-adịkarị ala karịa na plasma. Ngwongwo a bara uru mgbe ị na-atụle trimethoprim maka ọgwụgwọ ụfọdụ ụdị meningitis ma ọ bụ ọrịa sistemu ụjọ etiti ndị ọzọ.
Na nchịkọta, lipophilicity nke trimethoprim ntụ ntụ na-emetụta mmịnye ya nke ukwuu site n'ịkwado ebe ọ gafefe membranes ndu. Ngwongwo a na-enye aka na bioavailability ọnụ ya dị elu, nkesa anụ ahụ sara mbara, yana ịdị irè n'ozuzu ya dị ka ọgwụ nje. Ịghọta akụkụ pharmacokinetic ndị a dị oke mkpa maka ịkwalite ojiji ọgwụgwọ trimethoprim na ịmepụta usoro dị mma maka ngwa ụlọ ọgwụ dị iche iche.
Enwere ike iji ntụ ntụ trimethoprim mee ihe na usoro nnyefe ọgwụ na-adabere na lipid?
Enwere ike iji trimethoprim ntụ ntụ mee ihe na usoro nnyefe ọgwụ na-adabere na lipid bụ mpaghara na-adọrọ mmasị nke nchọpụta ọgwụ na-eme ka ihe ndị dị na lipophilic ọgwụ ahụ na-eme ihe. Usoro nnyefe ọgwụ na-adabere na lipid (LBDDS) enwetawo nlebara anya dị ukwuu n'afọ ndị na-adịbeghị anya dị ka atụmatụ iji kwalite bioavailability nke ọgwụ ndị na-adịghị edozi mmiri na-adịghị mma ma melite arụmọrụ ọgwụgwọ ha n'ozuzu ya. Nyere trimethoprim lipophilicity agafeghị oke, inyocha ntinye ya na sistemu ndị dị otú ahụ nwere ike inye ọtụtụ uru.
Usoro nnyefe ọgwụ egbugbere ọnụ na-agụnye ọtụtụ usoro, gụnyere ngwọta lipid, emulsions, usoro nnyefe ọgwụ na-eme onwe ya (SEDDS), na SLNs siri ike. Usoro ndị a nwere ike ịkwalite solubility na nnabata nke ọgwụ lipophilic dị ka trimethoprim site n'iweta ọgwụ ahụ n'ụdị edozichara ma ọ bụ site n'ịkwado ya solubilization na eriri afọ.
Otu n'ime uru ndị bụ isi nke iji trimethoprim ntụ ntụ na LBDDS nwere ike ime ka enwewanye bioavailability ọnụ. Ọ bụ ezie na trimethoprim enweelarị bioavailability dị mma nke ọnụ, ụfọdụ ndị ọrịa ma ọ bụ ihe achọrọ maka imepụta nwere ike irite uru site na nkwalite ọzọ. Site n'itinye trimethoprim n'ime ndị na-ebu lipid, ọ ga-ekwe omume ịgafe ụfọdụ usoro mgbasa nke achọrọ maka ụdị usoro onunu ogwu siri ike, nke nwere ike ibute nnabata ngwa ngwa na nke na-agbanwe agbanwe.
SEDDS, karịsịa, nwere ike ịbụ ụzọ na-adọrọ mmasị maka nnyefe trimethoprim. Usoro ndị a na-agụnye ngwakọta nke mmanụ, surfactants, na mgbe ụfọdụ ndị na-emekọ ihe na-emepụta mmanụ n'ime mmiri n'otu oge na-ejikọta ya na mgbasa ozi mmiri, dị ka mmiri mmiri eriri afọ. Site n'ịmepụta trimethoprim na SEDDS, ọ ga-ekwe omume ịnye ọgwụ ahụ n'ụdị solubilized, dị njikere maka nnabata. Nke a nwere ike ịba uru karịsịa maka ndị ọrịa nwere ọrụ eriri afọ na-emebi emebi ma ọ bụ ndị na-aṅụ ọgwụ ndị nwere ike imetụta solubility trimethoprim.
Ngwa ọzọ nwere ike nke LBDDS maka trimethoprim bụ n'ịmepụta usoro ntọhapụ a na-achịkwa. Site na itinye trimethoprim na lipid matrices ma ọ bụ ndị na-ebu lipid nanostructured, ọ ga-ekwe omume ịmegharị profaịlụ ntọhapụ ya, nwere ike inye ohere maka obere doses ugboro ugboro yana kwalite nnabata onye ọrịa. Usoro a nwere ike ịba uru karịsịa maka ọgwụgwọ ọgwụ nje na-adịte aka ma ọ bụ iji prophylactic mee ihe.
Sistemu dabere na lipid nwekwara ike inye uru n'ihe nkwụsi ike na ndụ nchekwa. Site na ichekwa trimethoprim pụọ na ihe mmebi dị ka ọkụ ma ọ bụ mmiri mmiri, usoro ndị a nwere ike ịgbatị ogologo ndụ ọgwụ ma ọ bụ nye ohere maka ọnọdụ nchekwa ọhụrụ.
Agbanyeghị, mmepe LBDDS maka trimethoprim abụghị ihe ịma aka. Nhọrọ nke ihe mgbakwunye lipid kwesịrị ekwesị, njikarịcha nhazi nhazi, yana ịhụ na ndakọrịta na akụrụngwa physicochemical nke trimethoprim bụ ihe niile dị oke egwu chọrọ nlebara anya nke ọma. Na mgbakwunye, mmetụta nke usoro dabere na lipid na trimethoprim's pharmacokinetics na pharmacodynamics ga-adị mkpa ka enyocha nke ọma iji hụ na a na-edobe ma ọ bụ kwalite nrụpụta antimicrobial.
Ntụle usoro iwu dịkwa mkpa mgbe ị na-emepụta usoro nke ọgwụ ndị emebere ka trimethoprim dabere na lipid. Ọ bụ ezie na ihe a na-arụ ọrụ bụ nke a maara nke ọma, usoro ọhụrụ nwere ike ịchọ nchebe ọzọ na nchọpụta arụmọrụ iji nweta nkwenye nchịkwa.
Site n'echiche nrụpụta, mmepụta nke LBDDS nwere ike ịdị mgbagwoju anya karịa ụdị usoro onunu ogwu siri ike. Enwere ike ịchọ akụrụngwa na usoro pụrụ iche, nke nwere ike imetụta ọnụ ahịa nke usoro ndị dị otú ahụ. Otú ọ dị, ọ bụrụ na enwere ike igosipụta uru ọgwụgwọ dị ịrịba ama, ihe ịma aka ndị a nwere ike ịkawanye mma site na mmụba nwere ike na nsonaazụ onye ọrịa.
N'ikpeazụ, ojiji nke trimethoprim ntụ ntụ n'ime usoro nnyefe ọgwụ na-adabere na lipid na-enye ohere na-atọ ụtọ maka mmepụta ọgwụ ọhụrụ. Site n'iji trimethoprim's lipophilic Properties, usoro ndị a dị elu nwere ike ịnye nkwalite bioavailability, profaịlụ ntọhapụ emegharịrị, yana nkwụsi ike. Ọ bụ ezie na ihe ịma aka dị na ịmepụta na ịmepụta usoro ndị dị otú ahụ, uru ndị nwere ike ime n'ihe gbasara ọgwụgwọ ọgwụgwọ na nnabata ndị ọrịa na-eme ka mpaghara a bụrụ ebe kwesịrị ekwesị maka nyocha na mmepe ọzọ.
Ọ bụrụ na ị nwekwara mmasị na ngwaahịa a ma chọọ ịmatakwu nkọwa ngwaahịa, ma ọ bụ chọọ ịmata maka ngwaahịa ndị ọzọ metụtara, biko nweere onwe gị ịkpọtụrụ. iceyqiang@aliyun.com.
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