Gabapentin Tsuagyog cov tshuaj tiv thaiv tshuaj, uas tseem siv los kho neuralgia. Nws cov kev siv tshuaj ntau npaum li cas yog qhov ncauj tshuaj ntsiav lossis ntsiav tshuaj. Nws yog yooj yim nqus thiab ncav cuag peak concentration hauv 2 - 3 teev. Lub xyoob yog koob tshuaj - Nyob nrog, nrog ib qho ntawm qhov ncauj ntawm 300mg ua rau muaj 60%; Tab sis raws li cov koob tshuaj nce, cov xyoob ntoo ua tau tsawg dua. Gabapentin yog dav faib thoob plaws lub cev, tshwj xeeb hauv cov kab ntsig thiab lub raum. Cov tshuaj tsis yog metabolized nyob rau hauv lub cev thiab tau tawm hauv nws daim qauv qub los ntawm ob lub raum. Nws txoj kev ua yeeb yam yog ib feem ntawm kev tshem tawm tus nqi ntawm cov hauv. Qhov kev tshem tawm ib nrab-lub neej ntawm Gabapentin yog 5-7 teev. Hauv cov neeg mob uas muaj lub raum tsis txaus, lawv cov excretion tau qeeb thiab cov ntshav tawm cov protein zoo nkauj heev (<5%). When stopping the medication, it should be gradually reduced, at least within one week. Patients with renal insufficiency must reduce their dosage when taking medication. Patients treated with morphine at the same time may experience an increase in blood concentration of gabapentin, and should be carefully observed for central nervous system suppression such as drowsiness, and the dosage should be appropriately reduced.
Cov ntaub ntawv ntxiv ntawm kev sib txuas lus:
|
|
|
Gabapentin CO
 |
|
|
|
|
Lub tshuab tshuaj ntsuab mucosal ntawm gabapentin tsuag ntawm Chitosan alginate muaj nanoparticles
Gabapentin Tsuag, raws li cov tshuaj tiv thaiv dav siv, tau qhia qhov ua tau zoo rau kev kho mob ntawm neuropathic mob thiab kev kho mob sib txawv rau ib nrab uas qaug cawv. Txawm li cas los xij, cov khoom noj tshuaj haus dej ib txwm muaj kev sib tw ua ntej, thiab siv cov roj ntsha tsis muaj zog, thiab siv lawv cov khoom siv tsis muaj zog, uas txwv lawv cov bioavailability. Nyob rau hauv xyoo tsis ntev los no, tsis muaj qhov tso tshuaj noj tshuaj ntsuab, tau dhau los ua qhov kev tshawb fawb tshuaj ntsuab vim lawv muaj peev xwm ua kom tsis txhob ua ntej kev tshawb fawb, thiab txhim kho kev ua raws li kev ua raws. Chitosan alginate muaj cov nanoparticles, raws li kev hloov tshuaj tshiab rau cov tshuaj ntsuab vim lawv cov tshuaj nplaum zoo, thiab cov yam ntxwv tso tawm.
Kev npaj thiab cov yam ntxwv ntawm chitosan alginate muaj nanoparticles
Tshuaj lom neeg ntawm Chitosan thiab Alginate
Chitosan yog lub ntuj cationic polysaccharide tau los ntawm Deacetylation ntawm Chitin. Cov amino pab pawg ({- nh ₂) ntawm nws cov molecular ntawm nws cov min}} nh α⁺ nyob rau hauv acidic tej yam kev mob, muab nws tus nqi zoo. Alginic acid yog anionic polysaccharide extracted los ntawm xim av algae, muaj}}}}}}} thiab-li kev sib txuas acid (g) glycosidic bonds. Alginate (xws li sodium alginate) tuaj yeem tsim cov qauv gel hauv lub xub ntiag ntawm cov calcium |), uas yog p rhiab (acidral / alkaline qhov kawg).
Kev npaj txoj kev ntawm composite nanoparticles
Chitosan alginate composite nanoparticles feem ntau yog npaj los ntawm ion gel txoj kev lossis tus kheej {{} kev sib dhos txoj kev:
Ion Gel Txoj Kev: Tom qab sib xyaw Chitosan tov thiab sodium alginate daws, hla ² +) yog ntxiv rau daim ntawv nanoparticatic sib txuas lus. PHOTHATHE ION IN TPP khi nrog amino pab pawg ntawm Chitosan los ua tus ntoo khaub lig ruaj khov}}}}}}}}}}} Txuas cov qauv.
Txoj Kev Sib Tham Tus Kheej: Siv cov kev sib txuas lus sib xyaw ntawm Chitosan thiab Alginate, xws li hydrophobic sib txuas lus, mus rau nteg ntom nanoparticles.
Cov yam ntxwv ntawm composite nanoparticles
Qhov loj me me thiab morphology: qhov me me ntawm cov neeg nanoparticles nanoparticles feem ntau ntawm 100-300 nm, kheej kheej, nrog ib qho chaw du thiab zoo dispersibility.
Zeta muaj peev xwm: tus nqi zoo ntawm Chitosan thiab tus nqi tsis zoo ntawm cov hluav taws xob muaj txiaj ntsig los ntawm kev sib sau ua ke nrog mucin thiab txhim kho kev nkag mus rau lub peev xwm.
Encapsulation efficiency and drug loading: By optimizing the preparation process (such as the ratio of chitosan to alginate, crosslinking agent concentration), high encapsulation efficiency (>80%) and high drug loading (>40%) ntawmGabapentin Tsuagtuaj yeem ua tiav.
Phemitivity: alginate gel yog ruaj khov nyob rau hauv acidic ib puag ncig thiab dissolves nyob rau hauv nruab nrab nruab nrab / alkaline ib puag ncig, uas tuaj yeem paub cov tshuaj tso tawm hauv cov hnyuv lossis mucosa.
Qauv thiab cov yam ntxwv ntawm lub cev ntawm qhov ncauj mucosa
Cov qauv kev ua haujlwm ntawm qhov ncauj mucosa
Qhov ncauj Mucosa yog tsim los ntawm txheej epithelial, Lamina propria, thiab subcucosal txheej
Cov txheej epithelial: unkeratinized stratified squamous squamous squamous, nrog ib thickness ntawm kwv yees li 500-800 μ m thiab ib lub sij hawm ntawm daim tawv nqaij. Epithelial hlwb tsim lub cev lub cev los ntawm kev sib tw, thiab cov tshuaj tuaj yeem nkag mus rau hauv lub cev los ntawm kev hloov ntshav lossis cov txheej txheem paracellular.
Kev txais cov txheej txheem: tsim los ntawm cov hlab ncauj sib txuas, cov hlab ntsha muaj zog, cov tshuaj sib xyaw ua ke thiab kev cuam tshuam ncaj qha ntawm txoj hlab ntshav ntawm lub cev, zam kev cuam tshuam thawj zaug.
Shipsged cov txheej: cov xoob txuas cov ntaub so ntswg muaj cov qog thiab cov ntaub so ntswg ua kom zoo, muab kev pab txhawb kev kho mob rau kev siv tshuaj.
Ib puag ncig physiological ntawm qhov ncauj mucosa
PE Nqi: Tus nqi PHIC yog 6.2-7.6, uas tsis muaj zog alkaline thiab muaj txiaj ntsig rau kev ruaj ntseg ntawm Chitosan alginate muaj cov nanoparticles.
Enzyme kev ua: qaub ncaug muaj ib qho me me ntawm cov amylase thiab protease, tab sis muaj tsis muaj zog depradation teebmeem ntawm Chitosan thiab Alginate.
Qaub kib zais cia: Thaum so, cov qaub ncaug zais cia yog 0.5-1.5 L / d, nrog tus nqi txaus ntawm 0.3-0.5 ML / Min, uas yuav ua rau cov tshuaj kho kom huv.
Qhov Zoo Ntawm Qhov Ncauj Tshuaj Xyuas Kev Nyab Xeeb Qhov ncauj
Zam kev cuam tshuam thawj zaug: cov tshuaj tau kaw ncaj qha mus rau hauv cov kab ncig ntawm lub cev los ntawm cov mucosa, txo lawv cov bioavailability.
Pib pib: Qeeb zog ntau tshaj plaws hauv qab lub mucosa txhawb kev nqus tshuaj sai sai, ua rau nws haum rau kev kho mob ntawm kev mob hnyav.
Cov neeg mob siab: cov tshuaj tsuag yog yooj yim siv, tshwj xeeb yog tsim nyog rau menyuam yaus, cov neeg laus lossis cov neeg mob uas muaj dysphagia.
Cov tshuaj ntsuab mucosal ntawm chitosan alginate muaj nanoparticles
Cov txuj ci nplaum
Cov tshuaj nplaum hauv qab, xws li hydrogen tsev (xws li kev sib txuas lus hluav taws xob, uas tau cog lus ntawm cov tshuaj khaws cia hauv cov tshuaj hauv cov mucosal. Adhesion mechanism ntawm Chitosan asosite nanoparticles tsuas yog suav nrog cov tswv yim nram qab no:
Kev Lag Luam Hluav Taws Xob: Cov pab pawg amino ntawm Chitosan khi rau sialic acid seem (tsis zoo ntawm cov tshuaj tua hluav taws xob.
Diffusion Theory: Chitosan molecular chains nkag mus rau hauv mucosal mucus txheej thiab ua hydrophobic sib cuam tshuam nrog molin lwg me me.
Adsorption Theory: Cov saum npoo ntawm nanoparticles Adsorbs mus rau mucosal nto los ntawm van der waquals rog lossis hydrophobic sib tham.
Lub cev qhuav dej: Thaum Nanoparticles nkag mus rau hauv Mucosa, dej tau raug ntiab tawm, sib sau cov cheeb tsam polymer muaj zog uas txhawb nqa Adhesion.
Cov nyhuv nplaum ntawm Chitosan
Chitosan yog lub ntsiab lus nplaum tseem ceeb ntawm kev sib xyaw ua ke nanoparticles, thiab nws cov adhesion tshuab muaj xws li:
Kev Sib Tham Hauv Hluav Taws Xob: Kev Sib Tham Sib Tham:- α⁺ ntawm Chitosan khi nrog cov quav tsis zoo (xws li sialic acid thiab mucin) los ua cov nplaum ruaj khov txheej.
Hydrogen Bonding Tsim: lub hydroxyl ({{}} oh}}} {}} cooh) thiab cov pab pawg hydroxyl ntawm Mucin.
Cov tshuaj ntsuab mucosal thaiv: Chitosan tuaj yeem ua kom lub focalas kinase (FAK) thiab Tyrosine Kinase scentaling pathwer, thiab kev txhawb nqa cov nyom ntawm cov roj ntsha, thiab txhawb kev nkag tshuaj nkag.
Cov Khoom Tseem Ceeb Technologies
Synergistic nyhuv ntawm alginate
Alginate txhim kho cov nplaum muaj cov khoom siv ntawm cov tshuaj ntsuab nanoparticles los ntawm cov txheej txheem nram qab no:
Gel network tsim: alginate thiab CA ² + crosslink los tsim cov gel network, uas nce cov mechanical network, uas nce cov tshuab zog ntawm nanoparticles thiab tiv thaiv cov qaub ncaug ntxuav.
Phemitivity: nyob rau hauv ib puag ncig / alkaline ib puag ncig, alginate gel dissolves, tso tshuaj yeeb thaum tuav cov nplaum ntawm nanoparticles.
Biocompatibility: alginate tuaj yeem txo cov cytotoxicity ntawm Chitosan thiab txhim kho kev ua haujlwm mucosal.
Adhesion Kinetics ntawm Composite Nanoparticles
Cov txheej txheem nplaum ntawm cov tshuaj ntsuab nanoparticles yuav muab faib ua peb theem:
Kev ntub dej theem: Nanoparticles nkag mus rau hauv cov mucosal nto, dej yog ntiab tawm, thiab cov nplaum ua ntej tsim.
Cov theem nkag mus: Chitosan molecular chains nkag mus rau hauv cov hnoos qeev txheej, ua cov kev sib cuam tshuam hydrogen thiab hluav taws xob nrog cov mucin.
Kev kho cov theem: Alginate Gel network yog tsim los txhim kho adhesion lub zog thiab ruaj khov.
Tso mechanism ntawm Gabapentin nyob rau hauv composite nanoparticles
Tshuaj Yeeb Tshuaj Yeeb Kinetics
Kev tso tawmGabapentin TsuagLos ntawm Chitosan alginate muaj cov nanoparticles ua raws cov cuab yeej hauv qab no:
Diffusion Mechanism: cov tshuaj diffuses mus rau hauv nruab nrab nruab nrab los ntawm cov kab ke lossis gel network ntawm cov nanoparticles.
Kev rho tawm mechanism: Chitosan thiab Alginate maj mam tsis tau nyob hauv Vivo ib puag ncig, thiab cov tshuaj raug tso tawm raws li tus cab kuj ploj mus.
Ion Txauv Mechanism: Hauv ib qho chaw muaj sia nyob hauv Anions, {{}} х emoparticle o los yog kev sib cais thiab tso yeeb tshuaj.
Tso cov yam ntxwv nkhaus
Kev tso tawm nkhaus ntawm cov tshuaj nanoparticles feem ntau yog cov yam ntxwv biphasicic:
Thawj zaug tawg tawm: cov tshuaj adsorbed nyob rau saum npoo ntawm nanoparticle tau tawm sai heev (0-2 teev), muab cov kev kho thawj zaug.
Nruam kev tawm tswv yim: maj mam tso cov tshuaj los ntawm diffusion thiab xaus keyolution kev sib cais (2-24 teev) kom muaj kev haus tshuaj yeeb tshuaj zoo.
Yam cuam tshuam rau kev tso tawm
Nanoparticle loj: Qhov me me qhov me me qhov loj me, qhov loj dua qhov chaw tshwj xeeb thaj tsam, thiab tus nqi tso tawm sai dua.
Qhov piv txwv ntawm Chitosan rau Alginate: qhov siab dua cov ntsiab lus Chitosan, tus muaj zog ntawm cov nplaum, tab sis nws yuav txo cov tshuaj tso tawm tshuaj.
Crosslinking tus neeg sawv cev muaj peev xwm: Qhov nce hauv Crosslinking tus neeg sawv cev tuaj yeem txhim kho cov mechanical zog ntawm cov nanoparticles, tab sis tej zaum yuav yog tshuaj tso yeeb tshuaj.
P tus nqi: alginate gel yog ruaj khov nyob rau acidic ib puag ncig, thiab tso yeeb tshuaj qeeb; Lub gel yaj nyob rau hauv nruab nrab / alkaline ib puag ncig, thiab cov tshuaj tso tawm yog nrawm.
Cim npe nrov: Gabapentin Tsuag, Cov Khoom Siv, Chaw Tsim Tshuaj, Hoobkas, Lag Luam Wholesale, Yuav, Nqe, Hlua, Rau Muag