Suugaanta la xidhiidha gudaha iyo dibaddaba ee diyaarinta dawooyinka dawooyinka hydroxypropyl methylcellulose (HPMC) sannadihii la soo dhaafay ayaa dib loo eegay, la falanqeeyay oo la soo koobay, iyo codsigeeda diyaarinta adag, diyaarinta dareeraha, diyaarinta sii-deynta joogtada ah iyo xakamaynta, diyaarinta kaabsulka, gelatin The latest Codsiyada goobta qaab-dhismeedka cusub sida qaabaynta xabagta iyo bioadhesives. Sababtoo ah farqiga u dhexeeya miisaanka kelli qaraabo iyo viscosity of HPMC, waxa ay leedahay sifooyinka iyo isticmaalka emulsification, adhesion, dhumucdiisuna, viscosity kordhaysa, laalista, gelling iyo samaynta filimada. Waxaa si weyn loogu isticmaalaa diyaarinta dawooyinka waxayna door weyn ka ciyaari doontaa goobta diyaarinta. Daraasad qoto dheer oo ku saabsan hantideeda iyo hagaajinta tignoolajiyada qaabeynta, HPMC ayaa si weyn loogu isticmaali doonaa cilmi baarista foomamka qiyaasta cusub iyo nidaamyada cusub ee gudbinta daroogada, taas oo kor u qaadeysa horumarka joogtada ah ee qaabaynta.
hydroxypropyl methylcellulose; diyaarinta dawooyinka; dawooyinka loo isticmaalo.
Qalabka dawooyinka ma aha oo kaliya saldhigga alaabta ee samaynta diyaargarowga daroogada cayriin, laakiin sidoo kale waxay la xiriirtaa dhibka habka diyaarinta, tayada daroogada, xasiloonida, badbaadada, heerka sii deynta daroogada, qaabka ficilka, waxtarka bukaan-socodka, iyo horumarinta cusub qaababka qiyaasta iyo waddooyinka cusub ee maamulka. xiriir dhow. Soo bixitaanka dawooyinka cusub ee dawooyinka ayaa inta badan kor u qaada hagaajinta tayada diyaarinta iyo horumarinta qaababka cusub ee qiyaasta. Hydroxypropyl methylcellulose (HPMC) waa mid ka mid ah dawooyinka ugu caansan gudaha iyo dibaddaba. Sababo la xiriira miisaankiisa molecular ee kala duwan iyo viscosity, waxa ay leedahay hawlaha emulsifying, xidhitaan, dhumuc, dhumuc, laalid, iyo koollada. Tilmaamaha iyo isticmaalka sida xinjirowga iyo sameynta filimada ayaa si weyn loogu isticmaalaa tignoolajiyada daawada. Maqaalkani wuxuu inta badan dib-u-eegayaa codsiga hydroxypropyl methylcellulose (HPMC) ee qaabaynta sannadihii ugu dambeeyay.
1.Tilmaamaha aasaasiga ah ee HPMC
Hydroxypropyl methyl cellulose (HPMC), qaacidada kelli waa C8H15O8-(C10 H18O6) n-C8H15O8, iyo cufnaanta molecular ee ku saabsan 86 000. Alaabta Tani waa wax semi-synthetic ah, taas oo qayb ka ah methyl iyo qayb ka mid ah polyhydroxypropyl ether. ee cellulose. Waxaa loo soo saari karaa laba siyaabood: Mid waa in methyl cellulose ee darajada ku habboon lagu daaweeyaa NaOH ka dibna lagu falceliyo propylene oxide heerkul sare iyo cadaadis sare. Waqtiga falcelinta waa in uu sii jiraa muddo dheer oo ku filan si uu u oggolaado methyl iyo hydroxypropyl si ay u sameeyaan ether bonds Waxay ku xiran tahay giraanta anhydroglucose ee cellulose ee qaabka cellulose, waxayna gaari kartaa heerka la rabo; Midda kale waa in lagu daaweeyaa suufka suufka ah ama alwaax ka sameysan soodhaha caustic soodhaha ah, ka dibna lagu falceliyo methane koloriin leh iyo propylene oxide si isdaba joog ah, ka dibna loo sii sifeeyo. , la jajabiyey oo laga dhigay budo ama granulos.
Midabka alaabtani waa cadaan ilaa caano caano ah, aan ur lahayn oo aan dhadhamin, qaabkuna waa budo si fudud u qulqulaya granular ama fiber. Alaabtan waxa lagu milmi karaa biyo si ay u sameeyaan xal kolloidal cad oo cad ama caano leh oo leh muuqaal gaar ah. Dhacdada is-weydaarsiga sol-gel waxay ku dhici kartaa isbeddelka heerkulka xalka oo leh xoogaa xoogaa ah.
Sababtoo ah farqiga u dhexeeya nuxurka labadan beddelka ah ee qaabka methoxy iyo hydroxypropyl, noocyo kala duwan oo alaab ah ayaa soo muuqday. Qaybo gaar ah, noocyada kala duwan ee alaabadu waxay leeyihiin sifooyin gaar ah. Viscosity iyo heerkulka gelation kulaylka, sidaas darteed waxay leeyihiin sifooyin kala duwan waxaana loo isticmaali karaa ujeedooyin kala duwan. Pharmacopoeia ee dalal kala duwan waxay leedahay xeerar kala duwan iyo matalaad ku saabsan qaabka: Pharmacopoeia Yurub waxay ku saleysan tahay darajooyinka kala duwan ee viscosities kala duwan iyo heerarka kala duwan ee beddelka alaabta lagu iibiyo suuqa, oo lagu muujiyay darajooyin lagu daray tirooyin, iyo cutubku waa "mPa s ”. Gudaha Maraykanka Pharmacopoeia, 4 nambar ayaa lagu daraa magaca guud ka dib si loo muujiyo nuxurka iyo nooca beddelka kasta ee hydroxypropyl methylcellulose, sida hydroxypropyl methylcellulose 2208. Labada lambar ee ugu horreeya waxay matalaan qiyaasta qiyaasta kooxda methoxy. Boqolkiiba, labada lambar ee ugu dambeeya waxay matalaan boqolkiiba qiyaastii hydroxypropyl.
Calocan's hydroxypropyl methylcellulose wuxuu leeyahay 3 taxane, oo kala ah taxanaha E, taxanaha F iyo taxanaha K, taxane kastaa wuxuu leeyahay noocyo kala duwan oo noocyo ah oo laga soo xusho. Taxanaha E waxaa inta badan loo isticmaalaa sida dahaarka filimada, loo isticmaalo dahaadhka kiniinka, koofiyadaha kiniinka xiran; Taxanaha E, F waxa loo istcimaalaa sidii viskosifiers iyo sii daaya wakiilada dib u dhigista ee diyaarinta indhaha, wakiilada hakinta, dhumucyada diyaarinta dareeraha, kiniiniyada iyo xidhayaasha granules; Taxanaha K waxaa inta badan loo isticmaalaa sidii horjoogayaasha sii daynta iyo agabka matrixka gel hydrophilic si loo sii daayo gaabis ah oo la xakameeyey.
Soosaarayaasha gudaha inta badan waxaa ka mid ah Fuzhou No. 2 Kiimikada Warshadaha, Huzhou Food iyo Kiimikada Co., Ltd., Sichuan Luzhou Qalabka Dawada, Warshada Kiimikada Hubei Jinxian No. 1, Feicheng Ruitai Fine Chemical Co., Ltd., Shandong Liaocheng Ahua Co. ., Ltd., Xi'an Huian dhirta kiimikada, iwm.
2.Faa'iidooyinka HPMC
HPMC waxa ay noqotay mid ka mid ah dawooyinka aadka looga isticmaalo gudaha iyo dibaddaba,sababta oo ah HPMC waxa ay leedahay faa'iidooyin aanay lahayn dawooyinka kale.
2.1 Biyo qabow
Ku milmay biyo qabow oo ka hooseeya 40 ℃ ama 70% ethanol, asal ahaan aan lagu milmi karin biyaha kulul ee ka sarreeya 60 ℃, laakiin way geli karaan.
2.2 Kiimiko ahaan aan shaqaynayn
HPMC waa nooc ka mid ah ether-ka cellulose-ka aan-ionic-ka ahayn, xalkeedu ma laha lacag ionic ah oo aan la falgelin cusbada birta ama xeryahooda organic ionic, sidaas darteed walxaha kale kama falceliyaan inta lagu jiro habka wax soo saarka ee diyaarinta.
2.3 Xasilooni
Waxay ku xasilan tahay aashitada iyo alkali labadaba, waxaana lagu kaydin karaa wakhti dheer inta u dhaxaysa pH 3 iyo 11 iyada oo aan isbeddel weyn lagu samaynin viscosity. Xalka aqueous ee HPMC waxa uu leeyahay saamaynta anti-mildew oo ilaaliya xasiloonida viscosity wanaagsan inta lagu jiro kaydinta muddada-dheer. Agabka dawooyinka ee isticmaalaya HPMC waxay leeyihiin xasilooni tayo fiican leh marka loo eego kuwa isticmaala maaddooyinka dhaqameed (sida dextrin, istaarijka, iwm.).
2.4 Laqabsiga Viscosity
Noocyada viscosity ee kala duwan ee HPMC ayaa lagu qasi karaa qaybo kala duwan, mawjaddeedana waxaa lagu bedeli karaa sharci gaar ah, waxayna leedahay xiriir toosan oo wanaagsan, sidaas darteed saamiga waxaa lagu dooran karaa iyadoo loo eegayo baahida.
2.5 dheef-shiid kiimikaad
HPMC laguma nuugo ama metabolized ee jirka, oo ma bixiso kulayl, sidaas darteed waa badbaado ah diyaarinta dawooyinka diyaarinta ah. 2.6 Badbaadada Guud ahaan waxaa loo arkaa in HPMC ay tahay wax aan sun ahayn oo aan xanaaq lahayn, qiyaasta dhexdhexaadka ah ee jiirarka waa 5 g·kg - 1, qiyaasta dhexdhexaadka ah ee jiirkana waa 5. 2 g · kg - 1. Qiyaasta maalinlaha ah wax dhib ah kuma laha jidhka bini'aadamka.
3.Codsiga HPMC ee qaababka
3.1 Sida walxaha dahaarka filimada iyo walxaha samaynta filimada
Isticmaalka HPMC sida qalab kaniini ah oo dahaarka leh, kaniiniga dahaarka leh ma laha faa'iidooyin muuqda oo lagu qarinayo dhadhanka iyo muuqaalka marka la barbar dhigo kiniiniyada dahaarka leh ee dhaqameed sida kiniinnada sonkorta leh, laakiin qallafsanaantiisa, friability, nuugista qoyaanka, heerka kala daadsanaanta. , korodhka miisaanka daboolka iyo tilmaamayaasha tayada kale ayaa ka fiican. Heerka viscosity hoose ee alaabtan waxaa loo isticmaalaa sida walxaha daahan filimka biyaha-milmi kara ee kiniiniyada iyo kiniiniyada, iyo heerka viscosity sare waxaa loo isticmaalaa sida wax daahan filim ee hababka dareeraha organic, sida caadiga ah at fiirsashada 2% ilaa 20 %.
Zhang Jixing iyo al. loo isticmaalo habka dusha sare ee saamaynta si loo hagaajiyo qaabaynta premix ee HPMC sida daaha filimka. Qaadashada walxaha filim samaynta ee HPMC, qadarka khamriga polyvinyl iyo plasticizer polyetylen glycol sida qodobbada baaritaanka, xoogga jilicsanaanta iyo permeability ee filimka iyo viscosity ee xal daahan filimka waa index kormeerka, iyo xiriirka ka dhexeeya kormeerka. index iyo qodobbada kormeerka waxaa lagu qeexay qaab xisaabeed, iyo habka qaabeynta ugu wanaagsan ayaa ugu dambeyntii la helay. Isticmaalkeedu waa siday u kala horreeyaan wakiilka filim-samaynta hydroxypropyl methylcellulose (HPMCE5) 11.88 g, alkolada polyvinyl 24.12 g, plasticizer polyetylen glycol 13.00 g, iyo viscosity hakinta daahan waa 20 mPa · s, permeability iyo saamaynta ugu fiican ee filimka gaadhay . Zhang Yuan waxa uu hagaajiyay habka diyaarinta, waxa uu HPMC u isticmaalay binder si uu u bedelo istaarijka istaarijka ah, waxana uu bedelay ki kor u qaadida xasiloonida kiniinka. Habka qaabeynta ugu fiican waxaa lagu go'aamiyay tijaabooyinka orthogonal, kuwaas oo ah, xoojinta slurry waxay ahayd 2% HPMC ee 70% ethanol xalinta inta lagu jiro daahan, iyo waqtiga walaaqaya inta lagu jiro granulation wuxuu ahaa 15 min. Natiijooyinka Kiniinnada dahaarka leh ee Jiahua ee ay diyaariyeen habka cusub iyo daawoyinka ayaa si weyn u wanaajiyay muuqaalka, wakhtiga kala daadsanaanta iyo adkaanta xudunta ah marka loo eego kuwa ay soo saareen habraacii asalka ahaa ee dawada, iyo heerka aqoonta ee kiniinada dahaarka leh ee filimka ayaa si weyn loo hagaajiyay. gaadhay in ka badan 95%. Liang Meiyi, Lu Xiaohui, iwm. sidoo kale waxay isticmaaleen hydroxypropyl methylcellulose sida walxaha samaynta filim si loogu diyaariyo kiniinka meelaynta xiidanka patinae iyo kiniiniga meelaynta mindhicirka, siday u kala horreeyaan. saameyn ku yeelato sii deynta daroogada. Huang Yunran waxa uu diyaariyey kiniinka meelaynta dhiigga ee Dragon's, oo uu HPMC ku mariyey xalinta lakabka bararka, jajabkiisuna waxa uu ahaa 5%. Waxaa la arki karaa in HPMC si weyn loogu isticmaali karo nidaamka gudbinta daroogada xiidan-bartilmaameedka.
Hydroxypropyl methylcellulose ma aha oo kaliya walaxda dahaarka filimka aad u fiican, laakiin sidoo kale waxaa loo isticmaali karaa sida wax-samaynta filimada ee qaabaynta filimada. Wang Tongshun iwm ayaa loo wanaajiyey in la qoro ee isku dhafka zinc licorice iyo aminolexanol filimka ka kooban afka, oo leh dabacsanaan, lebbisanaan, hufnaan, hufnaanta wakiilka filimka sida tusaha baaritaanka, u hesho rijeetada ugu fiican waa PVA 6.5 g, HPMC 0.1 g iyo 6.0 g of propylene glycol waxay buuxisaa shuruudaha si tartiib tartiib ah iyo badbaadada, waxaana loo isticmaali karaa warqadda diyaarinta ee filimka isku dhafan.
3.2 sida xidhidhka iyo kala daadsanaanta
Heerka viscosity hoose ee alaabtan waxa loo isticmaali karaa sida xidheyaal iyo kala daadinta kiniiniyada, kiniiniyada iyo granules, iyo heerka viscosity sare oo kaliya loo isticmaali karaa sida xidhe ahaan. Qiyaasta waxay ku kala duwan tahay noocyo iyo shuruudo kala duwan. Guud ahaan, qiyaasta binder ee kiniinnada qallalan qallalan waa 5%, iyo qiyaasta kiniinka granulation-ka qoyan waa 2%.
Li Houtao et al ayaa baadhay xiraha kiniiniyada tinidazole. 8% polyvinylpyrrolidone (PVP-K30), 40% sharoobada, 10% istaarijka slurry, 2.0% hydroxypropyl methylcellulose K4 (HPMCK4M), 50% ethanol ayaa la baaray sida ku dheggan kiniinnada tinidazole markeeda. diyaarinta kaniiniyada tinidazole. Isbeddelka muuqaalka kiniinnada caadiga ah iyo dahaarka ka dib ayaa la is barbardhigay, iyo friability, adkeyd, xaddidnaanta waqtiga kala-tagga iyo heerka kala dirida kiniinnada kala duwan ee dawooyinka ayaa la cabbiray. Natiijooyinka Kiniinnada ay diyaariyeen 2.0% hydroxypropyl methylcellulose waxay ahaayeen kuwo dhalaalaya, cabirka friability-ga ma helin wax gees ah oo googo'an iyo ifafaale gees ka gees ah, daahan ka dib, qaabka kiniiniga waa dhameystiran yahay muuqaalkuna wuu wanaagsanaa. Sidaa darteed, kiniiniyada tinidazole ee lagu diyaariyey 2.0% HPMC-K4 iyo 50% ethanol sida xidhayaasha ayaa la isticmaalay. Guan Shihai waxa uu bartay habka samaynta ee kiniiniyada Fuganning, waxa uu baadhay xabagta, waxana uu baadhay 50% ethanol, 15% starch paste, 10% PVP iyo 50% ethanol xalalka cufan, siman, iyo friability sida tilmaamayaasha qiimaynta. , 5% CMC-Na iyo 15% HPMC xal (5 mPa s). Natiijooyinka Xaashiyaha ay diyaariyeen 50% ethanol, 15% koollada istaarijka ah, 10% PVP 50% ethanol xal iyo 5% CMC-Na waxay lahaayeen dusha siman, laakiin cadaadis liidata iyo adkaanta hoose, taas oo aan dabooli karin baahida daboolka; 15% HPMC xal (5 mPa·s), oogada sare ee kiniinku waa siman yahay, friability-ku waa u qalma, iyo cadaadisku waa wanaagsan yahay, kaas oo buuxin kara baahiyaha daahan. Sidaa darteed, HPMC (5mPa s) ayaa loo doortay sida xabagta.
3.3 oo ah wakiilka ka joojinta
Heerka viscosity-sare ee alaabtan waxaa loo isticmaalaa sidii wakiilka ka joojinta si loogu diyaariyo diyaarinta dareeraha nooca cayrinta. Waxay leedahay saameyn hakin wanaagsan, way fududahay in dib loo kala firdhiyo, kuma dhegto gidaarka, waxayna leedahay qaybo qulqulaya oo fiican. Qiyaasta caadiga ah waa 0.5% ilaa 1.5%. Song Tian iyo al. loo isticmaalo walxaha polymer sida caadiga ah loo isticmaalo (hydroxypropyl methylcellulose, sodium carboxymethylcellulose, povidone, xanthan xanjo, methylcellulose, iwm) sida wakiilada hakinta si ay u diyaariyaan racecadotril. ka joojinta qalalan. Iyada oo loo marayo saamiga mugga sedimentation ee ganaaxyo kala duwan, index redispersibility, iyo rheology, viscosity ganaax iyo morphology microscopic ayaa la arkay, iyo xasiloonida qaybaha daroogada hoos tijaabo la dedejiyey ayaa sidoo kale la baaray. Natiijooyinka Cayrinta qalalan ee lagu diyaariyay 2% HPMC maadaama wakiilka cayrinta uu lahaa hab fudud iyo xasillooni wanaagsan.
Marka la barbar dhigo methyl cellulose, hydroxypropyl methyl cellulose waxay leedahay sifooyinka samaynta xal cad, oo kaliya qadar aad u yar oo ah walxo fibros ah oo aan kala firdhin ayaa jira, sidaas darteed HPMC waxaa sidoo kale loo isticmaalaa sida wakiilka joojinta ee diyaarinta indhaha. Liu Jie iyo al. loo isticmaalo HPMC, hydroxypropyl cellulose (HPC), carbomer 940, polyethylene glycol (PEG), sodium hyaluronate (HA) iyo isku darka HA/HPMC sida wakiilada hakinta si ay u diyaariyaan tilmaamo kala duwan ee Ciclovir ka joojinta indhaha, saamiga mugga sedimentation, size qayb iyo dib u kala firdhiso. waxaa loo xushay tilmaamayaasha baadhista si loo baadho wakiilka ugu fiican ee ka joojinta. Natiijooyinku waxay muujinayaan in joojinta indhaha ee acyclovir ay diyaarisay 0.05% HA iyo 0.05% HPMC sida wakiilka ganaaxa, saamiga mugga sedimentation waa 0.998, cabbirka qaybtu waa labis, dib-u-celinta waa wanaagsan tahay, diyaargarowga waa xasilloonida Galmada.
3.4 Sida xannibaadaha, wakiilka sii-deynta gaabis ah oo kontaroolan iyo wakiilka dalool-samaynta
Heerka viscosity-sare ee alaabtan waxaa loo isticmaalaa diyaarinta kiniiniyada sii-deynta joogtada ah ee hydrophilic gel matrix, blockers iyo wakiilada la xakameeyey ee kiniiniyada matrix-ka-isku-dhafka ah ee sii-deynta joogtada ah, waxayna leedahay saameynta dib u dhigista sii-deynta daroogada. Xoog saaristiisu waa 10% ilaa 80%. Darajooyinka viscosity-hoose waxaa loo isticmaalaa porogens ahaan sii-deynta joogtada ah ama diyaarinta sii-deynta la kantaroolay. Qiyaasta bilawga ah ee loo baahan yahay saamaynta daaweynta kiniinnada noocan oo kale ah ayaa si dhakhso ah loo gaari karaa, ka dibna sii-deynta joogtada ah ama saameynta sii-deynta ayaa la sameeyaa, iyo xoojinta daawada dhiigga ee waxtarka leh ayaa lagu hayaa jirka. . Hydroxypropyl methylcellulose waa fuuqbax si ay u sameeyaan lakab jel marka ay la kulmaan biyaha. Habka lagu sii daayo daroogada ee kiniinka matrixka inta badan waxaa ka mid ah faafinta lakabka jel iyo nabaad-guurka lakabka jel. Jung Bo Shim iyo al waxay diyaariyeen kiniiniyada sii-daynta joogtada ah ee carvedilol oo leh HPMC oo ah walxo sii-dayn joogto ah.
Hydroxypropyl methylcellulose ayaa sidoo kale si weyn loogu isticmaalaa kiniiniyada matrix-ka sii-daynta joogtada ah ee daawada dhaqameed ee Shiinaha, iyo inta badan maaddooyinka firfircoon, qaybo waxtar leh iyo hal diyaargarow oo daawo dhaqameed ah ayaa la isticmaalaa. Liu Wen iyo al. Waxa loo adeegsaday 15% hydroxypropyl methylcellulose sida walxaha matrixka, 1% lactose iyo 5% microcrystalline cellulose sidii buuxinyaal, iyo diyaarinta Jingfang Taohe Chengqi Decoction ee matrix afka ah oo sii daaya kiniiniyada. Qaabku waa isla'egta Higuchi. Nidaamka ka kooban formula waa mid fudud, diyaarintu waa sahlan tahay, iyo xogta sii daayo waa mid xasiloon, kaas oo buuxiya shuruudaha Pharmacopoeia Shiinaha. Tang Guanguang iyo al. loo isticmaalo wadarta saponins ee Astragalus sida daroogada model ah, diyaariyey kiniiniyada matrix HPMC, oo sahamiyey arrimaha saameeya sii daayo daroogada qaybaha wax ku ool ah ee dawooyinka dhaqanka Shiinaha ee kiniiniyada matrix HPMC. Natiijooyinka Markay qiyaasta HPMC kor u kacday, sii-deynta astragaloside-ka ayaa hoos u dhacday, boqolkiiba siideynta daawada waxay lahayd xiriir toosan oo ku dhow heerka kala dirida shaxanka. In kiniiniga hypromellose HPMC matrix, waxaa jira xiriir gaar ah oo u dhexeeya sii daayo ee qaybta wax ku ool ah ee daawada dhaqanka Chinese iyo qiyaasta iyo nooca HPMC, iyo habka loo sii daayo monomer kiimikada hydrophilic la mid ah. Hydroxypropyl methylcellulose kuma habboona oo kaliya xeryahooda hydrophilic, laakiin sidoo kale walxaha aan-hydrophilic ahayn. Liu Guihua waxa uu isticmaalay 17% hydroxypropyl methylcellulose (HPMCK15M) sida walxaha matrix-ka sii-daynta joogtada ah, waxa uuna Tianshan Xuelian u diyaariyay kiniiniyada matrix-ka sii-daynta joogtada ah ee qoyan iyo habka kiniiniga. Saamaynta sii-daynta joogtada ahi waxay ahayd mid cad, habka diyaarintuna waxa uu ahaa mid deggan oo macquul ah.
Hydroxypropyl methylcellulose ma aha oo kaliya in lagu dabaqo kaniiniyada matrix-ka sii-daynta joogtada ah ee maaddooyinka firfircoon iyo qaybaha waxtarka leh ee daawada dhaqameed ee Shiinaha, laakiin sidoo kale aad iyo aad u badan ayaa loo isticmaalaa diyaarinta isku dhafka daawada dhaqameed ee Shiinaha. Wu Huichao iyo al. loo isticmaalo 20% hydroxypropyl methyl cellulose (HPMCK4M) sida maadada matrixka, waxayna isticmaaleen habka budada tooska ah ee isku-buufinta si ay u diyaariyaan kiniiniga Yizhi hydrophilic gel matrix-ka kaas oo si joogto ah u sii deyn kara daawada si joogto ah oo joogto ah saacadaha 12. Saponin Rg1, ginsenoside Rb1 iyo Panax notoginseng saponin R1 ayaa loo adeegsaday tilmaamayaasha qiimeynta si loo baaro sii deynta vitro, iyo isla'egta sii deynta daroogada ayaa lagu rakibay si loo barto habka siideynta daroogada. Natiijooyinka Habka lagu sii daayo daroogada ayaa u hoggaansamaya isle'egta kinetic-ka eber iyo isla'egta Ritger-Peppas, kaas oo geniposide lagu sii daayay faafinta aan Fick ahayn, iyo saddexda qaybood ee Panax notoginseng ayaa lagu sii daayay nabaad-guurka lafaha.
3.5 Xabagta ilaalinta sida dhumuc iyo kolloid
Marka badeecadan loo isticmaalo sidii dhumuc ahaan, qiyaasta caadiga ah ee boqolkiiba waa 0.45% ilaa 1.0%. Waxa kale oo ay kordhin kartaa xasiloonida xabagta hydrophobic, samee kolloid ilaalin ah, waxay ka hortagtaa walxaha ka soo baxa dhuxusha iyo kicinta, taas oo joojinaysa samaynta sediments. Qiyaasta guud ee boqolkiiba waa 0.5% ilaa 1.5%.
Wang Zhen iyo al. isticmaalay habka naqshadaynta tijaabada ee L9 orthogonal si ay u baarto habka diyaarinta ee dawada firfircoon ee enema. Shuruudaha habka ugu wanaagsan ee go'aaminta kama dambaysta ah ee daawada firfircoonida daawada kaarboonka waa in la isticmaalo 0.5% sodium carboxymethyl cellulose iyo 2.0% hydroxypropyl methylcellulose (HPMC waxay ka kooban tahay 23.0% methoxyl group, hydroxypropoxyl Base 11.6%) sida dhumuc ahaan, xaaladaha habraaca ayaa gacan ka geysanaya xoojinta xasiloonida kaarboonka firfircoon ee daawada. Zhang Zhiqiang iyo al. Waxay soo saartay pH-xasaasi ah levofloxacin hydrochloride indhaha diyaar u ah in la isticmaalo oo leh saameyn sii-dayn joogto ah, iyadoo la adeegsanayo carbopol sida matrix gelka iyo hydroxypropyl methylcellulose oo ah wakiilka dhumucda. Daawaynta ugu fiican ee tijaabada ah, ugu dambeyntii waxay helaysaa daawada ugu fiican waa levofloxacin hydrochloride 0.1 g, carbopol (9400) 3 g, hydroxypropyl methylcellulose (E50 LV) 20 g, disodium hydrogen phosphate 0.35 g, fosfooraska acid 0.45 g of sodium 0.5 dihydrogede. , 0.03 g of ethyl paraben, iyo biyo lagu daray si ay u sameeyaan 100 mL. Imtixaanka, qoraagu wuxuu ku baadhay taxanaha hydroxypropyl methylcellulose METHOCEL ee shirkadda Colorcon oo leh tilmaamo kala duwan (K4M, E4M, E15 LV, E50LV) si loo diyaariyo dhumucyada kala duwan, natiijaduna waxay dooratay HPMC E50 LV sidii dhumuclaha. Thickerer loogu talagalay pH-xasaasiga leh levofloxacin hydrochloride jeelyada degdega ah.
3.6 sida walxaha kaabsal
Caadi ahaan, maaddada qolofka kaabsoosha ee kaabsooshadu waxay u badan tahay jelatin. Habka wax soo saarka qolof kaabsoosha waa mid fudud, laakiin waxaa jira qaar ka mid ah dhibaatooyinka iyo ifafaale ay ka mid yihiin ilaalinta liidata ee ka hortagga qoyaanka iyo dawooyinka xasaasiga ah ee ogsajiinta, yaraynta milanka daroogada, iyo daahitaanka burburka qolofka kaabsulka inta lagu jiro kaydinta. Sidaa darteed, hydroxypropyl methylcellulose waxaa loo isticmaalaa beddelka kaabsoosha jelatin ee diyaarinta kaabsoosha, taas oo hagaajinaysa qaabaynta wax soo saarka kaabsoosha iyo saamaynta isticmaalka, waxaana si weyn kor loogu qaaday gudaha iyo dibadda.
Isticmaalka theophylline sida daawada xakamaynta, Podczeck et al. la ogaaday in heerka kala dirida daroogada ee kaabsoosha leh hydroxypropyl methylcellulose qolof ka weyn yahay ka kaabsal gelatin. Sababta falanqaynta ayaa ah in burburka HPMC uu yahay burburka kaabsulka oo dhan isku mar, halka burburka kaabsal jelatin uu yahay burburka qaab dhismeedka shabakada marka hore, ka dibna kala go'a kaabsoosha oo dhan, sidaas darteed. Kaabsoosha HPMC waxa uu aad ugu haboon yahay qolofka Kaabsulka si loo sii daayo isla markiiba. Chiwele iyo al. Waxa kale oo la helay gunaanad la mid ah oo la barbardhigay kala dirida jelatin, jelatin/polyethylene glycol iyo qolofka HPMC. Natiijooyinku waxay muujiyeen in qolofyada HPMC ay si degdeg ah u milmeen xaaladaha pH ee kala duwan, halka kaabsoosha jelatin ay si weyn u saameeyeen xaaladaha pH ee kala duwan. Tang Yue iyo al. lagu baadhay nooc cusub oo qolof kaabsoosha ah oo loogu talagalay nidaamka xambaarka daawada budada qalalan ee maran qiyaas yar. Marka la barbardhigo qolofka kaabsal ee hydroxypropyl methylcellulose iyo qolof kaabsal ee gelatin, xasiloonida qolof kaabsoosha iyo sifooyinka budada qolof ku jira xaalado kala duwan ayaa la baaray, iyo tijaabada friability ayaa la sameeyay. Natiijooyinku waxay muujinayaan in marka la barbar dhigo kaabsal jelatin, qolof kaabsoosha HPMC ay ku fiican yihiin xasiloonida iyo ilaalinta budada, waxay leeyihiin iska caabin qoyaan ka xoog badan, oo ay leeyihiin friability hoose marka loo eego qolof kaabsal gelatin, sidaa darteed qolof kaabsal HPMC ayaa aad ugu habboon Kaabsoosha loogu talagalay neefsashada budada qalalan.
3.7 sida bioadhesive
Tiknoolajiyada bioadhesion waxay isticmaashaa qalabyo leh polymers bioadhesive. Iyadoo la raacayo xuubka bayoolojiga, waxay kor u qaadeysaa sii wadida iyo adkeynta xiriirka ka dhexeeya diyaarinta iyo xuubka xuubka, si daroogadu si tartiib ah loo sii daayo oo loo nuugo xuubka xuubka si loo gaaro ujeedada daaweynta. Hadda aad baa loo isticmaalaa. Daawaynta cudurada mareenka caloosha iyo mindhicirka, siilka, xuubka afka iyo qaybaha kale.
Tiknoolajiyada bioadhesion ee xiidmaha mindhicirka waa hab cusub oo gudbinta dawooyinka la sameeyay sanadihii ugu dambeeyay. Ma aha oo kaliya inay kordhiso wakhtiga degenaanshaha ee diyaarinta daroogada ee mareenka caloosha iyo mindhicirka, laakiin sidoo kale waxay wanaajisaa waxqabadka xiriirka ka dhexeeya daroogada iyo xuubka unugyada ee goobta nuugista, beddelo dheecaanka xuubka unugyada, oo ka dhigaya dhexgalka daroogada Unugyada epithelial mindhicirka yar ayaa la wanaajiyaa, taas oo hagaajinaysa bioavailability ee daawada. Wei Keda iyo al. waxay tijaabiyeen dawada xudunta u ah kiniiniga iyadoo la raacayo qiyaasta HPMCK4M iyo Carbomer 940 oo ah qodobbada baadhista, waxayna adeegsatay aaladda bioadhesion-ka ee iskeed u samaysatay si ay u cabbirto xoogga diirinta ee u dhexeeya kiniinka iyo biofilm-ka la ekaysiiyay tayada biyaha bacda. , oo ugu dambeyntii doortay waxa ku jira HPMCK40 iyo carbomer 940 si ay u noqdaan 15 iyo 27.5 mg ee aagga rijeetada ugu fiican ee NCaEBT ee kombuyuutarrada kiniinka, siday u kala horreeyaan, si loo diyaariyo koodhka kiniinka NCaEBT, taas oo muujinaysa in walxaha bioadhesive (sida hydroxypropyl methylcellulose) ay si weyn u yareeyn karto Hagaajinta adhesion ee diyaarinta ee nudaha.
Diyaargarowga bioadhesive afka ayaa sidoo kale ah nooc cusub oo ah habka gaarsiinta daawada kaas oo si aad ah loo darsay sanadihii ugu dambeeyay. Diyaargarowga bioadhesive afka ayaa u hoggaansami kara daawada qaybta ay saameysay ee daloolka afka, taas oo aan dheerayn oo kaliya wakhtiga daawadu ku jirto xuubka afka, laakiin sidoo kale waxay ilaalisaa xuubka afka. Saameyn daweyn oo ka sii wanaagsan iyo helitaanka noole ee daawada oo la hagaajiyay. Xue Xiaoyan iyo al. waxay hagaajisay samaynta kiniiniyada xabagta afka laga qaato ee insulin, iyadoo la isticmaalayo pectin tufaaxa, chitosan, carbomer 934P, hydroxypropyl methylcellulose (HPMC K392) iyo sodium alginate sida walxo bioadhesive ah, iyo qalajinta qalajinta si loogu diyaariyo insulin afka. Xabag labajibbaaran xaashida. Kiniinka xabagta afka ee la diyaariyey waxa uu leeyahay qaab-dhismeedka isbuunyada oo kale ah, kaas oo ku habboon in la sii daayo insulinta, waxana uu leeyahay lakabka ilaalinta hydrophobic, kaas oo hubin kara in si aan toos ahayn loo sii daayo daawada kana fogaato luminta daawada. Hao Jifu iyo al. Waxa kale oo loo diyaariyey kuulo buluug-jaalle ah oo afka laga qaato balastar bioadhesive iyadoo la isticmaalayo xabagta Baiiji, HPMC iyo kabomer sida walxo bioadhesive ah.
Nidaamyada gudbinta daawada siilka, tignoolajiyada bioadhesion ayaa sidoo kale si weyn loo isticmaalay. Zhu Yuting iyo al. loo isticmaalo carbomer (CP) iyo HPMC sidii qalab xabag ah iyo matrix-sii-daynta joogtada ah si loogu diyaariyo kiniiniyada siilka ee clotrimazole bioadhesive oo leh qaabab iyo saamiyo kala duwan, waxayna cabbireen adhessionkooda, wakhtiga isku dhejinta iyo boqolkiiba bararka deegaanka dheecaanka siilka macmalka ah. , daawaynta ku haboon ayaa loo eegay sida CP-HPMC1: 1, xaashida xabagta ee la diyaariyey waxay lahayd waxqabadka xabagista oo wanaagsan, nidaamkuna wuxuu ahaa mid fudud oo macquul ah.
3.8 sida jel jirka la mariyo
Sida diyaarinta dhejiska, jelku wuxuu leeyahay faa'iidooyin taxane ah sida badbaadada, quruxda, nadiifinta fudud, kharash yar, habka diyaarinta fudud, iyo ku habboonaanta daroogada. Jihada horumarka. Tusaale ahaan, jel transdermal waa nooc cusub oo qiyaas ah kaas oo aad loo darsay sanadihii ugu dambeeyay. Ma aha oo kaliya in laga fogaado burburinta daroogada ee mareenka caloosha iyo mindhicirka iyo in la yareeyo kala duwanaanshaha ugu sarreeya ee fiirsashada daawada dhiigga, laakiin sidoo kale waxay noqotay mid ka mid ah hababka siideynta daroogada waxtarka leh si looga gudbo dhibaatooyinka daroogada. .
Zhu Jingjie iyo al. bartay saamaynta matrices kala duwan on sii daayo of scutellarin alkohol plastid jel in vitro, oo lagu baadhay carbomer (980NF) iyo hydroxypropyl methylcellulose (HPMCK15M) sida matrices gel, oo la helay scutellarin ku habboon sutellarin. Gel matrix ee balaastikada khamriga. Natiijooyinka tijaabada ah waxay muujinayaan in 1. 0% carbomer, 1. 5% carbomer, 1. 0% carbomer + 1. 0% HPMC, 1. 5% carbomer + 1. 0% HPMC sida gel matrix Labaduba waxay ku habboon yihiin plastids aalkolada scutellarin. . Intii lagu guda jiray tijaabada, waxaa la ogaaday in HPMC ay bedeli karto habka siideynta daroogada ee matrixka kaarbomer jel iyadoo ku habboon isla'egta kinetic ee sii deynta daroogada, iyo 1.0% HPMC waxay hagaajin kartaa 1.0% carbomer matrix iyo 1.5% carbomer matrix. Sababtu waxay noqon kartaa in HPMC ay si dhakhso ah u fiddo, iyo balaadhinta degdega ah ee marxaladda hore ee tijaabada ayaa ka dhigaysa farqiga molecular ee maaddada jel-ka-carbomer mid weyn, taas oo dardargelinaysa heerka sii deynta daroogada. Zhao Wencui iyo al. loo isticmaalo carbomer-934 iyo hydroxypropyl methylcellulose sidii sideyaal si loogu diyaariyo jel indhaha ee norfloxacin. Habka diyaarinta waa mid fudud oo macquul ah, iyo tayada u hoggaansamaan jel indhaha ee "Pharmacopoeia Shiinaha" (2010 daabacaadda) shuruudaha tayada.
3.9 Horjoogaha roobka ee nidaamka is-microemulsifying
Is-microemulsifying dawada habka gudbinta (SMEDDS) waa nooc cusub oo ah habka gudbinta daawada afka, kaas oo ah isku-dhafan, xasilloon oo hufan oo ka kooban daroogo, wajiga saliidda, emulsifier iyo co-emulsifier. Halabuurka daawadu waa mid fudud, badbaadada iyo xasilloonidana waa wanaagsan yihiin. Daawooyinka liidata, walxaha polymer-ka ee biyaha ku milma, sida HPMC, polyvinylpyrrolidone (PVP), iwm, ayaa inta badan lagu daraa si ay u sameeyaan daawooyinka bilaashka ah iyo daawooyinka ku jira microemulsion waxay gaaraan kala dirid supersaturated ee mareenka caloosha iyo mindhicirka, si kordhiso milanka dawada oo wanaajiso bioavailability.
Peng Xuan iyo al. waxay diyaarisay silibinin supersaturated is-emulsifying drug delivery system (S-SEDDS). Oxyethylene hydrogenated castor oil (Cremophor RH40), 12% caprylic capry acid polyethylene glycol glyceride (Labrasol) oo ah co-emulsifier, iyo 50 mg·g-1 HPMC. Ku darida HPMC ee SSEDDS waxay kor u qaadi kartaa silibinin bilaash ah si ay ugu milanto S-SEDDS kana ilaaliso silibinin inay soo degto. Marka la barbar dhigo hababka dhaqameed ee is-microemulsion, xaddi badan oo surfactant ah ayaa inta badan lagu daraa si looga hortago daawaynta aan dhamaystirnayn. Ku-darka HPMC waxay ku ilaalin kartaa milanka silibinin ee dhexdhexaadiyaha kala dirida ilaa xad joogto ah, yaraynta emulsification ee qaababka is-microemulsion. qiyaasta wakiilka.
4.Gabagabadii
Waxa la arki karaa in HPMC si weyn loogu isticmaalay diyaarinta sababo la xidhiidha jidhkeeda, kiimikaad iyo bayooloji, laakiin HPMC waxa kale oo ay leedahay cillado badan oo xagga diyaarinta ah, sida ifafaalaha sii daynta ka hor iyo ka dib dillaaca. methyl methacrylate) si loo hagaajiyo. Isla mar ahaantaana, cilmi-baarayaasha qaarkood waxay baareen codsiga osmotic theory ee HPMC iyagoo diyaarinaya kiniinnada sii-deynta carbamazepine iyo kiniinnada sii-deynta joogtada ah ee verapamil hydrochloride si ay u sii daraaseeyaan habka sii deynta. Eray ahaan, cilmi-baarayaal badan oo badan ayaa qabanaya shaqo badan oo loogu talagalay codsiga wanaagsan ee HPMC ee diyaarinta, iyo daraasad qoto-dheer oo ku saabsan hantideeda iyo hagaajinta tignoolajiyada diyaarinta, HPMC ayaa si ballaaran loogu isticmaali doonaa foomamka qiyaasta cusub. iyo qaababka cusub ee qiyaasta. In cilmi-baarista nidaamka dawooyinka, ka dibna kor u horumarinta joogtada ah ee farmashiyaha.
Waqtiga boostada: Oct-08-2022