{"id":9130,"date":"2024-08-15T18:56:58","date_gmt":"2024-08-15T18:56:58","guid":{"rendered":"https:\/\/longchangextracts.com\/?p=9130"},"modified":"2024-08-15T18:56:58","modified_gmt":"2024-08-15T18:56:58","slug":"artemisinin-rapid-release-solid","status":"publish","type":"post","link":"https:\/\/longchangextracts.com\/hu\/artemisinin-gyors-felszabadulasu-szilard\/","title":{"rendered":"Az artemizinin gyors felszabadul\u00e1s\u00fa szil\u00e1rd diszperzi\u00f3 el\u0151\u00e1ll\u00edt\u00e1si folyamat\u00e1nak optimaliz\u00e1l\u00e1sa kett\u0151s hordoz\u00f3rendszer alkalmaz\u00e1s\u00e1val"},"content":{"rendered":"

Az artemizinin gyors felszabadul\u00e1s\u00fa szil\u00e1rd diszperzi\u00f3 el\u0151\u00e1ll\u00edt\u00e1si folyamat\u00e1nak optimaliz\u00e1l\u00e1sa kett\u0151s hordoz\u00f3rendszer alkalmaz\u00e1s\u00e1val
\nA mal\u00e1ria a mal\u00e1ria parazit\u00e1i \u00e1ltal okozott, sz\u00fanyogok \u00e1ltal terjesztett, vil\u00e1gszerte elterjedt, rendk\u00edv\u00fcl hal\u00e1los kimenetel\u0171, rosszindulat\u00fa fert\u0151z\u0151 betegs\u00e9g. A mal\u00e1ria parazit\u00e1k ciklikus terjed\u00e9se \u00e9s \u00f6sszetett \u00e9letciklusa miatt neh\u00e9z a mal\u00e1ria teljes felsz\u00e1mol\u00e1sa. A legt\u00f6bb hagyom\u00e1nyos mal\u00e1riaellenes gy\u00f3gyszer, mint p\u00e9ld\u00e1ul a klorokin, a kinin, az imikvin \u00e9s a piperakin, rezisztenci\u00e1t fejlesztett ki \u00e9s hat\u00e1stalann\u00e1 v\u00e1lt. Az artemizinin (ART) oszt\u00e1ly\u00fa mal\u00e1riaellenes gy\u00f3gyszerek gyors hat\u00e1s\u00faak, \u00e9s jelenleg elismert, hogy alacsony toxicit\u00e1s\u00faak, \u00e9s m\u00e9g nem mutattak nyilv\u00e1nval\u00f3 rezisztenci\u00e1t, \u00edgy els\u0151 vonalbeli mal\u00e1riaellenes gy\u00f3gyszerekk\u00e9 v\u00e1ltak. Az ART egy szeszkviterp\u00e9n-lakton, amelyet az Artemisia annua L. level\u00e9b\u0151l vonnak ki. Nemcsak az egyetlen els\u0151 vonalbeli mal\u00e1riaellenes gy\u00f3gyszer a mal\u00e1ria kezel\u00e9s\u00e9re, hanem sz\u00e1mos biol\u00f3giai aktivit\u00e1ssal is rendelkezik, mint p\u00e9ld\u00e1ul v\u00edrusellenes, immunszab\u00e1lyoz\u00f3, gyullad\u00e1scs\u00f6kkent\u0151, parazitaellenes, gombaellenes \u00e9s daganatellenes. Azonban rossz v\u00edz- \u00e9s lipidold\u00e9konys\u00e1ga miatt rosszul old\u00f3d\u00f3 gy\u00f3gyszer, in vivo nem teljes felsz\u00edv\u00f3d\u00e1ssal \u00e9s alacsony biol\u00f3giai hozz\u00e1f\u00e9rhet\u0151s\u00e9ggel. Az artemizinin klinikai alkalmaz\u00e1s\u00e1t korl\u00e1toz\u00f3 probl\u00e9m\u00e1k hat\u00e9kony megold\u00e1sa \u00e9rdek\u00e9ben az elm\u00falt \u00e9vekben sz\u00e1mos \u00faj m\u00f3dszert alkalmaztak az artemizinin alap\u00fa gy\u00f3gyszerformul\u00e1ci\u00f3khoz, amelyek k\u00f6z\u00fcl a szil\u00e1rd diszperzi\u00f3s technol\u00f3gia kapott figyelmet.<\/p>\n

A szil\u00e1rd diszperzi\u00f3 (SD) olyan diszperzi\u00f3s rendszer, amelyet szil\u00e1rd hidrof\u00f3b gy\u00f3gyszerhat\u00f3anyagok molekul\u00e1ris vagy mikrokrist\u00e1lyos \u00e1llapotban l\u00e9v\u0151 szil\u00e1rd hidrofil inert hordoz\u00f3ban t\u00f6rt\u00e9n\u0151 diszperg\u00e1l\u00e1s\u00e1val hoznak l\u00e9tre. Jelent\u0151sen n\u00f6velheti a hat\u00f3anyag oldhat\u00f3s\u00e1g\u00e1t \u00e9s kiold\u00f3d\u00e1s\u00e1t, el\u0151seg\u00edtheti a gy\u00f3gyszerek or\u00e1lis felsz\u00edv\u00f3d\u00e1s\u00e1t, jav\u00edthatja a biol\u00f3giai hozz\u00e1f\u00e9rhet\u0151s\u00e9get, valamint a megfelel\u0151 hordoz\u00f3k \u00e9s seg\u00e9danyagok kiv\u00e1laszt\u00e1s\u00e1val stabil \u00e9s nagym\u00e9rt\u00e9kben diszperg\u00e1lt hat\u00f3anyagokat, s\u0151t, ak\u00e1r tart\u00f3s \u00e9s szab\u00e1lyozott felszabadul\u00e1si hat\u00e1st is el\u00e9rhet. Ansari \u00e9s munkat\u00e1rsai a dihidroartemizinin szil\u00e1rd diszperzi\u00f3j\u00e1t \u00e1ll\u00edtott\u00e1k el\u0151 PVP K30 mint egyetlen viv\u0151anyag felhaszn\u00e1l\u00e1s\u00e1val, \u00e9s meg\u00e1llap\u00edtott\u00e1k, hogy a dihidroartemizinin amorf komplexk\u00e9nt l\u00e9tezett a viv\u0151anyaggal, amelynek oldhat\u00f3s\u00e1ga 50-szer nagyobb volt, mint a hat\u00f3anyag\u00e9; Yang \u00e9s munkat\u00e1rsai. az evodiamin szil\u00e1rd diszperzi\u00f3j\u00e1t poloxamer 188-at, mint optim\u00e1lis hordoz\u00f3t haszn\u00e1lva \u00e1ll\u00edtotta el\u0151, amely nagym\u00e9rt\u00e9kben jav\u00edtotta a hat\u00f3anyag old\u00f3d\u00e1s\u00e1t an\u00e9lk\u00fcl, hogy befoly\u00e1solta volna a hat\u00f3anyag tartalm\u00e1t \u00e9s morfol\u00f3gi\u00e1j\u00e1t; Li \u00e9s munkat\u00e1rsai szil\u00e1rd ART-diszperzi\u00f3t (ART-SD) \u00e9s tart\u00f3s felszabadul\u00e1s\u00fa ART-SD-t \u00e1ll\u00edtottak el\u0151 PEG 6000 lecitint kett\u0151s hordoz\u00f3k\u00e9nt \u00e9s III akrilgyant\u00e1t egyetlen hordoz\u00f3k\u00e9nt haszn\u00e1lva. Az egyetlen hordoz\u00f3val \u00f6sszehasonl\u00edtva, a szil\u00e1rd diszperzi\u00f3k k\u00e9sz\u00edt\u00e9se k\u00e9t vagy t\u00f6bb hordoz\u00f3b\u00f3l \u00e1ll\u00f3 vegyes hordoz\u00f3val t\u00f6bb el\u0151nnyel j\u00e1rhat a hat\u00f3anyag-felszabadul\u00e1si sebess\u00e9g szab\u00e1lyoz\u00e1s\u00e1ban \u00e9s a hat\u00f3anyag kiold\u00f3d\u00e1s\u00e1nak jav\u00edt\u00e1s\u00e1ban. Jelenleg azonban nem vil\u00e1gos, hogy a hordoz\u00f3 t\u00edpusa hat\u00e1ssal van-e az ART old\u00f3d\u00e1s\u00e1ra, \u00e9s a gyors felszabadul\u00e1s\u00fa ART-SD kett\u0151s hordoz\u00f3t haszn\u00e1l\u00f3 ART-SD el\u0151\u00e1ll\u00edt\u00e1s\u00e1nak folyamatfelt\u00e9teleit nem optimaliz\u00e1lt\u00e1k. Ez a cikk lecitint, a szil\u00e1rd diszperzi\u00f3khoz gyakran haszn\u00e1lt hordoz\u00f3t \u00e9s PEG 6000-et vagy PVP K30-at haszn\u00e1l kett\u0151s hordoz\u00f3k\u00e9nt, hogy \u00f6sszehasonl\u00edtsa a k\u00fcl\u00f6nb\u00f6z\u0151 hordoz\u00f3t\u00edpusok \u00e9s ar\u00e1nyok hat\u00e1s\u00e1t a hat\u00f3anyag kiold\u00f3d\u00e1s\u00e1ra. A kett\u0151s hordoz\u00f3s gyors felszabadul\u00e1s\u00fa ART-SD el\u0151\u00e1ll\u00edt\u00e1si folyamat\u00e1t optimaliz\u00e1ltuk, \u00e9s az optim\u00e1lis recept\u00far\u00e1val k\u00e9sz\u00edtett szil\u00e1rd diszperzi\u00f3ban a gy\u00f3gyszerhordoz\u00f3k l\u00e9tez\u00e9si \u00e1llapot\u00e1t IR \u00e9s DSC m\u00f3dszerekkel tiszt\u00e1ztuk, fontos alapot teremtve a rosszul old\u00f3d\u00f3 gy\u00f3gyszerek klinikai hat\u00e9konys\u00e1g\u00e1nak jav\u00edt\u00e1s\u00e1hoz.<\/p>\n

A szil\u00e1rd diszperzi\u00f3s technol\u00f3gia a gy\u00f3gyszereket nagym\u00e9rt\u00e9kben diszperg\u00e1lja a megfelel\u0151 hordoz\u00f3anyagokban, \u00e9s amorf, mikrokrist\u00e1lyos, molekul\u00e1risan diszperg\u00e1lt vagy kolloid\u00e1lisan diszperg\u00e1lt \u00e1llapotban l\u00e9tezik. A gyomor-b\u00e9lrendszeri folyad\u00e9kkal val\u00f3 \u00e9rintkez\u00e9s ut\u00e1n a gy\u00f3gyszer old\u00f3d\u00e1si sebess\u00e9ge felgyorsul, el\u0151seg\u00edtve a gy\u00f3gyszer felsz\u00edv\u00f3d\u00e1s\u00e1t \u00e9s jav\u00edtva a biol\u00f3giai hozz\u00e1f\u00e9rhet\u0151s\u00e9get, ez\u00e1ltal jav\u00edtva a rosszul old\u00f3d\u00f3 gy\u00f3gyszerek rossz or\u00e1lis felsz\u00edv\u00f3d\u00e1s\u00e1nak probl\u00e9m\u00e1j\u00e1t. A hordoz\u00f3 tulajdons\u00e1gai \u00e9s a hat\u00f3anyag-felszabadul\u00e1s jellemz\u0151i szerint a szil\u00e1rd diszperzi\u00f3kat gyors felszabadul\u00e1s\u00fa, szab\u00e1lyozott felszabadul\u00e1s\u00fa \u00e9s b\u00e9lsavval bevont szil\u00e1rd diszperzi\u00f3kra osztj\u00e1k. Ez a cikk hidrofil hordoz\u00f3anyagokat v\u00e1laszt ki, \u00e9s j\u00f3 nedvesed\u00e9si tulajdons\u00e1gaikat haszn\u00e1lja ki az ART gyors felszabadul\u00e1s\u00e1nak lehet\u0151v\u00e9 t\u00e9tel\u00e9re a gyors felszabadul\u00e1s\u00fa ART-SD-ben. Az 50 percen bel\u00fcli old\u00f3d\u00e1si sebess\u00e9g sokkal magasabb, mint a fizikai kever\u00e9kek \u00e9s az ART alapanyagok\u00e9, ami el\u0151ny\u00f6s az ART or\u00e1lis bead\u00e1s\u00e1nak hi\u00e1nyos felsz\u00edv\u00f3d\u00e1s\u00e1nak probl\u00e9m\u00e1j\u00e1nak megold\u00e1s\u00e1hoz.<\/p>\n

M\u00e1sodszor, a kett\u0151s hordoz\u00f3k nagyobb m\u00e9rt\u00e9kben k\u00e9pesek n\u00f6velni a hat\u00f3anyag kiold\u00f3d\u00e1s\u00e1t, mint az egyszer\u0171 hordoz\u00f3k. A sz\u00f3jalecitin szolubiliz\u00e1l\u00f3 tulajdons\u00e1gokkal rendelkezik, m\u00edg a PVP K30-nak a nedvesed\u00e9s fokoz\u00e1sa, az old\u00f3k\u00f6zeg fel\u00fcleti fesz\u00fclts\u00e9g\u00e9nek cs\u00f6kkent\u00e9se \u00e9s a gy\u00f3gyszer krist\u00e1lyosod\u00e1s\u00e1nak g\u00e1tl\u00e1sa a jellemz\u0151je. A PVP K30-at sz\u00e9les k\u00f6rben haszn\u00e1lj\u00e1k a nehezen old\u00f3d\u00f3 gy\u00f3gyszerek old\u00f3d\u00e1s\u00e1nak jav\u00edt\u00e1s\u00e1ra. A PEG 6000-et lecitinnel is kevert\u00e9k kett\u0151s hordoz\u00f3k\u00e9nt az ART-SD el\u0151\u00e1ll\u00edt\u00e1s\u00e1hoz, de a k\u00fcl\u00f6nb\u00f6z\u0151 kompozit hordoz\u00f3k hat\u00e1sa az ART-SD-b\u0151l sz\u00e1rmaz\u00f3 ART old\u00f3d\u00e1s\u00e1ra jelenleg nem tiszt\u00e1zott, \u00e9s a kett\u0151s hordoz\u00f3kat haszn\u00e1l\u00f3 ART-SD el\u0151\u00e1ll\u00edt\u00e1s\u00e1nak folyamatfelt\u00e9teleit nem optimaliz\u00e1lt\u00e1k. Ez a cikk a PVP K30 \u00e9s PEG 6000 kett\u0151s hordoz\u00f3k\u00e9nt kombin\u00e1lt foszfatidilkolin hat\u00e1s\u00e1t vizsg\u00e1lja az ART old\u00f3d\u00e1s\u00e1ra. Meg\u00e1llap\u00edthat\u00f3, hogy a foszfatidil-kolin PVP K30 jobb, \u00e9s meghat\u00e1roz\u00e1sra ker\u00fcl a kett\u0151 ar\u00e1nya. Ennek alapj\u00e1n optimaliz\u00e1lj\u00e1k a gyors felszabadul\u00e1s\u00fa ART-SD kett\u0151s hordoz\u00f3 old\u00f3szeres m\u00f3dszerrel t\u00f6rt\u00e9n\u0151 el\u0151\u00e1ll\u00edt\u00e1s\u00e1nak folyamatfelt\u00e9teleit, ami fontos alapot teremt az \u00faj ART-formul\u00e1k kifejleszt\u00e9s\u00e9hez.<\/p>\n

Ebben a k\u00eds\u00e9rletben az ART old\u00f3d\u00e1si sebess\u00e9g\u00e9t haszn\u00e1lt\u00e1k \u00e9rt\u00e9kel\u00e9si indexk\u00e9nt. A kett\u0151s hordoz\u00f3t\u00edpusok, az \u00f6sszetett hordoz\u00f3 ar\u00e1nyok, a reakci\u00f3id\u0151, az old\u00f3szer adagol\u00e1sa stb. egyt\u00e9nyez\u0151s sz\u0171r\u00e9s\u00e9n kereszt\u00fcl a kett\u0151s hordoz\u00f3rendszert haszn\u00e1l\u00f3, gyors felszabadul\u00e1s\u00fa ART-SD el\u0151\u00e1ll\u00edt\u00e1s\u00e1ra szolg\u00e1l\u00f3 optim\u00e1lis formul\u00e1t a k\u00f6vetkez\u0151k\u00e9ppen hat\u00e1roztuk meg: 50 mg ART, 50 mg sz\u00f3jalecitin, 350 mg PVP K30 (sz\u00f3jalecitin \u00e9s PVP K30 ar\u00e1nya 1:7). Az optim\u00e1lis elj\u00e1r\u00e1ssal el\u0151\u00e1ll\u00edtott szil\u00e1rd diszperzi\u00f3 hat\u00f3anyagtartalma 10,55% \u00b1 0,04% volt, az old\u00f3d\u00e1si egyens\u00falyt 30 perc alatt \u00e9rte el. Az 50 percen bel\u00fcli old\u00f3d\u00e1si sebess\u00e9g 87,21% \u00b1 2,28% volt, jelent\u0151sen magasabb, mint a PM 3,45% \u00b1 1,68% \u00e9s az ART alapanyag 0,05% \u00b1 0,15%. A DSC \u00e9s az IR elemz\u00e9s azt jelzi, hogy az ART \u00e9s a hordoz\u00f3 k\u00f6z\u00f6tt hidrog\u00e9nk\u00f6t\u00e9sek alakulnak ki, \u00e9s \u00faj amorf \u00e1llapotban l\u00e9teznek. Tov\u00e1bbi kutat\u00e1sokat fognak v\u00e9gezni annak meg\u00e1llap\u00edt\u00e1s\u00e1ra, hogy az ART-SD jav\u00edthatja-e az ART mint rosszul old\u00f3d\u00f3 gy\u00f3gyszer alacsony or\u00e1lis biol\u00f3giai hozz\u00e1f\u00e9rhet\u0151s\u00e9g\u00e9t, fokozhatja-e mal\u00e1riaellenes aktivit\u00e1s\u00e1t, \u00e9s hat\u00e9konyabb mal\u00e1riaellenes gy\u00f3gyszereket biztos\u00edthat-e a klinikai alkalmaz\u00e1shoz.<\/p>","protected":false},"excerpt":{"rendered":"

Az artemizinin gyors felszabadul\u00e1s\u00fa szil\u00e1rd diszperzi\u00f3 el\u0151\u00e1ll\u00edt\u00e1si folyamat\u00e1nak optimaliz\u00e1l\u00e1sa kett\u0151s hordoz\u00f3rendszer alkalmaz\u00e1s\u00e1val A mal\u00e1ria egy rendk\u00edv\u00fcl hal\u00e1los kimenetel\u0171, rosszindulat\u00fa fert\u0151z\u0151 betegs\u00e9g, amelyet mal\u00e1ria parazit\u00e1k okoznak, sz\u00fanyogok terjesztik, \u00e9s vil\u00e1gszerte sz\u00e9les k\u00f6rben elterjedt. A mal\u00e1ria parazit\u00e1k ciklikus terjed\u00e9se \u00e9s \u00f6sszetett \u00e9letciklusa megnehez\u00edtette a mal\u00e1ria teljes felsz\u00e1mol\u00e1s\u00e1t. A legt\u00f6bb hagyom\u00e1nyos mal\u00e1riaellenes gy\u00f3gyszer, p\u00e9ld\u00e1ul [...]<\/p>","protected":false},"author":1,"featured_media":0,"comment_status":"closed","ping_status":"open","sticky":false,"template":"","format":"standard","meta":{"footnotes":""},"categories":[20],"tags":[],"yoast_head":"\nOptimization of artemisinin rapid release solid dispersion preparation process using dual carrier system - China Chemical Manufacturer<\/title>\n<meta name=\"robots\" content=\"index, follow, max-snippet:-1, max-image-preview:large, max-video-preview:-1\" \/>\n<link rel=\"canonical\" href=\"https:\/\/longchangextracts.com\/hu\/artemisinin-gyors-felszabadulasu-szilard\/\" \/>\n<meta property=\"og:locale\" content=\"hu_HU\" \/>\n<meta property=\"og:type\" content=\"article\" \/>\n<meta property=\"og:title\" content=\"Optimization of artemisinin rapid release solid dispersion preparation process using dual carrier system - China Chemical Manufacturer\" \/>\n<meta property=\"og:description\" content=\"Optimization of artemisinin rapid release solid dispersion preparation process using dual carrier system Malaria is a highly lethal malignant infectious disease caused by malaria parasites, transmitted by mosquitoes, and widely spread worldwide. 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