簡介環糊精

環糊精(Cyclodextrin)是一種環狀低聚醣,由多個吡喃葡萄糖分子構成一個錐形筒狀結構,擁有一組親水性的外環與疏水性的內腔[2],可透過疏水性的內腔包接親脂性官能基,藉此提升該分子的溶解度、滲透性、穩定度,並降低揮發性以減少氣味產生[1],且不影響其化學性質、結構及活性[6]。除此之外,亦可包接有毒物質[3]如磷苯、聯苯及雙酚等有害物質以改善環境汙染[4],故環糊精(Cyclodextrin)及其衍生物被廣泛用於製藥、食品、化妝品、農業與環境工程等,加之目前美國FDA已核准許多含有環糊精(Cyclodextrin)之產品上市,故環糊精(Cyclodextrin)之市值具備極佳的成長潛力。根據研究指出:到2024年,全球市場規模將增長到2.1億美元[8]。

環糊精的種類

環糊精(Cyclodextrin)可透過其吡喃葡萄糖單體的數量區分為α-環糊精(α-Cyclodextrin)、β-環糊精,(β-Cyclodextrin)及γ-環糊精(γ-Cyclodextrin)三種。其分別包含6個、7個及8個吡喃葡萄糖單體[5],而溶解度分別為15%、1.9%及23%(w / v)。其中,β-環糊精(β-Cyclodextrin)因其內腔大小、可得性高,成本低等優點,使其成為藥物絡合劑的首選。[6]儘管β-環糊精(β-Cyclodextrin) 已被證實在藥物賦形劑的優秀表現,但其本身的低溶解度及可能帶有腎毒性使其在應用與長期使用方面有使用限制並可能帶來健康疑慮,故科學家將β-環糊精(β-Cyclodextrin)與1,4-BS(1,4-Butane Sultone) (CAS 1633-83-6)合成,改良為Sulfobutyl ether beta-cyclodextrin(SEβCD),此舉不僅提高了其溶解度亦降低了β-環糊精(β-Cyclodextrin)的腎毒性,使Sulfobutyl ether beta-cyclodextrin(SEβCD)在藥物開發市場上的應用潛力備受矚目。[7]

*方案1.磺基丁基醚β-環糊精(SEβCD)的合成反應示意圖

了解更多關於 Hopax 1,4-BS

延伸閱讀: Sulfobutyl Ether beta-Cyclodextrin(SEBCD)之市場應用

 

參考資料:

[1]Cyclodextrins in pharmaceutical formulations I: structure and physicochemical properties, formation of complexes, and types of complex https://pubmed.ncbi.nlm.nih.gov/26686054/

[2] Cyclodextrins in pharmaceutical formulations I: structure and physicochemical properties, formation of complexes, and types of complex

[3] The Cyclodextrins and Their Application in Environmental Biotechnology https://www.sciencedirect.com/science/article/pii/S0166111608703443

[4] Use of α-cyclodextrin to Promote Clean and Environmentally Friendly Disinfection of Phenolic Substrates via Chlorine Dioxide Treatment https://www.frontiersin.org/articles/10.3389/fchem.2020.00641/full

[5] Exploring versatile applications of cyclodextrins: an overview https://www.tandfonline.com/doi/pdf/10.3109/10717544.2014.938839

[6] Cyclodextrins: new drug delivery systems in dermatology https://www.researchgate.net/profile/Thorsteinn-Loftsson/publication/227597926_Cyclodextrins_new_drug_delivery_systems_in_dermatology/links/5e9d5d2992851c2f52b28dcf/Cyclodextrins-new-drug-delivery-systems-in-dermatology.pdf

[7] Utility of Sulfobutyl Ether beta-Cyclodextrin Inclusion Complexes in Drug Delivery: A Review https://www.ijpsonline.com/articles/utility-of-sulfobutyl-ether-betacyclodextrin-inclusion-complexes-in-drug-delivery-a-review-3659.html

[8] Global Cyclodextrin Market Growth 2019-2024 https://www.fiormarkets.com/report/global-cyclodextrin-market-growth-2019-2024-373093.html#:~:text=According%20to%20this%20study%2C%20over,US%24%20180%20million%20in%202019

發佈日期:2021.05.10