Sulfobutyl ether beta-cyclodextrin(SEβCD)之市場應用

市場趨勢 環糊精 1,4-BS (1,4-Butane Sultone) 生物 製藥 manufacturer solubility

 

簡介Sulfobutyl ether beta-cyclodextrin(SEβCD)

Sulfobutyl ether beta-cyclodextrin(SEβCD)為β-環糊精(β-cyclodextrin)與1,4-BS(1,4-Butane Sultone) (CAS 1633-83-6)所合成的一種環糊精(cyclodextrin)衍生物。由於β-環糊精(β-cyclodextrin)溶解度較低，長時間放置可能導致藥物沉澱；且具備腎毒性，在腸胃外給藥之應用途徑缺乏靈活性，故將其改良為Sulfobutyl ether beta-cyclodextrin(SEβCD)，有效降低了β-環糊精(β-cyclodextrin)的腎毒性並提升溶解度與血液相容性，促使其在臨床使用上具備優異的生物利用度與良好的耐受性。亦被美國藥典與歐洲藥典核准使用於多項藥物賦形劑上。

Sulfobutyl ether beta-cyclodextrin(SEβCD) 因具備優異的穩定性、滲透性、溶解度、低毒性及生物利用性，加之可透過將藥物分子置於內腔以控制藥物釋放時間，使Sulfobutyl ether beta-cyclodextrin(SEβCD)被廣泛應用於口服藥、眼部用藥、鼻腔用藥、肺部輸送、靜脈針劑及局部皮膚用藥，以下將為您統整Sulfobutyl ether beta-cyclodextrin(SEβCD)在臨床藥物應用上的表現與用途：

口服藥：

  • 已被用於一種治療胃部疾病用藥–法莫替丁(Famotidine)中，以增加水溶性並掩蓋法莫替丁(Famotidine)的苦味[2]
  • 已被用於提高類固醇藥物在水中的溶解度並提高這些疏水性API的生物利用度[3]
  • 已被用於一種激素類藥物–雷洛昔芬（Raloxifene（RXF）），以增加水溶性並克服吸收障礙[4]
  • 已被用於含有醋酸二咪唑酮（Diminazene Aceturate, DA）之藥物配方中，克服其於胃酸中降解的速率[13]
  • 已被用於第二代抗精神病劑–伊潘立酮（ILO）中，提高其溶解度[14]

眼部用藥：

  • 已被用於一種治療青光眼用藥–Pilocarpine 芸香眼藥水前驅藥中，以提高眼部耐受性[6]
  • 已被證實可延長藥物在角膜中的停留時間並提高生物利用度[7]

鼻腔用藥：

  • 已被用於一種治療鼻黏膜微血管疾病用藥–沙利度胺（Thalidomide）鼻粉中，用於提高沙利度胺（Thalidomide）鼻粉於鼻黏膜中的溶解度[8]

肺部輸送:

  • 已被用於一種肺部吸入性給藥的治療用藥中，用來提高白藜蘆醇(Resveratrol)的穩定性與水溶性[9]

靜脈針劑：

  • 市面上已有多種經FDA批准的注射劑中含有Sulfobutyl ether beta-cyclodextrin (SEβCD)，主要作為增溶劑使用[10]
  • 已被用於抗病毒藥物注射劑–瑞姆昔韋（REM）中，作為增溶劑使用[10]

局部用藥：

  • 已被用於一種離子電滲療法之藥物-丙泊酚(Propofol)中，可增加丙泊酚(Propofol)的被動滲透通量[11]
  • 已被用於一種治療二型單純皰疹病毒（HSV-2）的陰道用藥–阿昔洛韋(Acyclovir)，用於提高抗病毒效力[12]

Further reading:什麼是環糊精

了解更多關於 Hopax 1,4-BS

參考資料:

[1]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

[2]Enhancement of the Aqueous Solubility and Masking the Bitter Taste of Famotidine Using Drug/SBE-β-CyD/Povidone K30 Complexation Approach https://jpharmsci.org/article/S0022-3549(15)32460-6/abstract

[3]Solubilizing steroidal drugs by β-cyclodextrin derivatives https://pubmed.ncbi.nlm.nih.gov/28743551/

[4]Raloxifene/SBE-β-CD Inclusion Complexes Formulated into Nanoparticles with Chitosan to Overcome the Absorption Barrier for Bioavailability Enhancement https://www.mdpi.com/1999-4923/10/3/76

[5]Cyclodextrins as Drug Carrier Molecule: A Review https://www.mdpi.com/2218-0532/76/4/567

[6]Sulfobutyl Ether β-Cyclodextrin (SBE-β-CD) in Eyedrops Improves the Tolerability of a Topically Applied Pilocarpine Prodrug in Rabbits https://www.liebertpub.com/doi/abs/10.1089/jop.1995.11.95

[7]Chloramphenicol/sulfobutyl ether-β-cyclodextrin complexes in an ophthalmic delivery system: prolonged residence time and enhanced bioavailability in the conjunctival sac https://www.tandfonline.com/doi/abs/10.1080/17425247.2019.1609447

[8]Role of New Antifungal Agents in the Treatment of Invasive Fungal Infections in Transplant Recipients: Isavuconazole and New Posaconazole Formulations https://www.mdpi.com/2309-608X/1/3/345/htm

[9]Cyclodextrin Complexation for Enhanced Stability and Non-invasive Pulmonary Delivery of Resveratrol—Applications in Non-small Cell Lung Cancer Treatment https://link.springer.com/article/10.1208/s12249-020-01724-x

[10]Sulfobutylether-beta-cyclodextrin-enabled antiviral remdesivir: Characterization of electrospun- and lyophilized formulations https://www.sciencedirect.com/science/article/pii/S0144861721003982#bib0075

[11]Transdermal iontophoretic delivery of a liquid lipophilic drug by complexation with an anionic cyclodextrin https://www.sciencedirect.com/science/article/abs/pii/S0168365914004131

[12]Acyclovir-loaded sulfobutyl ether-β-cyclodextrin decorated chitosan nanodroplets for the local treatment of HSV-2 infections https://www.sciencedirect.com/science/article/abs/pii/S0378517320306608

[13]β-Cyclodextrin as a Functional Excipient Used for Enhancing the Diminazene Aceturate Bioavailability https://doi.org/10.3390/pharmaceutics11060295

[14]Inclusion Complex of Iloperidone with Sulfobutyl Ether Beta-Cyclodextrin: Characterization and Dissolution Studies https://www.mdpi.com/2504-3900/78/1/22

發佈日期：2021.05.10

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