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环糊精的药学应用案例—给药途径和剂型选择
1123 人阅读发布时间:2021-10-26 17:56
Examples on the pharmaceutical uses of cyclodextrins环糊精的药学应用案例
About 40% of drugs with market approval andnearly 90% of molecules in the discovery pipeline are poorly water-soluble and have low absorption. 上市药物中约 40% 和药物研发中近 90% 的分子水溶性差且吸收度低。Improved formulations with faster dissolution and enhanced absorption – a cost-effective strategy 具有更快溶出度和吸收度的改良配方-一种经济高效的策略
Native CDs have monographs in various Pharmacopoeias 天然环糊精被各国药典收载
Hydroxypropyl and sulfobutyl ether b-CDs (HP-b-CD and SBE-b-CD) are approved pharmaceutical ingredients in EU and USA 羟丙基和磺丁基醚-b-CD(HP-b-CD 和 SBE-b-CD)是欧盟和美国认可的药物成分
Random methylated b-CD (RM-b-CD), HP-g-CD and Sulfo-lipo CD are approved in some formulations 某些处方中批准了任意甲基化的 b-CD(RM-b-CD),HP-γ-CD 和磺基脂 CD
Number of Marketed Formulations for Various Administration Routes 各种剂型的市售制剂中的数量
~100 pharma products on the market containing Cyclodextrins 在市场上约 100 种药品包含环糊精
Parenteral Formulations Prostaglandin E1/a-CD 肠胃外制剂前列腺素 E1 / a-CD
Prostavasin – intrarterial infusion(Prostavasin –动脉注射)
Alprostadyl – Intra-cavernous injection(前列炔诺酮-海绵体内注射)
Vasodilator, a-CD is stabilizer and solubilizer(血管扩张剂,a-CD 是稳定剂和增溶剂)
Marketed since the beginning of 1982(自 1982 年初开始销售)
interarterial infusion, for treatment of stenosis in extremities or
thrombophlebitis.(动脉注射,用于治疗四肢或血栓性静脉炎的狭窄)
Used in babies with congenital heart defects(用于先天性心脏病的婴儿)
By injection into the penis, it is used to treat erectile dysfunction(通过注射到阴茎中,可用于治疗勃起功能障碍)
Further Tablets and Capsules for Oral Administration(溶解度提高起效重建)
Drospirenone + ethinyl estradiol + levomefolate calcium tablet as BCD-stabilized contraceptive Zaphyral, Yaz, Yasminelle)(以 BCD 稳定屈螺酮+乙炔雌二醇+左旋叶酸片的避孕药 Zaphyral,Yaz,Yasminelle))
HPBCD-enabled Umbralisib for the treatment of lymphoma (Ukoniq) (FDA approval: Feb. 2021)(含有 HPBCD 的 Umbralisib 用于治疗淋巴瘤 (Ukoniq) (FDA 批准:2021 年 2 月))
Parenteral Formulations Aripiprazole(肠胃外制剂-阿立哌唑)
Aripiprazole/SBE-b-CD(阿立哌唑/ SBE-b-CD)
Schizophrenia, bipolar affective disorder, phase I, maniac(精神分裂症,双相情感障碍,I 期,躁狂症)
Abilify: Single dose, ready to use intramuscular injection(Abilify:单剂,可立即使用肌肉注射)
7.5 mg/mL aripiprazole(7.5 mg / mL 阿立哌唑)
150 mg/mL SBE-b-CD(150 mg / mL SBE-b-CD)
Increased bioavailability compared to tablets(与片剂相比,提高了生物利用度)
Vaccines(疫苗)
Vaccine against Covid-19 approved by FDA in Feb 2021 HPBCD is an adjuvant(FDA 于 2021 年 2 月批准了针对 Covid-19 的疫苗 HPBCD 可作为佐剂)
ble to induce lymphocyte proliferation(能够诱导淋巴细胞增殖)
maintain a longer immune response(维持更长的免疫反应)
neduce the allergenic risk of the vaccine(降低疫苗的致敏风险)
Vaccine containing HPBCD against Newcastle disease for veterinary use(新城疫兽用疫苗含 HPBCD)
Vaccine containing sulfolipo CD against Porcine Circovirus for veterinary use(含抗猪圆环病毒的磺胺脂 CD 疫苗的兽用疫苗)
Patches for Transdermal Delivery(透皮贴剂)~300 papers on transdermal delivery in Scopus(Scopus 上有关透皮给药的 300 篇论文)
~80 papers on patches(patches 上有 80 篇论文)
Duloxetine/SBECD complex: 3x enhanced permeation through skin(度洛西汀/ SBECD 复合物:3 倍于皮肤的渗透性增强)
Kumar et al. Int. J. Pharm. 2021, 594, 120129 Cellulose/β-cyclodextrin nanofiber patch as a non-invasive, wearable epidermal glucose sensor(纤维素/β-环糊精纳米纤维贴片作为无创,可穿戴的表皮葡萄糖传感器)
Kim et al. RSC Adv., 2019, 9, 22790-22794 Hydrogel‐based microneedle (MN) arrays (BCD conjugated to gelatin) for transdermal delivery of curcumin(基于水凝胶的微针(MN)阵列(与明胶结合的 BCD)用于姜黄素的透皮递送介质)
Kim et al. Adv. Healthcare Mater. 2020, 9, 2000527
完整内容,请见 PDF 文件 「罗辅医药-环糊精的药学应用案例-给药途径和剂型选择」