• 文献检索
  • 文档翻译
  • 深度研究
  • 学术资讯
  • Suppr Zotero 插件Zotero 插件
  • 邀请有礼
  • 套餐&价格
  • 历史记录
应用&插件
Suppr Zotero 插件Zotero 插件浏览器插件Mac 客户端Windows 客户端微信小程序
定价
高级版会员购买积分包购买API积分包
服务
文献检索文档翻译深度研究API 文档MCP 服务
关于我们
关于 Suppr公司介绍联系我们用户协议隐私条款
关注我们

Suppr 超能文献

核心技术专利:CN118964589B侵权必究
粤ICP备2023148730 号-1Suppr @ 2026

文献检索

告别复杂PubMed语法,用中文像聊天一样搜索,搜遍4000万医学文献。AI智能推荐,让科研检索更轻松。

立即免费搜索

文件翻译

保留排版,准确专业,支持PDF/Word/PPT等文件格式,支持 12+语言互译。

免费翻译文档

深度研究

AI帮你快速写综述,25分钟生成高质量综述,智能提取关键信息,辅助科研写作。

立即免费体验

作为改善阿苯达唑生物药剂学行为策略的固体分散体的开发及体外评价

Development and in vitro evaluation of solid dispersions as strategy to improve albendazole biopharmaceutical behavior.

作者信息

Simonazzi Analía, Cid Alicia Graciela, Paredes Alejandro Javier, Schofs Laureano, Gonzo Elio Emilio, Palma Santiago Daniel, Bermúdez José María

机构信息

Instituto de Investigaciones para la Industria Química, Universidad Nacional de Salta - Consejo Nacional de Investigaciones Científicas y Técnicas, Av. Bolivia 5150, Salta 4400, Argentina.

Unidad de Investigación y Desarrollo en Tecnología Farmacéutica, Universidad Nacional de Córdoba - Consejo Nacional de Investigaciones Científicas y Técnicas, Haya de la Torre y Medina Allende, Ciudad Universitaria, Córdoba 5000, Argentina.

出版信息

Ther Deliv. 2018 Sep;9(9):623-638. doi: 10.4155/tde-2018-0037.

DOI:10.4155/tde-2018-0037
PMID:30189808
Abstract

AIM

Solid dispersions using Poloxamer 407 as carrier were developed to improve albendazole (ABZ) solubility and dissolution profiles.

METHODS

ABZ/poloxamer solid dispersions were prepared, and dissolution profiles were mathematically modeled and compared with physical mixtures, pharmaceutical ABZ and a commercial formulation.

RESULTS

Poloxamer 407 increased exponentially ABZ solubility, in about 400% when 95% w/w of polymer compared with its absence. Solid dispersions initial dissolution rate was three to 20-fold higher than physical mixtures, the drug and the commercial formulation. All the solid dispersions required less than 2.2 min to reach an 80% of ABZ dissolution, while the commercial formulation needed around 40 min.

CONCLUSION

Solid dispersions improved ABZ solubility and dissolution rate, which could result in a faster absorption and an increased bioavailability.

摘要

目的

开发以泊洛沙姆407为载体的固体分散体,以改善阿苯达唑(ABZ)的溶解度和溶出曲线。

方法

制备ABZ/泊洛沙姆固体分散体,并对溶出曲线进行数学建模,与物理混合物、药用ABZ和市售制剂进行比较。

结果

泊洛沙姆407使ABZ溶解度呈指数增加,与无聚合物时相比,当聚合物含量为95%(w/w)时,溶解度增加约400%。固体分散体的初始溶出速率比物理混合物、药物和市售制剂高3至20倍。所有固体分散体达到80% ABZ溶出所需时间少于2.2分钟,而市售制剂需要约40分钟。

结论

固体分散体改善了ABZ的溶解度和溶出速率,这可能导致更快的吸收和提高生物利用度。

相似文献

1
Development and in vitro evaluation of solid dispersions as strategy to improve albendazole biopharmaceutical behavior.作为改善阿苯达唑生物药剂学行为策略的固体分散体的开发及体外评价
Ther Deliv. 2018 Sep;9(9):623-638. doi: 10.4155/tde-2018-0037.
2
Albendazole solid dispersions prepared using PEG6000 and Poloxamer188: formulation, characterization and evaluation.采用聚乙二醇 6000 和泊洛沙姆 188 制备阿苯达唑固体分散体:制剂、表征和评价。
Pharm Dev Technol. 2020 Nov;25(9):1043-1052. doi: 10.1080/10837450.2020.1783553. Epub 2020 Jul 3.
3
Enhanced dissolution and systemic availability of albendazole formulated as solid dispersions.制备固体分散体提高阿苯达唑的溶出度和全身生物利用度。
Pharm Dev Technol. 2013 Mar-Apr;18(2):434-42. doi: 10.3109/10837450.2012.693509. Epub 2012 Jun 7.
4
Improved albendazole dissolution rate in pluronic 188 solid dispersions.提高阿苯达唑在泊洛沙姆 188 固体分散体中的溶出速率。
AAPS PharmSciTech. 2010 Dec;11(4):1518-25. doi: 10.1208/s12249-010-9517-6. Epub 2010 Oct 14.
5
Hot melt extrusion versus spray drying: hot melt extrusion degrades albendazole.热熔挤出法与喷雾干燥法:热熔挤出法会使阿苯达唑降解。
Drug Dev Ind Pharm. 2017 May;43(5):797-811. doi: 10.1080/03639045.2016.1220577. Epub 2016 Oct 20.
6
A novel hot-melt extrusion formulation of albendazole for increasing dissolution properties.一种用于提高溶出性能的阿苯达唑新型热熔挤出制剂。
Int J Pharm. 2016 Feb 29;499(1-2):175-185. doi: 10.1016/j.ijpharm.2016.01.006. Epub 2016 Jan 6.
7
Albendazole solid dispersions against alveolar echinococcosis: a pharmacotechnical strategy to improve the efficacy of the drug.阿苯达唑固体分散体治疗细粒棘球蚴病:提高药物疗效的药剂学策略。
Parasitology. 2020 Aug;147(9):1026-1031. doi: 10.1017/S0031182020000670. Epub 2020 Apr 27.
8
Preparation and Characterization of Poloxamer 407 Solid Dispersions as an Alternative Strategy to Improve Benznidazole Bioperformance.制备和表征泊洛沙姆 407 固体分散体作为改善苯并咪唑生物性能的替代策略。
J Pharm Sci. 2018 Nov;107(11):2829-2836. doi: 10.1016/j.xphs.2018.06.027. Epub 2018 Jul 10.
9
Effect of semicrystalline polymers on self-emulsifying solid dispersions of nateglinide: in vitro and in vivo evaluation.半结晶聚合物对那格列奈自乳化固体分散体的影响:体内外评价
Drug Dev Ind Pharm. 2018 Jan;44(1):56-65. doi: 10.1080/03639045.2017.1371739. Epub 2017 Sep 11.
10
Free flowing solid dispersions of the anti-HIV drug UC 781 with Poloxamer 407 and a maximum amount of TPGS 1000: investigating the relationship between physicochemical characteristics and dissolution behaviour.抗艾滋病病毒药物UC 781与泊洛沙姆407及最大量TPGS 1000的自由流动固体分散体:研究理化特性与溶出行为之间的关系。
Eur J Pharm Sci. 2008 Sep 2;35(1-2):104-13. doi: 10.1016/j.ejps.2008.06.010. Epub 2008 Jul 3.

引用本文的文献

1
Combining solubilization and controlled release strategies to prepare pH-sensitive solid dispersion loaded with albendazole: and studies.结合增溶和控释策略制备载阿苯达唑的pH敏感固体分散体:及研究
Front Vet Sci. 2024 Dec 20;11:1522856. doi: 10.3389/fvets.2024.1522856. eCollection 2024.
2
Modeling and evaluation of ivermectin release kinetics from 3D-printed tablets.3D 打印片剂中伊维菌素释放动力学的建模与评价。
Ther Deliv. 2024;15(11):845-858. doi: 10.1080/20415990.2024.2412511. Epub 2024 Oct 16.
3
Recent Patents on Solid Dispersions Emphasize Promising Benefits in Solubility Enhancement of Poorly Water-soluble Drugs.
固体分散体的最新专利强调了在提高难溶性药物溶解度方面的显著优势。
Recent Pat Nanotechnol. 2025;19(2):216-240. doi: 10.2174/0118722105229356231030065938.
4
Bioadhesive eutectogels supporting drug nanocrystals for long-acting delivery to mucosal tissues.支持药物纳米晶体长效递送至粘膜组织的生物粘附低共熔凝胶。
Mater Today Bio. 2022 Oct 25;17:100471. doi: 10.1016/j.mtbio.2022.100471. eCollection 2022 Dec 15.
5
Stiripentol Enteric Solid Dispersion-Loaded Effervescent Tablets: Enhanced Dissolution, Stability, and Absorption.依托泊苷肠溶性固体分散体-负载泡腾片:增强的溶解、稳定性和吸收。
AAPS PharmSciTech. 2022 May 10;23(5):141. doi: 10.1208/s12249-022-02261-5.
6
Albendazole solid dispersions against alveolar echinococcosis: a pharmacotechnical strategy to improve the efficacy of the drug.阿苯达唑固体分散体治疗细粒棘球蚴病:提高药物疗效的药剂学策略。
Parasitology. 2020 Aug;147(9):1026-1031. doi: 10.1017/S0031182020000670. Epub 2020 Apr 27.
7
Drug resistance in liver flukes.肝吸虫耐药性。
Int J Parasitol Drugs Drug Resist. 2020 Apr;12:39-59. doi: 10.1016/j.ijpddr.2019.11.003. Epub 2020 Jan 10.