• 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

热熔挤出技术在利用中评估甲芬那酸制剂的大鼠适口性、药效学作用和生物利用度。

Rat palatability, pharmacodynamics effect and bioavailability of mefenamic acid formulations utilizing hot-melt extrusion technology.

机构信息

Department of Pharmaceutics, College of Pharmacy, King Saud University , Riyadh , Saudi Arabia.

Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University , Alkharj , Saudi Arabia.

出版信息

Drug Dev Ind Pharm. 2019 Oct;45(10):1610-1616. doi: 10.1080/03639045.2019.1645161. Epub 2019 Jul 29.

DOI:10.1080/03639045.2019.1645161
PMID:31311329
Abstract

Mefenamic acid (MA) has been reported as a weakly soluble drug which presents weak absorption upon oral administration using conventional formulations. Solid dispersions (SDs) have been investigated extensively in literature for enhancing the solubility and bioavailability of weakly-soluble molecules. Hence, the aim of proposed study was to prepare MA novel formulations in the form of SDs using hot-melt extrusion technology in order to enhance its palatability, bioavailability, and pharmacodynamics effects/anti-inflammatory efficacy. Various SDs of MA were prepared using hot-melt extrusion technology, characterized physically and investigated for dissolution tests. Optimized SD formulations of MA were being subjected to palatability, pharmacodynamics, and pharmacokinetic studies in rats. Optimized SD of MA showed significant rat palatability tastes as compared with pure and marketed MA ( < .05). Anti-inflammatory efficacy of 20% SD and 25% SD of MA was found to be 86.44 and 89.83%, respectively, in comparison with 74.57 and 78.24% by pure MA and marketed MA, respectively. The anti-inflammatory efficacy of optimized SD was found to be significant as compared with pure and marketed MA ( < .05). The oral absorption of MA from optimized 20% SD was also noted as statistically significant as compared with pure MA ( < .05). The relative bioavailability of MA from 20 and 25% SDs was 2.97 and 2.24-folds higher than pure MA. The results of this study suggested that SDs prepared using hot-melt extrusion technology are capable to enhance palatability, anti-inflammatory efficacy, and oral bioavailability of MA in comparison with pure drug.

摘要

甲芬那酸(MA)已被报道为一种低溶解度药物,常规制剂口服后吸收性较弱。固体分散体(SDs)在文献中已被广泛研究,以提高低溶解度分子的溶解度和生物利用度。因此,本研究旨在通过热熔挤出技术制备 MA 的新型 SD 制剂,以提高其口感、生物利用度和药效/抗炎效果。采用热熔挤出技术制备了各种 MA 的 SD,并对其进行了物理性质表征和溶解试验研究。MA 的优化 SD 制剂正在大鼠中进行适口性、药效学和药代动力学研究。与纯 MA 和市售 MA( < .05)相比,MA 的优化 SD 表现出显著的大鼠口感。MA 的 20%SD 和 25%SD 的抗炎效果分别为 86.44%和 89.83%,而纯 MA 和市售 MA 的抗炎效果分别为 74.57%和 78.24%。与纯 MA 和市售 MA 相比,优化 SD 的抗炎效果具有统计学意义( < .05)。从优化的 20%SD 中口服吸收 MA 的效果也被认为与纯 MA 相比具有统计学意义( < .05)。20%和 25%SD 中 MA 的相对生物利用度分别比纯 MA 高 2.97 倍和 2.24 倍。本研究结果表明,与纯药物相比,热熔挤出技术制备的 SD 能够提高 MA 的口感、抗炎效果和口服生物利用度。

相似文献

1
Rat palatability, pharmacodynamics effect and bioavailability of mefenamic acid formulations utilizing hot-melt extrusion technology.热熔挤出技术在利用中评估甲芬那酸制剂的大鼠适口性、药效学作用和生物利用度。
Drug Dev Ind Pharm. 2019 Oct;45(10):1610-1616. doi: 10.1080/03639045.2019.1645161. Epub 2019 Jul 29.
2
Soluplus®/TPGS-based solid dispersions prepared by hot-melt extrusion equipped with twin-screw systems for enhancing oral bioavailability of valsartan.采用配备双螺杆系统的热熔挤出法制备的基于Soluplus®/TPGS的固体分散体,用于提高缬沙坦的口服生物利用度。
Drug Des Devel Ther. 2015 May 22;9:2745-56. doi: 10.2147/DDDT.S84070. eCollection 2015.
3
Development of hot melt co-formulated antimalarial solid dispersion system in fixed dose form (ARLUMELT): Evaluating amorphous state and in vivo performance.固定剂量形式的热熔共配制抗疟固体分散体系统(ARLUMELT)的研发:评估非晶态及体内性能。
Int J Pharm. 2015 Dec 30;496(1):137-56. doi: 10.1016/j.ijpharm.2015.09.069. Epub 2015 Oct 22.
4
Formulation of aripiprazole-loaded pH-modulated solid dispersions via hot-melt extrusion technology: In vitro and in vivo studies.载阿立哌唑的 pH 调控固体分散体的热熔挤出技术制备:体外和体内研究。
Int J Pharm. 2019 Jan 10;554:302-311. doi: 10.1016/j.ijpharm.2018.11.005. Epub 2018 Nov 3.
5
In Vivo Performance of Innovative Polyelectrolyte Matrices for Hot Melt Extrusion of Amorphous Drug Systems.用于热熔挤出无定形药物体系的创新聚电解质基质的体内性能。
Mol Pharm. 2020 Aug 3;17(8):3053-3061. doi: 10.1021/acs.molpharmaceut.0c00485. Epub 2020 Jul 13.
6
Influence of the microwave technology on solid dispersions of mefenamic acid and flufenamic acid.微波技术对甲芬那酸和氟芬那酸固体分散体的影响。
PLoS One. 2017 Jul 31;12(7):e0182011. doi: 10.1371/journal.pone.0182011. eCollection 2017.
7
Development of Solid Dispersion by Hot Melt Extrusion Using Mixtures of Polyoxylglycerides With Polymers as Carriers for Increasing Dissolution Rate of a Poorly Soluble Drug Model.熔融挤出法制备固体分散体-聚氧甘油酯与聚合物混合物作为载体以提高难溶性药物模型的溶出速率。
J Pharm Sci. 2019 Feb;108(2):888-896. doi: 10.1016/j.xphs.2018.09.019. Epub 2018 Sep 23.
8
Amorphous solid dispersions of cyclosporine A with improved bioavailability prepared via hot melt extrusion: Formulation, physicochemical characterization, and in vivo evaluation.采用热熔挤出法制备提高生物利用度的环孢素 A 无定形固体分散体:配方、理化性质评价及体内评价。
Eur J Pharm Sci. 2022 Jan 1;168:106036. doi: 10.1016/j.ejps.2021.106036. Epub 2021 Oct 9.
9
Influence of Plasdone S630 Ultra-an Improved Copovidone on the Processability and Oxidative Degradation of Quetiapine Fumarate Amorphous Solid Dispersions Prepared via Hot-Melt Extrusion Technique.聚维酮 S630Ultra-一种改良共聚维酮对富马酸喹硫平无定形固体分散体热熔挤出工艺及氧化降解的影响。
AAPS PharmSciTech. 2021 Jun 28;22(5):196. doi: 10.1208/s12249-021-02069-9.
10
Hot-Melt Extrusion: a Roadmap for Product Development.热熔挤出:产品开发路线图。
AAPS PharmSciTech. 2021 Jun 17;22(5):184. doi: 10.1208/s12249-021-02017-7.

引用本文的文献

1
Potential of solid dispersions to enhance solubility, bioavailability, and therapeutic efficacy of poorly water-soluble drugs: newer formulation techniques, current marketed scenario and patents.固体分散体提高难溶性药物溶解度、生物利用度和疗效的潜力:较新技术、现行市售情况和专利。
Drug Deliv. 2020 Nov 9;27(1):1625-1643. doi: 10.1080/10717544.2020.1846638.