• 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

美洛昔康自纳米乳化颗粒(SNEGs):制备、表征、分子模拟及体内抗炎活性评价

Self nanoemulsifying granules (SNEGs) of meloxicam: preparation, characterization, molecular modeling and evaluation of in vivo anti-inflammatory activity.

作者信息

Parekh Vidhi J, Desai Namita D, Shaikh Mushtaque S, Shinde Ujwala A

机构信息

a Department of Pharmaceutics , Bombay College of Pharmacy, Kalina, Santacruz (E) , Mumbai , India.

b Department of Pharmaceutical Analysis , Bombay College of Pharmacy, Kalina, Santacruz (E) , Mumbai , India.

出版信息

Drug Dev Ind Pharm. 2017 Apr;43(4):600-610. doi: 10.1080/03639045.2016.1275665. Epub 2017 Jan 17.

DOI:10.1080/03639045.2016.1275665
PMID:28005437
Abstract

Meloxicam, a BCS class II drug belonging to the class of NSAIDs is indicated in conditions of rheumatoid arthritis, ankylosing spondylitis and osteoarthritis in which rapid onset of drug action is desired to reduce inflammation and pain. The objective of the study was to thus develop Self Nanoemulsifying Granules (SNEGs) of Meloxicam (MLX) for enhancement of solubility; and subsequently dissolution rate, thus aiming for a faster onset of action. Preliminary studies along with molecular modeling studies were carried out for selection of appropriate lipids, surfactants and cosurfactants for the development of MLX-loaded Self Nanoemulsifying preconcentrate (SNEP). A charge inducer was incorporated into the formulation so as to increase the solubility of MLX in lipids and hence, drug loading. A three-factor D-optimal mixture design was used for optimization of MLX loaded SNEP. The role of charge inducer in increasing the drug loading of MLX in SNEDDS was studied by molecular dynamics simulation using Desmond. Optimized SNEP was adsorbed onto solid carriers to form SNEGs for improved stability and enhanced flow properties. Physical characterization studies of SNEGs, in vitro release studies, and in vivo evaluation of anti-inflammatory activity of the optimized formulation were performed. All the results indicated that MLX SNEGs can be a promising alternative to conventional oral NSAIDs therapy because of enhanced dissolution characteristics and subsequent rapid onset of action.

摘要

美洛昔康是一种属于非甾体抗炎药(NSAIDs)类别的BCS II类药物,适用于类风湿性关节炎、强直性脊柱炎和骨关节炎等病症,在这些病症中需要药物作用快速起效以减轻炎症和疼痛。因此,本研究的目的是开发美洛昔康(MLX)的自纳米乳化颗粒(SNEGs)以提高溶解度;进而提高溶出速率,从而实现更快的起效。为了开发载有MLX的自纳米乳化预浓缩物(SNEP),进行了初步研究以及分子建模研究,以选择合适的脂质、表面活性剂和助表面活性剂。将电荷诱导剂加入到制剂中,以增加MLX在脂质中的溶解度,从而提高药物载量。采用三因素D-最优混合设计对载有MLX的SNEP进行优化。使用Desmond通过分子动力学模拟研究了电荷诱导剂在增加SNEDDS中MLX药物载量方面的作用。将优化后的SNEP吸附到固体载体上以形成SNEGs,以提高稳定性并增强流动性。对SNEGs进行了物理表征研究、体外释放研究以及对优化制剂的体内抗炎活性评估。所有结果表明,由于溶出特性增强以及随后起效迅速,MLX SNEGs可能是传统口服NSAIDs疗法的一个有前景的替代方案。

相似文献

1
Self nanoemulsifying granules (SNEGs) of meloxicam: preparation, characterization, molecular modeling and evaluation of in vivo anti-inflammatory activity.美洛昔康自纳米乳化颗粒(SNEGs):制备、表征、分子模拟及体内抗炎活性评价
Drug Dev Ind Pharm. 2017 Apr;43(4):600-610. doi: 10.1080/03639045.2016.1275665. Epub 2017 Jan 17.
2
Utilization of spray drying technique for improvement of dissolution and anti-inflammatory effect of Meloxicam.利用喷雾干燥技术提高美洛昔康的溶出度和抗炎效果。
Pak J Pharm Sci. 2015 Jan;28(1):103-11.
3
Comparison of two self-nanoemulsifying drug delivery systems using different solidification techniques for enhanced solubility and oral bioavailability of poorly water-soluble celecoxib.比较两种使用不同固化技术的自微乳药物传递系统,以提高难溶性塞来昔布的溶解度和口服生物利用度。
Colloids Surf B Biointerfaces. 2024 Sep;241:114044. doi: 10.1016/j.colsurfb.2024.114044. Epub 2024 Jun 17.
4
Statistical modeling, optimization and characterization of solid self-nanoemulsifying drug delivery system of lopinavir using design of experiment.采用实验设计法对洛匹那韦固体自纳米乳化药物递送系统进行统计建模、优化及表征。
Drug Deliv. 2016 Oct;23(8):3027-3042. doi: 10.3109/10717544.2016.1141260. Epub 2016 Feb 16.
5
Nanostructured lipid carriers based nanogel for meloxicam delivery: mechanistic, in-vivo and stability evaluation.基于纳米结构脂质载体的纳米凝胶用于美洛昔康递送:作用机制、体内及稳定性评估
Drug Dev Ind Pharm. 2015;41(8):1368-75. doi: 10.3109/03639045.2014.950586. Epub 2014 Aug 25.
6
Formulation of meloxicam gel for topical application: In vitro and in vivo evaluation.美洛昔康凝胶的制剂研究:体外与体内评价。
Acta Pharm. 2010 Jun;60(2):153-63. doi: 10.2478/v10007-010-0020-0.
7
Characterization and evaluation of self-nanoemulsifying sustained-release pellet formulation of ziprasidone with enhanced bioavailability and no food effect.齐拉西酮自微乳释长效混悬型口服制剂的特性评价及其生物利用度的改善和不受食物影响。
Drug Deliv. 2016 Sep;23(7):2163-2172. doi: 10.3109/10717544.2014.950768. Epub 2014 Aug 22.
8
Surface-adsorbed reverse micelle-loaded solid self-nanoemulsifying drug delivery system of talinolol.他林洛尔的表面吸附反胶束负载固体自纳米乳化药物递送系统
Pharm Dev Technol. 2016 Mar;21(2):131-9. doi: 10.3109/10837450.2014.971379. Epub 2014 Oct 16.
9
A Self-nanoemulsifying Drug Delivery System for Poorly Water Soluble Tolbutamide: Development, Optimization and Pharmacodynamic Studies.一种用于难溶性甲苯磺丁脲的自纳米乳化药物递送系统:研制、优化及药效学研究
Pharm Nanotechnol. 2017;5(4):285-300. doi: 10.2174/2211738505666170915154920.
10
Improved Pharmacodynamic Potential of Rosuvastatin by Self-Nanoemulsifying Drug Delivery System: An in vitro and in vivo Evaluation.自乳化药物传递系统提高瑞舒伐他汀的药效学潜力:体外和体内评价。
Int J Nanomedicine. 2021 Feb 9;16:905-924. doi: 10.2147/IJN.S287665. eCollection 2021.

引用本文的文献

1
Systematic Approach in the Development of Chitosan Functionalized Iloperidone Nanoemulsions for Transnasal Delivery, In Vitro and In Vivo Studies.系统方法在壳聚糖功能化伊洛哌酮纳米乳剂经鼻给药中的应用:体外和体内研究。
AAPS PharmSciTech. 2024 Oct 21;25(8):247. doi: 10.1208/s12249-024-02964-x.
2
Development of a novel intramuscular liposomal injection for advanced meloxicam delivery: Preparation, characterization, pharmacokinetics, pharmacodynamics, and pain assessment in an orthopedic pain model.一种用于美洛昔康高级递送的新型肌肉注射脂质体的研发:在骨科疼痛模型中的制备、表征、药代动力学、药效学及疼痛评估
Int J Pharm X. 2024 Sep 14;8:100284. doi: 10.1016/j.ijpx.2024.100284. eCollection 2024 Dec.
3
Meloxicam in Combating Clinical Mastitis: Nanotechnology-Driven Hope and Opportunities.
美洛昔康治疗临床乳腺炎:纳米技术带来的希望与机遇
J Pharm Bioallied Sci. 2022 Jul-Sep;14(3):121-125. doi: 10.4103/jpbs.jpbs_649_21. Epub 2022 Sep 19.
4
Formulation and Evaluation of Baclofen-Meloxicam Orally Disintegrating Tablets (ODTs) Using Co-Processed Excipients and Improvement of ODTs Performance Using Six Sigma Method.采用共处理赋形剂的巴氯芬-美洛昔康口崩片(ODTs)的配方和评价以及使用六西格玛方法改善 ODTs 性能。
Drug Des Devel Ther. 2021 Oct 16;15:4383-4402. doi: 10.2147/DDDT.S327193. eCollection 2021.
5
Development and Characterization of A New Dimethicone Nanoemulsion and its Application for Electronic Gastroscopy Examination.开发和表征一种新的二甲硅油纳米乳及其在电子胃镜检查中的应用。
Int J Nanomedicine. 2020 Jul 29;15:5405-5416. doi: 10.2147/IJN.S251113. eCollection 2020.