新的布洛芬胺盐具有更好的溶解性和抗炎作用
Simay Denizkusu1, Ece Sabuncu2, Hande Sipahi2
1Department of Chemistry, Bogazici University, 34342, Bebek, Istanbul, Turkey.
ChemistryOpen
|October 14, 2024
概括
两种新的布洛芬囊胺盐 (IBU-CYS 1和IBU-CYS 2) 显著增强了布洛芬.
科学领域:
- 制药化学 制药化学 制药化学
- 药物输送系统 药物输送系统
- 药用化学 医学化学
背景情况:
- 易布洛芬是一种广泛使用的非类固醇抗炎药物 (NSAID),具有较差的水溶性,限制了其生物可用性和配方选择.
- 开发新的盐形式是改善现有药物的物理化学性质和治疗疗效的常见策略.
- 囊胺是一种二胺,已被探索其潜在的治疗应用,并作为盐形成的对抗剂.
研究的目的:
- 合成和描述新型布洛芬囊胺盐 (IBU-CYS 1和IBU-CYS 2),以提高布洛芬的溶解性和生物可用性.
- 评估合成盐的抗炎潜力和细胞毒性.
- 探索将IBU-CYS2纳入水凝配方以提高药物输送的可行性.
主要方法:
- 在1:1和2:1的比例中合成布洛芬囊胺盐.
- 使用光谱 (NMR,FT-IR,UV-Vis),热 (DSC,TGA,DTA) 和X射线衍射技术进行表征.
- 在水中的体外溶解性研究,评估LPS诱导的RAW264.7巨细胞中的抗炎活性,以及细胞毒性评估.
主要成果:
- 新型布洛芬囊胺盐 (IBU-CYS 1和IBU-CYS 2) 已成功合成和表征.
- 与布洛芬 (0.04 mg/mL) 相比,IBU-CYS 1 和IBU-CYS 2 的水溶性显著改善 (6.11 和 7.81 mg/mL).
- 实验室研究表明,在巨细胞中有效抑制炎症反应,没有观察到细胞毒性,这表明治疗潜力.
结论:
- 合成的布洛芬囊胺盐是一种有前途的方法,可以克服布洛芬的可溶性限制.
- 这些新型盐显示出开发改进的药物配方的潜力,具有增强的生物可用性和抗炎疗效.
- 对水凝封装IBU-CYS2的进一步研究可能会导致先进的药物输送系统.
更多相关视频
08:56Synthesis of a Borylated Ibuprofen Derivative Through Suzuki Cross-Coupling and Alkene Boracarboxylation Reactions
Published on: November 30, 2022
2.7K
13:38Synthesis and Characterization of an Aspirin-fumarate Prodrug that Inhibits NFκB Activity and Breast Cancer Stem Cells
Published on: January 18, 2017
12.2K
相关概念视频
01:29Drugs for Treatment of Ulcerative Colitis in IBD
126
Ulcerative colitis is a chronic inflammatory condition primarily affecting the colon and rectum. The primary drugs used in the treatment of ulcerative colitis are aminosalicylates. They exhibit anti-inflammatory and immunosuppressive properties. They modulate inflammatory mediators and inhibit the activity of nuclear factor κB (NF-κB). Aminosalicylates also reduce inflammation by inhibiting prostaglandin and leukotriene production and decreasing neutrophil chemotaxis and superoxide...
126
01:21Drugs for Treatment of Constipation-Predominant IBS
140
Pharmacological therapies for IBS-C are designed to alleviate abdominal discomfort and enhance bowel function. In patients with IBS-C, fiber supplements may help soften stools and decrease straining, but may also lead to increased gas production and bloating. Osmotic laxatives like milk of magnesia are frequently used to soften stools and increase stool frequency in IBS-C patients. In addition, two drugs approved for use in severe IBS-C adult cases are linaclotide (Linzess) and lubiprostone...
140
01:19Antiasthma Drugs: Leukotriene Modifiers
249
Leukotriene modifiers, or cysteinyl leukotriene receptor antagonists, are medications used to manage chronic asthma. These agents target specific inflammatory mediators produced during arachidonic acid metabolism, an essential process in generating inflammation in the body.
Leukotriene modifiers work through two distinct mechanisms:
Leukotriene modifiers work through two distinct mechanisms:
249
01:21Drugs for Treatment of Crohn's Disease in IBD Using Glucocorticoids
97
Glucocorticoids, a class of anti-inflammatory drugs, are pivotal in treating moderate to severe Crohn's disease by inducing remission. They exhibit their anti-inflammatory action by inhibiting the production of inflammatory cytokines such as tumor necrosis factor (TNF)-α, interleukin (IL)-1, and chemokines like IL-8. In addition, they reduce the expression of inflammatory cell adhesion molecules and inhibit gene transcription of nitric oxide synthase, phospholipase A2, cyclooxygenase-2...
97
01:27Combined Effects of Drugs: Synergism
3.7K
Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
Such synergistic combinations...
Such synergistic combinations...
3.7K
01:17Drugs for Treatment of Diarrhea-Predominant IBS
151
Diarrhea-predominant irritable bowel syndrome (IBS-D) is a subtype of IBS characterized primarily by frequent, loose, or watery stools, abdominal pain, and abdominal discomfort. Therapeutic approaches to managing IBS-D include dietary changes, stress management techniques, and pharmaceutical interventions.
Two specific drugs used in the treatment are alosetron (Lotronex) and eluxadoline (Viberzi). Alosetron, a 5-HT3 antagonist, works by slowing the movement of stools in the gut, reducing bowel...
Two specific drugs used in the treatment are alosetron (Lotronex) and eluxadoline (Viberzi). Alosetron, a 5-HT3 antagonist, works by slowing the movement of stools in the gut, reducing bowel...
151