含有多林的欧德拉吉特纳米颗粒用于腹刺激性肠综合征:配方,优化使用盒式设计,以及抗腹活性
Md Khalid Anwer1, Mohammed Muqtader Ahmed1, Mohammed F Aldawsari1
1Department of Pharmaceutics, College of Pharmacy, Prince Sattam Bin Abdulaziz University, Al-Kharj 11942, Saudi Arabia.
Pharmaceutics
|May 27, 2023
概括
这项研究开发了含有eluxadoline (ELD) 的eudragit纳米粒子 (ENPs),以改善腹刺激性肠综合征 (IBS-D) 的口服输送. 优化的ENP2配方显著降低了老鼠的腹症状,显示出增强的治疗潜力.
科学领域:
- 制药科学 制药科学
- 纳米技术纳米技术
- 药理学 药理学是指药理学的学科.
背景情况:
- 埃卢克萨多林 (ELD) 对腹性刺激性肠综合征 (IBS-D) 是有前途的,但其溶解性和生物可用性不佳.
- 开发有效的口服药物输送系统对于提高ELD的治疗疗效至关重要.
研究的目的:
- 为了制定和优化含有eluxadoline的eudragit纳米粒子 (ENPs).
- 在IBS-D.小鼠模型中评估优化ENP的抗腹活性.
主要方法:
- 用Eluxadoline装载的eudragit纳米粒子 (ENPs) 通过使用Box-Behnken设计进行了准备和优化.
- 物理化学表征包括粒子大小,PDI和泽塔潜力分析.
- 在体内对抗腹疗效的评估是在慢性克制压力诱导的IBS-D大鼠模型中进行的.
主要成果:
- 优化的配方 (ENP2) 显示了有利的粒子大小 (286 ± 3.67 nm),PDI (0.263 ± 0.01) 和泽塔电位 (31.8 ± 3.18 mV).
- 根据希古奇模型,ENP2表现出持续的药物释放.
- 在体内研究表明,与纯ELD相比,ENP2显著降低了排便频率和疾病活性指数.
结论:
- 基于Eudragit的聚合物纳米颗粒提供了一种有前途的方法来增强口服输送的eluxadoline.
- 开发的ENP显示出有效治疗易怒肠综合征与腹的巨大潜力.
相关概念视频
Drugs for Treatment of Diarrhea-Predominant IBS
223
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...
223
Drugs for Treatment of Constipation-Predominant IBS
236
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...
236
Drugs Affecting GI Tract Motility: Opioids as Antidiarrheal Agents
255
Diarrhea, a condition marked by frequent loose or watery bowel movements, can be triggered by multiple factors such as viral or bacterial infections, food intolerances, anxiety, medications, and digestive disorders. Symptoms may include abdominal pain, bloating, nausea, and cramping. Severe or prolonged diarrhea can lead to complications like electrolyte imbalances, malnutrition, and dehydration if left untreated.
Opioids, widely used antidiarrheal agents, mitigate diarrhea by slowing down...
Opioids, widely used antidiarrheal agents, mitigate diarrhea by slowing down...
255
Drugs Affecting GI Tract Motility: Adsorbents as Antidiarrheal Agents
260
Diarrhea is characterized by the occurrence of frequent, watery bowel movements. Various factors can trigger diarrhea, including viral or bacterial infections, foodborne illnesses, side effects from certain medications, and underlying digestive disorders. If not adequately managed, diarrhea can lead to complications such as dehydration, electrolyte imbalances, and nutrient deficiencies. Severe diarrhea can lead to significant weight loss, malnutrition, and weakened immune function.
Adsorbents...
Adsorbents...
260
Drugs Affecting GI Tract Motility: Bulk-Forming and Stimulant Laxatives
259
Laxatives enhance bowel movements and alleviate constipation. They augment the stool's bulk, stimulate intestinal muscle contractions, draw water into the intestines, or soften the stool. There are five key types of laxatives: bulk laxatives, stimulant laxatives, osmotic laxatives, stool softeners, and lubricant laxatives.
Bulk-forming laxatives, such as psyllium, methylcellulose, and polycarbophil, absorb water in the intestine, increasing stool bulk and promoting bowel movement. This...
Bulk-forming laxatives, such as psyllium, methylcellulose, and polycarbophil, absorb water in the intestine, increasing stool bulk and promoting bowel movement. This...
259
Drugs Affecting GI Tract Motility: Other Laxatives
293
Laxatives are primarily used to alleviate constipation, a common gastrointestinal disorder characterized by infrequent bowel movements and difficulty passing stools. They work by various mechanisms to increase the volume or frequency of bowel movements. The primary modes of action of laxatives include increasing stool bulk, softening the stool, stimulating intestinal motility, and osmotically drawing water into the intestines.
Osmotic or saline laxatives, like magnesium hydroxide or milk of...
Osmotic or saline laxatives, like magnesium hydroxide or milk of...
293


