通过微针阵列补丁通过皮肤递送瑞扎特里普坦:准备,表征和ex-vivo/in-vivo研究
Suhair S Al-Nimry1, Ahlam Z Alkilani2, Nareman A Alda'ajeh1
1Department of Pharmaceutical Technology, Jordan University of Science and Technology, Irbid, Jordan.
Pharmaceutical development and technology
|August 19, 2024
概括
利扎特里普坦水凝微针提供了更好的输送,绕过了第一通代谢,并增强了对偏头痛治疗的吸收. 这种透皮系统的生物可用性与口服利萨特里普坦相比显著更高.
科学领域:
- 制药科学 制药科学
- 生物材料工程 生物材料工程
- 药物输送系统 药物输送系统
背景情况:
- 口服利扎特里普坦经历了广泛的第一通代谢.
- 偏头痛期间的胃静止延迟了口服药物的吸收.
- 通过皮肤输送系统为克服这些局限性提供了一个有希望的替代方案.
研究的目的:
- 准备和评估含有瑞萨特里普坦的水凝微针,用于通过皮肤输送.
- 为了增强皮肤透,避免瑞三的第一通代谢.
- 评估新型微针配方的疗效和生物可用性.
主要方法:
- 利扎特里普坦水凝微针是使用微型成型技术制造的,其中含有不同度的氧甲基纤维素和甲型凝.
- 配方的特点是机械强度,封装效率和体外药物释放.
- 在生体内皮肤吸收和相对生物利用性研究在老鼠中进行.
主要成果:
- 成功制备了利扎特里普坦水凝微针 (F1-F5),具有有利的机械性能,可用于皮肤插入.
- 在体外研究显示,24小时内药物的累积释放率高 (93.1-100%).
- 优化的F3配方表现出优越的胀,机械强度,受控释放,相对于口服瑞萨特里普坦,相对于口服瑞萨特里普坦,相对生物利用率为179.59%.
结论:
- 里扎特里普坦装载的水凝微针提供了一个有效的透皮药物递送系统.
- 这种方法成功地绕过了第一通代谢,并增强了瑞扎特里普坦的透.
- 开发的微针系统具有显著的潜力,可以提高偏头痛管理中的治疗效果.
相关概念视频
01:22Drug Delivery: Miscellaneous Routes
329
Drug delivery methods like oral inhalation, nasal sprays, transdermal patches, eye drops, intravitreal injection, and rectal administration provide localized effects with reduced toxicity.
Oral inhalation and nasal sprays swiftly transfer drugs across the respiratory epithelium's mucosal layer. Inhaled glucocorticoids and bronchodilators directly target lung conditions such as asthma, while fluticasone nasal spray mitigates allergic rhinitis.
Transdermal patches transport drugs...
Oral inhalation and nasal sprays swiftly transfer drugs across the respiratory epithelium's mucosal layer. Inhaled glucocorticoids and bronchodilators directly target lung conditions such as asthma, while fluticasone nasal spray mitigates allergic rhinitis.
Transdermal patches transport drugs...
329
01:15Non-Oral Extravascular Drug Absorption Routes
207
Non-oral extravascular routes, which encompass sublingual, buccal, topical, intramuscular, and inhalation methods, primarily utilize passive diffusion to transport drugs into the systemic circulation. The absorption rates and effectiveness of these routes depend on the drug's physicochemical properties, as well as the patient's anatomical and pathophysiological state.
Lipophilic drugs that are stable at salivary pH (6) and exhibit minimal binding to the oral mucosa are absorbed more...
Lipophilic drugs that are stable at salivary pH (6) and exhibit minimal binding to the oral mucosa are absorbed more...
207
01:16Drug Delivery: Overview
279
The selection of a drug's delivery route depends upon its physicochemical properties, including lipid or water solubility and ionization, as well as the therapeutic requirement, such as immediate or sustained effect. These routes can be divided into three primary categories: enteral, parenteral, and topical.
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
Enteral delivery involves administering drugs directly through swallowing, sublingual placement, or buccal application. Orally administered drugs predominantly navigate the...
279
01:09Methods for Studying Drug Absorption: In situ
216
In situ experiments, such as the Doluisio method and Single-Pass Perfusion technique, provide critical insights into drug uptake by simulating in vivo conditions for drug absorption.
The Doluisio method involves perfusing a prepared segment of a rat's small intestine with a solution of radiolabeled drug and a non-absorbable marker. This helps to differentiate between absorbed and non-absorbed drug concentrations. The intestinal segment is connected at both ends using tubing and syringes,...
The Doluisio method involves perfusing a prepared segment of a rat's small intestine with a solution of radiolabeled drug and a non-absorbable marker. This helps to differentiate between absorbed and non-absorbed drug concentrations. The intestinal segment is connected at both ends using tubing and syringes,...
216
01:29Drug Delivery: Parenteral Route
450
The parenteral route is a critical method of drug administration. It delivers compounds directly into the systemic circulation and bypasses the gastrointestinal tract. This approach is particularly advantageous for drugs that exhibit poor absorption or instability when administered orally.
There are three primary parenteral routes: intravenous (IV), intramuscular (IM), and subcutaneous (SC). The IV route introduces the drug directly into the bloodstream, ensuring immediate action. The IM route...
There are three primary parenteral routes: intravenous (IV), intramuscular (IM), and subcutaneous (SC). The IV route introduces the drug directly into the bloodstream, ensuring immediate action. The IM route...
450