卡普里奥尔90是一种有效的肠道吸收增强剂,用于体内胰岛素,当与其他辅助剂相结合时,可以有效增强胰岛素的吸收
Fiona McCartney1, Philippe Caisse2, Camille Dumont2
1UCD School of Veterinary Medicine and UCD Conway Institute, University College Dublin, Belfield, Dublin 4, Ireland.
International journal of pharmaceutics
|October 29, 2025
概括
当与HCO-60或Gelucire® 44/14.4等溶解剂相结合时,Capryol® 90可以增强肠道透率. 这种组合显著改善了胰岛素的生物可用性,并降低了老鼠的血糖水平,表明了口服配方的潜力.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 生物制药生物制药公司
背景情况:
- 烯基醇单烯酸乙烯 ester Capryol® 90,具有较低的水溶性,限制其作为肠道透增强剂用于口服配方的使用.
- 开发口服递送系统需要新型辅助剂来克服吸收不良并提高生物可用性.
研究的目的:
- 评估Capryol® 90作为类的肠道透增强剂的潜力.
- 为了调查与溶解剂,化麻油 (HCO-60) 或Gelucire® 44/14的同时使用是否可以增强Capryol® 90的透增强能力.
主要方法:
- 在Ussing腔室中使用隔离的老鼠结肠粘膜进行ex vivo研究,以测量 [14C] - 曼尼托尔的跨体电阻 (TEER) 和表面透性 (Papp).
- 在体内研究中,使用Capryol® 90,单独或与HCO-60或Gelucire® 44/14一起,将胰岛素注入大鼠结环中.
- 监测大鼠血糖水平和计算相对胰岛素生物可用性.
主要成果:
- 与单独使用的药物相比,Capryol® 90与HCO-60或Gelucire® 44/14的同时使用显著降低了TEER (>80%) 并增加了 [14C] - 曼尼托透率 (11.7至17.1倍).
- 在体内,与Capryol® 90和HCO-60或Gelucire® 44/14联合使用的胰岛素导致大鼠血糖水平大幅下降.
- 胰岛素的相对生物利用率为Capryol® 90/HCO-60的约4.1%,而Capryol® 90/Gelucire® 44/14.4的相对生物利用率为3.8%.
结论:
- 卡普里奥尔90显示出作为口服和BCS III类药物配方的肠道透增强剂的潜力.
- 通过添加HCO-60或Gelucire® 44/14等溶解剂,Capryol® 90的增强透效应得到了显著的增强.
- 这种组合策略为改善具有挑战性的药物分子的口服输送提供了有希望的方法.
相关概念视频
Bioavailability Enhancement: Drug Stability Enhancement and GI Retention
193
Body:Improving a drug's stability in the gastrointestinal (GI) tract is paramount for enhancing its bioavailability and therapeutic effectiveness. Various strategies are employed to protect the drug from the harsh gastric milieu and to ensure its release and absorption at the desired site within the GI tract.Polymer coatings are one such method used to shield drugs from the stomach's acidic environment. By preventing premature drug release, these coatings improve the bioavailability of unstable...
193
Bioavailability Enhancement: Drug Permeability Enhancement
183
Body:After oral administration, poor permeability often limits the rate at which drugs are absorbed through the intestinal epithelium. Enhancing drug permeability is crucial for effective therapy, and several strategies have been developed to overcome this challenge.One effective strategy involves the use of lipid-based formulations. These formulations enhance dissolution and solubility, targeting physiological mechanisms to increase drug absorption. This includes stimulating bile salt...
183
Insulin Formulations: Types and Delivery
642
Insulin preparations are categorized by their duration of action into short-acting and long-acting types. Two strategies are used to modify insulin's absorption and pharmacokinetic profile: slowing the absorption post-subcutaneous injection, or altering human insulin's amino acid sequence or protein structure. These changes retain the insulin's ability to bind to the insulin receptor, but alter its behavior in solution or after injection.
Short-acting insulins are divided into...
Short-acting insulins are divided into...
642
Factors Influencing Drug Absorption: Physicochemical Parameters
806
The physicochemical characteristics of drugs play a crucial role in formulating stable and bioavailable drug products. The solubility of a drug, governed by the varying pH along the GI tract and its dissociation constant (pKa), is pivotal in determining its ionization state and absorption rate. Notably, weak acids and bases remain unionized and are absorbed more rapidly.
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
Enhanced drug absorption can be achieved by reducing particle sizes and increasing surface areas, thereby facilitating...
806
Bioavailability Enhancement: Drug Solubility Enhancement
212
Body:Bioavailability is a critical factor in determining a drug's effectiveness. It refers to the proportion of a drug that enters the circulation when introduced into the body and is, as a result, able to have an active effect. Enhancing bioavailability is essential for drugs with poor solubility, as it can significantly impact their therapeutic efficacy. Various methods are employed to increase the solubility of drugs, thereby enhancing their bioavailability.Micronization and nanonization are...
212
Methods for Studying Drug Absorption: In vitro
569
In vitro experiments are crucial for understanding the transport and absorption of drugs through biological materials. These studies employ varied methods such as the diffusion cell method, the everted sac technique, and the everted ring technique.
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
The diffusion cell method uses a two-compartment cell, including a donor compartment with the drug solution, which simulates the environment where the drug is applied, and a receptor compartment with a buffer solution, which simulates the environment...
569


