开发一种体外脂解模型,用于在脂基配方的消化过程中实时分析药物度
Lotte Ejskjær1, Patrick J O'Dwyer1, Callum D Ryan1
1School of Pharmacy, University College Cork, College Road, Cork, Ireland.
概括
这项研究引入了一种新的小规模方法,用于在消化过程中分析基于脂质的药物配方. 它使用替代性脂酶实时监测药物度,提供更快,更准确的方法.
科学领域:
- 制药科学 制药科学
- 药物输送系统 药物输送系统
- 生物化学 生物化学
背景情况:
- 评估肠道消化对基于脂质的口服药物配方的影响对于预测体内药物性能至关重要.
- 传统的体外脂解方法,如pH-stat技术,缺乏高吞吐量,可能会引入人工物.
- 需要小规模的高通量方法来实时监测消化过程中的药物度.
研究的目的:
- 探索在基于脂质的配方消化过程中小规模,线性紫外线检测药物度的替代性脂酶和消化条件.
- 为了比较使用Palatase® 20000 L的新方法与经典的猪胰腺脂解方法的性能.
- 建立一种实时监测药物度在分散和消化阶段的方法.
主要方法:
- 对各种固定和预溶解的脂质酶进行查,以消化基于脂质的配方.
- 替代性脂酶和猪胰腺蛋白之间的消化动力学和药物释放概况的比较.
- 使用MicroDISS ProfilerTM进行线性紫外线分析,在分散和消化过程中实时监测药物度.
主要成果:
- 帕拉塔斯 20000 升的消化动力学与猪胰腺素相当.
- 在基脂基配方消化过程中确定的药物度在新和古典方法之间是相似的.
- 对于中长链脂基配方,实时监测药物度可以在分散1小时和消化3小时内实现.
结论:
- 使用Palatase® 20000 L的小型线性紫外线检测方法为研究基于脂质的药物配方提供了与经典脂解的可行替代方案.
- 这种方法可以实时监测药物度,最大限度地减少与广泛的样本准备相关的工件.
- 该方法有助于更深入地了解在口服脂质制剂的分散和消化过程中的动态药物释放.
相关概念视频
01:16Methods for Studying Drug Absorption: In vitro
234
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...
234
01:09Methods for Studying Drug Absorption: In situ
234
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,...
234
01:15Theories of Dissolution: Diffusion Layer Model
769
Dissolution, the process by which drug particles dissolve in a solvent, is explained by the diffusion layer model, a theoretical framework that simulates the absorption of oral drugs and allows us to analyze experimental data.
This process starts with a thin layer, saturated with the drug, forming at the interface between the solid and liquid. The solute then diffuses from this layer into the main solution. The Noyes-Whitney equation suggests that the rate of dissolution relies on the diffusion...
This process starts with a thin layer, saturated with the drug, forming at the interface between the solid and liquid. The solute then diffuses from this layer into the main solution. The Noyes-Whitney equation suggests that the rate of dissolution relies on the diffusion...
769
01:27Factors Influencing Drug Absorption: Drug Dissolution
511
The pharmacokinetic journey of drugs from solid oral dosage forms into systemic circulation is multifaceted. It begins with disintegration, a prerequisite ensuring a solid dosage form's subdivision into minute particles. Dissolution occurs next as these granulated entities solubilize in gastrointestinal fluids. This solubilization is crucial for the succeeding stage, permeation, which describes the traversal of the drug across the intestinal membrane and its subsequent entry into the blood...
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