统计优化的聚合物膜Eletriptan化和伊托普里德化:一个活体药物动力学研究
Awaji Y Safhi1, Waqar Siddique2, Muhammad Zaman3
1Department of Pharmaceutics, College of Pharmacy, Jazan University, Jazan 45142, Saudi Arabia.
Pharmaceuticals (Basel, Switzerland)
|November 25, 2023
概括
针对埃利特里普坦化 (EHBR) 和伊托普里德化 (ITHC) 的新口膜显著提高了药物的生物可用性. 这些快速溶解的膜可以改善偏头痛的治疗和患者的遵从性.
科学领域:
- 制药技术 制药技术 制药技术
- 药物输送系统 药物输送系统
- 药理动力学 药理动力学
背景情况:
- 偏头痛严重影响日常生活.
- 目前的治疗方法可能在生物可用性和患者服药性方面存在局限性.
- 开发先进的药物输送系统对于有效的偏头痛管理至关重要.
研究的目的:
- 开发和评估立即释放的Eletriptan化 (EHBR) 和伊托普里德化 (ITHC) 的聚合物口膜.
- 提高这些药物治疗偏头痛的生物可用性和治疗疗效.
- 通过更方便,更有效的药物输送方法来提高患者的服药性.
主要方法:
- 聚合物口腔薄膜的配方,包括EHBR和ITHC.
- 在体外评估包括表面形态 (SEM),机械强度,分解时间 (DT) 和总溶解时间 (TDT).
- 在白色子身上进行体内药理动力学研究,以评估Cmax,AUC和MRT等参数.
主要成果:
- SEM证实在准备的片中表面光滑,药物分布均.
- 薄膜表现出极好的机械稳定性和快速分解 (DT: 13 ± 1 秒) 和溶解 (TDT: 42.6 ± 0.75 秒).
- 与口服溶液相比,体内研究表明Cmax显著增加 (130 ng/mL对于ITHC,119 ng/mL对于EHBR),这表明生物可用性得到改善.
结论:
- 成功地为EHBR和ITHC开发了稳定,快速起作用的口腔膜.
- 口腔膜配方可通过口腔粘膜增强药物透和生物可用性.
- 改善的药理动力学特征表明治疗潜力增加和患者对偏头痛治疗的遵从性增加.
相关概念视频
One-Compartment Open Model for IV Bolus Administration: General Considerations
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The one-compartment model is a pharmacokinetic tool that models the body as a single, uniform compartment, facilitating the understanding of drug distribution and elimination. This model is particularly beneficial for intravenous (IV) bolus administration, where the drug rapidly circulates throughout the body.
The drug's presence in the body is defined by an equation representing the difference between the rates of drug entry and exit. Key parameters—elimination rate constant,...
The drug's presence in the body is defined by an equation representing the difference between the rates of drug entry and exit. Key parameters—elimination rate constant,...
210
One-Compartment Open Model for IV Bolus Administration: Estimation of Elimination Rate Constant, Half-Life and Volume of Distribution
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The one-compartment open model is a simplified approach used in pharmacokinetics to understand the distribution and elimination of a drug administered through an intravenous bolus. This model assumes rapid drug dispersal throughout the body and elimination using a first-order process. Key pharmacokinetic parameters, such as the elimination rate constant (k), half-life (t1/2), and the apparent volume of distribution (Vd), can be estimated from this model. The elimination rate is calculated...
270
Drug Delivery: Enteral Route
463
The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
463
Two-Compartment Open Model: IV Bolus Administration
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The two-compartment model for intravenous (IV) bolus administration illustrates drug distribution in the body, subdividing it into central and peripheral compartments. This model operates on the concept of two-compartment kinetics. The drug's plasma concentration shows a bi-exponential decline following IV bolus administration, signaling the presence of two disposition processes: distribution and elimination.
The disparity between drug input and the sum of drug transfer rates between...
The disparity between drug input and the sum of drug transfer rates between...
533
One-Compartment Open Model for IV Bolus Administration: Estimation of Clearance
80
Clearance is a key pharmacokinetic parameter that quantifies the volume of body fluid from which a drug is entirely removed within a specific time frame. It is crucial in assessing how a drug is eliminated from the body and has critical clinical applications.
In the one-compartment open model for intravenous (IV) bolus administration, clearance is estimated by dividing the elimination rate by the plasma drug concentration. This equation leverages the elimination rate constant and the apparent...
In the one-compartment open model for intravenous (IV) bolus administration, clearance is estimated by dividing the elimination rate by the plasma drug concentration. This equation leverages the elimination rate constant and the apparent...
80
Methods for Studying Drug Absorption: In vitro
235
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...
235


