相关实验视频

Updated: May 26, 2025

A Workflow for Lipid Nanoparticle LNP Formulation Optimization using Designed Mixture-Process Experiments and Self-Validated Ensemble Models SVEM

A Workflow for Lipid Nanoparticle LNP Formulation Optimization using Designed Mixture-Process Experiments and Self-Validated Ensemble Models SVEM

Published on: August 18, 2023

基于QbD的配方开发和评估基于脂质纤维素的延长释放型多颗粒素 cinitapride 和其无PBPK建模

Muhammad Umair Saleem¹, Muhammad Harris Shoaib¹, Faaiza Qazi¹

¹Department of Pharmaceutics, Faculty of Pharmacy and Pharmaceutical Sciences, University of Karachi, Karachi 75270, Pakistan.

International journal of biological macromolecules

|February 23, 2025

概括

使用甘单酸盐 (GMS) 和乙烯纤维素 (EC) 的延长释放酸颗粒被开发用于功能性消化不良. 优化的颗粒显示出受控释放和可比的生物利用性,提供了潜在的单剂量治疗.

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
胃肠病学胃肠病学

背景情况:

功能性消化不良和胃肠道反流症需要有效的长期治疗选择.
目前的治疗方法可能在有效性或剂量频率上有局限性.
延长释放配方的开发可以改善患者的遵守性和治疗结果.

研究的目的:

开发和优化使用甘单酸盐 (GMS) 和乙烯纤维素 (EC) 的延长释放型酸基质颗粒.
评估药物释放动力学,物理特征和优化配方的in silico生物可用性.
评估开发的颗粒对于治疗功能性消化不良和胃肠道反流症的适用性.

主要方法:

用GMS和EC作为主要辅助剂的挤出球化制备颗粒.
采用中央复合设计 (CCD) 来优化配方变量,包括EC度,球化速度和时间.
评估了药物释放,颗粒球状性,面积比,化学相互作用,热稳定性和在中药物动力学建模 (PBPK).

主要成果:

乙基纤维素有效控制了多达12小时的酸释放,通过烧结将突发释放最小化.
颗粒球度和面积比显示与球化参数有直接的相关性.
优化的配方 (Fpred) 遵循Korsmeyer-Peppas模型,表明不同pH值的非fickian扩散.
在基PBPK建模预测可比的相对生物利用性与即时释放片,具有特定的Cmax,Tmax和AUC值.

结论:

基于脂质纤维素的延长释放性酸矩阵颗粒成功开发和优化.
该配方表现出理想的药物释放特征和物理性质.
开发的延长释放颗粒显示出作为功能性消化不良和胃肠道逆流疾病的有效单剂方案的潜力.

关键词:

中心复合设计设计锡尼塔普里德的使用方法挤出-球体化 - 球体化 PBPKK PBPK 的意思是什么意思颗粒颗粒是一种颗粒.在QbD中,它是QbD.

更多相关视频

Assembly of Cell Mimicking Supported and Suspended Lipid Bilayer Models for the Study of Molecular Interactions

Assembly of Cell Mimicking Supported and Suspended Lipid Bilayer Models for the Study of Molecular Interactions

Published on: August 3, 2021

A Package of Established Analytical Tools to Investigate the Solid-State Alteration of Lipid-Based Excipients

A Package of Established Analytical Tools to Investigate the Solid-State Alteration of Lipid-Based Excipients

Published on: August 9, 2022

相关概念视频

Physiological Pharmacokinetic Models: Incorporating Hepatic Transporter-Mediated Clearance

Physiological Pharmacokinetic Models: Incorporating Hepatic Transporter-Mediated Clearance

Drug transporters are critical in drug absorption, distribution, and excretion processes. They should be included in physiological-based pharmacokinetic (PBPK) models, which help predict human drug disposition. However, predicting this is challenging during drug development, especially when liver transport is involved. However, with a realistic representation of body transport processes, an accurate model may be possible.
A recent model describes pravastatin's hepatobiliary excretion,...

One-Compartment Open Model for IV Bolus Administration: General Considerations

One-Compartment Open Model for IV Bolus Administration: General Considerations

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,...

Factors Influencing Drug Absorption: Drug Dissolution

Factors Influencing Drug Absorption: Drug Dissolution

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...

Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH

Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH

Drug absorption within the gastrointestinal (GI) tract is a complex process influenced by several critical factors, including the site pH, the drug's dissociation constant (pKa), and the drug's lipophilicity. The GI tract exhibits a pH gradient, with an acidic environment in the stomach and a more alkaline environment in the small intestine. This pH variation directly affects the ionization state of drugs.
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...

Two-Compartment Open Model: IV Bolus Administration

Two-Compartment Open Model: IV Bolus Administration

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...

Factors Influencing Drug Absorption: Pharmaceutical Parameters

Factors Influencing Drug Absorption: Pharmaceutical Parameters

Solid dosage forms such as tablets and capsules undergo rigorous manufacturing processes to ensure stability and effectiveness. Their dissolution and absorption properties are influenced significantly by the choice of excipients (inactive ingredients that serve various roles in the formulation), and the methodology applied during production. The manufacturing parameters, such as compression force and granulation techniques, significantly affect dissolution rates. Elevated compression forces...