胃浮动持续释放颗粒的开发和表征,以提高帕丘利油的生物可用性
Chen Liu1,2, Yanan Wu2, Yeli Zou2
1General Hospital of Ningxia Medical University, Yinchuan, Ningxia, 750004, China.
Heliyon
|December 13, 2024
概括
这项研究开发了帕丘利油 (PO) 的胃漂浮颗粒,以改善其用于对抗Helicobacter pylori的输送. 这种新的系统增强了PO PO.
科学领域:
- 药理学 药理学是指药理学的学科.
- 材料科学 材料科学 材料科学
- 药物输送系统 药物输送系统
背景情况:
- 来自Pogostemon cablin的帕丘利油 (PO) 显示出对胃肠道感染的保护作用,特别是Helicobacter pylori.
- 局限的口服生物可用性和胃保留阻碍了传统PO配方的疗效.
研究的目的:
- 为帕丘利油开发一个胃浮动,持续释放的多单元系统.
- 增强帕丘利油的胃保留和口服生物可用性,以改善 H. pylori 治疗.
主要方法:
- 使用化二氧化 (CSD) 进行吸附和浮力,使用乙烯基纤维素 (EC) 和基甲基纤维素 (HPMC) 进行持续释放,制备了含油颗粒.
- 颗粒的特征包括油吸附,漂浮性质,药物释放特征,以及在老鼠体内胃保留研究.
- 差分扫描热度计 (DSC) 和里埃变换红外光谱法 (FTIR) 证实了PO和CSD之间的兼容性.
主要成果:
- 中央证券交易所表现出有利的石油吸附和浮力.
- 颗粒显示持续释放 (>90%超过10小时) 没有最初的爆发释放.
- 在体内研究表明,胃留超过7小时,与PO装载粉末相比,帕丘利酒精的生物可用性显著提高.
结论:
- 一个CSD/EC/HPMC矩阵成功地为帕丘利油制造了胃浮动,持续释放的颗粒.
- 这种系统有效地改善了帕丘利油的胃留和口服生物可用性.
- 开发的颗粒代表了一种有前途的策略,用于增强帕丘利油对胃杆菌感染的疗效.
相关概念视频
Factors Influencing Drug Absorption: Pharmaceutical Parameters
119
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...
119
Factors Influencing Drug Absorption: Physicochemical Parameters
225
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...
225
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
174
Orally administered drugs primarily enter the systemic circulation via passive diffusion through the intestinal membranes. The drug's absorption is influenced by drug stability in the gastrointestinal GI tract, membrane permeability, the surface area available for absorption, luminal drug concentration, and residence time in the lumen. Drug permeability can be enhanced by adjusting the lipophilicity, polarity, or molecular size of the drug, promoting its passive transport across intestinal...
174
Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH
1.1K
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...
A drug's pKa and the pH of the gastrointestinal (GI) tract play crucial roles...
1.1K
Factors Affecting Dissolution: Particle Size and Effective Surface Area
727
Dissolution kinetics, an essential aspect of oral drug delivery, is significantly influenced by the drug's particle size. According to the Noyes-Whitney dissolution model, the dissolution rate correlates directly with the drug's surface area. The larger the surface area, the higher the drug's solubility in water, leading to a faster drug dissolution rate. Reducing particle size increases the effective surface area, enhancing the dissolution process. Micronization and nanosizing are...
727
Factors Influencing Drug Absorption: Drug Dissolution
415
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...
415


