皮佩林-基酸作为植物化学抗骨关节炎组合:结构,溶解性和体内抗炎性研究
Ari Sartinah1,2, Hidehiro Uekusa3, Yuto Abekura3
1School of Pharmacy, Bandung Institute of Technology, Bandung 40132, Indonesia.
Heliyon
|June 7, 2024
概括
一个新的多组件系统,Pip-HBA,结合了piperine和4-hydroxybenzoic acid,增强了溶解度和抗炎活性. 这种新型配方显示出作为天然抗炎剂的开发潜力很大.
科学领域:
- 自然产品化学 自然产品化学
- 材料科学 材料科学 材料科学
- 药理学 药理学是指药理学的学科.
背景情况:
- 皮佩林 (Pip) 和4-基酸 (HBA) 是天然化合物,具有已知的抗炎性质.
- 开发新型配方可以提高活性药物成分的疗效和输送.
研究的目的:
- 从皮佩林和4-基酸合成和表征一种新的多组件系统 (Pip-HBA).
- 评估Pip-HBA系统的可溶性和抗炎活性.
主要方法:
- 用溶剂滴滴研磨和蒸发方法用于合成.
- 固态特征包括差异扫描热度计 (DSC),粉末X射线衍光计 (PXRD) 和里埃变换红外光谱法 (FTIR).
- 单晶X射线衍光测量 (SCXRD) 用于详细的结构分析.
主要成果:
- 通过DSC,PXRD和FTIR证实了Pip-HBA多组件系统的形成,其个别组件具有不同的特性.
- SCXRD阐明了新的Pip-HBA系统的三维结构.
- 与单独的piperine相比,Pip-HBA表现出增强的溶解性和优越的抗炎活性.
结论:
- 该Pip-HBA多元件系统代表了一种新的固体形式,具有改进的物理化学和生物特性.
- 该系统显示了作为天然抗炎治疗剂的进一步开发的巨大潜力.
相关概念视频
Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH
1.3K
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...
1.3K
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry
198
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...
198
Factors Influencing Drug Absorption: Physicochemical Parameters
257
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...
257
Combined Effects of Drugs: Synergism
3.8K
Synergism is a useful mechanism where combining two or more drugs is more effective than each constituent used alone. Such combinations are also called supra-additive interactions. The drugs collectively enhance the final therapeutic effect by acting on different targets. Another advantage is that the low dose of each constituent drug is sufficient to achieve the desired effect. This helps reduce the duration of therapy and lower the adverse effects of these drugs.
Such synergistic combinations...
Such synergistic combinations...
3.8K
Factors Influencing Drug Absorption: Drug Dissolution
466
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...
466
Analgesia and Pain Management
579
Pain is critical to various clinical pathologies, provoking an urgent need for effective management. Pain, whether acute or chronic, is a complex neurochemical process. Its alleviation depends on the type, with nonopioid analgesics effective for mild to moderate pain, such as musculoskeletal or inflammatory pain, while neuropathic pain responds best to anticonvulsants, tricyclic antidepressants, or serotonin/norepinephrine reuptake inhibitors. For severe acute or chronic pain, opioids may be...
579


