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相关概念视频

Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH01:21

Factors Affecting Dissolution: Drug pKa, Lipophilicity and GI pH

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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...
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Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists01:28

Chemotherapy-Induced Nausea and Vomiting: Neurokinin-1 Receptor Antagonists

264
Neurokinin 1 (NK1) receptors are distributed across the GI tract, vagal afferents, and key CNS regions including the central vomiting center and chemoreceptor trigger zone (CTZ) Chemotherapy agents stimulate enterochromaffin cells in the gastrointestinal (GI) tract to release large amounts of substance P (SP). SP is a neuropeptide released by specific sensory nerves in response to many different stressors, including those in the GI mucosa affected by chemotherapy.  SP binds and activates...
264
Factors Influencing Drug Absorption: Drug Dissolution01:27

Factors Influencing Drug Absorption: Drug Dissolution

721
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...
721
Factors Affecting Solubility04:01

Factors Affecting Solubility

33.9K
Compared with pure water, the solubility of an ionic compound is less in aqueous solutions containing a common ion (one also produced by dissolution of the ionic compound). This is an example of a phenomenon known as the common ion effect, which is a consequence of the law of mass action that may be explained using Le Chȃtelier’s principle. Consider the dissolution of silver iodide:
33.9K
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

268
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...
268
Factors Affecting Dissolution: Particle Size and Effective Surface Area01:23

Factors Affecting Dissolution: Particle Size and Effective Surface Area

1.0K
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...
1.0K

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相关实验视频

Updated: Sep 14, 2025

Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
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阿普雷皮坦:关于增强溶解性的审查

Lata Kothapalli1, Navdeep Singh1, Abhay Upare2

  • 1Department of Pharmaceutical Chemistry and Quality Assurance, Dr. D.Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune, Maharashtra, India.

Recent advances in drug delivery and formulation
|July 23, 2025
PubMed
概括

阿普雷皮坦 (APT) 是一种NK-1抗剂,面临着亲肠道输送的溶解性挑战. 通过纳米配方等技术提高APT溶解度对于其作为抗癌疗法的潜力以及对CINV的管理至关重要.

关键词:
这是一种抗的药物.这是一种阿普雷皮坦特 (Aprepitant).第五百零五章 没有了这是一种NK-1抗剂.溶解度 溶解度 溶解度 溶解度可溶性增强. 增加可溶性.

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科学领域:

  • 药理学 药理学是指药理学的学科.
  • 药物运输 药物运输 药物运输
  • 在瘤学瘤学.

背景情况:

  • 物质P和神经素 (NK-1) 受体与各种疾病有关.
  • 癌症中NK-1受体过度表达是一个治疗点.
  • 阿普雷皮坦 (APT) 是一种NK-1抗剂,在临床上用于化疗诱导的恶心和吐 (CINV).

研究的目的:

  • 审查阿普雷皮坦 (APT) 的可溶性增强技术.
  • 探索APT作为癌症治疗中的协同作用剂的潜力.
  • 为了应对APT的亲肠道剂型的发展所面临的挑战.

主要方法:

  • 在文献中搜索阿普雷皮坦 (APT) 化学和可溶性增强.
  • 使用的数据库:科学直接,PubMed,本瑟姆,谷歌学者.
  • 关键词:阿普雷皮坦,可溶性,NK1受体,肠道剂型.

主要成果:

  • 审查了改善APT溶解性的方法,包括纳米技术.
  • 创新技术为增强APT生物利用性提供了途径.
  • 讨论了各种可溶性增强技术的挑战和好处.

结论:

  • 由于APT的BCS等级为IV,它面临生物可用性挑战,特别是在内注射方面.
  • 提高溶解度是APT在CINV和癌症治疗中的有效性的关键.
  • 产药 (例如,Fosaprepitant) 和含有辅助剂的纳米配方对亲肠道APT输送有希望.