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相关概念视频

Factors Influencing Drug Absorption: Pharmaceutical Parameters01:28

Factors Influencing Drug Absorption: Pharmaceutical Parameters

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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...
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Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

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Polymorphism refers to the existence of a drug substance in multiple crystalline forms, known as polymorphs. Recently, this term has been expanded to include solvates (forms containing a solvent), amorphous forms (non-crystalline forms), and desolvated solvates (forms from which the solvent has been removed).
Some polymorphic crystals possess lower aqueous solubility than their amorphous counterparts, leading to incomplete absorption. For instance, the oral suspension of Chloramphenicol, which...
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Factors Affecting Dissolution: Particle Size and Effective Surface Area01:23

Factors Affecting Dissolution: Particle Size and Effective Surface Area

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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...
708
Biopharmaceutics and Pharmacokinetics: Overview01:28

Biopharmaceutics and Pharmacokinetics: Overview

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Understanding drugs, drug products, and their performance in pharmaceutical science is pivotal. Drugs, whether simple molecules or complex compounds, are designed to interact with the body's biological systems to diagnose, treat, or prevent diseases. Drug products include various delivery systems such as tablets, capsules, injections, and inhalers. The performance of these drug products is gauged by their ability to deliver the active ingredient to the desired site of action at the...
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Factors Influencing Drug Absorption: Drug Dissolution01:27

Factors Influencing Drug Absorption: Drug Dissolution

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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...
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Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

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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...
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使用理性设计优化儿科配方:探索无形固体分散技术与特尔比纳芬化作为案例研究.

Izabelle Amorim Ferreira Boza1, Stéfani Laise da Silva1, Nicolly Bittencourt Guedes2

  • 1Department of Chemistry, Center for Physical and Mathematical Sciences, Federal University of Santa Catarina, Florianópolis, SC, 88040-900, Brazil.

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概括

由于其溶解度较低,为特比纳芬化物 (TER) 开发儿科抗真菌配方具有挑战性. 研究人员确定Soluplus®是无形固体分散的有希望的载体,增强了儿童的TER溶解性和生物可用性.

关键词:
无形固体分散的无形固体分散口服药物管理口服药物管理儿科配方的儿童配方理性的设计理性的设计.溶解度 溶解度 溶解度 溶解度特尔比纳芬化水化合物

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科学领域:

  • 制药科学 制药科学
  • 药物运输 药物运输 药物运输
  • 儿科配方 儿科配方 儿科配方

背景情况:

  • 儿科配方面临着独特的挑战,特别是对于像特比纳芬化 (TER) 这样的药物,这是一种具有较低水溶性的抗真菌剂.
  • 头炎是一种常见的儿科真菌感染,需要有效的口服治疗,但TER的溶解性差阻碍了口服生物可用性.

研究的目的:

  • 合理选择合适的,经过儿科批准的载体,以提高TER的表面溶解度.
  • 使用喷雾干燥开发TER的无形固体分散 (ASD),以改善儿科患者的口服生物可用性.

主要方法:

  • 评估溶解度参数,平衡溶解度,以及用于载体选择的儿科剂量数.
  • 使用了Plasdone S-360 ULTRA®,HPMCAS L和Soluplus®作为潜在的载体.
  • 使用各种技术,描述药物载体相互作用和固态特性.
  • 用选择的载体进行喷雾干燥的TER的准备ASD.

主要成果:

  • TER的溶解度依赖于pH值,在pH值6.5的缓冲剂中观察到的最高溶解度为10%的Soluplus®.
  • 在6岁以上的儿童中,Soluplus®产生的儿科用剂量数最少 (0.23).
  • 喷雾干燥的ASD显著提高了TER的表面溶解度,并保持了长时间的超和.
  • 没有观察到相变或显著的药物载体相互作用.

结论:

  • 索鲁普卢斯 (Soluplus®) 是一种适合用于开发儿科口服配方TER无形固体分散物的载体.
  • 使用Soluplus®的TER喷雾干燥ASD为改善儿童口服生物可用性和疗效提供了一个有希望的策略.
  • 这种方法解决了为儿科患者开发有效的口服抗真菌治疗的挑战.