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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 Influencing Drug Absorption: Pharmaceutical Parameters01:28

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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: Drug Permeability, Stability and Stereochemistry01:20

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

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

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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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Factors Influencing Drug Absorption: Physicochemical Parameters01:22

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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...
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萨基纳维尔 - 皮皮林乳用混合物:制备,表征和溶解特征

Cinira Fandaruff1, María Isabel Quirós-Fallas2,3, José Roberto Vega-Baudrit2

  • 1Instituto de Tecnologías Emergentes y Ciencias Aplicadas (ITECA), UNSAM-CONICET, Escuela de Ciencia y Tecnología, Laboratorio de Cristalografía Aplicada, Av. 25 de Mayo 1169, San Martín 1650, Provincia de Buenos Aires, Argentina.

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概括

抗艾滋病毒药物萨基纳维尔基 (SQV) 的溶解率通过与皮佩林 (PIP) 形成欧性混合物而得到改善. 这种方法提高了药物的溶解性和生物可用性,为改善SQV提供了一个有希望的策略.

关键词:
溶解增强增强方法 溶解增强方法优德的混合物 优德的混合物皮佩里尼 (Piperine) 是一种可怕的药物.粉末衍射衍射的方法萨基纳维尔 萨基纳维尔 是一种小角X射线散射的小角度X射线散射.固态特征的固态特征表征

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科学领域:

  • 制药科学 制药科学
  • 材料科学 材料科学 材料科学
  • 药物运输 药物运输 药物运输

背景情况:

  • 萨基纳维尔基 (SQV) 具有较差的水溶性和较低的绝对生物可用性,限制了其治疗疗效.
  • 提高难溶药物的溶解率对于提高它们的口服吸收和生物可用性至关重要.

研究的目的:

  • 通过欧性混合物形成来提高萨基纳维尔基 (SQV) 的溶解率和生物可用性.
  • 为了研究SQV-piperine (PIP) 体系统的固态特性和溶解行为.

主要方法:

  • 使用液体辅助研磨和差分扫描热量计 (DSC) 选辅形材料.
  • 使用DSC,粉末X射线衍射 (PXRD),小角度X射线散射 (SAXS),里埃变换红外光谱学 (FT-IR) 和扫描电子显微镜 (SEM) 描述了欧阳系统.
  • 与纯SQV相比,评价了菌混合物的溶解概况.

主要成果:

  • 在SQV和piperine (PIP) 之间成功地形成了以0.6:0.4.4的摩尔比率为0.6:0.4.4的欧系统.
  • 萨克斯分析显示,欧混合物中的晶体结构发生了变化,尽管PXRD没有显示整体结构变化.
  • FT-IR证实在固态中没有分子相互作用.
  • 在SQV和PIP中,SQV的溶解率显著提高,SQV的55%在45分钟内溶解,而纯SQV的42%是如此.

结论:

  • 与皮佩林 (PIP) 形成欧性混合物是一种有效的策略,可以提高萨基纳维尔基 (SQV) 的溶解率.
  • 由于SQV-PIP的溶解系统的溶解特性得到了改进,因此有可能提高saquinavir的生物可用性.
  • 这项研究强调了辅体选择和优化结晶在优化难溶药物的输送方面的有用性.