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Related Concept Videos

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...
415
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...
1.1K
Factors Affecting Dissolution: Particle Size and Effective Surface Area01:23

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: Physicochemical Parameters01:22

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...
225
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

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 Influencing Drug Absorption: Pharmaceutical Parameters01:28

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

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Solubility of Hydrophobic Compounds in Aqueous Solution Using Combinations of Self-assembling Peptide and Amino Acid
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Solubilization techniques used for poorly water-soluble drugs.

Bing Xie1, Yaping Liu1, Xiaotong Li1

  • 1School of Pharmacy, China Pharmaceutical University, Nanjing 2111198, China.

Acta Pharmaceutica Sinica. B
|December 12, 2024
PubMed
Summary

Improving the solubility of poorly water-soluble drugs is crucial for drug development. This review explores various techniques, including carriers and crystallization, to enhance drug solubility and bioavailability.

Keywords:
CocrystalsInorganic carriersIonic liquidsLipid-based carriersNanocrystalsPolymer-based carriersPoorly water-soluble drugsSolubilization techniques

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery
  • Medicinal Chemistry

Background:

  • Approximately 40% of approved drugs and 90% of drug candidates exhibit poor water solubility.
  • Low solubility significantly limits drug efficacy and bioavailability, posing a major challenge in pharmaceutical development.
  • Addressing poor water solubility is critical for advancing drug development and therapeutic applications.

Purpose of the Study:

  • To provide a comprehensive overview of conventional and advanced solubilization techniques for poorly water-soluble drugs.
  • To detail the mechanisms, recent advances, and clinical translation potential of various solubility enhancement strategies.
  • To guide the selection of appropriate solubilization approaches, dosage forms, and administration routes for poorly water-soluble drugs.

Main Methods:

  • Review of conventional solubilization techniques: solubilizers, hydrotropes, cosolvents, prodrugs, salt modification, micronization, cyclodextrin inclusion, and solid dispersions.
  • Detailed examination of advanced strategies: crystallization, ionic liquids, and polymer-based, lipid-based, and inorganic-based carriers.
  • Summarization of approved carrier materials and successful applications in poorly water-soluble drugs.

Main Results:

  • Conventional and advanced techniques offer diverse mechanisms to improve drug solubility and bioavailability.
  • Several carrier materials and drug formulations have demonstrated successful clinical translation.
  • Emerging techniques show significant promise for overcoming solubility challenges.

Conclusions:

  • Effective solubilization is key to unlocking the therapeutic potential of poorly water-soluble drugs.
  • A systematic approach to selecting solubilization techniques, considering drug properties and intended use, is essential.
  • Continued research and development in novel drug delivery systems are vital for addressing the unmet needs of poorly water-soluble drugs.