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Related Concept Videos

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: 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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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...
907
Factors Influencing Drug Absorption: Physicochemical Parameters01:22

Factors Influencing Drug Absorption: Physicochemical Parameters

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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...
336
Solution Concentration and Dilution02:59

Solution Concentration and Dilution

84.9K
The relative amount of a given solution component is known as its concentration. Often, though not always, a solution contains one component with a concentration that is significantly greater than that of all other components. This component is called the solvent and may be viewed as the medium in which the other components are dispersed or dissolved. Solutions in which water is the solvent are, of course, very common on our planet. A solution in which water is the solvent is called an aqueous...
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Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

351
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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Updated: Jul 30, 2025

Manufacture of Concentrated, Lipid-based Oxygen Microbubble Emulsions by High Shear Homogenization and Serial Concentration
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High concentration formulation developability approaches and considerations.

Jonathan Zarzar1, Tarik Khan2, Maniraj Bhagawati3

  • 1Pharmaceutical Development, Genentech Inc, South San Francisco, CA, USA.

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|May 16, 2023
PubMed
Summary
This summary is machine-generated.

Developing high-concentration biologic drugs faces challenges like aggregation and viscosity. New predictive methods, including in-silico tools, accelerate the identification of these liabilities, speeding up clinical development.

Keywords:
Aggregationdevelopabilityhigh concentration formulationsin-silicophysical instabilitysubcutaneous administrationviscosity

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Area of Science:

  • Biopharmaceutical development
  • Protein formulation science
  • Drug delivery systems

Background:

  • Increasing demand for subcutaneous and ocular biologic administration necessitates higher drug concentrations.
  • Higher protein concentrations in drug substance (DS) and drug product (DP) increase risks of aggregation, precipitation, and viscosity.
  • Traditional formulation development is slow and costly due to high material requirements.

Purpose of the Study:

  • To review challenges in developing high-concentration biologic formulations.
  • To highlight advances in predictive analytics for identifying protein liabilities.
  • To discuss in-silico tools for risk assessment and understanding protein behavior at high concentrations.

Main Methods:

  • Review of experimental and in-silico methods for predicting high-concentration liabilities.
  • Focus on low-mass, high-throughput predictive analytics.
  • Examination of advanced in-silico tools and algorithms.

Main Results:

  • Emergence of new experimental and in-silico methods to predict high-concentration liabilities.
  • Advancements in low-mass and high-throughput analytics are available.
  • In-silico tools aid in identifying risks and understanding protein behavior.

Conclusions:

  • New predictive methods accelerate and de-risk the development of high-concentration biologic formulations.
  • Technological advancements enable faster identification of critical physico-chemical liabilities.
  • In-silico approaches are crucial for efficient drug development.