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Related Concept Videos

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 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: 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...
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Factors Influencing Drug Absorption: Drug Dissolution01:27

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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

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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 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.
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Navigating the Solution to Drug Formulation Problems at Research and Development Stages by Amorphous Solid Dispersion

Devika Tripathi1, Manjunatha Prabhu B H2, Jagannath Sahoo3

  • 1Pranveer Singh Institute of Technology (Pharmacy), Uttar Pradesh, Kanpur, India.

Recent Advances in Drug Delivery and Formulation
|December 8, 2023
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Summary

Amorphous Solid Dispersions (ASDs) enhance drug solubility by preventing recrystallization. Understanding drug-polymer interactions is key for stable, effective oral drug delivery systems.

Keywords:
Amorphous solid dispersioncrystallinity predictiondissolution behaviorphysical stabilitystabilization manufacturing strategies.thermodynamic concern

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Area of Science:

  • Pharmaceutical Sciences
  • Materials Science

Background:

  • Amorphous Solid Dispersions (ASDs) are crucial for enhancing drug solubility, particularly for poorly water-soluble compounds.
  • The amorphous state offers higher apparent solubility due to increased molecular mobility and free volume, but faces challenges with thermodynamic instability and recrystallization.

Purpose of the Study:

  • To provide a comprehensive review of Amorphous Solid Dispersions (ASDs) for oral drug delivery.
  • To highlight formulation challenges, manufacturing impacts, drug-polymer interactions, and miscibility factors critical for ASD development.

Main Methods:

  • Review of advanced analytical techniques for monitoring drug crystallinity and solubility, including ssNMR, ATR-FTIR, Raman, and dielectric spectroscopy.
  • Discussion of advanced manufacturing techniques like hot melt extrusion, KinetiSol, electro spraying, and electrospinning for ASD production.

Main Results:

  • ASDs significantly improve oral bioavailability of poorly soluble drugs.
  • Successful ASD development hinges on careful selection of polymers and understanding drug-polymer miscibility and interactions.
  • Monitoring drug solids during preparation, storage, and application is essential for stability.

Conclusions:

  • ASDs represent a promising strategy for oral drug delivery, but their complexity requires thorough understanding of formulation and process parameters.
  • Predicting ASD stability and performance relies heavily on comprehending drug-polymer interactions.
  • Continuous downstream processing and advanced manufacturing methods are vital for consistent ASD production.