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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...
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Theories of Dissolution: Diffusion Layer Model01:15

Theories of Dissolution: Diffusion Layer Model

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Dissolution, the process by which drug particles dissolve in a solvent, is explained by the diffusion layer model, a theoretical framework that simulates the absorption of oral drugs and allows us to analyze experimental data.
This process starts with a thin layer, saturated with the drug, forming at the interface between the solid and liquid. The solute then diffuses from this layer into the main solution. The Noyes-Whitney equation suggests that the rate of dissolution relies on the diffusion...
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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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In Vitro Drug Dissolution: Alternative Methods01:17

In Vitro Drug Dissolution: Alternative Methods

152
Alternative drug dissolution methods include the rotating bottle, intrinsic dissolution test, peristalsis, and the Franz diffusion cell method. The rotating bottle method involves meticulously rotating tightly capped controlled-release beads in a temperature-controlled bath. Periodic decanting of samples allows for residue assay, followed by refilling with fresh medium and testing at various pH levels to emulate the gastrointestinal tract conditions.In contrast, the intrinsic dissolution test...
152
Drug Dissolution: Requirements and Profile Comparison01:14

Drug Dissolution: Requirements and Profile Comparison

176
The acceptance criteria for dissolution profile data are anchored in Q values, representing the percentage of drug dissolved within a specified period. This assessment unfolds in three stages:First Stage: The test passes if all six drug dosage units are equal to or greater than Q plus 5%; otherwise, the sample proceeds to the second stage.Second Stage: The average of twelve units must be equal to or greater than Q, with no unit falling below Q - 15% to pass; if not, it progresses to the final...
176
Drug Delivery: Enteral Route01:18

Drug Delivery: Enteral Route

1.4K
The enteral drug administration involves three primary routes: oral, sublingual, and buccal. Oral ingestion is the most prevalent, safe, economical, and convenient method for drug administration. However, it has certain drawbacks, including limited absorption due to the drug's low water solubility or poor membrane permeability, possible emesis from GI mucosa irritation, destruction of drugs by digestive enzymes or low gastric pH, and irregular absorption along with food or other drugs.
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Transport Properties of Ibuprofen Encapsulated in Cyclodextrin Nanosponge Hydrogels: A Proton HR-MAS NMR Spectroscopy Study
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Oral controlled release dosage forms: dissolution versus diffusion.

Marival Bermejo1, Barbara Sanchez-Dengra1, Marta Gonzalez-Alvarez1

  • 1Department of Engineering, Pharmacokinetics and Pharmaceutical Technology Area, Miguel Hernandez University , Elche, Spain.

Expert Opinion on Drug Delivery
|April 7, 2020
PubMed
Summary

Controlled release (CR) dosage forms offer tailored drug delivery by modifying pharmacokinetic profiles. Selecting the right release mechanism balances API properties, desired targets, and formulation challenges for successful clinical trials.

Keywords:
Oral controlled releasediffusiondissolutionformulation selectionpredictive dissolutionrelease kinetics

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems

Background:

  • Controlled release (CR) dosage forms modify drug pharmacokinetic (PK) profiles, avoiding immediate release (IR) of active pharmaceutical ingredients (APIs).
  • CR technologies are crucial for managing chronic diseases, narrow therapeutic index drugs, and targeted gastrointestinal (GI) delivery.

Purpose of the Study:

  • To review diffusion and dissolution-limited CR systems, including release kinetics, formulation strategies, and marketed examples.
  • To discuss physiological variables impacting drug release and available in vitro dissolution techniques.
  • To provide expert opinion on selecting appropriate release mechanisms and optimizing CR dosage form design.

Main Methods:

  • Review of diffusion and dissolution-limited controlled release systems.
  • Analysis of formulation strategies and marketed/developing examples.
  • Examination of physiological variables (pH, volume, composition, physical forces, transit times) affecting release.
  • Review of in vitro dissolution techniques.

Main Results:

  • Diffusion and dissolution are key mechanisms in CR systems, often used in combination.
  • Physiological variables and in vitro methods significantly influence drug release profiles.
  • No single release mechanism is universally superior; selection depends on specific requirements.

Conclusions:

  • Choosing the optimal CR release mechanism requires balancing target needs, API characteristics, and formulation complexity.
  • Integrating in vivo predictive dissolution, mathematical modeling, and formulation data can enhance the success rate of new CR drug candidates in clinical trials.