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Related Concept Videos

Factors Influencing Drug Absorption: Drug Dissolution01:27

Factors Influencing Drug Absorption: Drug Dissolution

649
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...
649
Factors Affecting Dissolution: Particle Size and Effective Surface Area01:23

Factors Affecting Dissolution: Particle Size and Effective Surface Area

939
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...
939
Theories of Dissolution: Diffusion Layer Model01:15

Theories of Dissolution: Diffusion Layer Model

861
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...
861
Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry01:20

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

244
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...
244
Factors Influencing Drug Absorption: Pharmaceutical Parameters01:28

Factors Influencing Drug Absorption: Pharmaceutical Parameters

179
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...
179
Noncompartmental Analysis: Mean Transit, Absorption and Dissolution Time01:02

Noncompartmental Analysis: Mean Transit, Absorption and Dissolution Time

136
When drugs are administered extravascularly, a comprehensive evaluation through noncompartmental analysis becomes imperative. This analytical approach considers various parameters that play a crucial role in understanding the pharmacokinetics of these drugs.
One of the key parameters is the mean transit time (MTT), which refers to the total duration required for drug molecules to transit through the body. MTT is determined by calculating the ratio of the area under the moment curve to the area...
136

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Author Spotlight: Developing a Disposable Dosator for Preclinical Testing of Dry Powder Inhalers in Small Animal Models
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In vitro Dissolution Testing of Rifampicin Powder Formulations For Prediction of Plasma Concentration-Time Profiles

Prakash Khadka1, Ian G Tucker1, Shyamal C Das2

  • 1School of Pharmacy, University of Otago, Adams Building, 18 Frederick Street, P.O. Box 56, Dunedin, 9054, New Zealand.

Pharmaceutical Research
|November 29, 2022
PubMed
Summary
This summary is machine-generated.

Amorphous rifampicin powder showed faster in vitro dissolution than crystalline forms. However, simulations predicted similar in vivo plasma concentrations for both inhaled drug formulations.

Keywords:
amorphous and crystallinedissolutiondry powder inhalersrifampicinsimulation

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Area of Science:

  • Pharmacokinetics
  • Drug Delivery
  • Materials Science

Background:

  • Inhaled drug delivery aims for targeted lung or systemic absorption.
  • Rifampicin formulations require optimization for effective pulmonary delivery.
  • Amorphous and crystalline states impact drug dissolution and bioavailability.

Purpose of the Study:

  • Evaluate in vitro lung dissolution of amorphous vs. crystalline rifampicin in PEO and DPPC.
  • Predict in vivo plasma concentration-time profiles using in vitro dissolution data.
  • Assess the utility of in vitro dissolution testing for inhaled drug formulation design.

Main Methods:

  • Utilized a custom dissolution apparatus for respirable rifampicin particles.
  • Employed STELLA® software for in vivo pharmacokinetic simulations.
  • Applied one-compartment models with first-order or Michaelis-Menten elimination.

Main Results:

  • Amorphous rifampicin formulations exhibited significantly faster in vitro dissolution.
  • Faster dissolution suggested potential for enhanced in vivo absorption and plasma levels.
  • Simulations indicated comparable in vivo plasma concentration-time profiles for both formulations.

Conclusions:

  • Demonstrated the combined use of in vitro dissolution and simulation for predicting inhaled drug pharmacokinetics.
  • Highlighted the potential of these models for designing inhaled formulations with controlled release.
  • Emphasized achieving desired lung retention or systemic absorption through formulation optimization.