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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: Particle Size and Effective Surface Area01:23

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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

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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Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

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

Noncompartmental Analysis: Mean Transit, Absorption and Dissolution Time

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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.
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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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Formulation, Development, and Optimization of Fast Dissolving Tablets Containing Tapentadol Hydrochloride.

Chandrashekar Thalluri1, Mallikarjun Vasam2, Rajkumar Jampala3

  • 1Department of Pharmaceutics, Faculty of Pharmaceutical Science, Assam Downtown University, Gandhinagar, Panikhaiti, Guwahati-781026, Assam, India.

Pharmaceutical Nanotechnology
|December 24, 2024
PubMed
Summary

This study developed optimized Tapentadol fast-dissolving tablets (FDTs) using super disintegrants, achieving rapid disintegration and enhanced drug release for better patient compliance. The best formulation followed Fickian diffusion for drug release.

Keywords:
Tapentadolexpert design.fast dissolving tabletsin-vitro dissolutionsuper disintegrating agents

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Area of Science:

  • Pharmaceutical Sciences
  • Drug Delivery Systems

Background:

  • Tapentadol hydrochloride is a key analgesic for moderate to severe pain.
  • Fast-dissolving tablets (FDTs) improve patient compliance through rapid pain relief.
  • Optimizing FDTs requires careful selection of super disintegrants and formulation parameters.

Purpose of the Study:

  • To fabricate and optimize Tapentadol hydrochloride fast-dissolving tablets (FDTs).
  • To evaluate the impact of super disintegrants (croscarmellose sodium and crospovidone) on FDT properties.
  • To determine the optimal formulation using Response Surface Methodology (RSM).

Main Methods:

  • Formulation of nine Tapentadol hydrochloride FDTs (TH1-TH9) using direct compression.
  • Optimization of super disintegrant concentrations (croscarmellose sodium, crospovidone) via RSM.
  • Evaluation of disintegration time, drug release (Q15, Q30), and drug release kinetics using DD Solver.

Main Results:

  • The TH5 formulation demonstrated the fastest disintegration and highest drug release.
  • Super disintegrants significantly enhanced Tapentadol hydrochloride solubility and dissolution rate.
  • Drug release from the optimized TH5 formulation followed first-order kinetics and Fickian diffusion.

Conclusions:

  • Super disintegrants are critical for optimizing FDT disintegration time and dissolution profiles.
  • The optimized TH5 formulation offers rapid disintegration and drug release, enhancing patient compliance.
  • RSM is an effective tool for optimizing FDT formulations with confirmed stability.