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

Factors Affecting Dissolution: Drug Permeability, Stability and Stereochemistry

248
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...
248
Factors Affecting Dissolution: Particle Size and Effective Surface Area01:23

Factors Affecting Dissolution: Particle Size and Effective Surface Area

957
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...
957
Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism01:21

Factors Affecting Dissolution: Polymorphism, Amorphism and Pseudopolymorphism

372
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...
372
Factors Influencing Drug Absorption: Physicochemical Parameters01:22

Factors Influencing Drug Absorption: Physicochemical Parameters

390
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...
390
Factors Influencing Drug Absorption: Drug Dissolution01:27

Factors Influencing Drug Absorption: Drug Dissolution

651
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...
651

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Updated: Aug 22, 2025

Author Spotlight: Process Development for the Spray-Drying of Probiotic Bacteria and Evaluation of the Product Quality
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Itraconazole Amorphous Solid Dispersion Tablets: Formulation and Compaction Process Optimization Using Quality by

Hetvi Triboandas1, Kendal Pitt1, Mariana Bezerra1

  • 1Leicester School of Pharmacy, De Montfort University, Leicester LE1 9BH, UK.

Pharmaceutics
|November 11, 2022
PubMed
Summary
This summary is machine-generated.

This study developed itraconazole (ITZ) amorphous solid dispersions (ASDs) using hot-melt extrusion and inorganic salts to enhance solubility. KCl addition significantly improved tablet disintegration and dissolution, meeting quality targets for patient needs.

Keywords:
amorphous solid dispersion (ASD)hot-melt extrusion (HME)itraconazole (ITZ)quality by design (QbD)solubility enhancementtablet compaction

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Area of Science:

  • Pharmaceutical Technology
  • Drug Delivery Systems
  • Materials Science

Background:

  • BCS Class II drugs like itraconazole (ITZ) have poor solubility, necessitating formulation strategies for enhanced bioavailability.
  • Amorphous solid dispersions (ASDs) are a key approach to improve the solubility of poorly soluble drugs.
  • Hot-melt extrusion (HME) is an effective technique for producing ASDs.

Purpose of the Study:

  • To enhance the solubility and dissolution of itraconazole (ITZ) by creating amorphous solid dispersions (ASDs) with Kollidon® VA64 (KOL).
  • To investigate the role of inorganic kosmotropic salts in facilitating tablet disintegration and dissolution of ITZ-KOL ASDs.
  • To optimize tablet formulations using Quality by Design (QbD) principles for immediate-release applications.

Main Methods:

  • Production of ITZ-KOL ASDs via hot-melt extrusion (HME).
  • Formulation of tablets incorporating inorganic salts (KCl, NaCl, KBr, KHCO3, KH2PO4) to modulate disintegration and dissolution.
  • Application of Design of Experiments (DoE) to optimize tablet formulations and compaction processes.
  • Evaluation of tablet properties including tensile strength, disintegration time, and drug release.

Main Results:

  • The addition of inorganic salts, particularly KCl, significantly improved the disintegration and dissolution of ITZ-KOL ASD tablets.
  • Tablets containing KCl demonstrated acceptable tensile strength (>1.7 MPa) and rapid disintegration (<15 min).
  • Optimized formulations met Quality Target Product Profile (QTPP) requirements for immediate-release tablets, with rapid drug release achieved for both round and oblong shapes.

Conclusions:

  • Inorganic salts, such as KCl, are crucial for developing fast-disintegrating and enhanced-dissolving tablets of itraconazole amorphous solid dispersions.
  • Quality by Design (QbD) principles enabled the successful development and optimization of ITZ-KOL ASD tablet formulations.
  • The developed formulations offer flexibility in tablet shape, accommodating diverse patient needs for immediate-release itraconazole therapy.