PhD Scientific Days 2026

Pharmaceutical Sciences and Health Technologies 3.

Production and Testing of High Active Ingredient Tablets

Name of the presenter

Berenji, Péter

Institute/workplace of the presenter

Semmelweis University, Faculty of Pharmacy, Department of Pharmaceutics

Authors

Péter Berenji¹
1: Semmelweis University, Faculty of Pharmacy, Department of Pharmaceutics

Text of the abstract

Introduction: Granulation is a critical operation in the manufacture of solid oral dosage forms, especially for tablets with high active pharmaceutical ingredient (API) content. It improves flowability, compressibility, and content uniformity, while preventing ingredient sedimentation and reducing dusting. For micronized APIs, producing homogeneous granules with excellent rheological properties is essential for high-quality final products.
Aims: The strategic goal is to improve patient compliance by developing smaller, easier-to-swallow tablets with reduced excipient content. This study investigates different molecular weight polyethylene glycols (PEG 4000, 6000, 8000) as binders to produce wet granulation formulations with high API content (>85%).
Methods: Granules of five different APIs were produced using a Procept laboratory high-shear wet granulator and a Romaco Ventilus 2.5L fluid bed dryer. Granulation solutions contained purified water and PEG (1-10% w/w calculated on the API). The dried granules were regranulated on a 2 mm sieve and characterized for moisture content, bulk/tapped density, flowability, and particle size distribution using Malvern Mastersizer 3000. Tablets were then compressed using a Korsch single-punch press with a uniform external phase.
Result: PEG-based granulation yielded granules with narrower particle size distributions and superior rheological properties compared to traditional polyvinyl alcohol-based reference samples. While Metamizole sodium showed unexpected rheological behavior, Diosmin, Paracetamol, and Levetiracetam granules exhibited excellent flowability. These results led to improved tableting consistency, uniform weight distribution, and high-strength tablets with appropriate disintegration times.
Conclusion: Polyethylene glycols of various molecular weights are suitable binders for high-dose formulations across diverse chemical profiles. The technology enables the production of tablets with reduced size and high API loads, potentially enhancing patient adherence.
Funding: „PROJECT NO. EKÖP-24-KDP-2 HAS BEEN IMPLEMENTED WITH THE SUPPORT PROVIDED BY THE MINISTRY OF CULTURE AND INNOVATION OF HUNGARY FROM THE NATIONAL RESEARCH, DEVELOPMENT AND INNOVATION FUND, FINANCED UNDER THE 2024-2.1.2 UNIVERSITY RESEARCH SCHOLARSHIP PROGRAM - COOPERATIVE DOCTORAL PROGRAM FUNDING SCHEME.”