Related Experiment Video
Updated: Jan 7, 2026
05:44
Formation of Dispersible Taohong Siwu Tablets
Published on: February 3, 2023
2.0K
An integrated material-sparing method for determining dilution potential of direct compression tablet fillers
Weeraya Tharanon1, Yiwang Guo2, Jomjai Peerapattana1
1Division of Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Khon Kaen University, Khon Kaen 40002, Thailand.
Journal of Pharmaceutical Sciences
|December 25, 2025
Summary
This study introduces a novel, material-sparing method to assess the "dilution potential" of co-processed glutinous rice starch (CP-GRS) as a direct compression filler. The method successfully determined optimal drug loading for acetaminophen and ibuprofen, ensuring tablet quality and manufacturability.
Area of Science:
- Pharmaceutical Sciences
- Materials Science
- Chemical Engineering
Background:
- Direct compression (DC) tablet formulation requires fillers with optimal flowability and compactibility.
- Understanding the
- dilution potential
- of fillers is crucial for consistent tablet quality and manufacturability across diverse APIs and loadings.
Purpose of the Study:
- To develop and validate an integrated, material-sparing laboratory-scale method for evaluating the dilution potential of co-processed glutinous rice starch (CP-GRS).
- To assess CP-GRS as a DC tablet filler using acetaminophen (APAP) and ibuprofen (IBN) as model drugs.
Main Methods:
- Developed an integrated laboratory-scale method to evaluate filler dilution potential.
- Assessed tablet performance based on friability (<1% weight loss), disintegration time (DT <15 min), and flowability relative to microcrystalline cellulose (Avicel® PH102).
- Determined maximum API loading at critical pressure (Pc) to define dilution potential.
Main Results:
- Granular APAP (gAPAP) loaded up to 34% in CP-GRS at ~240 MPa.
- Fine APAP loaded up to 20% within 143-288 MPa.
- Ibuprofen (IBN) achieved 40% loading between 115-150 MPa.
Conclusions:
- The integrated method efficiently evaluates CP-GRS dilution potential, confirming its suitability as a DC filler.
- This material-sparing approach facilitates early-stage drug development by enabling rapid DC formulation optimization.
- The method's success with APAP and IBN suggests broad applicability for various APIs.
Keywords:
DiluentDilution potentialDirect compressionDisintegration timeExcipientFlowabilityFriabilityMore Related Videos
Related Concept Videos
01:28Factors Influencing Drug Absorption: Pharmaceutical Parameters
376
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...
376
01:09In Vitro Drug Dissolution: Compendial Testing Models II
207
Various dissolution methods are utilized to assess a drug’s dissolution rate, including the flow-through cell, paddle-over-disk, cylinder, and reciprocating disk methods.The flow-through cell apparatus (USP (United States Pharmacopeia) method 4) comprises a reservoir for the dissolution medium and a pump that propels the medium through the cell containing the test sample. This method is crucial for assessing modified-release dosage forms with minimally soluble active ingredients,...
207
01:17In Vitro Drug Dissolution: Alternative Methods
178
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...
178
01:14Drug Dissolution: Requirements and Profile Comparison
208
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...
208
01:13In Vitro Drug Dissolution: Compendial Testing Models I
193
Compendial dissolution methods are standardized procedures defined by pharmacopeias to evaluate the rate at which a drug dissolves in a specific medium. These methods ensure batch-to-batch consistency, enable quality control, and support the prediction of drug bioavailability. They are critical for both immediate and modified-release drug products.The apparatuses used for dissolution testing differ in their design and mechanical function, but all aim to simulate the physiological environment of...
193
01:25Determination of Multiple Dosing Parameters: Loading and Maintenance Doses
194
A loading dose is an essential pharmacological strategy to rapidly achieve the target plasma drug concentration necessary for an immediate therapeutic effect. This approach is especially critical for drugs characterized by slow absorption or extended half-lives, where delaying therapeutic plasma levels could compromise treatment outcomes. By administering a loading dose, clinicians ensure a prompt onset of drug action, even for agents with complex pharmacokinetic profiles.Achieving steady-state...
194