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Enhancing tablet disintegration characteristics of a highly water-soluble high-drug-loading formulation by
Preetanshu Pandey1, Christopher Levins1, Steve Pafiakis1
1a Drug Product Science and Technology, Bristol-Myers Squibb , New Brunswick , NJ , USA.
Pharmaceutical Development and Technology
|November 24, 2016
Summary
Fluid-bed granulation significantly improved tablet disintegration and dissolution for high drug loading formulations compared to high-shear wet granulation. This was attributed to the altered internal pore structure achieved with fluid-bed granulation.
Area of Science:
- Pharmaceutical Technology
- Materials Science
- Chemical Engineering
Background:
- High drug loading formulations (70% w/w API) often present challenges in tablet disintegration and dissolution.
- Traditional high-shear wet granulation (HSWG) can lead to long disintegration times and high sensitivity to tablet hardness.
Purpose of the Study:
- To enhance the disintegration and dissolution characteristics of a highly water-soluble tablet matrix.
- To investigate fluid-bed granulation (FBG) as an alternative manufacturing process for high drug loading tablets.
Main Methods:
- A 2^(4-1) fractional factorial design with center points was employed to optimize FBG parameters.
- Key process variables included disintegrant amount, spray rate, inlet temperature, and atomization air pressure.
- Tablet properties and internal pore structure were analyzed using mercury intrusion porosimetry.
Main Results:
- FBG significantly reduced tablet disintegration times compared to HSWG.
- Final blend particle size was significantly influenced by spray rate, inlet temperature, atomization air pressure, and their interaction.
- Compactibility was significantly affected by disintegrant amount, atomization air pressure, and spray rate.
- FBG produced tablets with a higher internal pore structure, correlating with improved disintegration.
Conclusions:
- Fluid-bed granulation offers a superior alternative to high-shear wet granulation for producing tablets with high drug loading.
- Optimizing FBG parameters allows for control over particle size, compactibility, and internal pore structure, leading to enhanced tablet performance.
- The improved disintegration observed with FBG is directly linked to the resulting higher internal porosity of the tablets.
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