Assessing Tablet-Sticking Propensity - Pharmaceutical Technology

Latest Issue
PharmTech

Latest Issue
PharmTech Europe

Assessing Tablet-Sticking Propensity
The authors designed an upper punch with a removable punch tip to determine a tablet formulation's propensity to stick by weighing the mass of powder adhered to the punch tip.


Pharmaceutical Technology
Volume 36, Issue 1, pp. 57-62


Figure 7: Sticking profiles for prototype and commercially available ibuprofen formulations.
Benchmarking sticking of a new ibuprofen formulation. A prototype ibuprofen formulation was tested alongside three commercially available ibuprofen formulations to quantify sticking risk before scale-up. The prototype formulation contained a 50% w/w level of ibuprofen and 5% w/w talc as the tableting lubricant. After 100 compressions, the prototype formulation had about 1500 g of powder adhered to the punch tip. The commercial ibuprofen formulations had lower sticking: Albemarle had the most, followed by BASF and Advil (See Figure 7). Using Advil as the gold-standard benchmark, the prototype formulation was deemed to be unsuitable for product scale-up without reformulation. The high level of sticking for the prototype ibuprofen formulation was attributed to literature reports of talc as a suboptimal tableting lubricant for sticky formulations (7, 8), in addition to ibuprofen's notorious propensity to stick. This quantitative assessment shows the benefit of testing prototype formulations and benchmarking alongside formulations known to (or not to) exhibit sticking behavior. Thus, unsuitable formulations can be flagged quickly during drug product design.

Conclusion

The simple method of using a removable punch tip is capable of quantitatively measuring sticking for formulations containing various levels of tableting lubricant and various grades and concentrations of sticky ingredients. This tool can be used to screen tableting formulations during drug-product design to optimize formulation composition, and potentially to study the effect of sticking on tableting process parameters (e.g., tableting speed and compression force) and tooling design features (e.g., metal composition, surface roughness, shape, curvature, and embossing).

Acknowledgments

The authors thank MDC Associates for assisting with the design and fabrication of the custom punch. They thank Gregory (Scott) Goeken, scientist, and John Kresevic, senior principal scientist, both at Pfizer, for providing the prototype and commercial ibuprofen formulation samples.

References

1. M. Roberts et al., J. Pharm. Pharmacol. 56 (3), 299–305 (2004).

2. T.S. McDermott et al., Powder Technol. 212 (1), 240–252 (2011).

3. D. Simmons, poster at the 12th Annual American Association of Pharmaceutical Scientists—Northeast Regional Discussion Group (Rocky Hill, CT, 2009).

4. J.J. Wang et al., J. Pharm. Sci. 93 (2), 407–417 (2004).

5. Y. Cheng et al., Proceedings of AICHE Annual Conference (Orlando, FL, 2006), pp. 1–13.

6. F. Waimer et al., Pharm. Dev. Technol. 4 (3), 359–367 (1999).

7. M. Bose, A. Sakr, and A. Warner, Pharm. Industrie 55 (5), 519–522 (1993).

8. A. Delacourte et al., Drug Dev. Ind. Pharm. 19 (9), 1047–1060 (1993).

What would you do differently? Email your thoughts about this paper to
and we may post them on http://PharmTech.com/.

Matthew P. Mullarney* is a principal scientist, Bruce C. MacDonald is a scientist, and Allan Hutchins is a laboratory technician, all at Pfizer, Eastern Point Road, Groton, CT 06340, tel. 860.715.4139, fax 860.441.3972,
.


ADVERTISEMENT

blog comments powered by Disqus
LCGC E-mail Newsletters

Subscribe: Click to learn more about the newsletter
| Weekly
| Monthly
|Monthly
| Weekly

Survey
FDASIA was signed into law two years ago. Where has the most progress been made in implementation?
Reducing drug shortages
Breakthrough designations
Protecting the supply chain
Expedited reviews of drug submissions
More stakeholder involvement
Reducing drug shortages
27%
Breakthrough designations
9%
Protecting the supply chain
41%
Expedited reviews of drug submissions
9%
More stakeholder involvement
14%
View Results
Jim Miller Outsourcing Outlook Jim Miller Health Systems Raise the Bar on Reimbursing New Drugs
Cynthia Challener, PhD Ingredients Insider Cynthia ChallenerThe Mainstreaming of Continuous Flow API Synthesis
Jill Wechsler Regulatory Watch Jill Wechsler Industry Seeks Clearer Standards for Track and Trace
Siegfried Schmitt Ask the Expert Siegfried SchmittData Integrity
Sandoz Wins Biosimilar Filing Race
NIH Translational Research Partnership Yields Promising Therapy
Clusters set to benefit from improved funding climate but IP rights are even more critical
Supplier Audit Program Marks Progress
FDA, Drug Companies Struggle with Compassionate Use Requests
Source: Pharmaceutical Technology,
Click here