The Disintegration and Dissolution of Nabumetone Dispersible Tablets - Pharmaceutical Technology

Latest Issue
PharmTech

Latest Issue
PharmTech Europe

The Disintegration and Dissolution of Nabumetone Dispersible Tablets
Nabumetone was complexed with β-cyclodextrin, and a 23 factorial design was used to prepare dispersible tablets containing the drug or its complex.The authors analyzed the effects of complexation as well as the levels of ammonium bicarbonate and crospovidone on tablet wetting time (WT), disintegration time (DT), and percent dissolution efficiency at 60 min (%DE60).


Pharmaceutical Technology



Table VI: Composition of the optimized formulations and comparison of the experimental values of the response parameters with the predicted values. All figures are courtesy of the authors.
The mathematical models representing the response parameters were validated by preparing a new formulation with a combination of factors within the experimental domain. The formulation was evaluated for the disintegration wetting and in vitro dissolution. Table VI lists the value of the observed responses and those predicted by mathematical models. The prediction error for the response parameters ranged from 3.39 to –2.44%. The low values of error prove the abilities of the generated mathematical models and reveal the capabilities of multiple linear regression analysis and analysis of variance in predicting the performance of the new formulation.

In this study, the enhancement of nabumetone solubility was possible by complexation with β-CD. Various solid-state characterization techniques confirmed the formation of the drug β-CD inclusion complexes. A 23 factorial study performed indicated that complexation, amounts of ammonium bicarbonate, and crospovidone played a vital role in the production of dispersible tablets with desirable wetting, disintegration, and dissolution. The results obtained indicate that factorial studies can be successfully used to quantify the effect of several formulation and processing variables on tablet properties, thereby minimizing the number of experimental trials and reducing formulation development cost.

Acknowledgments

The authors are grateful to Sri Prabhakar Kore, Chancellor, KLE Academy of Higher Education and Research, Deemed University, Belgium for providing facilities to carry out the research work. The authors also thank Microlabs (Bangalore) for the gift samples of nabumetone and Signet Chemical Corp. (Mumbai) for the gift samples of β-cyclodextrin.

H.N. Shivakumar, PhD,* is a professor at the department of pharmaceutical technology, K.L.E.S's College of Pharmacy, Bangalore, India,
B.G. Desai is a professor and head of the department of pharmaceutical technology, K.L.E.S's college of pharmacy. S. Narasimha Murthy, PhD, is an assistant professor at the department of pharmaceutics, The University of Mississippi (University, MS). Ashish Sharma is a clinical research associate at Pharmanet Clinical Service, Bangalore, India.

*To whom all correspondence should be addressed.

Submitted: Jan. 19, 2007. Accepted:Mar. 7, 2007

References

1. A. Burke, E. Smyth, and G.A. Fritzgerald "Analgesic–Antipyretic Agents; Pharmacotherapy of Gout," in The Pharmacological Basis of Therapeutics, L.L. Burton, J.S. Laso, and K.L. Parker Eds. (McGraw-Hill Medical Publishing Division, New York, 11th ed. 2006), pp. 671–715.

2. S.C. Sweetman "Analgesics and Anti-Inflammatory Drugs and Antipyretics," in The Complete Drug Reference (Pharmaceutical Press, London, 34th ed. 2005), pp. 1–115.

3. L. Chelakara et al., "Spherical Agglomeration of Mefenamic acid and Nabumetone to Improve Micromeritics and Solubility: A Technical Note," AAPSPharm SciTech. 7, Article 48 (2006).

4. N. Goyenechea et al., "Interaction of Nabumetone with Cyclodextrin in Solution and Solid State," J. Inclusion Phenomena Macrocyclic Chem. 44 (4), 283–288 (2002).

5. B.I. James, M.D. Roy, and C.P. Laurence, US Patent No. 5962022, (1994).

6. H. Jane et al., US Patent No. 6863901, (2005).


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