Controlling the Release of Highly Dosed and Highly Soluble Drugs - Pharmaceutical Technology

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Controlling the Release of Highly Dosed and Highly Soluble Drugs
The authors formulated bupropion hydrochloride tablets with various grades of methacrylic copolymers and analyzed the properties of the resulting dosage forms. This article is part of PharmTech's supplement "Solid Dosage and Excipients 2010."


Pharmaceutical Technology
Issue 34, pp. s14-s18

Conclusion


Table VI: Assay of bupropion hydrochloride under initial and three months accelerated storage stability conditions.
The current study, which was designed to control the release of bupropion hydrochloride with various ionic and nonionic Eudragit grades in matrix technology, yielded attractive results. The tablets prepared showed matching USP release profiles in the beginning and under accelerated stability conditions, thus demonstrating stable formulations. All three Eudragit polymers tested showed strong retardant properties. Among the polymers, the aqueous dispersions were more effective than the powder grade. Dissolution profiles within specifications were achieved at low polymer levels of 15%. Thus, excellent formulation options are available for highly soluble actives, particularly for highly dosed actives that result in low tablet weights. The strength of these formulations is evidenced by the growing number that is available on the international market. Furthermore, regulators require extended-release bupropion hydrochloride tablets to demonstrate 40% ethanol resistance, which was proven for all tested Eudragit formulations.


Table VII: Dissolution conditions for bupropion hydrochloride ethanol resistance as per FDA.
Eudragit polymers are well estabilshed in pharmaceutical coating applications. The current study showed that Eudragit polymers also can be used for matrix applications for controlling the drug release. Eudragit polymers enable the realization of small dosage forms with high drug content. The current study showed that Eudragit polymers can be used to formulate matrix systems with unique dissolution characteristics and superior tablet properties.

Shripad Gadhinglajkar is head of research and development projects in the formulation and development group, Gopeshkumar Singh is an assistant manager for formulation development, Smitha Shetty is an assistant manager in the analytical department, and Brigitte Skalsky* is a global marketing manager of pharmaceutical services, all at Evonik Röhm, Kirschenallee, 64293 Darmstadt, Germany, tel. +49 6151 18-4389, fax +49 6151 18-844389,
.

*To whom all correspondence should be addressed.

References:

1. D. Gallardo and M. Assmus, Pharma Polymers News Bull. (12), 1–2 (2005).

2. B. Skalsky, Pharma Polymers News Bull. (16/01), 2–3 (2009).

3. Eudragit Application Guidelines, (Evonik Röhm Pharma Polymers, Darmstadt, Germany, 11th ed., 2009).

4. The Merck Index, M.J. O'Neil, Ed. (Merck Research Laboratories, Whitehouse Station, NJ, 14th ed., 2006), p. 246

5. Physician's Desk Reference, J. Reed, Ed. (PDR Network, Montvale, NJ, 63rd ed., 2009), p. 1653

6. USP 32–NF 27 (US Pharmacopeial Convention, Rockville, MD, 2009), p. 1723

7. FDA, Individual Product Bioequivalence Recommendations, Bupropion Hydrochloride Extended Release Tablets (Rockville, MD, April 2008).

8. S. Bodinge et al., poster, AAPS (Los Angeles, 2009).

9. R. Meyer and A. Hussain, presentation, FDA's ACPS Meeting, (Rockville, MD, 2005).

10. D. Gallardo, M. Assmus, and B. Skalsky, presentation, CRS Annual Meeting (Miami, FL, 2005).


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