JOURNAL OF THE CZECH PHARMACEUTICAL SOCIETY AND THE SLOVAK PHARMACEUTICAL SOCIETY

Čes. slov. farm. 2010, 59(4):179-185

Technology of controlled-release tablets containing highly soluble active ingredients

B. Vladovičová1,*, V. Kormanová1, M. Vítková2, V. Hubinová1, M. Žabka2, K. Gardavská2
1 Zentiva a. s., Hlohovec, Slovenská republika
2 Univerzita Komenského v Bratislave, Farmaceutická fakulta, Katedra galenickej farmácie, Slovenská republika

The aim of this experimental study was the preparation of once-daily-dosed matrix tablets containing the highly soluble drugs metoprolole succinate and metformine hydrochloride using Eudragit® NE 30 D as the matrix forming polymer. Matrix tablets were prepared by compression of coated granules. The formation of the secondary structure from the coating polymer was evaluated. In the case of metoprolole succinate, the drug release was prolonged, 53% of the drug being released within 20 hours. Dissolution profile was modified by addition of a filler, then the drug was completely released within 24 hours what is not acceptable for experimental purpose. The described technology of the preparation of the once-daily-dosed matrix was used also for the highly dosed drug metformine hydrochloride. The release rate of metformine hydrochloride was evaluated in dependence on the polymer content. The prepared formulation showed similar dissolution characteristics as the marketed product used in therapy. A positive effect of curing on the stability of the dissolution profile was demonstrated. The results demonstrate that the reported technology of compression of Eudragit® NE 30 D coated granules is usable for the preparation of prolonged-release dosage forms containing highly soluble drugs.

Keywords: Eudragit® NE 30 D; prolonged release; secondary structure; metoprolole succinate; metformine hydrochloride

Received: August 2, 2010; Accepted: August 10, 2010; Published: April 1, 2010  Show citation

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Vladovičová B, Kormanová V, Vítková M, Hubinová V, Žabka M, Gardavská K. Technology of controlled-release tablets containing highly soluble active ingredients. Čes. slov. farm. 2010;59(4):179-185.
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