Dosage form design and in vitro/in vivo evaluation of cevimeline extended-release tablet formulations

Autor: Shinichiro, Tajiri, Taro, Kanamaru, Makoto, Kamada, Kamada, Makoto, Tsutomu, Konno, Hiroaki, Nakagami
Rok vydání: 2010
Předmět:
Zdroj: International Journal of Pharmaceutics. 383:99-105
ISSN: 0378-5173
DOI: 10.1016/j.ijpharm.2009.09.007
Popis: The objective of the present work is to develop an extended-release dosage form of cevimeline. Two types of extended-release tablets (simple matrix tablets and press-coated tablets) were prepared and their potential as extended-release dosage forms were assessed. Simple matrix tablets have a large amount of hydroxypropylcellulose as a rate-controlling polymer and the matrix is homogeneous throughout the tablet. The press-coated tablets consisted of a matrix core tablet, which was completely surrounded by an outer shell containing a large amount of hydroxypropylcellulose. The simple matrix tablets could not sustain the release of cevimeline effectively. In contrast, the press-coated tablets showed a slower dissolution rate compared with simple matrix tablets and the release curve was nearly linear. The dissolution of cevimeline from the press-coated tablets was not markedly affected by the pH of the dissolution medium or by a paddle rotating speed over the range of 50-200 rpm. Furthermore, cevimeline was constantly released from the press-coated tablets in the gastrointestinal tract and the steady-state plasma drug levels were maintained in beagle dogs. These results suggested that the designed PC tablets have a potential for extended-release dosage forms.
Databáze: OpenAIRE
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