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The Korean Society for Biotechnology and Bioengineering (한국생물공학회)
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Development and Evaluation of Gastro Retentive Floating Matrix Tablet Containing Valsartan Solid Dispersion

발사르탄 고체 분산체를 함유하는 위체류 매트릭스 부유 정제의 개발 및 평가

  • Cho, Young Ho (Department of Pharmaceutics & Biotechnology, Konyang University) ;
  • Lee, Jong-Hwa (Division of Research and Development, Korea Institute of Toxicology) ;
  • Lee, Gye Won (Department of Pharmaceutics & Biotechnology, Konyang University)
  • Received : 2016.08.20
  • Accepted : 2016.11.25
  • Published : 2016.12.31
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Abstract

Valsartan, a drug for the treatment of cardiovascular disease, exhibited low bioavailability which was caused by, at least in part, limited solubility at low pH. Present investigation deals with the preparation and characterization of gastro-retentive drug delivery system (GRDDS) using valsartan solid dispersion. We prepared solid dispersion using surfactants (Poloxamer 407) and alkalizer ($Na_2CO_3$) which may to be useful for improving solubility of valsartan at low pH and evaluated by saturated solubility of valsartan in distilled water. Valsartan gastro-retentive (GR) tablets containing solid dispersion prepared and evaluated by weight variation, floating time and dissolution rate. Compression at lower pressures resulted in the tablets floating over simulated gastric fluid (pH 1.2) for more than 17 h. In vitro release of valsartan from GR tablet was dependent on the amount of poloxamer 407 and hydroxypropyl methylcellulose. On the basis of evaluation parameter, formulation E-3 was selected as a final formulation. Therefore, it can be concluded that the GR tablets containing solid dispersion may be exploited successfully for the delivery of poorly drug such as valsartan.

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