Journal of Pharmaceutical Investigation

The Korean Society of Pharmaceutical Sciences and Technology (한국약제학회)
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Improvement of Solubility and Bioavailability of Poorly Water Soluble Piroxicam with L-Arginine Complex

L-아르기닌 복합체를 이용한 피록시캄의 용해도 및 생체이용률의 증가

  • 홍석천 (한국유나이티드제약(주) 중앙연구소) ;
  • 유창훈 (한국유나이티드제약(주) 중앙연구소) ;
  • 조동현 (한국유나이티드제약(주) 중앙연구소) ;
  • 신현종 (한국유나이티드제약(주) 중앙연구소) ;
  • 길영식 (한국유나이티드제약(주) 중앙연구소)
  • Published : 2003.06.20
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Abstract

Piroxicam-arginine complex was prepared to improve the solubility and dissolution rate of poorly water-soluble piroxicam. Its formation was identified by infrared spectrophotometry, differential thermal analysis and dissolution rate. Piroxicam complex dispersible tablets, commercial $Feldene^{\circledR}$ dispersible tablets and piroxicam physical mixture hard capsules were prepared to compare dissolution rate in water. Dissolved amounts (%) after 15 mins of piroxicam complex dispersible tablets, commercial $Feldene^{\circledR}$ dispersible tablets and piroxicam physical mixture hard capsules were 98%, 48% and 10%, respectively. The solubility of complex in water was significantly higher than that of piroxicam itself. In vivo, pharmacokinetic parameters were obtained after oral administrations of piroxicam complex and physical mixture at a does of 2 mg to New Zealand White Rabbit. The $C_{max}$ of piroxicam complex was similar to that of piroxicam. However, there were much difference between the two formulations with regard to $T_{max}$ and AUC. The $T_{max}$ of piroxicam alone was 4 hours, but that of piroxicam complex was 0.8 hours. In addition, the AUC of piroxicam complex was 1.38 times greater than that of piroxicam alone.

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