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Comparison of the Solubility and Pharmacokinetics of Sildenafil Salts
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  • Comparison of the Solubility and Pharmacokinetics of Sildenafil Salts
  • Comparison of the Solubility and Pharmacokinetics of Sildenafil Salts
저자명
Jung. Si-Young,Seo. Youn-Gee,Kim. Gun-Kook,Woo. Jong-Soo,Yong. Chul-Soon,Choi. Han-Gon
간행물명
Archives of pharmacal research : a publication of the Pharmaceutical Society of Korea
권/호정보
2011년|34권 3호|pp.451-454 (4 pages)
발행정보
대한약학회
파일정보
정기간행물|ENG|
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이 논문은 한국과학기술정보연구원과 논문 연계를 통해 무료로 제공되는 원문입니다.
서지반출

기타언어초록

To develop sildenafil lactate, a salt form of sildenafil with improved solubility and bioavailability of poorly water-soluble sildenafil base, this salt form was prepared using a spray dryer. Its solubility and pharmacokinetics in rabbits were evaluated compared with sildenafil base and sildenafil citrate. Sildenafil lactate improved the solubility of sildenafil in various solvents including distilled water compared with sildenafil citrate. It provided higher AUC and $C_{max}$ and, shorter $t_{1/2}$ values than did the other materials, indicating that it improved the oral bioavailability of sildenafil in rabbits. Our results suggest that sildenafil lactate would be useful to deliver sildenafil in a pattern that allows fast absorption and late metabolism. Furthermore, the plasma concentration at 0.25 h in sildenafil lactate was similar to the $C_{max}$ value at $T_{max}$ (0.5 h) in sildenafil citrate. Thus, sildenafil lactate might provide a faster onset of action and immediate erection compared with sildenafil citrate, the conventional drug.