Pharmacokinetic interaction between Kaempferia parviflora extract and sildenafil in rats

J Nat Med. 2015 Apr;69(2):224-31. doi: 10.1007/s11418-014-0882-4. Epub 2015 Jan 8.

Abstract

Kaempferia parviflora (KP) is a plant widely used in Southeast Asia. Its major compounds are 3,5,7,3',4'-pentamethoxyflavone (PMF), 5,7,4'-trimethoxylflavone (TMF), and 5,7-dimethoxyflavone (DMF). This study investigated the effect of KP extract on the blood levels and pharmacokinetics of sildenafil co-administration in rats. Rats were randomly assigned to four groups. Groups 1, 2, and 3 were given sildenafil 20 mg/kg daily for 9 days. On days 4-9 of each treatment period, the treated rats received KP extract (250 mg/kg) and vehicle (groups 2 and 3, respectively). Group 4 received KP extract only (250 mg/kg daily for 9 days). Daily blood concentrations of sildenafil, PMF, TMF, and DMF were determined by HPLC to evaluate the daily blood level interactions. Additional blood samples were collected at various times on the last day of treatment to evaluate the pharmacokinetic interactions. The KP extract decreased blood levels of sildenafil on the first day of co-administration by 95 % but the percentage reduction was insignificant on subsequent days. When co-administered with KP extract, the area under the curve (AUC), maximum concentration (C max), and half-life (T 1/2) of sildenafil were decreased by 60-65, 40-52, and 32-54 %, respectively, with the elimination rate constant (K e) increased by 37-77 %. In addition, PMF, TMF, and DMF concentrations and their AUC, C max, T max, K e, and T 1/2 values were changed after co-administration of KP extract and sildenafil.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Area Under Curve
  • Chromatography, High Pressure Liquid
  • Flavones / pharmacology*
  • Flavonoids / pharmacology
  • Herb-Drug Interactions*
  • Male
  • Piperazines / blood
  • Piperazines / pharmacokinetics*
  • Plant Extracts / pharmacology*
  • Purines / blood
  • Purines / pharmacokinetics
  • Rats, Wistar
  • Sildenafil Citrate
  • Sulfonamides / blood
  • Sulfonamides / pharmacokinetics*
  • Zingiberaceae / chemistry*

Substances

  • 3,5,7,3',4'-pentamethoxyflavone
  • Flavones
  • Flavonoids
  • Piperazines
  • Plant Extracts
  • Purines
  • Sulfonamides
  • 5,7-dimethoxyflavone
  • Sildenafil Citrate