Prandial effect on the systemic exposure of amisulpride
- 249 Downloads
A substituted benzamide, amisulpride is an atypical antipsychotic and a specific antagonist for dopamine D2 and D3 receptors. The prandial effect on amisulpride absorption remains unclear, therefore, this study was designed to investigate the effect of food on the systemic exposure to amisulpride in healthy volunteers. The study was a randomized, two-way crossed trial in which a single oral dose of amisulpride was administered on two occasions, with 7-days washout period between each drug administration. The volunteers were randomly divided into two groups and received amisulpride (50 mg) with Korean traditional food or under fasting state. Blood was serially taken, and the plasma amisulpride concentrations were measured by LC/MS/MS. At fasting state, amisulpride reached the first peak (37.1 ± 13.3 ng/ml) at ~2.3 h, and decreased down to 19.4 ± 4.3 ng/ml until 3.5 h, and then again went up to the second peak (25.3 ± 5.8 ng/ml) at 5 h followed by a slow decay with 10.6 h of half-life. In contrast, no double peaks were shown when the drug was given with meal. The maximum concentration of amisulpride (56.0 ± 12.7 ng/ml) was increased by a 1.5-fold compared with that under fasting (p > 0.05), and the time to peak shortened a little (1.7 ± 0.6 h).
KeywordsAmisulpride Food Systemic exposure
This study was supported by Yeungnam University research grant in 2010.
Conflict of interests
The authors declare no competing financial interests.
- Gschwend, M.H., P. Arnold, J. Ring, and W. Martin. 2006. Selective and sensitive determination of amisulpride in human plasma by liquid chromatography-tandem mass spectrometry with positive electrospray ionisation and multiple reaction monitoring. Journal of Chromatography B 831: 132–139.CrossRefGoogle Scholar
- Hamon-Vilcot, B., S. Chaufour, C. Deschamps, M. Canal, I. Zieleniuk, P. Ahtoy, P. Chretien, P. Rosenzweig, A. Nasr, and F. Piette. 1998. Safety and pharmacokinetics of a single oral dose of amisulpride in healthy elderly volunteers. European Journal of Clinical Pharmacology 54: 405–409.PubMedCrossRefGoogle Scholar
- Lim, H.K., S.J. Kim, C.U. Pae, C. Lee, and C.U. Lee. 2007. Comparison of amisulpride and risperidone in the treatment of psychosis in patients with dementia of the Alzheimer’s type. Journal of Korean Geriatric Psychiatry 11: 35–39.Google Scholar
- Malavasi, B., M. Locatelli, M. Ripamonti, and V. Ascalone. 1996. Determination of amisulpride, a new benzamide derivative, in human plasma and urine by liquid–liquid extraction or solid-phase extraction in combination with high-performance liquid chromatography and fluorescence detection. application to pharmacokinetics. Journal of Chromatography B 676: 107–115.CrossRefGoogle Scholar
- Yun, H.Y., M.S. Baek, and K.I. Kwon. 2006a. The effect of food on absorption of drug in the gastrointestinal tract. Korean Journal of Clinical Pharmacy 16: 147–154.Google Scholar