A relative bioavailability study of 500 mg calcium p-aminosalicylate film coating tablet in healthy individuals

Chinhwa Cheng a,b, Mei-Ling Chen b, Chiachi Tseng b, Yow-Shieng Uang c,
Chyn-Liang Huang d, Kuang-Yang Hsu a,*
a School of Pharmacy, Taipei Medical University, Taiwan, ROC
b Medical and Pharmaceutical Technology and Development Center, Taiwan, ROC
c Rosetta Pharmamate Co., Ltd., Taiwan, ROC
d Food and Drug Administration, Ministry of Health and Welfare, Executive Yuan, Taiwan, ROC

The purpose of this study is to evaluate the only available calcium p-aminosalicylate (Ca PAS) commercial product, which is one of the most commonly prescribed non-surveillance products fromthe Bureau of National Health Insurance (BNHI) database in Taiwan. An openrandomized, balanced, two-way crossover study was designed to evaluate the relative bioavailability (F) of a 500 mg Ca PAS F.C. tablet with a 500 mg Ca PAS suspension in 13 healthy individuals. Blood samples were collected according to a planned time schedule. The plasma concentrations of PAS were measured by a validated liquid chromatography coupled with tandem mass spectrometry (LC/MS/MS) method. Pharmacokinetic parameters of area under the plasma concentration-time curve from the time zero to the time of last quantifiable concentration (AUC0et), area under the  plasma concentration-time curve from time zero to infinity (AUC0eN), maximum plasma concentration (Cmax), time to reach measured maximum plasma concentration (Tmax), elimination half-life (T1/2), and mean residence time (MRT) were determined by non-compartment methods. F was calculated by [AUC0eN] of the test drug divided by [AUC0eN] of the reference drug. The mean geometric ratios of pharmacokinetic parameters, including AUC0et, AUC0eN, and Cmax obtained were 0.873, 0.874, and 0.569, respectively. The 90% confidence intervals of ln (AUC0et), ln (AUC0eN), and ln (Cmax) after being back natural log-transformed were (74.0e103.0%), (74.1e103.0%), and (38.4e84.3%), respectively. The relative bioavailability of the Ca PAS tablet was 87.4%.

Keywords: Calcium p-aminosalicylate (Ca PAS), Relative bioavailability (F)