Pharmacokinetics of Acrivastine After Oral and Colonic Administration

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Abstract
Six healthy male volunteers participated in this randomized, crossover open‐label pharmacokinetic study consisting of two dosing segments separated by a washout period of at least 5 days. During each dosing segment, each volunteer received 12 mg of acrivastine, an investigational histamine H1‐receptor antagonist, in a syrup form either orally or by colonic administration in random order. After oral and colonic administration, respectively, the following mean ± SD pharmacokinetic parameters were obtained: Cmax 179 ± 11 and 13.8 ± 5.2 ng/ml; tmax, 0.85 ± 0.13 and 3.60 ± 0.56 hr; AUC0–12 hr, 576 ± 57 and 104 ± 46 hr · ng/ml. Differences between the oral and colonic administration for all three parameters were statistically significant (P < 0.001). The mean ± SD relative bioavailability of acrivastine from colonic compared to oral dosing was 0.18 ± 0.09. It may be concluded, therefore, that appreciable absorption of acrivastine from the colon does not take place. These results suggest that comparison of pharmacokinetic profiles of some drugs after oral and colonic administration may be a useful technique for predicting bioavailability from a sustained release oral formulation.