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Arzneimittelforschung 2009; 59(5): 233-237
DOI: 10.1055/s-0031-1296390
Antihypertensives
Editio Cantor Verlag Aulendorf (Germany)

Bioequivalence Evaluation of Rilmenidine in Healthy Volunteers

Gerhard Groenewoud, Linda Potgieter, Bernhardt Meyer
Gerhard Groenewoud
,
Linda Potgieter
,
Bernhardt Meyer
Further Information

Publication History

Publication Date:
13 December 2011 (online)

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Abstract

The bioavailability of two rilmenidine tablet formulations was compared in healthy male (17) and female (8) subjects, aged 18 to 36 years, during a laboratory-blind, randomized, two-treatment, two-period, cross-over study under fasting conditions. In each treatment phase subjects received a single dose of 1.544 mg rilmenidine dihydrogen phosphate (CAS 85409-38-7), equivalent to 1 mg rilmenidine (CAS 54187-04-1). Consecutive dosing was separated by a drug-free wash-out period of 7 d. Following each dosing, serial venous blood samples were collected over a period of 48 h for the determination of plasma rilmenidine concentrations by means of a validated LC-MS/MS method. The most frequently reported drug-related adverse events were dizziness and headache ranging from mild to moderate in intensity. The geometric mean Cmax of rilmenidine for the reference and test products was 3.73 and 3.97 ng/ml, respectively. The corresponding geometric mean AUC(0–∞) was 34.0 and 35.1 ng • h/ml. Tmax for both products under investigation appeared at 1.33 h. The test product was shown to be bioequivalent to the reference product with respect to all pharmacokinetic variables investigated.

Key words

Antihypertensive agents - CAS 54187-04-1 - CAS 85409-38-7 - Hyperium® - Rilmenidine, bioavailability, bioequivalence, pharmacokinetics - Rilmenidine dihydrogen phosphate
 

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