Abstract

Objective: The bioavailability of a newly developed effervescent tablet containing 50 mg diclofenac Na (DIC-effervesc) was investigated and compared with an enteric-coated dragée (DIC-enteric). Subjects and method: 24 healthy, male and informed volunteers (mean body weight 78.8 kg, mean age 31.9 years) received in a randomized cross-over design a single dose of 50 mg diclofenac as DIC-effervesc and DIC-enteric. A total of 19 blood samples were obtained before and up to 12 h after administration according to the different properties of the galenic formulation. Diclofenac was analyzed by a sensitive HPLC method with a lower limit of quantification of 20 ng/ml. The bioavailability was compared as ratios of the geometric means of AUC0-¥ and Cmax. Results: DIC-effervesc shows no lag time, a tmax within 30 min and a double peak of Cmax in 15/24 subjects. The mean Cmax (arithm. mean ± SD) for DIC-effervesc is 950 ± 341 ng/ml (first Cmax) and for DIC-enteric 1364 ± 335 ng/ml. The mean AUC0-¥ (arithm. mean ± SD) amounts to 1097 ± 210 ng/ml´h for DIC-effervesc and 1262 ± 220 ng/ml´h for DIC-enteric. Based on the point estimator and the 90% interval DIC-effervesc is bioequivalent in respect to amount absorbed (86.4%; 81.8 – 91.3%). DIC-effervesc was well tolerated. Conclusion: The new effervescent tablet of diclofenac Na shows a rapid absorption without lag time, the same amount of absorption and a slightly lower Cmax (caused by a double peak phenomenon) in comparison to the enteric-coated dragée. A rapid onset of therapeutic effect is postulated in acute pain disorders.

Author Details

Authors

• B. Terhaag¹
• A. Hoffmann¹
• M. Barkworth²
• B. Vens-Cappell²

Departments

• ¹ Corporate Research and Development, ASTA Medica Group, Arzneimittelwerk Dresden, Radebeul, and
• ² Phoenix International McKnight, Hamburg,Germany

Address

Prof. Dr. B. Terhaag; Arzneimittelwerk Dresden GmbH, Department of Medical Research, Meißner Straße 35, D-01445 Radebeul, Germany

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