THE ABSOLUTE AND RELATIVE BIOAVAILABILITY OF DIPYRIDAMOLE FROM DIFFERENT PREPARATIONS AND THE INVITRO INVIVO COMPARISON

  • 1 June 1986
    • journal article
    • research article
    • Vol. 24  (6) , 298-302
Abstract
The in vitro liberation and the bioavailability (BV) of dipyridamole (D) in three different brands (A, B, C) were determined in a three way cross-over study on 12 healthy subjects. Also, the pharmacokinetics of D given intravenously was investigated. The in vitro liberation of B is only to be achieved by repeated touching. The tmax for the preparations, expressed as .hivin.x .+-. S.hivin.x amounts as follows: A:0.8 .+-. 0.06; B: 1.1 .+-. 0.1; C: 0.8 .+-. 0.09 hours and is in the case of B significantly different (p < 0.05) from the others. The cmax values (A: 1.01 .+-. 0.25; B: 1.16 .+-. 0.15; C: 1.51 .+-. 0.3 .mu.mol .cntdot. l-1) and the AUC values (A: 3.8 .+-. 0.9; B: 3.1 .+-. 0.5; C: 3.8 .+-. 0.7 .mu.mol .cntdot. h .cntdot. l-1) are not different. The absolute BV of D is 27 .+-. 5.5% (range: 11-44%) independent of the used brand. In 4 subjects a second tmax at the 4th-6th hour is to be observed irrespective of the way of dosing. An enterohepatic circulation is assumed. It is concluded that the determination of the in vitro liberation is a necessary and useful parameter, but cannot be used alone for characterization of the BV in every case, as e.g., for problem drugs.

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