Experiment 374159
Worktypes
Compounds isolated
Details
| Property | Value |
|---|---|
| Pharmacology | |
| Administration route | ORAL |
| Organism | Empty organism |
| Citation | KARLSSON,MO: DAHLSTROM,B: ECKERNAS,SA: JOHANSSON,M: ALM,AT:. (1990). PHARMACOKINETICS OF ORAL NOSCAPINE.. 1990(39) |
| Amount utilized | |
| Compound isolated | |
| Disease | THE RELATIVE BIOAVAILABILITY IN 20 HEALTHY VOLUNTEERS OF 100 MG, 200 MG AND 300 MG TABLETS OF NOSCAPINE AND 200 MG AS A SOLUTION HAS BEEN ASSESSED IN A FOUR-WAY CROSS-OVER STUDY, WITH REPEATED ADMINISTRATION OF THE 200 MG DOSE TO ASSESS INTRAINDIVIDUAL VARIABILITY. THERE WAS A DISPROPORTIONATE INCREASE IN THE AUC OF NOSCAPINE TABLETS, AS A 3-FOLD INCREASE IN DOSE PRODUCED A 9-FOLD RISE IN AUC. THIS DOSE-DEPENDENCY COULD MAINLY BE ATTRIBULTED TO SATURABLE FIRST-PASS METABOLISM OF THE DRUG. ADMINISTRATION OF NOSCAPINE AS A SOLUTION RESULTED IN A SIGNIFICANTLY HIGHER MAXIMAL CONCENTRATION AT AN EARLIER TIME-POINT AND A HIGHER AUC THAN THE CORRESPONDING DOSE AS TABLETS. REPEATED ADMINISTRATION OF NOSCAPINE TABLETS AND SOLUTION YIELDED HIGHER AUC ON THE SECOND DOSING OCCASION. NO CAUSE FOR THIS CARRY-OVER EFFECT WAS FOUND, AND THE CONTRIBUTION OF REMAINING NOSCAPINE WAS NEGLIGIBLE. THE TERMINAL HALF-LIFE OF NOSCAPINE, WHICH WAS INDEPENDENT OF FORMULATION OR DOSE SIZE WAS 4.5 H. BOTH INTER-AND INTRAINDIVIDUAL VARIABILITY IN NOSCAPINE KINETICS WERE VERY HIGH, E.G. 73% AND 51% CV OF THE AUC FOR THE 200 MG TABLET. |
| Dose amount | 200.0 MG |
| Number | 1 |
| Qualitative result | ACTIVE |
| Animal | HUMAN ADULT |
| Dose expression | DOSE |
| Gender | MALE |