Enhancement by a high fat meal of the absorption of orally administered T2000 (1,3‐bismethoxymethyl‐5,5‐diphenylbarbituric acid; I) in man
Bibliographic record
Abstract
I is presently under evaluation for potential utility in essential tremor and seizure disorders. The compound lacks prominent sedative‐hypnotic activity usually associated with this chemical class of drugs. I is biotransformed to monomethoxymethyl‐5,5‐diphenylbarbituric acid (II) and to 5,5‐diphenylbarbituric acid (III) in the rat, dog and man. II and III appear to be active metabolites. I has limited aqueous solubility; in an effort to enhance absorption from the gastrointestinal tract, we evaluated the influence of a high fat breakfast on gastrointestinal absorption of I in 23 healthy non‐smoking male volunteers between 19 and 54 years of age. The rate and extent of absorption was assessed by measuring the plasma levels of I, II and III over the course of 5 days after an oral dose of 400 mg of I. Results: The mean ratios for C max (fed/fasting) for I, II and III were 6.88, 3.14 and 1.59, respectively. Mean t max ratios (fed/fasting) for the 3 compounds were 0.65, 0.44 and 0.88 for I, II and III. Mean ratios for AUC 0‐t (fed/fasting) for I, II and III were 2.81, 2.74 and 1.53, respectively. Mean terminal half‐lives for I, II and III ranged between 18‐26, 16‐27 and 39‐43 hours, respectively. Conclusion: A high fat meal enhances the oral absorption of T2000 in man as indicated by higher C max , earlier t max and greater AUC after a high fat breakfast than in the fasting state. As expected, terminal half‐lives of all 3 compounds did not change.
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How this classification was reachedexpand
Full frame machine prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. The Gemma side is a direct model label for every work in the frame, read from the title-only record. The Codex side is a classifier learned from the 10,348 direct Codex labels and calibrated to design-weighted sample rates; fields without enough sample support carry no Codex call. Candidate is the union of the two sides; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels.
Distilled classifier scores by category (both heads)
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.000 | 0.000 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.000 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.000 | 0.000 |
| Scholarly communication | 0.000 | 0.000 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.000 | 0.000 |
| Insufficient payload (model declined to judge) | 0.001 | 0.000 |
Machine scores (provisional)
The two teacher heads of the student model, read on this work. A score orders the frame for review; it never asserts a category, and the validation status ships verbatim with every row.
Baseline scores from an immature model (maturity gate not passed, 7 training rounds). Scores rank; they never assert a category.
score_only:v0-immature-baseline · verbatim from the scoring run: score_only means the number may rank works, and no category label ships from itClassification
machine, unvalidatedMachine predicted; a candidate call from one source (direct Gemma or distilled Codex), not a consensus.
How this classification was reached, model by model and score by score, is at the end of the page under "How this classification was reached".