Controlled Recrystallization of Tubular Vinpocetine Crystals with Increased Aqueous Dissolution Rate and <i>In Vivo</i> Bioavailability
Why this work is in the frame
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Bibliographic record
Abstract
Vinpocetine was a BCS II drug, whose clinical applications had suffered from low oral bioavailability because of its inefficient dissolution in the GI tract. As the dissolution rate depended on the surface area of the drug crystals, we herein explored shape-controlled recrystallization via antisolvent process as an excipient-free strategy to improve the bioavailability of VIN. By adjusting the water/ethanol ratio, initial VIN concentration, and temperatures, morphologies of the crystalline products could be finely tuned from three-dimensional cubes and tubes, to two-dimensional frizzled plates, and finally to zero-dimensional microparticle clusters. Morphology analysis and in situ FBRM surveillance of the growing process suggested that a diffusion-limited crystal growth mechanism was responsible for the shape variation of VIN products. Finally, we tested the in vitro dissolution efficiency as well as the in vivo bioavailability of recrystallized VIN crystals. Results manifested that the tubular crystal showed a faster dissolution behavior as compared with the raw VIN, achieving an increased AUC 0-t of 484.0 ± 24.6 ng/mL·h, which was 1.3-fold that of the raw VIN product (386.6 ± 22.8 ng/mL·h). To the best of our knowledge, this was one in vitro to in vivo report for bioavailability improvement of BCS II drug by applying the shape-controlled recrystallization strategy.
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Full frame distilled prediction
Teacher imitationNot calibrated prevalence, not ground truth. Human validation pending. Learned from the 10,348 direct Codex labels and 10,348 direct Gemma labels. Candidate is the union of thresholded teacher heads; consensus is their intersection. These outputs are machine_predicted_unvalidated and are not human labels or direct frontier model labels.
Codex and Gemma teacher scores by category
| Category | Codex | Gemma |
|---|---|---|
| Metaresearch | 0.003 | 0.002 |
| Meta-epidemiology (narrow) | 0.000 | 0.000 |
| Meta-epidemiology (broad) | 0.001 | 0.000 |
| Bibliometrics | 0.000 | 0.000 |
| Science and technology studies | 0.001 | 0.001 |
| Scholarly communication | 0.000 | 0.001 |
| Open science | 0.000 | 0.000 |
| Research integrity | 0.000 | 0.000 |
| Insufficient payload (model declined to judge) | 0.000 | 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 it