Co-amorphous Form of Curcumin–Folic Acid Dihydrate with Increased Dissolution Rate
Bibliographic record
Abstract
Curcumin is a naturally occurring compound derived from turmeric. Despite its many medicinal properties, such as being an antioxidant, anti-inflammatory, tumor reducer, etc., applications of curcumin are restricted due to its low aqueous solubility and consequently its poor bioavailability. By converting the solid state of poorly water-soluble active pharmaceutical ingredients to coamorphous mixtures, solvates, cocrystals, and eutectics, the solubility can be significantly improved. In this study, U. S. Food and Drug Administration approved excipients were screened for their ability to form novel solid states with curcumin to increase its aqueous solubility. Excipients were screened based on their molecular complementarity with curcumin, using Mercury software. Folic acid dihydrate (FAD), suberic acid, and dextrose are the three coformers that are investigated in this study. It was found that a coamorphous mixture can be formed between curcumin and FAD. FAD has potential as a prenatal or a women’s health drug due to its use in pre-eclampsia and ovarian cancer treatments. This mixture was found to have an increased dissolution rate when compared with curcumin. After 1 h, 175 mg/L of curcumin was dissolved from the coamorphous mixture, while only 45 mg/L was dissolved from curcumin Form I. The coamorphous mixture is stable as it was shown to keep its amorphous behavior after 24 h in solution at elevated temperatures. Curcumin formed a eutectic with suberic acid at a mole fraction of 0.2, whereas it remained as a physical mixture with dextrose. Also, solution crystallization of curcumin with dextrose at a mole fraction of 0.5 resulted into a form II curcumin polymorph.
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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 | 0.001 | 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 | 0.001 |
| Insufficient payload (model declined to judge) | 0.002 | 0.001 |
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".