Complex dispersions of poloxamers and mesoporous carriers with ibrutinib
Bibliographic record
Abstract
Ibrutinib is an anticancer drug, a Bruton's tyrosine kinase inhibitor with poor solubility in aqueous media. This study reports on the study of the effectiveness of mesoporous carriers based on magnesium aluminometasilicate and poloxamers to improve the solubility and bioavailability of ibrutinib in the form of amorphous solid dispersions. The choice of the most effective composition was made on a parallel study of (a) a physical mixture of ibrutinib with a mesoporous carrier, (b) a solid dispersion with a poloxamer on a non-porous carrier, (c) a dispersion with a poloxamer deposited on a mesoporous carrier. Sample mixtures and dispersions with ibrutinib were tested to establish amorphism by various methods and to determine the solubility in aqueous media. The composition of ibrutinib-poloxamer P407-mesoporous carrier showed the best results in three standard media regarding the solubility of ibrutinib (increase in solubility at pH 1.2 - 129.6%, pH 4.5 - 300.2%, pH 6.8 - 363.3%). This composition became the basis for the tablet formulation and showed the best results in the Dissolution test (the dosage was dissolved in only 10 min of the test in pH 1.2 medium by 98.3%, pH 4.5 - 95.4%, pH 6.8 – 57.3%). These results were superior to those of the original Imbruvica capsules at all points in the study. In conclusion, the resulting formulation was stable under accelerated conditions according to the ICH Q1 Quality Guideline (40 °C, 75% relative humidity, 6 months).
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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) | 0.000 | 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 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".