Research Article
Development of an Oral Form of Azacytidine: Triacetyl-5-Azacytidine
Table 1
Stability of TAC and its metabolites at various pH.
| Sample | TAC (%) | DAC (%) | MAC (%) | ACT (%) |
| Control | 100 | | | |
| pH 1—1 hr | 99 | 1 | 0 | 0 | pH 1—3 hr | 74 | 22 | 4 | 0 | pH 1—6 hr | 38 | 41 | 21 | 0 | pH 1—29 hr | 1 | 22 | 31 | 46 |
| pH 3—1 hr | 97 | 3 | 0 | 0 | pH 3—3 hr | 96 | 4 | 0 | 0 | pH 3—6 hr | 92 | 6 | 2 | 0 | pH 3—29 hr | 93 | 4 | 2 | 1 |
| pH 5—1 hr | 98 | 2 | 0 | 0 | pH 5—3 hr | 94 | 6 | 0 | 0 | pH 5—6 hr | 98 | 2 | 0 | 0 | pH 5—29 hr | 94 | 4 | 1 | 1 |
| pH 7.4—1 hr | 96 | 4 | 0 | 0 | pH 7.4—3 hr | 91 | 7 | 2 | 0 | pH 7.4—6 hr | 85 | 12 | 3 | 0 | pH 7.4—29 hr | 69 | 17 | 13 | 1 |
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TAC: tri-acetyl-azacitidine; DAC: di-acetyl-azacitidine; MAC: mono-acetyl-azacitidine; ACT: azacitidine.
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