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OBJECTIVE To prepare methotrexate (MTX)-nicotinamide (NIC) coamorphous (MTX-NIC CA), evaluate its pharmacokinetic behavior in rats, and explore its solubilization mechanism. METHODS The coamorphous complex was prepared by melting method and characterized by powder X-ray diffraction and other techniques; the physical stability and thermodynamic stability of MTX-NIC CA were examined. The solubilization mechanism was studied by solubility profile method. The concentration of MTX in rat plasma was determined by high-performance liquid chromatography and the pharmacokinetic curve was drawn. RESULTS The physical stability of MTX-NIC CA was good; the reaction of MTX with NIC was a spontaneous enthalpy-driven reaction, and the mechanism of NIC for enhancing the solubility of MTX was that a soluble AL-type complex with a ligand-to-metal ratio of 1∶1 was formed in solution. Compared with the raw drug MTX, the tmax of MTX-NIC CA was prolonged, and the cmax, AUC0-t, AUC0-∞ and F were significantly increased (P<0.05). CONCLUSION The MTX-NIC CA is successfully prepared by melting method with good stability, and the formation of co-amorphous complex improves the bioavailability of poorly soluble drugs.
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| 科 Family | 属数 Number of genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) | 属 Genus | 种数 Number of species | 占总种数比例 Percentage of total species (%) |
|---|---|---|---|---|---|---|
| 鹅膏菌科Amanitaceae | 2 | 11 | 5.26 | 鹅膏菌属 Amanita | 10 | 4.78 |
| 小菇科 Mycenaceae | 2 | 12 | 5.74 | 丝盖伞属 Inocybe | 5 | 2.39 |
| 多孔菌科 Polyporaceae | 8 | 14 | 6.70 | 蜡蘑属 Laccaria | 5 | 2.39 |
| 红菇科 Russulaceae | 3 | 23 | 11.00 | 小皮伞属 Marasmius | 6 | 2.87 |
| 小菇属 Mycena | 11 | 5.26 | ||||
| 光柄菇属 Pluteus | 5 | 2.39 | ||||
| 红菇属 Russula | 17 | 8.13 | ||||
| 栓菌属 Trametes | 5 | 2.39 |
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