Modafinil compositionsc
A technology of composition and formation, applied in the direction of organic chemistry, etc., can solve problems such as poor solubility
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Embodiment 1
[0380] Racemic modafinil: malonic acid cocrystal
[0381] To a solution containing racemic modafinil (150 mg, 0.549 mmol) in acetic acid (600 microliters) was added malonic acid (114.9 mg, 1.104 mmol). The mixture was then heated on a hot plate at 67°C until all material dissolved. The solution was then dried under a stream of nitrogen to yield a 1:1 modafinil:malonic acid cocrystal as a colorless solid. The solid material was characterized using PXRD. The material was then dried overnight under a stream of nitrogen to yield the same material with a slight excess of malonate. The colorless solid was characterized by PXRD (Bruker), DSC, TGA, IR and Raman spectroscopy. The PXRD data of modafinil: malonic acid (1: 1) cocrystal is listed in Table IV, and the diffraction pattern is as figure 1 As shown in (data as is). DSC indicates an endothermic transition at about 106°C, and the differential thermogram is shown in figure 2 shown in . TGA differential thermal analysis ...
Embodiment 2
[0386] Racemic Modafinil: Glycolic Acid Cocrystal
[0387] Racemic modafinil (1 mg, 0.0037 mmol) and glycolic acid (0.30 mg, 0.0037 mmol) were dissolved in acetone (400 microliters). The solution was evaporated to dryness and the resulting solid was characterized by PXRD (Rigaku). PXRD data for modafinil:glycolic acid cocrystals are listed in Table IV. see Figure 8A and 8B . Figure 8A Represents the PXRD diffractogram after subtraction of background noise. Figure 8B Indicates the original PXRD data as is.
[0388] An alternative method of preparing modafinil: glycolic acid co-crystals was also performed. To a solution of modafinil (1 mg, 0.0037 mmol) dissolved in a mixture of acetone and methanol (3:1, 100 μl) was added glycolic acid (0.28 mg, 0.0037 mmol) dissolved in methanol (50 μl) ). The solvent was then evaporated to dryness under a stream of nitrogen to obtain a mixture of the two starting components. Acetone (200 microliters) was then added to the mixture...
Embodiment 3
[0390] Racemic modafinil:maleic acid cocrystal
[0391]To a solution of modafinil (150 mg, 0.549 mmol) in acetic acid (600 microliters) was added maleic acid (30.7 mg, 0.264 mmol). The mixture was then heated on a hot plate at 67°C until all material dissolved. The solution was then dried under a stream of nitrogen to yield a colorless amorphous material. Store the amorphous material in a sealed vial at room temperature. After 2 days, a solid material started to form which was collected and characterized using PXRD (Rigaku) as modafinil:maleic acid co-crystals as Figure 9A and 9B shown. Figure 9A Represents the PXRD diffractogram after subtraction of background noise. Figure 9B Represents raw PXRD data. PXRD data for modafinil:maleic acid cocrystals are listed in Table IV. Modafinil: maleic acid cocrystals can be obtained by Figure 9A Characterized by any one, any two, any three, any four, any five or any six or more peaks, including but not limited to 4.69, 6....
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