CN1675177A - 莫达非尼多晶型 - Google Patents
莫达非尼多晶型 Download PDFInfo
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- CN1675177A CN1675177A CNA038190850A CN03819085A CN1675177A CN 1675177 A CN1675177 A CN 1675177A CN A038190850 A CNA038190850 A CN A038190850A CN 03819085 A CN03819085 A CN 03819085A CN 1675177 A CN1675177 A CN 1675177A
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- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
Abstract
Description
2θ(度) | d() | I/I0(%) |
8.99 | 9.83 | 42 |
10.16 | 8.70 | 18 |
11.12 | 7.95 | 14 |
12.85 | 6.88 | 24 |
15.14 | 5.85 | 13 |
15.73 | 5.63 | 41 |
16.32 | 5.43 | 13 |
17.71 | 5.00 | 11 |
18.06 | 4.91 | 47 |
19.23 | 4.61 | 50 |
20.38 | 4.35 | 100 |
21.58 | 4.12 | 8 |
21.84 | 4.07 | 10 |
22.39 | 3.97 | 7 |
23.12 | 3.84 | 33 |
23.63 | 3.76 | 7 |
24.44 | 3.64 | 20 |
25.80 | 3.450 | 13 |
26.04 | 3.419 | 8 |
26.55 | 3.354 | 12 |
27.26 | 3.268 | 17 |
27.69 | 3.219 | 5 |
28.59 | 3.119 | 6 |
2θ(度) | d() | I/I0(%) |
8.95 | 9.87 | 72 |
10.11 | 8.74 | 19 |
10.92 | 8.09 | 15 |
11.84 | 7.47 | 20 |
14.16 | 6.25 | 37 |
15.08 | 5.87 | 19 |
16.25 | 5.45 | 15 |
17.40 | 5.09 | 48 |
17.66 | 5.02 | 21 |
17.97 | 4.93 | 51 |
19.76 | 4.49 | 16 |
20.35 | 4.36 | 100 |
21.10 | 4.21 | 40 |
21.76 | 4.08 | 16 |
22.36 | 3.97 | 10 |
23.61 | 3.76 | 9 |
24.44 | 3.64 | 19 |
25.14 | 3.54 | 15 |
25.74 | 3.458 | 12 |
26.52 | 3.358 | 13 |
27.12 | 3.285 | 15 |
28.59 | 3.119 | 9 |
29.6 | 3.039 | 8 |
2θ(度) | d() | I/I0(%) |
6.04 | 14.6 | 5 |
6.72 | 13.1 | 100 |
10.27 | 8.60 | 9 |
13.48 | 6.57 | 18 |
14.04 | 6.30 | 8 |
16.28 | 5.44 | 5 |
16.99 | 5.21 | 7 |
18.27 | 4.85 | 7 |
20.14 | 4.41 | 10 |
20.68 | 4.29 | 5 |
21.43 | 4.14 | 6 |
22.04 | 4.03 | 5 |
22.51 | 3.95 | 35 |
22.98 | 3.87 | 5 |
24.76 | 3.59 | 9 |
26.30 | 3.386 | 4 |
27.13 | 3.284 | 11 |
27.47 | 3.245 | 7 |
28.42 | 3.138 | 4 |
2θ(度) | d() | I/I0(%) |
7.77 | 11.4 | 14 |
10.48 | 8.44 | 49 |
11.52 | 7.67 | 35 |
11.94 | 7.40 | 28 |
13.30 | 6.65 | 29 |
14.19 | 6.24 | 31 |
15.59 | 5.68 | 43 |
16.44 | 5.39 | 31 |
16.76 | 5.29 | 47 |
18.05 | 4.91 | 33 |
19.09 | 4.64 | 100 |
19.46 | 4.56 | 42 |
20.16 | 4.40 | 38 |
20.48 | 4.33 | 34 |
21.80 | 4.07 | 39 |
22.11 | 4.02 | 35 |
22.97 | 3.87 | 58 |
23.38 | 3.80 | 51 |
23.92 | 3.72 | 35 |
24.74 | 3.60 | 35 |
26.00 | 3.424 | 24 |
26.92 | 3.309 | 28 |
2θ(度) | d() | I/I0(%) |
7.28 | 12.1 | 28 |
10.44 | 8.47 | 100 |
12.16 | 7.27 | 6 |
14.63 | 6.05 | 11 |
15.80 | 5.60 | 5 |
16.32 | 5.43 | 5 |
17.40 | 5.09 | 6 |
17.80 | 4.98 | 20 |
18.17 | 4.88 | 7 |
19.92 | 4.45 | 9 |
20.44 | 4.34 | 5 |
20.97 | 4.23 | 11 |
21.55 | 4.12 | 3 |
22.02 | 4.03 | 28 |
22.35 | 3.98 | 8 |
23.57 | 3.77 | 2 |
24.05 | 3.70 | 4 |
24.49 | 3.63 | 3 |
26.09 | 3.412 | 7 |
26.44 | 3.368 | 3 |
26.99 | 3.301 | 3 |
27.46 | 3.24 | 3 |
28.04 | 3.179 | 6 |
29.26 | 3.050 | 4 |
2θ(度) | d() | I/I0(%) |
6.95 | 12.7 | 100 |
10.49 | 8.42 | 14 |
13.72 | 6.45 | 21 |
14.25 | 6.21 | 8 |
17.30 | 5.12 | 4 |
18.68 | 4.75 | 4 |
19.85 | 4.47 | 4 |
20.11 | 4.41 | 6 |
20.48 | 4.33 | 6 |
21.01 | 4.23 | 10 |
21.73 | 4.09 | 5 |
22.72 | 3.91 | 50 |
2θ(度) | d() | I/I0(%) |
6.67 | 13.3 | 100 |
8.90 | 9.93 | 18 |
10.25 | 8.62 | 37 |
11.073 | 7.98 | 15 |
11.78 | 7.50 | 15 |
12.87 | 6.87 | 13 |
13.45 | 6.58 | 21 |
13.98 | 6.33 | 24 |
15.08 | 5.87 | 12 |
15.66 | 5.65 | 15 |
16.25 | 5.45 | 18 |
16.97 | 5.22 | 22 |
17.31 | 5.12 | 17 |
18.22 | 4.87 | 23 |
19.21 | 4.62 | 17 |
19.73 | 4.50 | 20 |
20.09 | 4.42 | 31 |
20.31 | 4.37 | 40 |
20.62 | 4.30 | 28 |
21.11 | 4.21 | 20 |
21.38 | 4.15 | 20 |
21.93 | 4.05 | 16 |
22.52 | 3.95 | 59 |
22.94 | 3.87 | 15 |
24.41 | 3.64 | 11 |
24.75 | 3.59 | 20 |
25.14 | 3.54 | 8 |
25.84 | 3.445 | 7 |
26.44 | 3.368 | 12 |
27.18 | 3.278 | 15 |
27.48 | 3.243 | 15 |
28.28 | 3.153 | 9 |
29.08 | 3.068 | 6 |
2θ(度) | d() | I/I0(%) |
7.07 | 12.5 | 18 |
11.18 | 7.91 | 42 |
14.12 | 6.27 | 53 |
15.77 | 5.61 | 41 |
18.02 | 4.92 | 53 |
19.97 | 4.44 | 100 |
20.71 | 4.29 | 62 |
21.24 | 4.18 | 75 |
22.44 | 3.96 | 57 |
25.13 | 3.54 | 37 |
25.55 | 3.484 | 67 |
27.04 | 3.294 | 18 |
28.44 | 3.136 | 33 |
29.34 | 3.041 | 11 |
2θ(度) | d() | I/I0(%) |
6.68 | 13.2 | 100 |
8.90 | 9.93 | 23 |
10.20 | 8.66 | 63 |
10.80 | 8.19 | 18 |
13.43 | 6.59 | 27 |
13.98 | 6.33 | 33 |
15.06 | 5.88 | 15 |
16.28 | 5.44 | 17 |
17.00 | 5.21 | 31 |
17.36 | 5.10 | 20 |
18.27 | 4.85 | 27 |
19.74 | 4.49 | 28 |
20.08 | 4.42 | 40 |
20.61 | 4.31 | 44 |
21.37 | 4.15 | 29 |
21.99 | 4.04 | 32 |
22.52 | 3.95 | 81 |
22.96 | 3.87 | 20 |
24.43 | 3.64 | 15 |
24.75 | 3.59 | 26 |
26.28 | 3.388 | 15 |
26.52 | 3.358 | 12 |
27.13 | 3.285 | 15 |
27.44 | 3.248 | 18 |
28.40 | 3.140 | 14 |
29.09 | 3.067 | 9 |
29.54 | 3.022 | 8 |
2θ(度) | d() | I/I0(%) |
6.95 | 12.7 | 21 |
9.80 | 9.02 | 32 |
11.00 | 8.03 | 46 |
13.89 | 6.37 | 18 |
15.57 | 5.69 | 40 |
17.73 | 5.00 | 29 |
19.72 | 4.50 | 100 |
20.34 | 4.36 | 26 |
20.92 | 4.24 | 19 |
22.08 | 4.02 | 44 |
24.68 | 3.61 | 22 |
25.16 | 3.54 | 68 |
28.02 | 3.181 | 7 |
29.74 | 3.002 | 15 |
2θ(度) | d() | I/I0(%) |
6.99 | 12.6 | 18 |
11.08 | 7.98 | 59 |
14.08 | 6.29 | 44 |
15.11 | 5.86 | 42 |
15.67 | 5.65 | 57 |
16.26 | 5.45 | 42 |
17.68 | 5.01 | 45 |
17.91 | 4.95 | 58 |
18.96 | 4.68 | 40 |
19.84 | 4.47 | 100 |
20.40 | 4.35 | 78 |
21.11 | 4.21 | 56 |
21.72 | 4.09 | 35 |
22.26 | 3.99 | 58 |
24.45 | 3.64 | 33 |
24.94 | 3.57 | 48 |
25.39 | 3.51 | 83 |
26.49 | 3.361 | 36 |
27.18 | 3.277 | 28 |
28.30 | 3.150 | 26 |
2θ(度) | d() | I/I0(%) |
7.06 | 12.5 | 19 |
8.99 | 9.82 | 21 |
10.20 | 8.67 | 21 |
11.08 | 7.97 | 63 |
11.86 | 7.45 | 28 |
13.04 | 6.78 | 34 |
14.15 | 6.26 | 52 |
15.16 | 5.84 | 45 |
15.74 | 5.63 | 66 |
16.30 | 5.43 | 42 |
17.42 | 5.09 | 70 |
17.96 | 4.94 | 73 |
19.08 | 4.65 | 34 |
19.88 | 4.46 | 94 |
20.37 | 4.36 | 100 |
21.17 | 4.19 | 78 |
21.78 | 4.08 | 42 |
22.36 | 3.97 | 56 |
23.61 | 3.76 | 28 |
24.45 | 3.64 | 35 |
25.08 | 3.55 | 39 |
25.45 | 3.497 | 85 |
26.05 | 3.418 | 28 |
26.56 | 3.353 | 34 |
27.25 | 3.269 | 26 |
27.68 | 3.220 | 26 |
28.39 | 3.141 | 27 |
阶段1第1天 | 阶段2第8天 | 阶段3第15天 | |
狗1 | B | C | A |
狗2 | C | A | B |
狗3 | A | B | C |
狗4 | C | B | A |
狗5 | B | A | C |
狗6 | A | C | B |
晶型 | Cmax(μg/ml) | C4h(μg/ml) | AUC0-24h(h.μg/ml) | 标准化的AUC |
I | 18.60±2.30 | 15.37±2.56 | 164.80±23.75 | 5.49 |
IV | 24.98±1.12 | 21.23±1.88 | 200.69±18.09 | 6.69 |
晶型 | MRT(h) | C1h(μg/ml) | C1.5h(μg/ml) | C2h(μg/ml) | C2.5h(μg/ml) | Cmax(μg/ml) | Tmax(h) |
I | 6.91±0.53 | 8.81±2.45 | 12.73±2.39 | 14.16±2.23 | 14.23±1.95 | 18.60±2.30 | 3.00 |
V | 6.11±0.36 | 12.41±2.07 | 15.31±2.06 | 16.56±2.48 | 16.37±2.38 | 18.72±2.09 | 1.67 |
Claims (49)
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US40206402P | 2002-08-09 | 2002-08-09 | |
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US10/635,445 | 2003-08-07 | ||
US10/635,445 US6992219B2 (en) | 2002-08-09 | 2003-08-07 | Modafinil polymorphic forms |
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FR2804322B1 (fr) * | 2000-01-31 | 2002-04-19 | Lafon Labor | Utilisation du modafinil pour la fabrication d'un medicament destine a corriger les troubles de la vigilance associes aux myopathies |
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CA2416792C (en) * | 2000-07-27 | 2010-02-09 | Teva Pharmaceutical Industries Ltd. | Crystalline and pure modafinil, and process of preparing the same |
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AR045314A1 (es) | 2003-05-13 | 2005-10-26 | Cephalon Inc | Composiciones farmaceuticas de analepticos y antidepresivos |
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AR045423A1 (es) | 2003-05-13 | 2005-10-26 | Cephalon Inc | Combinaciones de analiticos y antidepresivos |
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ATE442352T1 (de) | 2003-05-16 | 2009-09-15 | Cephalon France | Verfahren zur herstellung von modafinil |
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2003
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- 2003-08-08 WO PCT/IB2003/003215 patent/WO2004014846A1/en active Application Filing
- 2003-08-08 AU AU2003253128A patent/AU2003253128B2/en not_active Ceased
- 2003-08-08 EP EP03784340A patent/EP1575915A1/en not_active Withdrawn
- 2003-08-08 CN CN201210395545.8A patent/CN102875429B/zh not_active Expired - Fee Related
- 2003-08-08 CN CN2012103955547A patent/CN102875430A/zh active Pending
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