Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Patent
1998-04-29
2000-10-03
Dees, Jose'G.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
514171, 540114, A61K 3158, C07J 1700
Patent
active
061273538
DESCRIPTION:
BRIEF SUMMARY
BACKGROUND OF THE INVENTION
The present invention relates to a novel composition of matter, 9.alpha., 21-dichloro-16.alpha.-methyl-1,4-pregnadiene-11.beta.,17.alpha.-diol-3,20- dione-17-(2'-furoate) monohydrate, also designated mometasone furoate monohydrate, process for its preparation, and pharmaceutical preparation thereof.
Mometasone furoate is known to be useful in the treatment of inflammatory conditions. The compound is prepared by procedures disclosed in U.S. Pat. No. 4,472,393, which patent is hereby incorporated by reference.
When aqueous pharmaceutical compositions, e.g. suspensions, containing anhydrous mometasone furoate were subjected to stability testing by rotating for four weeks at room temperature and 35.degree. C., formation of a crystalline material which is different from the anhydrous mometasone furoate crystal was observed in suspension. Experiments were designed to determine the nature of the crystalline material. It was postulated that formulation of mometasone furoate compositions with the stable crystalline form would reduce the probability of crystal growth during long term storage of the suspension leading to a more stable product.
SUMMARY OF THE INVENTION
The present invention provides mometasone furoate monohydrate of formula I ##STR1## a process for preparing said compound by crystallization from a saturated aqueous water miscible organic solution. The present invention also provides aqueous stable pharmaceutical compositions of mometasone furoate monohydrate.
DESCRIPTION OF THE FIGURES
FIG. 1: Infrared spectrum of crystalline mometasone furoate monohydrate
FIG. 2: X-ray diffraction pattern of crystalline mometasone furoate monohydrate
DETAILED DESCRIPTION OF THE INVENTION
The composition of matter of the present invention, mometasone furoate monohydrate has the following characteristics. H=5.56%; Cl=13.17%
The crystalline mometasone furoate monohydrate exhibits an x-ray crystallographic powder diffraction pattern having essentially the values as shown in Table I.
TABLE 1 ______________________________________
Angle of Spacing
2.theta. d Relative Intensity
(degrees) (.ANG.) .vertline./.vertline.
______________________________________
7.795 11.3324 100
11.595 7.6256 6
12.035 7.3478 3
12.925 6.8437 11
14.070 6.2893 22
14.580 6.0704 5
14.985 5.9072 12
15.225 5.8146 33
15.635 5.6631 96
16.710 5.3011 15
17.515 5.0592 14
18.735 4.7324 12
20.175 4.3978 13
20.355 4.3593 6
20.520 4.3246 4
21.600 4.1108 5
21.985 4.0396 22
22.420 3.9622 8
22.895 3.8811 7
22.245 3.8234 14
23.550 3.7746 13
24.245 3.6680 4
24.795 3.5878 11
24.900 3.5729 5
24.800 3.4503 5
25.985 3.4262 3
26.775 3.3268 84
27.170 3.2794 10
27.305 3.2635 9
27.710 3.2167 5
28.385 3.1417 7
29.165 3.0594 1
29.425 3.0330 2
29.725 3.0030 2
30.095 2.9670 7
30.255 2.1516 3
30.490 2.9294 10
30.725 2.9075 6
31.115 2.8720 3
31.595 2.8294 47
32.135 2.7831 6
32.985 2.7133 7
33.400 2.6805 2
33.820 2.6482 2
34.060 2.6301 8
34.625 2.5885 4
34.795 2.5762 2
35.315 2.5394 1
36.780 2.4416 21
37.295 2.4090 2
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Single crystal data of mometasone furoate monohydrate exhibits the following values as shown in Table II.
TABLE II ______________________________________
Crystallographic Data.sup.a
Crystal system triclinic
Space group P1(C.sup.1.sub.1)-No. 1
______________________________________
a (.ANG.) 8.481 (1)
b (.ANG.) 11.816 (2)
c(.ANG.) 7.323 (1)
.alpha.(.degree.)
95.00 (1)
.beta.(.degree.)
110.66 (1)
.gamma.(.degree.)
73.27 (1)
V (.ANG..sup.3)
657.5 (3)
D.sub.calcd. (g cm.sup.-3)
1.362.sup.
______________________________________
a An Enraf-Nonius CAD-4 diffractometer (Cu-K.alpha. radiation, incident-beam graphite monochromator) was used for all measurements, Intensity data were corrected for the usual Lorentz and polarization effects; an empirical absorption correction was a
REFERENCES:
patent: 4472393 (1984-09-01), Shapiro
patent: 4775529 (1988-10-01), Sequeira et al.
patent: 4783444 (1988-11-01), Watkins et al.
Eckhart Charles
Etlinger Teresa
Levine Nancy
Yuen Pui-Ho
Badio Barbara
Battle Carl W.
Dees Jose'G.
Franks Robert A.
Maitner John J.
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