NOVEL CRYSTALLINE POLYMORPHIC FORM OF A CAMPTOTHECIN ANALOGUE
First Claim
Patent Images
1. A crystalline form A of topotecan hydrochloride having an XRPD pattern with peaks at 6.08, 6.94, 8.10, 9.96, 10.16, 11.68, 12.28, 13.08, 13.62, 14.32, 15.44, 16.46, 16.56, 17.58, 18.42, 19.32;
- 20.14, 21.22, 21.88, 22.54, 22.72, 23.38, 24.14, 24.36, 24.78, 25.02, 25.50, 26.42, 26.86, 27.18, 27.44, 28.10, 28.76, 29.42, 29.68 and 30.02°
2θ
(±
0.2°
).
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Abstract
The invention relates to a novel crystalline form of topotecan hydrochloride, and methods of making the same. The characteristic XRPD pattern and FT-IT patterns are shown in
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Citations
21 Claims
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1. A crystalline form A of topotecan hydrochloride having an XRPD pattern with peaks at 6.08, 6.94, 8.10, 9.96, 10.16, 11.68, 12.28, 13.08, 13.62, 14.32, 15.44, 16.46, 16.56, 17.58, 18.42, 19.32;
- 20.14, 21.22, 21.88, 22.54, 22.72, 23.38, 24.14, 24.36, 24.78, 25.02, 25.50, 26.42, 26.86, 27.18, 27.44, 28.10, 28.76, 29.42, 29.68 and 30.02°
2θ
(±
0.2°
). - View Dependent Claims (3, 8, 20, 21)
- 20.14, 21.22, 21.88, 22.54, 22.72, 23.38, 24.14, 24.36, 24.78, 25.02, 25.50, 26.42, 26.86, 27.18, 27.44, 28.10, 28.76, 29.42, 29.68 and 30.02°
- 2. A crystalline form A of topotecan hydrochloride having characteristic FT-IR peaks at 1743, 1656, 1596, 1560 and 1507 cm−
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5. A crystalline form A of topotecan hydrochloride having an XRPD pattern as shown in
FIG. 1 .
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6. A crystalline form A of topotecan hydrochloride having an FT-IR spectrum as shown in
FIG. 2 .
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7. A crystalline form A of topotecan hydrochloride having a water content in the range of about 10 to 12 wt %.
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12. A process for preparing crystalline form A of topotecan hydrochloride, comprising:
suspending topotecan hydrochloride in methanol;
stirring at a temperature ranging from 25 to 30°
C.;
cooling the reaction mass to −
10 to 25°
C.; and
recovering the topotecan hydrochloride form A by filtration and drying.- View Dependent Claims (13, 14, 15, 19)
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16. A process for preparing crystalline form A of topotecan hydrochloride, comprises suspending topotecan base in methanol;
- adding aqueous HCl and stirring at 25-30°
C.;
cooling the reaction mass to a temperature ranging from −
10 to 25°
C.; and
recovering the topotecan hydrochloride form A by filtration and drying. - View Dependent Claims (17, 18)
- adding aqueous HCl and stirring at 25-30°
Specification