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Thermally stable crystalline epirubicin hydrochloride

A kind of epirubicin hydrochloride and crystallization technology, applied in the field of epirubicin hydrochloride

Inactive Publication Date: 2011-08-31
苏洛克股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, some time later, U.S. Patent No. 7,091,469 disclosed that the stability of such amrubicin was more likely to be related to the formation of solvates than to the crystal structure of the substance

Method used

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  • Thermally stable crystalline epirubicin hydrochloride
  • Thermally stable crystalline epirubicin hydrochloride
  • Thermally stable crystalline epirubicin hydrochloride

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] (1) A solution (pH 3-4) of epirubicin hydrochloride (10.0 g) in water or an ethanol-water mixture was subjected to low-pressure evaporation at 40° C. until it was in a gel state of the solution.

[0048] (2) Then, 1-propanol in an amount 12 times the volume of the remaining solution was added to the remaining solution, and stirred at a temperature of 60° C. for 3 hours.

[0049] (3) The precipitated epirubicin hydrochloride crystals were then collected by filtration, washed in 10 ml of acetone and dried at room temperature.

[0050] (4) The product was 9.3 g of type II epirubicin hydrochloride crystals.

[0051] (5) if Figure 10 As shown, Form II crystalline epirubicin hydrochloride has a melting point of approximately 207°C with decomposition (hot stage 2°C / min). Figure 12 The IR spectrum (IR(KBr)) of Form II crystalline epirubicin hydrochloride is shown. At 3415, 2928, 1720, 1620, 1576, 1510, 1413, 1371, 1284, 1239, 1210, 1162, 1115, 1068, 1019, 991, 930, 908, 88...

Embodiment 2

[0053] (1) A solution (pH 3-4) of epirubicin hydrochloride (10.0 g) in water or an ethanol-water mixture was subjected to low-pressure evaporation at 40° C. until the gel state of the solution was reached.

[0054] (2) Then add pure ethanol in an amount 10 times the volume of the original solution to the remaining solution, and stir at a temperature of 60° C. for 2 hours.

[0055] (3) The precipitated epirubicin hydrochloride crystals were then collected by filtration, washed in 10 ml of ethanol and 10 ml of acetone and dried at room temperature.

[0056] (4) The product is 7.5 g of type II epirubicin hydrochloride crystals.

Embodiment 3

[0059] (1) This step is the same as Step 1 in Example 1 above.

[0060] (2) Pour 300ml of acetone into the gel solution of epirubicin hydrochloride.

[0061] (3) The precipitated epirubicin hydrochloride crystals were then collected by filtration and washed in 50 ml of acetone.

[0062] (4) The product was 9.7 g of type I epirubicin hydrochloride crystals.

[0063] Such as Figure 12 As shown, Form I crystalline epirubicin hydrochloride has a melting point of approximately 196°C with decomposition (hot stage 2°C / min). Figure 13 The IR spectrum (IR(KBr)) of epirubicin hydrochloride type I is shown. at 3430, 2934, 2027, 1724, 1617, 1583, 1508, 1445, 1412, 1284, 1236, 1211, 1162, 1121, 1064, 1018, 992, 931, 909, 876, 814, 792, 767, 738, 721 , 693, 588 and 465cm -1 See peaks / valleys everywhere.

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Abstract

A crystalline form of epirubicin hydrochloride, named herein as 'type II' crystalline epirubicin hydrochloride, has excellent thermal stability. Type II crystalline epirubicin hydrochloride has a powder X-ray diffraction pattern having average values of diffraction angle (2 theta) and relative intensity P(%) as presented in the Table of Fig. 1.

Description

[0001] related application [0002] This application is a continuation-in-part of U.S. Patent Application No. 10 / 877,221, filed June 25, 2004 (now U.S. Patent No. ____________), which requires U.S. Provisional Application No. 60 / 484,132 entitlement. Priority to the foregoing applications is hereby expressly claimed under 35 U.S.C. §§ 119, 120 and any other applicable statute and the contents of each foregoing application are hereby incorporated by reference in their entirety. technical field [0003] The field of the invention relates generally to crystalline (crystalline) form of epirubicin hydrochloride, a compound useful as an anticancer chemotherapeutic agent. In particular, the field of the invention relates to specific crystalline forms of epirubicin hydrochloride characterized by improved thermal stability. Furthermore, the present invention relates to a method for producing the aforementioned crystalline form of epirubicin hydrochloride, and a method for using the af...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/24
CPCC07H15/24
Inventor 亚历山大·扎布德金维克托·马特维安科阿列克埃·马特维韦亚历山大·伊特金
Owner 苏洛克股份有限公司
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