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Amorphous Adefuweizhi ester amorphous solid matter and its prepn

Adefovir dipivoxil and amorphous technology, which is applied in the field of adefovir dipivoxil amorphous solidified products and its preparation, can solve the problems of high cost, cumbersome operation, difficult medicine, etc., and achieve low cost, convenient operation, manufacturing and Formulated for easy effects

Inactive Publication Date: 2002-10-16
上海仲夏化学有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Usually, adefovir dipivoxil is obtained in the form of oil, which causes certain difficulties in the preparation of drugs. Even if there are reports about crystallization, the operation is cumbersome and the cost is high.

Method used

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  • Amorphous Adefuweizhi ester amorphous solid matter and its prepn

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Adefovir dipivoxil oil (5g) was added to a lyophilized vial, and ethanol (10ml) was added to dissolve at 15-20°C, then cooled to -75°C and rotated to solidify. Maintain -60~-50℃ for vacuum freeze-drying, and in the final stage, the temperature can be raised to -10~0℃ for drying. About 93% of the obtained adefovir dipivoxil amorphous cured product exists in an amorphous form.

Embodiment 2

[0016] Using chloroform (5ml) instead of ethanol (10ml), the others were the same as in Example 1 to obtain an amorphous solidified product of adefovir dipivoxil, of which about 90% existed in an amorphous form.

Embodiment 3

[0018] Adefovir dipivoxil oil (5 g) was added to a lyophilized vial, and benzene (10 ml) was added to dissolve at 15-20° C., then cooled to -10° C. and rotated to solidify. Maintain vacuum freeze-drying at -10-0°C, and heat up to 5-10°C for drying in the final stage. About 95% of the obtained adefovir dipivoxil amorphous cured product exists in an amorphous form. Example 4

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PUM

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Abstract

The present invention is amorphous Adefuweichi ester solid matter and its preparation process. The amorphous Adefuweichi ester solid matter is solid powder obtained through solidifying oil amorphous Adefuweichi ester and has, X-ray test shows, at least 80% amorphous component. The amorphous Adefuweichi ester solid matter of the present invention is easy to filter and dry, has excellent flowability and bulk density performance, and the present invention makes it easy to produce medicine composite containing Adefuweichi ester and its suitable for industrial production.

Description

technical field [0001] The invention relates to the field of medicinal chemistry, in particular to an amorphous cured product of adefovir dipivoxil and a preparation method thereof. Background technique [0002] The chemical name of Adefovir Dipivoxil is: 9-[2-[bis(pivaloyloxymethoxy)phosphonomethoxy]ethyl]adenine. Adefovir dipivoxil is a new type of antiviral drug, it can be used for the treatment of human or animal retrovirus infection (HIV, SIV, FIV), hepatitis B virus or other hepatitis virus, DNA virus infection (human cytomegalovirus virus or herpes virus, such as HSV1 or HSV2), etc. European Patent EP481214; Starrett et al., J.Med.Chem., 1994, 37:1857-1864; Starrett et al., Antiviral Res., 1992, 19:267-273; Benzaria et al., J.Med.Chem., 1996, 39 : 4958-4965; Zhang Yong et al., Journal of Shenyang Pharmaceutical University, 2001, 18(2): 95-97. Usually, adefovir dipivoxil is obtained in the form of oil, which causes certain difficulties in the preparation of the drug...

Claims

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Application Information

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IPC IPC(8): A61K31/675A61P31/12C07F9/6561
Inventor 张磊李辉夏文戟
Owner 上海仲夏化学有限公司
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