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Method for preparing hydrocortisone sodium succinate

A technology of hydrocortisone sodium succinate and pine succinic acid, applied in the field of medicinal chemistry, can solve the problems of increased process complexity, small production scale, high drying cost, stable product quality, stable reaction process, and reduced production cost. Effect

Active Publication Date: 2009-12-30
HENAN LIHUA PHARMA
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Problems solved by technology

[0008] The traditional production process of hydrocortisone sodium succinate salification is based on hydrocortisone succinic acid as raw material, which is dissolved in water to form salt. The disadvantages are: small production scale, low yield, high drying cost, and difficult dry
Chinese patent application number 200710057321.5 discloses a method for preparing hydrocortisone sodium succinate from hydrocortisone succinate monoester, but this method needs to react with buffer solution first, which increases the complexity of the process

Method used

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  • Method for preparing hydrocortisone sodium succinate

Examples

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Embodiment 1

[0014] Preparation of hydrocortisone succinic acid monoester: put 1Kg of hydrocortisone and 1.9kg of dimethylformamide into a dry reaction tank, stir to dissolve at 20-25°C. Open interlayer brine and cool down to 10±1°C, add 0.22Kg triethylamine, then slowly add 0.8Kg succinic anhydride, control the temperature at 15±1°C for 3.5 hours. Dilute it in 15Kg of purified water cooled to 2°C while stirring, let it stand at 5-8°C for 3 hours, filter and discharge, the refined product is white powder, and the yield is 95.2%.

Embodiment 2

[0016] Synthesis of hydrocortisone sodium succinate: 50 g of hydrocortisone succinate monoester was obtained by the method in Example 1, added into 200 ml of purified water at a dissolving temperature of 0-10° C., and stirred for about 50 minutes to dissolve completely. Add 9g of sodium bicarbonate, slowly add a proportion of acetone 100ml, add dropwise at a rate of about 2ml / min, after the dropwise addition, control the temperature at 0-10°C, keep warm for 2h, gradually dissolve, add 2.5g of charcoal, and decolorize for 30min , filter with filter bucket, concentrate under reduced pressure, T≤30℃, vacuum should be ≤-0.08MPa, concentrate to 46.32g of hydrocortisone sodium succinate, the color is white or off-white powder. The yield is 92.64%, and the melting point is 170℃ .

Embodiment 3

[0018] Synthesis of hydrocortisone sodium succinate: 50 g of hydrocortisone succinate monoester was obtained by the method in Example 1, added into 165 ml of purified water at a dissolving temperature of 10-20° C., and stirred for about 40 minutes to dissolve completely. Add 4.3g of sodium hydroxide, slowly add a proportioning amount of acetone 100ml, add dropwise at a rate of about 2ml / min, after the dropwise addition, control the temperature at 10-20°C, keep warm for 1.5h, gradually dissolve, add 2.5g of charcoal, Decolorize for 30 minutes, filter with filter funnel, concentrate under reduced pressure, T≤30℃, vacuum should be ≤-0.08MPa, concentrate to 45.86g of hydrocortisone sodium succinate, the color is white or off-white powder. The yield is 91.72%, melting point 170°C.

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Abstract

The invention provides a method for preparing hydrocortisone sodium succinate and belongs to the medicinal chemistry field. The method comprises the following steps: taking hydrocortisone hemisuccinat as raw material; adding pure water for dissolving under the temperature of 0-60 DEG C; adding sodium alkali to cause the pH value to be 7.5-11.0; adding acetone continuously drop by drop; preserving the temperature of 10-20 DEG C for reaction for 1-2h after dropwise adding; adding carbon into the reacted product for decoloring followed by filtering, reduced pressure concentrating and drying to obtain the product in the invention. The method in the invention has low reaction temperature and rapid reaction speed, is difficult to generate other impurities in the reaction process, and has less side reaction and high yield after concentration.

Description

1. Technical field: [0001] The invention relates to a preparation method of hydrocortisone sodium succinate, which belongs to the field of medicinal chemistry. 2. Background technology: [0002] Hydrocortisone sodium succinate is a salt compound of hydrocortisone, an adrenocortical hormone drug. It has various pharmacological effects such as anti-inflammatory, anti-allergic and immune suppression. Clinically, it is mostly used in the treatment of acute allergic diseases, status asthmaticus, adrenal crisis attack, and infectious toxic shock. It is also commonly used in the treatment of malignant lymphoma. Has the following pharmacological effects: [0003] (1) Anti-inflammatory effect: Glucocorticoids reduce and prevent tissue responses to inflammation, thereby reducing the manifestations of inflammation. [0004] (2) Immunosuppressive effect: prevent or inhibit cell-mediated immune response, delay allergic reaction, and reduce the expansion of primary immune response. ...

Claims

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Application Information

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IPC IPC(8): C07J5/00
Inventor 王泉常志刚孙传源李成发姬卫忠李新安宋永新
Owner HENAN LIHUA PHARMA
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