Preparation method of andrographolide bulk pharmaceutical

Abstract

The invention discloses a novel preparation method of an andrographolide bulk pharmaceutical, belonging to the field of pharmaceutical chemistry. The method comprises the following steps of: reacting andrographolidume serving as a raw material with succinyl oxide under the action of a catalyst to obtain a 14-deoxy-11,12-didehydroandrographolidume-3,19-disuccinate (dehydroandrographolide succinate) intermediate at high yield and high quality; reacting the intermediate with a mixed salt; and crystalizing to directly obtain andrographolide which is consistent with an injection standard. The andrographolide bulk pharmaceutical has the advantages of mild reaction conditions, total reaction yield of over 70 percent and purity of over 98 percent, and is suitable for industrial production.

Description

technical field

[0001] The invention relates to a preparation method of Yanhuning, which belongs to the field of medicinal chemistry. Background technique

[0002] The chemical name of Yanhuning is 14-deoxy-11,12-didehydroandrographolide-3,19-disuccinic acid half ester sodium potassium salt, which has heat-clearing, detoxifying and anti-viral effects, and is mainly used for viral pneumonia and virus For acute upper respiratory tract infection, Yanhuning and its injection are included in the national drug standards. At present, the preparation method of Yanhuning has the following public literature reports:

[0003] Invention patent CN1557812 "Andrographolide succinate half ester sodium potassium salt and its preparation" The method is to take the prescribed amount of Yanhuning, make a suspension with water for injection, and then use a certain amount of 2-4% sodium bicarbonate The solution is dissolved and clarified, and the pH value is adjusted within the range of 6.5-7.5...