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Preparation of tanshinol ethyl ester, pharmaceutical composition containing tanshinol ethyl ester and application of pharmaceutical composition in preparation of medicine for treating ischemic stroke

A technology for ischemic stroke and ethyl acetate, applied in the field of medicine, can solve the problems of limiting the protective effect of cerebral ischemia-reperfusion injury, not easily passing through the blood-brain barrier, affecting the treatment effect, etc., so as to improve cerebral ischemia and reperfusion. Perfusion injury, easy to penetrate the blood-brain barrier, simple process effect

Pending Publication Date: 2021-11-30
BINZHOU MEDICAL COLLEGE
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Problems solved by technology

However, the existence of the polar group carboxyl group and polyhydroxyl group in the Danshensu molecule causes it to have greater polarity and is not easy to pass through the blood-brain barrier, which affects the therapeutic effect. Acidosis” phenomenon, these problems limit the protective effect of the drug on cerebral ischemia-reperfusion injury

Method used

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  • Preparation of tanshinol ethyl ester, pharmaceutical composition containing tanshinol ethyl ester and application of pharmaceutical composition in preparation of medicine for treating ischemic stroke
  • Preparation of tanshinol ethyl ester, pharmaceutical composition containing tanshinol ethyl ester and application of pharmaceutical composition in preparation of medicine for treating ischemic stroke
  • Preparation of tanshinol ethyl ester, pharmaceutical composition containing tanshinol ethyl ester and application of pharmaceutical composition in preparation of medicine for treating ischemic stroke

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Embodiment 1

[0025] The preparation of embodiment 1. Danshensu ethyl ester

[0026] Danshensu 25g, absolute ethanol 250mL, sulfuric acid 2.5mL, anhydrous sodium sulfate 25g, mix well and react at 60°C for 24 hours; after the reaction, filter through filter paper, and dry the filtrate under reduced pressure at 60°C and 0.1MP , the residue was dissolved in 250 mL of ethyl acetate, washed with water 1 to 3 times, each time using 250 mL of water; the ethyl acetate phase was collected, and dried under reduced pressure at 60 ° C and 0.1 MP to obtain colorless oily ethyl danshensu. The yield is 98%, and the product purity is 99.92%.

Embodiment 2

[0027] Embodiment 2. The preparation of Danshensu ethyl ester

[0028] Danshensu 25g, absolute ethanol 500mL, sulfuric acid 5mL, anhydrous sodium sulfate 25g, mix well and react at 80°C for 8 hours; after the reaction, filter paper, and dry the filtrate under reduced pressure at 50°C and 0.05MP. The residue was dissolved in 500 mL of ethyl acetate, washed 1 to 3 times with 500 mL of water each time; the ethyl acetate phase was collected and dried under reduced pressure at 50°C and 0.05 MP to obtain colorless oily Danshensu ethyl ester, which The yield was 97%, and the product purity was 99.83%.

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Abstract

The invention belongs to the technical field of medicines and particularly relates to preparation of a tanshinol ethyl ester and application of the tanshinol ethyl ester in preparation of a medicine for treating ischemic stroke. The preparation method of the tanshinol ethyl ester, provided by the invention, is high in yield and good in purity; compared with tanshinol, the tanshinol ethyl ester has higher fat solubility, more easily penetrates through a blood-brain barrier, and is short in time of reaching a drug peak value and high in drug peak value concentration; and a toxicity test shows that a LD50 value of the tanshinol ethyl ester is higher than that of the tanshinol. Due to the characteristics of effectiveness and safety, the tanshinol ethyl ester is suitable for preparing the medicine for treating the ischemic stroke.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to the preparation of danshensu ethyl ester, a pharmaceutical composition containing danshensu ethyl ester and its application in the preparation of medicines for treating ischemic stroke. Background technique [0002] Stroke, also known as stroke or cerebrovascular accident, is a group of acute cerebrovascular diseases with sudden onset and common features of focal neurological deficit. In the International Classification of Diseases (ICD) compiled by the World Health Organization (WHO), cerebrovascular diseases are now listed as neurological diseases in more detailed clinical medical institutions, and are the most common diseases. Neurological diseases are characterized by high morbidity, disability, mortality and recurrence. This disease is more common in the elderly, and it is the three major causes of death of the elderly together with myocardial infarction and can...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/216A61P9/10C07C67/08C07C69/732
CPCA61K31/216A61P9/10C07C67/08C07C69/732
Inventor 曲桂武
Owner BINZHOU MEDICAL COLLEGE
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