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Method for refining cucurbitacin raw material and preparation thereof

A refining method and cucurbitacin technology, applied in the field of medicine, can solve the problems of no active carbon, no visible, etc., and achieve the effects of improving curative effect, ensuring curative effect and reducing toxicity

Inactive Publication Date: 2008-03-05
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The traditional extraction process of cucurbitacin is only drying after extraction, and the obtained extract often shows a certain color. In the existing literature, there is no process of using activated carbon treatment, and there are no reports of using refined raw materials to prepare various preparations.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0032] Embodiment 2 investigates the impact of alcohol content on yield in the final solution

[0033] Three portions of 2 grams of commercially available cucurbitacin raw materials were weighed and dissolved in 60, 80, and 100 ml of ethanol respectively to obtain a drug solution. According to the active carbon dosage of 0.1% (W / V), the active carbon is added into the drug alcohol solution, after stirring at room temperature for 20 minutes, the carbon is removed by filtration to obtain the solution. Add 200ml of distilled water respectively, stir and mix well, seal and place in the refrigerator (4 - 8°C). After standing overnight, a large amount of white precipitate was obtained, which was collected by filtration. Observe appearance and weigh, calculate yield. The results are shown in Table 2.

[0034] Table 2. Effect of alcohol content on yield in final solution

[0035] drug weight

[0036] It can be seen that the greater the amount of alcohol added, the lower...

Embodiment 3

[0037] Embodiment 3 investigates the impact of standing temperature on yield

[0038] Weigh 3 portions of 1 gram of commercially available cucurbitacin, add 30ml of ethanol, and store at 40°C - Dissolve in a water bath at 50°C, add 0.1% activated carbon, stir at 40°C for 20 minutes, add 100ml of water, - 8℃), -20℃ and room temperature (20 - 25°C) overnight, and investigate the precipitation at different temperatures, the results are shown in Table 3.

[0039] Table 3. Yields of drugs at different temperatures

[0040] -20℃

[0041] It can be seen that the yield of the drug obtained at -20°C is the highest, but the difference among the three is not very large. Since the operation at -20°C is inconvenient, time-consuming, and costly, considering comprehensive considerations, you can choose 6°C or room temperature.

Embodiment 4

[0042] Embodiment 4 water-adding speed is on the influence of gained crystal dissolution speed

[0043] Take three parts of 5.0 g of commercially available cucurbitacin raw materials, dissolve them (40-50 ° C water bath) in 150 ml of 95% medicinal ethanol, add 0.3 g of activated carbon (0.2%), stir at room temperature for 20 minutes, and filter respectively to obtain the filtrate three servings. Slowly add 500ml of water along the wall according to the speed of pouring (about 5000ml / min), about 1000ml / min, and about 500ml / min, respectively, opalescence appears, and then precipitation appears, seal it, and leave it at room temperature overnight. A large amount of white precipitate was formed, which was filtered by suction to obtain a white solid. After vacuum drying at 50°C, the obtained white solids were about 4.3g, 4.2g, and 4.3g, respectively. The content of cucurbitacin B in the refined cucurbitacin was determined to be around 62 μg / mg by HPLC, which was not different fro...

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Abstract

The present invention belongs to the field of medicine technology, and provides cucurbitacin refining process and preparation. The cucurbitacin refining process includes the following steps: 1. dissolving marketed cucurbitacin in C1-C4 alcohol-water dissolved ketone to obtain solution A containing cucurbitacin in 0.1-10 g each 100ml; 2. adding active carbon in0.01-10 g for each 100 ml, stirring for 1-60 min and filtering out carbon to obtain solution B; 3. adding water into solution B to reach alcohol / water volume ratio of 1 to 1-10, and stirring until the solution becomes turbid; 4. letting stand for over night; and 5. filtering, collecting precipitate and drying. The refining process can lower the toxicity of cucurbitacin product, has no altering on cucurbitacin B content and is suitable for industrial production. The cucurbitacin product may be prepared into different preparations for treating tumors, increasing peripheral blood leukocytes and treating hepatitis.

Description

Technical field: [0001] The invention belongs to the technical field of medicine, and relates to a method for refining a known substance, cucurbitacins, and various preparations prepared from refined raw materials obtained by the method. Background technique: [0002] Cucurbitacins belong to a class of tetracyclic triterpenoids with a 19-methyl group appearing at the C-9 position. They are mainly distributed in Cucurbitaceae plants. It is also found in higher plants such as wood family and some large fungi. Qiu Minghua, a researcher at the Kunming Institute of Botany, Chinese Academy of Sciences, led scientific and technical personnel to study 229 almost all cucurbitacin compounds on the basis of the discovery of a series of new types of cucurbitacin compounds, and proposed a new structural classification model, which was reconstructed from the previous five structural types. Divided into 12 categories, it has been recognized by the international academic community. At pre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07J9/00A61K31/575A61P35/00A61P1/16
Inventor 邓意辉石莉卢懿董晓辉
Owner SHENYANG PHARMA UNIVERSITY
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