Method for preparing limonin, composition and application thereof

A technology of limonin and composition, which is applied in the field of herbal medicine, can solve the problems of high industrial production cost, low extraction rate, hidden dangers of drug safety, etc., and achieve the effects of saving production time, high extraction efficiency, and improving safety

Inactive Publication Date: 2010-07-21
XIAN XINTONG PHARM RES CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] At present, the preparation method of limonin has been reported in the existing literature, but either the solvent is wasted in the preparation and the extraction rate is low, resulting in high production cost; or the prepared composition (product) has low purity and contains more impurities. Direct use brings great hidden dangers to drug safety, and it is difficult to pass approval for actual industrialization, and further purification is equivalent to increasing the cost of preparation
[0006] Specifically, Chinese Patent Application No. 00106285 discloses a method for extracting limonin from Rutaceae fruits, but the purity of limonin prepared by this method is very low (less than 90%);
[0007] Chinese patent application No. 00130622 discloses a process for extracting medicinal active substances from citrus seeds. However, the purity of limonin prepared by this process is very low. We have found that to obtain high-purity products, it is necessary to pass through silica gel chromatography. Recrystallization steps (much more than 2 times) are frequently used after the column, the extraction rate is low and the cost is high;
[0009] Chinese patent application No. 03118175 discloses a method for simultaneously extracting eight kinds of products such as pectin and naringin from pomelo, but this method will lose a large amount of lim...

Method used

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  • Method for preparing limonin, composition and application thereof
  • Method for preparing limonin, composition and application thereof
  • Method for preparing limonin, composition and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] The preparation method and safety detection of the high-purity limonin of embodiment 1

[0048] Get 10kg of pomelo core after drying at 50°C, pulverize, and pass through a 12-mesh sieve. Put it in an ultrasonic tank, adjust the frequency at 20KHZ, add 50L of acetic acid solution with a pH value of 3.2 and a concentration of 3% (v / v), start the ultrasonic wave, heat to 50°C, and extract by ultrasonic for 50 minutes; filter, add 40L of pH value to the filter residue The concentration of 3.2 is 3% (v / v) acetic acid solution, 50°C for ultrasonic extraction for 50min, cooled to room temperature, and filtered. The two filtrates were combined to obtain an extract.

[0049] Then, the extract was concentrated under reduced pressure to 1.0 g / ml (crude drug / feed liquid). In the chromatographic column of D101 macroporous resin (? 150×1500) (Jiangyin Jinque Chromatography Equipment Co., Ltd.), 40L of water was used for elution, and the flow rate was 100ml / min, and the eluent was d...

Embodiment 2

[0066] Example 2 Limonin inhibits the experiment of rat colon cancer induced by azoxymethane (AOM)

[0067] 2.1 Materials and methods

[0068] 2.1.1 Materials

[0069] Experimental animals 60-85g male weaned Wistar rats (certificate number: Yidongzi No. 2009028) were provided by the Experimental Animal Center of Xi'an Jiaotong University School of Medicine. Quality Certificate Number: Shaanxi Medical Dynamic Character: No. 09-125.

[0070] 2.1.2 Main Reagent Limonin (namely the colorless needle-like crystal limonin product obtained in Example 1), azoxymethane (AOM) (Sigma Company).

[0071] 2.2 Method

[0072] 2.2.1 Animal grouping and treatment 140 male Wistar rats (5 weeks old), weighing 60-80 g. The animal room was raised under the conditions of (23±2)°C temperature, (50±10)% relative humidity, normal light (12-hour day / night cycle), and fed with conventional feed. After adapting to the animal room for 1 week, the rats were randomly divided into 5 groups (AOM group, AO...

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Abstract

The invention provides a method for preparing a composition comprising high-purity limonin and a medicinal composition which is prepared by the method, has high safety and comprises the high-purity limonin. In the preparation method, the limonin of which the purity is over 98 percent can be obtained under the condition of recrystallization and purification for two times; and the impurities in the limonin do not damage the safety. Moreover, the invention also provides application of the medicinal composition in preparing a medicament for preventing and/or treating the colon cancer or the rectal cancer.

Description

technical field [0001] The invention belongs to the field of herbal medicines (Chinese herbal medicines). Specifically, the invention relates to a method for preparing high-purity limonin and a high-safety pharmaceutical composition containing high-purity limonin. In addition, the present invention also relates to the application of the above pharmaceutical composition in the preparation of medicaments for preventing and / or treating colon cancer or rectal cancer. Background technique [0002] Limomin, also known as evocarptonin, phrysinide, phellodactone, mainly exists in Rutaceae (Rutaceae) and Meliaceae (Meliaceae) plants, such as Citrus aurantium (navel orange, citrus, Among orange) pomelo, etc., the content in the core (seed) is higher, and the content in the peel is less (about 1 / 10,000 to 5 / 100,000). The chemical structure of limonoid is shown below: [0003] [0004] Limonin has anti-cancer, analgesic, anti-inflammatory, lowering cholesterol, inhibiting HIV-1 vir...

Claims

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Application Information

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IPC IPC(8): C07J73/00A61K31/585A61P35/00
Inventor 张登科
Owner XIAN XINTONG PHARM RES CO LTD
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