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Application and preparation of bitter orange extract meranzin hydrate for preparing enterocinetic kinetic medicaments

A hesperidone and bowel-promoting technology, which can be used in drug combinations, active ingredients of heterocyclic compounds, digestive system, etc., can solve problems such as no obvious curative effect

Inactive Publication Date: 2012-03-14
CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The Chinese Pharmacopoeia 2005 edition records that the pharmacological active ingredients of Citrus aurantium are hesperidin and naringin, but there are studies (see Guan Fulan et al. Effects of tangerine peel and hesperidin on isolated bowel movements. Shizhen Guoyi Guoyao, 2002, 13(2)) found that the two ingredients, hesperidin and naringin, had no significant effect on the intestinal motility test

Method used

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  • Application and preparation of bitter orange extract meranzin hydrate for preparing enterocinetic kinetic medicaments
  • Application and preparation of bitter orange extract meranzin hydrate for preparing enterocinetic kinetic medicaments
  • Application and preparation of bitter orange extract meranzin hydrate for preparing enterocinetic kinetic medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Example 1: Discovery of hydrated hesperidone as an active ingredient of Fructus Aurantii

[0017] Blank serum: healthy human serum, n=6;

[0018] Drug-containing serum: serum of healthy people after oral administration of Jiawei Xiaoyao Powder for 30 minutes, n=6.

[0019] Jiawei Xiaoyao San: Gardenia (1g), Danpi (1g), Bupleurum (1.7g); Poria (1.7g), Atractylodes macrocephala (1g), Angelica (1.7g); Magnolia officinalis (2g), Citrus aurantium (2g ), Radix Paeoniae Alba (1.7g), ginger (4g); kudzu root (2.7g), jujube (1g), mint (1g), licorice (1g). Simmer for 40 minutes × 2 times.

[0020] Sample processing: Take 1ml of blank serum, bathe in 100°C water for 10 minutes, smash it with a homogenizer, centrifuge at 8500 rpm for 20 minutes, take the supernatant and blow it with nitrogen flow, and set the volume to 150μl, to be tested; the drug-containing serum is processed The method is the same.

[0021] The blank serum, drug-containing serum and modified Xiaoyao powder pr...

Embodiment 2

[0023] Example 2: Separation and extraction of hydrated hesperidone from the crude drug Fructus Aurantii

[0024] Use silica gel column chromatography to separate and purify the unknown component X from Fructus Fructus Fructus Aurantii. The specific process is as follows: Weigh 2 g of Fructus Fructus Fructus, reflux and extract with 20 ml of ethyl acetate for 1.5 h, extract three times, concentrate under reduced pressure, add 2 ml of acetone to dissolve, and On a silica gel column, first elute with 100ml of petroleum ether, then with petroleum ether: acetone 20:1, 10:1, 100ml each of acetone, combine the eluents as eluent 1, concentrate under reduced pressure, add 2ml of methanol The solution was centrifuged at 15000r / min for 15min. Inject the supernatant. The purity was detected by analytical HPLC, and the purity calculated by the peak area normalization method was >98%. After 5 preparations by preparative HPLC, working under the condition of volume overload, the injection ...

Embodiment 3

[0026] Embodiment 3: Pharmacodynamic experiment of hydrated hesperidone

[0027] 180~220g SD rats (both male and female) were randomly divided into 6 groups, 15 in each group, respectively A (distilled water) group, B (hydrated hesperidone) group, C (hesperidin) group, D (pomelo Perididin) group, E (hesperidin hydrate + atropine) group, F (hesperidin + atropine) group, G (naringin + atropine) group.

[0028] Each group was fed with 0.3 mL / d of medicinal solution for 3 consecutive days, once a day. Group A was fed with 199% distilled water; B and E groups were fed with hydrated hesperidin (20mg / ml), C and F groups were fed with hesperidin (20mg / ml), D and G groups were fed with naringin ( 20mg / ml). After fasting for 12 hours on the 4th day, 0.3 mL of each of the above drugs was given by gavage, and 0.0003 g / kg morphine hydrochloride was intraperitoneally injected into groups E, F and G at the same time. After 20 minutes, 0.4 mL of dextran blue 2000 aqueous solution was fed. ...

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Abstract

The invention discloses application and a preparation of bitter orange extract meranzin hydrate for preparing enterocinetic kinetic medicaments. A method for preparing the meranzin hydrate comprises the following steps of: pulverizing bitter orange, and performing reflux by using ethyl acetate to extract filter liquor; concentrating the filter liquor under reduced pressure, adding acetone for dissolving, putting the mixture on a silicagel column, eluting by using petroleum ether and the acetone, merging eluent, and concentrating under the reduced pressure; and adding alcohol for dissolving and centrifuging, and freeze-drying supernatant to obtain the meranzin hydrate. In the application, the meranzin hydrate is separated and extracted from the bitter orange, and experiments prove that theenterocinetic kinetic effect of the bitter orange extract meranzin hydrate far exceeds that of hesperidin and naringin, so the prejudice that people consider the hesperidin and the naringin as the active ingredients of the traditional Chinese medicine bitter orange with the enterocinetic kinetic pharmacological effect all the time is corrected.

Description

technical field [0001] The invention relates to a traditional Chinese medicine Fructus aurantium extract, in particular to hydrated hesperidone extracted from Fructus aurantium and the application of hydrated hesperidone. Background technique [0002] Existing studies have shown that hydrated hesperidone, chemical name: 7-methoxy-8-(2',3'-dihydroxy-3'-methylbutyl)-coumarin, English name: merazin hydrate, the molecular weight is 278, and the chemical formula is: [0003] [0004] It is mainly found in plants such as Angelica Plaquedenta, Rutaceae Cnidium, Murata, and Murata microphylla, and it has not been reported to exist in Citrus aurantium (Citrus aurantium). [0005] The traditional Chinese medicine Citrus aurantium, Latin name Fructus Aurantii, alias only shell, river orange, business shell, fried orange shell, is the dry immature fruit of Rutaceae plant lime (Citrus aurantium L.) and its cultivars. It is known that Fructus Fructus Aurantii has the effect of promot...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/37A61P1/00A61P1/06
Inventor 黄熙任平秦锋
Owner CENT SOUTH UNIV
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