Preparation of low-glycosylation prunin and application in cough relieving and sputum reducing medicine

A low-glycosylation and glycosylation technology, applied in the preparation of sugar derivatives, sugar derivatives, sugar derivatives, etc., can solve the problem of low solubility and fat solubility, limited application of pruning, and low bioavailability of pruning. and other problems, to achieve the effects of stable quality, good cough and phlegm relief, and rapid curative effect.

Inactive Publication Date: 2018-02-23
MEIZHOU GOLDEN POMELO HEALTH TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, Pruning has extremely low solubility in water and fat solubility (<10mg / L), which greatly limits the application of Pruning and makes the bioavailability of Pruning low.

Method used

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  • Preparation of low-glycosylation prunin and application in cough relieving and sputum reducing medicine
  • Preparation of low-glycosylation prunin and application in cough relieving and sputum reducing medicine
  • Preparation of low-glycosylation prunin and application in cough relieving and sputum reducing medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0050] Embodiment 1: Preparation of low glycosylation pronin

[0051] (1) Preparation of naringin ultrafiltration solution

[0052] Naringin with a mass fraction of 50-98% is dissolved in sodium hydroxide or potassium hydroxide solution with a molar concentration of 0.1-1mol / L, and treated at 30-40°C for 30 minutes to form a naringin solution. Pump the prepared naringin solution into a polyethersulfone membrane ultrafilter with a molecular weight cut-off of 1000-2000Da, control the ultrafiltration pressure to 0.1-0.3MPa, and perform ultrafiltration until the volume of the ultrafiltration retentate is reduced to that of orange-red Stop when the volume of the flavonoid compound solution in the solution is 1 / 10 to 1 / 20, collect the ultrafiltration filtrate and the ultrafiltration retentate respectively, and the collected ultrafiltration filtrate is the naringin ultrafiltration solution.

[0053] (2) Preparation of highly glycosylated pronin solution

[0054] After step (1) is c...

Embodiment 2

[0061] Example 2: Purity Analysis of Low Glycosylation Pronin

[0062] 1. Liquid phase analysis conditions: chromatographic column (type C 18 250×4.6mm); flow rate: 1.0ml / min; mobile phase: 0.5% acetic acid solution: acetonitrile=7:3; detection wavelength: 346nm; injection volume: 10 μl.

[0063] 2, the preparation of mobile phase: prepare the acetic acid solution 1000ml of 0.5% with ultrapure water and glacial acetic acid (reagent pure), filter to no visible impurity with suction filter with liquid phase, ultrasonic half an hour debubbles; Get 500ml acetonitrile (analysis Pure) was filtered with a suction filter in the liquid phase until no impurities were visible to the naked eye, and the bubbles were removed by ultrasonication for half an hour.

[0064] 3. Preparation and analysis of sample solution with known concentration: take 5.0 mg of sample and dissolve in 10 ml of 50% DMSO solution respectively, shake to dissolve completely. Use a syringe and a syringe filter to f...

Embodiment 3

[0067] Example 3: Antitussive pharmacological experiment of low-glycosylated Prunin drug

[0068] 1. Experimental animals: NIH mice, male, weighing 18.0-22.0 g, normal grade standard, 90 in total. Weigh the animals first, number them, and select a total of 75 healthy mice with a body weight of 18.5-21.5 g. Sorted according to body weight, divided into five groups by random grouping method, 15 in each group. A negative control group, a positive control group, a low-dose group of low-glycosylated Prunin drug samples, a medium-dose group of low-glycosylated Prunin drug samples, and a high-dose group of low-glycosylated Prunin drug samples were set up.

[0069] 2. Sample source and processing

[0070] 1) Blank control group: physiological saline, NaCl content 0.9%.

[0071] 2) Positive control group: 2 tablets of methorphan were dissolved in 20 mg of normal saline to obtain a positive control methorphan solution, the concentration of methorphan was 1.5 mg / ml.

[0072] 3) Low-d...

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Abstract

The invention relates to preparation of low-glycosylation prunin and application in a cough relieving and sputum reducing medicine. Low-glycosylation prunin is prepared by conducting two times of bioenzyme catalysis on raw materials such as naringin. Through the two times of bioenzyme catalysis, the problem of poor water solubility and lipid solubility of prunin is solved, the solubility of pruninis increased by 75 folds or above through low glycosylation, the bioavailability is increased obviously, and prunin can be applied widely. Low-glycosylation prunin has a better cough relieving and sputum reducing effect and has an obvious efficacy on all kinds of cough and asthma caused by acute / chronic bronchitis or cold, there is no toxic and side effect, the efficacy of low-glycosylation prunin is more obvious than that of a traditional cough relieving medicine-(Nianci) Chuanbei Pipa Gao, and low-glycosylation prunin is an ideal cough relieving and sputum reducing medicine and has a wide market prospect. The chemical structural formula of low-glycosylation prunin is shown in the description.

Description

technical field [0001] The invention relates to the preparation of low-glycosylated pronin and its application in cough-relieving and phlegm-reducing medicines technical background [0002] Cough, sputum, and wheezing are common symptoms of respiratory diseases. They are especially common in daily life caused by acute and chronic bronchitis, colds, etc. Clinically, it is characterized by cough, sputum, wheezing and recurrent attacks. It is caused by infection or Acute and chronic non-specific inflammation of the trachea, bronchial mucosa and surrounding tissues caused by non-infectious factors. It belongs to the category of cough, phlegm retention and asthma in traditional Chinese medicine. It is a common disease and frequently-occurring disease. Especially middle-aged and elderly people are prone to bronchitis symptoms such as cough and expectoration due to the influence of environmental factors and living habits. During the onset period, they are not well treated and cont...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H17/07C07H1/08A61K31/7048A61P11/14A61P11/06A61P11/10C12P19/18
CPCC07H1/08C07H17/07C12P19/18
Inventor 周金林卢宇靖郭晓路黄宝华林丽薇李慧灵邓诚
Owner MEIZHOU GOLDEN POMELO HEALTH TECH CO LTD
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