CN103877014A

CN103877014A - Mangiferin oral solution and preparation method thereof

Info

Publication number: CN103877014A
Application number: CN201410113534.5A
Authority: CN
Inventors: 邓家刚; 黄慧学; 杨柯; 梁秋云
Original assignee: Individual
Current assignee: Individual
Priority date: 2014-03-26
Filing date: 2014-03-26
Publication date: 2014-06-25

Abstract

The invention provides a mangiferin oral solution and a preparation method thereof. The preparation method comprises the following steps: mixing mangiferin, polyethylene glycol 400 and water in a mass-volume ratio of 0.5g:(6-8)ml:(2-4)ml, heating and dissolving at 60-100 DEG C; adding glycerin to modify taste, wherein the mass-volume ratio of the glycerin to mangiferin is 0.5g:1ml. According to the mangiferin oral solution, the content of mangiferin is high, the dissolubility of the mangiferin is over 4 percent, and the dissolution is stable, so that the oral solution can be absorbed by a human body in a direct drinking manner by serving as an oral medicinal solution or drink, and the utilization of mangiferin is greatly improved; the preparation of the mangiferin oral solution is wide in raw material sources and simple in preparation method, and is suitable for large-scale industrial production.

Description

A kind of chimonin oral liquid and preparation method thereof

Technical field

The invention belongs to medicinal preparation for oral administration field, relate in particular to a kind of chimonin oral liquid and preparation method thereof.

Background technology

Chimonin (Mangiferin) is the main active of Anacardiaceae plant Fructus Mangifera Indicae (Mangifera indica L.) leaf, has another name called mangiferin, and Chinonin is the natural polyphenol compounds extracting from the liliaceous plant Rhizoma Anemarrhenae, molecular formula C ₁₉h ₁₈o ₁₁, molecular weight 422, its structural formula is as shown in the formula shown in 1:

Formula 1 chimonin chemical structural formula

Folium mangiferae is Guangxi province conventional crude drugs, records in " Guangxi medical material standard " nineteen ninety version, has many-sided physiologically active and pharmacological action.Chimonin has cough-relieving, eliminates the phlegm, and relievings asthma and antiinflammatory, immunity, hepatic cholagogic, antiviral, antitumor, the effect such as antibacterial.And that Folium mangiferae has distributional region is wide, herb resource is abundant, and raw material is easy to get, cheap, and even the four seasons such as can adopt at the advantage, and the content of its main component chimonin reaches 1.92%, so be one of Hot events of utilizing of tcm development.But due to the water solublity extreme difference (0.10mg/mL, 25 ℃) of chimonin, be difficult to make the stable medicinal liquid of suitable concn, limited its application clinically.Although there is the method that increases similarly chimonin dissolubility, as: chimonin-beta-schardinger dextrin-inclusion, chimonin-sodium salt, technology path complexity, operation is loaded down with trivial details, and key technology is difficult for grasping.

Summary of the invention

The object of the present invention is to provide a kind of chimonin oral liquid and preparation method thereof, be intended to solve by selecting suitable solvent and proportioning to make suitable oral liquid the problem of the poor solubility of chimonin.

The present invention is achieved in that and the invention provides a kind of chimonin oral liquid, comprises that by mass volume ratio be 0.5g: (6～8) ml: chimonin, PEG400, water and the glycerol of (2～4) ml: 1ml.

Preferably, the amount volume ratio of described chimonin, PEG400, water and glycerol is 0.5g: 8ml: 4ml: 1ml.

The present invention further provides the preparation method of above-mentioned chimonin oral liquid, comprise the following steps: be 0.5g by chimonin, PEG400 and water by mass volume ratio: (6～8) ml: 60～100 ℃ of heating for dissolving after (2～4) ml mixes, then the glycerol taste masking that to add with described chimonin mass volume ratio be 0.5g: 1ml.

Compare the shortcoming and defect with prior art, the present invention has following beneficial effect: in chimonin oral liquid of the present invention, chimonin content is very high, dissolution rate can reach more than 4%, and solution-stabilized, can be used as oral liquid medicine or beverage by the mode of directly drinking by human body is absorbed, improved significantly the utilization rate of chimonin; The raw materials wide material sources of chimonin oral liquid of the present invention, preparation method is simple, is suitable for large-scale industrialized production.

The specific embodiment

In order to make object of the present invention, technical scheme and advantage clearer, below in conjunction with embodiment, the present invention is further elaborated.Should be appreciated that specific embodiment described herein, only in order to explain the present invention, is not intended to limit the present invention.

Embodiment 1

(1) 0.5g chimonin, 8ml PEG400 and 2ml water are mixed to rear 100 ℃ of heating for dissolving, mixed solution is evenly clarified;

(2) toward the glycerol taste masking that adds again 1ml in described mixed solution, obtain chimonin oral liquid 1.

Embodiment 2

(1) 0.5g chimonin, 6ml PEG400 and 4ml water are mixed to rear 100 ℃ of heating for dissolving, mixed solution is evenly clarified;

(2) toward the glycerol taste masking that adds again 1ml in described mixed solution, obtain chimonin oral liquid 2.

Comparative example 1

0.5g chimonin, 4ml PEG400 and 6ml water are mixed to rear 100 ℃ of heating for dissolving, mixed solution muddiness, layering.

Effect embodiment assay

Get chimonin oral liquid 1 prepared by embodiment 1 and under HPLC chromatographic condition, carry out assay, detailed process is as follows:

(1) chromatographic condition: chromatographic column is Diamonsil C ₁₈(4.6mm × 250mm), mobile phase is acetonitrile-0.1% glacial acetic acid (15: 85), flow velocity 1ml/min, detection wavelength is 258nm, 30 ℃ of column temperatures, sample size is 10 μ l, chimonin theoretical cam curve should be not less than 3500 under these conditions.

Chimonin is a kind of carbon glycoside of tetrahydroxy pyrrone, belong to two benzene pyrrones compounds, dissolve in hot dilute methanol, its ultraviolet absorption peak is 240nm and 258nm (methanol is solvent), according to measurement result, take maximum absorption band 258nm as detecting wavelength, in test sample, disturb without other impurity, therefore detection wavelength is 258nm, utilize external standard method to calculate content.Analyze test sample, reference substance by this chromatographic condition, chimonin retention time is approximately 9min.

(2) content assaying method

The preparation of A, reference substance solution

Get chimonin reference substance appropriate, accurately weighed, put in 50ml volumetric flask, add 40% methanol, heating in water bath is cooled to room temperature after making to dissolve, and adds 40% methanol constant volume to scale, join every 1ml containing the dense reference substance storing solution of 200 μ g.

The preparation of B, need testing solution

Take chimonin oral liquid 0.5ml, put in 100ml volumetric flask, add 40% methanol appropriate, heating in water bath make its dissolve after, be cooled to room temperature, by 40% methanol constant volume to scale.Absorption sample solution is appropriate, and 0.22 μ m filtering with microporous membrane, to obtain final product.

C, linear relationship are investigated

Precision takes chimonin reference substance storing solution (concentration is 200 μ g/ml) 1.0,2.0,4.0,6.0,10.0,20.0 μ l and injects high performance liquid chromatograph, measures peak area, parallel 2 times by above-mentioned chromatographic condition.With peak area Y, to chimonin sample size X, (μ g) returns, and regression equation is Y=5 × 10 ⁶x-77232 (R ²=1), result is as shown in table 1 below:

Table 1 standard curve determination result

As can be seen from Table 1, chimonin concentration has good linear relationship with peak area within the scope of 0.20～2.60 μ g.

D, sample size are measured

The accurate need testing solution 10 μ l that draw inject HPLC chromatograph, record peak area, and substitution regression equation is asked content.Result is as shown in table 2 below:

Table 2 sample size is measured measurement result (n=3)

As can be seen from Table 2, the content of trying to achieve chimonin in chimonin oral liquid 1 by calculating is 4.04%, and chimonin dissolubility is promoted to 0.4g/mL from 0.10mg/mL, and dissolubility has improved 4 × 10 ³times, and preparation process is easy, easy operating.

The foregoing is only preferred embodiment of the present invention, not in order to limit the present invention, all any modifications of doing within the spirit and principles in the present invention, be equal to and replace and improvement etc., within all should being included in protection scope of the present invention.

Claims

1. a chimonin oral liquid, is characterized in that, comprises that by mass volume ratio be 0.5g: (6～8) ml: chimonin, PEG400, water and the glycerol of (2～4) ml: 1ml.

2. chimonin oral liquid as claimed in claim 1, is characterized in that, the amount volume ratio of described chimonin, PEG400, water and glycerol is 0.5g: 8ml: 4ml: 1ml.

3. the preparation method of chimonin oral liquid claimed in claim 1, it is characterized in that, comprise the following steps: be 0.5g by chimonin, PEG400 and water by mass volume ratio: (6～8) ml: 60～100 ℃ of heating for dissolving after (2～4) ml mixes, then the glycerol taste masking that to add with described chimonin mass volume ratio be 0.5g: 1ml.