A flos sophorae instant powder composition, a preparation method, a product and an application

By utilizing a method for preparing a Sophora japonica flower instant powder composition, and combining Sophora japonica flower, β-cyclodextrin, phospholipids, and polysaccharide coating agents, the problems of solubility and stability of the active ingredients in Sophora japonica flower instant powder were solved, achieving high bioavailability and whitening effect.

CN120392559BActive Publication Date: 2025-11-04XIAN NUOZHONGKANGJIAN BIOTECHNOLOGY CO LTD
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Patent Information

Application Number
CN202510815038.2
Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
Filing Date
2025-06-18
Publication Date
2025-11-04
Estimated Expiration
2045-06-18

AI Technical Summary

Technical Problem

Existing technologies have failed to provide highly active, highly bioavailable, and highly stable Sophora japonica flower instant powder, and have failed to fully utilize the synergistic effect of Sophora japonica flower active ingredients.

Method used

A composition of Sophora japonica flower instant powder, consisting of Sophora japonica flower, β-cyclodextrin, phospholipids, and polysaccharide coating agents (such as chitosan, sodium carboxymethyl cellulose, gelatin, sodium alginate, or gum arabic), is used to improve the solubility and stability of quercetin and rutin through ultrasonic extraction, acid hydrolysis, and polymer liposome technology.

Benefits of technology

It significantly improves the solubility, bioavailability, and solution stability of quercetin and rutin, and has a significant whitening effect.

✦ Generated by Eureka AI based on patent content.

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Abstract

The application provides a flos sophorae instant powder composition, a preparation method, a product and application, and belongs to the technical field of instant powder. The flos sophorae instant powder composition is composed of the following components: flos sophorae, beta-cyclodextrin, phospholipid and a polysaccharide coating agent, wherein the polysaccharide coating agent is at least one selected from chitosan, sodium carboxymethyl cellulose, gelatin, sodium alginate and gum arabic. The flos sophorae instant powder composition can be used to prepare a flos sophorae instant powder, liposomes are used to coat and effectively solubilize rutin and quercetin, and then the inhibition effect of flos sophorae extract on tyrosinase activity, the solution stability and the whitening effect are improved.
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Description

TECHNICAL FIELD

[0001] The present application belongs to the technical field of instant powder, and relates to a Sophora japonica L. instant powder composition, a preparation method, a product and application. BACKGROUND

[0002] Sophora japonica L. is the flower of Sophora japonica L. in the Leguminosae family, and is a traditional medicinal and edible resource. According to the Chinese Pharmacopoeia, Sophora japonica L. is slightly cold in nature and bitter in taste, and is related to the liver and large intestine channels, has the effects of cooling blood to stop bleeding and clearing liver to purge fire, and is widely used in the auxiliary treatment of hematochezia, hemorrhoids and hypertension. Sophora japonica L. is rich in flavonoids, among which rutin and quercetin are important active ingredients. The content of rutin in Sophora japonica L. is as high as 8%-20% of the dry weight of the flower. Rutin has the function of inhibiting the activity of tyrosinase by chelating copper ions (Cu 2+ ) in the active center of tyrosinase and competitively binding to the substrate site. The content of quercetin in Sophora japonica L. can reach 0.2%-2% of the dry weight. Quercetin can bind to tyrosinase through hydrophobic interaction, induce conformational changes and spontaneous fluorescence quenching, and interfere with the melanin synthesis pathway.

[0003] Chinese invention patent CN118986823A provides an anti-aging liposome composition and its application. The composition comprises Sophora japonica L. extract 0.1-1 parts, Pueraria lobata extract 1-4 parts, aminobutyric acid 2-6 parts, polyol 50-60 parts, emulsifier 2-6 parts, co-emulsifier 9-18 parts, cholesterol 0.2-1 part, water 10-35 parts, and the co-emulsifier includes co-emulsifier I polysorbate-20 and co-emulsifier II PPG-6 decyltetradecyl alcohol polyether-30, with a mass ratio of 1-4:8-14. During preparation, the Sophora japonica L. extract, Pueraria lobata extract, polyol, cholesterol, emulsifier and co-emulsifier I are uniformly mixed and homogenized, and then water and aminobutyric acid are added. Then, the co-emulsifier II is added after cooling. This technology innovatively combines Sophora japonica L. extract, Pueraria lobata extract and aminobutyric acid in a liposome system, solves the solubility and absorption rate problems of the main active ingredients in Sophora japonica L. extract and Pueraria lobata extract, and achieves a multi-channel anti-aging effect.

[0004] The Chinese invention patent CN117598958A provides a sophora japonica flower fermentation composition, a cosmetic with anti-wrinkle effect and a preparation method and application thereof. The preparation method comprises the following steps: taking sophora japonica flower bud powder, adding the sophora japonica flower bud powder into water, mixing and sterilizing to obtain a fermentation substrate; inoculating the fermentation substrate with plant lactobacillus, performing fermentation culture treatment, separating and sterilizing the fermentation substrate after the fermentation culture to obtain sophora japonica flower bud fermentation liquor, and performing drying treatment on the sophora japonica flower bud fermentation liquor to prepare the sophora japonica flower fermentation composition. The sophora japonica flower fermentation composition of the technology is fermented by using sophora japonica flower bud and compound probiotic lactobacillus, the main components are directionally converted into key substances with the effect of selectively eliminating harmful aging cells, and the sophora japonica flower fermentation composition has a significant effect on anti-aging and anti-wrinkle when applied to cosmetics.

[0005] At present, the sophora japonica extract is mainly used for the separation and purification of single components (such as rutin or quercetin), and the effect is single, and the synergistic effect of active components of sophora japonica cannot be fully utilized. The prior art has not provided an oral sophora japonica instant powder with high activity, high bioavailability and high stability. SUMMARY

[0006] Therefore, in view of the problems of the prior art, the purpose of the present application is to provide a preparation method, product and application of a sophora japonica instant powder.

[0007] To achieve the above-mentioned purpose, in one aspect, the present application provides a sophora japonica instant powder composition, which is composed of sophora japonica, beta-cyclodextrin, phospholipid and polysaccharide coating agent, and the polysaccharide coating agent is selected from at least one of chitosan, sodium carboxymethyl cellulose, gelatin, sodium alginate and gum arabic.

[0008] Preferably, the sophora japonica instant powder composition is composed of 100 parts of sophora japonica, 30-35 parts of phospholipid, 28-34 parts of beta-cyclodextrin and 3-7 parts of polysaccharide coating agent by weight; and the polysaccharide coating agent is composed of gum arabic and sodium carboxymethyl cellulose.

[0009] More preferably, the weight ratio of the gum arabic and sodium carboxymethyl cellulose is 1-9:1-9.

[0010] As an example of the present application, the sophora japonica instant powder composition is composed of the following ingredients by weight:

[0011] 100 parts of sophora japonica, 35 parts of phospholipid, 32 parts of beta-cyclodextrin, 1.5 parts of gum arabic and 1.5 parts of sodium carboxymethyl cellulose.

[0012] As an example of the present application, the sophora japonica instant powder composition is composed of the following ingredients by weight:

[0013] Sophora japonica 100 parts, phospholipid 35 parts, β-cyclodextrin 28 parts, gum arabic 3.5 parts and sodium carboxymethyl cellulose 3.5 parts.

[0014] As an example of the present application, the instant Sophora japonica powder composition consists of the following ingredients by weight parts:

[0015] Sophora japonica 100 parts, phospholipid 30 parts, β-cyclodextrin 34 parts, gum arabic 0.6 parts and sodium carboxymethyl cellulose 5.4 parts.

[0016] As an example of the present application, the instant Sophora japonica powder composition consists of the following ingredients by weight parts:

[0017] Sophora japonica 100 parts, phospholipid 30 parts, β-cyclodextrin 34 parts, gum arabic 5.4 parts and sodium carboxymethyl cellulose 0.6 parts.

[0018] In another aspect, the present application provides a method for preparing instant Sophora japonica powder using the above-mentioned instant Sophora japonica powder composition, comprising the following steps:

[0019] S1, mixing Sophora japonica with a solvent, ultrasonic extraction 1-3 times, taking the filtrate to obtain an ultrasonic extract;

[0020] S2, adjusting the pH of the ultrasonic extract obtained in step S1, high-pressure acid hydrolysis reaction to obtain an acid hydrolysis extract;

[0021] S3, mixing the acid hydrolysis extract obtained in step S2 with β-cyclodextrin and phospholipid, ultrasonic treatment, then mixing with a polysaccharide film forming agent, stirring, drying to obtain instant Sophora japonica powder.

[0022] Preferably, in step S1, the solvent is an ethanol aqueous solution, the ratio of Sophora japonica to solvent is 1:8-15, unit g:mL, the ultrasonic extraction temperature is 40-70℃, the ultrasonic extraction frequency is 20-35 kHz, the ultrasonic extraction power is 150-300 W, and the ultrasonic extraction time is 0.2-1 h.

[0023] More preferably, in step S1, the ethanol aqueous solution is an aqueous solution with an ethanol volume concentration of 60%-90%, the ratio of Sophora japonica to solvent is 1:10-15, unit g:mL, the ultrasonic extraction temperature is 50-70℃, the ultrasonic extraction power is 250-300 W, and the ultrasonic extraction time is 0.5-1 h.

[0024] Preferably, in step S2, the pH adjustment specifically involves adding hydrochloric acid to adjust the pH to 2-5; the high-pressure acid hydrolysis reaction pressure is 0.5-1.8 MPa, the high-pressure acid hydrolysis reaction temperature is 95-125℃, and the high-pressure acid hydrolysis reaction time is 10-30 min.

[0025] More preferably, in step S2, adjusting the pH specifically involves adding hydrochloric acid and adjusting the pH to 3.5-4; the pressure of the high-pressure acid hydrolysis reaction is 1.0-1.5 MPa, the temperature of the high-pressure acid hydrolysis reaction is 100-115°C, and the time of the high-pressure acid hydrolysis reaction is 15-20 min.

[0026] Preferably, in step S3, the power of the ultrasonic treatment is 80-120W, and the ultrasonic treatment time is 25-35min.

[0027] In another aspect, the present invention provides a Sophora japonica flower instant powder, which is prepared from the above-mentioned Sophora japonica flower instant powder composition or by the above-mentioned method.

[0028] In another aspect, the present invention provides the application of the sophora flower instant powder prepared by the above-mentioned sophora flower instant powder composition or method in the production of whitening products.

[0029] Preferably, the whitening product is an oral whitening product.

[0030] Compared with the prior art, the present invention has the following beneficial effects:

[0031] This invention provides a sophora japonica flower instant powder composition. By carefully selecting the ingredients and proportions and optimizing the preparation process, a sophora japonica flower instant powder with better solubilizing effect of rutin and quercetin, higher bioavailability, better solution stability, and significant whitening effect can be prepared, which is helpful for the development and utilization of sophora japonica flower and its effective components. Attached Figure Description

[0032] Figure 1 Photograph of the solution after standing for 14 days in a stability test of the Sophora japonica flower instant powder liquid system.

[0033] Figure 2 The graphs show the bioavailability of rutin and quercetin in Example 1 and Comparative Example 3.

[0034] Figure 3 The bar chart shows the skin tone scoring effect of the Sophora japonica flower instant powder provided in Example 1 in a human experiment. Different letters (a, b, or c) indicate significant differences between groups. p <0.05, the same letter label indicates that there is no significant difference between groups.

[0035] Figure 4 The bar chart shows the skin color improvement rate of the Sophora japonica flower instant powder provided in Example 1 in human experiments.

[0036] Figure 5 The bar chart shows the highest skin tone improvement rate in human experiments using the Sophora japonica flower instant powder provided in Example 1.

[0037] Figure 6Skin color characterization photos before and after taking the Flos Sophorae instant powder provided in Example 1 by human body experiment. DETAILED DESCRIPTION

[0038] Terms and statements of the present application:

[0039] 1. The articles "a", "an", and "the": Unless otherwise expressly specified to one (kind) of object, include plural objects.

[0040] 2. Numerical ranges: Unless otherwise expressly indicated, all ranges or ratios disclosed herein are to be understood to be inclusive of any and all sub-ranges or sub-ratios subsumed therein. For example, a stated range or ratio of 1 to 30 should be considered to include any and all sub-ranges or sub-ratios between the minimum value of 1 and the maximum value of 30, including by way of example only, 3 to 17, 4 to 10, 9 to 20, 6 to 18, 1 to 7, 20 to 30, and so forth; as well as fractional and whole increments such as 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19, 20, 21, 22, 23, 24, 25, 26, 27, 28, 29, and 30, and so forth.

[0041] The following non-limiting examples can make the ordinary skilled in the art more fully understand the present application, but not in any way limit the present application. The following content is only an exemplary description of the scope claimed by the present application, and the skilled in the art can make various changes and modifications to the present application according to the disclosed content, and it should also belong to the scope claimed by the present application.

[0042] The present application is further described below in the form of specific examples. The various chemical reagents used in the examples of the present application are obtained by conventional commercial routes unless otherwise specified. The contents described below are mass contents unless otherwise specified. It is understood to be carried out at room temperature unless otherwise specified.

[0043] In the following examples, some reagents are obtained as follows in Table 1:

[0044] Table 1

[0045]

[0046] In the following examples, the instruments and equipment used are as follows in Table 2:

[0047] Table 2

[0048]

[0049] Example 1

[0050] A Flos Sophorae instant composition consists of the following ingredients by weight parts.

[0051] Flos Sophorae 100 parts, phospholipid 35 parts, β-cyclodextrin 32 parts, gum arabic 1.5 parts, and sodium carboxymethyl cellulose 1.5 parts.

[0052] The method for preparing the instant sophora flower powder by using the instant sophora flower composition is as follows.

[0053] The sophora flower (hot air dried at 40-60℃, moisture content <15%, crushed and passed through a 20-mesh sieve) and 80% ethanol aqueous solution with a volume concentration of 80% are put into an extraction tank according to 1:10 (g:mL), the extraction temperature is set to 70℃, the ultrasonic power is 250W, the ultrasonic frequency is 30kHz, and the extraction time is 0.5h, the extraction liquid is filtered slowly by filter paper, the filter residue is subjected to secondary extraction, the extraction parameters are consistent with those of the first extraction, the two times of filtered liquid are combined, and then concentrated; then the concentrated liquid is placed in a high-pressure reaction kettle, a certain amount of 2mol / L hydrochloric acid solution is added, the pH value of the system is adjusted to 4, the pressure is set to 1.2 MPa, the temperature is 105℃, the hydrolysis time is 20min, and the pressure is rapidly reduced. Phospholipid and β-cyclodextrin are added in the system, the ultrasonic power is 100W, the treatment time is 30min, then gum arabic and sodium carboxymethyl cellulose are added, and stirred for 2h to obtain the polymer liposome. The polymer liposome is dried to obtain the instant sophora flower powder.

[0054] Example 2

[0055] An instant sophora flower composition is composed of the following ingredients by weight.

[0056] The instant sophora flower composition is composed of 100 parts of sophora flower, 35 parts of phospholipid, 28 parts of β-cyclodextrin, 3.5 parts of gum arabic, and 3.5 parts of sodium carboxymethyl cellulose.

[0057] The method for preparing the instant sophora flower powder by using the instant sophora flower composition is as follows.

[0058] The sophora flower (hot air dried at 40-60℃, moisture content <15%, crushed and passed through a 20-mesh sieve) and 90% ethanol aqueous solution with a volume concentration of 90% are put into an extraction tank according to 1:15 (g:mL), the extraction temperature is set to 70℃, the ultrasonic power is 250W, the ultrasonic frequency is 25kHz, and the extraction time is 0.5h, the extraction liquid is filtered slowly by filter paper, the filter residue is subjected to secondary extraction, the extraction parameters are consistent with those of the first extraction, the two times of filtered liquid are combined, and then concentrated; then the concentrated liquid is placed in a high-pressure reaction kettle, a certain amount of hydrochloric acid solution is added, the pH value of the system is adjusted to 3.5, the pressure is set to 1.2 MPa, the temperature is 105℃, the hydrolysis time is 20min, and the pressure is rapidly reduced. Phospholipid and β-cyclodextrin are added in the system, the treatment time is 30min, then gum arabic and sodium carboxymethyl cellulose are added, and stirred for 2h to obtain the polymer liposome, which is dried to obtain the instant sophora flower powder.

[0059] Example 3

[0060] An instant sophora flower composition is composed of the following ingredients by weight.

[0061] Sophora japonica 100 parts, phospholipid 30 parts, β-cyclodextrin 34 parts, gum arabic 0.6 parts and sodium carboxymethyl cellulose 5.4 parts.

[0062] The method for preparing the instant sophora japonica powder from the instant sophora japonica composition is as follows.

[0063] Sophora japonica (hot air dried at 40-60°C, moisture content <15%, crushed and passed through a 20-mesh sieve) and a 60% volume concentration ethanol aqueous solution are put into an extraction tank according to 1:10 (g:mL), the extraction temperature is set to 50°C, the ultrasonic power is 300W, and the ultrasonic frequency is 30 kHz, and extraction is performed for 1h, the extraction liquid is filtered slowly with filter paper, the filter residue is subjected to secondary extraction, the extraction parameters are consistent with those of the first extraction, the two times of filtered liquids are combined, and then concentrated; then the concentrated liquid is placed in a high-pressure reaction kettle, a certain amount of hydrochloric acid solution is added, the pH value of the system is adjusted to 4, the pressure is set to 1.2 MPa, the temperature is 115°C, the hydrolysis time is 15 min, the pressure is rapidly reduced, phospholipid and β-cyclodextrin are added to the system, the ultrasonic power is 100W, and after 25 min of treatment, gum arabic and sodium carboxymethyl cellulose are added, and stirred for 2h to obtain a polymer liposome, which is dried to obtain the instant sophora japonica powder.

[0064] Example 4

[0065] An instant sophora japonica composition is composed of the following ingredients by weight parts.

[0066] Sophora japonica 100 parts, phospholipid 30 parts, β-cyclodextrin 34 parts, gum arabic 5.4 parts and sodium carboxymethyl cellulose 0.6 parts.

[0067] The method for preparing the instant sophora japonica powder from the instant sophora japonica composition is as follows.

[0068] Sophora japonica (hot air dried at 40-60°C, moisture content <15%, crushed and passed through a 20-mesh sieve) and a 60% volume concentration ethanol aqueous solution are put into an extraction tank according to 1:10 (g:mL), the extraction temperature is set to 50°C, the ultrasonic power is 300W, and the ultrasonic frequency is 30 kHz, and extraction is performed for 1h, the extraction liquid is filtered slowly with filter paper, the filter residue is subjected to secondary extraction, the extraction parameters are consistent with those of the first extraction, the two times of filtered liquids are combined, and then concentrated; then the concentrated liquid is placed in a high-pressure reaction kettle, a certain amount of hydrochloric acid solution is added, the pH value of the system is adjusted to 4, the pressure is set to 1.2 MPa, the temperature is 115°C, the hydrolysis time is 15 min, the pressure is rapidly reduced, phospholipid and β-cyclodextrin are added to the system, the ultrasonic power is 100W, and after 25 min of treatment, gum arabic and sodium carboxymethyl cellulose are added, and stirred for 2h to obtain a polymer liposome, which is dried to obtain the instant sophora japonica powder.

[0069] Example 5

[0070] The method for preparing the instant sophora flower powder is as follows by using the instant sophora flower composition (sophora flower 100 parts, phospholipid 35 parts, β-cyclodextrin 32 parts, gum arabic 1.5 parts and sodium carboxymethyl cellulose 1.5 parts) described in Example 1.

[0071] The sophora flower (hot air dried at 40-60°C, moisture content <15%, crushed and passed through a 20-mesh sieve) and 80% ethanol aqueous solution are put into an extraction tank according to 1:8 (g:mL), the extraction temperature is set to 40°C, the ultrasonic power is 300W, the ultrasonic frequency is 35kHz, and the extraction is performed for 0.2h, the extraction liquid is filtered slowly with filter paper, the filter residue is extracted for the second time, the extraction parameters are the same as those of the first extraction, the two times of filtered liquids are combined and concentrated; then the concentrated liquid is placed in a high-pressure reaction kettle, a certain amount of hydrochloric acid solution is added, the pH value of the system is adjusted to 2.5, the pressure is set to 1.8MPa, the temperature is 125°C, the hydrolysis time is 30min, the pressure is rapidly reduced, phospholipid and β-cyclodextrin are added to the system, the ultrasonic power is 80W, and after the treatment time of 35min, gum arabic and carboxymethyl cellulose are added, and stirring is performed for 2h to obtain the polymer liposome, and the sophora flower instant powder is obtained after drying.

[0072] Example 6

[0073] The method for preparing the instant sophora flower powder is as follows by using the instant sophora flower composition (sophora flower 100 parts, phospholipid 30 parts, β-cyclodextrin 34 parts, gum arabic 5.4 parts and sodium carboxymethyl cellulose 0.6 parts) described in Example 4.

[0074] The sophora flower (hot air dried at 40-60°C, moisture content <15%, crushed and passed through a 20-mesh sieve) and 80% ethanol aqueous solution are put into an extraction tank according to 1:8 (g:mL), the extraction temperature is set to 40°C, the ultrasonic power is 300W, the ultrasonic frequency is 35kHz, and the extraction is performed for 0.2h, the extraction liquid is filtered slowly with filter paper, the filter residue is extracted for the second time, the extraction parameters are the same as those of the first extraction, the two times of filtered liquids are combined and concentrated; then the concentrated liquid is placed in a high-pressure reaction kettle, a certain amount of hydrochloric acid solution is added, the pH value of the system is adjusted to 2.5, the pressure is set to 1.8MPa, the temperature is 125°C, the hydrolysis time is 30min, the pressure is rapidly reduced, phospholipid and β-cyclodextrin are added to the system, the ultrasonic power is 80W, and after the treatment time of 35min, gum arabic and carboxymethyl cellulose are added, and stirring is performed for 2h to obtain the polymer liposome, and the sophora flower instant powder is obtained after drying.

[0075] Comparative Example 1

[0076] Compared with Example 1, the difference is that no hydrochloric acid solution is added to the high-pressure reaction kettle, the pH value of the system is not adjusted, the pH value is 6.4, and the rest is the same.

[0077] Comparative Example 2

[0078] The difference between the example 1 and the example 2 is that the pH value of the system is adjusted to 2 by adding hydrochloric acid solution in the high-pressure reactor, and the rest is the same.

[0079] Comparative example 3

[0080] The difference between the example 1 and the example 3 is that the solution is dried after hydrolysis and rapid decompression, and the extract of sophora flower is obtained. The phospholipid, β-cyclodextrin and the subsequent steps are omitted. The rest is the same.

[0081] Comparative example 4

[0082] The difference between the example 1 and the example 4 is that the dried sophora flower instant powder is obtained after adding phospholipid, β-cyclodextrin and ultrasonic treatment. The addition of gum arabic and carboxymethyl cellulose and the subsequent steps are omitted. The rest is the same.

[0083] Comparative example 5

[0084] The difference between the example 1 and the example 5 is that the ultrasonic extraction temperature of the mixture of sophora flower ethanol aqueous solution is changed to 80℃, and the rest is the same.

[0085] Comparative example 6

[0086] The difference between the example 1 and the example 6 is that the reaction pressure of the high-pressure acid hydrolysis is 2.6 MPa, and the reaction temperature of the high-pressure acid hydrolysis is 150℃.

[0087] Comparative example 7

[0088] The difference between the example 1 and the example 7 is that the reaction time of the high-pressure acid hydrolysis is 2h.

[0089] Comparative example 8

[0090] The difference between the example 1 and the example 8 is that the weight ratio of each component in the sophora flower instant composition is different, and the rest is the same. The weight ratio of each component in the sophora flower instant composition is changed to:

[0091] Sophora flower 100 parts, phospholipid 25 parts, β-cyclodextrin 42 parts, gum arabic 1.5 parts and carboxymethyl cellulose sodium 1.5 parts.

[0092] Comparative example 9

[0093] The difference between the example 1 and the example 9 is that the mixture of gum arabic and carboxymethyl cellulose is replaced by PVP (molecular weight 8000-12000) with the same weight, and the rest is the same.

[0094] Effect evaluation

[0095] 1. Test the solubility of sophora flower instant powder (calculated by rutin) and the solubility (calculated by quercetin).

[0096] Sample preparation: prepared according to each example and comparative example, comparative example 3 is sophora flower extract, the rest of each example is sophora flower instant powder.

[0097] Test method: 15g sample was weighed into 50mL deionized water, placed in a constant temperature water bath oscillator, constant temperature oscillation at 30℃ for 24h, centrifuged at 6000r / min for 15min with high speed centrifuge, 1mL supernatant was taken and diluted to 10mL with methanol in a volumetric flask, ultrasonic for 30min, filtered through 0.45μm filter membrane, and the extract was obtained. The concentration of quercetin and rutin in the extract was detected by HPLC, and then the concentration of rutin in the supernatant and the concentration of quercetin in the supernatant were calculated, which were the solubility (calculated by rutin) and solubility (calculated by quercetin).

[0098] The content of quercetin and rutin was determined by high performance liquid chromatography. The chromatographic conditions were as follows: C18 column (250 mm × 4.6 mm, 5 μm) was used as the chromatographic column; the mobile phase was 0.4% phosphoric acid aqueous solution:methanol = 60:40; the flow rate was 1.0 mL / min; the column temperature was 30℃; the detection wavelength was 360 nm; and the injection volume was 10 μL. The external standard method was used for quantification.

[0099] The experimental results are shown in Table 3 (n=3, mean ± standard deviation):

[0100] Table 3

[0101]

[0102] It can be seen that for the comparative example 3 sophora flower extract which is not treated with phospholipid, β-cyclodextrin, gum arabic and sodium carboxymethyl cellulose, the solubility of the two components quercetin and rutin in deionized water is very low. The polymer liposome embedding technology in each example utilizes the double-molecular layer structure of the internal hydrophobic and external hydrophilic formed by β-cyclodextrin and phospholipid to encapsulate quercetin and rutin in the hydrophobic region, thereby realizing the solubilization of quercetin and rutin. The liposome alone is unstable due to the charge effect system, and aggregation phenomenon easily occurs. The combination of gum arabic and sodium carboxymethyl cellulose stabilizes the liposome charge and improves the stability of the liposome inclusion compound, thereby improving the solubility (calculated by rutin) and solubility (calculated by quercetin).

[0103] 2. In vitro tyrosinase inhibition experiment of sophora flower instant powder

[0104] The inhibition of sophora flower instant powder on tyrosinase was determined by tyrosinase dopamine rate oxidation method.

[0105] A PBS buffer solution with pH of 6.8 was prepared with sodium phosphate dibasic and citric acid, and sample solutions with different mass concentrations, 5mmol / L L-dopa solution and 50U / mL tyrosinase solution were prepared with the buffer solution.

[0106] L-tyrosinase enzyme solution, PBS buffer and the sample solution were added into ABCD wells of the enzyme marker 96-well plate in sequence, mixed uniformly, and then incubated at 37°C for 10 min. L-dopa solution was quickly added into the four wells, and then incubated at 37°C for 5 min. The absorbance value was measured at 475 nm, and three groups of parallel experiments were set.

[0107] The inhibition rate of tyrosinase activity in vitro was calculated according to the following formula:

[0108] .

[0109] IC 50 values were given by the software.

[0110] In each group of experiments, the types and volumes of solutions added into the ABCD four wells were shown in Table 4 (‘-’ represents no addition of this component):

[0111] Table 4

[0112]

[0113] The IC 50 values of the products provided by each example and comparative example for inhibiting tyrosinase activity were shown in Table 5:

[0114] Table 5

[0115]

[0116] As shown in the above table, the sophora flower extract treated by high-pressure acid hydrolysis can significantly reduce the IC 50 value for inhibiting tyrosinase activity, which proves that it can realize the synergistic effect of tyrosinase inhibition by adjusting the proportion of rutin and quercetin dual-component active substances, and improve the application value of sophora flower.

[0117] For the comparative example 3 sophora flower extract which is not treated by phospholipid, β-cyclodextrin, gum arabic and sodium carboxymethyl cellulose, the inhibitory activity of the extract on tyrosinase is significantly improved by the polymer liposome embedding technology in each example.

[0118] 3. Sophora flower instant powder liquid system stability experiment.

[0119] 1.5 g of the products prepared in each example and each comparative example were dissolved in 50 mL of deionized water in sequence, respectively, and stirred uniformly. The pH value of the solution was adjusted to 4 using 20% citric acid / 20% sodium hydroxide. The solution was poured into a stoppered glass test tube, and autoclaved (115°C, 30 min). After sterilization, the sample was sealed and placed in a room temperature environment for 14 days, and the generation of solid precipitate was observed.

[0120] The evaluation indicators of the solution after standing at room temperature for 14 days are shown in Table 6 below:

[0121] Table 6

[0122]

[0123] The experimental results of the solutions from each example and comparative example after standing for 14 days are shown in Table 7 below:

[0124] Table 7

[0125]

[0126] like Figure 1 As shown, after standing for 14 days, the solution in Comparative Example 3 was opaque with a large amount of yellow crystal precipitate at the bottom, and Comparative Example 4 had a small amount of precipitate (liposomes are unstable). The systems of Examples 1-4 had no visible precipitate and had the best stability.

[0127] 4. Bioavailability test of Sophora japonica flower instant powder.

[0128] Experimental animals: SPF-grade male SD rats (weight 250±15g) were randomly assigned to groups. Husbandry conditions: Animal room temperature 22-25℃, relative humidity 50±10%, 12h light / dark cycle. They were fed normal water and food for one week to acclimatize to the environment.

[0129] Experimental Protocol: Rats were fasted for 12 hours prior to the gavage experiment, but had free access to water. Rats were randomly divided into two groups of six each, and were administered either Example 1 (Sophora japonica flower powder) or Control Example 3 (Sophora japonica flower extract dispersed in sodium carboxymethyl cellulose solution) by gavage, with the same content of active ingredients (quercetin and rutin) (60 mg / kg). Following oral administration, blood was collected in heparinized tubes via orbital puncture at designed time points of 0, 0.25, 0.5, 1, 1.5, 2, 4, 6, 8, 12, 16, 20, and 24 hours. Serum was collected by centrifugation at 6000 rpm for 10 minutes and then stored at -20°C for later use.

[0130] Plasma processing: When extracting quercetin and rutin from serum, 200 μL of plasma sample was added to 100 μL of phosphate buffer (pH 5.0), vortexed for 2 min, then 800 μL of ethyl acetate was added for extraction, vortexed for 4 min, and centrifuged at 3000 rpm for 10 min to separate the organic layer. The organic layer was transferred to a 1.5 mL centrifuge tube, dried under nitrogen, and the residue was dissolved in 100 μL of methanol and vortexed for 5 min. Then, the mixture was centrifuged at 9000 g for 10 min, and the supernatant was used for chromatographic analysis.

[0131] Experimental results are as follows Figure 2The blood concentration of active ingredients (rutin and quercetin) in the sample of Comparative Example 3 in rats is very low, and after treatment by the polymeric liposome technology, the drug absorption degree can be significantly improved, the peak concentration (Cmax) is increased, the in vivo retention time (MRT 0-∞ ) is prolonged, and the area under the drug-time curve (AUC 0-∞ ) is increased. Compared with the sophora flower extract of Comparative Example 3, the bioavailability of quercetin and rutin in the sophora flower instant powder of Example 1 is increased by 28.48 and 35.81 times, respectively. Therefore, the sophora flower instant powder preparation prepared in the present application can significantly improve the oral bioavailability of rutin and quercetin by improving the solubility of rutin and quercetin.

[0132] Further, according to the above method, the peak concentration, in vivo retention time and area under the drug-time curve of rutin of each example and comparative example are detected. The technical effects are summarized in Table 8 below:

[0133] Table 8

[0134]

[0135] The peak concentration, in vivo retention time and area under the drug-time curve of quercetin of each example and comparative example are detected. The technical effects are summarized in Table 9 below:

[0136] Table 9

[0137]

[0138] 5. Volunteer test of sophora flower instant powder

[0139] According to the test results above, the application effect of the sophora flower instant powder prepared in Example 1 in the oral whitening product is explored, and the specific process is as follows:

[0140] 5.1. Selection and requirements of volunteers

[0141] Ten healthy male and female subjects aged 25-40 years old are selected, and all subjects have no history of skin or systemic diseases. During the test period, the subjects use the test sample according to the requirements, and cannot use other products with whitening effect or may affect the test results.

[0142] 5.2. Sophora flower instant powder taking method

[0143] A certain amount of sophora flower instant powder is accurately weighed and dissolved in 200 mL of warm water for taking. It is taken twice a day before 10 o'clock after breakfast and before going to bed, and is taken continuously for 30 days.

[0144] 5.3. Test method

[0145] Test site constant temperature and humidity (temperature 20-22℃, relative humidity 45%-55%), after the test, the test subjects are washed with 35℃ water on the face, and then sit in the test environment for 30 minutes before starting the test.

[0146] Monitoring method: facial image acquisition and facial skin color and spot characteristics are statistically analyzed by using AISIA-Q2 skin detector.

[0147] Skin color quantification index: 0-20 points for white, 20-40 points for natural, 40-60 points for uneven skin color, 60-80 points for dull, and 80-100 points for dark. Each group of experiments is repeated 4 times, and the average value and standard deviation are calculated.

[0148] Detection time: before using the sample (D0, initial value), after using the sample for 30 days (D30, experimental value).

[0149] Skin color quantification: the detector quantifies the facial skin color in scale value, and the higher the quantification percentage indicates the darker the skin color.

[0150] The experimental results are shown in Figures 4-6 .

[0151] After taking the Flos Sophorae instant powder of example 1, the facial skin color of the subjects on the front face, left face and right face is obviously brightened, and the skin color scale value is reduced by 5.33%, 7.22% and 4.11% respectively. The average improvement of the facial skin color of the 10 subjects on the front face, left face and right face is 7.43%, 12.11% and 6.25%, and the highest improvement rate reaches 15.94%, 27.69% and 10.60%.

[0152] Conclusion:

[0153] The present application greatly improves the inhibition of tyrosinase activity of Flos Sophorae instant powder by adjusting the proportion of active substances and applying embedding technology.

[0154] Finally, it should be noted that the above content is only used to illustrate the technical solutions of the present application, and is not a limitation on the protection scope of the present application. Simple modifications or equivalent replacements of the technical solutions of the present application made by those skilled in the art do not deviate from the essence and scope of the technical solutions of the present application.

Claims

1. A composition of instant Sophora japonica flower powder, characterized in that, It consists of the following components by weight: 100 parts of Sophora japonica flowers, 30-35 parts of phospholipids, 28-34 parts of β-cyclodextrin, and 3-7 parts of polysaccharide coating agent; The polysaccharide coating agent is composed of gum arabic and sodium carboxymethyl cellulose. The method for preparing instant sophora flower powder using the aforementioned instant sophora flower powder composition includes the following steps: S1. Mix the Sophora japonica flowers with a solvent and extract with ultrasound 1-3 times. Collect the filtrate to obtain the ultrasonic extract. S2. Adjust the pH of the ultrasonic extract obtained in step S1, and perform high-pressure acid hydrolysis to obtain the acid hydrolyzed extract. S3. The acid hydrolyzed extract obtained in step S2 is mixed with β-cyclodextrin and phospholipids, ultrasonically treated, then mixed with polysaccharide coating agent, stirred, and dried to obtain Sophora japonica flower instant powder. In step S1, the temperature of the ultrasonic extraction is 40-70℃; In step S2, adjusting the pH specifically involves adding hydrochloric acid and adjusting the pH to 2.5-5; the pressure of the high-pressure acid hydrolysis reaction is 0.5-1.8 MPa, the temperature of the high-pressure acid hydrolysis reaction is 95-125℃, and the time of the high-pressure acid hydrolysis reaction is 10-30 min.

2. The instant sophora flower powder composition according to claim 1, characterized in that, The weight ratio of gum arabic to sodium carboxymethyl cellulose is 1-9:1-9.

3. A method for preparing instant sophora flower powder using the sophora flower instant powder composition according to any one of claims 1-2, characterized in that, Includes the following steps: S1. Mix the Sophora japonica flowers with a solvent and extract with ultrasound 1-3 times. Collect the filtrate to obtain the ultrasonic extract. S2. Adjust the pH of the ultrasonic extract obtained in step S1, and perform high-pressure acid hydrolysis to obtain the acid hydrolyzed extract. S3. The acid hydrolyzed extract obtained in step S2 is mixed with β-cyclodextrin and phospholipids, ultrasonically treated, then mixed with polysaccharide coating agent, stirred, and dried to obtain Sophora japonica flower instant powder. In step S1, the temperature of the ultrasonic extraction is 40-70℃; In step S2, adjusting the pH specifically involves adding hydrochloric acid and adjusting the pH to 2.5-5; the pressure of the high-pressure acid hydrolysis reaction is 0.5-1.8 MPa, the temperature of the high-pressure acid hydrolysis reaction is 95-125℃, and the time of the high-pressure acid hydrolysis reaction is 10-30 min.

4. The method according to claim 3, characterized in that, In step S1, the solvent is an aqueous ethanol solution, the ratio of the amount of Sophora japonica flower to the solvent is 1:8-15 (in g:mL), the frequency of the ultrasonic extraction is 20-35kHz, the power of the ultrasonic extraction is 150-300W, and the time of the ultrasonic extraction is 0.2-1h.

5. The method according to claim 4, characterized in that, In step S1, the ethanol-water solution is an aqueous solution with an ethanol volume concentration of 60%-90%, the ratio of the amount of Sophora japonica flowers to the solvent is 1:10-15 (in g:mL), the temperature of the ultrasonic extraction is 50-70℃, the power of the ultrasonic extraction is 250-300W, and the time of the ultrasonic extraction is 0.5-1h.

6. The method according to claim 3, characterized in that, In step S2, adjusting the pH specifically involves adding hydrochloric acid and adjusting the pH to 3.5-4; the pressure of the high-pressure acid hydrolysis reaction is 1.0-1.5 MPa, the temperature of the high-pressure acid hydrolysis reaction is 100-115℃, and the duration of the high-pressure acid hydrolysis reaction is 15-20 min; in step S3, the power of the ultrasonic treatment is 80-120 W, and the duration of the ultrasonic treatment is 25-35 min.

7. A kind of instant sophora flower powder, characterized in that, Prepared by the method described in any one of claims 4-6.

8. The use of the Sophora japonica flower instant powder composition according to any one of claims 1-2 or the Sophora japonica flower instant powder according to claim 7 in the production of whitening products.

Citation Information

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