Fructus aurantii processing method and application thereof

By employing a three-stage steaming process and a non-fermentation method for processing Citrus aurantium, the problems of existing technologies, such as the inability of fermentation processes to meet the standardized production requirements of traditional Chinese medicine, high loss rates of alkaloids and flavonoids, and long production cycles, have been solved, thus achieving standardization of Citrus aurantium processing and enhanced efficacy.

CN120983528APending Publication Date: 2025-11-21KANGMEI PHARMA
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Patent Information

Application Number
CN202511233712.2
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2025-09-01
Publication Date
2025-11-21

AI Technical Summary

Technical Problem

The existing processing methods for Citrus aurantium cannot meet the requirements of standardized production of traditional Chinese medicine due to the fermentation process, resulting in high loss rates of alkaloids and flavonoids, long production cycles, and low production efficiency.

Method used

A three-stage steaming process is adopted, including a first steaming, a second steaming, and a third steaming under different temperature and pressure conditions. Combined with drying and slicing steps, the fermentation step is eliminated, ensuring the standardization and effectiveness of the processing.

Benefits of technology

It increased the N-methyltyramine content by at least 2 times, reduced the generation of harmful substances, improved drug performance, and achieved standardized production and enhanced efficacy of traditional Chinese medicine.

✦ Generated by Eureka AI based on patent content.

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Abstract

The invention provides a fructus aurantii processing method and application thereof, and relates to the technical field of fructus aurantii processing, and the method comprises the following steps: performing first steaming on fructus aurantii at 100-110 DEG C under 0.1-0.2 Mpa, then performing second steaming at 75-85 DEG C under 0.05-0.1 Mpa, then performing third steaming at 110-120 DEG C under 0.1-0.2 Mpa, and drying to obtain processed fructus aurantii. The technical problems that in an existing processing method, a fermentation technology cannot meet the standard production requirement of traditional Chinese medicine, the loss rate of alkaloid flavonoids is high, the production period is long, and the production efficiency is low are solved. The technical effects of retaining flavonoid active ingredients to a great extent, directionally enhancing the medicine performance, inhibiting the growth of toxic substances and improving the medicine property of the steamed fructus aurantii are achieved, and the processing target of reducing toxicity and improving efficiency is achieved.
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Description

Technical Field

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[0001] The present invention relates to the technical field of processing Fructus Aurantii Immaturus, and in particular to a method for processing Fructus Aurantii Immaturus and its application. Background Art

[0002] Fructus Aurantii Immaturus is the dried immature fruit of Citrus aurantium L. and its cultivated varieties. It is harvested in July when the pericarp is still green, cut transversely into two halves from the middle, and dried in the sun or by low-temperature drying. Traditional Chinese medicine believes that Fructus Aurantii Immaturus is slightly cold in nature, bitter, pungent, and sour in taste, and belongs to the spleen and stomach meridians. It has the effects of regulating qi and relieving fullness, promoting qi circulation and relieving distension, and resolving phlegm. It is used for chest and hypochondriac qi stagnation, distending pain, indigestion of food accumulation, internal retention of phlegm-fluid, and visceral ptosis, etc.

[0003] The commonly used processing method of Fructus Aurantii Immaturus is to ferment first and then steam. Specifically, impurities and the core are removed, washed, soaked until 70% penetrated, taken out, fermented for 3 - 4 days, washed, steamed for 4 - 6 hours, and kept covered overnight. When the interior turns dark purple, take out, slice, and dry. The existing processing technology of fermenting and steaming Fructus Aurantii Immaturus has the following drawbacks: (1) The fermentation process depends on environmental microorganisms, with large batch-to-batch differences and unable to meet the requirements of modern standardized production of traditional Chinese medicine; (2) The loss rate of alkaloids and flavonoids during fermentation is high; (3) Generally, the fermentation of Fructus Aurantii Immaturus needs to last for 3 - 4 days, steam for 4 - 6 hours, and keep covered overnight, with a long production cycle and low production efficiency.

[0004] Therefore, there is an urgent need for a method for processing Fructus Aurantii Immaturus with high production efficiency, stable quality and safety, which can also increase the selectivity and safety in the clinical syndrome differentiation and medication of traditional Chinese medicine.

[0005] In view of this, the present invention is specifically proposed. Summary of the Invention

[0006] One of the purposes of the present invention is to provide a method for processing Fructus Aurantii Immaturus, which can solve the technical problems in the existing processing method such as the fermentation process being unable to meet the requirements of standardized production of traditional Chinese medicine, high loss rate of alkaloids and flavonoids, long production cycle and low production efficiency, and achieve the processing goal of "reducing toxicity and enhancing efficacy".

[0007] Another purpose of the present invention is to provide an application of the method for processing Fructus Aurantii Immaturus, which is beneficial to reducing toxicity and enhancing the efficacy of drugs.

[0008] In order to achieve the above purposes of the present invention, the following technical solutions are specifically adopted: In the first aspect, a method for processing Fructus Aurantii Immaturus includes the following steps: First, steam Fructus Aurantii Immaturus at 100°C to 110°C and 0.1 Mpa to 0.2 Mpa for the first steaming, then steam at 75°C to 85°C and 0.05 Mpa to 0.1 Mpa for the second steaming, then steam at 110°C to 120°C and 0.1 Mpa to 0.2 Mpa for the third steaming, and then dry to obtain the processed Fructus Aurantii Immaturus.

[0009] Furthermore, the first steaming time is 30 to 40 minutes.

[0010] Furthermore, the second steaming time is 6 to 8 hours.

[0011] Furthermore, the duration of the third steaming is 15 min to 25 min.

[0012] Furthermore, the degree of drying is such that the moisture content does not exceed 13%.

[0013] Furthermore, the process includes air-drying and slicing steps prior to drying.

[0014] Furthermore, the degree of drying is at least 60% dry.

[0015] Furthermore, the thickness of the slice is 2mm-4mm.

[0016] Furthermore, the N-methyltyramine content in the processed bitter orange peel increases by 2 to 4 times.

[0017] Secondly, the application of any of the above-mentioned methods for processing Citrus aurantium in drug preparation.

[0018] Compared with the prior art, the present invention has at least the following beneficial effects: The method for processing Citrus aurantium provided by this invention eliminates the fermentation step in the processing, thereby avoiding the growth of harmful substances and making the processing process easier to standardize, which is conducive to ensuring medication safety. Through a specific three-stage steaming process, the content of N-methyltyramine is increased by at least 2 times. N-methyltyramine has functions such as improving myocardial function, regulating vascular resistance, and antidepressant and mood-regulating effects, thus enhancing the drug's ability to regulate qi and relieve chest tightness. In summary, with the synergistic cooperation of each step and its parameters, this invention solves the technical problems in existing processing methods, such as the inability of fermentation processes to meet the standardized production requirements of traditional Chinese medicine, high loss rate of alkaloids and flavonoids, long production cycle, and low production efficiency. It achieves the technical effects of maximizing the preservation of flavonoid active ingredients, targeted enhancement of drug performance, inhibition of the growth of toxic substances, and improvement of the medicinal properties of steamed Citrus aurantium, realizing the processing goal of "reducing toxicity and increasing efficacy".

[0019] The application of the method for processing Citrus aurantium provided by this invention helps to reduce toxicity and enhance the efficacy of the drug. Detailed Implementation

[0020] The technical solution of the present invention will be clearly and completely described below with reference to the embodiments. Obviously, the described embodiments are only some embodiments of the present invention, and not all embodiments. Based on the embodiments of the present invention, all other embodiments obtained by those skilled in the art without creative effort are within the scope of protection of the present invention.

[0021] According to a first aspect of the present invention, a method for processing Citrus aurantium is provided, comprising the following steps: The dried bitter orange peel is first steamed at 100℃~110℃ and 0.1Mpa~0.2Mpa, then steamed at 75℃~85℃ and 0.05Mpa~0.1Mpa, and then steamed at 110℃~120℃ and 0.1Mpa~0.2Mpa, and then dried to obtain the processed bitter orange peel.

[0022] In this invention, the fermentation step in the processing is removed, which can avoid the growth of harmful substances and the generation of fungal toxins (such as aflatoxin), making the processing process easier to standardize and helping to ensure medication safety. At the same time, through a specific three-stage steaming process, the content of N-methyltyramine is increased by at least 2 times. N-methyltyramine has functions such as improving myocardial function, regulating vascular resistance, and antidepressant and mood-regulating effects, thus helping to enhance the drug's ability to regulate qi and relieve chest tightness.

[0023] In a preferred embodiment, the first steaming time can be 30 min to 40 min, with typical but non-limiting times being 30 min, 32 min, 34 min, 36 min, 38 min, or 40 min.

[0024] After cleaning, place the Citrus aurantium in a steaming machine and steam for 30 to 40 minutes at a steaming temperature of 100℃~110℃ and a steaming pressure of 0.1Mpa~0.2Mpa. This can promote tissue softening and allow some of the volatile oil to escape.

[0025] In a preferred embodiment, the second steaming time can be 6h to 8h, with typical but non-limiting times being 6h, 6.5h, 7h, 7.5h, or 8h.

[0026] When Citrus aurantium is steamed in a steaming machine at a temperature of 75℃~85℃ and a pressure of 0.05Mpa~0.1Mpa for 6h~8h, it can induce the activation of endogenous enzymes and directionally convert tyrosine into N-methyltyramine, which has higher alkaloid activity.

[0027] It should be noted that the alkaloid retention mechanism (synergistic principle) is as follows: mild conditions promote the methylation reaction of alkaloids and induce the activation of endogenous enzymes. Tyrosine generates tyramine (containing free amino groups) through decarboxylation, and further methylation forms N-methyltyramine with higher pharmacological activity. Compared with traditional processes, the content of N-methyltyramine can be increased by at least 2 times.

[0028] In a preferred embodiment, the third steaming time can be 15 min to 25 min, with typical but non-limiting times being, for example, 15 min, 20 min, or 25 min.

[0029] The bitter orange peel is steamed in a steaming machine at a temperature of 110℃~120℃ and a pressure of 0.1Mpa~0.2Mpa for 15min~25min to inactivate enzymes and stabilize components, thus preventing the enzymatic hydrolysis of alkaloids such as N-methyltyramine.

[0030] In a preferred embodiment, the degree of drying can be such that the moisture content does not exceed 13%.

[0031] It should be noted that the process includes air-drying and slicing steps before drying. The degree of air-drying is at least 60% dry, and the thickness of the slices can be 2mm-4mm. Typical but non-limiting thicknesses include 2mm, 2.2mm, 2.4mm, 2.6mm, 2.8mm, 3mm, 3.2mm, 3.4mm, 3.6mm, 3.8mm, and 4mm.

[0032] In this invention, the N-methyltyramine content in the processed bitter orange peel can be increased by 2 to 4 times compared to the unprocessed bitter orange peel.

[0033] In summary, through the coordinated operation of each step and its parameters, this invention solves the technical problems in existing processing methods, such as the inability of fermentation processes to meet the standardized production requirements of traditional Chinese medicine, high loss rates of alkaloids and flavonoids, long production cycles, and low production efficiency. It achieves the technical effects of maximizing the preservation of flavonoid active ingredients, directionally enhancing drug performance, inhibiting the growth of toxic substances, and improving the medicinal properties of steamed bitter orange peel, thus realizing the processing goal of "reducing toxicity and increasing efficacy".

[0034] According to a second aspect of the present invention, the application of the above-described method for processing Citrus aurantium in drug preparation is provided.

[0035] The application of the method for processing Citrus aurantium provided by this invention helps to reduce toxicity and enhance the efficacy of the drug.

[0036] The present invention will be further illustrated below by way of examples. Unless otherwise specified, the materials in the examples are prepared according to existing methods or purchased directly from the market.

[0037] Example 1 A method for processing Citrus aurantium includes the following steps: (1) Place the cleaned and selected bitter orange peel in a steaming machine and steam for 35 minutes at a steaming temperature of 105℃ and a steaming pressure of 0.15Mpa; (2) After the bitter orange peel is slightly dried, it is placed in a steaming machine and steamed for 7 hours at a steaming temperature of 80℃ and a steaming pressure of 0.08Mpa. (3) Steam for another 20 minutes at a steaming temperature of 115℃ and a steaming pressure of 0.15Mpa, then remove; (4) Dry until 60% dry, slice to a thickness of 3mm, and dry until the moisture content does not exceed 13% to obtain processed bitter orange peel.

[0038] The properties of Citrus aurantium before and after processing are shown in Table 1.

[0039] Table 1

[0040] Note: "-" indicates not detected.

[0041] As can be seen, no aflatoxin was detected, while N-methyltyramine was significantly elevated and tyrosine was significantly decreased, indicating that the conversion efficiency was high.

[0042] Example 2 The only difference between this embodiment and embodiment 1 is that in step (1), steaming is carried out at a steaming temperature of 100°C and a steaming pressure of 0.1 MPa. The remaining steps and parameters are the same as in Example 1, and the processed bitter orange peel is obtained.

[0043] The properties of Citrus aurantium before and after processing are shown in Table 2.

[0044] Table 2

[0045] Note: "-" indicates not detected.

[0046] Example 3 The only difference between this embodiment and embodiment 1 is that, in step (1), steaming is carried out at a steaming temperature of 110°C and a steaming pressure of 0.2 MPa. The remaining steps and parameters are the same as in Example 1, and the processed bitter orange peel is obtained.

[0047] The properties of Citrus aurantium before and after processing are shown in Table 3.

[0048] Table 3

[0049] Note: "-" indicates not detected.

[0050] Example 4 The only difference between this embodiment and embodiment 1 is that, in step (2), steaming is carried out at a steaming temperature of 75°C and a steaming pressure of 0.05 MPa. The remaining steps and parameters are the same as in Example 1, and the processed bitter orange peel is obtained.

[0051] The properties of Citrus aurantium before and after processing are shown in Table 4.

[0052] Table 4

[0053] Note: "-" indicates not detected.

[0054] Example 5 The only difference between this embodiment and embodiment 1 is that, in step (2), steaming is carried out at a steaming temperature of 85°C and a steaming pressure of 0.1 MPa. The remaining steps and parameters are the same as in Example 1, and the processed bitter orange peel is obtained.

[0055] The properties of Citrus aurantium before and after processing are shown in Table 5.

[0056] Table 5

[0057] Note: "-" indicates not detected.

[0058] Example 6 The only difference between this embodiment and embodiment 1 is that, in step (3), steaming is carried out at a steaming temperature of 110°C and a steaming pressure of 0.1 MPa. The remaining steps and parameters are the same as in Example 1, and the processed bitter orange peel is obtained.

[0059] The properties of Citrus aurantium before and after processing are shown in Table 6.

[0060] Table 6

[0061] Note: "-" indicates not detected.

[0062] Example 7 The only difference between this embodiment and embodiment 1 is that in step (3), steaming is carried out at a steaming temperature of 120°C and a steaming pressure of 0.2 MPa. The remaining steps and parameters are the same as in Example 1, and the processed bitter orange peel is obtained.

[0063] The properties of Citrus aurantium before and after processing are shown in Table 7.

[0064] Table 7

[0065] Note: "-" indicates not detected.

[0066] Comparative Example 1 A method for processing Citrus aurantium includes the following steps: Take 100kg of cleaned and selected bitter orange peel, place it in an environment of 35℃ and 75% humidity for 4 days to ferment continuously, then place it in a steaming machine and steam it for 5 hours at 105℃ and normal pressure. After steaming overnight, take it out, dry it until it is 60% dry, slice it, and dry it until the moisture content does not exceed 13% to obtain the processed bitter orange peel.

[0067] The properties of Citrus aurantium before and after processing are shown in Table 8.

[0068] Table 8

[0069] Note: "-" indicates not detected.

[0070] It is evident that the detection of aflatoxin, N-methyltyramine, and tyrosine all showed a decreasing trend, indicating that during the fermentation process, microorganisms decomposed N-methyltyramine through enzymatic hydrolysis. N-methyltyramine was consumed by microorganisms as a substrate, and the acidified environment also accelerated the degradation of N-methyltyramine. At the same time, tyrosine and N-methyltyramine failed to complete an effective conversion.

[0071] Comparative Example 2 The only difference between this comparative example and Example 1 is that the steaming in step (1) was not performed; The remaining steps and parameters are the same as in Example 1, and the processed bitter orange peel is obtained.

[0072] The properties of Citrus aurantium before and after processing are shown in Table 9.

[0073] Table 9

[0074] Note: "-" indicates not detected.

[0075] Comparative Example 3 The only difference between this comparative example and Example 1 is that, in step (1), steaming is carried out at a steaming temperature of 90°C and a steaming pressure of 0.05 MPa. The remaining steps and parameters are the same as in Example 1, and the processed bitter orange peel is obtained.

[0076] The properties of Citrus aurantium before and after processing are shown in Table 10.

[0077] Table 10

[0078] Note: "-" indicates not detected.

[0079] Comparative Example 4 The only difference between this comparative example and Example 1 is that, in step (1), steaming is carried out at a steaming temperature of 120°C and a steaming pressure of 0.25 MPa. The remaining steps and parameters are the same as in Example 1, and the processed bitter orange peel is obtained.

[0080] The properties of Citrus aurantium before and after processing are shown in Table 11.

[0081] Table 11

[0082] Note: "-" indicates not detected.

[0083] Comparative Example 5 The only difference between this comparative example and Example 1 is that the steaming in step (2) was not performed; The remaining steps and parameters are the same as in Example 1, and the processed bitter orange peel is obtained.

[0084] The properties of Citrus aurantium before and after processing are shown in Table 12.

[0085] Table 12

[0086] Note: "-" indicates not detected.

[0087] Comparative Example 6 The only difference between this comparative example and Example 1 is that, in step (2), the steaming is carried out at a steaming temperature of 70°C and a steaming pressure of 0.03 MPa. The remaining steps and parameters are the same as in Example 1, and the processed bitter orange peel is obtained.

[0088] The properties of Citrus aurantium before and after processing are shown in Table 13.

[0089] Table 13

[0090] Note: "-" indicates not detected.

[0091] Comparative Example 7 The only difference between this comparative example and Example 1 is that, in step (2), steaming is carried out at a steaming temperature of 90°C and a steaming pressure of 0.15 MPa. The remaining steps and parameters are the same as in Example 1, and the processed bitter orange peel is obtained.

[0092] The properties of Citrus aurantium before and after processing are shown in Table 14.

[0093] Table 14

[0094] Note: "-" indicates not detected.

[0095] Comparative Example 8 The only difference between this comparative example and Example 1 is that the steaming in step (3) was not performed; The remaining steps and parameters are the same as in Example 1, and the processed bitter orange peel is obtained.

[0096] The properties of Citrus aurantium before and after processing are shown in Table 15.

[0097] Table 15

[0098] Note: "-" indicates not detected.

[0099] Comparative Example 9 The only difference between this comparative example and Example 1 is that, in step (3), steaming is carried out at a steaming temperature of 105°C and a steaming pressure of 0.05 MPa. The remaining steps and parameters are the same as in Example 1, and the processed bitter orange peel is obtained.

[0100] The properties of Citrus aurantium before and after processing are shown in Table 16.

[0101] Table 16

[0102] Note: "-" indicates not detected.

[0103] Comparative Example 10 The only difference between this comparative example and Example 1 is that, in step (3), steaming is carried out at a steaming temperature of 125°C and a steaming pressure of 0.25 MPa. The remaining steps and parameters are the same as in Example 1, and the processed bitter orange peel is obtained.

[0104] The properties of Citrus aurantium before and after processing are shown in Table 17.

[0105] Table 17

[0106] Note: "-" indicates not detected.

[0107] It is evident that, through the coordinated operation of each step and its parameters, this invention solves the technical problems in existing processing methods, such as the inability of fermentation processes to meet the standardized production requirements of traditional Chinese medicine, high loss rates of alkaloids and flavonoids, long production cycles, and low production efficiency. It achieves the technical effects of maximally preserving the active components of flavonoids, directionally enhancing drug performance, inhibiting the growth of toxic substances, and improving the medicinal properties of steamed bitter orange peel, thus realizing the processing goal of "reducing toxicity and increasing efficacy".

[0108] Finally, it should be noted that the above embodiments are only used to illustrate the technical solutions of the present invention, and not to limit them; although the present invention has been described in detail with reference to the foregoing embodiments, those skilled in the art should understand that modifications can still be made to the technical solutions described in the foregoing embodiments, or equivalent substitutions can be made to some or all of the technical features; and these modifications or substitutions do not cause the essence of the corresponding technical solutions to deviate from the scope of the technical solutions of the embodiments of the present invention.

Claims

1. A method for processing Citrus aurantium, characterized in that, Includes the following steps: The dried bitter orange peel is first steamed at 100℃~110℃ and 0.1Mpa~0.2Mpa, then steamed at 75℃~85℃ and 0.05Mpa~0.1Mpa, and then steamed at 110℃~120℃ and 0.1Mpa~0.2Mpa, and then dried to obtain the processed bitter orange peel.

2. The method for processing Citrus aurantium according to claim 1, characterized in that, The first steaming time is 30-40 minutes.

3. The method for processing Citrus aurantium according to claim 2, characterized in that, The second steaming time is 6 to 8 hours.

4. The method for processing Citrus aurantium according to claim 3, characterized in that, The third steaming time is 15 min to 25 min.

5. The method for processing Citrus aurantium according to any one of claims 1-4, characterized in that, The degree of dryness is such that the moisture content does not exceed 13%.

6. The method for processing Citrus aurantium according to claim 5, characterized in that, The process includes air drying and slicing before drying.

7. The method for processing Citrus aurantium according to claim 6, characterized in that, The degree of drying is at least 60% dry.

8. The method for processing Citrus aurantium according to claim 6, characterized in that, The thickness of the slice is 2mm-4mm.

9. The method for processing Citrus aurantium according to claim 5, characterized in that, The N-methyltyramine content in the processed bitter orange peel increases by 2 to 4 times.

10. The application of the method for processing Citrus aurantium according to any one of claims 1-9 in drug preparation.