A traditional Chinese medicine composition for improving constipation, a preparation method and application thereof
Patent Information
- Application Number
- CN202611478576.8
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2026-09-22
- Publication Date
- 2026-10-27
AI Technical Summary
然而,该工艺存在明显缺陷:白术挥发油中的苍术酮与厚朴酚在高温共煎时易发生缔合反应而损失;桃仁中的脂肪酶会水解部分苷类成分(如苦杏仁苷),导致活性成分保留率低,药效不稳定
通过桃仁预处理灭酶,显著提高了苦杏仁苷的保留率(≥95%),避免了提取过程中苷类成分的水解损失。
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Figure CN122973530A_ABST
Abstract
Description
Technical Field
[0001] This invention relates to the field of traditional Chinese medicine composition technology, and in particular to a traditional Chinese medicine composition for improving constipation, its preparation method and application. Background Technology
[0002] Constipation is a common gastrointestinal motility disorder in clinical practice, with slow transit constipation and constipation-predominant irritable bowel syndrome being particularly prevalent. Traditional Chinese medicine has unique advantages in improving constipation, often using formulas containing ingredients such as Atractylodes macrocephala, Citrus aurantium, Magnolia officinalis, Prunus persica, and Glycyrrhiza uralensis to exert its therapeutic effects by strengthening the spleen and replenishing qi, promoting qi circulation and relieving stagnation, and moistening the intestines to facilitate bowel movements.
[0003] Existing technology CN118319990B discloses a traditional Chinese medicine composition containing raw Atractylodes macrocephala, Citrus aurantium, and Prunus persica, and its preparation method, which employs a mixed oil-water extraction process. However, this process has significant drawbacks: atractylone and magnolol in the volatile oil of Atractylodes macrocephala are easily lost due to association reactions during high-temperature co-decoction; lipases in Prunus persica hydrolyze some glycosides (such as amygdalin), resulting in low retention of active ingredients and unstable efficacy.
[0004] To address the aforementioned issues, existing technologies have proposed an improved approach of "fractional extraction and targeted enrichment," which involves extracting medicinal materials from different fractions separately. However, this approach still has the following shortcomings: ① Peach kernels are not subjected to enzyme inactivation treatment before extraction, and lipases and β-glucosidase may still hydrolyze some amygdalin in the early stages of extraction; ② The volatile oil inclusion method is singular, using only β-cyclodextrin or hydroxypropyl-β-cyclodextrin, leaving room for improvement in drug loading, stability, and intestinal absorption; ③ The polysaccharide fraction is not molecular weight fractionated, resulting in insufficient purity of active polysaccharides and unstable intestinal flora regulation; ④ During final granulation, the fractions are simply mixed, failing to achieve spatiotemporal matching release of different active ingredients in the gastrointestinal tract, thus affecting the overall efficacy. Summary of the Invention
[0005] The purpose of this invention is to provide a traditional Chinese medicine composition, preparation method and application for improving constipation. Through a complete technology chain of "pretreatment enzyme inactivation - three-domain directional extraction - ternary inclusion - membrane separation polysaccharide fractionation - three-phase time-sequential release", the active ingredients are efficiently retained, directionally enriched and synergistically released.
[0006] To achieve the above objectives, the present invention provides a traditional Chinese medicine composition for improving constipation, comprising the following raw materials in parts by weight: 50-70 parts of raw Atractylodes macrocephala, 10-15 parts of Citrus aurantium, 10-15 parts of Magnolia officinalis, 8-12 parts of Prunus persica, and 5-8 parts of processed Glycyrrhiza uralensis. The traditional Chinese medicine composition comprises A stream of volatile oil inclusion complex, B stream of ethanol extract dry powder, and C stream of polysaccharide dry powder; The A-flow volatile oil inclusion complex is a hydroxypropyl-β-cyclodextrin-phospholipid ternary inclusion complex of the volatile oils of raw Atractylodes macrocephala and Citrus aurantium; The B-flow ethanol extract dry powder is a 70%-80% ethanol reflux extract of Magnolia officinalis, Prunus persica, and Glycyrrhiza uralensis. The C-flow polysaccharide powder is a polysaccharide with a molecular weight of 5-100 kDa obtained by enzymatic hydrolysis-assisted water extraction and membrane separation of the A-flow and B-flow drug residues.
[0007] Preferably, the mass ratio of volatile oil, hydroxypropyl-β-cyclodextrin, and soybean lecithin in the A-flow volatile oil inclusion complex is 1:6:0.5 to 1:10:1, the volatile oil inclusion rate is ≥90%, and the atractylone retention rate is ≥90%.
[0008] Preferably, the total transfer rate of magnolol and honokiol in the B-flow ethanol extract powder is ≥90%, and the retention rate of amygdalin is ≥85%.
[0009] Preferably, the polysaccharide purity in the C-flow polysaccharide dry powder is ≥60%, and the molecular weight distribution of the polysaccharide is concentrated in the range of 10-50 kDa.
[0010] A method for preparing a traditional Chinese medicine composition for improving constipation includes the following steps: Peach kernel pretreatment for enzyme inactivation: After coarse crushing, peach kernels are subjected to steam flash evaporation or microwave inactivation to ensure that lipase activity is ≤0.1 U / mg; Preparation of A-flow: Raw Atractylodes macrocephala and Citrus aurantium were extracted with supercritical CO2 fluid to obtain volatile oil; the volatile oil was then ternarily encapsulated with hydroxypropyl-β-cyclodextrin and soybean lecithin to obtain A-flow volatile oil inclusion complex; Preparation of B-flow: Take the enzyme-inactivated peach kernel, magnolia bark, and prepared licorice root, reflux extract with 70%-80% ethanol, concentrate and dry to obtain B-flow ethanol extract dry powder; C-flow preparation: The residues after A-flow preparation and B-flow preparation are combined, and cellulase and pectinase are added for enzymatic hydrolysis-assisted water extraction. The extract is collected by ultrafiltration membrane to remove polysaccharides with a molecular weight of 5-100 kDa, which are then concentrated and dried to obtain C-flow polysaccharide dry powder. Final mixing and granulation: Mix and granulate the volatile oil inclusion complex (A stream), the ethanol extract dry powder (B stream), and the polysaccharide dry powder (C stream) according to the proportion of raw materials.
[0011] Preferably, when pretreating peach kernels to inactivate enzymes, the conditions for steam flash inactivation are 100-105℃ for 1-3 min, or the conditions for microwave inactivation are 300-600 W for 30-90 s. During A-flow preparation, the supercritical CO2 extraction pressure is 20-25 MPa, the temperature is 40-45℃, the amount of anhydrous ethanol as an entrainer is 2%-4% of the raw material, the ternary inclusion temperature is 30-40℃, and the stirring time is 2-4 h.
[0012] Preferably, during the preparation of B-flow, the ethanol concentration is 75%, 0.1%-0.3% ascorbic acid is added or nitrogen gas is purged for protection, and the extraction is carried out twice under reflux at 60-70℃, each time for 1.5-2 hours.
[0013] Preferably, during the preparation of C-flow, the enzymatic hydrolysis conditions are as follows: pH 5.0-5.5, cellulase dosage 10-20 U / g residue, pectinase dosage 5-15 U / g residue, enzymatic hydrolysis at 45-55℃ for 2-3 h; after enzyme inactivation, water is added and decocted twice; polysaccharides with a molecular weight of 5-100 kDa are collected by ultrafiltration membrane.
[0014] The application of a traditional Chinese medicine composition for improving constipation in the preparation of enteric-coated microcapsules, wherein the enteric-coated microcapsules comprise, from the inside out, a microcapsule core, an immediate-release layer, an enteric coating, and a colon coating; the microcapsule core contains B-stream ethanol extract powder and C-stream polysaccharide powder, and the immediate-release layer contains A-stream volatile oil inclusion complex.
[0015] Application of traditional Chinese medicine compositions or enteric-coated microcapsules in the preparation of drugs for treating slow transit constipation, constipation-predominant irritable bowel syndrome, postoperative ileus, or regulating intestinal flora.
[0016] Therefore, the present invention employs the above-mentioned traditional Chinese medicine composition for improving constipation, its preparation method, and its application, with the following technical effects: By pretreating peach kernels to inactivate enzymes, the retention rate of amygdalin was significantly improved (≥95%), avoiding the hydrolytic loss of glycosides during the extraction process.
[0017] The use of supercritical CO2 extraction combined with hydroxypropyl-β-cyclodextrin-phospholipid ternary inclusion complex not only improved the extraction and inclusion rates of volatile oils, but also significantly improved the solubility, stability and bioavailability of the inclusion complex, with a solubility more than 3 times higher than that of ordinary β-cyclodextrin mono-inclusion complex.
[0018] Membrane separation and fractionation of polysaccharide fractions yielded active polysaccharides with molecular weights of 5-100 kDa, significantly improving polysaccharide purity and gut microbiota regulation activity.
[0019] By designing a three-phase time-release formulation, the A stream of volatile oil is rapidly released in the stomach to exert a prokinetic effect, the B stream is released in the intestine to exert a lubricating and repairing effect, and the C stream is released in the colon to regulate the intestinal flora. The three streams work synergistically to enhance the efficacy, which is significantly better than that of a simple mixed formulation. Attached Figure Description
[0020] Figure 1 This is a performance verification diagram of a traditional Chinese medicine composition for improving constipation with high efficiency retention. Figure 1 (a) in the figure is a schematic diagram showing the results of the retention rate of atractylone in the traditional Chinese medicine composition; Figure 1 (b) in the figure is a schematic diagram showing the results of the transfer rates of magnolol+ and magnolol in the traditional Chinese medicine composition; Figure 1 (c) in the figure is a schematic diagram showing the retention rate of amygdalin in the traditional Chinese medicine composition; Figure 1 (d) in the figure is a schematic diagram showing the polysaccharide yield of the traditional Chinese medicine composition; Figure 1 (e) in the figure is a schematic diagram showing the results of the volatile oil inclusion rate of the traditional Chinese medicine composition; Figure 2 This image shows the effect of a traditional Chinese medicine composition used to improve constipation when used to treat constipation. Figure 2 (a) in the figure is a schematic diagram of the charcoal powder propulsion rate when the traditional Chinese medicine composition is used to treat constipation; Figure 2 (b) in the diagram is a schematic diagram of the time to defecation of the first pill when the traditional Chinese medicine composition is used to treat constipation. Detailed Implementation
[0021] The technical solution of the present invention will be further described below with reference to the accompanying drawings and embodiments.
[0022] Unless otherwise defined, the technical or scientific terms used in this invention shall have the ordinary meaning as understood by one of ordinary skill in the art to which this invention pertains.
[0023] Raw Atractylodes macrocephala is the dried rhizome of Atractylodes macrocephala (Asteraceae family); Citrus aurantium is the dried young fruit of Citrus aurantium (Rutaceae family) and its cultivated varieties; Magnolia officinalis is the dried bark, root bark, and branch bark of Magnolia officinalis (Magnolia officinalis family) or Magnolia officinalis var. ...
[0024] Example 1 A traditional Chinese medicine composition for improving constipation, comprising the following raw materials in the indicated weight proportions: 60 parts raw Atractylodes macrocephala, 12 parts Citrus aurantium, 12 parts Magnolia officinalis, 10 parts Prunus persica, and 6 parts processed Glycyrrhiza uralensis. The composition includes the following steps: Peach kernel pretreatment for enzyme inactivation: Peach kernels were coarsely crushed to 10-20 mesh and then subjected to flash steam inactivation at 105℃ for 2 minutes. After enzyme inactivation, the kernels were dried at low temperature (≤50℃) and then pulverized through an 80-mesh sieve. The lipase activity of the peach kernels after enzyme inactivation was determined to be 0.05 U / mg, and the amygdalin retention rate was 97.2%.
[0025] Preparation by flow A: Raw Atractylodes macrocephala and Citrus aurantium were sliced, dried at 45℃, and pulverized through a 20-mesh sieve. Supercritical CO2 extraction was performed at a pressure of 22 MPa, a temperature of 42℃, a CO2 flow rate of 20 L / h, and an entrainer of anhydrous ethanol at 3% of the raw material, for a extraction time of 2.5 h. The volatile oil was collected, and the atractylone extraction rate was found to be 0.52% (based on crude drug).
[0026] A ternary inclusion complex was formed by combining volatile oil, hydroxypropyl-β-cyclodextrin, and soybean lecithin in a mass ratio of 1:8:0.8. First, soybean lecithin was dissolved in anhydrous ethanol and mixed thoroughly with the volatile oil. This mixture was then slowly added dropwise to a saturated aqueous solution of hydroxypropyl-β-cyclodextrin at 35°C, and stirred at 35°C for 3 hours. The inclusion complex was then freeze-dried to obtain flow A of the volatile oil inclusion complex. The inclusion rate of the volatile oil was determined to be 96.5%, and the retention rate of atractylone in the inclusion complex was 93.6%.
[0027] Preparation of B-stream extract: Take the crude powders of peach kernel, magnolia bark, and prepared licorice root after enzyme inactivation, add 75% ethanol (containing 0.2% ascorbic acid), and reflux at 65℃ twice, 1.5 h each time. Combine the extracts, concentrate under reduced pressure until no alcohol odor remains, centrifuge at high speed, and vacuum dry the supernatant to obtain the B-stream ethanol extract powder. The total transfer rate of magnolol and honokiol was determined to be 94.2%, and the retention rate of amygdalin was 92.8%.
[0028] Preparation of C-flow: The residues from A and B flows were combined, the pH was adjusted to 5.2, and cellulase (15 U / g residue) and pectinase (10 U / g residue) were added. Enzymatic hydrolysis was performed at 50℃ for 2.5 h. After enzyme inactivation, the mixture was decocted twice with water. The extracts were combined, and polysaccharides with molecular weights of 5-100 kDa were collected by ultrafiltration. The polysaccharides were concentrated under reduced pressure and freeze-dried to obtain C-flow polysaccharide powder. The polysaccharide purity was determined to be 63.5%, with the molecular weight distribution mainly concentrated in the 10-50 kDa range.
[0029] Preparation of three-phase time-release enteric-coated microcapsules: The dry powder of polysaccharide in stream C and the dry extract powder of ethanol extract in stream B are mixed in the proportion of raw drugs, and microcrystalline cellulose and cross-linked polyvinyl ketone are added to make microcapsule cores; the volatile oil inclusion complex in stream A is dissolved in an aqueous solution containing binder and sprayed onto the surface of the microcapsule core to form an immediate-release layer; enteric coating (Eudragit L100-55, plasticizer triethyl citrate) is applied until the weight gain is 10%; then colon coating (Eudragit FS30D) is applied until the weight gain is 12%, and then the capsules are filled to obtain enteric-coated microcapsules.
[0030] Release rate determination: The release rate of volatile oil in stream A was 85.4% in 0.1 mol / L hydrochloric acid for 2 h; the release rate of stream B was 78.6% in phosphate buffer at pH 6.8 for 2 h; and the release rate of stream C was 65.2% in medium containing 0.5% pectinase at pH 7.4 for 2 h.
[0031] Efficacy test: In the mouse charcoal propulsion test, the charcoal propulsion rate in the treated group was 84.1%; the time to first defecation was 128 min. This is a significant improvement compared to existing technologies.
[0032] Example 2 Weigh the raw materials according to the following weight ratio: 50 parts of raw Atractylodes macrocephala, 15 parts of Citrus aurantium, 10 parts of Magnolia officinalis, 8 parts of Prunus persica, and 5 parts of processed Glycyrrhiza uralensis.
[0033] Peach kernel pretreatment involved microwave enzyme inactivation: 400 W for 60 s, resulting in a lipase activity of 0.08 U / mg.
[0034] Preparation by A-stream: Supercritical CO2 extraction conditions were 20 MPa pressure, 40℃ temperature, 2% entrainer dosage, and 3 h extraction time. For ternary inclusion, the mass ratio of volatile oil, hydroxypropyl-β-cyclodextrin, and soybean lecithin was 1:6:0.5, the inclusion temperature was 30℃, and the stirring time was 2 h. The inclusion rate of volatile oil was 92.3%, and the retention rate of atractylone was 90.5%.
[0035] B-stream preparation: 70% ethanol was added, and 0.1% ascorbic acid was added. The mixture was refluxed at 60°C twice, 2 hours each time. The total transfer rate of magnolol and honokiol was 91.6%, and the retention rate of amygdalin was 89.3%.
[0036] Preparation by C-flow: Enzymatic hydrolysis was performed at pH 5.0 with 10 U / g cellulase and 5 U / g pectinase on the residue at 45℃ for 2 h; 5-100 kDa polysaccharides were collected by ultrafiltration. The polysaccharide purity was 60.8%.
[0037] Final mixing and granulation: Mix the A-flow inclusion complex, B-flow dry extract powder, and C-flow polysaccharide dry powder according to the proportion of raw materials, and add conventional excipients to make granules.
[0038] Example 3 Weigh the raw materials according to the following weight ratio: 70 parts of raw Atractylodes macrocephala, 10 parts of Citrus aurantium, 15 parts of Magnolia officinalis, 12 parts of Prunus persica, and 8 parts of prepared Glycyrrhiza uralensis.
[0039] Peach kernel pretreatment involved steam flash evaporation to inactivate enzymes: 100℃ for 3 min, resulting in a lipase activity of 0.06 U / mg.
[0040] Preparation by A-stream: Supercritical CO2 extraction pressure 25 MPa, temperature 45℃, entrainer dosage 4%, extraction time 2 h. For ternary inclusion, the mass ratio of volatile oil, hydroxypropyl-β-cyclodextrin, and soybean lecithin was 1:10:1, the inclusion temperature was 40℃, and the stirring time was 4 h. The inclusion rate of volatile oil was 97.1%, and the retention rate of atractylone was 94.8%.
[0041] B-stream preparation: 80% ethanol concentration, nitrogen protection, reflux extraction at 70℃ twice, 1.5 h each time. The total transfer rate of magnolol and honokiol was 93.5%, and the retention rate of amygdalin was 91.2%.
[0042] Preparation by flow filtration: Enzymatic hydrolysis was performed at pH 5.5 with 20 U / g cellulase and 15 U / g pectinase on the residue at 55℃ for 3 h. Polysaccharides with molecular weights of 10-50 kDa (narrower distribution) were collected by ultrafiltration. The polysaccharide purity was 66.2%.
[0043] Formulation: Sustained-release microcapsules were prepared, with the colon coating made of pectin-chitosan, resulting in a 15% increase in weight.
[0044] Example 4 Weigh the raw materials according to the proportions in Example 1.
[0045] Peach kernel pretreatment: Microwave enzyme inactivation at 600 W for 30 s, lipase activity was 0.04 U / mg.
[0046] Preparation by flow A: Supercritical CO2 extraction pressure 24 MPa, temperature 44℃, entrainer dosage 3.5%, extraction time 2.2 h. Ternary inclusion ratio 1:9:0.9, inclusion temperature 38℃, stirring time 3.5 h. Volatile oil inclusion rate 96.8%, atractylone retention rate 94.1%.
[0047] B-stream preparation: Extracted twice with 75% ethanol containing 0.3% ascorbic acid at 68℃, 1.8 h each time. The total transfer rate of magnolol and honokiol was 93.9%, and the retention rate of amygdalin was 92.5%.
[0048] C-flow preparation: Enzymatic hydrolysis at pH 5.3, with 18 U / g cellulase and 12 U / g pectinase in the residue, at 52℃ for 2.8 h; ultrafiltration to collect polysaccharides with molecular weights of 5-100 kDa, with a polysaccharide purity of 64.8%.
[0049] Formulation: Triphasic time-release enteric-coated microcapsules were prepared according to the method in Example 1, with coating weight gains of 8% (enteric coating) and 10% (colonic coating).
[0050] Example 5 The A-flow inclusion complex, B-flow dry extract powder, and C-flow polysaccharide dry powder were prepared according to the formulation and process of Example 1.
[0051] Mix B-flow dry powder and C-flow polysaccharide dry powder to form microcapsule cores; spray A-flow inclusion complex solution to form an immediate-release layer; coat with enteric coating (Eudragit L100-55) until weight gain is 9%; then coat with colon coating (Eudragit FS30D) until weight gain is 13%.
[0052] Release rate: Flow A had a release rate of 88.7% in 0.1 mol / L hydrochloric acid for 2 h; Flow B had a release rate of 81.3% in pH 6.8 buffer for 2 h; Flow C had a release rate of 70.5% in pH 7.4 medium containing 0.5% pectinase for 2 h.
[0053] Comparative Example 1 Weigh out raw Atractylodes macrocephala, Citrus aurantium, Magnolia officinalis, Prunus persica, and Glycyrrhiza uralensis in the same proportions as in Example 1.
[0054] All medicinal materials were mixed and extracted using a dual oil-water extraction method: volatile oil and water-soluble components were extracted by boiling in water. The volatile oil was collected and combined with the water decoction, then concentrated and dried. The peach kernels contained undeactivated enzymes, the volatile oil was not encapsulated, and the polysaccharides were not graded. Simple mixing granulation was used.
[0055] Results: Atractylone retention rate was 40.2%, magnolol and honokiol transfer rate was 68.5%, amygdalin retention rate was 52.1%, and polysaccharide yield was 8.5%. The charcoal powder propulsion rate in mice was 58.3%, and the time to first defecation was 215 min.
[0056] Comparative Example 2 Weigh the raw materials according to the same proportions as in Example 1.
[0057] Following the original fractional extraction scheme, but omitting the peach kernel enzyme inactivation step, the volatile oil in stream A was extracted with hydroxypropyl-β-cyclodextrin mono-inclusion (without phospholipids), stream B was extracted with ethanol, and stream C was extracted with enzymatic hydrolysis and water extraction but without membrane separation and polysaccharide fractionation. The final mixture was simply granulated.
[0058] Results: Uninactivated peach kernel enzymes resulted in a mandelic acid retention rate of only 81.5% in the B-flux; the inclusion rate of mono-inclusion volatile oil was 88.0%, and the retention rate of atractylone was 85.3%; the polysaccharide purity was only 55.2% (ungraded); the charcoal propulsion rate in mice was 72.6%, and the time to first defecation was 162 min.
[0059] Table 1 Comparison of Technical Effects
[0060] From Table 1, Figure 1 and Figure 2 It is evident that the retention rate, inclusion rate, and efficacy indicators of the active ingredients in Examples 1-5 of this invention are significantly better than those in Comparative Examples 1 and 2, demonstrating that this invention has achieved unexpected technical effects through innovative methods such as peach kernel enzyme inactivation, ternary inclusion, polysaccharide fractionation, and three-phase time-sequential release.
[0061] Therefore, the present invention employs the above-mentioned traditional Chinese medicine composition, preparation method and application for improving constipation, which improves the retention rate, stability and bioavailability of active ingredients, and realizes the targeted and timed release of active ingredients in the gastrointestinal tract, thereby significantly enhancing the therapeutic effect.
[0062] 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 preferred embodiments, those skilled in the art should understand that modifications or equivalent substitutions can still be made to the technical solutions of the present invention, and these modifications or equivalent substitutions cannot cause the modified technical solutions to deviate from the spirit and scope of the technical solutions of the present invention.
Claims
1. A traditional Chinese medicine composition for improving constipation, characterized in that, The raw materials include the following parts by weight: 50-70 parts of raw Atractylodes macrocephala, 10-15 parts of Citrus aurantium, 10-15 parts of Magnolia officinalis, 8-12 parts of Prunus persica, and 5-8 parts of processed Glycyrrhiza uralensis. The traditional Chinese medicine composition mainly comprises A stream of volatile oil inclusion complex, B stream of ethanol extract dry powder, and C stream of polysaccharide dry powder; The A-flow volatile oil inclusion complex is a hydroxypropyl-β-cyclodextrin-phospholipid ternary inclusion complex of the volatile oils of raw Atractylodes macrocephala and Citrus aurantium; The B-flow ethanol extract dry powder is a 70%-80% ethanol reflux extract of Magnolia officinalis, enzyme-inactivated peach kernel, and prepared licorice root; the lipase activity of the enzyme-inactivated peach kernel is ≤0.1 U / mg; The C-flow polysaccharide dry powder is a polysaccharide with a molecular weight of 5-100 kDa obtained by enzymatic hydrolysis with cellulase and pectinase-assisted water extraction and membrane separation of the A-flow and B-flow drug residues. During C-flow preparation, the enzymatic hydrolysis conditions are as follows: pH 5.0-5.5, cellulase dosage 10-20 U / g residue, pectinase dosage 5-15 U / g residue, enzymatic hydrolysis at 45-55℃ for 2-3 h; after enzyme inactivation, add water and decoct twice; ultrafiltration membrane is used to retain and collect polysaccharides with a molecular weight of 5-100 kDa.
2. The traditional Chinese medicine composition for improving constipation according to claim 1, characterized in that, The mass ratio of volatile oil, hydroxypropyl-β-cyclodextrin, and soybean lecithin in the A-flow volatile oil inclusion complex is 1:6:0.5 to 1:10:1, the volatile oil inclusion rate is ≥90%, and the atractylone retention rate is ≥90%.
3. The traditional Chinese medicine composition for improving constipation according to claim 1, characterized in that, The total transfer rate of magnolol and honokiol in the B-flow ethanol extract powder is ≥90%, and the retention rate of amygdalin is ≥85%.
4. The traditional Chinese medicine composition for improving constipation according to claim 1, characterized in that, The polysaccharide powder contains ≥60% polysaccharide purity, and the molecular weight distribution of the polysaccharide is concentrated in the range of 10-50 kDa.
5. A method for preparing a traditional Chinese medicine composition for improving constipation according to claim 1, characterized in that, Includes the following steps: Peach kernel pretreatment for enzyme inactivation: After coarse crushing, peach kernels are subjected to steam flash steaming or microwave inactivation. Preparation of A-flow: Raw Atractylodes macrocephala and Citrus aurantium were extracted with supercritical CO2 fluid to obtain volatile oil; the volatile oil was then ternarily encapsulated with hydroxypropyl-β-cyclodextrin and soybean lecithin to obtain A-flow volatile oil inclusion complex; Preparation of B-flow: Take the enzyme-inactivated peach kernel, magnolia bark, and prepared licorice root, reflux extract with 70%-80% ethanol, concentrate and dry to obtain B-flow ethanol extract dry powder; C-flow preparation: The residues after A-flow preparation and B-flow preparation are combined, and cellulase and pectinase are added for enzymatic hydrolysis-assisted water extraction. The extract is collected by ultrafiltration membrane to remove polysaccharides with a molecular weight of 5-100 kDa, which are then concentrated and dried to obtain C-flow polysaccharide dry powder. Final mixing and granulation: Based on the weight parts of the traditional Chinese medicine composition described in claim 1, the A stream volatile oil inclusion complex, the B stream ethanol extract dry powder, and the C stream polysaccharide dry powder are mixed and granulated according to the proportion of raw herbs.
6. A method for preparing a traditional Chinese medicine composition for improving constipation according to claim 5, characterized in that, When pretreating peach kernels to inactivate enzymes, the conditions for steam flash inactivation are 100-105℃ for 1-3 min, or the conditions for microwave inactivation are 300-600 W for 30-90 s. During A-flow preparation, the supercritical CO2 extraction pressure is 20-25 MPa, the temperature is 40-45℃, the amount of anhydrous ethanol as an entrainer is 2%-4% of the raw material, the ternary inclusion temperature is 30-40℃, and the stirring time is 2-4 h.
7. A method for preparing a traditional Chinese medicine composition for improving constipation according to claim 5, characterized in that, For B-stream preparation, the ethanol concentration is 75%, and 0.1%-0.3% ascorbic acid is added or nitrogen gas is purged for protection. The mixture is then refluxed at 60-70℃ for multiple extractions, each lasting 1.5-2 hours.
8. An enteric-coated microcapsule, characterized in that, Made from the traditional Chinese medicine composition of claim 1, the enteric-coated microcapsule comprises, from the inside out, a microcapsule core, an immediate-release layer, an enteric coating, and a colon coating; the microcapsule core contains B-stream ethanol extract dry powder and C-stream polysaccharide dry powder, and the immediate-release layer contains A-stream volatile oil inclusion complex.
9. The use of the traditional Chinese medicine composition according to claim 1 or the enteric-coated microcapsules according to claim 8 in the preparation of drugs for treating slow transit constipation, constipation-predominant irritable bowel syndrome, postoperative ileus, or regulating intestinal flora.
Citation Information
Patent Citations
A Chinese medicine composition for treating constipation, preparation method and application
CN118319990B