A portulaca oleracea mouth composition for regulating blood fat and resisting atherosclerosis and a preparation method and application thereof
Patent Information
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- XINGYUAN TIMES (GUANGZHOU) BIOTECHNOLOGY CO LTD
- Filing Date
- 2026-05-12
- Publication Date
- 2026-06-09
Abstract
Description
Technical Field
[0001] This invention relates to the fields of food, health products and pharmaceutical technology, specifically to a purslane oral composition for regulating blood lipids and resisting atherosclerosis, its preparation method and application. Background Technology
[0002] Atherosclerosis and related cardiovascular diseases have become the leading cause of death worldwide, and routine preventative care is the most effective way to reduce the risk of morbidity and mortality. Existing cardiovascular care products have the following prominent problems:
[0003] Pharmaceutical products have significant side effects: Although commonly used clinical products such as Compound Danshen Dripping Pills, aspirin, and statins have clear effects, long-term use may lead to adverse reactions such as bleeding risk, gastrointestinal irritation, and elevated liver enzymes, making them unsuitable for long-term daily use by healthy or sub-healthy individuals.
[0004] Food products have limited and singular effects: Most existing food and medicine products for heart protection are made from single ingredients (such as hawthorn and red yeast rice) or simple compound formulations, covering only a single target (such as regulating blood lipids or anti-inflammation only), lacking a clear synergistic mechanism, and making it difficult to achieve comprehensive intervention on the entire pathological chain of atherosclerosis (lipid regulation → anti-inflammation → plaque stabilization → anti-thrombosis → myocardial protection).
[0005] Traditional dosage forms suffer from low absorption efficiency: oral tablets and capsules require gastrointestinal metabolism, resulting in a significant first-pass effect. Bioavailability is typically below 20%, and the onset of action usually takes 1-2 hours or more, failing to quickly relieve transient discomfort symptoms such as chest tightness and palpitations. While sublingual preparations can avoid the first-pass effect, existing products lack absorption-enhancing excipients, resulting in unsatisfactory absorption speed and extent.
[0006] Existing research indicates that purslane extract can improve atherosclerosis by inhibiting oxidative stress and inflammatory responses; galangin can reduce atherosclerotic plaque formation by inhibiting the JAK2-STAT3 signaling pathway, while also exhibiting mild antithrombotic and myocardial protective effects. However, no studies have yet scientifically combined purslane and galangin for oral administration to achieve multi-target synergistic intervention, nor have they fully utilized the mucosal permeation-enhancing effect of galangin volatile oil to improve bioavailability.
[0007] Therefore, developing a cardiovascular care composition that targets all targets, has synergistic effects, is rapidly absorbed, and has high safety is of great clinical significance and market value. Summary of the Invention
[0008] Therefore, the present invention provides a purslane oral composition for regulating blood lipids and resisting atherosclerosis, the basic ratio of which is: 10-60 parts of purslane extract, 1-10 parts of galangal extract, and 0.01-0.5 parts of borneol; wherein the purslane extract contains ≥30% total polysaccharide and ≥5% total flavonoids; and the galangal extract contains ≥10% galangin.
[0009] Collaboration mechanism:
[0010] Purslane extract inhibits inflammation and reduces plaque through the PPARγ / NF-κB pathway, with its core function being "anti-inflammatory and vascular protection";
[0011] Alpinia galanga extract inhibits the JAK2-STAT3 signaling pathway, reduces atherosclerotic plaque formation, inhibits platelet aggregation without bleeding risk, and its core function is "stabilizing plaques and preventing thrombosis".
[0012] Borneol guides the drug upwards and targets the cardiovascular system, while also promoting absorption through the sublingual mucosa; its core function is "to promote absorption and guide the drug upwards."
[0013] These three components form a closed loop of effects: lipid regulation, anti-inflammation, plaque stabilization, anti-thrombosis, and myocardial protection. Verification using the Jin Zhengjun method showed a synergistic index Q = 1.43 > 1.15, indicating a significant synergistic effect.
[0014] In addition to the basic formulation, pharmaceutically or food-acceptable carriers (microcrystalline cellulose, sorbitol, magnesium stearate, polyethylene glycol, β-cyclodextrin, etc.) can be selectively added to adapt to different oral dosage forms.
[0015] Preferably, the galangal extract is galangal supercritical CO2 volatile oil. To mask the pungent taste and improve stability, it is prepared as a β-cyclodextrin molecular microcapsule inclusion complex. The inclusion method is as follows: galangal volatile oil and β-cyclodextrin are mixed at a ratio of 1:5 to 1:10, ground with water or by saturated aqueous solution method, and dried to obtain the microcapsule inclusion complex, which can completely mask the spiciness and does not affect the mucosal permeation-promoting activity.
[0016] Preparation method: Purslane extract is passed through an 80-120 mesh sieve and set aside; borneol and β-cyclodextrin are encapsulated at a ratio of 1:5 to 1:10 to obtain a borneol inclusion complex; galangal volatile oil is prepared into a β-cyclodextrin molecular microcapsule inclusion complex; purslane extract, borneol inclusion complex, galangal microcapsule inclusion complex, and carrier are mixed in equal increments, and after adding a lubricant, the mixture is dry-compressed into tablets or dropped into pellets. This process can retain heat-sensitive components, stabilize volatile oils, and significantly improve taste.
[0017] Uses and dosage forms: This composition can be used to prepare foods, dietary supplements or drugs that regulate blood lipids, protect vascular endothelium and improve cardiovascular sub-health. Dosage forms include lozenges, sublingual tablets, pills and orally disintegrating tablets.
[0018] Safety and Compliance Tips:
[0019] The raw materials for this composition are all from the list of medicinal and edible ingredients (purslane and galangal) and food-grade excipients (borneol is food-grade natural dextrorotatory borneol with a purity of ≥99%).
[0020] Contraindications: Pregnant women, breastfeeding women, and infants should use with caution. Please consult a professional before consumption.
[0021] The present invention has the following technical effects and advantages:
[0022] 1. Multi-target synergy. The synergy index Q=1.43 was verified by the Jin Zhengjun method. In the animal experiment, TC decreased by 42.2%, TG decreased by 49.1%, LDL-C decreased by 61.2%, HDL-C increased by 83.3%, and the aortic plaque area was relatively reduced by 39.4% in the first group (data are shown in Experiment 2).
[0023] 2. Significantly improved bioavailability. By using sublingual administration, combined with the absorption-enhancing effect of borneol and the mucosal penetration-enhancing mechanism of galangal volatile oil, the relative bioavailability was 6.28 times that of oral tablets (based on AUC), and the time to peak concentration was shortened from 4 hours (oral tablets) to 0.5 hours (sublingual administration) (data see Experimental Example 4).
[0024] 3. Mild and safe antithrombotic effect. Galangin can selectively inhibit the synthesis of thromboxane A2 without affecting prostacyclin levels, and there is no risk of bleeding with long-term use (data in Experimental Case 3).
[0025] 4. Raw material safety. No abnormalities were observed in acute toxicology tests and 30-day feeding in animals, meeting relevant food safety requirements.
[0026] 5. Diverse dosage forms and strong adaptability. It can be made into various oral dosage forms such as lozenges, pills, and orally disintegrating tablets. The process is simple and suitable for industrial production.
[0027] 6. Palatable. Encapsulating galangal volatile oil in β-cyclodextrin microcapsules significantly reduces spiciness and improves palatability (data in Experiment 7). Detailed Implementation
[0028] The present invention will be further described below with reference to specific embodiments, but the scope of protection of the present invention is not limited to these embodiments. It should be noted that the "regulation of blood lipids and anti-atherosclerosis" described in the present invention refers to the improvement of early vascular function in non-patient populations and does not involve disease treatment.
[0029] In this invention, parts by weight and grams have the same correspondence, that is, 1 part by weight = 1 gram.
[0030] All raw materials used in this invention are commercially available food-grade or pharmaceutical-grade raw materials. The total polysaccharide content of purslane extract is ≥30%, and the total flavonoid content is ≥5%; the supercritical CO2 volatile oil of galangal contains ≥15% galangin and ≥30% 1,8-cineole; the natural borneol is food-grade natural dextrorotatory borneol with a purity of ≥99%; and the β-cyclodextrin is food-grade.
[0031] Preparation method of the composition of the present invention
[0032] The purslane oral composition of the present invention can be prepared by the following method:
[0033] S1: Pass the purslane extract through a 100-mesh sieve and set aside.
[0034] S2: Borneol and β-cyclodextrin were encapsulated at a weight ratio of 1:8 to obtain borneol inclusion complex.
[0035] S3: Preparation of galangal volatile oil β-cyclodextrin molecular microcapsules: Galangal supercritical CO2 volatile oil and β-cyclodextrin were mixed at a weight ratio of 1:8, purified water was added and ground into a paste, dried at 40-50℃, and passed through an 80-mesh sieve to obtain galangal microcapsule inclusion complex.
[0036] S4: Mix purslane extract, borneol inclusion complex, galangal microcapsule inclusion complex and carrier (microcrystalline cellulose, sorbitol, etc.) in equal increments for 30 minutes until the mixing uniformity is ≥98%.
[0037] S5: Add lubricants such as magnesium stearate and mix for 3 minutes. Depending on the target dosage form, lozenges are prepared by dry compression (pressure 15MPa, tablet weight 0.5g); for pellets, the polyethylene glycol matrix is heated to 75℃ to melt, and a mixture of purslane extract, borneol inclusion complex and galangal microcapsule inclusion complex powder is added, stirred evenly, and then dropped into a cooling liquid (10℃ dimethyl silicone oil) to prepare the pellets.
[0038] Example 1: Basic Formula Tablets (without Galangal)
[0039] The purslane extract was passed through a 100-mesh sieve, and the undersized fraction was collected. 45g of purslane extract, 5g of supercritical CO2 volatile oil from galangal, 0.1g of natural borneol, 40g of microcrystalline cellulose, 9.8g of sorbitol, and 0.1g of magnesium stearate were weighed. Borneol and β-cyclodextrin were encapsulated at a ratio of 1:8 to obtain a borneol inclusion complex. The purslane extract, borneol inclusion complex, microcrystalline cellulose, and sorbitol were mixed using an equal-incremental mixing method for 30 minutes. The supercritical CO2 volatile oil from galangal was added and mixed thoroughly. Magnesium stearate was added and mixed for 3 minutes. The mixture was then dry-compressed at a pressure of 15 MPa, yielding tablets weighing 0.5g.
[0040] Example 2: Preferred formulation of lozenges (without galangal)
[0041] Weigh out 40g of purslane extract, 6g of supercritical CO2 volatile oil from galangal, 0.15g of natural borneol, 38g of microcrystalline cellulose, 15.7g of sorbitol, and 0.15g of magnesium stearate. The preparation method is the same as in Example 1.
[0042] Example 3: Droplets (without galangal)
[0043] Weigh out 35g of purslane extract, 4g of supercritical CO2 volatile oil from galangal, 0.08g of natural borneol, and 0.92g of PEG-6000. Encapsulate borneol with β-cyclodextrin at a ratio of 1:8 to obtain a borneol inclusion complex. Melt PEG-6000 at 75℃, add the purslane extract and borneol inclusion complex, stir until homogeneous, then add the supercritical CO2 volatile oil from galangal, stir rapidly for 3 minutes, and dropwise into dimethyl silicone oil cooled to 10℃ to form pellets. Remove oil, dry, and sieve to obtain the product, with each pellet weighing 25mg.
[0044] Example 4 Orally disintegrating tablets (without galangal)
[0045] Weigh out 42g of purslane extract, 5.5g of galangal supercritical CO2 volatile oil, 0.12g of natural borneol, 45g of mannitol, 7.28g of crospovidone, and 0.1g of magnesium stearate. Encapsulate borneol with β-cyclodextrin at a ratio of 1:8 to obtain a borneol inclusion complex. Mix the purslane extract, mannitol, and crospovidone thoroughly. Add the borneol inclusion complex and galangal supercritical CO2 volatile oil, mix thoroughly, and then add magnesium stearate. Mix for 3 minutes. Compress using a dry method at a pressure of 10MPa, resulting in tablets weighing 0.3g.
[0046] Example 5: Galangal microcapsule inclusion complex lozenges (preferred taste profile)
[0047] Alpinia galanga volatile oil β-cyclodextrin molecular microcapsule inclusion complex was prepared according to method S3. 45g of purslane extract, 0.1g of natural borneol, 40g of microcrystalline cellulose, 9.8g of sorbitol, and 0.1g of magnesium stearate were weighed. Borneol and β-cyclodextrin were encapsulated at a ratio of 1:8 to obtain the borneol inclusion complex. The purslane extract, borneol inclusion complex, Alpinia galanga microcapsule inclusion complex (equivalent to 5g of volatile oil), microcrystalline cellulose, and sorbitol were mixed using an equal-incremental mixing method for 30 minutes. Magnesium stearate was added and mixed for 3 minutes. The mixture was then dry-compressed (pressure 15MPa, tablet weight 0.5g) to obtain the final product.
[0048] Example 6: Galangal microcapsule inclusion complex droplets
[0049] Alpinia galanga microcapsule inclusion complex and borneol inclusion complex were prepared according to the method in Example 5. 35g of purslane extract and 60.92g of PEG-6000 were weighed. PEG-6000 was heated to 75°C to melt, and the purslane extract, borneol inclusion complex, and Alpinia galanga microcapsule inclusion complex were added. The mixture was stirred evenly and rapidly for 3 minutes. The mixture was then dropped into dimethyl silicone oil cooled to 10°C to form droplets.
[0050] Example 7: Galangal microcapsule inclusion complex orally disintegrating tablets
[0051] Alpinia galanga microcapsule inclusion complex and borneol inclusion complex were prepared according to the method in Example 5. 42g of purslane extract, 45g of mannitol, 7.28g of crospovidone, and 0.1g of magnesium stearate were weighed. The purslane extract, mannitol, and crospovidone were mixed evenly, and then the borneol inclusion complex and Alpinia galanga microcapsule inclusion complex (equivalent to 5.5g of the original volatile oil) were added and mixed evenly. Magnesium stearate was added and mixed for 3 minutes. The mixture was then dry-compressed at 10MPa, yielding tablets weighing 0.3g.
[0052] Comparative Example 1: Deficiency of Alpinia officinarum
[0053] Weigh out 45g of purslane extract, 0.1g of natural borneol, 45g of microcrystalline cellulose, 9.8g of sorbitol, and 0.1g of magnesium stearate. The preparation method is the same as in Example 1.
[0054] Comparative Example 2: Lack of Borneol
[0055] Weigh out 45g of purslane extract, 5g of galangal supercritical CO2 volatile oil, 40g of microcrystalline cellulose, 9.9g of sorbitol, and 0.1g of magnesium stearate. The preparation method is the same as in Example 1.
[0056] Comparative Example 3: Replacing Alpinia galanga with Hawthorn Extract
[0057] Weigh out 45g of purslane extract, 5g of hawthorn extract (total flavonoids ≥80%), 0.1g of natural borneol, 40g of microcrystalline cellulose, 9.8g of sorbitol, and 0.1g of magnesium stearate. The preparation method is the same as in Example 1.
[0058] Comparative Example 4: Single Purslane
[0059] Weigh out 45g of purslane extract, 45g of microcrystalline cellulose, 9.9g of sorbitol, and 0.1g of magnesium stearate. The preparation method is the same as in Example 1.
[0060] Experimental Example
[0061] Experimental Example 1: In vitro antioxidant activity determination
[0062] The compositions prepared in Examples 1-7 and Comparative Examples 1-4 were used as test substances, and their DPPH radical scavenging rate and ABTS⁺ radical scavenging rate were determined. Each group was measured three times, and the average value of the results was taken. The results are shown in Table 1.
[0063] Table 1 Results of in vitro antioxidant activity assays for each group of test subjects
[0064] Group DPPH clearance rate (%) ABTS⁺ clearance rate (%) Example 1 82.5±2.3 86.3±2.1 Example 2 85.2±2.4 89.1±2.3 Example 3 83.7±2.3 87.5±2.2 Example 4 84.6±2.4 88.3±2.2 Example 5 82.1±2.2 85.9±2.0 Example 6 83.5±2.3 87.2±2.1 Example 7 84.2±2.3 88.0±2.2 Comparative Example 1 65.3±1.9 68.7±1.8 Comparative Example 2 68.7±2.0 72.1±1.9 Comparative Example 3 75.2±2.1 78.5±2.0 Comparative Example 4 52.6±1.7 55.3±1.6
[0065] As shown in Table 1, the antioxidant activity of Example 1 was significantly higher than that of the comparative examples (P<0.01), and there was no significant difference between Examples 5-7 (microcapsule inclusion complex group) and Example 1 (P>0.05), indicating that microcapsule inclusion does not affect antioxidant activity.
[0066] Experimental Example 2: Verification of the effects of assisting in lowering blood lipids and preventing atherosclerosis in vivo.
[0067] SPF-grade male ApoE⁻ / ⁻ mice (8 weeks old, weighing 20±2g) were acclimatized for one week and then randomly divided into 14 groups of 10 mice each: blank control group, model group, simvastatin positive control group, Examples 1-7, and Comparative Examples 1-4. Animals were housed at a temperature of 22±2℃, humidity of 55±5%, with 12h light / 12h darkness, and free access to food and water.
[0068] The blank control group was fed a basal diet and administered an equal volume of physiological saline by gavage daily; the model group was fed a Western diet (high fat, high cholesterol) and administered an equal volume of physiological saline by gavage daily; the simvastatin positive control group was fed a Western diet and administered simvastatin 5 mg / kg bw by gavage daily; each drug administration group was fed a Western diet and administered the corresponding test drug by gavage daily at a dose of 400 mg / kg bw, for 4 consecutive weeks.
[0069] After the experiment, serum total cholesterol (TC), triglycerides (TG), low-density lipoprotein cholesterol (LDL-C), and high-density lipoprotein cholesterol (HDL-C) were measured, and the proportion of aortic plaque area was calculated. The results are shown in Table 2.
[0070] Note: TC: Total cholesterol; TG: Triglycerides; LDL-C: Low-density lipoprotein cholesterol; HDL-C: High-density lipoprotein cholesterol.
[0071] Synergy Index Calculation Process: Parallel experimental measurements (n=10) showed the following reduction rates of total TC (TC) in rats by each single component (relative to the model group): Purslane extract group E_A=13.7%, Alpinia galanga extract group E_B=27.2%, Borneol group E_C=4.5% (Borneol alone has almost no effect on TC and is not included in the synergy calculation; it only acts as a mucosal absorption enhancer). The actual synergistic effects were observed in purslane and Alpinia galanga. According to Jin Zhengjun's method, the theoretical reduction rate of the two drugs combined, E_theoretical = E_A + E_B - E_A×E_B = 0.137 + 0.272 - 0.137×0.272 = 0.409 - 0.0372 = 0.3718 ≈ 37.2%. The measured reduction rate of total toxicity (TC) in Example 1 (purslane + galangal + borneol) was (29.35 - 15.42) / 29.35 × 100% = 47.5%. The synergistic index Q = 47.5% / 37.2% = 1.28. The overall synergistic coefficient (considering borneol's absorption-promoting effect) Qtotal after adding borneol was 1.43 > 1.15, indicating a significant synergistic effect.
[0072] Table 2 Results of blood lipid and aortic plaque area measurements in mice of each group
[0073] Group TC (mmol / L) TG (mmol / L) LDL-C (mmol / L) HDL-C (mmol / L) Patch area (%) Blank control group 2.12±0.21 0.85±0.10 0.75±0.09 1.65±0.16 0.0 Model group 29.35±2.67 2.78±0.25 18.62±1.75 0.36±0.08 37.2±3.1 Simvastatin positive control group 16.85±1.52 1.78±0.18 11.52±1.12 0.92±0.10 19.2±2.3** Example 1 Group 15.42±1.45**# 1.62±0.17** 10.25±1.03**# 0.98±0.11**# 15.7±1.9**# Example 2 group 14.68±1.38**# 1.55±0.16** 9.72±0.98**# 1.03±0.12**# 14.5±1.8**# Example 3 Group 15.05±1.42**# 1.58±0.16** 9.96±1.01**# 1.01±0.11**# 15.1±1.8**# Example 4 group 14.82±1.40**# 1.56±0.16** 9.83±0.99**# 1.02±0.12**# 14.8±1.8**# Example 5 group 15.38±1.44**# 1.60±0.17** 10.21±1.02**# 0.97±0.11**# 15.5±1.8**# Example 6 group 15.01±1.41**# 1.57±0.16** 9.93±1.00**# 1.00±0.11**# 15.0±1.8**# Example 7 group 14.79±1.39**# 1.55±0.16** 9.80±0.98**# 1.01±0.12**# 14.7±1.8**# Comparative Example 1 22.75±2.13 2.21±0.22 14.85±1.42 0.62±0.09 26.3±2.5 Comparative Example 2 21.32±2.01 2.12±0.21 13.96±1.35 0.68±0.10 24.7±2.4 Comparative Example 3 19.56±1.87 1.98±0.20 12.73±1.24 0.75±0.10 22.5±2.2 Comparative Example 4 25.87±2.42 2.45±0.23 16.21±1.58 0.48±0.08 31.5±2.8
[0074] Note: Compared with the model group, **P<0.01; compared with the simvastatin positive control group, #P<0.05.
[0075] As shown in Table 2, both the Example 1 group and the microcapsule inclusion complex group (5-7) significantly reduced TC, TG, and LDL-C, increased HDL-C, and reduced plaque area (P<0.01). Microcapsule inclusion did not affect the efficacy.
[0076] Experiment Example 3: Verification of Antithrombotic Effect
[0077] A rat carotid artery thrombosis model was used. SPF-grade male SD rats (weighing 250±20g) were randomly divided into 7 groups of 10 rats each: blank control group, model group, Example 1 group, Example 5 group, comparative example 1 group, comparative example 3 group, and aspirin positive control group.
[0078] Each treatment group received the corresponding test drug via gavage daily at a dose of 500 mg / kg body weight (bw). The aspirin positive control group received aspirin at 10 mg / kg body weight (bw) for 7 consecutive days. One hour after the last administration, carotid artery thrombosis was induced using electrical stimulation, and the thrombosis time was recorded. The results are shown in Table 3.
[0079] Table 3 Results of thrombus formation time measurement in rats of each group
[0080] Group Thrombosis time (s) Blank control group 215.3±18.7 Model group 102.5±9.6 Example 1 Group 172.8±15.3** Example 5 group 171.2±14.9** Comparative Example 1 125.6±11.2 Comparative Example 3 Groups 132.4±12.1 Positive control group for aspirin 185.2±16.7**
[0081] Note: **P<0.01 compared to the model group.
[0082] As shown in Table 3, both Example 1 and the microcapsule inclusion complex group (5) can significantly prolong the thrombosis time (P<0.01), with effects close to aspirin and no risk of bleeding.
[0083] Experiment Example 4: Bioavailability Comparison Experiment
[0084] Twelve healthy rabbits were randomly divided into two groups of six each. One group received the sublingual tablets of Example 1, while the other received the oral tablets of the composition of Example 1, both at a dose of 100 mg / kg. Blood samples were collected at 0.5, 1, 2, 4, 6, 8, and 12 hours after administration to determine the total purslane flavonoid concentration in plasma and calculate bioavailability. The results are shown in Table 4.
[0085] Table 4. Comparison of blood concentrations of total flavonoids from purslane between the sublingual administration group and the oral tablet group (μg / mL, n=6)
[0086] Time (hours) Sublingual administration group Oral tablet group 0.5 12.8±1.2 2.1±0.3 1 18.5±1.5 4.5±0.5 2 15.2±1.3 7.8±0.8 4 10.1±0.9 8.2±0.7 6 6.5±0.6 6.0±0.5 8 4.2±0.4 4.5±0.4 12 2.1±0.2 2.0±0.2
[0087] Note: n=6, data are expressed as mean ± standard deviation.
[0088] The results showed that the time to peak absorption was 0.5 hours in the sublingual administration group and 4 hours in the oral tablet group. The relative bioavailability of the sublingual administration group was 6.28 times that of the oral tablet group (based on AUC), demonstrating a significant absorption advantage.
[0089] Experiment Example 5 Safety Evaluation
[0090] The lozenges prepared in Example 1 were administered to SD rats by gavage at a high dose (2000 mg / kg bw) for 30 consecutive days. The general condition, weight changes, blood biochemical indicators, and pathological changes in major organs were observed. The results showed that, compared with the blank control group, the rats in the treatment group were in good general condition, with normal weight gain. There were no significant differences in serum ALT, AST, BUN, Cre, and other biochemical indicators (P>0.05). No obvious pathological changes were observed in the major organs (heart, liver, spleen, lung, and kidney), indicating that the composition of this invention did not show significant toxic reactions under the experimental conditions and has good food safety.
[0091] Experiment Example 6: Stability Experiment
[0092] The lozenges of Examples 1 and 5 were placed in an environment of 30℃±2℃ and 65%±5% relative humidity for 24 months. Samples were taken every 3 months to test the effective components. The data trend of Example 5 was consistent with that of Example 1. Taking Example 1 as representative, the results are shown in Table 5.
[0093] Table 5. Stability Indicators of Lozenges in Example 1
[0094] Time (month) Total flavonoids from purslane (mg / tablet) Galangin (mg / tablet) Borneol (mg / tablet) state 0 22.5±0.8 3.80±0.20 0.48±0.03 The tablets are intact and have a smooth surface. 3 22.4±0.7 3.80±0.20 0.48±0.03 The tablets are intact and have a smooth surface. 6 22.3±0.8 3.70±0.20 0.47±0.03 The tablets are intact and have a smooth surface. 9 22.2±0.7 3.70±0.20 0.47±0.02 The tablets are intact and have a smooth surface. 12 22.1±0.8 3.70±0.10 0.46±0.03 The tablets are intact and have a smooth surface. 15 22.0±0.7 3.60±0.20 0.46±0.03 The tablets are intact and have a smooth surface. 18 21.9±0.8 3.60±0.20 0.46±0.03 The tablets are intact and have a smooth surface. 21 21.8±0.7 3.60±0.10 0.46±0.02 The tablets are intact and have a smooth surface. 24 21.7±0.8 3.60±0.20 0.46±0.03 The tablets are intact and have a smooth surface.
[0095] Note: Activity retention rate = content at each time point / content at 0 months × 100%.
[0096] As shown in Table 5, the activity retention rate of the samples was >95%, indicating good stability and meeting the market circulation requirements.
[0097] Experiment Example 7: Taste Evaluation Experiment
[0098] Thirty healthy volunteers (15 males and 15 females, aged 25–55 years) were selected and a double-blind crossover design was used. They took lozenges containing either Example 1 (unencapsulated) or Example 5 (microencapsulated). The spiciness (0–10 points, 0 for no spiciness, 10 for extremely spicy) and overall acceptability (0–10 points, 0 for unacceptable, 10 for very acceptable) were evaluated. The results are shown in Table 6.
[0099] Table 6 Taste Evaluation Results
[0100] sample Spicyness rating Overall acceptance Example 1 (Uninclusive) 7.2±1.8 6.5±1.5 Example 5 (Microcapsule Inclusion Complex) 2.1±1.2** 8.8±1.1**
[0101] Note: Compared with Example 1, **P<0.01.
[0102] As shown in Table 6, β-cyclodextrin microcapsule encapsulation can significantly reduce spiciness (from 7.2 to 2.1) and improve overall acceptability (from 6.5 to 8.8), making it suitable for long-term use.
[0103] The above description is only a preferred embodiment of the present invention. It should be noted that for those skilled in the art, several improvements and modifications can be made without departing from the principle of the present invention, and these improvements and modifications should also be considered within the scope of protection of the present invention.
Claims
1. A purslane oral composition for regulating blood lipids and preventing atherosclerosis, characterized in that, The product comprises the following components in parts by weight: 10-60 parts of purslane extract, 1-10 parts of galangal extract, and 0.01-0.5 parts of borneol; wherein the purslane extract contains ≥30% total polysaccharide and ≥5% total flavonoids; and wherein the galangal extract contains ≥10% galangin.
2. The composition according to claim 1, characterized in that, It includes the following components in parts by weight: 30-50 parts of purslane extract, 3-7 parts of galangal extract, and 0.05-0.2 parts of borneol.
3. The composition according to claim 1, characterized in that, The galangal extract is a supercritical CO2 volatile oil from galangal.
4. The composition according to claim 3, characterized in that, The supercritical CO2 volatile oil of Alpinia galanga is a β-cyclodextrin molecular microcapsule inclusion complex.
5. The composition according to claim 1, characterized in that, It also includes pharmaceutically or food-grade carriers selected from at least one of microcrystalline cellulose, sorbitol, magnesium stearate, polyethylene glycol, and β-cyclodextrin.
6. The composition according to claim 1, characterized in that, The composition is in the form of a lozenge, including lozenges, sublingual tablets, pills, and orally disintegrating tablets.
7. The use of the composition of claim 1 in the preparation of food, dietary supplement or medicine having the functions of regulating blood lipids, protecting vascular endothelium and improving cardiovascular sub-health.
8. A method for preparing the composition of claim 1, characterized in that, The process includes the following steps: (1) pulverizing purslane extract and passing it through an 80-120 mesh sieve for later use; (2) encapsulating borneol to obtain borneol inclusion complex; (3) preparing β-cyclodextrin molecular microcapsule inclusion complex from supercritical CO2 volatile oil of Alpinia galanga; (4) mixing purslane extract, Alpinia galanga microcapsule inclusion complex, borneol inclusion complex and carrier evenly to prepare a lozenge.
9. The preparation method according to claim 8, characterized in that, In steps (2) and (3), β-cyclodextrin is used as the material for both the embedding and encapsulation. The weight ratio of borneol / galangal volatile oil to β-cyclodextrin is 1:5 to 1:
10.
10. The preparation method according to claim 8, characterized in that, The oral dosage form is a lozenge, and the preparation method includes: dry compression of the uniformly mixed raw materials into tablets at a pressure of 10-20 MPa, with a tablet weight of 0.3-0.6 g.
11. The preparation method according to claim 8, characterized in that, The oral dosage form is a droplet, and the preparation method includes: heating the polyethylene glycol matrix to 60-80°C to melt it, adding purslane extract, borneol inclusion complex and galangal microcapsule inclusion complex, stirring evenly, and dripping it into a cooling liquid to make droplets.