Blood stasis dispersing and stagnation eliminating health care cream and preparation method thereof

Abstract

The invention discloses a blood stasis dispersing and stagnation eliminating health care cream and a preparation method thereof. The blood stasis dispersing and stagnation eliminating health care cream is composed of active components such as safflower general flavone, frankincense-myrrh co-extract and pericarpium citri reticulatae volatile oil and an emulsion matrix. Targeted delivery and long-acting release of blood activating components are achieved through a supercritical combined extraction-micro-capsule wrapping-gradient emulsification technology, the effects of remarkably reducing the size and improving the hardness on qi and blood stasis type nodules are achieved, and the transdermal efficiency is improved by 180% compared with that of a traditional ointment.

Description

Technical Field

[0001] The present invention belongs to the technical field of traditional Chinese medicine external preparations, and specifically relates to a compound cream based on multi-channel synergistic action and its preparation process, which is applicable to improving sub-health symptoms such as local swelling and pain caused by qi and blood stasis and nodular hyperplasia. Background Art

[0002] Modern people generally have problems of qi and blood stasis caused by sedentary lifestyle, cold body constitution, etc. Most existing external medicines use a single blood-activating ingredient (such as ordinary safflower oil), which has defects such as a single action target and insufficient deep penetration. The traditional plaster preparation process is likely to cause loss of volatile components (such as the high-temperature inactivation rate of frankincense and myrrh > 40%). The present invention realizes the synergistic effect and targeted slow release of multiple components through innovative low-temperature extraction and microcapsule encapsulation technology. Summary of the Invention

[0003] Technical Problem

[0004] Provide an external preparation with both rapid stasis-removing and long-term nodule-eliminating functions, and solve the technical bottlenecks of low transdermal efficiency and easy degradation of active ingredients in traditional preparations.

[0005] Technical Solution

[0006] 1. Composition of raw materials (by mass percentage):

[0007] Blood-activating group (12 - 20%):

[0008] Total safflower flavonoids 3 - 6%, notoginsenoside 2 - 5%, ligustrazine extract 2 - 4%

[0009] Nodule-dissipating group (8 - 15%):

[0010] Frankincense - myrrh co-extract 3 - 7%, ginseng polysaccharide 2 - 5%

[0011] Qi-regulating group (6 - 12%):

[0012] Volatile oil of dried tangerine peel 2 - 4%, hesperidin of fructus aurantii 1 - 3%, gingerol 1 - 2%

[0013] Collateral-unblocking group (5 - 10%):

[0014] Fencholene 1 - 3%, tetrahydroxylene of cyperus rotundus 1 - 2%, costunolide 1 - 2%

[0015] Matrix excipients (55 - 70%):

[0016] Glycerol monostearate and distearate 15 - 20%, potassium sorbate 0.2 - 0.5%, purified water as the balance.

[0017] 2. Preparation method:

[0018] a. Preparation of active ingredients:

[0019] Boswellia - Myrrh co - extract: Supercritical CO 2 co - extraction technology (pressure 28 MPa, temperature 42 °C) is adopted.

[0020] Low - temperature ethanol extract: Safflower and Notoginseng are extracted by dynamic counter - current extraction with 50% ethanol (flow rate 1.5 mL / min)

[0021] Volatile oil components: Tangerine peel, Fructus Aurantii and Aucklandia lappa are extracted by steam - microwave synergistic extraction (power 400 W).

[0022] b. Microencapsulation treatment:

[0023] Thermosensitive components (tetramethylpyrazine, gingerol) are encapsulated with sodium alginate - chitosan microcapsules (encapsulation efficiency ≥ 92%).

[0024] c. Emulsion system construction:

[0025] Oil phase: Glycerol monostearate and distearate, Boswellia - Myrrh co - extract are mixed and heated to 60 °C.

[0026] Aqueous phase: Ginseng polysaccharide and potassium sorbate are dissolved in purified water and heated to 60 °C.

[0027] Gradient emulsification: The aqueous phase is injected into the oil phase at a rate of 1.5 mL / s, and simultaneously high - shear homogenization is carried out at 10000 rpm.

[0028] d. Low - temperature filling: The microencapsulated components are added at 45 °C and aseptically filled into light - proof aluminum tubes.

[0029] Beneficial effects

[0030] 1. Four - dimensional synergistic mechanism:

[0031] Total flavonoids of safflower inhibit platelet aggregation (inhibition rate of ADP - induced is 83.6%).

[0032] Boswellia - Myrrh co - extract down - regulates the expression of TNF - α (decrease by 56.4%).

[0033] Microencapsulated tetramethylpyrazine realizes sustained release (cumulative release rate in 8 hours is 89.2%).

[0034] Volatile oil of tangerine peel enhances transdermal penetration (the in vitro skin penetration coefficient is increased by 2.3 times).

[0035] 2. Clinical data:

[0036] 150 patients with thyroid nodules apply externally 2 times a day. After 12 weeks:

[0037] Those with a reduction in nodule volume of ≥ 30% account for 63.8%

[0038] The hardness score (SWE value) decreased by 41.5%. Description of the Drawings

[0039] Figure 1 It is a process flow chart of a health cream for promoting blood circulation to remove stasis and dissipating nodules. Detailed Implementation Modes

[0040] Example 1

[0041] Raw material ratio (total mass 1000 g):

[0042] Blood-activating group: 50 g of total flavonoids of safflower, 30 g of notoginsenoside, 20 g of ligustrazine extract

[0043] Nodule-dissipating group: 60 g of co-extract of frankincense and myrrh, 40 g of ginseng polysaccharide

[0044] Qi-regulating group: 30 g of volatile oil of dried tangerine peel, 20 g of hesperidin of fructus aurantii, 15 g of gingerol

[0045] Collateral-unblocking group: 25 g of fenchylene, 15 g of tetrahydroaromatic hydrocarbon of cyperus rotundus, 10 g of costunolide

[0046] Matrix excipients: 180 g of glyceryl monostearate and distearate, 4 g of potassium sorbate, 521 g of purified water

[0047] Preparation process:

[0048] 1. The co-extract of frankincense and myrrh is purified by molecular distillation (temperature 120 °C, pressure 5 Pa).

[0049] 2. The extracts of safflower and notoginseng are eluted by gradient with macroporous resin (type D101).

[0050] 3. The particle size of microencapsulated ligustrazine is controlled at 150 - 200 nm (drug loading 22.4%).

[0051] 4. The oil phase and the water phase are emulsified by high-shear at 60 °C (10000 rpm, 8 minutes).

[0052] 5. The microencapsulated components are added at 45 °C, and the verification of aseptic packaging shows by transmission electron microscopy that the microcapsule structure is complete and the particle size distribution is uniform (PDI = 0.18).

[0053] Ultrasonic elastography shows that after 8 weeks of use, the Young's modulus value of breast nodules decreased by 39.7 kPa.

Claims

1. A health cream for removing blood stasis and eliminating stagnation, characterized in that It is composed of the following components in percentage by mass: Blood circulation group 12-20%: 3-6% safflower total flavonoids, 2-5% notoginseng saponins, 2-4% ligustrazine extract Dispersing group 8-15%: frankincense-myrrh co-extract 3-7%, ginseng polysaccharide 2-5% Qi-regulating group 6-12%: Tangerine peel volatile oil 2-4%, Citrus aurantium flavonoids 1-3%, dried gingerol 1-2% Tongluo group 5-10%: fennel 1-3%, cypermethrin 1-2%, costusroot lactone 1-2% Matrix excipients 55-70%: mono- and distearic acid glyceryl 15-20%, potassium sorbate 0.2-0.5%, and the balance purified water.

2. The health cream according to claim 1, characterized in that The ligustrazine extract is encapsulated by sodium alginate-chitosan microcapsules, with an encapsulation rate of ≥90% and a particle size of ≤200nm.

3. The health cream according to claim 1, characterized in that The preferred ratio of active components is: 5% total flavonoids of safflower, 3% notoginseng saponins, 2% ligustrazine extract, 6% frankincense-comyrrha co-extract, 4% ginseng polysaccharide, 3% volatile oil of tangerine peel, 2% flavonoids of fructus aurantii, 1.5% gingerol, 2.5% fennel, 1.5% tetrasaccharide of cyperus rotundus, and 1% costus lactone.

4. A method for preparing the health-care cream for removing blood stasis and eliminating stagnation according to any one of claims 1 to 3, characterized in that The following steps are involved: a. Preparation of Frankincense-Myrrh Co-extract by Supercritical CO2 Extraction b. Dynamic countercurrent extraction of active ingredients from safflower and Panax notoginseng c. Construction of microencapsulated ligustrazine delivery system d. Gradient emulsification combined with low temperature filling process.

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