Cannabidiol slow-release wound inflammation-diminishing and pain-relieving ointment and preparation method thereof

Abstract

The invention provides a cannabidiol slow-release wound inflammation-diminishing and pain-relieving ointment and a preparation method thereof. The analgesic ointment is prepared from the following components in percentage by mass: 0.1%-0.5% of cannabidiol, 1%-8% of menthol, 5%-10% of borneol and the balance of vaseline. After the pain-relieving ointment is smeared on a wound, a layer of protective film is formed, cannabidiol continuously diminishes inflammation and relieves pain, and menthol, borneol and other components bring cool feeling, relieve discomfort and promote wound recovery. The analgesic ointment is suitable for daily nursing of common wounds, such as bruises and incisions, and is suitable for standing preparation of household medicine boxes.

Description

TECHNICAL FIELD

[0001] The application belongs to the technical field of wound care, and particularly relates to a cannabidiol sustained-release type wound anti-inflammatory analgesic ointment and a preparation method thereof. BACKGROUND

[0002] In daily life, general wounds such as abrasions and cuts are relatively common, and the nursing needs of such wounds are concentrated on three core aspects of rapid anti-inflammatory analgesia, forming an effective protective barrier and promoting wound healing. The wound care products on the market have the following technical problems: The anti-inflammatory analgesic component has a short action time: the active components in most products are released quickly, and although pain can be relieved in a short time, they need to be frequently applied, increasing the complexity of nursing operations and easily damaging the temporary protective structure on the surface of the wound.

[0003] There is a lack of long-acting protective film: ordinary ointments are easily rubbed off by clothes, contacted with moisture, etc. after being applied, and cannot continuously isolate external bacterial contamination, increasing the risk of wound infection.

[0004] Therefore, it is necessary to improve the existing analgesic ointment. SUMMARY

[0005] The purpose of the present application is to provide a cannabidiol sustained-release type wound anti-inflammatory analgesic ointment which has a long-lasting anti-inflammatory analgesic effect, can form a stable wound protective film and is suitable for daily home care, and a preparation method thereof.

[0006] A cannabidiol sustained-release type wound anti-inflammatory analgesic ointment is composed of the following components in mass percentage: cannabidiol 0.1%-0.5%, menthol 1%-8%, borneol 5%-10% and the balance of petrolatum.

[0007] Optionally, the mass percentage of cannabidiol is 0.2%-0.4%.

[0008] Optionally, the mass percentage of menthol is 3%-6%.

[0009] Optionally, the mass percentage of borneol is 7%-9%.

[0010] Optionally, the cannabidiol sustained-release type wound anti-inflammatory analgesic ointment is composed of the following components in mass percentage: cannabidiol 0.3%, menthol 5%, borneol 8% and the balance of petrolatum.

[0011] Optionally, the melting point of the petrolatum is 45-55℃.

[0012] Optionally, the purity of the cannabidiol is ≥99%.

[0013] Optionally, the pH value of the cannabidiol sustained-release type wound anti-inflammatory analgesic ointment is 6.5-7.5.

[0014] A preparation method of the above-mentioned cannabidiol sustained-release type wound anti-inflammatory analgesic ointment, comprising the following steps: S101: Take vaseline and place it in a reaction kettle, melt it at 50-60 DEG C with a stirring speed of 100-150 r / min, and keep it warm for 30-40 min to obtain a vaseline melt; S102: Crush the borneol into a particle size of 100-200 meshes, add it to the vaseline melt, continue to stir for 30-40 min until the borneol is completely dissolved, and obtain a mixed solution A; S103: Add the menthol to the mixed solution A, cool it to 40-45 DEG C, adjust the stirring speed to 200-250 r / min, and stir for 20-30 min to obtain a mixed solution B; S104: Dissolve the cannabidiol in ethanol to obtain a cannabidiol ethanol solution; slowly drop the cannabidiol ethanol solution into the mixed solution B while stirring at a speed of 200-250 r / min, continue to stir for 40-50 min after the dropping is completed; S105: Stop heating, naturally cool to 25-30 DEG C, reduce the stirring speed to 50-80 r / min, stir for 10-15 min, and cool to room temperature to obtain the cannabidiol sustained-release type wound anti-inflammatory analgesic ointment.

[0015] Optionally, in S104, the mass ratio of cannabidiol to ethanol is 1:5-1:10; and the dropping speed of the cannabidiol ethanol solution into the mixed solution B is 30-40 drops / min.

[0016] Beneficial effects In the present application, by compounding cannabidiol, menthol, borneol and vaseline in a specific ratio, the functions of anti-inflammatory analgesia and wound protection are synergized, the problems of short action time and weak protection effect of existing products are solved, the anti-inflammatory analgesic effect is long-lasting, and a stable wound protection film can be formed. Moreover, the analgesic ointment is free of antibiotics and addictive, and is suitable for daily wound care of all people in the family. Specific implementation

[0017] An embodiment of the present application provides a cannabidiol sustained-release type wound anti-inflammatory analgesic ointment, which is composed of the following components in mass percentage: cannabidiol 0.1%-0.5%, menthol 1%-8%, borneol 5%-10%, and the balance of vaseline. By compounding cannabidiol, menthol, borneol and vaseline in a specific ratio, the functions of anti-inflammatory analgesia and wound protection are synergized, the problems of short action time and weak protection effect of existing products are solved, the anti-inflammatory analgesic effect is long-lasting, and a stable wound protection film can be formed. Moreover, the analgesic ointment is free of antibiotics and addictive, and is suitable for daily wound care of all people in the family.

[0018] CBD, as the core anti-inflammatory analgesic ingredient, has the effects of anti-inflammatory, analgesic, and promoting cell repair, and is non-addictive and highly safe. The dispersibility of CBD in petrolatum can achieve slow release and prolong the anti-inflammatory analgesic effect. Menthol has a cooling effect and can quickly relieve the burning and stinging sensation of the wound. Its volatile components can also help open the pores of the skin and promote the penetration and absorption of CBD and borneol. Borneol has the effects of clearing heat, relieving pain, reducing swelling, and promoting tissue regeneration. It can synergistically enhance the anti-inflammatory effect of CBD and reduce the irritation of menthol, thereby improving the comfort of use. Petrolatum, as the base, has good sealing and moisturizing properties. After application, it can form a stable protective film on the wound surface, isolate bacteria and external stimuli, and provide a slow-release carrier for CBD, menthol, and borneol, ensuring that the active ingredients continuously act on the wound.

[0019] Specifically, CBD is the core of anti-inflammatory analgesic, but direct addition can lead to rapid release and only maintain the effect for 2-4 hours. The present application selects petrolatum as the base, utilizes its semi-solid properties and sealing properties, and encapsulates CBD in the intermolecular gaps of oil. After application, the protective film formed by petrolatum on the wound surface slows down the diffusion rate of CBD, changes its release from rapid to uniform and slow, and ultimately achieves long-acting anti-inflammatory for 8-12 hours. At the same time, the content of CBD is limited to 0.1%-0.5%, which avoids insufficient anti-inflammatory effect due to low content and waste of ingredients and mild skin irritation due to high content.

[0020] In addition, menthol can quickly relieve stinging by activating cold receptors in the skin, and its volatile components can open the intercellular gaps of the stratum corneum, promoting the transdermal absorption of CBD and borneol and improving the effect. High-concentration menthol can cause stinging on damaged skin, while the molecular structure of borneol can form hydrogen bonds with menthol, reducing its irritation to nerve endings in the skin. Through the synergistic cooperation between components, the irritation of the analgesic paste to the skin can be effectively reduced.

[0021] In some embodiments, the mass percentage of CBD is 0.2%-0.4%. By optimizing the content of CBD, the anti-inflammatory analgesic effect can be ensured while avoiding insufficient effect due to low content or waste of ingredients and mild skin irritation due to high content. For example, a content of 0.2%-0.4% can achieve better slow-release efficiency, making the anti-inflammatory effect last for 8-12 hours.

[0022] In some embodiments, the mass percentage of menthol is 3%-6%. A content of 3%-6% of menthol can provide a significant cooling effect while avoiding skin irritation due to high content (especially for sensitive skin) or a lack of cooling sensation due to low content. This range can better assist the penetration of CBD and improve the anti-inflammatory effect.

[0023] In some embodiments, the mass percentage of borneol is 7%-9%. The borneol content of 7%-9% can better synergize with cannabidiol to reduce inflammation, further neutralize the irritation of menthol, and improve the use comfort; and the borneol in this range can enhance the stability of the petrolatum protective film, so as to avoid the protective film from falling off due to temperature changes.

[0024] In some embodiments, the cannabidiol sustained-release wound anti-inflammatory analgesic ointment is composed of the following components in mass percentage: cannabidiol 0.3%, menthol 5%, borneol 8%, and the balance of petrolatum. This proportion is the optimal formula, cannabidiol 0.3% can achieve the best sustained-release anti-inflammatory effect, menthol 5% provides obvious cooling sensation without irritation, borneol 8% synergizes with cannabidiol to enhance anti-inflammatory effect, and the balance of petrolatum forms a stable protective film; the overall product has a 12-hour sustained anti-inflammatory analgesic effect, a protective film retention rate of more than 90%, and the highest use comfort.

[0025] In some embodiments, the melting point of petrolatum is 45-55℃. The melting point of 45-55℃ makes the petrolatum semi-solid at room temperature, which is easy to spread and can quickly solidify to form a protective film after application, while ensuring uniform dispersion of active ingredients in the matrix and achieving stable sustained release.

[0026] In some embodiments, the purity of cannabidiol is ≥99%. High-purity cannabidiol can avoid impurities irritating the wound, while ensuring the stability of the anti-inflammatory analgesic effect, allowing long-term storage without additional preservatives, and further improving product safety.

[0027] In some embodiments, the pH value of the cannabidiol sustained-release wound anti-inflammatory analgesic ointment is 6.5-7.5. The pH value is close to the pH value of human skin, avoiding skin irritation and allergy caused by excessively high or low pH value, and having a wide range of applications.

[0028] The present application also provides a preparation method of a cannabidiol sustained-release wound anti-inflammatory analgesic ointment, comprising the following steps: S101: Take petrolatum and place it in a reaction kettle, heat and melt at 50-60℃, the stirring speed is 100-150r / min, and keep warm for 30-40min to obtain a petrolatum melt; S102: Crush the borneol to a particle size of 100-200 mesh, add it to the petrolatum melt, continue to stir for 30-40min, until the borneol is completely dissolved, to obtain a mixed liquid A; S103: Add menthol to the mixed liquid A, cool to 40-45℃, adjust the stirring speed to 200-250r / min, and stir for 20-30min to obtain a mixed liquid B; S104: Cannabidiol is dissolved in ethanol to obtain a cannabidiol ethanol solution; the cannabidiol ethanol solution is slowly added to the mixed solution B, and stirring is performed at a speed of 200-250 r / min during the addition; after the addition is completed, stirring is continued for 40-50 min; S105: Stop heating and naturally cool to 25-30°C; the stirring speed is reduced to 50-80 r / min and stirring is performed for 10-15 min; after cooling to room temperature, a cannabidiol sustained-release wound anti-inflammatory analgesic ointment is obtained.

[0029] In the above preparation method, through the process of step-by-step dissolution, gradient temperature control, and ethanol-assisted dissolution, the menthol, the cannabidiol, and the ice flakes are uniformly dispersed in the vaseline, and uneven sustained release caused by aggregation of active ingredients is avoided. Heating and melting the vaseline at 50-60°C can avoid damage to the activity of cannabidiol at high temperature, and adding menthol at 40-45°C can prevent loss due to volatilization. Ethanol-assisted dissolution can improve the solubility of cannabidiol, and finally achieve stable product quality and consistent efficacy.

[0030] In some embodiments, in S104, the mass ratio of cannabidiol to ethanol is 1:5-1:10; the cannabidiol ethanol solution is slowly added to the mixed solution B at an addition speed of 30-40 drops / min. This can further promote the fusion between the components and better play the effect of the analgesic ointment.

[0031] The following are examples and comparative examples.

[0032] In the examples and comparative examples, the purity of cannabidiol is 99.9%. The vaseline is a medical-grade vaseline with a melting point of 50°C.

[0033] In the examples and comparative examples, the preparation method of the analgesic ointment is as follows: S101: The vaseline is placed in a reaction kettle and heated and melted at 55°C, with a stirring speed of 120 r / min, and the temperature is maintained for 35 min to obtain a vaseline melt.

[0034] S102: The ice flakes are crushed to a particle size of 200 mesh and added to the vaseline melt; stirring is continued for 35 min until the ice flakes are completely dissolved to obtain a mixed solution A.

[0035] S103: The menthol is added to the mixed solution A, the temperature is reduced to 40°C, the stirring speed is adjusted to 220 r / min, and stirring is performed for 25 min to obtain a mixed solution B.

[0036] S104: Cannabidiol is dissolved in ethanol to obtain a cannabidiol ethanol solution; the cannabidiol ethanol solution is slowly added to the mixed solution B, and stirring is performed at a speed of 200-250 r / min during the addition; after the addition is completed, stirring is continued for 40-50 min;

[0037] S105: stop heating, naturally cool to 25°C, reduce stirring speed to 50 r / min, stir for 10 min, and obtain the analgesic cream after cooling to room temperature.

[0038] It can be understood that, for the comparative examples not containing part of the components, in the preparation method, the corresponding processing steps for the components are not performed.

[0039] The mass percentages of the components in the examples and comparative examples are as follows. In each of the examples and comparative examples, the sum of the mass percentages of the components is 100%.

[0040]

[0041] Test Example (1) Anti-inflammatory effect Select 60 healthy mice, all make the same area (1 cm x 1 cm) of abrasion wounds on the back, and randomly divide them into 10 groups (5 groups of examples + 4 groups of comparative examples + 1 group of blank control group), 6 in each group. The blank control group is not smeared with any product, and the other groups are smeared with the corresponding product according to the dosage of 0.5 g / cm 2 . Observe the redness area at 12 h after smearing, and calculate the redness regression rate. Redness regression rate = (initial redness area - redness area at test time) / initial redness area x 100%.

[0042] (2) Analgesic effect Select 100 healthy volunteers (age 18-60 years old), all make the same depth (0.5 mm) of incision wounds on the arm, and randomly divide them into 10 groups (5 groups of examples + 4 groups of comparative examples + 1 group of blank control group), 10 in each group. The blank control group is not smeared with any product, and the other groups are smeared with the corresponding product according to the dosage of 0.5 g / cm 2 . The volunteers subjectively record the duration (unit: h) from the start of the wound to the complete relief of pain, and take the average value of each group.

[0043] (3) Stability of protective film Smear the products of each example and comparative example on a polyurethane film with a thickness of 0.2 mm, and place it in an environment of 37°C and 60% humidity. Observe the integrity of the protective film at 12 h, and calculate the retention rate. Retention rate = remaining protective film area / initial protective film area x 100%.

[0044] (4) Skin irritation Select 100 sensitive skin volunteers (age 18-40 years old), and randomly divide them into 10 groups (5 groups of examples + 4 groups of comparative examples + 1 group of blank control group), 10 in each group. The blank control group is not smeared with any product, and the other groups are smeared with each product (0.1 g / cm 2), covering 3cm x 3cm of the patch, and after 12h, the patch was removed, and whether the skin appeared red, swollen, itchy, stinging, and other allergic reactions was observed, and the incidence of allergic reactions was calculated. The incidence of allergic reactions = the number of people with allergic reactions / the total number of people in each group x 100%.

[0045] (5) Sustained-release effect The release rate of cannabidiol of each product within 12h was determined by high performance liquid chromatography (HPLC); 10g of the product was placed in a dialysis bag and soaked in 100mL of normal saline (37℃, stirring speed 100r / min), and 5mL was taken at 2h, 4h, 8h, 10h, and 12h (after sampling, an equal amount of normal saline was added), and the concentration of cannabidiol in the sample was determined, and the cumulative release rate was calculated. The 12h cumulative release rate = the mass of cannabidiol released cumulatively within 12h / the total mass of cannabidiol in the product x 100%.

[0046] The test results are shown in the following table.

[0047]

[0048] As can be seen from the above table, the five examples all perform excellently in various indicators, especially example 3, the comprehensive performance of which is far superior to the comparative examples and the blank control group, proving that the pain-relieving paste of the present application has obvious advantages. The comparative examples all have obvious defects in indicators such as anti-inflammatory, analgesic, protective, and safety due to the absence of core components (such as no cannabidiol in comparative example 1, no menthol in comparative example 2, and no borneol in comparative example 3) or components beyond the scope (comparative example 4), further verifying the necessity of the proportion of the components of the present application.

[0049] The above description is merely preferred embodiments of the present application and is not intended to limit the present application, and any modification, equivalent replacement, and improvement within the spirit and principle of the present application shall be included in the protection scope of the present application.

[0050] For those skilled in the art, according to the idea of the present application, there will be changes in specific embodiments and application scope, and in conclusion, the content of the specification should not be understood as a limitation of the present application.

Claims

1. A cannabidiol sustained-release wound anti-inflammatory and analgesic ointment, characterized in that: It consists of the following components in the indicated mass percentages: cannabidiol 0.1%-0.5%, menthol 1%-8%, borneol 5%-10%, and the balance petrolatum.

2. The cannabidiol sustained-release wound anti-inflammatory and analgesic ointment as described in claim 1, characterized in that: The mass percentage of cannabidiol is 0.2%-0.4%.

3. The cannabidiol sustained-release wound anti-inflammatory and analgesic ointment as described in claim 1, characterized in that: The menthol content is 3%-6% by mass.

4. The cannabidiol sustained-release wound anti-inflammatory and analgesic ointment as described in claim 1, characterized in that: The borneol comprises 7%-9% by mass.

5. The cannabidiol sustained-release wound anti-inflammatory and analgesic ointment as described in claim 1, characterized in that: It consists of the following components by weight percentage: 0.3% cannabidiol, 5% menthol, 8% borneol, and the balance petrolatum.

6. The cannabidiol sustained-release wound anti-inflammatory and analgesic ointment as described in any one of claims 1-5, characterized in that: The melting point of the petroleum jelly is 45-55℃.

7. The cannabidiol sustained-release wound anti-inflammatory and analgesic ointment as described in any one of claims 1-5, characterized in that: The purity of the cannabidiol is ≥99%.

8. The cannabidiol sustained-release wound anti-inflammatory and analgesic ointment as described in any one of claims 1-5, characterized in that: The pH value of the cannabidiol sustained-release wound anti-inflammatory and analgesic ointment is 6.5-7.

5.

9. A method for preparing a cannabidiol sustained-release wound anti-inflammatory and analgesic ointment according to any one of claims 1-8, characterized in that: Includes the following steps: S101: Place petroleum jelly in a reaction vessel, heat it to melt at 50-60℃, stir at 100-150 r / min, and keep it at this temperature for 30-40 min to obtain petroleum jelly melt; S102: Crush borneol to a particle size of 100-200 mesh, add it to the petroleum jelly melt, and continue stirring for 30-40 minutes until the borneol is completely dissolved to obtain mixture A; S103: Add menthol to mixture A, cool to 40-45℃, adjust the stirring speed to 200-250r / min, stir for 20-30min to obtain mixture B; S104: Dissolve cannabidiol in ethanol to obtain a cannabidiol ethanol solution; slowly add the cannabidiol ethanol solution dropwise to mixture B while stirring at a speed of 200-250 r / min. After the addition is complete, continue stirring for 40-50 min. S105: Stop heating, allow to cool naturally to 25-30℃, reduce stirring speed to 50-80r / min, stir for 10-15min, and cool to room temperature to obtain the cannabidiol sustained-release wound anti-inflammatory and analgesic ointment.

10. The preparation method according to claim 9, characterized in that: In S104, the mass ratio of cannabidiol to ethanol is 1:5-1:10; the cannabidiol ethanol solution is slowly added to mixture B at a rate of 30-40 drops / min.

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