CN114073687A - Application of cannabidiol in preparation of medicine for preventing and treating acne rosacea - Google Patents

Application of cannabidiol in preparation of medicine for preventing and treating acne rosacea Download PDF

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Publication number
CN114073687A
CN114073687A CN202110969262.9A CN202110969262A CN114073687A CN 114073687 A CN114073687 A CN 114073687A CN 202110969262 A CN202110969262 A CN 202110969262A CN 114073687 A CN114073687 A CN 114073687A
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cannabidiol
medicament
rosacea
medicine
preventing
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蒋献
王莲
李焰梅
夏林欢
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West China Hospital of Sichuan University
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West China Hospital of Sichuan University
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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/045Hydroxy compounds, e.g. alcohols; Salts thereof, e.g. alcoholates
    • A61K31/05Phenols
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/10Anti-acne agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

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  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Dermatology (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

The invention provides an application of cannabidiol in preparing a medicine for preventing and treating acne rosacea. Also discloses a medicament for preventing and/or treating acne rosacea, which is prepared by using cannabidiol as an active ingredient and adding pharmaceutically acceptable auxiliary materials or auxiliary ingredients. The cannabidiol can effectively improve erythema and edema, improve telangiectasia, reduce inflammation and prevent and/or treat rosacea, and provides a new clinical choice.

Description

Application of cannabidiol in preparation of medicine for preventing and treating acne rosacea
Technical Field
The invention belongs to the field of biological medicines, and particularly relates to application of cannabidiol in preparation of a medicine for preventing and treating acne rosacea.
Background
Rosacea is a chronic inflammatory dermatosis mainly occurring in erythema and telangiectasia of face center, dry desquamation and seborrhea appear on face in early stage, there are symmetrically distributed erythema, capillary vessel further dilates in middle and later stage, hair follicle enlarges, acne-like papule and nasal nodule appear, and eye inflammation such as conjunctivitis, keratitis, etc. can be caused when the eye inflammation is serious.
Rosacea is a multifactorial disease whose causes include: the phenomena of dilated face capillaries, damaged skin barrier, dry desquamation and hypersecretion of sebum and formation of erythema caused by stimulating diet, strenuous exercise, high temperature, cold, light and wind; chronic skin inflammation and nerve immunity abnormality caused by improper use of skin care products, environmental pollution, irregular long-term work and rest, bad life habits and other factors; skin barrier damage and natural immune function abnormality caused by microorganism invasion of demodex and the like and skin microecological imbalance, and the phenomena of dryness, desquamation and excessive sebum secretion occur to generate inflammation; or skin thinning and increased telangiectasia due to topical long term use of corticosteroid hormones.
Clinically, the rosacea is divided into the following 4 main types according to different parts, different periods and different skin damage characteristics, different types can be mutually overlapped, and partial types can be mutually converted.
(1) Erythema telangiectasia type: most of the hair is firstly sent to the cheek part, and the few hair is firstly sent to the nose or the periphery of the mouth; showing paroxysmal flushing of the cheek, aggravating flushing due to emotional agitation, environmental temperature change or solarization, and may also gradually show persistent erythema or telangiectasia; a few patients are accompanied by pruritus and few patients are also accompanied by psychogenic symptoms such as dysphoria, melancholy, insomnia and the like.
(2) Papulopustular type: some patients can develop papules and pustules on the basis of erythema and telangiectasia, and are mostly seen in the cheek; some patients develop papules and pustules while erythema telangiectasia occurs, and most of them are around the mouth or in the nose.
(3) Hypertrophic type: most of the disease is seen in the nose or around the mouth, and the few disease is seen in the cheek, forehead and ear; hypertrophy of the nose changes the skin lesions known as "nasal tumors".
(4) Eye type: the eye type is few and is often accompanied with the three types; eyelash follicles and related glands of the eyelids, including meibomian glands, sebaceous glands and sweat glands; manifested by subjective symptoms of ocular foreign body sensation, photosensitivity, blurred vision, burning, stinging, dryness or itching.
Clinically, the treatment of the acne rosacea adopts the externally applied azelaic acid cream, brimonidine gel and other medicines, but the medicines have poor treatment effect and are easy to relapse, and the adverse reaction of local stimulation is generated in the using process, so that the skin is damaged; in addition, tacrolimus ointment, metronidazole gel and the like are also used for treating the acne rosacea clinically, but drug resistance and certain toxic and side effects are easy to occur. Therefore, how to treat rosacea safely and effectively remains a problem in the field of dermatology.
Cannabidiol (CAS number: 13956-29-1) is a phyto-cannabinoid derived from industrial cannabis, has anti-inflammatory, immunomodulatory, antioxidant, anti-apoptotic and anti-cancer effects, and has demonstrated therapeutic potential in epilepsy, neurodegenerative diseases, schizophrenia, multiple sclerosis and arthritis. However, the therapeutic effect of cannabidiol on rosacea has not been reported.
Disclosure of Invention
The invention aims to provide a new application of cannabidiol.
The invention provides application of cannabidiol in preparation of a medicine for preventing and/or treating acne rosacea.
Further, the cannabidiol is extracted from cannabis sativa or obtained by organic synthesis.
Furthermore, the purity of the cannabidiol is higher than 98%.
Furthermore, the medicine is used for preventing and/or treating skin erythema.
Further, the above-mentioned drug is a drug for preventing and/or treating skin edema.
Further, the above-mentioned medicament is a medicament for preventing and/or treating telangiectasia.
Further, the above-mentioned drugs are drugs for reducing inflammation.
The invention also provides a medicine for preventing and/or treating skin rosacea, which is a preparation prepared by using cannabidiol as an active ingredient and adding pharmaceutically acceptable auxiliary materials or auxiliary ingredients.
Further, the mass fraction of cannabidiol in the preparation is not less than 1%.
Obviously, many modifications, substitutions, and variations are possible in light of the above teachings of the invention, without departing from the basic technical spirit of the invention, as defined by the following claims.
The present invention will be described in further detail with reference to the following examples. This should not be understood as limiting the scope of the above-described subject matter of the present invention to the following examples. All the technologies realized based on the above contents of the present invention belong to the scope of the present invention.
Drawings
Fig. 1 shows clinical photographs, skin mirror photographs and HE staining results of LL37 in the construction of the rosacea model group and the control group.
Fig. 2 is a clinical photograph of rosacea in each group of mice.
FIG. 3 shows the results of HE staining of mice in each group.
Detailed Description
The starting materials used in the present invention are, unless otherwise stated, known products obtained by purchasing commercially available products.
The cannabidiol is provided by Beijing Taidou Biotechnology Limited, and the purity is more than or equal to 98 percent.
LL37 is an antimicrobial peptide used in the construction of an animal model of rosacea, purchased from shishi biotechnology (shanghai) ltd.
EXAMPLE 1 formulation of pharmaceutical composition for treatment of rosacea
Dissolving cannabidiol in a mixed solution of propylene glycol and 10% dimethyl sulfoxide to prepare a cannabidiol preparation with the mass fraction of 1%.
Experimental example 1 treatment of acne rosacea with cannabidiol
1. Establishment of mouse animal model with rosacea
1.1 BALB/c female mice of 6-7 weeks old are purchased from the experimental animal center of Sichuan university and are fed with special mouse feed and are adapted to the environment for 1 week.
1.2 skin preparation and experimental grouping: 1 day before the experiment, hair with an area of about 4.0cmx2.5cm was removed from the back of BALB/c mice using pet hair clippers and depilatory cream, and the experiment was divided into the following 2 groups: LL-37 group and control group.
1.3 modes of administration and dosages
LL-37 was dissolved in ultrapure water to prepare a 320. mu.M solution of LL-37. After local anesthesia of the mice, the central part of the mouse skin preparation area is selected as an injection area. LL-37 group preparation was injected intradermally with LL-37 solution and control group was injected intradermally with ultrapure water. Injections were given 1 time every 12 hours, 50 μ l each, for a total of 4 times. Observations were made 12 hours after the last injection and mice were sacrificed, direct observations and dermoscopic observations are shown in figure 1. Clear erythema with edema was seen in group LL37, HE further showed intradermal telangiectasia, inflammatory cell infiltration, and no corresponding expression in the control group, indicating successful establishment of the rosacea mouse animal model.
The above results indicate that LL37 can be successfully used to construct a mouse animal model of rosacea.
2. Treatment of acne-like skin lesions with cannabidiol
2.1 BALB/c female mice of 6-7 weeks old are purchased from the experimental animal center of Sichuan university and are fed with special mouse feed and are adapted to the environment for 1 week.
2.2 skin preparation and experimental grouping: 1 day before the experiment, hair was removed in an area of about 4.0cm x2.5cm from the back of BALB/c mice using pet clippers and depilatory cream. The experiments were divided into the following groups of three each: LL37 control (modeled using LL37 only), 1% CBD (treated with the formulation of example 1 with a CBD mass fraction of 1% and modeled with LL 37), matrix (treated with matrix without CBD: propylene glycol + 10% DMSO and modeled with LL 37) and blank control (modeled without LL 37).
2.3 modes of administration and dosages
In the 1% CBD group and the matrix group, 1% CBD and matrix were externally applied to the back of the mice 3 days in advance, 2 times a day, and each dose was 0.1ml/cm2LL37 control and blank control were not treated. After 3 days, the mice were locally anesthetized in the 1% CBD group, the vehicle group, and the LL37 control group, respectively, and the central part of the prepared skin area of the mice was selected as an injection area, and an LL37 solution was injected intradermally at a concentration of 320 μ M1 time per 12 hours and 50 μ l each time for 4 times. In the blank control group, ultrapure water was injected intradermally 1 time every 12 hours and 50. mu.l of ultrapure water was injected 4 times. Observations were made 12 hours after the last injection and mice were sacrificed and HE staining was performed.
As can be seen from fig. 2, LL37 control group: distinct, darker colored erythema with clear borders and obvious symptoms of rosacea. 1% CBD group: pale erythema with unclear borders was observed. Matrix group: erythema comparable to the LL37 control was seen. The blank control group had no significant erythema.
As can be seen in fig. 3, HE staining results for LL37 control group showed visible telangiectasia and more lymphocytic, neutrophil infiltration in the dermis. HE staining results in the 1% CBD group showed no significant vasodilation in the dermis, with only a small amount of lymphocyte infiltration visible. The stroma group showed more lymphocyte and neutrophil infiltration in the dermis. The blank control group had no vasodilation and no significant cellular infiltration.
The results show that cannabidiol can effectively reduce inflammation, improve erythema and edema, reduce telangiectasia and treat acne rosacea.
In conclusion, the invention provides an application of cannabidiol in preparation of a medicine for treating acne rosacea. Cannabidiol can effectively improve erythema and edema of rosacea, improve telangiectasia and reduce inflammation. The medicine for treating the acne rosacea, which takes the cannabidiol as the active ingredient, provides a new choice for clinical application.

Claims (8)

1. Use of cannabidiol in the manufacture of a medicament for the prevention and/or treatment of rosacea.
2. The use of claim 1 wherein the cannabidiol is not less than 98% pure.
3. The use according to claim 1, wherein the medicament is a medicament for the prevention and/or treatment of cutaneous erythema.
4. The use according to claim 1, wherein the medicament is a medicament for the prevention and/or treatment of skin edema.
5. Use according to claim 3 or 4, wherein the medicament is a medicament for the prevention and/or treatment of telangiectasia.
6. The use of claim 1, wherein the medicament is a medicament for reducing inflammation.
7. A medicine for preventing and/or treating skin rosacea is characterized in that the medicine is a preparation prepared by taking cannabidiol as an active ingredient and adding pharmaceutically acceptable auxiliary materials or auxiliary ingredients.
8. The medicament of claim 7, wherein cannabidiol is present in the formulation at a weight fraction of no less than 1%.
CN202110969262.9A 2020-08-21 2021-08-23 Application of cannabidiol in preparation of medicine for preventing and treating acne rosacea Pending CN114073687A (en)

Applications Claiming Priority (2)

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CN2020108508968 2020-08-21
CN202010850896 2020-08-21

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Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN109419665A (en) * 2017-08-25 2019-03-05 汉义生物科技(北京)有限公司 A kind of active matter rapid osmotic system containing Cannador or cannabidiol
CN110604709A (en) * 2019-09-21 2019-12-24 云南辰锦威生物科技有限公司 Facial mask for moisturizing, repairing and removing acne
CN110769819A (en) * 2017-02-15 2020-02-07 博塔尼克斯制药有限公司 Cannabinoid formulations for the treatment of acne

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110769819A (en) * 2017-02-15 2020-02-07 博塔尼克斯制药有限公司 Cannabinoid formulations for the treatment of acne
CN109419665A (en) * 2017-08-25 2019-03-05 汉义生物科技(北京)有限公司 A kind of active matter rapid osmotic system containing Cannador or cannabidiol
CN110604709A (en) * 2019-09-21 2019-12-24 云南辰锦威生物科技有限公司 Facial mask for moisturizing, repairing and removing acne

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
李焰梅,郝丹,蒋献.: "《大麻二酚在皮肤科的研究进展》", 《中国皮肤性病学杂志》 *

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