CN110876742A - Pharmaceutical composition for repairing skin injury and application thereof - Google Patents

Pharmaceutical composition for repairing skin injury and application thereof Download PDF

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Publication number
CN110876742A
CN110876742A CN201911109553.XA CN201911109553A CN110876742A CN 110876742 A CN110876742 A CN 110876742A CN 201911109553 A CN201911109553 A CN 201911109553A CN 110876742 A CN110876742 A CN 110876742A
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astaxanthin
skin
pharmaceutical composition
repairing
sodium sulfonate
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CN201911109553.XA
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刘红妹
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Guangzhou Home Cosmetics Co Ltd
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Guangzhou Home Cosmetics Co Ltd
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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
    • A61K31/185Acids; Anhydrides, halides or salts thereof, e.g. sulfur acids, imidic, hydrazonic or hydroximic acids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/12Ketones
    • A61K31/122Ketones having the oxygen directly attached to a ring, e.g. quinones, vitamin K1, anthralin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00Drugs for dermatological disorders
    • A61P17/02Drugs for dermatological disorders for treating wounds, ulcers, burns, scars, keloids, or the like

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

Abstract

The invention discloses a pharmaceutical composition for repairing skin injury, which comprises the following components in parts by weight (1-10): (50-200) astaxanthin and guaiazulene sodium sulfonate. The invention also discloses application of the pharmaceutical composition in preparing medicines and cosmetics for repairing skin injury. According to the invention, the astaxanthin and the guaiazulene sodium sulfonate are combined for use, so that the repairing effect on skin injury is greatly improved, especially the repairing effect on superficial skin injury is greatly improved; after the repair by the pharmaceutical composition, the skin can be complete, and the vascular damage and inflammatory cell infiltration are obviously reduced.

Description

Pharmaceutical composition for repairing skin injury and application thereof
Technical Field
The invention relates to the technical field of skin repair, in particular to a pharmaceutical composition for repairing skin injury and application thereof.
Background
Astaxanthin is the strongest antioxidant found in the nature by human at present, and has the antioxidant capacity far higher than vitamin C, vitamin E, β -carotene, lycopene, lutein, tea polyphenol and natto, and is widely applied to preparing health products at present, namely guaiazulene sodium sulfonate with a chemical name of 1, 4-dimethyl-7-isopropyl azulene-3-sodium sulfonate, has stronger biological activity, has the functions of medicine, anti-inflammation, antibiosis, antianaphylaxis, tissue regeneration and the like, and has high safety, so the astaxanthin is widely applied to industries such as health products, cosmetics and cosmetics.
Skin injuries, including deep skin injuries and superficial skin injuries, mainly injuries to the epidermis, superficial injuries which are common in daily life, such as skin injuries after laser cosmetology, strong sunlight sunburn, skin injuries after acne, skin injuries after micro-needle treatment and the like, and superficial skin injuries, the skin is mainly repaired by using cosmetics or external medicines which are applied topically. The currently used cosmetics are full of eyes and have uneven quality, the external medicines are mainly Chinese patent medicines such as pearl powder and the like, the quality is difficult to control, and the effect is slow.
Disclosure of Invention
The technical problem to be solved by the invention is to provide a pharmaceutical composition for repairing skin injury, which can quickly repair skin injury and effectively reduce vascular damage and inflammatory cell infiltration.
The invention also aims to solve the technical problem of providing an application of the pharmaceutical composition for repairing skin injury in preparing a medicine for repairing skin injury.
The invention also aims to solve the technical problem of providing the application of the pharmaceutical composition for repairing skin injury in preparing cosmetics for repairing skin injury.
In order to solve the technical problem, the invention provides a pharmaceutical composition for repairing skin injury, which comprises the following components in parts by weight (1-10): (50-200) astaxanthin and guaiazulene sodium sulfonate.
As an improvement of the technical scheme, the paint comprises the following components in percentage by weight (2-8): (50-130) astaxanthin and guaiazulene sodium sulfonate.
As an improvement of the technical scheme, the astaxanthin is extracted and separated from haematococcus pluvialis.
As an improvement of the technical scheme, the astaxanthin is coated by hydroxypropyl- β -cyclodextrin.
Correspondingly, the invention also discloses application of the pharmaceutical composition for repairing skin injury in preparing a medicine for repairing skin injury.
As an improvement of the above technical solution, the skin lesion is a superficial skin lesion.
Correspondingly, the invention also discloses application of the pharmaceutical composition for repairing skin injury in preparing cosmetics for repairing skin injury.
As an improvement of the above technical solution, the skin lesion is a superficial skin lesion.
As an improvement of the technical scheme, the dosage of the pharmaceutical composition for repairing skin injury is 0.1-5 wt% of the weight of the cosmetic product.
The implementation of the invention has the following beneficial effects:
according to the invention, the astaxanthin and the guaiazulene sodium sulfonate are combined for use, so that the repairing effect on skin injury is greatly improved, especially the repairing effect on superficial skin injury is greatly improved; after the repair by the pharmaceutical composition, the skin can be complete, and the vascular damage and inflammatory cell infiltration are obviously reduced.
Drawings
FIG. 1 is a graph showing the healing of a skin lesion in rats in a control group;
FIG. 2 is a graph showing healing of skin lesions in rats in the astaxanthin group;
FIG. 3 is a graph of the healing of skin lesions in rats in the sodium guaazulene sulfonate group;
FIG. 4 is a graph showing the healing of skin lesions of rats in a combination of astaxanthin and guaiazulene sodium sulfonate;
FIG. 5 is a histopathological image of the skin of rats in the control group;
FIG. 6 is a histopathology of skin of rats in the astaxanthin group;
figure 7 is a histopathology image of the skin of rats in the group of sodium guaiazulene sulfonate;
FIG. 8 is a histopathological image of the skin of rats in combination of astaxanthin and guaiazulene sodium sulfonate.
Detailed Description
In order to make the objects, technical solutions and advantages of the present invention more apparent, the present invention will be described in further detail with reference to the accompanying drawings.
The invention provides a pharmaceutical composition for repairing skin injury, which comprises the following components in parts by weight (1-10): (50-200) astaxanthin and guaiazulene sodium sulfonate; wherein, the astaxanthin has strong oxidation resistance, can effectively block the damage of cell membranes and proteins caused by oxygen free radicals at the skin injury part, and can also reduce the degradation of dermal fiber collagen. The guaiazulene sodium sulfonate has the functions of diminishing inflammation, resisting bacteria, resisting allergy, regenerating tissues and the like. The invention greatly improves the repairing effect on skin injury, in particular to the repairing effect on superficial skin injury by combining the two components; after the repair by the pharmaceutical composition, the skin can be complete, and the vascular damage and inflammatory cell infiltration are obviously reduced.
Specifically, when the weight ratio of the astaxanthin to the guaiazulene sodium sulfonate is less than 0.005, the astaxanthin has poor synergistic effect on the guaiazulene sodium sulfonate, so that the damage of oxygen free radicals to cell membranes and proteins cannot be effectively inhibited, and the repair speed is greatly reduced; when the weight ratio of the astaxanthin to the guaiazulene sodium sulfonate is more than 0.2, the guaiazulene sodium sulfonate cannot fully play the roles of diminishing inflammation and regenerating tissues.
Preferably, the pharmaceutical composition for repairing skin injury comprises the following raw materials in parts by weight: comprises (2-8) by weight: (50-130) astaxanthin and guaiazulene sodium sulfonate; more preferably, astaxanthin: sodium guaiazulene sulfonate 1: 20.
Wherein, the astaxanthin is divided into astaxanthin and artificially synthesized astaxanthin. When astaxanthin is synthesized by chemical means, chemical substances of impurities, such as unnatural byproducts generated in the synthesis process and the like, are inevitably introduced, and the bioavailability safety of the astaxanthin is reduced, so that the natural astaxanthin is adopted in the method.
Preferably, the present invention employs astaxanthin biologically extracted from Haematococcus pluvialis; further preferably, in the present invention, the method for extracting and separating astaxanthin from haematococcus pluvialis comprises:
(1) adding hydrochloric acid 50 times the amount of Haematococcus pluvialis and 4mol/L concentration into Haematococcus pluvialis, soaking at 70 deg.C for 20min for breaking cell wall, filtering, and collecting residue;
(2) adding a mixed solution of dichloromethane and ethanol with the amount of 50 times that of haematococcus pluvialis, wherein the dichloromethane: extracting with 2:1 ethanol at 40 deg.C for 3 times, filtering, mixing filtrates, adding 4% KOH alcoholic solution, saponifying at 10 deg.C for 10min, adjusting pH to neutral with hydrochloric acid, and concentrating to dry;
(3) extracting astaxanthin by using dichloromethane, performing gradient elution by using silica gel as a stationary phase and dichloromethane and ethanol as mobile phases, wherein the gradient concentration is from 100:0 to 92:8, and separating to obtain an astaxanthin finished product.
The purity of the astaxanthin obtained by the method is more than or equal to 99 percent; the effect is good.
Preferably, the astaxanthin is coated by hydroxypropyl- β -cyclodextrin, so that the skin utilization rate can be greatly improved, the percutaneous permeation and absorption capacity of the whole pharmaceutical composition can be improved, and the degradation and deterioration of active substances can be reduced.
Specifically, in the pharmaceutical composition for repairing skin injury, the total content of astaxanthin and guaiazulene sodium sulfonate is less than 10 wt%.
Specifically, the pharmaceutical composition can be a solution or a paste; but is not limited thereto. When the pharmaceutical composition is a solution, the astaxanthin and the guaiazulene sodium sulfonate can be dissolved in physiological saline or other medicinal alcohol solvents (such as ethanol, propanol, glycerol and the like) to form a 0.1% solution (g of astaxanthin and guaiazulene sodium sulfonate/100 mL of solvent), and then a finished product of the pharmaceutical composition can be obtained. When the pharmaceutical composition is a paste, the astaxanthin, the guaiazulene sodium sulfonate, the emulsifier, the solvent, the thickener and the like can be mixed, homogenized and emulsified at 40-80 ℃, and then cooled to normal temperature to obtain the pharmaceutical composition. Specifically, the emulsifier can be tween series or span series, but is not limited thereto. The solvent can be selected from high molecular weight oleum ricini, glycerol, ether solvent, ester solvent (such as ethyl acetate), etc., but is not limited thereto; the thickener can be selected from xanthan gum, arabic gum, high molecular weight polyethylene glycol, etc., but is not limited thereto. Specifically, in the medicinal composition of the paste agent, the content of astaxanthin and guaiazulene sodium sulfonate is less than or equal to 5 wt%, and preferably 0.5-2 wt%.
Correspondingly, the invention also discloses application of the pharmaceutical composition for repairing skin injury in preparing a medicine for repairing skin injury. More specifically, the skin lesion is a superficial skin lesion. Specifically, the pharmaceutical composition can be a solution or a paste.
Correspondingly, the invention also discloses application of the pharmaceutical composition for repairing skin injury in preparing cosmetics for repairing skin injury. More specifically, the skin lesion is a superficial skin lesion.
Specifically, the cosmetic can be cream; in the final product, the content of astaxanthin and guaiazulene sodium sulfonate is 0.1-5 wt%. Preferably 1 to 3 wt%. The cosmetic also comprises common adjuvants for skin care products, such as solvent, emulsifier, plasticizer, thickener, antiseptic, etc., and its preparation method is the same as that of existing cosmetic.
The invention repairs superficial skin injury by combining astaxanthin and guaiazulene sodium sulfonate, and specifically comprises the following steps:
experimental materials (one):
preparing an astaxanthin solution, namely weighing astaxanthin powder wrapped by hydroxypropyl- β -cyclodextrin, and adding normal saline to prepare a 50ppm astaxanthin solution;
preparing a guaiazulene sodium sulfonate solution: weighing guaiazulene sodium sulfonate and adding physiological saline to prepare 0.1% guaiazulene sodium sulfonate solution;
preparing the composition solution of astaxanthin and guaiazulene sodium sulfonate, namely weighing astaxanthin powder wrapped by hydroxypropyl- β -cyclodextrin, and guaiazulene sodium sulfonate and physiological saline to prepare a solution containing 50ppm of astaxanthin and 0.1 percent of guaiazulene sodium sulfonate.
(II) experimental method:
taking 32 healthy SD rats with half each male and female, no pregnancy, body mass of 180-200 g, 2-3 months of month age, randomly dividing into 4 groups, namely a model control group, an astaxanthin group, a guaiazulene sodium sulfonate group, an astaxanthin and guaiazulene sodium sulfonate composition group, and 8 SD rats in each group. Removing two sides of a spine of a rat back before an experiment to be used as an experiment part, repeatedly sticking a depilated part of the rat by using an adhesive tape, circularly puncturing the rat in each group by using a roller pin with the diameter of 0.5mm after the rat becomes red obviously, ensuring deep injury of the epidermis, simulating a skin damage model, then not coating any object on the rat skin damage part except a model control group, respectively coating corresponding astaxanthin solution, guaiazulene sodium sulfonate solution, astaxanthin and guaiazulene sodium sulfonate composition solution on the rat skin damage part for 2 times every day for 3 continuous days, observing the red swelling and healing recovery conditions of the skin damage part in each group, and having no inflammation or other adverse reactions. Meanwhile, after the experiment is finished, the skin is cleaned, the cervical vertebra is removed to kill the mouse, the skin is quickly taken down, the mouse is quickly thrown into 10% neutral formaldehyde fixing solution for fixation, and tissue sections are made for histomorphology observation.
(II) detection results:
as can be seen from the graphs in figures 1 to 4, the astaxanthin and the guaiazulene sodium sulfonate can promote the healing of the damaged skin of the rat, but a certain amount of scabs still exist after the combination is used for 3 days, and the combination of the astaxanthin and the guaiazulene sodium sulfonate can effectively promote the healing of the whole skin.
As can be seen from the graphs of 5-8, the astaxanthin and the guaiazulene sodium sulfonate have a repairing effect on the injury of the skin of the rat caused by the circular puncture of the roller needles, but the combination of the astaxanthin and the guaiazulene sodium sulfonate can completely repair the skin, so that the damage of blood vessels and the infiltration of inflammatory cells are obviously reduced.
The invention is illustrated in the following by specific examples:
example 1
The embodiment provides a medicament for repairing skin injury, which is a paste agent and has the following formula:
0.2% of astaxanthin, 5% of guaiazulene sodium sulfonate, 800.8% of tween, 10% of glycerol, 2% of castor oil, 8% of aloe gel, 2% of xanthan gum and 72% of water.
The preparation method comprises the following steps: mixing the above materials at 60 deg.C, homogenizing, emulsifying, and cooling to room temperature.
Example 2
The embodiment provides a medicine for repairing skin injury, which is a solution preparation, and specifically, astaxanthin powder wrapped by hydroxypropyl- β -cyclodextrin, guaiazulene sodium sulfonate and physiological saline are weighed to prepare a solution containing 600ppm of astaxanthin and 0.4% of guaiazulene sodium sulfonate, so that the medicine for repairing skin injury is obtained.
Example 3
The embodiment provides a medicine for repairing skin injury, which is a solution preparation, and specifically comprises astaxanthin powder wrapped by hydroxypropyl- β -cyclodextrin, guaiazulene sodium sulfonate and physiological saline to prepare a solution containing 50ppm of astaxanthin and 0.1% of guaiazulene sodium sulfonate, so that the medicine for repairing skin injury is obtained.
Example 4
The embodiment provides a medicament for repairing skin injury, which is a paste agent and has the following formula:
0.1% of astaxanthin, 8% of guaiazulene sodium sulfonate, 601% of tween, 10% of glycerol, 3% of castor oil, 8% of aloe vera gel, 2% of xanthan gum, 0.9% of polysorbate and 67% of water.
The preparation method comprises the following steps: mixing the above materials at 60 deg.C, homogenizing, emulsifying, and cooling to room temperature.
Example 5
The embodiment provides a skin care product for repairing skin injury, which comprises the following components in percentage by weight:
astaxanthin 0.2%, guaiazulene sodium sulfonate 3.5%, tween 800.5%, glycerin 8%, castor oil 4%, aloe vera gum 5%, xanthan gum 2%, polysorbate 0.5%, fruit fat 4%, water 72%.
The preparation method comprises the following steps: mixing the above materials at 60 deg.C, homogenizing, emulsifying, and cooling to room temperature.
Example 6
The embodiment provides a skin care product for repairing skin injury, which comprises the following components in percentage by weight:
astaxanthin 0.09%, guaiazulene sodium sulfonate 1.81%, tween 600.6%, glycerol 7.5%, castor oil 4%, aloe vera gum 5%, xanthan gum 3%, polysorbate 0.5%, fruit fat 4.5%, water 73%.
The preparation method comprises the following steps: mixing the above materials at 65 deg.C, homogenizing, emulsifying, and cooling to room temperature.
And (3) actual effect experiment:
typical case 1: when a certain woman is applied to a Binhe district of 48 years old, the woman is in Xining city, and the Binhe district of Haidong city, the skin is red and swollen due to sunburn, and the skin drops locally; rub with the product of example 5 twice daily; the red swelling is eliminated after two days; four days later, the skin was smooth, without desquamation, and completely recovered. Patient representation: has no irritation and anaphylaxis, and is convenient for use.
Typical case 2: zhang somewhere, man, 24 years old, Shenzhen, Nanshan Ding taifenghua, Shenzhen, carelessly bruise during exercise, damaged epidermis after bruise, and a lot of small bleeding spots with strong pain. Film coating was performed 3 times a day with the drug of example 4; the pain is obviously improved the next day, and the pain is eliminated after three days; after one week, the skin surface was smooth and completely recovered.
While the foregoing is directed to the preferred embodiment of the present invention, it will be understood by those skilled in the art that various changes and modifications may be made without departing from the spirit and scope of the invention.

Claims (9)

1. A pharmaceutical composition for repairing skin injury is characterized by comprising the following components in parts by weight (1-10): (50-200) astaxanthin and guaiazulene sodium sulfonate.
2. The pharmaceutical composition for repairing skin lesions according to claim 1, which comprises (2-8) by weight: (50-130) astaxanthin and guaiazulene sodium sulfonate.
3. The pharmaceutical composition for repairing skin lesions of claim 1 or 2, wherein the astaxanthin is isolated from Haematococcus pluvialis.
4. The pharmaceutical composition for repairing skin lesions according to claim 1 or 2, wherein said astaxanthin is selected from astaxanthin coated with hydroxypropyl- β -cyclodextrin.
5. Use of the pharmaceutical composition for repairing skin damage according to any one of claims 1 to 4 in the preparation of a medicament for repairing skin damage.
6. The use of claim 5, wherein the skin lesion is a superficial skin lesion.
7. Use of the pharmaceutical composition for skin damage repair according to any one of claims 1 to 4 for the preparation of a cosmetic for skin damage repair.
8. The use of claim 7, wherein the skin lesion is a superficial skin lesion.
9. The use according to claim 7, wherein the pharmaceutical composition for repairing skin lesions is used in an amount of 0.1 to 5 wt% based on the weight of the cosmetic product.
CN201911109553.XA 2019-11-14 2019-11-14 Pharmaceutical composition for repairing skin injury and application thereof Pending CN110876742A (en)

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2004359640A (en) * 2003-06-06 2004-12-24 Toyo Shinyaku:Kk Collagen production enhancing skin care preparation for external use
CN101045165A (en) * 2007-04-28 2007-10-03 南通大学 Hydroxypropyl beta-cyclodextrin clathrate of astaxanthin, and its preparing method
CN103232375A (en) * 2013-04-03 2013-08-07 大连医诺生物有限公司 Novel high-efficiency extraction process for astaxanthin in Haematococcus pluvialis
CN103393592A (en) * 2013-08-05 2013-11-20 四川国康药业有限公司 Sodium azulene sulfonate gel and its preparation method and use
CN105254550A (en) * 2015-10-28 2016-01-20 佛山市普达美生物医药科技有限公司 Method for extraction separation of astaxanthin from haematococcus pluvialis
WO2018062427A1 (en) * 2016-09-29 2018-04-05 Astareal Co., Ltd. Use of astaxanthin for reducing progression of damage caused to human skin
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JP2004359640A (en) * 2003-06-06 2004-12-24 Toyo Shinyaku:Kk Collagen production enhancing skin care preparation for external use
CN101045165A (en) * 2007-04-28 2007-10-03 南通大学 Hydroxypropyl beta-cyclodextrin clathrate of astaxanthin, and its preparing method
CN103232375A (en) * 2013-04-03 2013-08-07 大连医诺生物有限公司 Novel high-efficiency extraction process for astaxanthin in Haematococcus pluvialis
CN103393592A (en) * 2013-08-05 2013-11-20 四川国康药业有限公司 Sodium azulene sulfonate gel and its preparation method and use
CN105254550A (en) * 2015-10-28 2016-01-20 佛山市普达美生物医药科技有限公司 Method for extraction separation of astaxanthin from haematococcus pluvialis
WO2018062427A1 (en) * 2016-09-29 2018-04-05 Astareal Co., Ltd. Use of astaxanthin for reducing progression of damage caused to human skin
CN108309869A (en) * 2018-04-29 2018-07-24 佛山云裳化妆品有限公司 It is a kind of to have effects that the skin care compositions of skin repair and its application
CN108451825A (en) * 2018-04-29 2018-08-28 佛山云裳化妆品有限公司 A kind of skin conditioning composition after depilation and application

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Application publication date: 20200313