CN106344586B - Application of protopanaxatriol in preparing medicine for preventing and treating telangiectasia - Google Patents

Application of protopanaxatriol in preparing medicine for preventing and treating telangiectasia Download PDF

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CN106344586B
CN106344586B CN201610601200.1A CN201610601200A CN106344586B CN 106344586 B CN106344586 B CN 106344586B CN 201610601200 A CN201610601200 A CN 201610601200A CN 106344586 B CN106344586 B CN 106344586B
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protopanaxatriol
telangiectasia
ppt
present
pharmaceutical composition
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CN106344586A (en
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范代娣
段志广
马晓轩
黄蓉
范翠英
刘彦楠
严建亚
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SHAANXI GIANT BIOGENE TECHNOLOGY Co Ltd
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SHAANXI GIANT BIOGENE TECHNOLOGY 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
    • A61K31/56Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
    • A61K31/575Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids substituted in position 17 beta by a chain of three or more carbon atoms, e.g. cholane, cholestane, ergosterol, sitosterol

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  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
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Abstract

The invention provides application of protopanaxatriol in preparing a medicament for preventing and treating telangiectasia. The invention also provides a pharmaceutical composition for treating or preventing telangiectasia. The pharmaceutical composition comprises a therapeutically or prophylactically effective amount of protopanaxatriol as an active ingredient, and a pharmaceutically acceptable carrier.

Description

Application of protopanaxatriol in preparing medicine for preventing and treating telangiectasia
Technical Field
The invention relates to the field of biological medicines, in particular to application of protopanaxatriol (PPT) in treating or preventing telangiectasia.
Background
Telangiectasia is commonly called as redness, and is mainly a phenomenon that facial capillaries are easy to contact and sense external environment changes due to the fact that the stratum corneum of the face is weak, and therefore redness is generated on the face, particularly the cheek parts, caused by telangiectasia. The face of a patient with red streaks appears significantly redder or purple-red than normal skin tone. People often refer to plateau faces or red-face eggs, most of which have red cheeks on two sides and circular boundaries and are generally arranged in a thread shape. The skin is thin and sensitive, has obvious reactions to cold, heat and emotional excitement, influences the beauty, causes psychological shadow to patients and brings inconvenience to daily life.
Telangiectasia is mainly characterized by skin telangiectasia and is caused by low skin immunity or external environment stimulation, and is mainly formed by skin cutin damage, loss of the natural protection of the cuticle of the blood capillary, and vasodilatation, damage and hyperplasia caused by the external environment stimulation. Once formed, the skin of the face is more easily stimulated by external factors such as cold, heat, ultraviolet rays and the like, so that the capillary expansion is more serious.
The main causes of telangiectasia are the following:
(1) long-term application of drugs or cosmetics containing damaged skin stratum corneum, such as topical long-term application of corticosteroids, causes telangiectasia, leading to thinning, atrophy, and telangiectasia; alternatively, the use of cosmetic grades containing exfoliating ingredients such as fruit acids, salicylic acid, etc. can result in damaged, thinned, fragile skin.
(2) Influence of geographical location: mainly due to the stimulation of plateau climate, the skin is lack of oxygen caused by high altitude, and the ultraviolet rays are stronger, which can cause the increase of the number of red blood cells and the expansion and rupture of capillary vessels.
(3) Environmental factors: the face mask is easy to cause frostbite in high and cold areas, so that the blood circulation is not smooth, and the blood vessel wall is stagnated to make the face present spider-web red blood streak; cold stimuli, air drying, sand-blown climates, sun exposure, increased tolerance of the capillaries beyond the normal range, and dilated rupture of the capillaries.
(4) Cosmetic care factors: polishing the horny layer, and tendering the skin by photons in beauty parlors cause damage to the horny layer to cause red blood streak.
In addition to the above main causes, some complications of local or systemic diseases may also cause telangiectasia rupture, or hot diet, drinking, etc. may be linked to the onset of telangiectasia.
At present, the treatment of the telangiectasia mainly rebuilds the healthy physiological barrier of the skin, realizes the protection of the capillary vessel and simultaneously assists the inhibition of the telangiectasia. The common treatment methods at present comprise irradiating the skin by laser with specific wavelength, coating medicines to reduce vascular permeability, selecting skin care products with anti-allergy effect, and the like. In addition, the food and drink are prohibited from being spicy and pungent, and the sufficient sleep and good heart condition are kept, so that the improvement can be gradually realized.
Disclosure of Invention
The invention aims to provide a novel pharmaceutical composition for treating or preventing telangiectasia. It is a further object of the present invention to provide the use of protopanaxatriol (PPT) in the manufacture of a medicament for the treatment or prevention of telangiectasia.
The present inventors have conducted extensive studies to find that protopanaxatriol (PPT) has a strong effect of inhibiting telangiectasia, and thus have completed the present invention.
Namely, the present invention comprises:
1. a pharmaceutical composition for treating or preventing telangiectasia, comprising: protopanaxatriol (PPT) as an active ingredient, and a pharmaceutically acceptable carrier.
2. The pharmaceutical composition of item 1, wherein the protopanaxatriol (PPT) is the only active ingredient.
3. The pharmaceutical composition of item 1 or 2, wherein the telangiectasia is colloquially known as red blood streak.
4. The pharmaceutical composition according to any one of items 1 to 3, wherein the content of protopanaxatriol (PPT) in the pharmaceutical composition is 0.1% by weight or more.
5. Use of protopanaxatriol (PPT) in the manufacture of a medicament for the treatment or prevention of telangiectasia.
6. The use according to item 5, wherein protopanaxatriol (PPT) is the sole active ingredient of the medicament.
7. The use according to item 5 or 6, wherein the protopanaxatriol (PPT) is contained in the medicament in an amount of 0.1% by weight or more.
8. The use according to any one of claims 5 to 7, wherein the telangiectasia is commonly known as red blood streak.
According to the present invention, there can be provided a pharmaceutical composition for treating or preventing telangiectasia that significantly inhibits telangiectasia, and use of protopanaxatriol (PPT) for the preparation of a medicament for treating or preventing telangiectasia.
Drawings
FIG. 1 comparison of the effect of the volunteers after 14 days of application of the ointment of example 1 and a normal cream.
Detailed Description
The present invention will be described in detail with reference to specific embodiments. In the absence of conflict, scientific terms used in this specification have the meaning commonly understood by one of ordinary skill in the art to which this specification pertains.
First, in one aspect, the present invention is a pharmaceutical composition (pharmaceutical composition of the present invention) comprising: protopanaxatriol (PPT) as an active ingredient, and a pharmaceutically acceptable carrier. The pharmaceutical composition of the invention can be used for treating or preventing telangiectasia (commonly known as red blood streak).
In the present specification, protopanaxatriol (PPT) refers to a compound represented by the following chemical formula 1.
[ chemical formula 1 ]
Figure BDA0001061407780000041
The protopanaxatriol (PPT) is a known compound and can be prepared by a method known in the art, for example, protopanaxatriol (PPT) can be prepared by enzymatically hydrolyzing ginsenoside Re.
The pharmaceutical composition of the present invention may comprise protopanaxatriol (PPT) as the only active ingredient, and may also comprise other active ingredients.
As the pharmaceutically acceptable carrier, one skilled in the art can routinely select it according to the needs of the dosage form and the like. The pharmaceutical composition of the present invention is preferably applied by application to the skin, and therefore the dosage forms of the pharmaceutical composition of the present invention are preferably those capable of being applied by application to the skin, such as ointments, gels, liniments, tinctures, wet cloths, and the like.
In the pharmaceutical composition of the present invention, the content of protopanaxatriol (PPT) may be 0.1% by weight or more, preferably 0.2% by weight or more, more preferably 0.5% by weight or more, more preferably 1% by weight or more, more preferably 2% by weight or more, more preferably 5% by weight or more, more preferably 10% by weight or more.
In another aspect, the present invention provides the use of protopanaxatriol (PPT) (use of the invention) in the manufacture of a medicament (e.g. a pharmaceutical composition of the invention) for the treatment or prevention of telangiectasia.
Furthermore, in another aspect, the present invention also provides a method of treating telangiectasia in a subject, comprising the step of administering to the subject a pharmaceutical composition of the present invention.
Here, the subject may be a mammal, and may be, for example, a human, rat, rabbit, sheep, pig, cow, cat, dog, monkey, and the like, and is preferably a human.
The pharmaceutical composition of the present invention is preferably applied by application to the skin. The administration amount varies depending on the degree of symptoms, age, sex, body weight, sensitivity of the patient, administration method, administration period, administration interval, properties of the pharmaceutical preparation, kind of the active ingredient and the like, and is not particularly limited.
Examples
The present invention will be described in detail with reference to specific examples. The following examples are given to facilitate the understanding of the present invention and are not intended to limit the present invention.
EXAMPLE 1 Protopanaxatriol (PPT) ointment
Making into ointment (100 tubes, 10 g/tube, protopanaxatriol (PPT) content 100 mg/tube)
Figure BDA0001061407780000051
The main process flow is as follows: adding glycerol and 1, 3-butanediol into a vacuum emulsification tank, heating to 70 ℃, stirring at the rotating speed of 150rpm, then sequentially adding methyl paraben, propyl paraben, octadecanol, glyceryl monostearate, vaseline and lanolin, adjusting the rotating speed to 300rpm, stirring for 15min, cooling to 50 ℃, adding protopanaxatriol (PPT), continuously stirring for 20min, vacuumizing, adjusting the rotating speed to 3000rpm, stirring for 15min to complete emulsification, cooling to room temperature and filling. The net content is about 10 g/tube, and the protopanaxatriol (PPT) content is 100 mg/tube.
Example 2 Protopanaxatriol (PPT) gel
The gel (100 tubes, 20 g/tube, protopanaxatriol (PPT) content 250 mg/tube) is prepared according to the following mixture ratio
Figure BDA0001061407780000052
Figure BDA0001061407780000061
Carbomer 941 was taken and a small amount of water was added to swell in the formulation tank. Dissolving protopanaxatriol (PPT) with ethanol under stirring, sequentially adding propylene glycol and glycerol, slowly adding the solution into carbomer matrix under stirring, adding triethanolamine dropwise, adding purified water to 2000g, and stirring to obtain semitransparent protopanaxatriol (PPT) gel.
Example 3 therapeutic Effect of a pharmaceutical composition comprising protopanaxatriol (PPT) as an active ingredient on telangiectasia
And (3) experimental design: 30 volunteers with telangiectasia were selected, other skin diseases were excluded, the content of the test was informed in detail, informed consent was obtained, and the therapeutic effect of the composition on telangiectasia was volunteered.
The test contents are as follows: the ointment produced according to example 1 is applied to the left face of a volunteer, about 0.5g of ointment is applied to the left face every time, common face cream is applied to the right face, the application amount is 0.5g, the ointment is applied once in the morning and at night, the application amount is kept consistent every day, the volunteer is followed after continuously applying the ointment for 14 days, the subjective judgment and the comparison of front and back pictures of the volunteer are carried out, and the total effective rate is recorded and counted.
TABLE 3 volunteers tested the effect of protopanaxatriol (PPT) ointment on facial telangiectasia
Figure BDA0001061407780000062
It should be noted that any feature or combination of features described as part of one embodiment in this specification can be applied to other embodiments as well, without significantly departing from the spirit of the invention; further, the technical features described as the constituent elements of the different technical aspects may be combined in any manner to constitute the other technical aspects, without significantly departing from the gist of the present invention. The present invention also includes technical means obtained by combining the above cases, and these technical means are described in the present specification.
While the present invention has been described with respect to the specific embodiments and examples, it will be understood by those skilled in the art that these are not intended to limit the scope of the present invention, which should be determined from the claims.
Industrial applicability
The pharmaceutical composition of the present invention can significantly inhibit telangiectasia, and thus it is useful as a medicament for treating or preventing vasodilation.

Claims (2)

1. Use of protopanaxatriol (PPT) in the manufacture of a medicament for the treatment or prevention of telangiectasia, wherein protopanaxatriol (PPT) is the sole active ingredient of the medicament, said telangiectasia being facial red blood filaments.
2. The use according to claim 1, wherein the protopanaxatriol (PPT) is present in the medicament in an amount of 0.1% by weight or more.
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Citations (4)

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CN101695513A (en) * 2009-10-28 2010-04-21 上海永神生物科技有限公司 Composition with anti-tumor effect and application thereof
CN103520014A (en) * 2012-07-05 2014-01-22 株式会社爱茉莉太平洋 Composition for topical skin application containing ginsenoside F2 derived from hydroponic ginseng
CN105168278A (en) * 2008-11-28 2015-12-23 株式会社爱茉莉太平洋 Composition For Preventing Or Treating Artherosclerosis
CN105769955A (en) * 2015-01-09 2016-07-20 株式会社爱茉莉太平洋 Composition comprising ginseng extracts with enhanced ginsenoside contents

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2007008896A (en) * 2005-07-04 2007-01-18 Shoyaku Hakko Kenkyusho:Kk Anti-inflammatory analgesic agent for external use for skin and method for producing the same

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN105168278A (en) * 2008-11-28 2015-12-23 株式会社爱茉莉太平洋 Composition For Preventing Or Treating Artherosclerosis
CN101695513A (en) * 2009-10-28 2010-04-21 上海永神生物科技有限公司 Composition with anti-tumor effect and application thereof
CN103520014A (en) * 2012-07-05 2014-01-22 株式会社爱茉莉太平洋 Composition for topical skin application containing ginsenoside F2 derived from hydroponic ginseng
CN105769955A (en) * 2015-01-09 2016-07-20 株式会社爱茉莉太平洋 Composition comprising ginseng extracts with enhanced ginsenoside contents

Non-Patent Citations (1)

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Title
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