JP3496967B2 - Antiplasmin agent - Google Patents

Description

Description: BACKGROUND OF THE INVENTION 1. Field of the Invention The present invention relates to an anti-plasmin agent having a high anti-plasmin action and effective in inflammation, and more particularly, to cosmetics, pharmaceuticals, or periodontitis. The present invention relates to an antiplasmin agent which can be used for prevention of toothpaste and oral products. 2. Description of the Related Art Guava is called a bunjirou or banyanagi, and is a plant belonging to the genus bunjiro in the family Myrtaceae, and its scientific name is Psidium guajaba L. Generally, the berries are eaten raw, jam, juice, or the like. The distribution is native to tropical America, but is widely cultivated in tropical and subtropical areas, cultivated in southern Kyushu in Japan, and wild in the Ryukyu Islands. Guava is also used as a drug in enteritis, dysentery, and indigestive diarrhea.
Leaves are considered a substitute for tea. Further, Japanese Patent Application Laid-Open No. 5-2 filed by the present applicant has
In Japanese Patent Publication No. 46837, the use of a solvent extract of guava leaves as cosmetics is used to achieve whitening, prevention of rough skin, and the like. [0004] Nishikawayanagi is a plant belonging to the dicotyledonous plant net, the leaf-flowering sub-net, the camellia, the gourd family, and the gourd genus. The scientific name is Tamarix chinensis roua.
s Lour). In general, it is a young branch with leaves of a plant called gyoryu. This plant is native to China, but is a deciduous small tree that has been introduced to Japan for appreciation and planted in gardens and the like. Applications include perspiration, antipyretic, diuretic, antitussive, antibacterial (pneumococci, α-streptococci, staphylococci, influenza), and the like. Further, Japanese Patent Application Laid-Open No. Hei 5-3 filed by the present applicant
In JP 06213, the use of whitening, prevention of rough skin, etc. is attempted by using a solvent extract of Nishikawayanagi as a cosmetic. Rishimi is a plant belonging to the genus Rapaceae and the genus Rapese, and its scientific name is Trapa natans L.
It is a dried version of the fruit of a plant, usually called "Hishi". Eel is distributed in the subtropics from temperate regions of Japan, Korea and China, and is an annual plant that grows in ponds and swamps and is actually edible. It is used as a nutrient tonic and antipyretic. Further, Japanese Patent Application Laid-Open No. Hei 5-3 filed by the present applicant
In JP 06214, the use of whitening, prevention of rough skin, and the like is attempted by using a solvent extract of Rishimi as a cosmetic. By the way, it is known that when the skin is irradiated with ultraviolet rays UVB twice the minimum erythema amount, erythema and edema are formed. Histamine,
It has been reported that chemical mediators such as serotonin, prostaglandins E ₂ , F _2a and kinin are involved. In addition, plasmin activity in rabbit skin tissue is enhanced after UV irradiation, plasmin activity fluctuates well in parallel with the degree of skin swelling, and skin swelling is caused by administration of tranexamic acid, an antiplasmin agent. Is known to be severely suppressed. Therefore, this plasmin is also one of the important chemical mediators in the UV inflammatory response. [0009] On the other hand, various substances are known as substances having an antiplasmin action which can be used as a raw material of cosmetics, but synthetic products have no guarantee of safety when applied to human skin for a long time. , Use is being restricted. On the other hand, many natural products have weak antiplasmin action. But,
From the viewpoint of safety for human skin, natural products have been required for many years, which have been eaten by humans and have been guaranteed in terms of safety, and have been required to have a strong antiplasmin action. [0010] An object of the present invention is to provide an antiplasmin agent which is safe when applied to the human body such as skin and has a large antiplasmin action. Means for Solving the Problems In order to solve the above problems, the present inventors have screened and examined plants which have been used for food for many years and whose safety to the human body has been confirmed. The useful thing was examined as an antiplasmin agent. As a result, it is known in the above-mentioned publication that the applicant of the present application applied that the solvent extract of Guava, Hishimi, Nishikawayanagi is effective as a cosmetic. As a result, the present invention has been completed by newly finding that these solvent extracts are effective as a raw material of an antiplasmin agent or as a quasi-drug. That is, the present invention is an antiplasmin agent comprising one or more solvent extracts of guava, ishibumi, and ishikawayanagi. Guava, Hishimi, Nishikawayanagi can be used in water or a hydrophilic organic solvent such as ethanol,
Extract with methanol, acetone, etc. However,
Naturally, extraction with water, ethanol, or a mixed solvent thereof is preferable because the extraction of the antiplasmin agent raw material is performed. In some cases, glycerin, 1,
Polyhydric alcohols such as 3-butylene glycol and propylene glycol or a mixture of polyhydric alcohol and water can also be used for extraction. Further, it is also effective to freeze-dry and use as a powder depending on the method of use. These extracts can be used alone or in combination with other cosmetic or quasi-drug raw materials, for example, liquid oils such as squalane and jojoba oil, solid oils such as beeswax and cetyl alcohol, various activators, glycerin Various types of antiplasmin agents can be prepared by blending with humectants such as 1,3-butylene glycol and various drugs.
For example, lotions, creams, emulsions, packs and the like can be used in various forms depending on the purpose. An embodiment which is an actual method of use will be described below, but the present invention is not limited to this embodiment. Production examples of the extracts of Guava, Rishimi and Nishikawayanagi used in the present invention are shown below. (Production Example 1) 300 ml of ethanol was added to 10 g of a young branch (dried product) with a leaf of a ginkgo biloba, and the mixture was left for 5 days with occasional stirring. This was filtered, evaporated and freeze-dried. (Production Example 2) 300 ml of 50% ethanol was added to 10 g of a young branch (dried product) with a leaf of ginger, and the mixture was left for 5 days with occasional stirring. This was filtered, evaporated and freeze-dried. (Production Example 3) 300 ml of purified water was added to 10 g of a young branch (dry product) having a leaf of ginger, and the mixture was heated for 3 hours. This was allowed to cool, filtered, and lyophilized. (Production Example 4) 10 g of guava leaves (dried product)
To the mixture was added 300 ml of ethanol, and the mixture was left for 5 days with occasional stirring. This was filtered, evaporated and freeze-dried. (Production Example 5) 10 g of guava leaves (dried product)
Add 300 ml of 50% ethanol to the mixture and mix with occasional stirring.
Left for days. This was filtered, evaporated and freeze-dried. (Production Example 6) 10 g of guava leaves (dried product)
300 ml of purified water was added to the mixture and heated for 3 hours. This was allowed to cool, filtered, and lyophilized. Production Example 7 300 ml of methanol was added to 10 g of Ryomi (dried product), and the mixture was left for 5 days with occasional stirring. This was filtered, evaporated and freeze-dried. (Production Example 8) 50 pieces for 10 g of Rishimi (dried product)
% Ethanol was added and left for 5 days with occasional stirring. This was filtered, evaporated and freeze-dried. Example 1 (Preparation of lotion) Weight% Olive oil 0.5 Extract of Production Example 1 0.5 Polyoxyethylene (20E.O.) sorbitan monostearate 2.0 Polyoxyethylene (60E. O.) hydrogenated castor oil 2.0 ethanol 30.0 1.0% aqueous solution of sodium hyaluronate 5.0 purified water 60.0 [Example 2 (preparation of ointment)]% by weight Macrogol 4000 49.8 Macrogol 400 49.8 Extract of Preparation Example 0.4 0.4 Example 3 is a lotion prepared by changing the extract of Preparation Example 1 of Example 1 to the extract of Preparation Example 3. Example 4 is an ointment prepared by replacing the extract of Production Example 2 of Example 2 with the extract of Production Example 4. Example 5 is a lotion prepared by changing the extract of Production Example 1 of Example 1 to the extract of Production Example 5. Example 6 is an ointment prepared by replacing the extract of Production Example 2 of Example 2 with the extract of Production Example 6. Example 7 is a lotion prepared by changing the extract of Production Example 1 of Example 1 to the extract of Production Example 7. Example 8 is an ointment prepared by replacing the extract of Production Example 2 of Example 2 with the extract of Production Example 8. Antiplasmin test Test method Plasminogen-removed fibrinogen type 2-0.6% aqueous solution (4 ml) was placed in a 9 cmφ dish, and the pH was 7.4.
Was added and stirred, and 0.1 ml of thrombin (10 units / ml) was added dropwise, mixed gently, and allowed to stand for 30 minutes. The addition of thrombin turned fibrinogen into fibrin and formed a gel. Sample 0.1 ml and plasmin solution (10 units / ml)
After 30 μl of the 0.1 ml mixed solution was placed on a petri dish gel, the mixture was allowed to stand at 37 ° C. for 2 hours. Then, the dissolved area of the fibrin gel was measured. A similar experiment was conducted using water instead of the specimen, and the inhibition rate of plasmin activity was determined by the following equation. (Equation 1) When tranexamic acid and ε-aminocaproic acid were tested as positive controls, the 50% inhibitory concentrations were 30 mg / ml for tranexamic acid and 40 mg / ml for ε-aminocaproic acid. The results are shown in Table 1 below. [Table 1] As is clear from the results shown in Table 1, the extracts of Guava, Rishimi and Nishikawayanagi of Production Examples 1 to 8 were found to have a very large antiplasmin action. (Usage test) The face of five women was divided into left and right sides, and the lotion and the ointment of the example were set on one side, and the lotion and the ointment of the comparative example were set on the other side. Three months later, they were evaluated for anti-inflammatory properties. In Comparative Examples, various extracts of Production Examples were replaced with water from Examples (Comparative Examples 1 and 2).
2). In addition, 20 persons were divided into 4 groups and tested using the samples shown in Table 2 below. [Table 2] The evaluation was made according to the following evaluation criteria, and the results are summarized in Table 3 below. (Evaluation Criteria) Example is very good 3 Example is considerably better 2 Example is slightly better 1 No difference 0 Comparative example is slightly better -1 Comparative example is much better − 2 The comparative example is much better -3 As is clear from the results of the use test in Table 3 above, the lotions and ointments containing antiplasmin containing the extracts of guava, ishimi and Nishikawayanagi of the present invention suppress inflammation when applied to the skin. It turned out to be effective. According to the present invention, an antiplasmin agent having a high antiplasmin action and a high safety effective against inflammation is provided.

──────────────────────────────────────────────────続 き Continued on the front page (58) Fields surveyed (Int. Cl. ⁷ , DB name) A61K 35/78 BIOSIS (DIALOG) CA (STN) JICST file (JOIS) MEDLINE (STN)

Claims (1)

(57) [Claim 1] An antiplasmin agent comprising one or more solvent extracts of guava leaves, Nishikawayanagi and Rishimi.