JP5098156B2 - Water secretion promoter - Google Patents

Description

  The present invention relates to pharmaceuticals, quasi drugs, cosmetics or foods that promote water secretion and are effective in improving or preventing symptoms such as constipation and dry eye.

  With the advent of an aging society, stress society, and computer society, dry syndrome (dry syndrome) has become a problem in recent years as one of the modern diseases. Dry syndrome is a dry phenomenon that occurs in various parts of the body, and typical diseases include dry eyes (dry eyes), dry mice (dry mouth), dry skin (dry skin), Sjogren's syndrome, driver jain, etc. are included, and accompanying these symptoms, various systemic symptoms such as difficulty in taste, difficulty in swallowing, dental caries, periodontal disease, sleep disorder, constipation, joint pain, etc. come to be complained. In particular, in recent years, with the rapid spread of computers, the number of patients complaining of dry eye has increased rapidly, which has become a social problem.

  Dry eye is a disorder in which keratoconjunctival epithelial cells are damaged due to quantitative or qualitative abnormalities of tears, and symptoms such as dry eyes, eye pain, redness of the eyes, and eye discomfort. Accompany. In addition, 60% of eyestrain patients are said to be accompanied by dry eyes, and prevention or improvement of dry eyes is important in preventing or improving eyestrain.

  Sjogren's syndrome, a typical disease of dry syndrome, is an autoimmune disease mainly characterized by dry eyes and dry mouth, and exhibits various systemic symptoms. In addition to Sjogren's syndrome, these dry syndromes are also caused by stress, age-related changes, and the use of various drugs (anticholinergic drugs, antihistamines, antipsychotics). In particular, stress and age-related changes cause a decrease in water secretion capacity throughout the body.

  The treatment of dry syndrome is currently centered on symptomatic treatment. For example, in the treatment of dry eye, instillation of artificial tears for the purpose of replenishing deficient water and sodium hyaluronate for the purpose of retaining water are the main treatment methods, but sufficient treatment methods have been established. Not.

  On the other hand, in the case of constipation, lack of water in the intestinal tract may cause onset, and by increasing the water in the intestinal tract, constipation is resolved by improving the movement of the intestinal tract.

  Such dry syndrome is considered to be improved if water secretion in the living body can be promoted, but no preventive or therapeutic agent having both efficacy and safety has been known so far.

  Conventionally, hyaluronic acid accumulation promoters containing herbal extracts such as aloe vera, rakanka and eucommia as active ingredients have been disclosed as drugs for symptoms such as dry eye containing herbal medicines as active ingredients (see Patent Document 1).

  The herbal medicine (Syogyo) is a dried product of immature or mature fruits of the leguminosae (Leguminosae) honey beetle (Gleditsia sinensis LAMARCK), and its pharmacological effects such as expectorant and diuretic effects are known Non-patent document 1). However, wrinkles are not known to promote water secretion, constipation based on this, and to improve dry eye.

JP 2003-238432 A Namba Tsuneo, “Wakan Encyclopedia [I]”, Yoikusha, p.248-249

  An object of the present invention is to provide a prophylactic or therapeutic agent for dry syndrome by providing a natural product-derived water secretion promoter having high safety and sufficient effects.

  As a result of intensive studies to solve the above-mentioned problems, the present inventors have found that certain herbal medicines or extracts thereof have an excellent water secretion promoting action, and have completed the present invention.

That is, the present invention
(1) A preventive or ameliorating agent for dry syndrome, characterized by containing sputum.
(2) A water secretion promoter characterized by containing koji.
(3) A therapeutic or prophylactic agent for constipation, characterized by containing sputum.
(4) A therapeutic or prophylactic agent for dry eye, comprising wrinkles.
(5) An eye drop composition characterized by blending wrinkles.
(6) An eye drop for treating or preventing dry eye, characterized by comprising wrinkles.
(7) Intestinal water secretion promoter characterized by blending sputum (8) A lacrimal secretion promoter characterized by blending sputum.

  It was found that sputum used in the present invention has an action of promoting secretion of intestinal water and promoting secretion of tears.

  In the present invention, cocoon is a crude drug powder or extract obtained by pulverizing immature fruits or mature fruits of legumes. The extract referred to here includes an extract extracted from a herbal medicine using water, a polar solvent, or a mixture thereof, a dry extract, a flow extract, and the like.

  The dose of sputum in the present invention can be appropriately increased or decreased in consideration of age, gender, body weight, etc., but is usually 100 mg to 50 g, preferably 500 mg in the case of an oral drug as an active ingredient equivalent per day for an adult. In the case of a parenteral preparation, it is 0.01 mg to 5 g, preferably 0.05 mg to 2 g.

  In the present invention, vitamins, amino acids, excipients, pH adjusting agents, cooling agents, suspending agents, antifoaming agents, thickening agents, solubilizing aids, in a qualitative and quantitative range that does not impair the effects of the invention. Agents, disintegrants, binders, lubricants, antioxidants, coating agents, coloring agents, flavoring agents, surfactants, plasticizers, fragrances, etc. Oral or parenteral preparations such as capsules, powders, granules, chewable tablets, dry syrups, eye drops, nasal drops, creams, lotions, gels, ointments, patches, and emulsions can be used.

  Hereinafter, the present invention will be described in detail with reference to examples and test examples.

  The buds were immature fruits of Chinese cabbage from Hubei Province, China.

  Shred 500g of bulk drug substance, add 50 volumes of 50v / v% ethanol, extract by heating at about 80 ° C, distill off ethanol under reduced pressure after filtration, and perform further concentration. I got an extract.

  200 mg of the koji extract obtained in Example 1 was dissolved in 90 mL of physiological saline, and the pH was adjusted to 7.4 using borax. The total volume was made up to 100 mL using physiological saline, and sterile eye drops were obtained by filter sterilization. The osmotic pressure at this time was 296 mOsm.

Test example 1
For the test, 10-week-old Wistar male rats (Nippon Charles River) were used.

  Rats were given the gut extract obtained in Example 1 at a dose of 1.5 g / kg (raw drug equivalent) into the duodenum, and after 15 minutes, 30 minutes, 45 minutes, and 60 minutes It was measured. In addition, water was administered to the control group.

  For the measurement of lacrimal secretion, phenol red thread (Zonquick (trade name), manufactured by Menicon Co., Ltd.) was used, one end of which was inserted into the conjunctival sac of the rat for 1 minute, and the length of the tear that soaked into the thread Was measured with calipers, and the amount of lacrimal secretion was determined from the cumulative value. The number of cases in all groups was 10.

  The results are shown in FIG.

  As is apparent from FIG. 1, the lacrimal secretion group increased with time in the sputum administration group as compared with the control group, and a significant increase in tear secretion was confirmed 60 minutes after administration.

  As a result, it became clear that sputum prevents or improves dry eye because it promotes lacrimation.

Test example 2
In the test, a male Japanese white rabbit (Kitayama Labes) having a body weight of about 2.5 kg was used. In rabbit eyes, 50 μL of 0.4 w / v% oxybuprocaine hydrochloride was instilled twice at intervals of 3 minutes, and 3 minutes later, 50 μL of the eye drop obtained in Example 2 was instilled into the conjunctival sac. A 3 w / v% ATP solution was used as a positive control drug, and physiological saline was used as a control drug.

  Tear secretion volume is 5 minutes, 10 minutes, 15 minutes, 25 minutes and 30 minutes after instillation of eye drop sample, tear fluid is collected by inserting one end of Schirmer test paper into the conjunctival sac for 1 minute, The length was measured with a caliper and obtained from the accumulated value. The number of cases in all groups was 6.

  The results are shown in FIG.

  As is clear from FIG. 2, the lacrimal secretion was promoted in the 3 w / v% ATP solution as the positive control drug and the eye drop of the present invention. As a result, it became clear that sputum prevents or ameliorates dry eye by promoting tear secretion.

Test example 3
For the test, SD male rats aged 8 weeks were used.

  Rats fasted overnight were orally administered with the koji extract obtained in Example 1 at a dose of 1.5 g / kg (in terms of crude drug), and 1 hour later, the abdomen was opened, and both ends of the small intestine were ligated, and the intestine was removed. The extracted contents of the intestinal tract were filtered by centrifugation and the weight of water in the centrifuge tube was measured.

  Distilled water was orally administered to the rats in the control group, and the same treatment and measurement as the test drug were performed. The number of cases in all groups was 5.

  The results are shown in FIG.

  As is apparent from the figure, administration of sputum extract significantly increased intestinal endocrine secretion, and it was revealed that sputum has a preventive or ameliorating effect on constipation.

Test example 4
For the test, 10-week-old Wistar male rats (Nippon Charles River) were used. Rats were administered the sputum extract obtained in Example 1 into the duodenum at a dose of 1.5 g / kg (in terms of drug substance), and the vaginal action was visually evaluated.

  In the vaginal administration group, 10 cases out of 10 showed a gagging effect within 60 minutes after vaginal administration. These results revealed that sputum prevents or improves constipation.

  According to the present invention, provision of pharmaceuticals having preventive or ameliorating effects on dry syndrome, dry eye, constipation, etc., or functional foods, foods for specified health use, cosmetics, etc. for people who are concerned about dry syndrome, dry eyes, constipation, etc. Became possible.

It is the figure which showed the lacrimal secretion promotion effect | action of a cocoon extract, the amount of tear secretion (mm) was shown on the vertical axis | shaft, and the measurement time (minute) was shown on the horizontal axis | shaft. It is the figure which showed the lacrimal secretion promotion effect | action of a cocoon extract, the amount of tear secretion (mm) was shown on the vertical axis | shaft, and the measurement time (minute) was shown on the horizontal axis | shaft. It is the figure which showed the intestinal endocrine promoting effect of the koji extract, the intestinal endocrine secretion amount (g / site) was shown on the vertical axis, and each sample was shown on the horizontal axis.

Claims (5)

A therapeutic or prophylactic agent for constipation, characterized by containing sputum. A therapeutic or prophylactic agent for dry eye, characterized by containing wrinkles. An eye drop for treating or preventing dry eye, characterized by comprising wrinkles. An intestinal hydration promoter characterized by blending salmon. A lacrimal secretion promoter characterized by containing sputum.

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