JP2005298450A - Composition for preventing or treating climacteric syndrome - Google Patents

Abstract

[PROBLEMS] To include general malaise caused by the disruption of female hormone balance such as climacteric disorder, juvenile climacteric disorder, premenstrual syndrome (PMS), hot flash, cold, irritability, anxiety, swelling, low back pain, breast pain, acne, etc. Provided is a prophylactic or therapeutic drug for climacteric syndrome, which is extremely effective for indefinite complaints, sexual pain and urinary incontinence due to skin elasticity reduction, urogenital atrophy, hyperlipidemia, obesity, and osteoporosis.
[MEANS FOR SOLVING PROBLEMS] For preventing or treating climacteric disorder, comprising at least one selected from the group consisting of fennel, oxon, seisei, auren, goshuyu, sojutsu, soyou, spruce, clove, yokuinin, and ryokyo. Composition.
[Selection figure] None

Description

  The present invention relates to a preventive or therapeutic agent for climacteric syndrome or the like containing a crude drug.

  Female hormone is a steroid hormone that governs reproductive function, and is a general term for estrogen (follicular hormone) and progesterone (luteal hormone). Among them, estrogen is known to play a central role in the development and function maintenance of female genital organs, and is used as a general term for hormones that exhibit estrus and similar substances. Naturally, there are estrone, estradiol, estriol, and estetrol, and estradiol is the main one. Synthetic estrogens having the same biological activity are also known, and estrogens have a stilbene structure, except for some synthetic forms such as stilbesterol.

  The source of estrogen is mainly ovarian granulosa cells, but it is also secreted from the fetal placenta, adrenal gland, and ovary during pregnancy. Estrogen secretion from the ovary is governed by gonadotropins secreted from the anterior pituitary gland, but conversely, estrogen has a feedback effect on the pituitary gland type, and the interaction between them establishes the sexual cycle (See Non-Patent Document 1 above).

Estrogen works through its receptors, and the main physiological functions are endometrial growth, myometrial development, secondary sexual characteristics, mediation of menstrual cycle, maternal change during pregnancy, mammary gland For example, promotion of growth and secretion of the tube.
In addition, since estrogen has receptors in various tissues as well as the target tissue diencephalon-anterior pituitary gland-genitals and mammary glands, not only the above-mentioned effects on reproductive function, but also brain, cardiovascular, It acts on the skeleton, skin, and other systemic tissues, is deeply involved in the health of adult women, and is considered a hormone that creates women (see Non-Patent Document 2).

  This hormone deficiency or hormonal imbalance can cause abdominal pain, swelling, low back pain, abdominal bloating, breast pain, acne, anxiety, irritability and other symptoms such as premenstrual syndrome (PMS), menstrual abnormalities, and menopause. Invited, and if endogenous estrogen continues to decline, it is said that skin elasticity declines, sexual pain and urinary incontinence due to urogenital atrophy, hyperlipidemia (change in lipid metabolism), obesity, osteoporosis, etc. Yes. In women about 20 to 40 years old, due to excessive stress and diet associated with social advancement, the function is reduced and the hormone balance is disrupted, resulting in a decrease in endogenous hormones. Since the symptoms are similar to those of climacteric disorder, it is called juvenile climacteric disorder and the disease is increasing. Thus, lack of hormone secretion or hormonal imbalance prevents women's QOL (see Non-Patent Document 3).

  However, currently used estrogen agonists have problems such as gastrointestinal disorders, thrombosis, uterine bleeding, liver disorders, etc., and uterine cancers and breast cancers may develop when administered for a long time. Known in Japan, only 2-3% of hormone replacement therapy (HRT) using estrogen for the purpose of treating climacteric disorder or the like (see Non-Patent Document 4). In addition, due to various risks, it has been reported that the test of the estrogen single administration group in WHI (Women's Health Initiative) has been discontinued (see Non-Patent Document 5), and anxiety about HRT is expanding. In recent years, understanding of the concept of hormonal balance, diseases associated with its malfunction, and how to cope with it has increased, and many women seek safety and convenience, and plants that contain estrogen agonists in line with their lifestyles. Taking medicines and health foods / supplements containing extracts or fractional ingredients. Plants, extracts and fractions containing estrogen active substances are referred to as phytoestrogens. For example, soy isoflavones such as genistein and daidzein (see Non-Patent Document 6), Pueraria Mirifica (Gaucurea) (see Non-Patent Document 7) , Red clover (see non-patent document 8), black cohosh (see non-patent document 9), licorice (licorice) (see non-patent document 8), kudzu root, yokuinin (see non-patent document 10), etc. also have an estrogen-like action. It has been reported.

Supervised by Kazutomo Imabori and others, "Encyclopedia of Biochemistry", Tokyo Chemical Doujin, 1990, p. 172 Edited by Akita Suzuki et al., “Estrogen-Action from a New Perspective-” Medical View, 1999, p. 10 Yuji Takeya, “Women and Preventive Medicine”, Nakayama Shoten, 1998, p. 239 Edited by Akita Suzuki et al., “Estrogen-Action from a New Perspective-” Medical View, 1999, p. 68 NIH Asks Participants in Women's Health Initiative Estrogen-Alone Study to Stop Study Pils, Begin Flow-up Phaseb. D. , Director of the Women's Health Initiative and Acting Director of the National Heart, Lung, and Blood Institute, NIH News, http: //www.press.go. -03-02.htm E. Cheng et al., Science, 120, 575, 1954 S. Chansakaow et al., Plant Med, 66, 572, 2000 D. T.A. Zava et al., Proc. Soc. Exp. Biol. Med. 217, 369, 1998 Z. Liu et al., Wei Sheng Yan Jiu, 30, 77, 2001 Edited by Akita Suzuki et al., “Estrogen-Action from a New Perspective-” Medical View, 1999, p. 114

  The problems of the present invention include general malaise, hot flashes, coldness, irritability, anxiety, swelling, low back pain, breast pain, caused by disruption of female hormone balance such as menopause, juvenile menopause, and premenstrual syndrome (PMS). Provides prophylactic or therapeutic agents for menopausal syndromes that are extremely effective for low-side effects such as acne, acne, and sexual sexual pain and urinary incontinence due to atrophy of the genitourinary organs, hyperlipidemia, obesity, and osteoporosis It is to be.

  The present inventors have found that administration of a crude drug having an estrogen-like action is extremely effective for the prevention or treatment of climacteric syndrome and completed the present invention.

  One aspect of the present invention is a prophylactic or therapeutic agent for climacteric disorders comprising at least one member selected from the group consisting of fennel, oxon, seisei, auren, goshuyu, sojutsu, soyou, spruce, clove, yokuinin, and ryokyo. It is a composition.

  Another aspect of the present invention is a juvenile menopause characterized by containing at least one member selected from the group consisting of fennel, oxon, seisei, auren, goshuyu, sojutsu, soyou, spruce, clove, yokuinin, and ryokyo. It is a preventive or therapeutic agent composition for a disorder.

  Another aspect of the present invention is a premenstrual syndrome characterized by containing at least one member selected from the group consisting of fennel, oxon, seisei, auren, goshuyu, sojutsu, soyou, spruce, clove, yokuinin, and ryokyo. It is a preventive or therapeutic agent composition.

  The present invention improves the indefinite complaints and pathological changes caused by the imbalance of female hormone Bon balance and estrogen deficiency, general malaise, indefinite complaints such as hot flashes, coldness, irritability, anxiety, swelling, and reduced skin elasticity It has become possible to provide pharmaceuticals and the like effective for the treatment and prevention of sexual intercourse pain, urinary incontinence, hyperlipidemia, osteoporosis and the like due to urogenital atrophy.

In the following, fennel, oxon, seisei, auren, goshuyu, sojutsu, soyou, spruce, clove, yokuinin, and ryokyo used in the present invention will be described.
Fennel is the fruit of the Umbelliferae fennel Foeniculum vulgare Miller.

  Ogon (Yellow Gon) is the root excluding the pericarp of Labiatae, Scutellaria baicalensis Georgi.

  Ousei (yellow spirit) is the rhizome of Polygonatum sibiricum (Liliaceae).

  Ouren (Yo Ren) is a rhizome from which most of the roots of Ranunculaceae's Coptis japonica or other related plants are removed.

  Goshuyu is a fruit of the Rutaceae Goshuyu Evodia rutaecarpa or Evodia officinalis.

  Sojutsu (蒼朮) is the rhizome of Compositae, Atractylodes lancea or Atractylodes chinensis.

  Soyo (Soyo) is the leaf and branch of Perilla frutescens Britton or other related plants of Labiatae.

Spruce (orange peel) is a mature fruit of Citrus aurantium L. or Daidai C.aurantium L.var.daidai of Rutaceae.
Clove is a spider of Syzygium aromaticum Merrill (Eugenia caryophyllata Thunberg) of Myrtaceae.

  Yokuinin is a seed excluding the seed coat of Gramineae columbum coix lacryma-jobi.

  Ryokyo is a rhizome of Alpinia officinarum of Zingiberaceae.

  Fennel, Ogon, Ousei, Auren, Goshuyu, Sojutsu, Soyo, Spruce, Clove, Yokuinin, and Ryokyo may be herbal medicines or extracts. The extract may be any of water extract, flow extract, soft extract, dry extract, and tincture.

  The composition of the present invention is used for the prevention or treatment of indefinite complaints and climacteric disorders, juvenile climacteric disorders and premenstrual syndrome caused by female hormone imbalance.

  The effective dose of Fennel, Ogon, Ousei, Oren, Goshuyu, Sojutsu, Souyou, Spruce, Clove, Yokuinin, and Ryokyo is 50 mg to 10,000 mg per day for healthy adults, preferably 100 mg to 5000 mg as healthy adults. is there.

  The composition of the present invention contains at least one of Fennel, Ogon, Ousei, Ouren, Goshuyu, Sojutsu, Soyo, Spruce, Clove, Yokuinin, and Ryokyo, and other known additives, for example, as needed. Mixing the form, disintegrating agent, binder, lubricant, antioxidant, coating agent, coloring agent, flavoring agent, surfactant, plasticizer, etc., in a conventional manner, granules, powders, capsules, Oral preparations such as tablets, dry syrups and liquids can be prepared.

  Furthermore, preference can also be given by mixing another physiologically active ingredient, a mineral, a vitamin, an amino acid, a hormone, a nutrient component, a fragrance | flavor, etc. as needed. Herbal medicines are not particularly limited, but Izui, Yakukaku (Ikarisou), melancholy, glaze, Ezokogi (Sashigoka, Gokahashi), Yonji, Yongxiao, Jaundice, Jaundice, Distant, What's 烏, Description , Musk, kudzu, valerian, carocon, dried cocoon, licorice, bellflower, bellflower root, cocoon, cocoon, coconut leaf, coconut leaf, agate Ginseng, Katsuki, Kobuk, Beef, Gumiko, Pepper, Torikone, Saiko, Spicy, Ishizuchi, Yamiko, Yam, Yamashiko, Seiyo, Sanroku, Yamana, Yamaboshi, Sanriku, Yamakage , Western mountain robe, mountain medicine, ground bone skin, ginger, shrunk sand, serpent bed child, Sadako, glaze, sasang, sone, urma, commercial land, ground yellow, mature ground yellow, agar, river kyu, river bone, river Crust, persimmon, white mulberry, radish, stone persimmon, stone persimmon, stone bone, bone graft, pre-wheat, persimmon white persimmon, continuation, large persimmon, large persimmon, soybean Ginseng, bamboo ginseng, Chen skin, Toki, Tochu, party ginseng, citron, Taojin, ginseng, 巴戟 天, anti-nasal, Mumon winter, white shrimp, birch, coral, bon bonsai, self-protection, Koei Yin, prosthetic fat , Muirapuama, woody incense, peony skin, benevolent grass, masochist, longan, meat, royal jelly, licorice and the like.

  Hereinafter, the present invention will be described more specifically with reference to examples and test examples. In addition, when each herbal medicine is blended as an extract, the amount of the crude drug equivalent is shown in parentheses.

Test example 1
Experimental materials: 30% ethanol extract of estradiol and fennel, oxon, seisei, ouren, goshuyu, shujutsu, soyou, spruce, clove, yokuinin, ryoko.
Experimental animals: Wistar female rats (10 weeks old, purchased from Charles River)
Test method: Estrogen effect measurement test using uterine weight as an index The estrogen effect measurement test using uterine weight as an index was performed according to the method of Ishimi et al. (Y. Ishimi et al., Endocrinology, 140, 1893, 1999). That is, in an aseptic environment, the rat was anesthetized with pentobarbital, the back was incised, the ovary was removed (hereinafter referred to as “OVX”), and after 30 days of OVX, a 30% ethanol extract of the herbal medicine described in the above experimental material ( Suspension in 0.5% sodium carboxymethyl cellulose and 0.2 mL / 100 g) was orally administered once a day for 13 consecutive days. One day after the final oral administration, laparotomy was performed under pentobarbital anesthesia, the uterus was removed, the content liquid was removed, and the uterine weight was measured. In the normal group, the back was incised in the same manner as described above, the ovary was treated pseudo, returned to the body, and then sutured. The normal group and the control group were administered with 0.5% carboxymethylcellulose sodium at a dose rate of 0.2 mL / 100 g.

[Experimental results] Effects of Fennel, Ogon, Ousei, Ouren, Goshuyu, Sojutsu, Soyou, Spruce, Clove, Yokuinin, Ryokyo The uterine weight of rats treated with OVX was significantly reduced compared to the normal (sham surgery) group did. On the other hand, fennel 500 mg / kg, oxon 500 mg / kg, horsetail 500 mg / kg, auren 500 mg / kg, clove 500 mg / kg, and yokuinin 1000 mg / kg significantly suppressed the decrease in uterine weight due to ovariectomy. kg, Sojutsu 500 mg / kg, Soyo 500 mg / kg, Spruce 500 mg / kg, and Ryokyo 500 mg / kg showed a tendency to suppress and an estrogenic effect was observed. On the other hand, estradiol suppressed the decrease in uterine weight at a dose of 0.1 mg / kg.

According to the present invention, development of a preventive or therapeutic agent for climacteric disorder, juvenile climacteric disorder and premenstrual syndrome suitable for long-term oral administration is expected.

Claims (3)

  A prophylactic or therapeutic composition for climacteric disorders, comprising at least one member selected from the group consisting of fennel, oxon, seisei, auren, goshuyu, sojutsu, soyou, spruce, clove, yokuinin, and ryokyo.   A prophylactic or therapeutic composition for juvenile climacteric disorders, comprising at least one selected from the group consisting of fennel, oxon, seisei, auren, goshuyu, sojutsu, soyou, spruce, clove, yokuinin and ryokyo . A prophylactic or therapeutic agent composition for premenstrual syndrome, comprising at least one member selected from the group consisting of fennel, oxon, seisei, auren, goshuyu, sojutsu, soyou, spruce, clove, yokuinin, and ryokyo.