KR101072175B1 - Compositions for the urinary dysfuction and edema containing decursin and/or decursinol angelate, or angelica extract containing decursin and/or decursinol angelate - Google Patents

Abstract

The present invention relates to a therapeutic agent for treating urination disorders and edema comprising a decoxin and / or a decosinol angelate, or a sugar extract which contains the decosin and / or decosinol angelate as an active ingredient.

Prostate hypertrophy and urinary incontinence using the composition for treating urination disorders and edema comprising the decosin and / or the decosinol angelate of the present invention, or the Angelica extract comprising the decosin and / or decosinol angelate as an active ingredient While having an excellent effect on the urination disorder disease and edema represented by the long-term use, it is possible to provide a safe, supplemental treatment and health supplements to improve the function of the human body safely without additional side effects.

Angelica Extract, Decusin, Decusinol Angelate, Prostatic Hyperplasia, Urination Disorder, Edema

Description

COMPOSITIONS FOR THE URINARY DYSFUCTION AND EDEMA CONTAINING DECURSIN AND A composition for treating urination disorders and edema, comprising decansin and / or decosinol and / or decansinol angelate as an active ingredient / OR DECURSINOL ANGELATE, OR ANGELICA EXTRACT CONTAINING DECURSIN AND / OR DECURSINOL ANGELATE}

The present invention relates to a therapeutic agent for treating urination disorders and edema comprising a decoxin and / or a decosinol angelate, or a sugar extract which contains the decosin and / or decosinol angelate as an active ingredient.

Urinary dysfuction is a condition involving difficulty in normal urination by any factor, especially benign prostatic hyperplasia (BPH) in men with aging and in women or men, except for prominent factors such as surgery and the use of certain drugs. Urinary incontinence is the leading cause of illness.

Prostatic hyperplasia is one of the most common benign species occurring in middle-aged men and is considered to be the second largest cause of hormonal imbalance due to aging and male hormones. Since prostatic hyperplasia is not a fatal disease, it is rare to progress seriously, but the prevalence is high in 60% of men in their 60s, and it interferes with daily life with urination disorders such as nocturia, residual urination, urgent need, and urination failure. In addition, secondary prostate problems such as edema, renal dysfunction, sleep disorders, sexual life, depression, etc., significantly reduce the quality of life, so most prostatic hyperplasia patients are treated to address urination disorders. .

Drug treatment for enlarged prostate is represented by α1-adrenergic receptor blockers such as prazosin and terazosin, finasteride, etc., which relieve urinary tract by relaxing muscles around the urethra to widen the urethra. 5-α reductase inhibitors, anti-male hormones, etc. may be used, but it may require considerable time to see the therapeutic effect (2-3 weeks to 6 months), or may have a decreased effect on long-term use. There was a problem that frequently causes side effects such as headache, tachycardia, sexual dysfunction.

Efforts have also been made to use herbal preparations to minimize these side effects, which are of interest to saw palmetto and β-sitosterol. Compared to the above drug therapy, the rate of causing side effects such as sexual dysfunction is low, but the pharmacological action has not been sufficiently verified, and it is recognized that the drug is insufficient.

Urinary incontinence is a condition that causes urine to go out and wet underwear regardless of my doctor, and 40% of all middle-aged women and older women have these symptoms, which leads to a prevalence and decreased quality of life comparable to men's prostate hypertrophy. Occurs in both.

In women, urinary incontinence often occurs due to abdominal pressure in the case of abdominal pressure during daily life due to fluctuations in the position of the bladder or weakening of the urethral sphincter, and abnormal contraction or overactive bladder of the bladder muscle. Urgent urinary incontinence is typical, and in men, urinary incontinence due to weakening of the urethral sphincter muscle due to aging and residual urination accompanied by enlarged prostate gland occurs. As a treatment method, there are drug therapies for stabilizing the smooth muscle of the bladder and increasing the contractile force of the urethral sphincter, but the effect is transient and insufficient, and in recent years, surgery, pelvic muscle movement, etc. are generally selected.

Overactive bladder, a concept recognized as a symptom common to enlarged prostate and urinary incontinence, is a recent term that refers to a phenomenon in which urine urges or becomes tired with aging regardless of gender, and in women, sphincter decline, and men In many cases, it is due to enlarged prostate, and especially in prostatic hyperplasia, it is known that 20% to 41% are accompanied by an overactive bladder.

At the time of aging and growing interest in the quality of life of the elderly, it is effective for urinary disorders such as prostate hyperplasia and urinary incontinence, which are the most prevalent aging diseases, and minimize the risk of side effects from long-term use. The demand is estimated to be very high.

In the pharmacological action of decursin, decursinol angelate, decurcinol, and / or two or more species of Angelica gigas, which are the main components of Korean Angelica gigas Nakai There has been much research on this. Among them, those effective for leukemia cancer cells (Patent Publication No. 2001-0080265), those having analgesic activity (Patent Registration Publication No. 10-0397950), and those effective for lung cancer and liver cancer (Patent Registration Publication No. 10-0187881). And a study which found that it acts as an inhibitor of renal toxicity when using an anticancer agent (Patent Publication No. 2000-0026683). In the above study, the ear extract containing Deceacin and / or Decasinol Angelate, or Decasin and / or Decasinol Angelate, which have renal damage prevention and renal function protection, was treated with protein kinase-C (PKC). In view of the activation, the inventors of the present invention presumed that this substance may have an action similar to that of the α1-adrenergic receptor blocker, and in this respect it will have a positive effect with respect to urination disorder and edema. However, there have been no studies on the urination and anti-edema effects of decansin and / or decusinol angelate, or the Angelica extract containing decusin and / or decusinol angelate. There have been no cases of application to urination disorders and edema diseases such as prostate hyperplasia and urinary incontinence.

In accordance with the above object, the present invention provides a therapeutic agent for treating urination disorders and edema comprising a sugar extract, which contains Decasin represented by the following Chemical Formula 1 or Decasin represented by the following Chemical Formula 1 as an active ingredient.                     

(1)

(One)

In addition, the present invention provides a therapeutic agent for treating urination disorders and edema comprising a Angelica extract containing Decusinol Angelate or Decusinol Angelate represented by Formula 2 as an active ingredient.

(2)

(2)

In addition, the composition of the present invention is composed of the decosinol represented by the following formula 3 to the sugar extract extract containing the above-mentioned decusin and / or decusinol angelate, or decosin and / or decusinol angelate It may further include one or more selected from the group.

(3)

(3)

The urination disorders include both primary and secondary urination disorders known to cause urination disorders, and among them, have the most desirable effect on prostatic hyperplasia or urinary incontinence. In addition, there is a desirable therapeutic effect in irritable bladder, urine control of children, and is effective in secondary symptoms known to accompany the disease or symptom, but is not limited thereto.

The edema disease includes both primary and secondary edema-induced diseases known to cause edema symptoms, and among them, shows the most desirable effect on lower extremity edema that occurs after surgery, after chemotherapy, or after radiation therapy.

The above-mentioned decusin, decosinol angelate or decosinol can be obtained by extracting, separating and purifying from Angelica gigas, and specific extraction and purification methods are described in the literature (Lee Ji-Joon et al., Biochemical Society, 1, 25-32). (1970); and Korean J. Pharmacogn ., 21, 64-68 (1990)) and Patent Registration No. 10-2385092, but is not limited thereto, even if the solvent, extraction conditions, etc. are different Any extraction method can be used to obtain cine, decosinol angelate or decosinol.

The Angelica extract may further include all salts, organic salts, complexes, and the like, which are known to be incidental in the extraction process, in addition to the above-mentioned decusin, decusinol angelate or decusin.

The decusin, decosinol angelate or decosinol can be synthesized and used as specific methods (Tetsuhiro Nemoto et al., Tetrahedron Letters , 41, 9569-9574 (2000); Lan Xie et al. J. Med) Chem ., 42, 2662-2672 (1999); Patent Application No. 2000-25749; and Patent Registration No. 10-0417624), but is not limited thereto, even if the synthesis conditions, such as the above decker Any synthetic method can be used to obtain cine, decosinol angelate or decosinol.

In the case of using the synthesized decusin, decosinol angelate, or decosinol as the composition for treating urination disorder and edema, all inorganic salts, organic salts, complexes, and the like, which are known to accompany the synthesis of the raw materials, are used. It may further include.

The above compounds are inorganic salts selected from the group consisting of sodium salts, potassium salts, magnesium salts, calcium salts or organic salts selected from the group containing lysine, ethanolamine, N, N'-dibenzylethylenediamine, It may be in the form of a pharmaceutically acceptable salt.

In addition, the present invention comprises a decancin and / or Decusinol Angelate, or a Angelica extract as the active ingredient of Decusin and / or Decusinol Angelate, and further comprises a pharmaceutically acceptable carrier or pharmaceutical additive Treatment for urination disorder and treatment for edema are provided.

In addition, the present invention includes a decancin and / or Decusinol Angelate, or a Angelica extract as the active ingredient of Decusin and / or Decusinol Angelate, and further comprises a pharmaceutically acceptable carrier or food additive Adjuvant agents and supplements with urination disorder treatment and edema treatment are provided.

The composition comprising the decancin and / or decusinol angelate used in the present invention, or the Angelica extract, which is used as an active ingredient of the decusin and / or decusinol angelate, according to the target disease, the purpose and the condition of the patient. The dosage can be changed and used, and it is preferable to administer 1 to 100 mg, more preferably 3 to 30 mg once per day, usually 1 deg. In addition, the above dosage may be administered orally or parenterally formulated.

In addition, a composition comprising a decancin and / or decusinol angelate, or a Angelica extract comprising the decansin and / or decosinol angelate as an active ingredient in the present invention, improves acne during the clinical trial process of the present inventors. Improvement and improvement of facial color, reduction of thyroid mass, improvement of urinary tract stones, hematuria and urination pain, improvement of ischemic vascular disease and peripheral disease, improvement of erectile dysfunction, improvement of physical strength, hair growth Effect, treatment effect for cystitis or bladder dysfunction after radiation treatment was confirmed. In this regard, further investigations by the inventors are underway.

Hereinafter, the present invention will be described in more detail with reference to Examples. However, these examples do not limit the scope of the present invention.

Example

<Target>

As shown in Table 1 below, 32 patients with benign prostatic hyperplasia, 15 patients with urinary incontinence, and 14 patients with various edema were subjected to clinical trials to evaluate the effect on the composition of the present invention.

TABLE 1

Target Patient ＼ Target Disease Benign prostatic hyperplasia Incontinence edema Number of patients 32 persons 15 people 14 people age 24 to 83 years 13 years old-81 years old
(13 years old male child) 56 years old-72 years old Disease period 1 month to 10 years 1 month to 10 years 1 month to 10 years

Detailed profiles of the 14 patients with edema are as follows.

3 cases: systemic edema patients with related diseases such as diabetes, hypertension, fatty liver

11 cases: Coronary surgery, cerebrovascular surgery, cardiac surgery

      Three Cases of Prostate Cancer Surgery

      A Case of Perineal Leg Edema After Bladder Cancer Surgery

      A Case of Lower Extremity Edema and Multiple Masses of the Thyroid after Cervical Cancer Surgery (In Same Patient)

      A Case of Multiple Mass of Axilla

      Two Cases of Edema After Radiation Therapy

<How to administer>

Formulation is made of a capsule containing 300 mg of Decusin and Decusinol Angelate mixture, using Decusin and Decusinol Angelate, obtained by culturing and extracting Korean Angelica extract as described in Patent Registration No. 10-0385092. It was. It was taken at about 9 am daily with about 50 ml of drinking water once a day for 3 weeks to 10 months.

<How to diagnose>

The following items were diagnosed and the results are shown in Table 2.                     

-paperweight

-Urination rate test (5 seconds before urination, 10-15 seconds during urination)

Urine test

Workplace check

Ultrasound screening (except for PSA positive patients)

Table 2

division compare effect Great usually No effect (according to IPSS) Enlarged prostate 91% improvement 21 people (67%) 8 people (24%) 3 people (9%) Incontinence 90% better 11 people (83%) 2 people (7%) 3 people (10%) edema 100% improvement 14 people (100%) 0 (0%) 0 (0%)

In the patients with enlarged prostate, the effect was judged as follows based on IPSS (International Prostate Symptom Score).

-Excellent: The effect appears within 1 day after drinking.

-Moderate (effective): It takes effect within 2-3 days after drinking.

-Invalid: No effect after 3-5 days after drinking.

The improvement effect was observed in 91% of patients 1 to 2 days after the administration of the composition of the present invention compared to the α1-adrenergic receptor blocker, which is known to have a 50-60% improvement in the National Prostate Symptom Score (IPSS) at 2 to 3 weeks of administration. The results showed that the improvement of symptoms was not smooth. The urinary tract was too narrow, the cyst was found in the prostate, the drunkard, the suspected bladder disease, and the diabetes were severe. .

Urinary incontinence showed a smooth treatment effect with an effective rate of 90%, except for patients with too long incontinence or suspected other related diseases. In this case, the results were cured by drinking twice.

In patients with edema, prostate hypertrophy treatment effect by α1-adrenergic receptor blockade was confirmed, and edema treatment effect was expected due to the same mechanism, but all 14 patients who participated in the experiment had a remarkable therapeutic effect. Got it. In patients with systemic edema as a related disease such as diabetes, hypertension, fatty liver, after drinking, remarkable weight loss and clinical value of related diseases such as blood sugar drop were improved, and multiple masses of thyroid or axilla were lost. . In particular, edema alleviation is particularly rapid in patients with lower extremity edema after surgery such as coronary arteries and radiation therapy, and is expected to be an alternative to edema alleviation after surgery and chemotherapy.

In either case, no side effects reported by α1-adrenergic receptor blockers, 5-α reductase inhibitors, or various edema treatment products, and any other side effects have not been reported for 10 months, thus making them a safe and effective treatment for urination disorders and edema. I confirmed it. It is remarkable that the improvement of the administration of the composition of the present invention is due to erectile dysfunction, which is a side effect accompanying prostatic hypertrophy, and is known to worsen during men's hormone treatment and seriously affect the quality of life of patients. .

Claims (14)

As an active ingredient, a mixture of decusin represented by the following general formula (1) and decosinol angelate represented by the following general formula (2), or decosin represented by the following general formula (1) and decosinol angelate represented by the following general formula (2) Comprising Angelica extract, therapeutic agent for treating urination disorders and edema.

(One) delete delete delete The composition for treating urination disorder according to claim 1, wherein the urination disorder disease is enlarged prostate or incontinence. The edema therapeutic composition according to claim 1, wherein the edema disease is lower limb edema developed after surgery, after chemotherapy, or after radiation therapy. delete delete delete delete delete A therapeutic agent for treating urination disorder, comprising decansin and decosinol angelate, or Angelica extract, which is an active ingredient of decosin and decosinol angelate, and further comprising a pharmaceutically acceptable carrier or medicament additive. Edema treatment. Treatment of urination disorders and edema due to urination disorders, including decansin and decusinol angelate, or Angelica extract, which is an active ingredient of decusin and decusinol angelate, and comprising a pharmaceutically acceptable carrier or food additive Adjuvant with therapeutic action. A supplement comprising a decancin and a decosinol angelate, or a Angelica extract comprising the decansin and decosinol angelate as an active ingredient, and comprising a pharmaceutically acceptable carrier or food additive.