KR101841553B1 - Composion containing ornithine or its salt with the effect of improving sexual function - Google Patents

Abstract

Ornithine or ornithine salt, and is effective for improving male sexual function without side effects.

Description

[0001] The present invention relates to a composition for improving sexual function comprising ornithine or ornithine salt,

The present invention relates to a composition for improving sexual function, and more particularly to a composition for improving sexual function comprising ornithine or ornithine salt.

The most common sexual dysfunction is erectile dysfunction. In general, erectile dysfunction is known to be caused by a psychological cause, a physiological cause, or a combination of these two factors. In recent years, physiological causes are understood to be the most important factors of erectile dysfunction, and accordingly, many studies on physiological mechanisms of penile erection have been made.

Erectile dysfunction refers to a phenomenon in which the arteries in the corpus cavernosum are relaxed, filled with blood, relaxed in the smooth muscle, and pressure of the veins causes the pressure of the corpuscles to rise because the blood flow can not escape.

Nitric oxide (NO) is known to be involved in the erection process. The substance that produces nitric oxide (NO) binds to receptors on the endothelial cell membrane to increase the concentration of free calcium in endothelial cells, Thereby promoting the synthesis of nitrogen monoxide (NO) and the glass. The liberated nitric oxide (NO) enters the cavernosal smooth muscle cells and activates the guanylate cyclase of the smooth muscle to increase the production of cGMP, which causes smooth muscle relaxation by increasing cGMP, It is an erection.

There are three types of erectile dysfunction drugs currently on the market depending on their mechanism of action. The first is an inhibitor of an enzyme called phosphodiesterase (PDE-5), which is present in erectile tissue. Viagra (sildenafil citrate), Levitra (vardenafil) and Cialis (tadalafil) The second is prostaglandin E1 agonist that directly acts on the erectile tissues to expand the blood vessels. Examples are Caverject, MUSE, Befer which are mainly composed of alprostadil. Third, Dopamine agonists acting on dopamine D1 / D2 receptors, such as Urprima, which is predominantly apomorphine. In addition, there are a-adrenoceptor antagonists, guanylate cyclase stimulators, and serotonin (5-hydroxytryptamine) receptor agonists.

However, most of the erectile dysfunction drugs developed so far require serious attention because serious side effects are reported, and they are classified as special management medicines because of the problem of misuse. Viagra, a treatment for erectile dysfunction through inhibition of PDE-5, causes side effects such as visual impairment and blood sugar increase in patients with heart disease. Levitra may cause headache, nausea, facial flushing, etc., Blood pressure may drop dramatically when a patient taking a nitrate agent is taking this drug.

Therefore, it would be necessary to develop a new sexual function-improving agent which can minimize side effects.

Korean Unexamined Patent Publication No. 10-2004-0048166 (published on June 07, 2004) discloses a composition for improving sexual function. More specifically, it relates to a composition for improving sexual function, A hydrolyzate of phloroglucinol, which is a strong antioxidant for protecting vascular endothelial cells, and a seaweed extract powder, which essentially contains fucosterol, which regulates the activity of ACE (angiotensin converting enzyme), which is known to inhibit erection by causing vasoconstriction The present invention relates to a composition for improving sexual function, which is composed of various vegetable raw materials, which provide essential nutrients for maintaining energy and sexual function, and showing excellent effects on sexual function without side effects.

It is an object of the present invention to develop and provide a new sexual function improving agent which can minimize the occurrence of side effects in vivo.

The present invention provides a composition for improving sexual function, which comprises an ornithine or ornithine salt as an active ingredient. Ornithine is recognized as a food in Japan and Thailand, and is a safe ingredient used as a dietary supplement in the United States and Europe. In the meantime, liver function improvement, fatigue recovery, skin nutrition, and hangover resolution has been known functions, such as sexual function improvement is not known.

Meanwhile, in the present invention, the sexual composition of the present invention may be a food or medicine.

On the other hand, in the present invention, ornithine may be L-ornithine. Since the form existing in the natural state is L-type, L-type ornithine has an advantage that it is easy to obtain.

In the present invention, the ornithine salt may be in the form of ornithine coupled with an oral or pharmaceutically acceptable salt. Examples of the ornithine salt include ornithine hydrochloride, ornithine sulfate, ornithine hydrochloride, ornithine aspartate, Glutamic acid salt, ornithine vitamin C salt, and ornithine alpha ketoglutaryl acid salt.

Meanwhile, the composition for improving sexual function of the present invention may contain at least one selected from vitamin B3, vitamin B6, vitamin E and zinc as an auxiliary component. These components are the main components of the semen, and are essential components for replenishing the amount of semen. The important fact that has been overlooked in relation to erectile dysfunction is that the existing erectile dysfunction treatment focused only on the erection itself and did not pay attention to the health of the human body, that is, the replenishment of semen after ejaculation. When men are full of semen, the sexual desire is stronger, and the foot function is improved by most men. Therefore, it is preferable that these components are added as auxiliary components in the present invention.

Meanwhile, the present invention provides a food composition for improving sexual function, which comprises ornithine or ornithine salt as an active ingredient, wherein the ornithine or ornithine salt is preferably 0.1 to 50 wt% It should be included. When the amount is less than 0.1% by weight, the effect is insufficient. When the amount is more than 50% by weight, the increase in the effect on the usage amount is insignificant, which is uneconomical.

In the food composition of the present invention, the ornithine or ornithine salt is suitably fed in an amount of 0.1 to 3 g per day, preferably 0.2 to 2.0 g per day.

Meanwhile, the food composition for sexual function improvement of the present invention can be formulated into granules, tablets, capsules, beverages, gums, circles and the like, , An alcoholic beverage, a drink, a vitamin complex, and other health supplement foods. However, the present invention is not limited thereto.

On the other hand, the present invention provides a pharmaceutical composition for improving sexual function, which comprises ornithine or ornithine salt as an active ingredient.

The content of ornithine or ornithine salt contained in the pharmaceutical composition for improving sexual function of the present invention is preferably adjusted according to the method of use of the preventive and therapeutic agent, the condition of the recipient, the kind of the disease and the severity of the disease. The content of ornithine or ornithine salt in the composition of the present invention may be 0.1 to 50% by weight, but is not limited thereto. However, if the content is less than 0.1% by weight, the effect of improving sexual function may be insufficient. If the content is more than 50% by weight, the rate of increase in effect relative to the amount of use may be low.

On the other hand, in the pharmaceutical composition for sexual function improvement of the present invention, the ornithine or ornithine salt is suitably used in an amount of 0.1 to 3 g, preferably 0.2 to 2.0 g, per day.

In addition, the pharmaceutical composition for improving sexual function of the present invention may further comprise a pharmaceutically acceptable carrier, diluent or excipient in addition to the active ingredient. Examples of usable carriers, excipients or diluents include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate, cellulose, methylcellulose, Microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate and mineral oil. These may be used singly or in combination.

On the other hand, the formulation of the pharmaceutical composition for sexual function improvement of the present invention may be in a preferable form depending on the method of use, and may be a method known in the art so as to provide rapid, sustained or delayed release of the active ingredient after administration to mammals To be formulated. Examples of specific formulations include those selected from granules, POWDERS, SYRUPS, LIQUIDS AND SOLUTIONS, INJECTIONS, CAPSULES, PILLS, soft or hard gelatin capsules, It can be either.

On the other hand, the dose of the pharmaceutical composition for sexual function improvement of the present invention is preferably determined in consideration of the administration method, the age, sex and weight of the recipient, severity of disease, and the like. For example, the pharmaceutical composition for improving sexual function of the present invention can be administered in an amount of 0.1 to 3 g per day on the basis of an adult male, based on the active ingredient ornithine. However, the dosage is merely an example, and may be changed depending on the condition of the recipient.

The composition containing the ornithine of the present invention can improve male sexual function without side effects as confirmed in the following experimental examples.

Hereinafter, the present invention will be described in detail with reference to the following Examples, Experimental Examples and Formulation Examples. However, the scope of the present invention is not limited to the following examples and formulations, and includes modifications of equivalent technical ideas.

[Example 1: preparation of ornithine hydrochloride]

10 Kg of L-arginine was dissolved in 70 L of purified water and arginine derived from Bacillus Caldovelox was added at a rate of 50,000 U per Kg of arginine, followed by stirring at 50 DEG C for 24 hours.

After that, hydrochloric acid was added to lower the pH to 5, and the mixture was heat-treated at 70 ° C for 10 minutes and then cooled to 50 ° C.

Thereafter, 300 g of activated carbon was added and decolorized for 2 hours, followed by filtration with a press filter. The filtrate was concentrated under vacuum to 55 [deg.] Bricks.

Thereafter, the concentrate was slowly added to the concentrate to crystallize, followed by dehydration and drying. 7Kg of ornithine hydrochloride powder having a purity of 98.5% was obtained through the above process.

[Example 2: preparation of ornithine premix]

1800 g of the ornithine prepared in Preparation Example 1, 8 g of vitamin B3, 1 g of vitamin B6, 15 g of vitamin E and 6 g of zinc were put into a V-mixer and mixed for 30 minutes to prepare an ornithine premix.

[Experimental Example 1: Measurement of sperm count as male sexual function improvement effect]

The effects of the male sexual function improving food obtained in the present invention were examined in five males aged 45 to 55 years whose sexual function was lowered. Sperm was collected 15 days after ingestion of the ornithine powder prepared in Preparation Example 1 twice a day, and compared with the number of sperm samples collected before 15 days before consumption.

Comparison of sperm count in semen before and after ingestion 15 days before ingestion After 15 days of ingestion Number of sperm (average of 5 people) 15,000,000 / mL 25,000,000 / mL

[Experimental Example 2: Experiment of Male Sexual Function Improvement Effect]

The effects of the male sexual enhancement food developed through the present invention were examined in 30 male males aged 45 to 55 years. The powder prepared in Examples 1 and 2 and the two control groups were fed twice daily for 2 days (Redmax Co., Ltd. - Korea Ginseng Corp. - 70 mL / capsule) for 40 days, and the sexual function was improved for 30 days from 10 days after ingestion And compared with 30 days before ingestion.

Among the 15-question International Index of Erectile Function (a validated, multidimensional, self-administered questionnaire) used for clinical evaluation of erectile dysfunction and its outcome, (Questions 1 to 5, 15, possible total score 1 to 30), maximum ability (questions 9 and 10, possible total score 0 to 10), libido (questions 11 and 12; possible total scores 2 to 10) ; Possible total score of 0 ~ 15) and total satisfaction (question 13, 14; possible total score 2 ~ 10).

The scores in each field were obtained by adding scores for each question. In the International Index, the mean score of foot function increased by 37% (P <0.01) from 13.5 before ingestion to 18.5 after ingestion (Table 2).

The mean scores of orgasmic function, sexual desire, sexual satisfaction, and overall satisfaction were also significantly increased by ingestion. Particularly, in the case of sexual desire, the test group consuming the premix of Example 2 was superior to the control group of arginine and redmax, which is thought to be due to the faithful supplementation of the semen.

After ingestion, mean score of foot function index 30 days before ingestion 10 to 40 days after ingestion Ornithin Premix Arginine Red Max Foot function ¹

13.5 ± 0.8 18.5 ± 1.8 21.6 ± 2.0 18.3 ± 2.0 22.5 ± 2.1 Maximum capacity ² 5.4 ± 0.4 6.4 ± 0.4 7.1 ± 0.4 6.8 ± 0.4 7.0 ± 0.4 Sexuality ³ 6.5 ± 0.5 7.2 ± 0.4 8.5 ± 0.4 7.0 ± 0.4 7.8 ± 0.4 Sexual Satisfaction ⁴ 4.8 ± 0.5 6.5 ± 0.5 9.8 ± 0.6 6.3 ± 0.5 7.5 ± 0.5 Overall Satisfaction ⁵ 3.9 ± 0.4 5.5 ± 0.4 6.6 ± 0.4 5.3 ± 0.4 6.3 ± 0.5 ^{1 to} 6 questions available Total score: 1 to 30 points
² 2 questions possible Total score: 0 ~ 10 points
³ 2 questions possible Total score: 2 ~ 10 points
⁴ 3 questions possible Total score: 0 ~ 15 points
⁵ 2 questions possible Total score: 2 ~ 10 points

[Preparation Example 1: Preparation of pharmaceutical composition for improving sexual function]

In Production Example 1, a pharmaceutical composition for improving sexual function was prepared as follows.

(1) Manufacture of powders

2 g of ornithine hydrochloride was mixed with 1 g of lactose and filled in an airtight container to prepare a powder.

(2) Preparation of tablets

100 mg of ornithine hydrochloride, 100 mg of corn starch, 100 mg of lactose and 2 mg of magnesium stearate were mixed and tableted according to a conventional tablet preparation method.

(3) Manufacture of capsules

100 mg of ornithine hydrochloride, 100 mg of corn starch, 100 mg of lactose and 2 mg of magnesium stearate were mixed and filled in gelatin capsules to prepare capsules.

(4) Injection preparation

100 mg of ornithine hydrochloride was dissolved in an appropriate amount of distilled water for injection and the pH was adjusted to about 7.5. Then, the solution was filled and sterilized in a 2-ml volume ampoule to prepare an injection.

[Preparation Example 2: Preparation of food composition for sexual function improvement]

In Production Example 2, a food composition for sexual function improvement was prepared as follows.

(1) beverage manufacturing

0.0001% by weight of chitosanic acid amide, 0.0004% by weight of nicotinic acid amide, 0.0001% by weight of sodium riboflavin hydrochloride, 0.0001% by weight of pyridoxine hydrochloride, 0.001% by weight of inositol, 0.002% by weight of orotic acid, 1% by weight of ornithine hydrochloride, And the health drink was prepared by a conventional method.

(2) health supplement manufacturing

A mixture of 55% by weight of Spirulina, 10% by weight of guar gum enzyme hydrolyzate, 0.01% by weight of vitamin B1 hydrochloride, 0.01% by weight of vitamin B6 hydrochloride, 0.23% by weight of DL-methionine, 0.7% by weight of magnesium stearate, And 10% by weight of ornithine hydrochloride were mixed to prepare a refillable health supplement food by a conventional method.

(3) Manufacture of alcoholic beverages

Ornithine hydrochloride 0.5% (w / v) was added to the shochu and centrifuged at 7,000 rpm for 15 minutes under vacuum or mixed at 9,000 rpm using a high-speed mixer to prepare shochu containing ornithine.

Claims (5)

8 parts by weight of vitamin B3, 1 part by weight of vitamin B6, 15 parts by weight of vitamin E and 6 parts by weight of zinc relative to 1800 parts by weight of ornithine or Ornithine salt.
The method of claim 1,
L-ornithine. &Lt; / RTI &gt;
The method according to claim 1,
Ornithine hydrochloride, ornithine hydrochloride, ornithine sulfate, ornithine acetate, ornithine aspartate, ornithine glutamate, ornithine vitamin C salt or ornithine alpha ketoglutarylate. Composition.
8 parts by weight of vitamin B3, 1 part by weight of vitamin B6, 15 parts by weight of vitamin E and 6 parts by weight of zinc are mixed with 1800 parts by weight of ornithine or Ornithine salt.
2. The composition of claim 1,
Wherein the composition is a food.