KR20200058929A - A composition comprising an extract of combined natural products for treating and preventing Male Infertility - Google Patents

Abstract

Male infertility accounts for 50% of all causes of infertility, of which 30-45% are idiopathic with unknown cause. Decreased sperm quality, such as decreased sperm or reduced mobility, is responsible for male infertility, and effective treatments have not been established. A total of 16 infertile men take herbal medicines to improve sperm function for 10 weeks, and perform examination of semen. Statistically, sperm concentration, straight motility, and total number of sperm are significantly improved and no special side effects are found.

Description

A composition comprising an extract of combined natural products for treating and preventing Male Infertility}

The present invention relates to a pharmaceutical composition and a health functional food for the prevention and treatment of male infertility, and in detail, to improve the activity of sperm and increase the number of sperm at the same time, extract of a complex natural product having the effect of treating and preventing male infertility It relates to a pharmaceutical composition characterized in that it comprises as an active ingredient.

Male infertility is a condition in which a child cannot give birth due to male causes even though he has had a normal sex life for at least one year. About 15% of married couples are infertile, and the male cause is considered to be 40-60%. Male infertility can be caused by hormonal problems, including testosterone, problems with testicles due to exposure or infection or trauma toxins, sperm problems, or even abnormal sperm discharge.

Although many advances have been made in the treatment of infertility to date, male infertility treatments that improve sperm motility are absent, and the development of drugs that can improve pregnancy is also very low. In the prior art, despite medical and surgical treatment, L-carnitine is currently used as a drug capable of improving the quality of semen in men with poor quality of semen without knowing the cause, but it does not show a distinct effect.

Sperm motility can be a good indicator of sperm viability (Noran et al., 1998). Common indicators for evaluating sperm quality include sperm concentration, malformed sperm rate, live sperm rate, and semen amount. , pH, sperm initial vitality, and sperm mass movement.

On the other hand, in mammals, including humans, sperm, which is a germ cell, is an important vehicle for transmitting male genetic information to the next generation, and spermatogenesis, which involves a series of complex processes that produce sperm, preserves species It is an essential process for genetic diversity. In this complex and productive sperm formation process, germline stem cells, sperm stem cells, are recognized as important basic cells that maintain sperm formation throughout the life of men. In particular, sperm stem cells, which play a direct role in sperm production, are also considered as essential research areas for the treatment of male infertility and improvement of fertility.

Since the 1990s, research on functional supplements made from herbal medicines as the main raw material has been actively conducted in Korea to improve sexual function. “Nugra” developed by the Rural Development Administration and marketed since 2001, “Long Time F” developed by Chong Kun Dang as a health supplement for stabilization with octacosanol as the main ingredient, and sexual enhancement medicine developed by the Korea Institute of Science and Technology. ” Various natural products based products such as Cheonbo 204 ”and“ Red Max ”developed by Korea Ginseng Corporation as the main raw material are sold.

However, there are no medicines or foods to improve sperm concentration, mobility, and sperm count in men.

KR 1020070094394 A KR 101751211 B1

An object of the present invention is to provide a pharmaceutical composition and a health functional food composition for treating and preventing male infertility by increasing sperm concentration, sperm straightness, and total number of sperm in men by using an extract of a complex natural product as an active ingredient. .

In order to achieve the above object, the pharmaceutical composition for the prevention and treatment of male infertility of the present invention is characterized by containing a complex extract selected from 14 natural products as an active ingredient.

Here, the natural products include Cusaeae Semen, Rehmanniae Radix Preparata, Epimedii Herba, Morindae Radix, Cynomorii Herba, Cornus Fructus, Goji (Lycii Fructus) Two or more complex extracts selected from the group consisting of Dioscoreae Rhizoma, Rubi Fructus, Ginseng Radix, Cinnamomi Cortex, Poria Sclerotium, Plantaginis Semen and Schizandrae Fructus It is preferable to include as an active ingredient.

The male infertility is preferably one or more sperm-related infertility selected from azoospermia, empathy, contractorism and malformation spermosis.

As another specific example, when all of the natural product is contained, 12 parts by weight of soil, 12 parts by weight of sulfur, 12 parts by weight of yin and yang, 12 parts by weight of Pagukcheon, 10 parts by weight of ginseng, 10 parts by weight of cornus, Gojija 10 parts by weight, 10 parts by weight of acid, 6 parts by weight of ginseng, 6 parts by weight of cinnamon, 6 parts by weight of Bokryeong, 4 parts by weight of tea and 4 parts by weight of Omija are provided as active ingredients.

Meanwhile, the health functional food for preventing and improving male infertility of the present invention is characterized by containing the complex extract as an active ingredient.

Here, the health functional food is preferably in the form of powder, granule, tablet, capsule, pill, suspension, emulsion, syrup, tea bag, leached tea or healthy beverage.

In addition, the health supplement for preventing and improving male infertility of the present invention is characterized by containing the complex extract as an active ingredient.

The complex extract of the natural product of the present invention increases the sperm motility of men and increases the number of sperm, and thus can be usefully used in pharmaceutical compositions, health functional foods and health supplements for the prevention and treatment of male infertility. .

The terms or words used in the specification and claims should not be interpreted as being limited to ordinary or lexical meanings, and the inventor can appropriately define the concept of terms in order to explain his or her invention in the best way. Based on the principle that it should be interpreted as meanings and concepts consistent with the technical spirit of the present invention.

The pharmaceutical composition for treating and preventing male infertility of the present invention is characterized by containing as an active ingredient a complex extract selected from 14 natural products in order to achieve the above-described object.

In addition, the natural products include Cusaeae Semen, Rehmanniae Radix Preparata, Epimedii Herba, Morindae Radix, Cynomorii Herba, Cornus Fructus, Goji (Lycii Fructus) Two or more natural products selected from the group consisting of Dioscoreae Rhizoma, Rubi Fructus, Ginseng Radix, Cinnamomi Cortex, Poria Sclerotium, Plantaginis Semen, and Schisandrae Fructus Mixed ones can be extracted.

In addition, the complex extract may be extracted with water, a lower alcohol of C1 to C4, or a mixed solvent thereof, preferably a mixed solvent of water or water and ethanol, more preferably a mixed solvent of water and ethanol.

In addition, the composite extract may have an effect of increasing sperm motility.

In addition, the composite shell extract may have an effect of increasing sperm count.

In addition, the male infertility includes azoospermia, empathy, contractor and malformed sperm, and preferably includes all infertility related to sperm.

On the other hand, the health functional food for preventing male infertility of the present invention is characterized by containing a complex extract of natural products as an active ingredient.

Hereinafter, the present invention will be described in detail. The composite extract of the present invention can be obtained through the following general extraction process.

The natural product was selected from the group consisting of water, C1 to C5 lower alcohol or a mixture thereof as a solvent for extraction after washing.

The pharmaceutical composition for preventing and treating male infertility according to the present invention includes 0.1 to 99% by weight of the extract based on the total weight of the composition.

The pharmaceutical composition comprising the complex extract of the present invention may further include suitable carriers, excipients and diluents commonly used in the preparation of the composition.

The pharmaceutical dosage form of the extract of the present invention may be used in the form of their pharmaceutically acceptable salts, or may be used alone or in combination with other pharmaceutically active compounds, as well as in a suitable collection.

The pharmaceutical composition comprising the extract according to the present invention is in the form of an oral dosage form such as powder, granule, tablet, capsule, suspension, emulsion, syrup, aerosol, external preparation, suppository and sterile injectable solution, respectively, according to a conventional method. It can be formulated and used.

Carriers, excipients and diluents that may be included in the composition comprising the extract include lactose, dextrose, sucrose, sorbitol, mannitol, xylitol, erythritol, maltitol, starch, acacia rubber, alginate, gelatin, calcium phosphate, calcium silicate , Cellulose, methyl cellulose, microcrystalline cellulose, polyvinylpyrrolidone, water, methylhydroxybenzoate, propylhydroxybenzoate, talc, magnesium stearate, and mineral oil.

In the case of formulation, it is prepared using diluents or excipients such as fillers, extenders, binders, wetting agents, disintegrating agents and surfactants.

Solid preparations for oral administration include tablets, pills, powders, granules, capsules, etc. These solid preparations contain at least one excipient in the extract, for example starch, calcium carbonate, sucrose. Or it is prepared by mixing lactose, gelatin, and the like. In addition, lubricants such as magnesium stearate and talc are used in addition to simple excipients.

Liquid preparations for oral administration include suspensions, intravenous solutions, emulsions, syrups, etc. In addition to commonly used simple diluents such as water and liquid paraffin, various excipients, such as wetting agents, sweeteners, fragrances, and preservatives, can be included. have.

Formulations for parenteral administration include sterile aqueous solutions, non-aqueous solvents, suspensions, emulsions, lyophilized preparations, and suppositories. As the water-insoluble agent and the suspension agent, propylene glycol, polyethylene glycol, vegetable oil such as olive oil, and injectable ester such as ethyl oleate may be used. As a base for suppositories, witepsol, macrogol, tween, cacao butter, laurin butter, and glycerogelatin may be used.

The preferred dosage of the extract of the present invention depends on the patient's condition and body weight, the degree of disease, the drug form, the route and duration of administration, but can be appropriately selected by those skilled in the art. However, for the desired effect, the extract of the present invention is preferably administered at 0.0001 to 10 g / kg per day, preferably 0.01 to 1 g / kg per day. The administration may be administered once a day, or may be divided into several times. The above dosage does not limit the scope of the present invention in any way.

The present invention also provides a sperm exercise enhancer comprising the complex extract, and this sperm exercise enhancer is intended to improve fertilization rate during in vitro fertilization. The present invention also provides a vaginal and vaginal cleansing agent for women and vaginal inserts as a male fertility treatment agent for enhancing sperm movement including the extract. The present invention also provides an additive for sperm storage for in vitro fertilization containing the extract in order to improve fertilization rate during in vitro fertilization.

The present invention provides a health functional food comprising the extract showing the preventive effect of male infertility and food additives acceptable food supplement.

Health functional foods to which complex extracts can be added include, for example, various general foods, beverages, gums, teas, and vitamin complexes.

In addition, the complex extract may be added to food or beverage for the purpose of preventing male infertility. At this time, the amount of the extract in the food or beverage can be added at 0.01 to 15% by weight of the total food weight, the health functional beverage composition is added at a rate of 0.02 to 5 g, preferably 0.3 to 1 g, based on 100 g Can be.

The health functional beverage composition of the present invention is an essential component other than containing the extract in the above-mentioned content range, there is no particular limitation, and further contains various components such as various flavoring agents or natural carbohydrates, such as ordinary beverages. can do.

Examples of the above-mentioned natural carbohydrates include monosaccharides such as glucose and fructose; Disaccharides such as maltose, sucrose, etc .; And polysaccharides, for example, conventional sugars such as dextrin, cyclodextrin, and sugar alcohols such as xylitol, sorbitol, and erythritol. As flavoring agents other than those described above, natural flavoring agents such as taumatin, stevia extract, for example rebaudioside A, glycyrrhizine, etc .; And synthetic flavoring agents, such as saccharin, aspartame, and the like. The content of the natural carbohydrate is generally about 1 to 20 g per 100 g of the composition of the present invention, preferably about 5 to 12 g.

In addition to the above, the extract of the present invention is a variety of nutrients, vitamins, minerals (electrolytes), synthetic and natural flavors, colorants and neutralizers (cheese, chocolate, etc.), pectic acid and salts thereof, alginic acid and salts thereof, organic acids, protective properties It may contain colloidal thickeners, pH adjusting agents, stabilizers, preservatives, glycerin, alcohol, carbonic acid used in carbonated beverages, and the like.

In addition, the extracts of the present invention may contain natural fruit juice, fruit juice beverage, fruit flesh for the production of vegetable beverages, and the like. These ingredients can be used independently or in combination. At this time, the proportion of the additive is not very important, but preferably selected from the range of 0.01 to about 20 parts by weight per 100 parts by weight of the extract of the present invention.

Hereinafter, preferred embodiments of the present invention will be described in detail. In addition, in the following description, many specific matters such as specific components are described, which are provided to help a more comprehensive understanding of the present invention, and it is common in the art that the present invention can be practiced without these specific details. It will be obvious to those who have the knowledge of. And, in the description of the present invention, when it is determined that a detailed description of a related known function or configuration may unnecessarily obscure the subject matter of the present invention, the detailed description will be omitted.

Example

12 g of sediment, 12 g of sulcus, 12 g of yin and yang gu, 10 g of ginseng, 10 g of ginseng, 10 g of cornus officinalis, 10 g of goji wolfberry, 10 g of wild medicine, 6 g of ginseng, 6 g of cinnamon, 6 g of bokyeong, 4 g of tea roaster, 4 g g and 4 g of Omija were added 3 liters of water, extracted repeatedly with reflux cooling for 2 hours, and then filtered and concentrated under reduced pressure. The concentrated filtrate was freeze-dried with a freeze dryer under reduced pressure to obtain an extract powder and stored at 4 ° C. Before use in the experiment, the dried extract was dissolved in physiological saline and mixed vigorously at room temperature for 2 minutes.

Test example

For the samples of the above examples, experiments were conducted using the sperm movement enhancement efficacy evaluation method to find out the effect on the sperm count and motility change of human sperm. The hot water extract (120cc) was warmed twice a day after eating for 10 weeks in 16 male infertility patients with abnormal semen test findings.

The semen test was re-executed 10 weeks after taking the complex extract and compared with the pre-treatment semen test findings. As a result of treatment with the complex extract for 10 weeks, it was confirmed that sperm concentration, sperm straight motility, and total sperm count increased significantly.

<Changes of sperm indicators after 10 weeks of herbal medicine (KHM) administration>

Variable Baseline Post-KHM treatment
(10 weeks) (n = 16) P value Semen volume (ml) 2.2 (1.90, 3.05) ^* 2.25 (1.53, 2.98)
0.509 [Mean: 2.63 ± 1.21] ^¶ [Mean: 2.51 ± 1.32] Sperm concentration
(× 10 ⁶ / ml) 53.0 (12.38, 74.25) 47.0 (30.93, 110.0) 0.030 * [Mean: 50.68 ± 35.13] [Mean: 69.03 ± 50.19] Sperm motility (%) 38.7 (30.00, 48.25) 42.5 (29.00, 60.38) 0.088 [Mean: 37.94 ± 11.39] [Mean: 47.31 ± 20.19] Sperm progressive motility (%) (n = 11) 22.0 (19.00, 37.50) 40.0 (24,00, 55.20) 0.013 * [Mean: 25.92 ± 11.18] [Mean: 39.35 ± 17.20] Total motile sperm count
(× 10 ⁶ ) 34.04 (12.69, 69.96) 63.36 (21.20, 97.83) 0.044 * [Mean: 46.46 ± 39.39] [Mean: 72.25 ± 60.49] Sperm morphology (%) 2.0 (1.00, 2.75) 2.0 (1.00, 3.75) 0.297 [Mean: 1.88 ± 0.96] [Mean: 2.53 ± 1.78]

* Data is displayed as median with lower and upper quartiles.

 Data are expressed as mean ± standard deviation

Hereinafter, a pharmaceutical composition containing the extract of the present invention and a formulation example of a health functional food will be described, but this is not intended to limit the present invention, but only to be specifically described.

Formulation Example 1: Preparation of powder

Complex extract powder 20 mg

Lactose 100 mg

Talc 10 mg

The above ingredients were mixed and filled in an airtight fabric to prepare a powder.

Formulation Example 2: Preparation of tablets

Complex extract powder 10 mg

* 100 mg corn starch

Lactose 100 mg

Magnesium stearate 2mg

After mixing the above components, tablets were prepared by tableting according to a conventional tablet manufacturing method.

Formulation Example 3: Preparation of capsules

Complex extract powder 10 mg

Crystalline cellulose 3 mg

Lactose 14.8 mg

Magnesium stearate 2mg

The above ingredients were mixed and filled in gelatin capsules according to a conventional capsule preparation method to prepare capsules.

Formulation Example 4: Preparation of Injection

Complex extract powder 10 mg

Mannitol 180 mg

Sterile distilled water for injection 2794 mg

Na2HPO412H2O 26 mg

It was prepared with the above ingredient content per ampoule (2 ml) according to a conventional injection preparation method.

Formulation Example 5: Preparation of liquid formulation

Complex extract powder 10 mg

Isomerized sugar 10 g

5 g mannitol

An appropriate amount of purified water

Each component is added and dissolved in purified water according to a conventional liquid preparation method, a suitable amount of lemon scent is added, and the above components are mixed, and then purified water is added to adjust the total to 100 ml and sterilized by filling in a brown bottle. Did.

Formulation Example 6: Preparation of healthy drinks

Complex extract powder 10 mg

Vitamin C 15 g

Vitamin E (powder) 100 g

Iron lactate 19.75 g

Zinc oxide 3.5 g

Nicotinic acid amide 3.5 g

Vitamin A 0.2 g

Vitamin B1 0.25 g

Vitamin B2 0.3 g

An appropriate amount of water

After mixing the above components according to a conventional health drink manufacturing method, after stirring and heating at 85 ° C. for about 1 hour, the resulting solution is filtered, obtained in a sterilized 2 liter container, sealed and sterilized, and stored in the refrigerator for refrigeration. It was used to prepare a health drink composition according to. Although the above composition ratio is a mixture of components suitable for a preference drink in a preferred embodiment, the mixing ratio may be arbitrarily modified according to regional and ethnic preferences such as demand hierarchy, country of demand, and usage.

The preferred embodiments of the present invention have been described above, but the present invention is not limited to the specific embodiments described above, and those skilled in the art can perform various modifications without departing from the gist of the present invention. Of course it is possible. Therefore, the scope of the present invention should not be construed as being limited to the above embodiment, but should be defined by the claims and equivalents as well as the claims below.

Claims (6)

Cuscutae Semen, Rehmanniae Radix Preparata, Epimedii Herba, Morindae Radix, Cynomorii Herba, Corni Fructus, Goji (Lycii Fructus), Wild Medicine (Dioscoreae Rhizoma) (Rubi Fructus), Ginseng (Ginseng Radix), Cinnamon (Cinnamomi Cortex), Bokryeong (Poria Sclerotium), Chajeon (Plantaginis Semen) and Omija (Schisandrae Fructus) selected from the group consisting of a mixture of two or more natural extracts mixed Pharmaceutical composition for the prevention and treatment of male infertility, including as an active ingredient.
The pharmaceutical composition for preventing and treating male infertility according to claim 1, wherein the male infertility is at least one sperm-related infertility selected from azoospermia, sperm reduction, contractile sperm and malformed spermosis.
The method of claim 1, wherein the complex extract is 100 parts by weight, 12 parts by weight of soil, 12 parts by weight of sulfur, 12 parts by weight of yin and yang, 10 parts by weight of gyeokyang, 10 parts by weight of ginseng, 10 parts by weight of cornflower, 10 parts by weight of goji berries , 10 parts by weight of acid powder, 10 parts by weight of bokbunja, 6 parts by weight of ginseng, 6 parts by weight of cinnamon, 6 parts by weight of boknyeong, 4 parts by weight of tea roaster and 4 parts by weight of Omija
Lion (Cuscutae Semen), Rehmanniae Radix Preparata, Epimedii Herba, Morindae Radix, Cynomorii Herba, Corni Fructus, Wolfberry (Lycii Fructus), Wild Medicine (Dioscoreae Rhizoma) (Rubi Fructus), Ginseng (Ginseng Radix), Cinnamon (Cinnamomi Cortex), Bokryeong (Poria Sclerotium), Chajeon (Plantaginis Semen) and Omija (Schisandrae Fructus) selected from the group consisting of a mixture of two or more natural extracts mixed A health supplement for improving male infertility, which is included as an active ingredient.
In the fourth,
The health functional food is a health functional food composition characterized in that it is in the form of powder, granule, tablet, capsule, pill, suspension, emulsion, syrup, tea bag, leach tea or healthy beverage.
Lion (Cuscutae Semen), Rehmanniae Radix Preparata, Epimedii Herba, Morindae Radix, Cynomorii Herba, Corni Fructus, Wolfberry (Lycii Fructus), Wild Medicine (Dioscoreae Rhizoma) (Rubi Fructus), Ginseng (Ginseng Radix), Cinnamon (Cinnamomi Cortex), Bokryeong (Poria Sclerotium), Chajeon (Plantaginis Semen) and Omija (Schisandrae Fructus) selected from the group consisting of a mixture of two or more natural extracts mixed A health supplement for improving male infertility, characterized by containing as an active ingredient.