RU2159122C1 - Means and method for improving sperm quality - Google Patents

Abstract

FIELD: medicine. SUBSTANCE: method involves applying Polygonum aviculare L. s.I knot-grass extract for improving ejaculate quality. The means has 10% of extractive substances containing in Polygonum aviculare L.s.I knot-grass extract as active base. The drug is to be administered for normalizing spermatogenesis at a dose of 12.0-10.0 g daily during the full cycle of spermatogenesis. EFFECT: enhanced effectiveness in treating male infertility; simplified method. 3 cl, 8 tbl

Description

 The invention relates to clinical and experimental medicine, in particular to the pharmacology of herbal remedies that improve the quality of sperm, as well as to urology, andrology, and can be used to treat infertility in men.

 It is known that the ability to fertilize directly depends on the quality of sperm. The problem of infertility is of social and national importance, which is confirmed by the high frequency of infertile marriages worldwide (about 15%) and especially in Russia (14.8-24.7%). 45% of men who are barren have infertility of sperm, while fertility is more dependent on motility, and not on the number of sperm (Topka E.G., Gorpichenko I.I., Malyshkin I.N. Etiology , pathogenesis, clinical picture and treatment of secondary male infertility // Urology and Nephrology. - 1993. - N 5.- P. 43-48).

 Of the known herbal products that improve sperm quality and are used in cases of spermatogenesis disorders, the closest and only drug registered in Russia is the Indian-made complex herbal preparation - speman (HIMALAYA). (Vidal Handbook. Medications in Russia. - M.: AstraFarmServis, 1998. - S. G-49).

 This drug is produced by a foreign company and is very expensive due to the complex composition of medicinal herbs that grow in different countries of the world and have limited raw materials.

 For the treatment of male infertility, it is recommended to take speman 2 tablets 3 times a day for 4-6 months. Taking the drug reduces the viscosity of sperm, increases the number and motility of sperm. The drug is recommended mainly for the treatment of oligospermia (Vidal Handbook. Medications in Russia. - M .: AstraFarmServis, 1995. - P. 832).

 As disadvantages of this drug, it should be noted that it is not effective in the treatment of pathospermia, since it does not affect the number of pathological forms of sperm. In addition, speman increases sperm motility insufficiently.

 Today, male infertility treatment is carried out according to the general scheme, which, depending on the patient’s condition, includes hormone therapy, immunomodulating therapy, biostimulating drugs, nonspecific stimulants, which include various vitamin preparations, anti-inflammatory antimicrobial therapy, if necessary, antioxidants, cytomidines, etc. (Balabolkin M. I., Gorokhova TR Conservative treatment of male infertility. - Soviet medicine, 1988. - N 5.- P. 36-43, Sexology and andrology, edited by Vozianov AF and Go pichenko II, Publishing House of the "Outline" - 1997. - S. 754-757).

 Despite the variety of tools and recommended treatment regimens, the effectiveness of treating male infertility is very low. The task of the invention is to improve the quality of sperm by expanding the arsenal of tools and methods that contribute to improving the quality of ejaculate.

 The problem is solved in that as a means of improving the quality indicators of sperm, it is proposed to use the infusion of grass of the mountaineer bird Polygonum aviculare L. s. I., sem. Buckwheat (Polygonaceae).

 The applicant first discovered that the water extract of the mountaineer bird has the ability to improve sperm quality, which is characterized by an increase in the number of motile spermatozoa and a decrease in the number of pathologically altered spermatozoa in both percentage and absolute ratio.

 It is known to use the mountaineer bird as an anti-inflammatory, diuretic, astringent, uterotonic, vitamin remedy that promotes the elimination of calculi in kidney stone disease, which increases the excretion of salts (Mashkovsky MD Medicines: A guide for pharmacotherapy for doctors. - In 2 hours . - Vilnius: Gamta, 1993. - Part 1. - P. 443. Krylov G.V., Kozakova NF Herbalist: Medicinal plants and their use. - Novosibirsk: Det. Lit., 1993. - S. 132-133).

 Alcoholic extract of the grass of the mountaineer bird is recommended as a means of anti-inflammatory activity (US Pat. N 2064300, class A 61 K 35/78, publ. 07.27.96).

 The effect of water infusion of grass of the mountaineer bird on the sexual activity of rats (US Pat. RF N 2127596, class A 61 K 35/78, publ. 20.03.99).

 However, the effect of this drug on sperm quality was not detected during the experiment.

 Information on the effect of the mountaineer bird on the qualitative characteristics of the ejaculate of humans and animals in the literature, the applicant has not been found.

 The problem is also solved with the help of a sperm-improving agent containing an active principle and a pharmaceutically acceptable excipient, in which extract ingredients of the mountaineer grass in the amount of 10-100 wt.% And the rest are an excipient.

 As a pharmaceutically acceptable carrier can be used: methyl cellulose, carboxymethyl cellulose, starch, sugar, calcium or magnesium stearate, stearic acid, polyvinylpyrrolizone, talc, gum arabic, etc., as well as any combination thereof.

 The content of the active principle in a dose of 10-100% in the dosage form is determined by the fact that these doses are the most pharmaceutically acceptable and convenient when taking the drug to normalize spermatogenesis.

 The specified drug for the convenience of storage, sale and administration by patients is carried out in powder, tablet or capsule form.

 The problem is also solved by the method of using the above medicinal product.

 A method for improving the quality of sperm by oral administration of a medicinal product containing 10-100% of extractive substances of the mountaineer grass as an active principle and excipient, in a daily dose of 1.0-10 g during the period of the full cycle of spermatogenesis.

 Admission of a medicinal product containing extractives of the poultry grass herb extract as an active ingredient less than 1.0 g daily does not significantly increase sperm motility and decrease the number of pathological sperm forms.

 The use of a medicinal product containing extractives of an infusion of highlander grass as an active ingredient in a dose of more than 10 g per day does not provide a stable improvement in sperm quality, since in the first week there is a multiple increase in the number of motile forms of spermatozoa, and then there is a decrease in the number of motile forms of spermatozoa to the previous level.

 The use of a medicinal product containing extractive substances as an active ingredient in the infusion of grass of the mountaineer bird, during the period of a full cycle of spermatogenesis allows us to achieve a stable improvement in the quality of sperm.

 The performance of the claimed inventions is confirmed by the experiments and examples described below. In examples 1-6, an infusion of grass of the mountaineer Polygonum aviculare L.s.I., sem. Buckwheat (Polygonaceae), prepared according to the generally accepted methodology (State Pharmacopoeia of the USSR. - XI ed. - M .: Medicine, 1968. - S. 370 - 372). 100 g of air-dried above-ground (leaves, flowers and stems) parts of the mountaineer grass was poured with 1 liter of boiling distilled water, kept in a water bath for 15 minutes, then removed from heat and allowed to cool for 15 minutes, after which it was filtered, and received 989 ml of infusion, 1 ml of which contained 100 mg of extractive substances. To evaluate the stimulating effect of the mountaineer, experimental studies were conducted on laboratory animals male rats and mice, in each group of at least 10 animals. Statistical processing of data was carried out using Student's t-test for small samples (n <30). In studies, a significance level of p = 0.05 was considered reliable.

 Example 1. The effect of infusion from the grass of the mountaineer bird on the spermogram of healthy male rats and mice.

 Male Wistar rats and outbred mice were injected intragastrically, using a metal probe, an infusion of poultry grass at a dose of 50 mg / kg per day, calculated on the amount of extractive substances during the complete spermatogenesis cycle, which is 30 days in rats and mice. The control animals were injected with the same amount of distilled water.

 It was established that the infusion of the mountaineer, in comparison with the control, increased the number of motile spermatozoa (by 23% and 36%), decreasing the number of sedentary (by 62% and 62%) and immobile forms (78% and 79%), as well as the number pathological sperm (45% and 41%). The remaining indicators of the spermogram of animals changed slightly (table. 1).

 Example 2. The effect of the highlander on quantitative indicators of spermogram of male rats on the background of inhibition of sexual function by various doses of folliculin.

 The model is based on the antagonism of androgen and estrogen hormones. Male animals were divided into groups that were injected intramuscularly with estrone (in the form of Folliculin in Oil for Injection) at a dose of 10 U / kg (0.001 mg / kg) per day. The control animals were injected intramuscularly with sterile olive oil in equivalent volumes. Upon achievement of persistent inhibition of sexual behavior, which occurred at 30 days, the animals for another 30 days (a full cycle of spermatogenesis) were injected intragastrically with an infusion of mountaineer at a dose of 100 mg / kg per day in terms of the amount of extractive substances against the background of continued injections of folliculin.

 From the table. 2 it follows that the mountaineer is able to normalize the qualitative characteristics of the ejaculate, increasing the number of motile spermatozoa and reducing the number of sedentary, motionless and pathological spermatozoa against the background of inhibition of sexual function by folliculin.

 Example 3. The effect of the mountaineer on the quantitative indicators of spermogram of male rats on the background of inhibition of sexual function by metamizil.

 The model is based on the inhibition of the pituitary gonadotropic function by metamisil (benzylic acid diethylaminopropyl ester hydrochloride), which, dissolved in distilled water, was daily administered subcutaneously to male rats at a dose of 60 mg / kg / day. The control was a group that received only solvent in an adequate volume. Upon achievement of persistent inhibition of sexual behavior, which occurred by 30 days, the animals were injected intragastrically with an extract of mountaineer at a dose of 100 mg / kg per day even in the course of the period of the full cycle of spermatogenesis (30 days), based on the content of extractive substances against the background of continued injections of metamizil.

 From the table. 3 it follows that the mountaineer is able to normalize the qualitative characteristics of the ejaculate, reducing the number of sedentary, motionless and pathological spermatozoa against the background of inhibition of sexual function by metamizil.

 Example 4. The effect of the mountaineer on the quantitative indicators of spermogram of male rats on the background of inhibition of sexual function by androcur.

 The model is based on the ability of cyproterone acetate to competitively block testosterone receptors in target organs, thereby inhibiting sexual function. Cyproterone acetate in the form of the Androkur preparation was dissolved in distilled water, and the resulting suspension was daily administered intragastrically to male rats at doses of 1 and 5 mg / kg / day (therapeutic interval). The control was a group that received only distilled water. Upon achievement of persistent inhibition of sexual behavior, which occurred at 30 days, the animals during the period of the full cycle of spermatogenesis (30 days) were also administered intragastrically infusion of mountaineer at a dose of 100 mg / kg per day in terms of the amount of extractive substances against the background of continued administration of androcure.

 The results presented in table. 4, clearly show that the use of infusion of the mountaineer of the bird according to the claimed method leads to the normalization of the qualitative characteristics of the ejaculate, increasing the number of motile spermatozoa and reducing the number of sedentary, motionless and pathological spermatozoa against the inhibition of sexual function by different doses of cyproterone acetate.

 Example 5. The effect of the mountaineer on the quantitative indicators of spermogram of male rats on the background of inhibition of sexual function by Proscar.

 The model is based on the ability of finasteride to block 5α-reductase, preventing the conversion of testosterone to more active and capable of binding to dihydrotestosterone receptors and thus inhibiting sexual function. Finasteride in the form of the “Proscar” preparation was dissolved in distilled water and the resulting suspension was daily administered intragastrically to male rats at doses of 1 mg / kg / day. The control was a group that received only distilled water. Upon achievement of persistent inhibition of sexual behavior, which occurred at 30 days, the animals during the period of the full cycle of spermatogenesis (30 days) were still administered intragastrically infusion of the mountaineer at a dose of 100 mg / kg per day, calculated on the content of extractive substances against the background of the continued introduction of proscar.

 From the table. 5 it follows that the mountaineer is able to normalize the qualitative characteristics of the ejaculate, increasing the number of motile spermatozoa and reducing the number of sedentary, motionless and pathological spermatozoa against the background of inhibition of sexual function by finasteride.

 Example 6. The effect of the mountaineer bird on quantitative indicators of spermogram of male rats on the background of inhibition of spermatogenesis by low doses of alkeran.

 To identify the effects of stimulation of spermatogenesis with the infusion of the highlander, a toxic model with the cytostatic drug melphalan (Alkeran) was used. Male rats were divided into 3 groups. Two groups received distilled water for 10 days, and one group received a highlander infusion daily intragastrically at a dose of 100 mg / kg / day (in terms of the amount of extractives) during the same time. On day 11, one of the first two groups received 1 ml of distilled water intraperitoneally and was designated as "Control I". Animals of the second group received a single intraperitoneal injection of 10 μg / kg of alkeran and were designated as "Control II". The prelander group also received 10 μg / kg of alkerana once intraperitoneally. 72 hours after the administration of cytostatic, seminal fluid was taken for examination and the quality indicators in the ejaculate were determined. After the study, the animals of the third group continued to administer the highlander infusion in the same manner and in the same dose for another 15 days, examining the ejaculate on days 5, 7, 10 and 15 after the administration of alkeran. When assessing the number of motile sperm cells, sedentary forms with pathological types of movement were conditionally assigned to this group.

 In the table. Figure 6 shows the dynamics of changes in the spermogram indicators against the background of the introduction of male rats of the infusion of mountaineer at a dose of 100 mg / kg / day after a single injection of alkeran. The results of the experiment indicate the presence of the protective action of the mountaineer bird in relation to the number of motile and pathological forms of spermatozoa against the background of the cytostatic effect of alkeran.

 The studies (examples 1-6) clearly show that the infusion of the grass of the mountaineer avian Polygonum aviculare L. s. I., sem. Buckwheat (Polygonaceae) has a positive effect on sperm quality, increases the number of motile sperm and reduces the number of pathological forms. Therefore, the infusion of grass of the mountaineer bird can be recommended for the treatment of male infertility in both oligospermia and pathospermia.

 For clinical and experimental studies on sick men with irregularities in the spermogram, the agent obtained according to paragraph 2 of the formula in various dosage forms was used.

 Example 7. The effect of the infusion of the mountaineer bird on the sperm parameters of patients with impaired ejaculation due to chronic inflammatory diseases of the reproductive system.

100 g of dry grass of the mountaineer bird was poured into 1 liter of boiling distilled water, kept for 15 minutes in a water bath, then removed and left to cool for 15 minutes, after which it was filtered. Then the infusion was evaporated to a powder state at a temperature not exceeding 60 ^o C. Received 9.93 g of dry extractives.

 The obtained extractives of the mountaineer grass in the form of a powder were used both to obtain various dosage forms and as an independent drug.

In addition to the powder, the following tablets and capsules prepared by the well-known method were used in the experiment:
1. tablets A weighing 0.5 g, containing:
active principle (extractives of the mountaineer bird) - 0.45 g (90%);
filler: starch 0.045 g (9%) and magnesium stearate 0.005 g (1%)
2. tablets B weighing 0.5 g, containing:
active principle (extractives of the mountaineer) - 0.25 g (50%);
filler: methyl cellulose - 0.25 g (50%);
3. capsules A containing:
active principle (extractives of the mountaineer) 50 mg (50%):
filler: sugar - 50 mg (50%)
4. capsules B included only the active principle (extractives of the mountaineer bird) in the amount of 100 mg per capsule, without filler.

 The study involved sick volunteers - men aged 25 to 37 years old, suffering from chronic prostatitis (49 people), chronic vesiculoprostatitis (37 people) and chronic orthoepidimitis (23 people) for at least 5 years. Among the patients of the main group, depending on body weight, subgroups were allocated that received, in addition to standard therapy, powder of the extract of highlander, tablets or capsules. The control group with similar diseases and history received only generally accepted standard therapy.

 The powder was prescribed to patients at a dose of 1.0 g daily, for 3 months, a full cycle of spermatogenesis. Patients with a body weight of up to 70 kg received “tablets B” or “capsules A” at the rate of 10 g of the drug per day, divided into 3 doses, for 3 months, a full cycle of spermatogenesis. Patients with a body weight of more than 70 kg received “tablets A” or “capsules B” at the rate of 10 g of the drug per day, divided into three doses, for 3 months, a full cycle of spermatogenesis.

 The results of the study are shown in table 7.

 The data obtained (table. 7) indicate the presence of a normalizing effect of drugs containing, as an active principle, extractive substances from the infusion of poultry grass on spermatogenic function in chronic diseases of the reproductive system in men of reproductive age.

 Example 8. The effect of drugs obtained from the herb of the mountaineer bird on the sperm parameters of men with impaired ejaculation due to age-related involution of the reproductive system.

100 g of dry grass of the mountaineer bird was poured into 1 liter of boiling distilled water, kept for 15 minutes in a water bath, then removed and left to cool for 15 minutes, after which it was filtered. Then the infusion was evaporated to a powder state at a temperature not exceeding 60 ^o C. Received 9.89 g of dry extractive substances.

 The obtained extractives of the mountaineer grass in the form of a powder were used both to obtain various dosage forms and as an independent drug.

In addition to the powder, the following tablets and capsules prepared by the well-known method were used in the experiment:
1. tablets And weighing 0.5 g, containing:
active principle (extractives of the mountaineer bird) - 0.45 g (90%);
filler: starch 0.045 g (9%) and magnesium stearate 0.005 g (1%)
2. tablets B weighing 0.5 g, containing:
active principle (extractives of the mountaineer) - 0.25 g (50%);
filler: methyl cellulose - 0.25 g (50%);
3. capsules A containing:
active principle (extractives of the mountaineer) 50 mg (50%):
filler: sugar - 50 mg (50%)
4. capsules B included only the active principle (extractives of the mountaineer bird) in the amount of 100 mg per capsule, without filler.

 The study involved 35 male volunteers aged 49 to 58 years. The powder was prescribed to patients at a dose of 1.0 g daily, for 3 months, a full cycle of spermatogenesis. Patients with a body weight of up to 70 kg received “tablets B” or “capsules A” at the rate of 10 g of the drug per day, divided into 3 doses, for 3 months, a full cycle of spermatogenesis. Patients with a body weight of more than 70 kg received “tablets A” or “capsules B” at the rate of 10 g of the drug per day, divided into three doses, for 3 months, a full cycle of spermatogenesis.

 The control group did not receive treatment of a similar age group.

 The experimental results are given in table. 8, indicate the presence of a stimulating effect of drugs containing extractive substances of an extract of the herb of the mountaineer bird as an active principle on spermatogenic function in men who are in late ontogenesis.

 The studies carried out in the framework of the claimed method using a medicinal product containing, as an active principle, extractives of the infusion of grass of the mountaineer bird in an amount of 10 to 100% (Tables 7, 8), clearly confirm the improvement in the characteristics of the ejaculate.

 The advantage of the new drug for improving sperm quality can be considered that the mountaineer is a widespread plant with unlimited raw materials. The inventive method is very simple to implement and can be used in the treatment of astheno- and pathospermia of various etiologies. The proposed method allows treatment in both inpatient and outpatient settings, compared with the prototype (treatment with sperman) significantly reduces the duration of treatment. The methodically claimed method is most consistent with the objectives of pathogenetic therapy, which can significantly increase the therapeutic effect of the treatment of infertility in men.

 The use of infusion of the herb of the mountaineer bird in the framework of the claimed inventions in the form of a dietary supplement will also lead to an increase in the number of motile spermatozoa and a decrease in the number of pathological forms in the ejaculate, which will positively affect not only the patient's well-being, but also the reproduction of the offspring.

Claims (4)

 1. The use of infusion of grass of the mountaineer bird as a means of improving sperm quality.  2. An agent that improves the quality of sperm, containing an active principle and a pharmaceutically acceptable excipient, characterized in that as an active principle it contains extractives of infusion of grass of mountaineer, in an amount of at least 10%.  3. The tool according to p. 2, characterized in that it is made in powder, tablet or capsule form.  4. A method for improving the quality of sperm by oral administration of a drug, characterized in that the drug is administered a means of improving the quality of sperm containing a pharmaceutically acceptable carrier and at least 10% of the extractives of the mountaineer, in a daily dose of 0.1-10 g during the period of the full cycle of spermatogenesis.

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