Composition for treating prostatitis and preparation method and application thereof

Abstract

The invention discloses a composition for treating prostatitis and a preparation method and application thereof. The composition is prepared from the following components in parts by weight: 5 to 15 parts of ergothioneine, 10 to 20 parts of cistanche total glycosides, 25 to 45 parts of phytosterol, 450 to 550 parts of pumpkin seed oil, 180 to 250 parts of fructus cannabis oil and 250 to 350 parts of auxiliary materials. Through the synergistic effect of various natural active components, the composition maintains the balance of overall metabolism of a body while reducing inflammation and inhibiting prostate cell proliferation, side effect risks possibly brought by a traditional single-component treatment scheme are avoided, and the composition has higher clinical application potential. The composition disclosed by the invention has a wide market application prospect and popularization value by virtue of good safety and compliance.

Description

Technical Field

[0001] The present invention relates to the fields of medicines and health products, and in particular to a composition for treating prostatitis, a preparation method thereof and an application thereof. Background Art

[0002] Prostate health is an important component of a man's overall health. Prostatitis can also lead to benign prostatic hyperplasia (BPH), manifesting as symptoms such as dysuria, urgency and pain during urination, hematuria, perineal pain, and erectile dysfunction, severely impacting a man's quality of life and mental health. BPH caused by prostatitis leads to symptoms such as difficulty urinating and frequent urination at night. Without timely intervention, this can lead to urinary retention, bladder impairment, and even renal dysfunction.

[0003] Adjuvant treatment for prostatitis generally involves the use of nonsteroidal anti-inflammatory drugs (NSAIDs) to relieve inflammation and pain, or alpha-blockers to improve urination symptoms. Patients with benign prostatic hyperplasia (BPH) often require long-term use of hormonal medications such as 5α-reductase inhibitors or androgen receptor antagonists to control their condition. NSAIDs can cause gastrointestinal bleeding and liver and kidney damage; hormonal medications are also associated with adverse reactions such as sexual dysfunction and breast development, and require long-term medication maintenance to maintain their effects. On the other hand, some patients respond poorly to conventional treatments, with symptoms prone to recurrence, and there is a lack of safe and effective long-term management options.

[0004] Therefore, developing new products that have no toxic side effects, can be used for a long time, and can effectively maintain prostate health has become a technical problem that needs to be solved urgently and is also an important development direction in the field of prostatitis prevention and treatment. Summary of the Invention

[0005] To address the deficiencies in the prior art, the present invention provides a composition for treating prostatitis, its preparation method, and its use. Through the synergistic effects of multiple natural active ingredients, the present invention enables the composition to reduce inflammation and inhibit cell proliferation while maintaining overall metabolic balance. This avoids the risk of side effects associated with traditional single-ingredient treatments and offers greater clinical application potential. With its excellent safety and compliance, the composition of the present invention has broad market application prospects and promotional value.

[0006] The present invention provides a composition, which comprises the following components in parts by weight:

[0007] 5-15 parts of ergothioneine, preferably 8-12 parts; 10-20 parts of total glycosides of Cistanche deserticola, preferably 13-18 parts; 25-45 parts of phytosterols, preferably 30-40 parts; 450-550 parts of pumpkin seed oil, preferably 480-520 parts; 180-250 parts of hemp seed oil, preferably 200-230 parts; and 250-350 parts of auxiliary materials.

[0008] In some embodiments, the purity of the ergothioneine is ≥95%, and the purity of the total glycosides of Cistanche deserticola is ≥80%.

[0009] In the present invention, thioneine provides a basic and powerful free radical scavenging effect, while the total glucosides of Cistanche assist in regulating the endogenous antioxidant system. The two work together to reduce oxidative damage from the source and directly inhibit the inflammatory response. The dual action effectively improves the prostate microenvironment. Phytosterols can play a role in vivo by inhibiting the inflammatory response in prostate tissue. Phytosterols can promote the stability and absorption of thioneine and the total glucosides of Cistanche, while pumpkin seed oil and hemp seed oil supplement essential fatty acids, repair prostate cell membrane structure, and improve tissue microenvironment, further consolidating the effect of thioneine and the total glucosides of Cistanche in the synergistic treatment of prostatitis.

[0010] In some embodiments, the plant sterol is any one of stigmasterol, campesterol, β-sitosterol, brassicasterol, avenasterol, spinachsterol and ergosterol; preferably, the plant sterol is campesterol.

[0011] In some embodiments, the hemp seed oil has a peroxide value of ≤10.0 and an acid value of ≤2.0.

[0012] In some embodiments, the mass ratio of thioneine to the total glycosides of Cistanche is 1: (1 to 5); thioneine has the best antioxidant effect at a certain dose, but there may be absorption saturation at high doses. The total glycosides of Cistanche can improve the distribution and utilization of thioneine in local tissues by promoting microcirculation. The present invention, by compounding thioneine with the total glycosides of Cistanche at a mass ratio of 1: (1 to 5), ensures that thioneine fully exerts its antioxidant effect, avoids absorption disorders or potential adverse reactions caused by excessively high doses used alone, and at the same time achieves the best effect output through the auxiliary effect of the total glycosides of Cistanche.

[0013] In some embodiments, the auxiliary material is any one or more of edible gum, glycerin, emulsifier, filler, stabilizer, glidant and thickener.

[0014] In some embodiments, the filler is any one of microcrystalline cellulose, lactose, and pregelatinized starch.

[0015] In some embodiments, the glidant is colloidal silicon dioxide or magnesium stearate.

[0016] The present invention also provides a method for preparing the composition, comprising the following steps:

[0017] S1: uniformly mixing the total glycosides of Cistanche deserticola, thioneine, and phytosterols, and adding the mixture to a mixed solution of pumpkin seed oil and hemp seed oil to obtain a mixture 1;

[0018] S2: Add auxiliary materials to the mixture 1, and homogenize the mixture using a homogenizer to obtain the composition.

[0019] The present invention also provides a preparation, which uses the composition as an active ingredient.

[0020] In some embodiments, the preparation is a capsule, granule, tablet, powder, pill, oral solution, or syrup.

[0021] In order to prepare the dosage form into tablets, various carriers well known in the art can be widely used. Examples of carriers are as follows: diluents and absorbents, such as starch, dextrin, calcium sulfate, lactose, mannitol, sucrose, sodium chloride, glucose, urea, calcium carbonate, kaolin, microcrystalline cellulose, aluminum silicate, etc.; wetting agents and binders, such as water, glycerol, polyethylene glycol, ethanol, propanol, starch slurry, dextrin, syrup, honey, glucose solution, acacia slurry, gelatin slurry, sodium methylcellulose, shellac, methylcellulose, potassium phosphate, polyvinyl pyrrolidone, etc.; disintegrants, such as dry starch, alginate, agar powder, brown algae starch, sodium bicarbonate and citric acid, calcium carbonate, polyoxyethylene sorbitan fatty acid esters, sodium lauryl sulfate, methylcellulose, ethylcellulose, etc.; disintegration inhibitors, such as sucrose, tristearin, cocoa butter, hydrogenated oil, etc.; absorption accelerators, such as quaternary ammonium salts, sodium lauryl sulfate, etc.; lubricants, such as talc, silicon dioxide, corn starch, stearate, boric acid, liquid paraffin, polyethylene glycol, etc. The tablets can be further made into coated tablets, such as sugar-coated tablets, film-coated tablets, enteric-coated tablets, or double-layer tablets and multi-layer tablets.

[0022] The present invention also provides the use of the composition in the preparation of medicines and / or health products for treating prostatic hyperplasia, preferably benign prostatic hyperplasia.

[0023] The present invention also provides the use of the composition in the preparation of medicines and / or health products for treating prostatitis, preferably chronic prostatitis.

[0024] The dosage of the composition of the present invention depends on many factors, such as the nature and severity of the prostatitis to be treated, the sex, age, weight, personality and individual response of the subject or animal, the route of administration, the number of doses, etc., and therefore the dosage of the present invention can vary widely. Based on the actual amount of effective drug contained in the final formulation of the composition of the present invention, appropriate adjustments are made to achieve the required therapeutically effective amount to complete the treatment of the present invention.

[0025] In summary, compared with the prior art, the present invention achieves the following technical effects:

[0026] 1. The composition of the present invention can significantly reduce the expression levels of multiple inflammatory factors in prostate tissue, including but not limited to TNF-α, IL-6, IL-1β, etc., by scientifically and rationally selecting and proportioning ergothioneine, total glucosides of Cistanche, phytosterols, pumpkin seed oil and hemp seed oil, and significantly inhibit local inflammatory response, thereby effectively controlling the progression of prostatitis and alleviating the patient's discomfort symptoms.

[0027] 2. The composition of the present invention can effectively inhibit the abnormal proliferation of prostate cells, prevent the increase in prostate volume and the symptoms such as dysuria and frequent urination caused by it, and also has a good preventive and auxiliary therapeutic effect on related diseases such as prostate hyperplasia.

[0028] 3. Observation results of long-term use of the composition of the present invention showed that the weight of experimental animals and subjects remained stable, without obvious weight loss or other adverse physiological reactions, indicating that the composition of the present invention has excellent safety and tolerability and is suitable for long-term use or as an auxiliary treatment for chronic diseases. BRIEF DESCRIPTION OF THE DRAWINGS

[0029] In order to more clearly illustrate the technical solutions of the embodiments of the present invention, the following briefly introduces the drawings required for use in the embodiments. It should be understood that the following drawings only illustrate certain embodiments of the present invention and therefore should not be regarded as limiting the scope. For ordinary technicians in this field, other relevant drawings can be obtained based on these drawings without paying any creative work.

[0030] Figure 1 This is the statistical result of the expression level of the inflammatory factor IL-1β in Test Example 1 of the present invention.

[0031] Figure 2 This is the statistical result of the expression level of the inflammatory factor IL-6 in Test Example 1 of the present invention.

[0032] Figure 3 This is the statistical result of the expression level of the inflammatory factor TNF-α in Test Example 1 of the present invention.

[0033] Figure 4 This is the statistical result of cell survival rate in Test Example 2 of the present invention.

[0034] Figure 5 The statistical results of mouse weight in Test Example 3 of the present invention are shown. DETAILED DESCRIPTION

[0035] To help those skilled in the art better understand the present invention, the technical solutions in the embodiments of the present invention are clearly and completely described. Obviously, the described embodiments are only part of the embodiments of the present invention, not all of them. Based on the embodiments of the present invention, all other embodiments obtained by those skilled in the art without creative work should fall within the scope of protection of the present invention.

[0036] The specific preparation method of the composition of this embodiment into granules is as follows:

[0037] (1) Mix thioneine, total glycosides of Cistanche deserticola and phytosterols with auxiliary materials, and gradually add pumpkin seed oil and hemp seed oil to ensure that the drug ingredients are fully integrated with the oil;

[0038] (2) Starch is selected as the matrix of the granules, and a binder, hydroxypropyl methylcellulose, is added and mixed thoroughly. The formula mixture is mixed with 20-30 v / m% water by a wet granulation method until uniform wet granules are formed.

[0039] (3) The wet granules are granulated using a high-efficiency fluidized bed granulator, and then dried and packaged.

[0040] Unless otherwise specified, the experimental methods used in the following examples are conventional methods. The materials and reagents used are all commercially available unless otherwise specified.

[0041] Ergothioneine: Xi'an Tianfeng Biotechnology Co., Ltd., CAS No.: 71686-01-6;

[0042] Total glycosides of Cistanche deserticola: Sichuan Weikeqi Biotechnology Co., Ltd., wkq-17376;

[0043] Phytosterols: Campesterol, Shanghai Huicheng Biotechnology, GY1216;

[0044] Pumpkin seed oil: Ji'an Huatianbao Chinese Herbal Medicine Biology, HTBJA013;

[0045] Hemp seed oil: Jiangxi Global Natural Flavors Co., Ltd., JC-20.

[0046] Example 1

[0047] The composition of this embodiment includes the following components: 10 parts of thioneine, 15 parts of total glycosides of Cistanche, 30 parts of phytosterols, 500 parts of pumpkin seed oil, 200 parts of hemp seed oil, 220 parts of gelatin, 65 parts of glycerol, and 15 parts of xylitol.

[0048] Example 2

[0049] The composition of this embodiment includes the following components: 5 parts of ergothioneine, 10 parts of total glycosides of Cistanche, 25 parts of phytosterols, 450 parts of pumpkin seed oil, 180 parts of hemp seed oil, 180 parts of gelatin, 60 parts of glycerol, and 10 parts of xylitol.

[0050] Example 3

[0051] The composition of this embodiment includes the following components: 15 parts of thioneine, 20 parts of total glycosides of Cistanche, 45 parts of phytosterols, 550 parts of pumpkin seed oil, 250 parts of hemp seed oil, 250 parts of gelatin, 90 parts of glycerol, and 10 parts of xylitol.

[0052] Example 4

[0053] The composition of this embodiment includes the following components: 15 parts of thioneine, 10 parts of total glycosides of Cistanche, 30 parts of phytosterols, 500 parts of pumpkin seed oil, 200 parts of hemp seed oil, 220 parts of gelatin, 65 parts of glycerol, and 15 parts of xylitol.

[0054] Comparative Example 1

[0055] The composition of this comparative example includes the following components: 15 parts of total glycosides of Cistanche deserticola, 30 parts of phytosterols, 500 parts of pumpkin seed oil, 200 parts of hemp seed oil, 220 parts of gelatin, 65 parts of glycerol, and 15 parts of xylitol.

[0056] Comparative Example 2

[0057] The composition of this embodiment includes the following components: 10 parts of ergothioneine, 30 parts of phytosterols, 500 parts of pumpkin seed oil, 200 parts of hemp seed oil, 220 parts of gelatin, 65 parts of glycerol, and 15 parts of xylitol.

[0058] Comparative Example 3

[0059] The composition of this embodiment includes the following components: 10 parts of thioneine, 15 parts of total glycosides of Cistanche deserticola, 500 parts of pumpkin seed oil, 200 parts of hemp seed oil, 220 parts of gelatin, 65 parts of glycerol, and 15 parts of xylitol.

[0060] Comparative Example 4

[0061] The composition of this embodiment includes the following components: 25 parts of ergothioneine, 15 parts of total glycosides of Cistanche deserticola, 30 parts of phytosterols, 500 parts of pumpkin seed oil, 200 parts of hemp seed oil, 220 parts of gelatin, 65 parts of glycerol, and 15 parts of xylitol.

[0062] Comparative Example 5

[0063] The composition of this comparative example includes the following components: 10 parts of thioneine, 30 parts of total glycosides of Cistanche deserticola, 30 parts of phytosterols, 500 parts of pumpkin seed oil, 200 parts of hemp seed oil, 220 parts of gelatin, 65 parts of glycerol, and 15 parts of xylitol.

[0064] Test Example 1 Effect of the Composition on Lipopolysaccharide-Induced Prostate Cell Inflammation

[0065] The effects of the particles prepared in Examples 1 to 4 and Comparative Examples 1 to 5 on lipopolysaccharide-induced prostate cell inflammation were determined in the following steps:

[0066] Human prostate cancer cells (PC-3 cells) were cultured in F-12K complete medium containing 10% serum and 1% double antibody, and cultured overnight in a 37°C carbon dioxide incubator. Then, the cell density was adjusted to 3×10 6 The cells were then divided into a model group and a treatment group. The model group was treated with LPS to a final concentration of 7 μg / mL, while the treatment group was treated with the compositions of Examples 1-4 and Comparative Examples 1-5 to a final concentration of 50 μg / mL. Finally, after incubating each group for 24 hours, IL-1β, IL-6, and TNF-α were detected using ELISA kits.

[0067] The results are as follows Figures 1 to 3 As shown, compared with the model group, Examples 1 to 4 all showed significant differences in reducing the levels of prostate inflammatory factors, indicating that the above composition has a good anti-inflammatory effect and can effectively inhibit prostate inflammation. The compositions of Comparative Examples 1 to 5 were not significantly effective in treating prostate inflammation.

[0068] Test Example 2 Effect of the Composition on Prostate Cell Proliferation

[0069] Human normal prostate epithelial cells (RWPE-1 cells) were cultured with K-SFM culture medium, and 0.05 mg / mL of BPE, 5 ng / mL of EGF, and 1% of double resistance were added to the culture medium and placed in a 37 ° C carbon dioxide incubator for overnight culture. The cell density was then adjusted to 1 × 10 / mL and plated in a 96-well plate. The cells were divided into a blank group, a model group, and a drug administration group, wherein the model group and the drug administration group were both added with 0.1 μmol / L of testosterone, and the drug administration group was respectively added with the substances of the compositions of Examples 1 to 4 and Comparative Examples 1 to 5 to a final concentration of 50 μg / mL. After incubation for 24 hours, it was replaced with TP- culture medium, and the drug administration group was re-added with the compositions of Examples 1 to 4 and Comparative Examples 1 to 5, and the incubation was continued for 48 hours. Finally, the cell viability was detected using the CCK-8 method.

[0070] The results are as follows Figure 4 As shown, compared with the model group, Examples 1 to 4 have significantly reduced the survival rate and the number of prostate cells, which can effectively inhibit the excessive proliferation of prostate cells. Compared with the model group, there is no significant difference in the survival rate of prostate cells in Comparative Examples 1 to 5.

[0071] Test Example 3 Effect of the composition on mouse body weight

[0072] The purchased mice were first acclimatized in an SPF animal room for 1 week at a temperature of 21-24°C and a humidity of 50-70%. They were fed SPF mouse feed and sterile water. Their health was closely observed during the period. After confirming that there were no abnormalities, mice with similar weight and good health were randomly divided into 5 groups, namely, a control group, Example 1 group, Example 2 group, Example 3 group and Example 4 group, with 6 mice in each group, half of which were male and half were female. They were placed in different cages to avoid cross-interference and ensure that the mice could move freely and eat.

[0073] 12 hours before formal administration, mice were fasted, but free drinking water was allowed to reduce the burden on the gastrointestinal tract during administration and improve the absorption efficiency of the drug. Through precise calculation, the mice in the embodiment group were gavage-administered, and the drug was accurately prepared according to a dosage of 100 mg / kg (about 5 times the daily usage) to ensure that each mouse could obtain sufficient and uniform drug. 4 hours after administration, the normal diet of the mice was restored. They were first fed with an appropriate amount of clean water and easily digestible food, and the eating and digestion of the mice were observed to ensure that the mice were stable before returning to normal feeding. The mice were weighed every week and the weight change trend was recorded as an important indicator for evaluating drug safety and tolerance. The experiment lasted for 4 weeks, during which the experimental environment was kept stable to avoid external interference and ensure the accuracy and reliability of the experimental data. After 4 weeks, the experiment was terminated, and all data were systematically sorted and analyzed to provide a scientific basis for subsequent research.

[0074] like Figure 5 As shown, after 4 weeks of high-dose administration, there was no significant difference in body weight change among all treatment groups during the administration period, indicating that the tested composition did not cause obvious adverse reactions during long-term administration, showing its safety and good tolerance, and can be taken for a long time.

[0075] The above description is only a preferred embodiment of the present invention and is not intended to limit the present invention. Any modifications, equivalent substitutions, improvements, etc. made within the spirit and principles of the present invention should be included in the scope of protection of the present invention.

Claims

1. A composition, characterized in that The composition comprises the following components in parts by weight:

2. The composition according to claim 1, characterized in that The mass ratio of ergothioneine to total glycosides of Cistanche deserticola is 1:(1-5).

3. The composition according to claim 1, characterized in that The auxiliary materials are any one or more of edible gum, glycerin, emulsifier, filler, stabilizer, flow aid and thickener.

4. The composition according to claim 3, characterized in that The filler is any one of microcrystalline cellulose, lactose, and pregelatinized starch.

5. The composition according to claim 3, characterized in that The glidant is colloidal silicon dioxide or magnesium stearate.

6. The method for preparing the composition according to any one of claims 1 to 5, characterized in that: The steps include: S1: uniformly mixing the total glycosides of Cistanche deserticola, thioneine, and phytosterols, and adding the mixture to a mixed solution of pumpkin seed oil and hemp seed oil to obtain a mixture 1; S2: Add auxiliary materials to the mixture 1, and homogenize the mixture using a homogenizer to obtain the composition.

7. A preparation, characterized in that The preparation comprises the composition according to any one of claims 1 to 5 as an active ingredient.

8. The preparation according to claim 7, characterized in that The preparation is capsule, granule, tablet, powder, pill, oral liquid, or syrup.

9. Use of the composition according to any one of claims 1 to 5 in the preparation of medicines and / or health products for treating benign prostatic hyperplasia.

10. Use of the composition according to any one of claims 1 to 5 in the preparation of medicines and / or health products for treating prostatitis.

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