CN1313079C - Traditional Chinese medicine preparation for treating prostatitis and preparation method thereof - Google Patents

Abstract

The present invention relates to a traditional Chinese medicine preparation for treating prostatitis and a preparation technology thereof. The medicine is prepared from motherwort herb, avicularin, safflower, rape bee pollen, rhizoma anemarrhenae (sauted by salt) and amur corktree bark (sauted by salt). Compared with the prior art, the rpes invention has the characteristics of good therapeutic effect, quick apparent rate, low apse rate and small untoward reaction. The present invention has obvious clinical effect on the treating of chronic disease of prostate.

Description

Traditional Chinese medicine preparation for treating prostatitis and its preparation process

Technical field: The present invention relates to a kind of traditional Chinese medicine preparation for treating prostatitis and its preparation process, which belongs to the field of traditional Chinese medicine technology.

Technical background: Chronic prostatitis is a common and frequently-occurring disease of men. It has the characteristics of many types of diseases, high incidence rate, and older age. According to domestic statistics, its incidence rate accounts for 35% to 40% in adult men, and it has a tendency to increase year by year, causing many problems for work, life, and study. inconvenient. At present, there are many drug options for the treatment of chronic prostatitis, but the curative effect is not satisfactory, and the recurrence rate is high.

Summary of the invention: The object of the present invention is to provide a traditional Chinese medicine preparation for treating prostatitis and its preparation process. This preparation has the functions of clearing away heat and promoting dampness, promoting blood circulation and dispelling stagnation, and can effectively treat chronic prostatitis; the effect is relatively obvious, and the treatment cost Inexpensive; the preparation method process is simple, the medicine quality control is convenient, strict; the present invention is constituted like this: the traditional Chinese medicine preparation for the treatment of prostatitis: calculate according to weight component, it is made up of motherwort 187.5-1500, safflower 125-1000, safflower 62.5 -500, rapeseed bee pollen 25-200, Anemarrhena 37.5-300 and Phellodendron 37.5-300. Specifically: Calculated by weight, it is prepared from 750g of motherwort, 500g of safflower, 250g of safflower, 100g of rapeseed bee pollen, 150g of salt-fried anemarrhena and 150g of salt-fried phellodendron. The preparations are all medically permitted preparations, including oral preparations, such as: tablets, capsules, soft capsules, granules, oral liquid preparations, dripping pills, pills, wine preparations, tinctures, extracts; injection preparations, Including: ordinary injections, powder injections, freeze-dried powder injections, infusions; other special preparations, including sustained and controlled release preparations, film preparations, and gels.

The preparation process of the traditional Chinese medicine preparation for treating prostatitis: according to the weight components, take 187.5-1500 motherwort, 125-1000 safflower, 62.5-500 safflower, 25-200 rape bee pollen, 37.5-300 anemarrhena, and 37.5-300 cork phellodendri 1. Take rapeseed bee pollen and break the wall and use a high-speed pulverizer to crush it into a fine powder of more than 80 mesh; add 5-20 times the amount of water to decoct the remaining motherwort, sage, safflower, Anemarrhena, and Phellodendron 1-5 times, each time 1-5 hours, coarse filtration, 1000～10000rpm centrifugation, combined centrifuged obtained water liquid, concentrated under reduced pressure to form extract, dried under reduced pressure; dry extract was crushed into fine powder above 80 mesh, and rape bee pollen fine powder was added , and then different preparations can be made by different methods.

The capsules are prepared in the following way: the rapeseed bee pollen is broken and crushed into 120-mesh fine powder with a high-speed pulverizer. The remaining motherwort, sage, safflower, anemarrhena, and Phellodendron cork were decocted twice, each time for 2 hours, adding 12 times the amount of water for the first time, adding 10 times the amount of water for the second time, combining the decoction, and decompressing. When concentrated to 50°C, the measured relative density is 1.33-1.37. The extract is dried; the dry extract is crushed into a fine powder of 80 mesh or more, added with rape bee pollen fine powder and starch, mixed evenly, granulated with 85% ethanol, and dried. , the whole grain, filling, that is, capsules.

Tablets are prepared in the following way: take rapeseed bee pollen and break the wall and crush it into 80-mesh fine powder with a high-speed pulverizer. The remaining motherwort, succulents, safflower, anemarrhena, and cortex were decocted with 5 times the amount of water for 5 times, 5 hours each time, combined with decoction, concentrated under reduced pressure to obtain extract, and dried under reduced pressure; the dry extract was crushed into The 80-mesh fine powder is added with rapeseed bee pollen fine powder and magnesium stearate, mixed evenly, granulated with 75% ethanol, compressed into tablets, and coated with film coating auxiliary materials to obtain tablets.

The granules are prepared in the following way: the rapeseed bee pollen is broken and crushed into 80-mesh fine powder with a high-speed pulverizer. Add 10 times the amount of water to decoct the remaining motherwort, sage, safflower, Anemarrhena anemarrhena, and Cortex Phellodendri respectively for 1 hour, and centrifuge at 1000 rpm. For the fine powder, add rapeseed bee pollen and starch slurry with a concentration of 10% and mix evenly to make a soft material, sieve, make granules, dry, and granulate to obtain granules.

The pills are prepared in the following way: the rapeseed bee pollen is broken and crushed into 120-mesh fine powder with a high-speed pulverizer. Add 20 times the amount of water to decoct the remaining motherwort, sage, safflower, Anemarrhena anemarrhena, and Cortex Phellodendri, respectively, twice, each time for 2 hours, and centrifuge at 7000rpm, combine and centrifuge the obtained water, concentrate under reduced pressure to form an extract, and dry under reduced pressure; The dry extract is crushed into 120-mesh fine powder, mixed with rapeseed bee pollen fine powder, added with refined honey and boiled water with a relative density of 1.37, and made into pellets to obtain pills.

According to the theory of motherland's medicine, the present invention adopts motherwort, sage, safflower, rape bee pollen, Anemarrhena (stir-fried with salt), Phellodendron Phellodendri (stir-fried with salt). Among them, Motherwort promotes blood circulation and removes blood stasis; Leonurus can clear the dampness and heat of the lower body, diuresis and relieve stranguria; safflower pungent dissipates temperature and clears the blood, can activate blood and remove blood stasis, regulate meridians, and relieve pain; The medicine goes down, and it is specially designed to enter the kidney, and has a strong effect of nourishing yin and reducing fire, and reducing asthenic heat. The combination of various medicines can play the functions of clearing away heat and promoting dampness, promoting blood circulation and dispelling stagnation. In addition, pollen is the nemesis of prostatitis, especially rapeseed bee pollen has the best effect, so adding rapeseed bee pollen in the present invention has a good curative effect on chronic prostatitis with damp-heat holding stasis syndrome. Aiming at the prior art, the present invention breaks the wall of rape bee pollen and uses it as medicine, because the outside of the pollen has a hard spore wall that is resistant to acid, alkali and biodegradation, which cannot be directly absorbed by the human body, and its active ingredients can be strengthened after breaking the wall utilization and increase bioavailability. Compared with the prior art: the medicine provided by the invention has the characteristics of good curative effect, rapid effect, low recurrence rate and small adverse reaction. The clinical effect to the treatment of chronic prostatic disease is very remarkable; the preparation method process of the medicine provided by the invention is simple, and the product quality is easy to be controlled; especially when preparing various pharmaceutical dosage forms in the present invention, the auxiliary materials are preferably selected, so that the obtained medicine The quality of preparations can meet the requirements of relevant national standards.

Detailed ways:

Embodiment 1 of the present invention: Capsules: get Leonurus 750g, 500g of succulents, 250g of safflower, 100g of rape bee pollen, 150g of Anemarrhena anemarrhena (stir-fried with salt), 150g of Phellodendron Phellodendri (stir-fried with salt), take rape bee pollen and use after breaking the wall High-speed pulverizer crushed into 120 mesh fine powder. The remaining motherwort, sage, safflower, anemarrhena, and Phellodendron cork were decocted twice, each time for 2 hours, adding 12 times the amount of water for the first time, adding 10 times the amount of water for the second time, combining the decoction, and decompressing. When concentrated to 50°C, the measured relative density is 1.33 to 1.37. The extract is dried; the dry extract is crushed into a fine powder of more than 80 meshes, mixed with rapeseed bee pollen fine powder and starch, and granulated with 85% ethanol. Dry, granulate, and fill to obtain capsules. This product is taken orally, three times a day, 2 capsules each time.

Embodiment 2 of the present invention: Tablet: Leonurus 1500g, Leonurus 1000g, Safflower 500g, Rapeseed bee pollen 200g, Anemarrhena anemarrhena (stir-fried with salt) 300g, Cortex Phellodendri (stir-fried with salt) 300g

Get the rapeseed bee pollen and break the wall and grind it into 80 mesh fine powder with a high-speed pulverizer. The remaining motherwort, succulents, safflower, anemarrhena, and cortex were decocted with 5 times the amount of water for 5 times, 5 hours each time, combined with decoction, concentrated under reduced pressure to obtain extract, and dried under reduced pressure; the dry extract was crushed into The 80-mesh fine powder is added with rapeseed bee pollen fine powder and magnesium stearate, mixed evenly, granulated with 75% ethanol, compressed into tablets, and coated with film coating auxiliary materials to obtain tablets.

Embodiment 3 of the present invention: Granules: motherwort 187.5g, safflower 125g, safflower 62.5g

Rapeseed bee pollen 25g Anemarrhena (stir-fried with salt) 37.5g Phellodendron (stir-fried with salt) 37.5g

Get the rapeseed bee pollen and break the wall and grind it into 80 mesh fine powder with a high-speed pulverizer. Add 10 times the amount of water to decoct the remaining motherwort, sage, safflower, Anemarrhena anemarrhena, and Cortex Phellodendri respectively for 1 hour, and centrifuge at 1000 rpm. For the fine powder, add rapeseed bee pollen and starch slurry with a concentration of 10% and mix evenly to make a soft material, sieve, make granules, dry, and granulate to obtain granules.

Embodiment 4 of the present invention: Pills: Leonurus 750g, 500g of safflower, 250g of safflower, 100g of rape bee pollen, 150g of Anemarrhena (stir-fried with salt), 150g of Cortex Phellodendri (stir-fried with salt)

Get the rapeseed bee pollen and break it into a 120-mesh fine powder with a high-speed pulverizer. Add 20 times the amount of water to decoct the remaining motherwort, sage, safflower, Anemarrhena anemarrhena, and Cortex Phellodendri, respectively, twice, each time for 2 hours, and centrifuge at 7000rpm, combine and centrifuge the obtained water, concentrate under reduced pressure to form an extract, and dry under reduced pressure; The dry extract is crushed into 120-mesh fine powder, mixed with rapeseed bee pollen fine powder, added with refined honey and boiled water with a relative density of 1.37, and made into pellets to obtain pills.

In order to meet the needs of patients, this preparation can be prepared into other dosage forms, such as: soft capsules, mixtures, dripping pills, concentrated pills, and even injections; these dosage forms have their own advantages and can be used by both doctors and patients to the greatest extent; the needs of different groups of people.

Capsule quality control method of the present invention is:

Identification: Take the powder of this product and observe under a microscope: the pollen grains are light yellow, oval, sub-circular or round, and the germination holes are difficult to see, and a few have 3 germination holes.

Take 1g of the content of this product under the item of loading difference, add 5ml of ethanol to soak for 2 hours, filter, and use the filtrate as the test solution, and take another berberine hydrochloride reference substance, add methanol to make a solution containing 0.1mg per 1ml , as a reference solution. According to the thin-layer chromatography (Appendix VIB, Chinese Pharmacopoeia 2000 Edition), 3 μl of each of the above two solutions was drawn, respectively spotted on the same silica gel G thin-layer plate, and mixed with n-butanol-acetic acid-water (4:1:1) ) as the developing agent, develop, take out, dry in the air, and put it under ultraviolet light (365nm) for identification. In the chromatogram of the test product, at the position corresponding to the chromatogram of the reference product, the same yellow fluorescent spots appear.

Take 5g of the content of this product under the item of loading difference, add 30ml of methanol, ultrasonically treat for 30 minutes, filter, evaporate the filtrate to remove methanol, add 10ml of water, add to the D ₁₀₁ macroporous adsorption resin column (diameter 2.5cm , length 28cm), eluted with water until the lotion was colorless, discarded the water eluate, continued to elute with ethanol, collected 80ml of the colored part of the ethanol eluate, added 8ml of hydrochloric acid, heated to reflux for 1 hour, and washed with 40% Adjust the pH to neutral with sodium hydroxide solution, concentrate to about 10ml, add 10ml of water, add 20ml of toluene and shake to extract, separate the toluene layer, evaporate to dryness, add 1ml of toluene to the residue to dissolve as the test solution. In addition, pluckengenin was taken, and 20ml of toluene was added to make a solution containing 5mg per 1ml, as a reference substance solution. According to the thin-layer chromatography (Appendix VIB, Chinese Pharmacopoeia 2000 Edition), 5 μl of each of the above two solutions was drawn, respectively spotted on the same silica gel G thin-layer plate, and toluene-acetone (8.5:1.5) was used as the developer to develop , take it out, dry it in the air, spray it with 5% vanillin sulfuric acid solution to develop color, and bake it at 105°C until the spot color develops clearly. In the chromatogram of the test product, there are spots of the same color at the position corresponding to the chromatogram of the reference product.

Determination of content: stachydrine hydrochloride is measured according to high performance liquid chromatography (an appendix VID of Chinese Pharmacopoeia 2000 edition), and the cation exchanger of sulfonic acid group bonded silica gel (SCX) is used as filling for chromatographic conditions and system suitability test agent; use 0.05mol/L potassium dihydrogen phosphate-triethylamine (100:0.1) (adjust the pH value to 2.3 with phosphoric acid) as the mobile phase; the detection wavelength is 192nm. The number of theoretical plates should not be less than 1500 based on the calculation of stachydrine hydrochloride.

For the preparation of the reference substance solution, accurately weigh an appropriate amount of stachydrine hydrochloride reference substance, add methanol to make a solution containing 0.5mg per 1ml, and get final product;

For the preparation of the test solution, get 20 capsules of this product, pour out the contents, grind finely, and accurately weigh 1.5g, put it in a conical flask, add 50ml of ethanol accurately, weigh it, and ultrasonically process it (150W, 50kHz) for 30 minutes. Minutes, take it out, let it cool, weigh it, make up the lost weight with ethanol, filter, accurately measure 25ml of the subsequent filtrate, evaporate to dryness in a water bath, add 20ml of water to the residue to dissolve, transfer it quantitatively to a separatory funnel, and use ethyl acetate Extract the ester three times, 25ml each time, discard the ethyl acetate solution, evaporate the water to dryness in a water bath, add 10ml of ethanol to the residue to dissolve, and add it to a neutral alumina-activated carbon column (inner diameter 150mm, 3g: 1g, 100-200 purpose, ethanol wet column, first on alumina, then on activated carbon), elute with ethanol, collect eluent 100ml, evaporate to dryness in a water bath, add 0.05mol/L phosphoric acid to dissolve the residue and transfer it to a 10ml measuring bottle, add 0.05mol/L phosphoric acid to the mark, shake well, and centrifuge to obtain;

Determination method, respectively accurately absorb 20 μ l of the reference substance solution and the test solution, inject it into the liquid chromatograph, measure, and obtain that each capsule of this product contains stachydrine hydrochloride (C ₇ H ₁₃ ClNO ₂ ) not less than 2.4 mg .

Clinical efficacy:

1. Treatment objects and items: Anyone who meets the diagnostic criteria of Western medicine for CP and the criteria for excluding cases can be included in the scope of research objects. Subjective symptom inquiry before and after treatment, including four groups of symptoms such as pain or discomfort symptoms, urinary tract symptoms, sexual and reproductive symptoms, and systemic symptoms; , knot and other six aspects; comparative analysis of comprehensive curative effect.

Two, treatment method: check blood, urine, stool routine and liver, kidney function before treatment, and normal person is given the aqueous preparation of medicine of the present invention, takes continuous medication for one month, checks blood, urine, stool routine and liver, kidney function, during treatment Without other drugs. Observational research on curative effect was carried out.

3. Clinical curative effect:

1. In order to facilitate the discussion of the improvement of CP symptoms by the present invention, we observed from four aspects of pain or discomfort symptoms, urinary tract symptoms, sexual and reproductive symptoms and systemic symptoms, and the results are shown in the following table: symptom no get well markedly effective get better invalid efficient(%) Pain or discomfort Urinary tract symptoms Sexual and reproductive symptoms Systemic symptoms 122128116124 44654355 37322822 30292137 1122410 90.9898.4479.3191.94

From the results, it can be seen that the present invention has a better effect on improving the pain or discomfort symptoms, urinary tract symptoms, sexual and reproductive symptoms and systemic symptoms of CP, especially for urinary tract symptoms.

2. Prostate digital examination: 66 cases were cured, 37 cases were markedly effective, 15 cases were improved, 22 cases were ineffective, and the effective rate was 81.67%. The result shows that the present invention has a better effect on the local signs of the prostate.

3. Observation of side effects: 140 routine CP patients had no obvious discomfort after taking the medicine of the present invention, and blood, urine, stool routine and liver and kidney function tests were all normal.

4. Comprehensive curative effect evaluation: According to the curative effect evaluation standard, among 140 CP patients, 64 cases were cured, accounting for 45.71%; 37 cases were markedly effective, accounting for 26.43%; 22 cases were improved, accounting for 15.71%; 17 cases were ineffective, accounting for 12.14%. The total effective rate is 87.85%. It can be seen that the present invention has a good therapeutic effect on CP.

Experiment: excipient screening

During the preparation process, whether the added auxiliary materials are appropriate directly affects the quality of the preparation and the effect of clinical application, so the applicant conducted a series of experiments to obtain the best process.

Angle of repose is measured using the tilting box method: fill a rectangular box with fine powder, the degree of looseness is appropriate, and gradually tilt the box until the fine powder starts to flow out. The angle at which the box is tilted is the angle of repose. If the result is greater than 45%, the fluidity is poor and easy to loose.

Hygroscopicity test: take the test product, about 2g, put it in a weighing bottle, weigh it accurately, open the cap of the weighing bottle, put it into an environment with a relative humidity of 92%, and place it in a constant temperature incubator at 25°C for 84 hour, take out the weighing bottle, accurately weigh after capping, and calculate the percentage of moisture absorption. The lower the value of the result, the less hygroscopic it is.

Disintegration time limit inspection: use the rotating basket method, lift-type disintegration apparatus, take 6 tablets and 6 capsules, and observe the situation of passing through the sieve within 30 minutes. Pills Take the pills and observe how they pass through the sieve within 60 minutes. The higher the pass rate, the better the disintegration, which is more suitable for human body absorption. Capsules D ethanol syrup gelatin paste Concentration (%) Angle of repose (°) Hygroscopicity test (%) Disintegration time limit 2055272 5046252 8540181 3045233 5048251 7050221 1046252 2048273 3043242

tablet D Ethanol Syrup Gelatin paste Concentration (%) Angle of repose (°) Hygroscopicity test (%) Disintegration time limit 2554252 5545261 7542190 3043253 5046221 7050224 1046271 2047253 3042242

Granules D Ethanol Syrup   Starch Slurry Concentration (%) Angle of repose (°) Hygroscopicity test (%) Disintegration time limit 2054252 5545261 8042271 3045253 5046221 7051243 1042201 2047253 3044244

Pills Refined honey Relative density hygroscopicity test (%) disintegration time limit 1.35452 1.37331 1.40503

Through the auxiliary material screening experiment, the preparation made by using the selected auxiliary material in the present invention has stable quality, controllable product quality and good formability.

Claims (5)

1. A traditional Chinese medicine preparation for treating prostatitis. Calculated according to weight components, it consists of motherwort 187.5-1500,  storage 125-1000, safflower 62.5-500, rape bee pollen 25-200, Anemarrhena 37.5-300 and Phellodendron Phellodendri 37.5-300 prepared into tablets, capsules, granules or pills; characterized in that: according to weight components, take motherwort 187.5-1500,  storage 125-1000, safflower 62.5-500, rape bee pollen 25-200 , Anemarrhena 37.5-300, Phellodendron 37.5-300, take rapeseed bee pollen and break the wall and use a high-speed pulverizer to crush it into a fine powder above 80 mesh; Decoct with twice the amount of water for 1-5 times, 1-5 hours each time, coarsely filter, centrifuge at 1000-10000rpm, combine and centrifuge the obtained water, concentrate under reduced pressure to obtain extract, and dry under reduced pressure; dry extract is crushed into 80 mesh Add rape bee pollen fine powder to the above fine powder, and then use different methods to make different preparations. 2. The traditional Chinese medicine preparation for treating prostatitis according to claim 1, characterized in that: the capsule is prepared in the following way: take the rapeseed bee pollen and break the wall and crush it into a 120-mesh fine powder with a high-speed pulverizer. The remaining motherwort,  storage, safflower, Anemarrhena, and Cortex Phellodendri were decocted twice, each time for 2 hours, adding 12 times the amount of water for the first time, adding 10 times the amount of water for the second time, combining the decoction, and decompressing. When concentrated to 50°C, the measured relative density is 1.33-1.37. The extract is dried; the dry extract is crushed into a fine powder of 80 mesh or more, added with rape bee pollen fine powder and starch, mixed evenly, granulated with 85% ethanol, and dried. , the whole grain, filling, that is, capsules. 3. The traditional Chinese medicine preparation for treating prostatitis according to claim 1, wherein the tablet is prepared in the following way: taking rapeseed bee pollen and crushing it into a 80-mesh fine powder with a high-speed pulverizer. The remaining motherwort,  storage, safflower, Anemarrhena, Phellodendron cortex were decocted with 5 times the amount of water for 5 times, 5 hours each time, combined with water decoction, concentrated under reduced pressure to obtain an extract, dried under reduced pressure; the dry extract was crushed into The 80-mesh fine powder is added with rapeseed bee pollen fine powder and magnesium stearate, mixed evenly, granulated with 75% ethanol, compressed into tablets, and coated with film coating auxiliary materials to obtain tablets. 4. The traditional Chinese medicine preparation for treating prostatitis according to claim 1, characterized in that the granules are prepared in the following way: take rapeseed bee pollen and break the wall and crush it into 80-mesh fine powder with a high-speed pulverizer. Add 10 times the amount of water to decoct the remaining motherwort,  storage, safflower, Anemarrhena anemarrhena, and Cortex Phellodendri respectively for 1 hour, and centrifuge at 1000 rpm. For the fine powder, add rapeseed bee pollen and starch slurry with a concentration of 10% and mix evenly to make a soft material, sieve, make granules, dry, and granulate to obtain granules. 5. The traditional Chinese medicine preparation for treating prostatitis according to claim 1, characterized in that: the pill is prepared in the following way: take the rapeseed bee pollen and break it into a 120-mesh fine powder with a high-speed pulverizer. Add 20 times the amount of water to decoct the remaining motherwort,  storage, safflower, Anemarrhena anemarrhena, and Phellodendron Phellodendri respectively, for 2 hours each time, centrifuge at 7000 rpm, combine and centrifuge the obtained water, concentrate under reduced pressure to form an extract, and dry under reduced pressure; The dry extract is crushed into 120-mesh fine powder, mixed with rapeseed bee pollen fine powder, added with refined honey and boiled water with a relative density of 1.37, and made into pellets to obtain pills.