CN1327874C - Chinese medicine formulation for treating chronic prostatitis and its preparing method - Google Patents

Abstract

The invention relates to a traditional Chinese medicine preparation for treating chronic prostatitis and a preparation method thereof, which is mainly prepared from Polygonum cephalosporin and Rhizoma Chuanxiong; adding ethanol to Polygonum cephalosa and Rhizoma Chuanxiong, refluxing extraction, and filtering to obtain a filtrate; recovering ethanol from the filtrate And be concentrated to the thick paste of certain relative density; The thick paste is dried and pulverized into fine powder, has just prepared the active component of Chinese medicine preparation of the present invention; The active component that obtains is prepared into required preparation according to conventional method; This The preparation has unique curative effect on treating urinary system infection and can effectively treat chronic prostatitis.

Description

Traditional Chinese medicine preparation for treating chronic prostatitis and preparation method thereof

Technical field: The present invention relates to a traditional Chinese medicine preparation for treating chronic prostatitis and a preparation method thereof, belonging to the technical field of traditional Chinese medicine.

Background technology: Chronic prostatitis belongs to the category of "lench syndrome", "white turbidity", "lumbar pain" and "sperm turbidity" in traditional Chinese medicine. Its incidence, observed from the pathological point of view, accounts for about 30-50% of autopsies; the epidemiology of the population has not yet seen complete statistics, but most authors report that it accounts for about 35% of adult male patients in urology outpatient clinics . Chronic prostatitis is a clinical syndrome mainly manifested by lower urinary tract symptoms and local pain. It is often composed of several diseases with unique forms caused by different reasons, so it is also called Chronic Prostatitis Syndromes. , CPS). The pathological features of chronic prostatitis are: ①multifocal; ②inflammation wrapping; ③obstruction of glandular ducts, poor drainage; ④fibrosis of glandular lobe. At present, western medicine generally adopts antibiotics to treat this disease; however, the effect is not satisfactory. The reasons are as follows: ① For a small number of bacterial prostatitis with a clear etiology, the antibacterial drugs cannot fully penetrate into the gland due to the barrier function of the prostate acinar epithelium. and the majority of non-bacterial prostatitis are ineffective with antibiotics; ②The above-mentioned pathological and anatomical characteristics make it difficult for the drug to reach the sick place, or cannot form an effective blood drug concentration after arriving at the sick place , and low concentrations of drugs can easily induce drug resistance of pathogenic microorganisms; ③ abnormal systemic or local immunity.

Although this disease generally does not cause serious damage to important organs and is life-threatening, due to the special symptoms of the disease, patients often suffer from abnormal pain, which not only affects the quality of life of the patient himself, but also may affect family happiness and even social labor. productivity. In recent years, more and more data show that the rate of antibiotic resistance is gradually increasing, and once bacteria enter the prostate from the urethra or blood circulation, treatment becomes quite difficult. For non-bacterial prostatitis, antibiotics appear redundant and powerless. Some people tried α-receptor blockers or non-steroidal drugs for symptomatic treatment, and their efficacy was not optimistic. In recent years, the use of herbal medicines to treat this disease (such as Shenitong) has also appeared in foreign countries, and certain clinical curative effects have been achieved. However, with the continuous improvement of living standards, people are more advocating natural therapy, and the quality and quantity of medical care have been raised. higher requirement. Therefore, it is very necessary to seek new drugs with high efficiency and low toxicity. In recent years, reports on the treatment of chronic prostatitis by traditional Chinese medicine have increased year by year, and there are many researches on the development of new Chinese medicines for this disease, but most of the products have single functions and the therapeutic effect is not particularly satisfactory. Through long-term clinical practice, we have conducted an in-depth discussion on the pathogenesis of chronic prostatitis, and believe that damp-heat injection, qi and blood stasis are the basic pathogenesis, and only by examining the cause and treating it can the curative effect be improved.

SUMMARY OF THE INVENTION: The object of the present invention is to provide a traditional Chinese medicine preparation for treating chronic prostatitis and its preparation method.

The present invention utilizes the excellent antibacterial and anti-inflammatory activity of Polygonum cephalosporin in combination with the theory of traditional Chinese medicine and many years of clinical treatment experience of famous old Chinese medicine practitioners. Traditional Chinese medicine is composed of empirical prescriptions, which are used for frequent urination, urgency, dripping urine, hot or cloudy urethra caused by damp-heat injection, qi and blood stagnation; chronic prostatitis such as perineum, lower abdomen, lumbosacral pain, etc. see the above syndrome waiting.

The present invention is constituted as follows: the traditional Chinese medicine preparation for treating chronic prostatitis: calculated according to weight components, it is mainly prepared from Polygonum cephalosporin 10-50, Ligusticum chuanxiong 5-20; Chuanxiong 12g prepared. The preparation method of the traditional Chinese medicine preparation for treating chronic prostatitis: Weigh the raw materials Polygonum cephalosporin and Rhizoma Chuanxiong, add 8-20 times the amount of 30-80% ethanol to the Polygonum cephalosporin and Rhizoma Chuanxiong in the weight ratio, and reflux extraction 1-5 times, 1-5 hours each time, combine the extracts and filter to obtain the filtrate; recover the ethanol from the filtrate and concentrate it to a thick paste with a certain relative density; dry the thick paste and grind it into fine powder to prepare the The active component of the traditional Chinese medicine preparation of the present invention; the obtained active component is prepared into a required preparation according to a conventional method. The traditional Chinese medicine preparation for treating chronic prostatitis: calculated according to the weight components, there are also: 5-25g of fennel and 2-15g of Angelica dahurica. That is to say: this traditional Chinese medicine preparation for the treatment of chronic prostatitis is prepared from Polygonum cephalum 30g, Ligusticum chuanxiong 12g, Rhizome 12g and Angelica dahurica 10g. The preparation method of this traditional Chinese medicine preparation for the treatment of chronic prostatitis: take the raw materials Polygonum cephalosporin, Rhizoma Chuanxiong, Rhizoma Fructus and Angelica dahurica, and add Polygonum cephalosporin, Rhizoma Chuanxiong, Rhizoma Fructus and Radix Angelicae Dahurica by 8-20 times Measure 30-80% ethanol, reflux extraction 1-5 times, 1-5 hours each time, combine the extracts, filter to obtain the filtrate; recover the ethanol from the filtrate and concentrate it to a thick paste with a certain relative density; dry the thick paste And pulverized into fine powder, just prepared the active component of the traditional Chinese medicine preparation of the present invention; The obtained active component is prepared into oral preparation or injection preparation according to conventional methods.

Further speaking: the traditional Chinese medicine preparation for treating chronic prostatitis: calculated according to the weight components, there is also Achyranthes bidentata 5-25. Therefore, this pharmaceutical preparation is prepared from: Polygonum cephalosporin 30g, Rhizoma Chuanxiong 12g, Rhizome 12g, Angelica dahurica 10g and Achyranthes bidentata 12g.

Its preparation method: Weigh Polygonum cephalosporin, Rhizoma Chuanxiong, Rhizoma fennel, Angelica dahurica and Achyranthes bidentata as raw materials, and add 8-20 times the weight ratio of Polygonum cephalosporin, Rhizoma chuanxiong, Rhizoma fennel, Angelica dahurica and Achyranthes bidentata. Measure 30-80% ethanol, reflux extraction 1-5 times, 1-5 hours each time, combine the extracts, filter to obtain the filtrate; recover the ethanol from the filtrate and concentrate it to a thick paste with a certain relative density; dry the thick paste And be pulverized into fine powder, just prepared the active component of Chinese medicine preparation of the present invention; The active component that obtains is prepared into oral preparation according to conventional method, comprises: granule preparation (containing effervescent granule), hard capsule preparation, soft capsule Preparations, tablet preparations (including effervescent tablets, controlled-release tablets, sustained-release tablets, orally disintegrating tablets, chewable tablets, etc.), dropping pill preparations, oral liquids, and syrup preparations. The more specific preparation method is as follows: weigh Polygonum cephalum 30g, Rhizoma Chuanxiong 12g, Rhizome 12g, Angelica dahurica 10g and Achyranthes bidentata 12g, add 8-20 times the amount of 30-80% ethanol, reflux extraction 1-5 times, each After 1-5 hours, combine the extracts, filter to obtain the filtrate, recover the ethanol from the filtrate and concentrate it to a thick paste with a certain relative density, dry and pulverize it into a fine powder, add appropriate amount of auxiliary materials, mix well, and granulate to make 1000g of granules , to obtain granules.

The active components of the Chinese medicine preparation obtained in the present invention can be prepared by adding various conventional adjuvants required when preparing different dosage forms, such as disintegrants, lubricants, adhesives, etc., into any commonly used preparation.

The present invention is based on the Miao medicine Polygonum cephalosporin and its single preparation Relinqing granule which has unique curative effect on treating urinary tract infection. Combination, the combination of these drugs makes the effects of each drug synergistic and can effectively treat chronic prostatitis. Among them, Polygonum cephalosa tastes slightly bitter, pungent, cool in nature, and returns to the kidney and bladder meridian. Grass or ground part, has the functions of clearing heat and dampness, detoxifying and relieving pain, promoting blood circulation and dispelling blood stasis, diuresis and treating stranguria, used for dysentery, nephritis, cystitis, urinary tract stones, pelvic inflammatory disease, prostatitis, rheumatism, bruises, sores Eczema etc. This medicine is very suitable for the syndrome of "heat-drenching" mentioned in traditional Chinese medicine, so Polygonum cephalosporin is used as the king medicine in this prescription. Chuanxiong is pungent in taste and warm in nature, and belongs to the liver, gallbladder, pericardium, and triple burner meridians. "Drugs and Chemicals" contains: "Chuanxiong enters the three meridians of liver, gallbladder, and triple burner." "It belongs to pure yang" and "can ascend and descend." It is called "blood qi medicine", which is good at treating blood stasis and qi stagnation. It ranks first among the medicines for promoting blood circulation and removing blood stasis. Ligusticum Chuanxiong and Polygonum cephalosporin are compatible, which not only has the functions of clearing heat and dampness, diuresis and treating stranguria, but also enhances the effect of unblocking Qi and blood, promoting blood circulation and relieving pain, so it is a ministerial drug. Fenxuezi is bitter in the mouth and flat in nature. Return kidney, stomach warp. "Compendium of Materia Medica" contains: "Bird wormwood can treat white turbidity, pain in the stem, hemorrhoids and bad sores." "Yielin Urgyao·Medicinal Properties" pointed out that wormwood can "slow the liver, strengthen the kidney, clear the small intestine fire, and dissolve bladder water." "Chinese Materia Medica" says that the function of scorpion is to clear away dampness and heat, distinguish turbidity from secretion, and dispel wind and dry dampness. It is mainly used for syndromes such as white turbidity, ointment stranguria, leukorrhea, and rheumatic arthralgia. It is an important medicine for treating dampness and stasis in the lower Jiao and cloudy urine. For example, in the syndrome of stranguria, it is often used to add and subtract the Qingyin, and take the medicine as the main medicine to treat dampness and heat, mixed clear and turbid, symptoms such as turbid urine, short red urine, burning hot astringent pain in the urethra, etc., and the curative effect is quite good. In this prescription, it is mainly compatible with Polygonum cephalosporin to enhance the effect of clearing dampness and heat in the lower jiao, distinguishing turbidity, diuresis and treating stranguria. Angelica dahurica is pungent in taste, warm in nature, and belongs to the lung, large intestine, and stomach meridians. Function Tongqiao pain relieving, dispelling wind and dehumidification, reducing swelling and evacuating pus. Clinically, it is mostly used for pain diseases, leukorrhea, carbuncle and sores in women. For example, it is stated in "The Classic": "The main woman leaks the red and white, and the blood closes the yin and swells." Women have bleeding and low back pain, which can erode pus." In the stranguria syndrome, this medicine is often used together with Chuanxiong to enhance the effect of promoting qi and blood circulation, stimulating menstruation and relieving pain (such as Duliang pill). In addition, Angelica dahurica is also a commonly used drug in traditional Chinese medicine surgery. For example, the classic surgical prescription Jinhuang ointment and Chonghe powder all use Angelica dahurica, which has the function of promoting blood circulation, reducing swelling, promoting qi and relieving pain. It is generally used for the initial onset of carbuncle, swelling and pain, diffuse swelling without head embolism. Therefore, Fenxue and Baizhi are used as adjuvant drugs in the prescription to help the monarch and ministers. Achyranthes bidentata is sour in taste, bitter, and flat in nature, and returns to the Liver and Kidney Channels. "Chinese Materia Medica" calls it Achyranthes bidentata to show its difference from Sichuan Achyranthes bidentata. "Compendium of Materia Medica" pointed out: "Achyranthes bidentata tastes thick and qi is thin, and it can nourish when walking, and its nature is good and descends, so it enters the liver and kidney." Jie." Its functions have the functions of nourishing liver and kidney, strengthening tendons and bones, promoting blood circulation to stimulate menstruation, drawing blood downward, diuresis and treating stranguria. Cure mainly soreness of waist and knees, flaccidity and weakness of lower limbs, amenorrhea due to stagnation of blood, stranguria with heat, stranguria with blood, carbuncle, swelling and malignant sore. As pointed out in "Compendium of Materia Medica", Achyranthes bidentata "cures chronic malaria, cold and heat, five stranguria, hematuria, pain in the stem, diarrhea, carbuncle and malignant sore." etc. Therefore, Achyranthes bidentata is often combined with Rhizoma Chuanxiong, Eucommia, and Parasitic to enhance the effects of nourishing liver and kidney, strengthening muscles and bones, promoting blood circulation and relieving pain. It is often used together with Phellodendron Phellodendri, Rhizoma Phellodendri, and Plantago, and enters the lower burner to clear away dampness and heat, diuresis and relieve stranguria. In addition, Achyranthes bidentata can induce various medicines to descend, and can also be used as medicine for guiding scriptures, so it is used as envoy medicine. Achyranthes bidentata is compatible with the above four herbs, which not only has the effect of nourishing the liver and kidney, but also enhances the functions of diuresis and stranguria, promoting blood circulation and removing blood stasis.

Taking a comprehensive view of the whole prescription, guided by the theory of traditional Chinese medicine, warm and cool medicines are used together, the symptoms and root causes are treated together, and both attack and tonic are used, which is mainly to attack evil. The formula is reasonable, the medicine is precise and appropriate, and it has local characteristics. The combination of various medicines can clear away heat and dampness, diuresis and relieve stranguria, promote blood circulation and relieve pain, and also have the effect of nourishing liver and kidney.

Experimental research in the pharmacology laboratory of the Sichuan Antibiotic Industry Research Institute shows that Polygonum cephalum has obvious anti-pathogenic microorganisms and a wide antibacterial spectrum, including a variety of Gram-positive bacteria, Escherichia coli, Neisseria gonorrhoeae, Proteus, urealyticum Mycoplasma, Chlamydia trachomatis, etc., and these may be the pathogens that cause prostatitis. The diuretic effect experiment of Polygonum cephalosporin extract powder on anesthetized rabbits and normal rats: It is confirmed that the drug 17.4g crude drug/kg dose has obvious diuretic effect on anesthetized rabbits; 8.7g crude drug/kg dose has obvious diuretic effect on normal rats It has obvious diuretic effect. At the same time, Polygonum cephalosporin extract powder has a good anti-inflammatory effect on inflammatory models such as rat paw swelling, mouse ear swelling and rat granuloma, and has a good dose-effect relationship. In addition, Polygonum cephalum is used in mouse pain models created by writhing method and radiation heat stimulation method, and it is confirmed that it has a certain analgesic effect. Polygonum cephalosporin extract powder 4g/Kg was administered to rats with prostatitis for 20 consecutive days, and it had obvious therapeutic effect on the prostatitis of rats. The above pharmacological effects such as antibacterial, anti-inflammatory, diuretic, and analgesic not only target pathogens, but also target unfavorable pathological factors, which provides an experimental basis for the selection of Polygonum cephalosporin as a monarch drug. Ligusticum chuanxiong contains ligustrazine, which can regulate blood coagulation and reduce the viscosity of whole blood; it can significantly increase coronary flow in isolated rat or guinea pig hearts; Aggregation can be significantly inhibited, and the aggregated platelets can be quickly depolymerized; it can improve the deformation of red blood cells in rabbits and reduce the viscosity of whole blood; in addition, Ligustrazine can significantly increase the blood flow of rabbit kidneys, and has a significant diuretic effect. Therefore, modern studies have confirmed that Rhizoma Chuanxiong does have obvious effects of promoting blood circulation, removing blood stasis, promoting qi and relieving pain. Lemongrass, whose rhizome contains saponin A, diosgenin, etc., has obvious antifungal effect, and has the effect of lowering blood fat and reducing the incidence of aortic atherosclerosis. Angelica dahurica, its root contains imperatorin, isoimperatorin and various trace elements. It has antipyretic, analgesic and anti-inflammatory effects. Baizhi decoction can be administered into the stomach, and the hot plate test of mice can significantly increase the pain threshold, and it can also significantly inhibit the ear inflammation of mice caused by xylene. Experimental studies have confirmed that isoimperatorin has an antispasmodic effect on the ileum of rabbits. The results of in vitro experiments show that Angelica dahurica has different degrees of inhibitory effects on Escherichia coli, Shigella, Proteus, typhoid and paratyphoid bacillus, Pseudomonas aeruginosa and some Gram-positive bacteria. Achyranthes bidentata contains triterpene saponins and a variety of polysaccharides, etc., which have obvious anti-inflammatory and analgesic effects; Achyranthes bidentata decoction administered into the stomach has significant effects on the high and low shear rate whole blood viscosity and erythrocyte aggregation index of normal rats. Reducing the effect can prolong the prothrombin time and plasma recalcification time, which can partly explain the mechanism of Achyranthes bidentata for promoting blood circulation. In addition, experiments have shown that Achyranthes bidentata has an immune-enhancing effect on animals with normal or low immune function. The above pharmacological experimental results provide an experimental basis for the rationality and effectiveness of this prescription.

The prescription of this product is designed for chronic prostatitis with damp-heat and blood stasis syndrome on the basis of pharmacological research and clinical practice experience, following the theory of traditional Chinese medicine and the principle of formulating prescriptions. This product is based on clearing away heat and dampness, promoting blood circulation and relieving pain. After the applicant completed the prescription demonstration, fixed dosage form, and optimized process, he also completed the quality standard, safety and pharmacodynamic experiments to prove that this prescription is effective for the treatment of chronic prostatitis. Safe and effective preparation.

Pharmacy Section:

Formulation and Process Studies:

The determination of the extraction process route of this process is based on consulting the modern research literature of traditional Chinese medicine at home and abroad. Two preparation techniques. And the extract powder of the present invention prepared by these two kinds of processes is tested sample, compares the advantages and disadvantages of two kinds of extraction process extracts of the preparation of the present invention from antibacterial and anti-inflammation angle respectively, research result shows: alcohol extraction process extract Antibacterial and anti-inflammatory is better. Therefore determined that preparation technology of the present invention is alcohol extraction technology. And the alcohol extraction process was optimized by orthogonal test, three repeated tests were carried out according to the L ₉ (3 ⁴ ) orthogonal test arrangement table, with the extract yield and quercetin content as indicators, the ethanol concentration, ethanol dosage, extraction time , extraction frequency four factors were optimized and investigated, and the best extraction process was selected. Finally, the selection of the granulation method, the selection of the type of excipients and the determination of the dosage, the determination of the water content of the powder, the determination of the granulation pressure and other molding process research were carried out, and the formulation prescription and production method were determined. The pilot scale-up test proves that the process is simple and easy to operate, and it is suitable for large-scale production.

Quality Standards Study:

According to the relevant requirements under the Chinese Pharmacopoeia (version one in 2000) granules and the "Measures for the Administration of Drug Registration", a large number of literature searches have been carried out. illustrate. Adopt thin-layer chromatography to carry out qualitative identification to Rhizoma Chuanxiong, Rhizoma Fenugreek, Angelica dahurica, and Achyranthes bidentata in the present invention, wherein the Rhizoma Rhizoma Chuanxiong is used as a qualitative index to identify Rhizoma Chuanxiong, Diosgenin is used as a qualitative index to identify Rhizoma Rhizoma Rhizome, and Radix Angelicae Dahurica is used as a qualitative index Indexes are used to identify Angelica dahurica, and oleanolic acid is used as a qualitative index to identify Achyranthes bidentata. The results showed that the three batches of samples (batch numbers were 040801, 40802, and 040803 respectively) all showed the same color spots on the corresponding positions of the reference substance or reference medicinal material chromatogram, negative without interference, and included in the main text. With reference to "Guizhou Provincial Traditional Chinese Medicinal Materials, Ethnic Medicinal Materials Quality Standards" content measurement item of "Polygonum cephalum" recorded, with reference to high performance liquid chromatography ("Chinese Pharmacopoeia" 2000 edition an appendix VID), the content of quercetin in the present invention Content determination is carried out research, through methodological systematic investigation and the content determination of three batches of samples (batch numbers are respectively 040801, 040802, 040803), quercetin is well separated from other components in the present invention, and quercetin is in the scope of 0.0804～0.4823 μ g The linearity was good, the average addition yield was 98.61%, RSD=1.13% (n=5). The results show that this method is simple, rapid, specific, sensitive and accurate. And it is stipulated that each bag of this product should contain no less than 5.6mg of quercetin. At the same time, it is stipulated that each index of the granule is in compliance with the relevant regulations under the granule item of Appendix I of "Chinese Pharmacopoeia" 2000 edition.

The results show that the standard is stable and easy to implement, has strong controllability and good repeatability, and can control the quality of the present invention.

Preliminary Stability Study:

Room temperature test:

In accordance with the "Technical Requirements for Stability Research of New Traditional Chinese Medicines" and regulations, three batches of samples (batch numbers 040801, 040802, and 040803) were packaged with drugs for clinical trials and investigated at room temperature. The inspection time is 3 months, except for the inspection once in the current month, and the inspection will be conducted once a month thereafter. The assessment items are formulated according to the draft quality standards for clinical trial drugs, combined with the investigation items required for granules in the "Stability Test Requirements for New Traditional Chinese Medicines". The proposed assessment items are: traits, identification, inspection (particle size, moisture, solubility, packaging amount difference, microbial limit), content determination. It is detected by the detection method stipulated in the draft quality standard of drugs for clinical trials. Assessment results: The three batches of samples were placed at room temperature for 3 months, and compared with the "0" month, there was no significant change in all test indicators, indicating that the quality of this product is basically stable.

Accelerated Test Study:

The investigation project is drawn up with reference to the quality standard (draft) of the drug for clinical trials of the present invention, and in conjunction with the investigation project required by the "Traditional Chinese Medicine New Drug Stability Test Requirements", the accelerated test research of the present invention has been carried out. Three batches of samples (batch numbers respectively 040801, 040802, and 040803) were subjected to a three-month accelerated test (40°C ± 2°C, 75% ± 5% RH) in drug packaging for clinical trials. Softening), identification, inspection (particle size, moisture, solubility, loading difference, microbial limit), and content determination items. Compared with the "0" month, the test indicators of each item have no obvious changes, indicating that the quality of this product is basically stable. , the packaging materials used have no effect on the drug.

The research results of the above pharmacy part show that the process of the present invention is reasonable and feasible, and the quality is stable and controllable.

Pharmacology and Toxicology:

Main pharmacodynamic studies:

Anti-inflammatory test results show that, compared with the vehicle control group, high, medium and low dose groups (20.0, 10.0, 5.0g crude drug/kg) of the present invention can obviously suppress the ear swelling caused by xylene (p＜0.01), swelling inhibition The rates are 80.6%, 77.4% and 67.7% respectively. The high, medium and low dose groups (14.4, 7.2, 3.6 g/kg) of the present invention all have inhibitory effect on the formation of rat cotton ball granuloma, and the inhibition rates are 28.8%, 15.7% and 21.5% respectively.

The results of the analgesic test showed that, compared with the vehicle control group, the high dose group (20.0 g/kg) of the present invention could significantly inhibit the writhing times of mice caused by acetic acid (p<0.05). Compared with before administration, the high-dose group of the present invention has inhibitory effect on the pain caused by heat radiation irradiation on rat tails, and the pain threshold is increased by 69.1%.

The results of the carbon particle clearance test show that the high, middle and low dose groups (20.0, 10.0, 5.0g/kg) of the present invention can significantly increase the K value of the phagocytosis rate, the half-life of phagocytosis is obviously prolonged, and can promote the phagocytosis of the reticuloendothelial system in mice ability.

Carrageenan causes rat acute prostatitis test result to show, compares with model group, the present invention's high, middle dosage (14.4,7.2g/kg) makes the leukocyte number in the rat prostatic fluid significantly reduce, lecithin corpuscle density Significantly increased, with significant statistical significance (p<0.01, p<0.05). Histopathological results showed that there was no significant change in the morphology of the prostate tissue in the normal control group, but in the model group, hyperemia, edema, and obvious inflammatory cell infiltration were seen in the prostate tissue. Compared with the model group, the low-dose group (3.6g/kg) of the present invention has no obvious improvement on the morphology of the rat prostate, and obvious prostate edema and inflammatory cell infiltration can be seen, but the gland damage is lighter. Compared with the model group, the high and middle dose groups (14.4, 7.2g/kg) of the present invention have obvious improvement on the morphology of the rat prostate, wherein both of them can significantly reduce interstitial edema and gland destruction (p<0.01) , the high dose significantly reduced the inflammatory cell infiltration (p<0.05), and the middle dose significantly reduced the inflammatory cell infiltration (p<0.01). Inspection conclusion: Compared with the model group, the middle and high dose groups of the present invention have improved the morphology of prostatitis in rats, and there is no significant difference between the two.

Carrageenan-induced rat chronic prostatitis test results show that, compared with the model group, the high-dose group rat prostate coefficient of the present invention significantly reduces, and has inhibitory effect on carrageenan-induced rat prostatic hyperplasia (p＜0.05) . Histopathological results showed that compared with the model group, the histomorphology of the low and middle dose groups of the present invention had no obvious improvement. The high-dose group of the present invention significantly reduces fibroblast proliferation and inflammatory cell infiltration (p<0.05), and the histomorphology of the high-dose group of the present invention is significantly improved.

The results of acute blood stasis rat test showed that after the rats were modeled, the low, medium and high shear whole blood viscosity and hematocrit increased significantly compared with the normal control group. Compared with the model group, the high and middle dose groups (14.4,7.2g/kg) of the present invention can significantly reduce the whole blood viscosity (p＜0.01) under the high, medium and low shear rates of acute blood stasis rats; Dose group can significantly reduce hematocrit (p<0.05).

Water load anesthetized rabbit ureter intubation diuretic test result shows, the present invention high, middle dose group (7.6,3.8g/kg) has obvious diuretic effect (p＜0.05, p＜0.01) to anesthetized rabbit, onset time ratio Positive drug hydrochlorothiazide and front row back to the Spring Festival Gala.

In summary, the present invention has analgesic, anti-inflammatory, immunity-enhancing, diuretic effects, and can improve the clinical indicators and histopathological changes caused by carrageenan-induced acute and chronic prostatitis in rats, and can also Reduce the whole blood viscosity of rats with acute blood stasis, and have the effect of promoting blood circulation and removing blood stasis.

The antibacterial test result in vitro of the present invention shows: the antibacterial test result to 221 clinical pathogenic bacteria in vitro shows that the present invention has certain antibacterial activity to test bacterial strain; Good; the change of the inoculum amount has a certain influence on the antibacterial activity of the present invention, and when the inoculum amount increases, the MIC also increases. Changes in the pH value of the medium have no significant impact on the antibacterial activity of the present invention.

Acute Toxicity Study:

With the maximum drug concentration, the maximum administration volume was 1.0ml/20g, 193g/kg ^-1 was given by intragastric administration or intraperitoneal injection once, and the mice were continuously observed for 14 days. As a result, none of the mice died. On the day of administration, the autonomous activities of individual animals decreased slightly, and no other obvious abnormalities were found; 1 day later, no obvious abnormalities were found in all animals; during the experiment, no abnormalities were found in the aspects of eating, breathing, heart rate, and hair color of the mice. Show that the maximum tolerated dose of the present invention by gavage or intraperitoneal injection of mice is 193g/kg ^-1 , which is 152 times of the clinical human dosage (the clinical human dosage is 76g crude drug/day/person for human dosage, based on 60kg/ people count).

Long-term Toxicity Studies:

High, medium and low dose groups (38.6g/kg, 19.3g/kg, 9.7g/kg) of the present invention are approximately equivalent to (30 times, 15 times, 7.5 times) the human dose, and the non-toxic dose is 19.3g .kg ^-1 is about 15 times the human dose (the human dose is 76g/day/person, calculated as 60kg/person). Intragastric administration, continuous administration for 13 weeks, the hematological indicators and blood biochemical indicators of the rats were measured during the 13 weeks of administration and the recovery period of 2 weeks after drug withdrawal, and the general performance of the rats was observed during the experiment, and the food intake was recorded. Consumption and body weight changes. At the end of three months of administration and two weeks of recovery period, 20 and 10 rats in each group were taken for systematic autopsy, the organ index was calculated, and the organs were detected by histopathology. The results show that the present invention has no significant changes to the activity status, body weight, food intake, ^etc. of the rats after intragastric administration for 13 weeks; content, hematocrit decreased, and the number of lymphocytes increased), individual blood biochemical indicators (increased blood urea nitrogen and uric acid) changed to a certain extent, and the above indicators could be recovered after 2 weeks of drug withdrawal; Compared with the control group, the testis weight of rats decreased by 3.6% and 8%, respectively. No obvious toxic reaction related to the drug effect was found in the animals of the middle and low dose groups. In histological examination, no pathological changes related to the medication of the present invention were found in each dosage group. Under the conditions of this test, the non-toxic dose of the present invention to rats by continuous intragastric administration for 13 weeks is 19.3 g.kg ^-1 , which is approximately equivalent to 15 times of the human dose (the human dose is 76 g/day/person, According to 60kg/person).

Detailed ways:

Embodiment 1 of the present invention: Weigh 30 g of Polygonum cephalum, 12 g of Rhizoma Chuanxiong, 12 g of Achyranthes fennel, 10 g of Angelica dahurica and 12 g of Achyranthes bidentata, add 10 times the amount of 60% ethanol, reflux extraction 3 times, each time for 1.5 hours, and combine 3 The second extract is filtered to obtain the filtrate, and the ethanol is recovered from the filtrate and concentrated to 60° C. to measure a thick paste with a relative density of 1.25-1.30. The thick paste is dried under reduced pressure and crushed into fine powder, and then 10 g of aspartame is added. Appropriate amount of lactose, 3g of magnesium stearate, mixed evenly, and dry pressed to make 1000g of granules to obtain granules. This product is taken after boiling water, 1 bag at a time, three times a day.

Example 2 of the present invention: Weigh 30 g of Polygonum cephalum, 12 g of Rhizoma Chuanxiong, 12 g of Rhizoma Fenugreek, 10 g of Angelica dahurica and 12 g of Achyranthes bidentata, add 8 times the amount of 60% ethanol, reflux extraction once for 1 hour, and combine the extracts, Filtrate to obtain the filtrate, recover the ethanol from the filtrate and concentrate it to 60°C to measure a thick paste with a relative density of 1.25, dry and pulverize into a fine powder, add appropriate amount of auxiliary materials, mix well, and granulate to make 1000g of granules to obtain the granule preparation .

Embodiment 3 of the present invention: Weigh 30g of Polygonum cephalum, 12g of Rhizoma Chuanxiong, 12g of Rhizoma chinensis, 10g of Angelica dahurica and 12g of Achyranthes bidentata, add 20 times the amount of 80% ethanol, reflux extraction 5 times, each time for 5 hours, and combine the extraction liquid, filtered to obtain the filtrate, the filtrate was recovered from ethanol and concentrated to 60 ° C to measure a thick paste with a relative density of 1.30, dried and crushed into fine powder, adding an appropriate amount of auxiliary materials, mixed evenly, and granulated to make 1000g of granules. Granular formulation.

Embodiment 4 of the present invention: Weigh 30 g of Polygonum cephalum, 12 g of Rhizoma Chuanxiong, 12 g of Rhizoma fennel, 10 g of Angelica dahurica and 12 g of Achyranthes bidentata, add 8 times the amount of 60% ethanol, reflux extraction 2 times, each time for 1 hour, and combine 2 The extract was filtered to obtain the filtrate, and the ethanol was recovered from the filtrate and concentrated to 60°C to measure a thick paste with a relative density of 1.25-1.30. The thick paste was dried under reduced pressure and crushed into fine powder, and an appropriate amount of polyethylene glycol 4000 was added. , after heating and mixing well, drop into another immiscible cooling liquid, simethicone, and drop into pills to obtain drop pills. The polyethylene glycol 4000 can be changed to polyoxyethylene (40) monostearate; the simethicone coolant can be changed to any one of liquid paraffin or vegetable oil.

Embodiment 5 of the present invention: Weigh 10 g of Polygonum cephalosporin, 5 g of Ligusticum chuanxiong, 5 g of Rhizoma fennel, 2 g of Angelica dahurica and 5 g of Achyranthes chinensis, add 8 times the amount of 60% ethanol, and reflux extraction twice, each time for 1 hour, Combine the two extracts, filter to obtain the filtrate, recover the ethanol from the filtrate and concentrate it to 60°C to measure the thick paste with a relative density of 1.25-1.30, dry the thick paste under reduced pressure and crush it into fine powder, directly put it into capsules or add Appropriate amount of 2% sodium carboxymethyl cellulose solution, moistened with water, granulated, mixed evenly, packed into capsules, and 1000 capsules were prepared to obtain the capsule preparation. The 2% sodium carboxymethylcellulose solution can be replaced with ethanol.

Embodiment 6 of the present invention: Weigh 50 g of Polygonum cephalosporin, 20 g of Rhizoma Chuanxiong, 25 g of Rhizoma Fenugreek, 15 g of Angelica dahurica and 25 g of Achyranthes bidentata, add 20 times the amount of 60% ethanol, and reflux extraction 4 times, each time for 4 hours, Combine 4 extracts, filter to obtain the filtrate, reclaim the ethanol from the filtrate and concentrate to a thick paste with a relative density of 1.25-1.30 (measured at 60°C); dry the thick paste under reduced pressure and pulverize it into a fine powder, add 2% carboxymethyl Sodium cellulose solution and water were used to moisten the granules, dried, and compressed into 1000 tablets to obtain tablet preparations.

Example 7 of the present invention: Weigh 30 g of Polygonum cephalosporin, 12 g of Rhizoma Chuanxiong, 12 g of Rhizoma Fenugreek and 10 g of Angelica dahurica, add 10 times the amount of 60% ethanol, reflux and extract 3 times, each time for 1.5 hours, and combine the extracts 3 times , filtered to obtain the filtrate; recover the filtrate to an appropriate amount of ethanol, refine, filter, add an appropriate amount of activated carbon to the filtrate, boil for 15 minutes, filter, add an appropriate amount of water for injection, stir well, adjust the pH value of the solution to 7.0-7.4, and use a microporous filter Membrane filtration until clarity, potting, and sterilization at 100°C for 30 minutes to obtain the injection.

Embodiment 8 of the present invention: Weigh 10 g of Polygonum cephalosporin, 5 g of Ligusticum chuanxiong, 5 g of Rhizoma chinensis and 2 g of Angelica dahurica, add 8 times the amount of 30% ethanol, reflux extraction for 1 time, 1 hour, and filter to obtain the filtrate; Recover ethanol and concentrate to a thick paste with a relative density of 1.25 (measured at 60°C); dry the thick paste under reduced pressure and pulverize it into a fine powder, add an appropriate amount of polyethylene glycol 4000, heat and mix well, and then drop another In the miscible cooling liquid simethicone, drop into pills to obtain drop pills. The polyethylene glycol 4000 can be replaced with polyoxyethylene (40) monostearate, and the simethicone coolant can be replaced with any one of liquid paraffin or vegetable oil.

Embodiment 9 of the present invention: Weigh 50 g of Polygonum cephalosporin, 20 g of Ligusticum chuanxiong, 25 g of Rhizoma chinensis and 15 g of Angelica dahurica, add 20 times the amount of 80% ethanol, reflux and extract 5 times, each time for 5 hours, and combine the extracts 5 times , filtered to obtain the filtrate; the filtrate was reclaimed ethanol and concentrated to an appropriate amount, added an appropriate amount of preservative and simple syrup, adjusted the total amount to 1000ml, stirred evenly, filtered, filled, 10ml per tube, sterilized, and the oral liquid was obtained. Wherein the corrective agent simple syrup can also be used instead as honey.

Example 10 of the present invention: Weigh 30 g of Polygonum cephalosporin and 12 g of Rhizoma Chuanxiong, add 10 times the amount of 60% ethanol, reflux and extract 3 times, each time for 1.5 hours, combine the extracts for 3 times, and filter; the filtrate is recovered Concentrate the ethanol to an appropriate amount, add an appropriate amount of preservatives and simple syrup to make the total amount to 1000ml, stir well, and filter to obtain a syrup preparation.

Example 11 of the present invention: Weigh 10 g of Polygonum cephalosporin and 5 g of Ligusticum chuanxiong, add 8 times the amount of 60% ethanol, reflux extraction once for 1 hour, and filter to obtain the filtrate; recover ethanol from the filtrate and concentrate to relative density It is a thick paste of 1.25 (measured at 60°C); the thick paste is dried under reduced pressure and crushed into a fine powder, and an appropriate amount of diluent composed of PEG400 and beeswax is added, grinded evenly, and set aside; another gelatin solution (100 parts of gelatin, 50 parts of glycerin) , 120 parts of water) for subsequent use; under the conditions of room temperature 23±2° C. and relative humidity 40%, the liquid medicine and gelatin are hydraulically made into pills to obtain soft capsule preparations. PEG400 can be replaced with vegetable oil (it can be one or a mixture of soybean oil, peanut oil, tea oil.)

Embodiment 12 of the present invention: Weigh 50 g of Polygonum cephalosporin and 20 g of Ligusticum chuanxiong, add 20 times the amount of 80% ethanol, reflux and extract 5 times, each time for 5 hours, combine the extracts 5 times, and filter to obtain the filtrate; The ethanol was recovered from the filtrate and concentrated to a thick paste with a relative density of 1.30 (measured at 60°C); the thick paste was dried under reduced pressure and pulverized into a fine powder, mixed evenly, and then 10 g of aspartame, appropriate amount of lactose, and 3 g of magnesium stearate were added. , mixed, granulated, and made into 1000g of granules to obtain granules. The flavoring agent aspartame can be replaced with sucrose, and lactose can be replaced with dextrin.

Claims (10)

1. A traditional Chinese medicine preparation for treating chronic prostatitis, characterized in that it is mainly prepared from 10-50 Polygonum cephalum and 5-20 Rhizoma Chuanxiong according to the weight components. 2. The traditional Chinese medicine preparation for treating chronic prostatitis according to claim 1, characterized in that it is prepared from 30 g of Polygonum cephalum and 12 g of Rhizoma Chuanxiong. 3. The preparation method of the traditional Chinese medicine preparation for treating chronic prostatitis as claimed in claim 1 or 2, characterized in that: taking the raw materials Polygonum cephalosporin and Rhizoma Chuanxiong, adding 8- 20 times the amount of 30-80% ethanol, reflux extraction 1-5 times, 1-5 hours each time, combine the extracts, filter to obtain the filtrate; recover the ethanol from the filtrate and concentrate it to a thick paste with a certain relative density; The paste is dried and crushed into fine powder to prepare the active component of the preparation; the obtained active component is prepared into the required preparation according to the conventional method. 4. The traditional Chinese medicine preparation for treating chronic prostatitis according to claim 1, characterized in that: calculated according to the weight components, there are also: 5-25 pieces of fennel and 2-15 pieces of Angelica dahurica. 5. The traditional Chinese medicine preparation for treating chronic prostatitis according to claim 4, characterized in that it is prepared from 30g of Polygonum cephalosporin, 12g of Rhizoma Chuanxiong, 12g of Rhizoma chinensis and 10g of Angelica dahurica. 6. The traditional Chinese medicine preparation for treating chronic prostatitis according to claim 4, characterized in that: calculated by weight components, there is also Achyranthes bidentata 5-25. 7. The traditional Chinese medicine preparation for treating chronic prostatitis according to claim 6, characterized in that it is prepared from 30g of Polygonum cephalosporin, 12g of Rhizoma Chuanxiong, 12g of Rhizoma chinensis, 10g of Angelica dahurica and 12g of Achyranthes bidentata. 8. The preparation method of the traditional Chinese medicine preparation for treating chronic prostatitis as claimed in claim 5, characterized in that: take the raw materials Polygonum cephalosporin, Rhizoma Chuanxiong, Rhizoma fennel and Angelica dahurica, and mix the Polygonum cephalosporin and Ligusticum chuanxiong in the weight ratio , Fenugreek and Angelica dahurica add 8-20 times the amount of 30-80% ethanol, reflux extraction 1-5 times, each time 1-5 hours, combine the extracts, filter to obtain the filtrate; the filtrate is reclaimed ethanol and concentrated to a certain A thick paste with a relative density; the active component of the preparation is prepared by drying the thick paste and pulverizing it into fine powder; the obtained active component is prepared into an oral preparation or an injection preparation according to a conventional method. 9. The preparation method of the traditional Chinese medicine preparation for treating chronic prostatitis as claimed in claim 7, characterized in that: weighing the raw materials Polygonum cephalosporin, Rhizoma Chuanxiong, Rhizome fennel, Angelica dahurica and Achyranthes chinensis, and weighing the head Add 8-20 times the amount of 30-80% ethanol to Polygonum chinensis, Rhizoma Chuanxiong, Rhizoma Fenugreek, Angelica dahurica and Achyranthes bidentata, reflux extraction 1-5 times, 1-5 hours each time, combine the extracts, and filter to obtain the filtrate; The filtrate recovers ethanol and concentrates to a thick paste with a certain relative density; the thick paste is dried and pulverized into fine powder to prepare the active component of this preparation; the obtained active component is prepared into granules, hard Capsule preparation, soft capsule preparation, tablet preparation, drop pill preparation, oral liquid or syrup preparation. 10. The preparation method of traditional Chinese medicine preparation for treating chronic prostatitis according to claim 9, characterized in that: weigh 30g of Polygonum cephalum, 12g of Rhizoma Chuanxiong, 12g of Rhizome fennel, 10g of Angelica dahurica and 12g of Achyranthes bidentata, and add 8-20 times Measure 30-80% ethanol, reflux and extract 1-5 times, each time for 1-5 hours, combine the extracts, filter to obtain the filtrate, recover the ethanol from the filtrate and concentrate it to a thick paste with a certain relative density, dry and grind it into Fine powder, add appropriate amount of auxiliary materials, mix well, granulate, and make 1000g of granules to obtain granules.