CN103768285A - Banana peel and shepherdspurse herb antihypertension tablet and preparation method thereof - Google Patents

Abstract

The invention relates to the field of medicinal preparations, and in particular relates to a banana peel and shepherdspurse herb antihypertension tablet. The tablet is characterized by being prepared from the following bulk drugs in parts by weight: 20-30 parts of banana peel, 15-25 parts of kudzuvine root, and 15-25 parts of shepherdspurse herb. The invention also provides a process for preparing the shepherdspurse herb antihypertension tablet. The process comprises the following steps: extracting the three bulk drugs with 80 percent ethanol to obtain a medicinal extract solution, and concentrating the extract solution to obtain extract with relative density of 1.20-1.25g/mL; directly spraying the concentrated extract into the drying chamber of a spray dryer, and drying to obtain hollow spherical particles with bulk density of 0.2-0.6g/cm<3>; adding proper auxiliary materials, preparing particles with required size by a dry-method granulation process, adding a lubricant, uniformly mixing, and tabletting.

Description

Chestnut Jiangya tablet and preparation method thereof

technical field

The present invention relates to the field of pharmaceutical preparations, in particular to a Chinese chestnut antihypertensive tablet, which is characterized in that it is prepared from 20-30 parts of banana peel, 15-25 parts of kudzu root, and 15-25 parts of shepherd's purse as raw materials. The invention also discloses The preparation method of this fragrant chestnut antihypertensive tablet is disclosed.

Background technique

Essential hypertension (essential hypertension, EH), also known as hypertension, is a clinical syndrome characterized by an increase in systemic arterial pressure. is the most common cardiovascular disease. It is not only a disease of hemodynamic abnormalities, but also a metabolic disease, which coexists with metabolic disorders such as fat and sugar, and more importantly, it is accompanied by adverse remodeling of target organs such as the heart, brain, and kidneys. It is regarded as an independent risk factor for cardiovascular events, and has become the most important risk factor for major human death diseases such as coronary heart disease and cerebrovascular disease.

A large number of experimental research results have preliminarily shown that Chinese medicine has better curative effect on symptoms and the effect of preventing or reversing target organ damage in the treatment of essential hypertension, which is beyond the reach of western medicine; it also has the advantages of low toxicity, safety and low cost , with better social and economic benefits. Essential hypertension is a common clinical cardiovascular disease, which belongs to the category of "dizziness", "headache" and "liver wind" in traditional Chinese medicine. Traditional Chinese medicine believes that the general pathogenesis of hypertension is: liver failure, stagnation of qi, hyperactivity of liver fire, and imbalance of liver and kidney yin and yang. Its pathological mechanism has both deficiencies and excesses: excess liver-qi stagnation begins, and then liver-qi stagnation turns into fire and liver-fire hyperactivity; Deficiency syndrome: liver stagnation transforms fire into yin and causes liver and kidney yin deficiency; or liver qi deficiency, wood does not produce fire, and the child is sick to the mother, resulting in heart qi and kidney qi deficiency, qi deficiency and blood fatigue, qi deficiency and water stagnation, long-term illness, heart and kidney yang deficiency.

Most scholars believe that the imbalance of liver and kidney yin and yang is the pathological basis, and hyperactivity of liver fire is an important pathogenesis of hypertension in the early stage. The treatment cannot be separated from the methods of purging the liver, calming the liver, nourishing the liver, and nourishing the kidney. Traditional Chinese medicine treatment of high blood pressure is mainly based on oral administration of traditional Chinese medicine, including decoctions, granules, capsules, pills, tablets, etc., which have been widely adopted. A large number of clinical data show that Chinese medicine has advantages in treating hypertension and its complications. It is mainly manifested in the following aspects: First, most of the traditional Chinese medicine antihypertensive drugs are compound preparations, which have many targets in the body, can regulate the body as a whole, and have a significant effect on improving clinical symptoms. Secondly, the six major classes of western antihypertensive drugs currently used all have side effects in varying degrees, and their scope of application is limited. Traditional Chinese medicine is a natural medicinal material, and its rational application has relatively small side effects on the body. Thirdly, the antihypertensive effect of traditional Chinese medicine is moderate, and once it takes effect, the effect lasts for a long time. Finally, in addition to internal medicine, Chinese medicine can also provide multi-faceted and multi-method treatment with external treatments such as acupuncture, qigong, massage, medicated pillow, acupoint sticking, and medicated foot bath. Therefore, it can be seen that Chinese medicine has broad prospects in the treatment of essential hypertension, and has great potential in the development of new antihypertensive Chinese medicines.

The invention prepares a shepherd's blood pressure reducing tablet, which is mainly composed of banana peel, kudzu root and shepherd's purse. Banana peel has the effects of clearing away heat, moistening the lungs, smoothing the intestines, and detoxifying. It is mainly used in the folks for the treatment of symptoms such as high blood pressure, hardening of the arteries, constipation, dysentery, and tonsillitis. "Modern Dictionary of Chinese Materia Medica" records that 30-60g of banana peel or fruit stalk, decocted and taken, can be used for the treatment of hypertension. Pueraria lobata can dilate coronary vessels and cerebrovascular, increase coronary flow and cerebral blood flow, Pueraria total brass can reduce myocardial oxygen consumption, increase oxygen supply, can directly dilate blood vessels, reduce peripheral resistance, and have obvious antihypertensive effect , can better relieve the "neck tightness" symptoms of hypertensive patients; puerarin can inhibit platelet aggregation, and the drug has a wide range of beta-receptor blocking effects. Shepherd's purse is sweet and mild in nature, cools blood and heats up blood, calms the liver and lowers blood pressure, and diuresis. It is used to treat hypertension and conjunctival congestion and astringent pain. The Chinese patent medicine Xiangqi Jiangya Granules has been clinically used for many years, and its antihypertensive effect is obvious. Preclinical studies have shown that Xiangqi Jiangya Granules can significantly lower blood pressure, dilate coronary vessels, reduce myocardial oxygen consumption, improve some hemodynamic indicators and improve heart function. Acute and chronic toxicology experiments found no obvious toxic side effects, and the drug was administered 296 times the clinically proposed dose, and no animal death occurred, showing good safety. However, granules are often hygroscopic, and attention should be paid to moisture-proof packaging. When the size or density of various granules varies greatly, segregation is easy to occur, resulting in inaccurate dosage. Therefore, we combine the two technologies of spray drying and dry granulation and tabletting, which can significantly reduce the amount of excipients used in the preparation, and further compress into tablets to obtain the Camelina antihypertensive tablets. The preparation has the following advantages: ① clear curative effect, has the function of clearing the liver and lowering blood pressure, calming the liver and calming the wind, and is suitable for the treatment of essential hypertension with hyperactivity of liver fire; ② accurate dosage and uniform content, with the number of tablets as the dosage unit; ③ Good chemical stability, because of its small size and compactness, it is less affected by external air, light, moisture and other factors, and can be protected by coating if necessary; ④It is more convenient to carry, transport, and take; ⑤Production mechanization, automation, and output Large and low cost. According to literature reports at home and abroad, there is no relevant patent application for Xianglin Jiangya Tablets at present.

Contents of the invention

The present invention relates to the field of pharmaceutical preparations, in particular to a Chinese chestnut antihypertensive tablet, which is prepared from the following raw materials in parts by weight:

Banana peel 20-30

Pueraria 15-25

Shepherd's purse 15-25

Chestnut buckwheat tablet of the present invention, the preferred weight ratio of each component is:

banana peel 25

Pueraria 20

Shepherd's purse 20

In the present invention, at first, the medicinal material extract is evaporated to dry solvent by spray drying method to obtain dry extract powder, comprising the following steps:

1) Take three kinds of raw medicinal materials according to the prescription, extract three times with 80% ethanol for 2 hours each time, and combine the extracts. The filtrate was concentrated to obtain a clear paste.

2) Spray the concentrated extract into a drying chamber of a spray dryer, and dry to obtain hollow spherical particles with a bulk density of 0.2-0.6 g/cm ³ . Spray drying is a method of spraying a drug solution or suspension in a drying chamber, and rapidly evaporating the solvent in the droplets under the action of hot air flow to directly obtain spherical dry fine particles. In recent years, the spray drying method has been widely used in the drying of traditional Chinese medicine extracts.

The present invention adopts the orthogonal design method to carry out the screening and optimization of the spray drying process, and selects four factors, which are respectively: A-relative density (g/mL) after concentration of the extract, B-material liquid temperature (° C.), C-intake air temperature (°C), D-exhaust air temperature (°C) take three levels for each factor (see Table 1), arrange the test with the orthogonal test design L9 (3 ⁴ ), and carry out spray drying. The results were scored comprehensively based on yield, moisture content and drying results, as shown in Table 2.

Table 1. Factor level table of spray drying process

Table 2. Results of Orthogonal Experimental Design of Spray Drying Process

Discussion: The experimental results show that the order of influence on spray drying is D>A>B>C, among which, D factor (exhaust air temperature) is the main influencing factor, followed by A factor (relative density of the concentrated extract), and again It is B factor (feed liquid temperature) and C factor (inlet air temperature).

Therefore, according to the results of orthogonal experiments, the optimal process is A ₃ B ₂ C ₃ D ₃ , the relative density of the concentrated extract is 1.20-1.25g/mL, the temperature of the feed liquid is 45°C, and the temperature of the air inlet is 250°C. The exhaust air temperature is 105°C. Under the control of the above process parameters, particles with good appearance, dryness, excellent solubility, dispersibility and fluidity can be obtained. Further validation experiments demonstrated the reproducibility of the process. The bulk density of the obtained particles was determined to be between 0.2 and 0.6 g/cm ³ . The determination formula of bulk density is as follows (formula 1):

ρ ₀ =m/V ₀ (Formula 1)

Among them, ρ ₀ - bulk density, kg/m ³ ; M - weight of material, kg; V ₀ - bulk volume of material, m ³ .

Bulk density refers to the weight per unit volume of powdery or granular materials in the piled state. Here, the weight of the material refers to the weight of the material naturally accumulated in a certain container; the accumulated volume refers to the volume of the container used. The bulk of the material contains both internal porosity and interstices between particles.

In the present invention, the dry extract powder and appropriate auxiliary materials are passed through an 80-mesh sieve for three times, mixed, and granules of required size are obtained through a dry granulation process.

The granules obtained after dry granulation were mixed with a lubricant, and then compressed using a rotary tablet press (Rimek Mini Press-IIS/F), with a tablet weight of 500 mg. Through adjustment, a sheet with qualified hardness can be obtained. When the rotation speed of the equipment is 30rpm, all indicators are qualified, and the test results are as follows in Table 3:

Table 3, the test results of various indicators of the tablet

The present invention prepares a shepherd's blood pressure reducing tablet, which is mainly composed of banana peel, kudzu root and shepherd's purse. The curative effect is clear, it has the functions of clearing the liver and lowering blood pressure, calming the liver and quenching the wind, and is suitable for the treatment of the syndrome of hyperactivity of liver fire in essential hypertension. The pharmacodynamic results are mainly evaluated by the spontaneously hypertensive rat (SHR) model.

Pharmacodynamics experiment of the present invention:

The results of the study on spontaneously hypertensive rats (SHR) showed that the 80% alcohol extract of Xiangqi Jiangya Tablets has a good antihypertensive effect on the spontaneously hypertensive rat (SHR) model: it has a good acute antihypertensive effect on this model It also has a good therapeutic antihypertensive effect, with large antihypertensive range and long antihypertensive time, and also has the characteristics of long-term effect. Compared with the antihypertensive effect of Xiangqi Jiangya Granules, the antihypertensive effect of Xiangqi Jiangya Tablets is similar; and compared with the use of banana peel alone, the curative effect of Xiangqi Jiangya Tablets is significantly improved. This shows that the combination of spray-drying and dry granulation to prepare Xiangqi Jiangya Tablets still has a similar therapeutic effect to granules, and the process reduces the amount of excipients, improves compliance, and is more stable in storage and transportation. more convenient. And the effect is better than using banana peel alone, which shows that the three raw materials have obvious synergistic effects on the antihypertensive effect of spontaneously hypertensive rats, which is in line with the traditional Chinese medicine treatment concept. The results are shown in Tables 4, 5, and 6. .

Table 4. Acute hypotensive effect on SHR animal model

Table 5. Therapeutic antihypertensive effect on SHR animal model

Table 6. Long-acting antihypertensive effect on SHR animal model

Detailed ways

Example 1

Recipe: 1000g banana peel, 800g kudzu root, 800g shepherd's purse.

Preparation process: crush banana peel into ^1cm3 coarse grains, kudzu root into ^2cm3 small pieces, shepherd's purse into 3cm long strips, extract three times with 80% ethanol for 2 hours each time, combine extracts, filter, and concentrate the filtrate to relative The density is 1.20g/mL, and the filtrate concentrate is sent to a spray drying drying chamber for spray drying. The spray drying conditions are that the temperature of the feed liquid is 45°C, the temperature of the inlet air is 250°C, and the temperature of the exhaust air is 105°C. Then pass the dry extract powder and appropriate auxiliary materials through an 80-mesh sieve for 3 times, mix, and obtain granules of required size through a dry granulation process. The granules obtained after dry granulation are mixed with magnesium stearate and then compressed using a rotary tablet machine with a rotating speed of 30 rpm. Finally, the fragrant chestnut antihypertensive tablet was prepared.

Example 2

Recipe: 1000g banana peel, 1000g kudzu root, 1000g shepherd's purse.

Preparation process: crush banana peel into ^1cm3 coarse grains, kudzu root into ^2cm3 small pieces, shepherd's purse into 3cm long strips, extract three times with 80% ethanol for 2 hours each time, combine extracts, filter, and concentrate the filtrate to relative The density is 1.25g/mL, and the concentrated filtrate is sent to a spray drying chamber for spray drying. The conditions for spray drying are that the temperature of the feed liquid is 40°C, the temperature of the inlet air is 150°C, and the temperature of the exhaust air is 85°C. Then pass the dry extract powder and appropriate auxiliary materials through an 80-mesh sieve for 3 times, mix, and obtain granules of required size through a dry granulation process. The granules obtained after dry granulation are mixed with micropowder silica gel and then pressed into tablets using a rotary tablet press with a rotational speed of 30 rpm. Finally, the fragrant chestnut antihypertensive tablet was prepared.

Example 3

Recipe: 1000g banana peel, 500g kudzu root, 500g shepherd's purse.

Preparation process: crush banana peel into ^1cm3 coarse grains, kudzu root into ^2cm3 small pieces, shepherd's purse into 3cm long strips, extract three times with 80% ethanol for 2 hours each time, combine extracts, filter, and concentrate the filtrate to relative The density is 1.23g/mL, and the filtrate concentrate is sent to a spray drying drying chamber for spray drying. The spray drying conditions are that the temperature of the feed liquid is 40°C, the temperature of the inlet air is 150°C, and the temperature of the exhaust air is 105°C. Then pass the dry extract powder and appropriate auxiliary materials through an 80-mesh sieve for 3 times, mix, and obtain granules of required size through a dry granulation process. The granules obtained after dry granulation are mixed with talcum powder and compressed into tablets using a rotary tablet machine with a rotational speed of 30 rpm. Finally, the fragrant chestnut antihypertensive tablet was prepared.

Example 4

Recipe: 1000g banana peel, 1250g kudzu root, 1250g shepherd's purse.

Preparation process: crush banana peel into ^1cm3 coarse grains, kudzu root into ^2cm3 small pieces, shepherd's purse into 3cm long strips, extract three times with 80% ethanol for 2 hours each time, combine extracts, filter, and concentrate the filtrate to relative The density is 1.25g/mL, and the concentrated filtrate is sent to a spray drying chamber for spray drying. The conditions for spray drying are that the temperature of the feed liquid is 40°C, the temperature of the inlet air is 150°C, and the temperature of the exhaust air is 85°C. Then pass the dry extract powder and appropriate auxiliary materials through an 80-mesh sieve for 3 times, mix, and obtain granules of required size through a dry granulation process. The granules obtained after dry granulation are mixed with micropowder silica gel and then pressed into tablets using a rotary tablet press with a rotational speed of 30 rpm. Finally, the fragrant chestnut antihypertensive tablet was prepared.

Claims (6)

1. the preparation method of fragrant shepherd's purse hypertension pill, be crude drug and add suitable adjuvant to be prepared from by 20-30 part Pericarpium Musae, 15-25 part Radix Puerariae, 15-25 part Herba Capsellae, it is characterized in that described method is made up of the following step: measure three kinds of raw medicinal materials by prescription, 80% ethanol extraction three times, each 2 hours, merge extractive liquid,, extracting solution concentrated the relative density clear paste that is 1.20～1.25g/mL.Spray in the hothouse of spray dryer extracting concentrated solution, after being dried, obtain bulk density at 0.2～0.6g/cm ³hollow spheres particle, add suitable adjuvant, cross 80 mesh sieve 3 times, mix, obtain the granule of required size by dry granulation technique, add lubricant, mix, tabletting and get final product.

2. the preparation method of fragrant shepherd's purse hypertension pill according to claim 1, is characterized in that it is to be prepared from by the raw medicinal material of following weight portion: 25 parts of Pericarpium Musae, 20 parts of Radix Puerariaes, 20 parts, Herba Capsellae.

3. the preparation method of fragrant shepherd's purse hypertension pill according to claim 1, it is characterized in that described drying process with atomizing condition is that the relative density of extracting solution after concentrated is 1.20～1.25g/mL, feed temperature is 45 ℃, and inlet temperature is 250 ℃, and temperature of outgoing air is 105 ℃.

4. the preparation method of fragrant shepherd's purse hypertension pill according to claim 1, is characterized in that described adjuvant is one or more in the pharmaceutical grade adjuvants such as methylcellulose, hydroxypropyl methylcellulose, microcrystalline Cellulose, pregelatinized Starch, lactose, mannitol and derivant thereof.

5. the preparation method of fragrant shepherd's purse hypertension pill according to claim 1, is characterized in that described lubricant is one or more in the pharmaceutical grade adjuvants such as stearic acid, magnesium stearate, calcium stearate, micropowder silica gel, Pulvis Talci and derivant thereof.

6. the heparin modified Evacet preparation of claim 5, wherein freeze drying protectant is selected from one or more in sucrose, lactose, glucose, mannitol.