CN1698669A - Banxia Xiexin Decoction preparation and its preparation method and application - Google Patents

Abstract

The invention discloses a preparation of pinellia decoction for purging stomach fire, its preparing method and application, wherein the preparation comprises using compound pinellia decoction as raw medicinal materials, extracting effective substances with water or ethanol, preparing powdered extract through spray drying or decompression drying, charging medicinal auxiliary materials and preparing granule through dry method palletizing or wet method palletizing, finally filling into capsule or carrying pelleting to form the tablet. The preparation has good curative effect for superficial gastritis especially gastritis caused by Helicobacter pylori, and gastric ulcer, the invention also has the advantages of easy administration and small amount of dosage.

Description

Banxia Xiexin Decoction preparation and its preparation method and application

technical field

The invention relates to a Chinese medicine compound Banxia Xiexin Decoction preparation and a preparation method thereof, in particular to capsules and tablets which take the Chinese medicine compound Banxia Xiexin Decoction as an active ingredient.

Background technique

Superficial gastritis is a common and frequently-occurring disease with a long course and easy recurrence. Western medicine generally adopts triple or quadruple therapy, which has high treatment costs and large side effects. Banxia Xiexin Decoction is a classic prescription in "Treatise on Febrile Diseases" written by Zhang Zhongjing. It is a common prescription for modern Chinese medicine clinical treatment of chronic gastritis and gastric ulcer. It has good curative effect, low recurrence rate and few side effects, but there is no such prescription The preparation is on the market, and it is taken in decoction in clinical application. The dosage is large, and the medicine is also greatly affected by gastric emptying, which brings inconvenience to the treatment and use of patients.

Contents of the invention

The technical problem to be solved in the present invention is to disclose a preparation of Banxia Xiexin Decoction and its preparation method and application, so as to overcome the problems in the prior art that the dosage is large, the medicine is also greatly affected by gastric emptying, and it is used for the treatment of patients. Inconvenient defect.

The Banxia Xiexin Decoction preparation of the present invention comprises a therapeutically effective dose of Banxia Xiexin Decoction extract and a pharmaceutically acceptable carrier;

Said Banxia Xiexin Decoction extract is extracted by adopting the raw material medicine of the following proportioning by weight:

Medicinal Pinellia 18-24, Scutellaria baicalensis 13-19, Codonopsis or Ginseng 13-19, Dried Ginger 13-19,

Jujube 13-19, Zhi Licorice 7-13, Coptidis 2-8.

The added amount of said carrier is 30%-80% of the weight of the extract preparation of Banxia Xiexin Decoction;

The carrier includes one or more of fillers, disintegrants, lubricants or wetting agents;

The filler is selected from one of starch, pregelatinized starch, microcrystalline cellulose, sodium carboxymethylcellulose or polyvinylpyrrolidone;

The disintegrating agent is selected from sodium carboxymethyl starch, sodium carboxymethylcellulose or their mixtures, the lubricant is selected from magnesium stearate or talcum powder, and the wetting agent is selected from water, ethanol solution or polyvinylpyrrolidone in ethanol solution A sort of.

The above-mentioned Banxia Xiexin Decoction preparation includes tablets and capsules.

The preparation method of above-mentioned Banxia Xiexin Decoction preparation comprises the steps:

The above raw materials are reflux extracted with 15 to 25 times the amount of water or 15 to 22 times the amount of 50% to 80% ethanol solution. The extraction time is 1 to 2 hours. After 2 hours, the extracts were combined, filtered, the filtrate was concentrated to a relative density of 1.05-1.15 at 60° C., and spray-dried or dried under reduced pressure to obtain extract powder.

The air inlet temperature during spray drying is 120-160°C; the vacuum degree of decompression drying is -0.06--0.1MPa.

The extract powder is sieved, adding fillers, disintegrants and wetting agents to wet granules by methods known in the art, or adding fillers and disintegrants to dry granules by methods known in the art to obtain the granules of the present invention. Banxia Xiexin Decoction preparation;

Fill the obtained preparation in capsules to obtain Banxia Xiexin Decoction capsules;

Or further add a lubricant to the Banxia Xiexin Decoction preparation, compress into tablets by a method known in the art, and coat with a film to obtain Banxia Xiexin Decoction tablets.

The Banxia Xiexin Decoction preparation of the present invention, including capsules and tablets, can be used to treat diseases such as chronic gastritis and gastric ulcer. The disease decides.

The invention replaces the traditional dosage form with a modern dosage form that is convenient to take. The characteristics of the invention are that the ratio of raw materials is reasonable, the active ingredients are refined and the dosage is reduced, and the prepared capsules and tablets disintegrate quickly, so that the medicine can be excreted by the stomach. The effect of air is small, and the therapeutic effect can be fully exerted at the treatment site.

The Banxia Xiexin tablet or capsule prepared by the method has high content of active ingredients, has good curative effect on superficial gastritis, especially gastritis and gastric ulcer caused by Helicobacter pylori, is convenient to take, and has a small dosage.

Detailed ways

Example 1

Weigh 2kg of medicinal materials according to the prescription of Banxia Xiexin Decoction, of which:

Medicinal Pinellia 0.46kg, Scutellaria baicalensis 0.33kg, Ginseng 0.33kg, Dried Ginger 0.32,

Jujube 0.32kg, Zhigancao 0.19kg, Coptis 0.05kg

Use 36kg of 70% ethanol solution, heat and reflux in a water bath to extract twice, add 20kg for the first time, extract for 2h, add 16kg for the second time, extract for 1h; filter, and the relative density of the filtrate when concentrated to 25°C is 1.1, spray-dried to obtain Extract powder. The extract powder was sieved, added 148g of microcrystalline cellulose, 26g of polyvinylpyrrolidone and 26g of sodium carboxymethylcellulose, granulated by dry pressing, and filled with capsules to make Banxia Xiexin Capsules.

Example 2

Weigh 2kg of medicinal materials according to the prescription of Banxia Xiexin Decoction, of which:

Medicinal Pinellia 0.40, Scutellaria baicalensis 0.31, Codonopsis 0.32, dried ginger 0.32,

Jujube 0.31, Zhigancao 0.21, Coptis 0.13.

Use 44kg of 60% ethanol solution, heat and reflux in a water bath to extract twice, add 24kg for the first time, extract for 2h, add 20kg for the second time, extract for 1h; filter, the relative density of the filtrate when concentrated to 25°C is 1.1, and spray dry to obtain Extract powder. The extract powder was sieved, added 148g of microcrystalline cellulose, 26g of polyvinylpyrrolidone and 26g of sodium carboxymethylcellulose, granulated by dry pressing, and filled with capsules to make Banxia Xiexin Capsules.

Example 3

Adopt the method of Example 2, and granulate by dry pressing method known in the art, add magnesium stearate 4g tabletting after granulation, make Pinellia Xiexin Tablet, acrylic resin adopts known method film-coating for tablet Clothes.

Example 4

According to the same method as in Example 1, the drying method was changed to drying under reduced pressure, and the dried product was pulverized to obtain extract powder.

Example 4

According to the same method as in Example 2, change "70% ethanol solution, extract twice under reflux in a water bath" to "decoct in water twice".

Example 5

Pharmacodynamic study of Banxia Xiexin Decoction tablets and capsules on Helicobacter pylori-infected gastritis model

1. Experimental materials

Drugs and reagents Banxia Xiexin Decoction tablets and capsules (self-made), Livzon Dele (produced by Zhuhai Livzon Pharmaceutical Factory), urokinase, oxidase, catalase (purchased from Sigerma), 0.9% chlorine Sodium chloride injection, 5% Na ₂ HCO ₃ solution, PBS solution (prepared by yourself).

Animals Wister rats, 4 months old, weighing 112-158 g, were provided by the Animal Center of our hospital.

2. Method

2.1 Preparation of drug samples for testing According to the dosage in Table 1, use 0.9% sodium chloride injection to prepare a suitable concentration for testing.

2.2 Preparation of Helicobacter pylori (HP) infection model

2.2.1 HP strain culture Take the gastric mucosal tissue forceps of patients with chronic active gastritis examined in the gastroscope room, inoculate it on Campylobacter jejuni selective medium, place it in a micro-aerobic environment, and culture it at 37°C for 72 hours, check the colonies, Gram Negative bacillus stained with urokinase, oxidase, and catalase were positive. After confirming that it was HP bacteria, it was subcultured as the test strain.

2.2.2 Infection method 176 Wister rats, half male and half male, were randomly divided into 12 groups (two groups consisted of 8 rats, and one group was a blank group without HP infection), 16 rats in each group, and raised in separate cages. After fasting for 12 hours, use 5% Na ₂ HCO ₃ solution 2ml/ig for ig, give mixed Hp strains (10 ¹² cfu/L bacterial solution) 2ml/ig for 15min, and eat after 30min. 1 infection per week, 4 times in total.

2.3 Anti-Hp infection gastritis test

2.3.1 Experimental grouping and administration method One week after the last Hp infection, the administration was divided into the following groups: low-dose sample group (one group for No. 1, No. 2, No. 3, and No. 4), high-dose sample group (No. , No. 2, No. 3, and No. 4 each group), NS control group, positive drug (Livzon Dele) control group, ig administration once a day, and the course of treatment was 10 days. The dosage is shown in Table 1. After the administration, the above 10 groups were randomly divided into 2 groups, 8 animals in each group, and the animals were sacrificed acutely on the day after the end of treatment and 1 month after the end of treatment, and the stomach was taken out by aseptic operation, cut open along the greater curvature of the stomach, and PBS The contents of the stomach were washed away with liquid, and 5 pieces of tissue were taken from relatively fixed parts of the pyloric end for direct smear, urease test, and Hp culture, and the rest were fixed in 10% formaldehyde solution prepared by PBS solution for pathological examination. Pathological examination method: The gastric tissue sections were stained with HE, and the pathological changes of the gastric mucosa of each tested animal were observed with a microscope.

2.3.2 Judgment of results The three tests of Hp: no Hp detected by smear microscopy, negative urease test reaction, and no HP found in Hp culture were negative conversion, and the negative conversion rate of each group was calculated based on the number of negative animals. The negative conversion rate was the HP clearance rate, and the HP negative conversion rate was the eradication rate one month after the end of treatment.

3. Results

3.1 Preparation of HP-infected gastritis model A group of HP-infected groups were randomly selected, and gastric mucosal tissues were taken for smear microscopy and urokinase test. HP could be detected in 8 rats in the infection group, and gastric mucosal tissues of 8 rats in the blank control group Neither HP was detected.

3.2 Anti-HP effect of tested samples

3.2.1 The clearance rate and eradication rate of HP Each test group and the positive control drug group have a certain clearance rate and eradication rate of HP, Banxia Xiexin Decoction tablet and capsule high dose group and the positive control drug group The effect is better, and the difference is very significant compared with the control group (P<0.01). Other groups also have certain anti-HP effects, and the difference is significant compared with the control group (P<0.05). Among them, the high-dose group of Banxia Xiexin Decoction tablets and capsules had the same effect as the positive control group, and there was no significant difference between them (P>0.05). The results are shown in Table 1.

                                                                                                       

Groups Dosage on HP clearance rate on HP eradication rate

          (mg/kg)    N  Clearance rate (%) Negative number of HP eradication rate (%)

Normal saline control group 20ml/kg 8 1 12.5 0 0

Banxia Xiexin Decoction Tablet Low Dose 150 8 3 37.5 1 12.5

Quantity group

Banxia Xiexin Decoction Tablet High Dosage 200 8 6 75.0 5 62.5

Quantity group

Banxia Xiexin Decoction Capsules Low 100 8 5 62.5 4 50.0

Dose group

Banxia Xiexin Decoction Capsule High 200 8 7 87.5 6 75.0

Dose group

Livzon Dele Group 40 8 7 87.5 6 75.0

3.2.2 Pathological changes Normal saline control group: destruction of gastric mucosal glands, interstitial edema with inflammatory cell infiltration. Banxia Xiexin Decoction Tablet Low-dose Group: Focal inflammatory cell response in gastric mucosa. In the high-dose group of Banxia Xiexin Decoction tablets and the low-dose group of Banxia Xiexin Decoction capsules: gastric mucosal glands were normal, with a small amount of inflammatory cells in the superficial layer. High-dose Banxia Xiexin Tang capsule high-dose group and Livzon Dele group: the gastric glands were normal and no inflammatory cells were seen.

4. Summary

The research results showed that both Banxia Xiexin Decoction tablets and capsules had good anti-HP effects, and the high-dose Banxia Xiexin Decoction capsule group had the best effect, which was equivalent to the anti-HP effect of the positive control drug.

Claims (10)

1. A Banxia Xiexin Decoction preparation, characterized in that it comprises a therapeutically effective dose of Banxia Xiexin Decoction extract and a pharmaceutically acceptable carrier, said Banxia Xiexin Decoction extract adopts the following weight Extraction of raw materials with ratio of parts: Medicinal Pinellia 18-24, Scutellaria baicalensis 13-19, Codonopsis or ginseng 13-19, dried ginger 13-19, Jujube 13-19, Zhi Licorice 7-13, Coptidis 2-8. 2. The Banxia Xiexin Decoction preparation according to claim 1, characterized in that the added amount of said carrier is 30%-80% of the weight of the Banxia Xiexin Decoction preparation. 3. The Banxia Xiexin Decoction preparation according to claim 1, wherein said carrier includes one or more of fillers, disintegrants, lubricants or wetting agents. 4. The Banxia Xiexin Decoction tablet according to claim 1, wherein the filler is selected from one of starch, pregelatinized starch, microcrystalline cellulose, sodium carboxymethylcellulose or polyvinylpyrrolidone. The disintegrating agent is selected from sodium carboxymethyl starch, sodium carboxymethylcellulose or their mixtures, the lubricant is selected from magnesium stearate or talcum powder, and the wetting agent is selected from water, ethanol solution or ethanol solution of polyvinylpyrrolidone One of. 5. The Banxia Xiexin Decoction preparation according to any one of claims 1 to 4, characterized in that it comprises tablets and capsules. 6. The preparation method of Banxia Xiexin Decoction according to any one of claims 1 to 4, characterized in that it comprises the following steps: The raw material medicine is reflux extracted with water or ethanol solution, the extraction time is 1-2 hours, filtered, the relative density of the filtrate is 1.05-1.15 when the filtrate is concentrated to 60 DEG C, spray-dried or dried under reduced pressure to obtain the extract powder. 7. The preparation method of Banxia Xiexin Decoction preparation according to claim 6, characterized in that, the raw material drug is mixed with 15 to 25 times the amount of water or 15 to 22 times the amount of 50% to 80% of the The ethanol solution was refluxed for extraction. 8. The preparation method of the Banxia Xiexin Decoction preparation according to claim 6, characterized in that 2 to 3 times of reflux extraction are performed, each time for 1 to 2 hours. 9. An extract of Banxia Xiexin Decoction, which is characterized in that it is extracted by using the raw material medicine in the following proportions by weight: Medicinal Pinellia 18-24, Scutellaria baicalensis 13-19, Codonopsis or ginseng 13-19, dried ginger 13-19, Jujube 13-19, Zhi Licorice 7-13, Coptidis 2-8. 10. The application of the Banxia Xiexin Decoction extract according to claim 9 in the preparation of medicines for the treatment of chronic gastritis and Helicobacter pylori-associated gastric ulcer.