CN106139078A

CN106139078A - Antidiarrheal pharmaceutical composition antidiarrheal medicament and preparation method thereof

Info

Publication number: CN106139078A
Application number: CN201610601853.XA
Authority: CN
Inventors: 陈林; 邹节明; 李春
Original assignee: SANJIN GROUP HUNAN SANJIN PHARMACEUTICAL CO Ltd
Current assignee: SANJIN GROUP HUNAN SANJIN PHARMACEUTICAL CO Ltd
Priority date: 2016-07-27
Filing date: 2016-07-27
Publication date: 2016-11-23

Abstract

The invention provides a kind of antidiarrheal pharmaceutical composition, described pharmaceutical composition is mainly made up of following components by weight: Herba Plantaginis 20 30 parts, Semen Raphani 5 10 parts, fevervine 25 35 parts, 23 parts of catechu, Pericarpium Citri Reticulatae 10 20 parts, Elephantopus scaber L. 25 35 parts, Rhizoma Zingiberis 5 15 parts, Radix Scutellariae 15 25 parts, the Rhizoma Atractylodis Macrocephalae 10 20 parts, Radix Puerariae 5 15 parts, Flos Ilicis Asprellae 5 15 parts, Rhizoma Corydalis 15 25 parts.Present invention also offers antidiarrheal preparation, including described pharmaceutical composition and medical auxiliary materials.Present invention also offers the preparation method of described pharmaceutical composition, described method specifically, decocting extract described compositions, precipitate with ethanol after concentration, after carry out second time concentrate out cream, to obtain final product.

Description

Antidiarrheal pharmaceutical composition antidiarrheal pharmaceutical agent and preparation method thereof

Technical Field

The invention relates to the field of pharmacy, and particularly relates to an antidiarrheal pharmaceutical composition, an antidiarrheal medicine and a preparation method thereof.

Background

Diarrhea is a common symptom, commonly called as diarrhea, and means that the frequency of defecation obviously exceeds the frequency of ordinary daily habit, the stool quality is thin, the water content is increased, the daily defecation amount exceeds 200g, or the diarrhea contains undigested food or bloody pus and mucus. Diarrhea is often accompanied by symptoms such as a sense of urgency, anal discomfort, incontinence, etc.

Diarrhea is classified into acute and chronic types. Acute diarrhea is acute, and the course of disease is within 2-3 weeks. Chronic diarrhea refers to recurrent diarrhea with a course of more than two months or in a period of 2-4 weeks in the intermittent period. Acute diarrhea may be caused by the following reasons

(1) People with bacterial infection may have enteritis or bacillary dysentery after eating food or drinking beverage contaminated by bacteria such as escherichia coli, salmonella, shigella, etc., and have symptoms of abdominal pain, diarrhea, vomiting, tenesmus, fever, etc. in different degrees.

(2) Viral infection in humans is susceptible to viral diarrhea following food or other viral infections, such as: after infection with rotavirus, norwalk virus, coxsackie virus, ercha and other viruses, symptoms such as abdominal pain, diarrhea, nausea, vomiting, fever, general malaise and the like appear.

(3) Food poisoning is an acute toxic disease caused by eating food contaminated with bacteria and toxins thereof, or eating uncooked lentils, and the like. Deteriorated food and polluted water are main infection sources, and unclean hands, tableware and flies with bacteria are main transmission ways. The patient may have acute gastrointestinal symptoms such as vomiting, diarrhea, abdominal pain, fever, etc.

(4) Uncooked and cold food is favored and often drunk with ice beer, which can result in gastrointestinal dysfunction, accelerated intestinal motility and diarrhea.

(5) Food retention dyspepsia, irregular diet, excessive eating, and indigestible food, or food retention in stomach due to stomach hypomotility, and symptoms such as abdominal distention, diarrhea, nausea, emesis, acid regurgitation, heartburn, and belch (hiccup).

(6) People like staying in an air-conditioned room or sleeping with an air conditioner when catching a cold in summer, and the abdomen is easy to catch a cold, so that the intestinal peristalsis is accelerated to cause diarrhea.

Chronic diarrhea may be caused by the following causes:

(1) intestinal infectious diseases (chronic amebic dysentery); ② chronic bacterial diseases; ③ tuberculosis of intestine; pear-shaped flagellosis and schistosomiasis; intestinal candidiasis.

(2) Non-infectious inflammation of the intestinal tract (inflammatory bowel disease) (crohn's disease and ulcerative colitis); ② radiation enteritis; ③ ischemic colitis; diverticulitis; uremic enteritis.

(3) Tumors, namely colorectal cancer; ② colon adenomatosis (polyps); ③ small intestinal malignant lymphoma; amine precursor takes up decarboxylated cytoma, gastrinoma, carcinoid, intestinal vasoactive intestinal peptide tumor, etc.

(4) Primary malabsorption of small intestine; ② secondary malabsorption of small intestine.

In the prior art, a lot of medicines are used for treating diarrhea, and most medicines cannot treat all kinds of diarrhea firstly, and secondly, the medicines have the defect that the medicines are not suitable for being absorbed by human bodies so that the medicine effect cannot be fully exerted. In addition, according to the theory of traditional Chinese medicine, all the heat-clearing and detoxifying drugs can cause diarrhea caused by the impaired function of the spleen and the stomach, so that the diarrhea caused by damp-heat is difficult to treat, and therefore a composition capable of clearing heat and detoxifying and simultaneously playing a role in treating the diarrhea is needed, so that the diarrhea caused by damp-heat can be well treated.

In view of the above, the present invention is particularly proposed.

Disclosure of Invention

The first purpose of the invention is to provide a composite forward osmosis membrane which can effectively improve water flux, achieve high salt rejection rate and has an antibacterial effect.

The second purpose of the invention is to provide a preparation method of the composite forward osmosis membrane, the method is simple to operate, and the selected parameters are particularly suitable for preparing the composite forward osmosis membrane provided by the invention.

In order to achieve the above purpose of the present invention, the following technical solutions are adopted:

one aspect of the invention relates to an antidiarrheal pharmaceutical composition, which is mainly prepared from the following components in parts by weight: 20-30 parts of plantain herb, 5-10 parts of radish seed, 25-35 parts of paederia scandens, 2-3 parts of catechu, 10-20 parts of dried orange peel, 25-35 parts of elephantopus scaber, 5-15 parts of dried ginger, 15-25 parts of radix scutellariae, 10-20 parts of bighead atractylodes rhizome, 5-15 parts of kudzu root, 5-15 parts of roughhaired holly root and 15-25 parts of corydalis tuber.

Preferably, the pharmaceutical composition is mainly prepared from the following components in parts by weight: 24-26 parts of plantain herb, 7-8 parts of radish seed, 28-32 parts of paederia scandens, 2-3 parts of catechu, 14-16 parts of dried orange peel, 28-32 parts of elephantopus scaber, 8-12 parts of dried ginger, 18-22 parts of radix scutellariae, 14-16 parts of bighead atractylodes rhizome, 8-12 parts of kudzu root, 8-12 parts of roughhaired holly root and 18-22 parts of corydalis tuber.

The pharmaceutical composition takes plantain herb, radish seed and Chinese fevervine herb as monarch drugs, catechu, dried orange peel and elephantopus scaber as ministerial drugs, dried ginger, radix scutellariae, bighead atractylodes rhizome and kudzuvine root as adjuvant drugs, and roughhaired holly root and corydalis tuber as conductant drugs. The components are compatible with each other. Wherein,

gan Jiang is pungent, warm in nature and good in flavor, and helps the herbs reach all parts of the body. The dried ginger is used as the component of the adjuvant, so that the problem that the pharmaceutical composition is not easy to absorb can be effectively solved.

Corydalis tuber is warm in nature, pungent and bitter in taste, enters heart, spleen, liver and lung, is a wonderful product for promoting blood circulation to remove blood stasis and promoting qi circulation to relieve pain, and can improve the solubility of active ingredients of other medicines, thereby enhancing the curative effect.

The scutellaria has the efficacies of clearing heat and drying dampness, purging fire and removing toxicity, stopping bleeding, preventing miscarriage and the like, and in addition, the scutellaria has the antibacterial effect and also has better effect on bacterial diarrhea in the prescription

Kudzuvine root, sweet in nature, pungent and cool. Has the functions of expelling pathogenic factors from muscles, allaying fever, promoting eruption, promoting the production of body fluid to quench thirst, invigorating yang and stopping diarrhea. It is commonly indicated for exterior syndrome with fever, stiffness and pain of neck and back, measles without adequate eruption, thirst due to fever, diabetes due to yin deficiency, dysentery due to heat-purging and diarrhea due to spleen deficiency.

Another aspect of the invention relates to an antidiarrheal pharmaceutical preparation, which comprises the pharmaceutical composition and pharmaceutical excipients.

Preferably, the antidiarrheal pharmaceutical formulation is a tablet, an extract, or a granule, preferably, the antidiarrheal is a tablet.

The antidiarrheal medicine can be prepared into various dosage forms, preferably tablets, by adding various pharmaceutical excipients according to different administration requirements.

The preparation method of the antidiarrheal pharmaceutical composition in another aspect of the invention specifically comprises the steps of decocting the composition with water, concentrating, precipitating with ethanol, and concentrating for the second time to obtain an ointment.

Preferably, the water-decocting is carried out twice, the first time of water-decocting is 50-70 minutes, and the second time of water-decocting is 40-50 minutes.

Preferably, the weight of the water added in each time of decoction is 5-7 times of the weight of the medicinal materials.

Preferably, the water decocted extractive solution is concentrated at 65-75 deg.C under vacuum and reduced pressure until the relative density of the medicinal liquid is 1.15-1.25.

Preferably, ethanol with the volume 1-2 times of the liquid medicine is added during the alcohol precipitation.

Preferably, the liquid medicine is sealed and kept still for 20-28 hours before the second concentration, and the second concentration is carried out at 65-65 ℃ under reduced pressure until the relative density of the liquid medicine is 1.15-1.20. Compared with the prior art, the invention has the beneficial effects that:

(1) the antidiarrheal pharmaceutical composition can treat various kinds of diarrhea caused by various reasons, has wide treatment range and good curative effect, and is particularly suitable for treating the diarrhea caused by damp-heat;

(2) the antidiarrheal pharmaceutical composition of the invention has the effects of clearing away heat and toxic materials;

(3) the antidiarrheal medicinal composition is easier to be absorbed by human body, thereby more fully exerting the drug effect;

(4) the preparation method of the invention has the advantages of delicate process, specific parameters and good reproducibility, is particularly suitable for preparing the pharmaceutical composition of the invention, and is convenient for further preparing the pharmaceutical composition into various dosage forms which are convenient to take.

Detailed Description

Embodiments of the present invention will be described in detail below with reference to examples, but it will be understood by those skilled in the art that the following examples are only illustrative of the present invention and should not be construed as limiting the scope of the present invention. The examples, in which specific conditions are not specified, were conducted under conventional conditions or conditions recommended by the manufacturer. The reagents or instruments used are not indicated by the manufacturer, and are all conventional products available commercially.

Example 1

Preparing the following Chinese herbal medicines

20kg of plantain herb, 10kg of radish seed, 25kg of paederia scandens, 2kg of catechu, 10kg of dried orange peel, 25kg of elephantopus scaber, 5kg of dried ginger, 15kg of radix scutellariae, 10kg of bighead atractylodes rhizome, 5kg of kudzu root, 5kg of roughhaired holly root and 15kg of corydalis tuber.

Parching Atractylodis rhizoma and Raphani semen, and decocting in water. The water amount is 5 times of the total weight of the medicinal materials during decoction for 60 minutes, and then the decocted liquid medicine is filtered and collected, and is decompressed and concentrated at 65 ℃ until the relative density of the liquid medicine is 1.15.

Then adding ethanol with the volume equal to that of the liquid medicine, and carrying out alcohol precipitation.

Sealing and standing the medicinal liquid for 20 hr, concentrating at 60 deg.C under reduced pressure until the relative density of the medicinal liquid is 1.15. Obtaining the extract.

Example 2

Preparing the following Chinese herbal medicines

30kg of plantain herb, 5kg of radish seed, 35kg of paederia scandens, 3kg of catechu, 20kg of dried orange peel, 35kg of elephantopus scaber, 15kg of dried ginger, 25kg of radix scutellariae, 20kg of bighead atractylodes rhizome, 15kg of kudzu root, 15kg of roughhaired holly root and 25kg of corydalis tuber.

Parching Atractylodis rhizoma and Raphani semen, and decocting in water. Decocting twice, wherein the water amount is 5 times of the total weight of the medicinal materials in the first decocting, filtering after 50 minutes, collecting filtrate, the water amount is 5 times of the total weight of the medicinal materials in the second decocting, filtering after 40 minutes, collecting filtrate, combining the liquid medicines decocted in the two times, concentrating under reduced pressure at 65 ℃, and concentrating until the relative density of the liquid medicine is 1.25.

Then adding ethanol with the volume 1.5 times of the liquid medicine for alcohol precipitation.

Sealing and standing the medicinal liquid for 28 hr, concentrating at 65 deg.C under reduced pressure until the relative density of the medicinal liquid is 1.20. Obtaining the extract.

Example 3

Preparing the following Chinese herbal medicines

24kg of plantain herb, 7kg of radish seed, 32kg of paederia scandens, 3kg of catechu, 16kg of dried orange peel, 32kg of elephantopus scaber, 12kg of dried ginger, 18kg of radix scutellariae, 14kg of bighead atractylodes rhizome, 12kg of kudzu root, 8kg of roughhaired holly root and 22kg of corydalis tuber.

Parching Atractylodis rhizoma and Raphani semen, and decocting in water. Decocting twice, wherein the water amount is 6 times of the total weight of the medicinal materials in the first decocting, filtering after 70 minutes, collecting filtrate, the water amount is 5 times of the total weight of the medicinal materials in the second decocting, filtering after 50 minutes, collecting filtrate, combining the liquid medicines decocted in the two times, concentrating under reduced pressure at 75 ℃, and concentrating until the relative density of the liquid medicine is 1.20.

Then adding ethanol with the volume 2 times of the liquid medicine for alcohol precipitation.

Sealing and standing the medicinal liquid for 24 hr, concentrating at 60 deg.C under reduced pressure until the relative density of the medicinal liquid is 1.20. Obtaining the extract.

Example 4

Preparing the following Chinese herbal medicines

26kg of plantain herb, 8kg of radish seed, 28kg of paederia scandens, 2kg of catechu, 14kg of dried orange peel, 28kg of elephantopus scaber, 8kg of dried ginger, 22kg of radix scutellariae, 16kg of bighead atractylodes rhizome, 8kg of kudzu root, 12kg of roughhaired holly root and 18kg of corydalis tuber.

Parching Atractylodis rhizoma and Raphani semen, and decocting in water. Decocting twice, wherein the water amount is 6 times of the total weight of the medicinal materials in the first decocting, filtering after 50 minutes, collecting filtrate, the water amount is 6 times of the total weight of the medicinal materials in the second decocting, filtering after 40 minutes, collecting filtrate, combining the liquid medicines decocted in the two times, concentrating under reduced pressure at 65 ℃, and concentrating until the relative density of the liquid medicine is 1.25.

Example 5

Preparing the following Chinese herbal medicines

Example 6

Further preparation of extract

Granulating and finishing:

material picking: taking the extract and the starch according to the prescription amount.

Spray drying the fluid extract to obtain dry extract powder, mixing the dry extract powder with appropriate amount of adjuvant, high-efficiency wet granulating, stirring for 60 + -5 s, and opening cutter for 30 + -5 s to obtain wet granule.

And (3) drying: drying the wet granules by a boiling dryer, and discharging when the moisture of the dry granules is 4.5-7.5%.

Sieving and granulating: sieving the prepared granules with a 20-mesh sieve, grading the coarse granules with the 20-mesh sieve, and adding the granules into qualified granules.

Total mixing: adding 2% of talcum powder and 0.5% of magnesium stearate into the qualified granules, and uniformly mixing.

Tabletting:

calculating the slice weight: the weight of the tablet to be pressed is the total weight of the granules after the total mixing/theoretical number of tablets

And (4) installing a tabletting mold and performing deep drawing with the diameter of 8.5 mm. And (3) gradually adding qualified particles into the feed hopper, adjusting the weight of the tablets to be qualified, then testing the tablets, and tabletting the tablets after all the tablets are qualified through an intermediate inspection project to obtain 96 ten thousand tablets.

Sugar coating: color: yellow colour

The operation method comprises the following steps:

material picking: every pot with 33-38 kg of vegetarian slices takes about 25kg of sucrose, 25-30 kg of talcum powder, about 200g of gelatin, about 20g of lemon yellow and 60-70 g of wax powder. Carefully checking whether the content materials are consistent with the content of the label.

Preparing syrup: heating appropriate amount of sucrose and distilled water to obtain 65-75% concentrated syrup, and adding 0.3% edible pigment when colored syrup is required to obtain colored syrup.

Preparing a gelatin solution: heating appropriate amount of gelatin and distilled water to obtain 15% gelatin slurry solution.

Sugar coating: adding plain tablets into a pan, opening a coating pan, heating and drying for 45-60min, adding a proper amount of gelatin slurry and talc powder to coat 3-5 layers of isolating layers, adding a proper amount of dilute syrup and talc powder to coat 7-10 layers of powder, adding a proper amount of dilute syrup and talc powder to coat 4-6 layers of smooth layers, adding a proper amount of colored syrup to coat 3-5 layers of colored sugar layers from shallow to deep until the sugar tablets are round, smooth and uniform in color, adding a proper amount of insect wax powder to polish, taking out the sugar tablets, putting the sugar tablets into a dry clean cloth bag, weighing and recording. The water content of the sugar-coated tablet is controlled to be less than or equal to 5 percent, and the weight gain of the sugar-coated tablet is controlled to be more than or equal to 100 percent.

Test example 1

600 diarrhea patients with various causes of disease were recruited, and the patients were averagely divided into 6 groups, the groups 1 to 5 were treated by the pharmaceutical compositions prepared in examples 1 to 5, and the group 6 was treated by the commercial berberine, and after 3 days, the improvement of the patients was counted, and the results were divided into three types of recovery, improvement and ineffectiveness, and the number of the patients in each group was counted, as shown in the following table:

group/status (person)	Recovery method	Improvement of life	Invalidation
				1	81	15	4
2	91	9	0
				3	93	5	2
4	92	8	0
				5	96	4	0
6	56	32	12

As can be seen from the above table, the pharmaceutical composition of the present invention has significantly better effect on treating diarrhea than the commercially available pharmaceutical composition, the total recovery rate is greater than 80%, and the pharmaceutical composition prepared by the preferred embodiment of the present invention has better curative effect.

Test example 2

Setting comparison groups 1-4, wherein the pharmaceutical compositions in the comparison groups are based on the pharmaceutical composition and the preparation method thereof in example 5, wherein the comparison group 1 is removed of rhizoma Zingiberis from the components, and the other components and preparation conditions are kept unchanged; the corydalis tuber in the components is removed in the comparison group 2, and the other components and the preparation conditions are kept unchanged; removing radix Puerariae from the control group 3, and keeping the rest components and preparation conditions unchanged; the control group 4 had the radix Scutellariae removed, and the other components and preparation conditions remained unchanged.

400 diarrhea patients with various causes of disease were recruited, and the average was divided into 4 groups, and the 1 st to 4 th groups were administered the pharmaceutical compositions prepared in comparative examples 1 to 4, respectively, for treatment for 3 days, and the disease improvement status of the patients was counted, and the results were divided into three types of recovery, improvement and ineffectiveness, and the number of the patients in each category was counted, as shown in the following table:

group/status (person)	Recovery method	Improvement of life	Invalidation
				1	81	15	4
2	75	18	17
				3	85	14	1
4	79	20	1

Therefore, the dried ginger, the corydalis tuber, the radix scutellariae and the radix puerariae all play an important role in fully playing the drug effect, and the cure rate is reduced due to the lack of any one of the dried ginger, the corydalis tuber, the radix scutellariae and the radix puerariae.

Case 1

After taking berberine, the tablet medicine prepared according to the methods of the embodiment 5 and 6 is taken by 15 tablets per day, the diarrhea symptom is obviously improved after 2 days, and the patient is completely cured after 3 days.

Case 2

If the patient suffers from bacterial diarrhea for one week and does not have improved symptoms after taking berberine in a dose of about 35 years old in plum, Beijing, the patient takes 12 tablets per day, and after 1 day, the diarrhea symptoms are remarkably improved and completely cured after 3 days.

While particular embodiments of the present invention have been illustrated and described, it would be obvious that various other changes and modifications can be made without departing from the spirit and scope of the invention. It is therefore intended to cover in the appended claims all such changes and modifications that are within the scope of this invention.

Claims

1. The antidiarrheal pharmaceutical composition is characterized by being mainly prepared from the following components in parts by weight: 20-30 parts of plantain herb, 5-10 parts of radish seed, 25-35 parts of paederia scandens, 2-3 parts of catechu, 10-20 parts of dried orange peel, 25-35 parts of elephantopus scaber, 5-15 parts of dried ginger, 15-25 parts of radix scutellariae, 10-20 parts of bighead atractylodes rhizome, 5-15 parts of kudzu root, 5-15 parts of roughhaired holly root and 15-25 parts of corydalis tuber.

2. The pharmaceutical composition of claim 1, wherein the pharmaceutical composition is prepared from the following components in parts by weight: 24-26 parts of plantain herb, 7-8 parts of radish seed, 28-32 parts of paederia scandens, 2-3 parts of catechu, 14-16 parts of dried orange peel, 28-32 parts of elephantopus scaber, 8-12 parts of dried ginger, 18-22 parts of radix scutellariae, 14-16 parts of bighead atractylodes rhizome, 8-12 parts of kudzu root, 8-12 parts of roughhaired holly root and 18-22 parts of corydalis tuber.

3. An antidiarrheal pharmaceutical formulation comprising the pharmaceutical composition of claim 1 or 2 and a pharmaceutical excipient.

4. The antidiarrheal pharmaceutical formulation of claim 3, wherein said antidiarrheal pharmaceutical formulation is a tablet, an extract, or a granule, preferably said antidiarrheal drug is a tablet.

5. The preparation method of the antidiarrheal pharmaceutical composition according to claim 1 or 2, which comprises the steps of decocting the composition with water, concentrating, precipitating with ethanol, and concentrating for the second time to obtain an ointment.

6. The process of claim 5, wherein the water-decocting is carried out twice, the first time for 50-70 minutes and the second time for 40-50 minutes.

7. The method of claim 6, wherein the weight of the water added at each time of water decoction is 5-7 times of the weight of the medicinal materials.

8. The method of claim 5, wherein the water-decocted extractive solution is concentrated at 65-75 deg.C under reduced pressure to a relative density of 1.15-1.25.

9. The method as claimed in claim 5, wherein ethanol is added in an amount of 1-2 times the volume of the solution during the alcohol precipitation.

10. The method according to claim 5, wherein the liquid medicine is sealed and left standing for 20-28 hours before the second concentration, and the second concentration is performed at 60-65 ℃ under reduced pressure until the relative density of the liquid medicine is 1.15-1.20.