WO2006122485A1

WO2006122485A1 - A pharmaceutical composition for treating diabetes and process thereof

Info

Publication number: WO2006122485A1
Application number: PCT/CN2006/000952
Authority: WO
Inventors: Zhang Zou; Quyi Zhong; Hong Su; Guihua Chen; Yaoxin Zheng
Original assignee: Guangzhou Zhongyi Pharmaceutical Company Limited
Priority date: 2005-05-18
Filing date: 2006-05-12
Publication date: 2006-11-23
Also published as: RU2362578C1; CN100355442C; CN1861176A

Abstract

A pharmaceutical composition for treating diabetes, and process thereof. The active ingredients of the pharmaceutical composition are prepared from radix rehmanniae, radix astragali, rhizoma dioscoreae, radix puerariae, radix trichosanthis, stigma maydis, fructus schisandrae sphenantherae and glibenclamide. The pharmaceutical composition has the functions of nourishing kidney and yin, supplementing the vital energy and promoting the production of body fluid. It is used in treating diabetes due to deficiency of both vital energy and yin, namely type II diabetes.

Description

Medicine composition for treating diabetes and preparation method thereof

Technical field

The present invention relates to a pharmaceutical composition, and more particularly to a Chinese and Western medicine combination composition for treating diabetes. It belongs to the technical field of medicines.

Background technique

Diabetes, which is called "diabetes disease" by Chinese medicine, is a common endocrine and metabolic disease characterized by high blood sugar, which is caused by absolute or relative deficiency of insulin. The main clinical symptoms are: polyuria, polydipsia, polyphagia, weight loss. Compared with non-diabetics, the incidence of cardiovascular and cerebrovascular diseases, blindness and mortality in diabetic patients are 2 to 5 times higher, and the rate of lower extremity ulcers and amputation is 20 times higher. At present, diabetes has become the third largest non-communicable disease after relaying cardiovascular diseases and tumors in developed countries, and it is a worldwide public health problem that seriously threatens human health.

According to the survey, the global incidence of diabetes is about 120 million in 1994, about 135 million in 1997, about 175 million in 2000, and is expected to reach 239 million in 2010, and the number of cases will increase by 200% in developing countries, China, India, Some developing countries in Africa are the main affected areas. Both clinical and marketplaces urgently need an effective drug for the treatment of diabetes.

At present, the use of chemical synthetic drugs for the treatment of diabetes at home and abroad, the recent results are satisfactory, but the long-term effect is not good, easy to produce side effects and complications.

In the invention patent application publication CN1562188A published on January 12, 2005, a thirst-quenching preparation is prepared, and the raw material composition thereof is pueraria 4000g, rehmannia 240g, astragalus 80g, trichosanthin 400g, corn whisker 400g, schisandra chinensis 80g, yam 40 g, glibenclamide 0.3 g composition. In this group, the high dose of puerarin is used as a medicinal herb. In the proportion of raw materials, the single-flavored medicinal root is up to 4000 parts by weight, while the sum of the other medicinal herbs is only 1240 parts by weight. The amount of pueraria root is much higher than that of Fangzhong. Other medicines, and much higher than the clinical doses of the Chinese Pharmacopoeia, also affect the effective function of the other drugs in the prescription, the prescription composition is obviously unreasonable, and according to the preparation method disclosed by the invention, due to the extract of Pueraria The rate of the paste is high, and the amount of the preparation is large, which is not convenient to take and carry.

Summary of the invention

SUMMARY OF THE INVENTION It is an object of the present invention to provide a novel pharmaceutical composition which can coordinate the characteristics of various drugs in various ways to exert the optimal therapeutic effect of each drug.

The object of the present invention is achieved by the following technical solution - a pharmaceutical composition for treating diabetes, characterized in that the active ingredient of the pharmaceutical composition is as follows

Confirmation Made of raw materials - 600-1200 parts by weight of Radix Rehmanniae, 200-400 parts by weight of Astragalus, 100-200 parts by weight of yam, 1000-2000 parts by weight of Pueraria, 1000-2000 parts by weight of Tianhuan, 1000-2000 parts by weight of corn, 5重量份。 The schisandra chinensis 200-400 parts by weight, glibenclamide 0. 2-1. 5 parts by weight.

The active ingredient of the preferred pharmaceutical composition of the present invention is prepared from the following ratios of the drug substance: - 600-900 parts by weight of Rehmannia glutinosa, 200-300 parts by weight of Astragalus, 100-150 parts by weight of Yam, 1000-1500 parts by weight of Radix Puerariae, 1000-1500 parts by weight of the smallpox, 1000-1500 parts by weight of the corn, 200-300 parts by weight of the Schisandra chinensis, and 0.2-1.0 parts by weight of glibenclamide.

The active ingredient of a further preferred pharmaceutical composition of the present invention is prepared from the following ratios of raw materials: 636 parts by weight of rehmannia, 212 parts by weight of astragalus, 106 parts by weight of yam, 1060 parts by weight of pueraria, 1060 parts by weight of geranium, 1060 parts by weight of corn, 1060 Parts by weight, 212 parts by weight of Schisandra chinensis, 1 part by weight of glibenclamide.

The pharmaceutical composition of the invention is based on the famous doctor Ye Tianshi of the Qing Dynasty, "Yuquan San" and "Xiaofang", and functions to nourish the kidney and nourish the yin, and to replenish the vital energy. Fangzhongdi Huang Zishen Yangyin; Huangqi Yiqi, fastening phlegm, Shengjinzhike, a total of medicine. Yam benefits lung spleen gas, lung and kidney yin, with the rehmannia glutinous spleen and Shengjin to tonify kidney water true yin; Gegen Shengyang Shengjin, help Huang Qi Sheng temper, scattered fine lungs, a total of medicine. Tianhua powder clear stomach heat, nourishing stomach yin, moist lung dryness, go to the middle of the coke quenching; corn must be water swelling, so that the kidney is open and fixed, ordering, a total of adjuvant. The schisandra chinensis is sour, the upper part can converge the lung yin, the lower can solidify the kidney and stimulate the body, the internal energy can stimulate the body and the nerves, the external energy can absorb the sweat, so that the water is not in a hurry, it is for the medicine; the whole party plays the kidney and nourish the yin and benefit The effect of Qishengjin. Combined with the western medicine glibenclamide, this side can alleviate the symptoms of Chinese medicine for quenching thirst and achieve the purpose of lowering blood sugar.

According to the theory of traditional Chinese medicine and the practical application of the product, the various flavors in the pharmaceutical composition of the present invention reasonably optimize the proportion and combination of the prescription, and the effect thereof is obviously superior to the "diabetes preparation" and glibenclamide, and provides for the treatment of diabetic patients. A safe and effective formulation achieves the objectives of the present invention.

The pharmaceutical composition of the present invention can be formulated into a variety of clinically desirable dosage forms, including pills, pills, tablets, capsules, granules, soft capsules or powders, according to the technical requirements of the formulation.

The following describes the preparation process of various commonly used dosage forms:

1. Preparation of pills:

Take radix puerariae, rehmannia root, corn stalk, trichosanthin, astragalus, schisandra, yam and boiled water once, filter, filter the filtrate to the appropriate amount, let cool, add ethanol to make the solution alcohol content 60%, let stand for 24 hours, filter The filtrate is concentrated to an alcohol-free taste, and 2 times the amount of water is added to the concentrated paste, and after stirring and dissolving completely, the pretreated macroporous adsorption resin is passed. After eluting with water until the effluent was colorless, it was eluted with 70% ethanol, and the eluate was collected until it was colorless, and concentrated to obtain an extract. Take polyethylene glycol 6000 (PEG-6000) and stearic acid into the container, heat to 100 ~ 110 ° C, after all melting, add glibenclamide and the above extract, evenly dispersed, with liquid paraffin Pills are prepared by dropping the coolant, and the dropping pills are taken out, and the paraffin is dried, that is, the pills are obtained.

2. Preparation of pills:

Method 1: Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, and Corn. Add boiling water for five hours, filter, and concentrate the filtrate to an appropriate amount. Astragalus, Schisandra, and Yam will be pulverized into a coarse powder. Mix well with the concentrate, dry, and pulverize into fine powder. Mix well. The water is pill, dried, added with glibenclamide, coated with black iron oxide, talc and an appropriate amount of binder, light-coated, and dried to form a pellet.

Method 2: Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, and Corn. Add boiling water for five hours, filter, and concentrate the filtrate to the appropriate amount. Astragalus, Schisandra, Yam is pulverized into a coarse powder, mixed with the concentrate, dried, and pulverized into fine powder. Mix well. Pills were prepared by mechanical pelleting, dried, glibenclamide was added, black iron oxide, talc and appropriate amount of binder were applied, light-coated, and dried to prepare pellets.

Method 3: Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, and Corn. Add boiling water for five hours, filter, and concentrate the filtrate to an appropriate amount. The scutellaria, schisandra, and yam are pulverized into coarse powder, mixed with the concentrate, dried, and pulverized into fine powder. Mix well. The granules were pelletized by a one-step granulator, and glibenclamide was added and compressed into pellets.

Method 4: Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, and Corn. Add boiling water for five hours, filter, and concentrate the filtrate to an appropriate amount. Astragalus, Schisandra, Yam pulverized into fine powder, and concentrate into a granulator to make granules. Glyburide is added and compressed into pellets.

3. Preparation of capsules:

Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, and Corn. Add boiling water for five hours. Filter it. The filtrate is concentrated to an appropriate amount. Astragalus, Schisandra, Yam is pulverized into a coarse powder, mixed with the concentrate, dried, pulverized into fine powder, and added to the grid. Lebenone and appropriate amount of dextrin, mixed, granulated, filled, and made into capsules.

4. Preparation of tablets - Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, Corn must be boiled for one hour for five hours, filtered, and the filtrate is concentrated to an appropriate amount. Astragalus, Schisandra, Yam is pulverized into a coarse powder, and mixed with the concentrate, dried. The granules are added to the granules, and the granules are added to the granules. The granules are added to the granules, and the mixture is granulated, dried, and mixed with 0.5% magnesium stearate and compressed into tablets.

5. Preparation of granules:

Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, and Corn. Add boiling water for five hours, filter, and concentrate the filtrate to a suitable amount. 芪, nanzizi, yam crushed into coarse powder, mix well with the concentrate, dry, pulverize into fine powder, add glibenclamide and appropriate amount of dextrin, mix and prepare granules.

6, the preparation of soft capsules:

Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, and Corn. Add boiling water for five hours. Filter it. The filtrate is concentrated to an appropriate amount. Astragalus, Schisandra, Yam is pulverized into a coarse powder, mixed with the concentrate, dried, pulverized into fine powder, and added to the grid. The lebenol is mixed, and an equal amount of polyethylene glycol-400 and a small amount of glycerin are added, mixed, and compressed into soft capsules.

7. Preparation of powder - Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, Corn must be boiled for one hour for five hours, filtered, and the filtrate is concentrated to an appropriate amount. Astragalus, Schisandra, Yam is pulverized into a coarse powder, mixed with the concentrate, dried, smashed. To form a fine powder, add glibenclamide, mix and prepare a powder.

The following is a process study to demonstrate that the pharmaceutical composition of the present invention is stable in process and controllable in quality:

1. Materials and methods

1. 1 material

The "diabetes preparation" was prepared by the formulation of Example 4 of the publication CN1562188A.

The "preparation of the present invention" was prepared by the formulation of Example 1 of the present invention.

1. 2 methods

Thick paste amount X dry solid content

1. 2. 1 extract yield = X 100%

Extracting the amount of medicine

1. 2. 2 Other items: According to the 2000 edition of the Chinese Pharmacopoeia

2. Data:

Conclusion: It can be seen from the above experimental results that the "prescription of the present invention" is more reasonable and the process is better than the "diabetes preparation". It is more stable and consumes less, and the quality of the finished product is stable and controllable. The composition of the present invention has good formulation stability as compared with the prior art, and the finished product has good disintegration (disintegration) properties and formulation uniformity. The therapeutic effects of the pharmaceutical composition of the present invention are illustrated below by animal pharmacodynamic experiments.

1 Materials and methods

1. 1 material

1. 1. 1 drugs and reagents

The "diabetes preparation" is a sample prepared according to the formulation of Example 4 of the publication CN1562188A; the "preparation of the present invention" is a powder prepared by the prescription of the embodiment 1 of the present invention. Dilute to the desired concentration with water before the experiment.

Glibenclamide: Product of New Technology Development Company of Tianjin Pharmaceutical Research Institute; Streptozotcin (STZ) SIGMA Chemical Company, USA; Glucose Standard Solution: Shanghai Institute of Biological Products, Ministry of Health; Glucose Oxidase: From Guangdong Provincial Clinical Testing Center purchased; Cholesterol standard solution: produced by Beijing Chemical Plant; Enzymatic triglyceride determination kit (imported packaging): Shanghai Changzheng Medical Science Co., Ltd.; High fat emulsion composition: Cholesterol: 5g, Dutch import packaging Sodium deoxycholate: 0.3g, SERVA products, New York, USA; lard: 20g (commercially available), plus Tween 80 (Japanese product packaging) and 1, 2 propylene glycol (Shanghai Reagent First Factory) , formulated into 50ml emulsion, that is.

1. 1. 2 main instruments BBO automatic biochemical analyzer: Corning, the United States products.

1.1.3 Animals MH mice and SD rats were provided by the Medical Laboratory Animal Farm of the Guangdong Provincial Health Department.

1. 2 methods

1.2.1 Effects on blood glucose in normal mice

Thirty healthy mice weighing 23~25g, male and female, were randomly divided into 4 groups: normal control group was intragastrically administrated with equal volume of normal saline, positive control glibenclamide 2mg/kg was administered, "thirst The preparation group is "administered by the stomach", and the dose is equivalent to 34.94g of crude drug/kg, containing 2mg of glibenclamide, and the "prescription of the present invention" group is administered with "the preparation powder of the present invention", and is administered. The dose is equivalent to 8.64g of crude drug per kg, containing 2mg of glibenclamide. After 3 days of routine feeding, fasting for 12 hours, blood was taken from the eyelids, blood glucose was measured by glucose oxidase method, and the blood glucose level was used as a basic blood glucose level, and then administered by oral gavage, and blood glucose was measured at 3 and 7 hours after administration, respectively. Times. The basal blood glucose level is subtracted from the blood glucose level after administration as the blood glucose drop value after administration.

1.2.2 Effect of streptozotocin on blood glucose in diabetic rats

Healthy rats weighing 150-180 g were selected, male and female, and after 5 days of routine feeding, fasting for 12 hours. According to the literature method, streptozotocin (50 mg/5 ml/kg, prepared in pH 4.5 in citric acid buffer) was quickly injected from the tail vein of the rat once, and the normal group was injected with an equal amount of buffer. Two weeks later, blood was taken for blood glucose measurement, and rats with blood glucose levels higher than 16.8 mmol/L and urine sugar continuously +++ or more were selected as qualified diabetic rats.

Qualified diabetic rats were randomly divided into 4 groups, and a normal control group was set up. The drug was administered orally once a day for four weeks. The normal and model control groups were intragastrically administered with an equal volume of normal saline, and the positive control group was administered with glibenclamide 1 mg/kg, and the "diabetes preparation group" was administered with "diabetes preparation powder" at a dose equivalent to 17.47 g. The amount of raw drug/kg, containing 1 mg of glibenclamide, the "preparation of the present invention" group is administered with "the preparation powder of the present invention", and the dose is equivalent to 4.32 g of the drug amount/kg, containing 1 mg of glibenclamide. The blood glucose (glucose oxidase method) was taken the next day after stopping the drug to compare the differences between the groups.

1.2.3 Effects on cholesterol, triglyceride, liver and kidney function and hemorheology in diabetic rats with hyperlipidemia

The preparation method of streptozotocin-induced diabetic rat model is the same as experiment 1.2.2. Forty healthy diabetic rats were randomly divided into 4 groups, and a normal control group was set up. The normal and model control groups were intragastrically administered with an equal volume of normal saline, and the positive control group was administered with glibenclamide 1 mg/kg, and the "diabetes preparation group" was administered with "diabetes preparation powder" at a dose equivalent to 17.47 g. The drug amount/kg contains 1 mg of glibenclamide, and the "preparation of the present invention" group is administered with "the preparation powder of the present invention", and the dose is equivalent to 4.32 _g of the drug amount/kg, and contains 1 mg of glibenclamide. At the same time as the morning administration, the high-fat emulsion (5 ml/kg/time) was administered in the afternoon for 3 weeks. After stopping the drug for 12 hours, the ether was lightly anesthetized, and the heart was taken for blood cholesterol measurement (ethanol extraction to improve iron-sulfuric acid colorimetry) and triglyceride (enzymatic method - GPO).

1. 3 Statistical analysis data are expressed as ± s, and differences between groups are determined by t test.

2 results

2. 1 effect on blood glucose in normal mice (see Table 1 for results)

Table 1 Effect on blood glucose in normal mice (±s, n=10)

Dosage base 3⁄4» sugar value post-drug blood drop (mmol L) group

(g kg) (mmol/L) 3h after drug 7h after drug

4.70+0.90 1.37± 0.93 0.99+ 1.17

Glibenclamide 2X 10-3 5.26+ 1.59 2.07 ± 0.46* 3.23+ 1.57** Diabetes preparation 34.94 4.83 ± 1.23 2.12 ± 0. 63* 3.17 ± 1.67** Preparation of the invention 8.64 5.14 ± 1.52 2.25 ±0. 42 * 3.43 ± 1.55** Note: Compared with the control group: *P<0.05;**P<0.01 (the same below)

2.2 Effect on blood glucose of streptozotocin-induced diabetic rats (see Table 2 for results)

Table 2 Effect on blood glucose of streptozotocin-induced diabetic rats (±s,

Dose blood glucose value (mmol/L)

Group

X (gkg) before drug use

ο

Normal 5.56±0.95 0.25±0.11

Photograph 24.23 ±3.94 -1.52±4.69

Glibenclamide 1X10-3 25.64±3.47 2.90±3.02*

Diabetes preparation 17.47 25.19±2.98 3.05 ±1.90*

Formulation of the invention 4.32 24.69±3.73 3.66 ±2.57**

2.3 Effects on cholesterol and triglyceride in diabetic rats with hyperlipidemia (Results are shown in Table 3)

Table 3 Effect on cholesterol and triglyceride in diabetic rats with hyperlipidemia (±s, η=ΪΟ)

Dose serum total cholesterol serum triglyceride

Group

(gkg) (mmol/L) (mmolL)

Normal 0.60±0.28 1.48 ±0.49

Photograph 1.59±0.51 2.96 ±1.45

Glibenclamide 1.44±0.43 2.52±1.12

Diabetes preparation 17.47 1.25 ±0.33 1.95±0.71

Formulation of the invention 4.32 0.96+0.21**ΛΛ 1.58±0.71*Δ

Compared with the glibenclamide and the diabetes-preventing group, AP<0.05 and AAP<0.01.

in conclusion:

1. It can be seen from the above experimental results that the glibenclamide group, the "prescription of the present invention" and the "diabetes preparation" have a significant effect on the blood glucose of normal mice and streptozotocin diabetic rats, and the control group. Comparing <0.05 or P<0.01, there was no significant difference in the hypoglycemic effect between the three; "The preparation of the present invention" has a significant inhibitory effect on the serum total cholesterol and serum triglyceride in diabetic hyperlipidemia rats, and There were significant differences between the control group, the glibenclamide group and the Xiaoke preparation. PO.05 or corpse <0.01;"glibenclamidegroup" and "diabetes preparation" had high blood fat and diabetes The serum total cholesterol and serum triglyceride did not inhibit the increase, and the effect of the "prescription of the present invention" was better than that of "the elimination". Thirsty preparation" and glibenclamide group.

2. According to the traditional Chinese medicine theory and the practical application of the product, the present invention rationally optimizes the proportion and combination of prescriptions, and the effect thereof is obviously superior to the "diabetes preparation" and glibenclamide, and the dosage is significantly lower than " The thirst-quenching preparation is convenient for taking and carrying, and provides a safe and effective preparation for the treatment of diabetic patients, and achieves the object of the present invention. The technical solutions of the present invention are further illustrated by some embodiments below.

Example 1 : Preparation of pellets

Weigh the raw Chinese herbal medicines and glibenclamide according to the following dosages:

Rehmannia 636 parts by weight, astragalus 212 parts by weight, yam 106 parts by weight, puerarin 1060 parts by weight, 10,60 parts by weight of trichosanthin, 1060 parts by weight of corn, 212 parts by weight of schisandra, and 1 part by weight of glibenclamide. Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, Corn, and boil for one hour. Add the filtrate to the appropriate amount. The scutellaria, schisandra and yam are pulverized into a coarse powder. Mix well with the concentrate, dry, pulverize into fine powder, and mix. . The water is pill, dried, added with glibenclamide, coated with black iron oxide, talc and an appropriate amount of binder, light-coated, and dried to form a pellet.

Example 2: Preparation of pellets

Rehmannia 600 parts by weight, Astragalus 200 parts by weight, Yam 100 parts by weight, Pueraria 1000 parts by weight, Trichosanthin 1000 parts by weight, Corn must be 1000 parts by weight, South Schisandra 200 parts by weight, Glibenclamide 1.5 parts by weight. Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, Corn, and boil for one hour. Add the filtrate to the appropriate amount. The scutellaria, schisandra and yam are pulverized into a coarse powder. Mix well with the concentrate, dry, pulverize into fine powder, and mix. . The water is pill, dried, added with glibenclamide, coated with black iron oxide, talc and an appropriate amount of binder, light-coated, and dried to form a pellet.

Example 3: Preparation of capsules

Rehmannia 636 parts by weight, astragalus 212 parts by weight, yam 106 parts by weight, puerarin 1060 parts by weight, 10,60 parts by weight of trichosanthin, 1060 parts by weight of corn, 212 parts by weight of schisandra, and 1 part by weight of glibenclamide. Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, and Corn. Add boiling water for five hours. Filter it. The filtrate is concentrated to an appropriate amount. Astragalus, Schisandra, Yam is pulverized into a coarse powder, mixed with the concentrate, dried, pulverized into fine powder, and added to the grid. Lebenone and an appropriate amount of dextrin, mixed, granulated, and filled into capsules.

Example 4: Preparation of capsules Weigh the raw material Chinese herbal medicine and 1200 parts by weight of glibenclamide - Rehmannia glutinosa, 400 parts by weight of astragalus, 200 parts by weight of yam, 2000 parts by weight of puerarin, 2000 parts by weight of geranium powder, 2000 parts by weight of corn, and 400 parts by weight of schisandra chinensis. 2重量份。 Glyburide 0. 2 parts by weight. Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, and Corn. Add boiling water for five hours. Filter it. The filtrate is concentrated to an appropriate amount. Astragalus, Schisandra, Yam is pulverized into a coarse powder, mixed with the concentrate, dried, pulverized into fine powder, and added to the grid. Lebenone and an appropriate amount of dextrin, mixed, granulated, and filled into capsules. '

Example 5: Preparation of tablets

Rehmannia 636 parts by weight, astragalus 212 parts by weight, yam 106 parts by weight, puerarin 1060 parts by weight, 10,60 parts by weight of trichosanthin, 1060 parts by weight of corn, 212 parts by weight of schisandra, and 1 part by weight of glibenclamide. Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, and Corn. Add boiling water for five hours. Filter it. The filtrate is concentrated to an appropriate amount. Astragalus, Schisandra, Yam is pulverized into a coarse powder, mixed with the concentrate, dried, pulverized into fine powder, and added to the grid. The sucrose and the appropriate amount of dextrin, mixed, granulated, dried, mixed with 0.5% magnesium stearate, compressed into tablets.

Example 6: Preparation of tablets

Weigh the raw Chinese herbal medicine and glibenclamide according to the following dosage: 1200 parts by weight of Radix Rehmanniae, 400 parts by weight of Astragalus, 200 parts by weight of yam, 2000 parts by weight of puerarin, 2000 parts by weight of geranium, 2000 parts by weight of corn, 400 parts by weight of Schisandra chinensis. 5重量份。 glibenclamide 1. 5 parts by weight.

Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, and Corn. Add boiling water for five hours. Filter it. The filtrate is concentrated to an appropriate amount. Astragalus, Schisandra, Yam is pulverized into a coarse powder, mixed with the concentrate, dried, pulverized into fine powder, and added to the grid. % 脲和和和和和。。。。。。。。。。。。。。。。。。。。。。。。。。。。

Example 7: Preparation of granules

Weigh the raw Chinese herbal medicine and 600 parts by weight of glibenclamide-rehmannia, 200 parts by weight of astragalus, 100 parts by weight of yam, 1000 parts by weight of puerarin, 1000 parts by weight of geranium, 1000 parts by weight of corn, and 200 parts by weight of schisandra chinensis. 2重量份。 Glyburide 0. 2 parts by weight. Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, and Corn. Add boiling water for five hours. Filter it. The filtrate is concentrated to an appropriate amount. Astragalus, Schisandra, Yam is pulverized into a coarse powder, mixed with the concentrate, dried, pulverized into fine powder, and added to the grid. Lebenone and appropriate amount of dextrin, mixed with hooks, made into granules.

Example 8: Preparation of soft capsules

Weigh the raw Chinese herbal medicines and glibenclamide according to the following dosages - 重量份。 Respectively, 900 parts by weight of radix, 300 parts by weight of jaundice, 150 parts by weight of yam, 1500 parts by weight of pueraria, 1500 parts by weight of geranium, 1500 parts by weight of corn, 300 parts by weight of schisandra, and 0.2 parts by weight of glibenclamide. Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, Corn, and boil for one hour for 5 hours. Filter it. The filtrate is concentrated to an appropriate amount. Astragalus, Schisandra, Yam is pulverized into a coarse powder, mixed with the concentrate, dried, pulverized into fine powder, added. The glibenclamide is mixed, and an equal amount of polyethylene glycol-400 and a small amount of glycerin are added and mixed to prepare a soft capsule.

Example 9: Preparation of powder

900 parts by weight of rehmannia, 300 parts by weight of astragalus, 150 parts by weight of yam, 1500 parts by weight of puerarin, 1500 parts by weight of geranium powder, 1500 parts by weight of corn, 300 parts by weight of schisandra, 1 part by weight of glibenclamide, radix pueraria, puerarin The corn must be boiled for one hour for five hours, filtered, and the filtrate is concentrated to an appropriate amount. Astragalus, Schisandra, yam crushed coarse powder, mixed with the concentrate, dried, pulverized into fine powder, and mixed with glibenclamide. Into the powder.

Example 10: Preparation of pellets

600 parts by weight of Rehmannia glutinosa, 200 parts by weight of Astragalus, 100 parts by weight of yam, 1000 parts by weight of Pueraria, 1000 parts by weight of Tianhua powder, 1000 parts by weight of corn, 200 parts by weight of Schisandra chinensis, and 1 part by weight of glibenclamide. Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, and Corn. Add boiling water for five hours, filter, and concentrate the filtrate to the appropriate amount. Astragalus, Schisandra, Yam pulverized into coarse powder, mix well with concentrate, dry, pulverize into fine powder, mix uniform. The water is pill, dried, black iron oxide, talc and an appropriate amount of binder, and added to the glibenclamide, light-coated, dried, and pelletized.

Example 11: Preparation of pellets

500 parts by weight of rehmannia, 200 parts by weight of astragalus, 130 parts by weight of yam, 1100 parts by weight of puerarin, 1200 parts by weight of trichosanthin, 1300 parts by weight of corn, 250 parts by weight of schisandra, and 0.5 parts by weight of glibenclamide. Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, Corn, and boil for one hour. Add the filtrate to the appropriate amount. The scutellaria, schisandra and yam are pulverized into a coarse powder. Mix well with the concentrate, dry, pulverize into fine powder, and mix. . The water is pill, dried, black iron oxide, talc and an appropriate amount of binder, and added to the glibenclamide, light-coated, dried, and made into a pellet.

Example 12: Preparation of pellets Weigh the raw Chinese herbal medicines and glibenclamide according to the following dosages:

Rehmannia 750 parts by weight, Astragalus 250 parts by weight, Yam 130 parts by weight, Pueraria 1300 parts by weight, Trichosanthin 1300 parts by weight, Corn 1300 parts by weight, Schisandra chinensis 250 parts by weight, glibenclamide 0.5 parts by weight. Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, Corn, and boil for one hour. Add the filtrate to the appropriate amount. The scutellaria, schisandra and yam are pulverized into a coarse powder. Mix well with the concentrate, dry, pulverize into fine powder, and mix. . The water is pill, dried, black iron oxide, talc and an appropriate amount of binder, and added to the glibenclamide, light-coated, dried, and made into a pellet.

Example 13: Preparation of tablets

1000 parts by weight of Radix Rehmanniae, 220 parts by weight of Astragalus, 110 parts by weight of yam, 1000 parts by weight of puerarin, 1700 parts by weight of Tianhua powder, 1500 parts by weight of corn, 205 parts by weight of Schisandra chinensis, 0.4 parts by weight of glibenclamide. Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, and Corn. Add boiling water for five hours. Filter it. The filtrate is concentrated to an appropriate amount. Astragalus, Schisandra, Yam is pulverized into a coarse powder, mixed with the concentrate, dried, pulverized into fine powder, and added to the grid. The lenamide and the appropriate amount of dextrin, mixed, granulated, dried, mixed with 0.5% magnesium stearate, compressed into tablets.

Example 14: Preparation of granules

Rehmannia 650 parts by weight, Astragalus 205 parts by weight, Yam 120 parts by weight, Pueraria 1700 parts by weight, Trichosanthin 1500 parts by weight, Corn 1100 parts by weight, Schisandra chinensis 220 parts by weight, Glyburide 0. 8 parts by weight. Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, and Corn. Add boiling water for five hours. Filter it. The filtrate is concentrated to an appropriate amount. Astragalus, Schisandra, Yam is pulverized into a coarse powder, mixed with the concentrate, dried, pulverized into fine powder, and added to the grid. Lebenone and an appropriate amount of dextrin, mixed and made into granules.

Example 15: Preparation of Soft Capsules

Rehmannia 950 parts by weight, Astragalus 350 parts by weight, Yam 180 parts by weight, Pueraria 1500 parts by weight, Trichosanthin 1100 parts by weight, Corn 1200 parts by weight, Schisandra 280 parts by weight, Glibenclamide 1.2 parts by weight. Take Radix Rehmanniae, Radix Puerariae, Trichosanthin, and Corn. Add boiling water for five hours. Filter it. The filtrate is concentrated to an appropriate amount. Astragalus, Schisandra, Yam is pulverized into a coarse powder, mixed with the concentrate, dried, pulverized into fine powder, and added to the grid. The lebenol is mixed, and an equal amount of polyethylene glycol-400 and a small amount of glycerin are added and mixed to prepare a soft capsule.

Example 16: Preparation of a powder Weigh the raw Chinese herbal medicines and glibenclamide according to the following dosages:

Resveratrol, radix rehmanniae, radix rehmanniae, radix rehmanniae, rehmannia glutinosa, rehmannia glutinosa, rehmannia glutinosa, rehmannia glutinosa, rehmannia glutinosa, rehmannia glutinosa, rehmannia glutinosa, radix granules, granules, 1200 parts by weight, 1200 parts by weight, 1000 parts by weight , Trichosanthin, corn must be boiled for one hour for five hours, filtered, the filtrate is concentrated to the appropriate amount, Astragalus, Schisandra, yam crushed coarse powder, mixed with the concentrate, dried, pulverized into fine powder, added to glibenclamide Evenly, made into powder.

Example 17: Preparation of a pill

Weigh the raw Chinese herbal medicine and 636 parts by weight of glibenclamide-dihedron, 212 parts by weight of astragalus, 106 parts by weight of yam, 1060 parts by weight of puerarin, 1060 parts by weight of trichosanthin, 1060 parts by weight of corn, and 212 parts by weight of schisandra chinensis. Glibenclamide 1 part by weight. Take radix puerariae, rehmannia root, corn stalk, trichosanthin, astragalus, schisandra, yam and boiled water once, filter, filter the filtrate to the appropriate amount, let cool, add ethanol to make the solution alcohol content 60%, let stand for 24 hours, filter The filtrate is concentrated to a non-alcoholic taste. Add 2 times of water to the concentrated paste, stir and dissolve completely, and then pass through the pretreated macroporous adsorption resin, and elute with water until the effluent is colorless, and elute with 70% ethanol. After collecting the eluate until it is colorless, it is concentrated to obtain an extract. Take polyethylene glycol 6000 (PEG-6000) and stearic acid into the container, heat to 100 ~ 110 ° C, after all melting, add glibenclamide and the above extract, evenly dispersed, with liquid paraffin Pills are prepared by dropping the coolant, and the dropping pills are taken out, and the paraffin is dried, that is, the pills are obtained.

Example 18: Preparation of a pill

Weigh the raw Chinese herbal medicine and 750 parts by weight of glibenclamide-rehmannia, 250 parts by weight of astragalus, 130 parts by weight of yam, 1300 parts by weight of puerarin, 1300 parts by weight of geranium, 1300 parts by weight of corn, and 250 parts by weight of schisandra chinensis. 5重量份。 Glyburide 0. 5 parts by weight. Take radix puerariae, rehmannia root, corn stalk, trichosanthin, astragalus, schisandra, yam and boiled water once, filter, filter the filtrate to the appropriate amount, let cool, add ethanol to make the solution alcohol content 60%, let stand for 24 hours, filter The filtrate is concentrated to a non-alcoholic taste. Add 2 times of water to the concentrated paste, stir and dissolve completely, and then pass through the pretreated macroporous adsorption resin, and elute with water until the effluent is colorless, and elute with 70% ethanol. After collecting the eluate until it is colorless, it is concentrated to obtain an extract. Take PEG 6000 (PEG-6000) and stearic acid into the container, heat to 100 ~ 110 ° C, after all melting, add glibenclamide and the above extract, after the dispersion is hooked, to the liquid The paraffin is made into a pellet of a coolant, and the pellet is taken out, and the paraffin is dried, and the pellet is obtained.

Claims

Rights request

A pharmaceutical composition for treating diabetes, characterized in that the active ingredient of the pharmaceutical composition is prepared from the following ratio of the raw material medicine: 600-1200 parts by weight of Radix Rehmanniae, 200-400 parts by weight of Astragalus, 100-200 of Yam重量份, 葛根 1000-2000 parts by weight, trichosant 1000-2000 parts by weight, corn must be 1000-2000 parts by weight, schisandra chinensis 200-400 parts by weight, glibenclamide 0. 2-1.5 parts by weight.

The pharmaceutical composition according to claim 1, wherein the active ingredient is prepared from the following ratio of the drug substance:

Rehmannia 600-900 parts by weight, Astragalus 200-300 parts by weight, Yam 100-150 parts by weight, Pueraria 1000-1500 parts by weight, Trichosanthin 1000-1500 parts by weight, Corn must-have 1000-1500 parts by weight, Schisandra chinensis, 200-300 weight份份份, 格列本尿 0. 2-1. 0 parts by weight.

3. The pharmaceutical composition according to claim 2, wherein the active ingredient is prepared from the following ratios of raw materials: 636 parts by weight of rehmannia, 212 parts by weight of astragalus, 106 parts by weight of yam, and 1060 parts by weight of puerarin. 1060 parts by weight of trichosanthin, 1060 parts by weight of corn, 212 parts by weight of Schisandra chinensis, and 1 part by weight of glibenclamide.

A pharmaceutical composition according to Claim 1, 2 or 3, which is a pill, a pill, a tablet, a capsule, a granule, a soft capsule or a powder.

A method for preparing the pharmaceutical composition according to claim 4, characterized in that the method comprises the steps of: taking radix pueraria, rehmannia, corn mustard, trichosanthin, astragalus, schisandra, yam and boiling water once, filtering, The filtrate is concentrated to an appropriate amount, allowed to cool, and ethanol is added to make the solution contain 60% alcohol. It is allowed to stand for 24 hours, filtered, and the filtrate is concentrated to an alcohol-free taste. Add 2 times of water to the concentrated paste, stir and dissolve completely, and pass in advance. The treated macroporous resin was adsorbed and eluted with water until the effluent was colorless, and eluted with 70% ethanol. The eluate was collected until it was colorless, and concentrated to obtain an extract. Take polyethylene glycol 6000 (PEG-6000) and stearic acid into the container, heat to 100~110 °C, after all melting, add glibenclamide and the above extract, disperse evenly, then use liquid paraffin Pills are prepared by dropping the coolant, and the dropping pills are taken out, and the paraffin is dried, that is, the pills are obtained.

A method for preparing a pharmaceutical composition according to claim 4, characterized in that the method comprises the following steps: taking rehmannia root, puerarin, trichosanthin, corn, and boiling water for five hours, filtering, concentration of the filtrate, jaundice, south Schisandra and yam are pulverized into fine powder, and the concentrate is granulated in a one-step granulator, and glibenclamide is added to be compressed into a pellet.

A method for preparing a pharmaceutical composition according to claim 4, characterized in that the method comprises the following steps: taking rehmannia, pueraria, trichosanthin, corn, and boiling water for five hours, filtering, concentration of the filtrate, jaundice, south Schisandra and yam are pulverized into coarse powder, mixed with concentrated solution, dried, pulverized into fine powder, and made into powder; the obtained powder is mixed, water is pelleted, dried, and glibenclamide is added, and black iron oxide is added. , talc and binder, light coating, made into pellets.

8. A method of preparing a pharmaceutical composition according to claim 7, wherein the obtained powder is taken and mixed. The pellets were prepared by a mechanical pelleting machine, dried, and glibenclamide was added, and the coating was dried with a black iron oxide, talc, and a binder, and dried to prepare a pellet.

9. A method of preparing a pharmaceutical composition according to claim 7, wherein the obtained powder is taken and mixed. Granules were prepared in a one-step granulator, and glibenclamide was added and compressed into pellets.

The method for preparing a pharmaceutical composition according to claim 7, wherein the obtained powder is obtained by adding glibenclamide and 0.2% sodium carboxymethylcellulose, mixing, granulating, and filling. Capsules.

The method for preparing a pharmaceutical composition according to claim 7, wherein: the obtained powder is added, glibenclamide and starch are added, mixed, granulated, dried, and mixed with an appropriate amount of magnesium stearate, and pressed. tablet.

A method of preparing a pharmaceutical composition according to claim 7, wherein the method comprises the steps of: taking the obtained powder, adding glibenclamide and dextrin, and mixing to prepare a granule.

The method for preparing a pharmaceutical composition according to claim 7, wherein: the obtained powder is added, and the glibenclamide is added to the hook, and then an equal amount of polyethylene glycol-400 and a small amount of glycerin are added, and the mixture is mixed. , pressed into soft capsules.

The method for preparing a pharmaceutical composition according to claim 7, wherein the obtained powder is added, glibenclamide is added, and the mixture is mixed to prepare a powder.