WO2005049057A1

WO2005049057A1 - Use of cassia sophera linn. for treating diabetes

Info

Publication number: WO2005049057A1
Application number: PCT/CN2003/000995
Authority: WO
Inventors: Xingbo Feng
Original assignee: Xingbo Feng
Priority date: 2003-11-24
Filing date: 2003-11-24
Publication date: 2005-06-02
Also published as: AU2003304545A1; CN1764466A

Abstract

The invention relates to the use of Cassia sophera Linn. and its extract for treating diabetes and ameliorating the symptoms of diabetes. The invention relates to the use of traditional Chinese medicine. The invention's medicine has an excellent blood glucose lowering effect. The invention's medicine will show an effect in two weeks of administration and show a significant effect in four weeks. So Cassia sophera Linn. And its extract can be used as desirable medicines for treating diabetes and ameliorating the symptoms of diabetes.

Description

Application of mangosteen and its extract in medicine for treating diabetes and improving symptoms thereof

The invention belongs to the field of medicinal use of traditional Chinese medicine.

Background technique

Anemone (Cassia sophera Li dish.), A medicinal plant, Cassia spp. According to the "Traditional Chinese Medicine Dictionary": "Amaranth, also known as Amaranth Cassia, is flat, non-toxic, and has a sweet taste. It has the effect of removing phlegm and thirst, making people sleepless, and regulating the effect. It is also known as Antipyretics. Alcoholic extracts from the leaves of Mang Mangosteen have the effect of relaxing the small intestine and bronchial smooth muscle of guinea pigs.

Summary of the invention

The purpose of the present invention is to prepare a medicament for treating diabetes and improving its symptoms by using mangosteen and its water extract.

The water extraction method is as follows:

1. Frying method: Water is used as the solvent, and the effective ingredients are extracted by heating and boiling. Generally, it must be extracted 2-4 times, and the amount of solvent is generally 6-20 times the amount of awn.

2. Infiltration method: After cold soaking or warm soaking, the mango is passed through the mango with a solvent at an appropriate temperature to dissolve the components of the mango.

3. Immersion method: Cold soaking or warm soaking of amaranth for a large number of solvents, and after the ingredients are dissolved and equilibrated, the extraction solution is directly released.

4. Ultrasonic extraction method: After soaking the awns, put them into ultrasonic waves together with the solvent, and use the effect of ultrasound to dissolve the awns. ,

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Correction page (Article 91) 5. Microwave extraction method: Put the awn in the microwave together with the solvent, and use the microwave to polarize the molecules to dissolve the components.

When the present invention is used to prepare a medicament for treating diabetes and improving its symptoms, the oral or gastrointestinal administration is safe. In the case of oral administration, it can be administered in any conventional form, such as Sanqi! ], Granules, tablets, capsules, pills, solutions, suspensions, syrups, buccal tablets, sublingual tablets, etc .; When the drug is administered parenterally, it can take any conventional form, such as injections (such as Intravenous injection), ointments, suppositories, transdermal administration, inhalants, etc.

The medicament prepared by the present invention for treating diabetes and improving its symptoms is composed of ramie or its water extract together with solid or liquid excipients. The solid or liquid excipients used herein are well known in the art, Here are some specific examples. Powder is an internal powder, and its excipients are lactose, starch, dextrin, calcium carbonate, synthetic or natural aluminum sulfate, magnesium oxide, magnesium stearate, sodium bicarbonate, dry Yeast, etc .; the excipients of the solution are water, glycerol, propylene glycol, monosyrup, ethanol, ethylene glycol, polyethylene glycol, sorbitol, etc .; the excipients of the ointment can be fatty oil, lanolin, petrolatum , Glycerin, beeswax, paraffin wax, liquid paraffin, resin, high-grade wax, etc.

The dosage of effective substance can be changed according to the way of taking, the age and weight of the patient and the severity of the disease and other similar factors. The oral dose is: 10.0-15.0mg / kg, twice daily. / kg, once a day.

The medicine of the invention has better effects of lowering blood sugar, treating diabetes and improving symptoms. detailed description

The beneficial effects of the medicament prepared by the present invention are further explained by the following test examples. These test examples include pharmacodynamic tests and clinical efficacy observation tests.

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Correction page (Article 91) Test example 1 Effect of burdock extract on hyperglycemic animal model in Wistar rats 1.1 Test materials

Drugs Mang Mang extract, provided by the Research Institute of New Drugs, Institute of Regenerative Medicine, Jilin University, batch number: 20010708; Xiaoke pills are produced by Guangzhou No. 1 Chinese Medicine Factory, approval number: (1994) No. 11146.

Animal Wistar rats, male and female, weighing 195g-240g, provided by the Laboratory Animal Department of Jilin University, quality certificate number: Yidongzi No. 10-5110; main reagents and instruments streptozotocin STZ produced by the American sigma chemical company , Lot Number: 89H0604

Blood glucose test strip produced by Beijing Yicheng Bioelectronic Technology Co., Ltd.

JPS-III fast blood glucose tester produced by Beijing Yicheng Bioelectronic Technology Co., Ltd.

Centrifuge Beijing Medical Centrifuge Factory, Model: LDZ5-2.

Fully automatic biochemical analyzer produced by Hitachi, Japan, Model: Hitachi 7170A.

1.2 Test method

Test conditions and methods:

After the introduction of Wistar rats from the Animal Department of Jilin University, they were bred in the animal room of the Basic Medical College of Jilin University at room temperature 22-25 ° C, humidity 30-60%, feed composition: cornmeal 39%, bean cake noodle 25 ° /. , Wheat bran noodles 14%, sorghum noodles 10%, bone meal 2.5%, fish meal 5%, yeast 3.5%, and additives 1%.

Take the mango extract powder to prepare 5.2% (g / v), 2.6% (g / v), 1.3% (g / v) large, medium and small doses of test solution. Xiaoke pill is formulated into a test solution with a concentration of 20% (g / v).

110 Wistar rats, male and female, were introduced from the Animal Department of Jilin University. They were acclimatized for 1 week in the room, fasted for 4 hours, weighed, measured for blood glucose, and marked. Choose a positive blood glucose level

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Correction page (Article 91) 100 male and female rats in the normal range and in good condition were tested, and 10 rats were left as the normal control group. 90 Wistar rats were modeled with streptozotocin STZ at 0.054 g / kg. The vegetarian STZ was formulated into a 2.0% solution with a 0.05 mol / L citric acid solution pH 4.5, and is now used. After fasting for 16 hours without fasting, rats were injected with streptozotocin STZ solution once intraperitoneally according to their weight. On the eighth day after fasting for 4 hours, the blood glucose was measured, and a blood glucose level of greater than 10 mmol / L was established as a model. Compared with the normal control group, there was a significant difference P <0.001. Fifty-four hyperglycemic model animals were randomly divided into five groups, with 10 to 11 animals in each group. The groups are: normal control group, model group, Xiaoke Wan group 2.0g / kg, which is equivalent to 4 times the clinical dosage; mango extract large dose group 0.62g / kg, medium dose group 0.31g / kg, low dose group 0.15g / kg, equivalent to 8, 4, or 2 times the clinical dosage.

The model group was given 10 ml / kg of water, and each administration group was given 10 ml / kg of test solution. Gavage is administered around 9am every day for four consecutive weeks. Blood glucose and body weight are measured weekly, and the dose is calculated once based on the new weight. Animals were sacrificed after the fourth week of administration, blood tests were performed for blood routine, blood biochemical indicators, blood rheology and insulin content, and pancreas were taken for histopathological examination. The results obtained by each group are represented by the mean () ± standard deviation (S), and the results are compared with the model group to perform a t-test between the groups to determine their significance.

1.3 Test results

1.3.1 Impact on Blood Sugar

At the third week after administration, the blood glucose of the mango extract in the high-dose group, the middle-dose group and the model group significantly decreased, P <0.05. At the fourth week, the blood glucose levels of the large and medium doses of the mango extract were lowered. Compared with the model group, the blood glucose level was significantly statistically significant P <0.05, see Table 1.

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Correction page (; Article 91) Move 1 group

Volume S

Table 1 Effect of Mangman extract on blood glucose value (mmol / L) in hyperglycemic model rats (ΐ 士 s) Normal control group ~~ Model group Xiaoke Wan group Medium dose group Small dose group ¾ Group 10ml / kg 2. Og / kg 0.62g / kg 0.31g / kg 0.15g / kg

10 8 9 10 9 8 Before dosing 6.11 ± 0.53 17.52 ± 2.40 17.22 ± 3.22 17.04 ± 3.34 17.10 ± 2.63 16.34 ± 3.32 One week 6.19 ± 0.50 17.15 ± 2.23 16.84 ± 3.06 15.54 ± 3.23 15.10 ± 2.36 15.72 ± 3.15 Two weeks 6.12 ± 0.41 15.85 ± 3.02 14.57 ± 3.02 13.59 ± 2.60 14.06 ± 2.53 15.18 ± 3.23 Three weeks 6.22: t0.31 14.05 ± 3.52 11.97 ± 2.53 10.93 ± 2.58 * 10.71 ± 2, 72 * 13.05 ± 3.26 Four weeks 5.89: t0.46 13.80 ± 4.16 9.38 ± 2.83 * 9.07 ± 2.78 * 9.45 ± 1.98 * 11.71 ± 3.53 Compared with the model group, * P <0.05

Test Yi ί! 2 Clinical observation of the drug of the present invention in the treatment of diabetic patients

2.1—General information See Table 2 Table 2

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Correction page (Article 91) 2.2 Treatment results

2.2.1 The glucose-lowering effect of the present invention is extremely significant

It can be clearly seen from Table 2 that these 25 diabetic patients consumed it for 28 days. Except for 2 patients who had diarrhea and general discomfort, the others had a significant hypoglycemic effect. After taking and comparing the blood glucose level, the average blood glucose was reduced by 2.0mmol. / L, reduced by 14.1mmol / L in severe patients. After t-test analysis, the t-value = 3.161, and at the degrees of freedom N = N-1 = 23-1 = 22, p = 0.01 and t = 2.819, so the effect of reducing glucose is extremely significant.

2.2.2 The longer you drink, the better the effect

2.2.2.1 The results of one week of drinking are shown in Table 3:

Analysis of hypoglycemic effect after drinking for a week

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Correction page (Article 91) Perform 1: test according to Table 3, the result is: t = 1.962, when the degree of freedom Nl = 22-l = 21, t = 2.080 at ρ = 0.05, and t = 1.721 at p = 0,10, so drink for one week Although effective, it is not significant. 2.2.2.2 The analysis of the effect of drinking for two weeks is shown in Table 4:

Table 4 Analysis of hypoglycemic effect after drinking for two weeks

t test result, t = 2.2637, when the degrees of freedom N = N-1 = 22-1 = 21, p = 0.05 t = 2.080, p = 0.10 t = 2.831, so the difference is significant, that is, the effect is obvious.

2.2.2.3 The effect analysis after drinking for three weeks is shown in Table 5:

Correction page (; Article 91) Table 5 Analysis of hypoglycemic effect after drinking for three weeks

t test result, t = 2.5043, when the degree of freedom N = N-1 = 19-1 = 18, p = 0.05 t = 2.101 p = 0.01 t = 2.878, so the effect is significant.

2.2.2.4 The analysis of the effects of drinking for four weeks is shown in Table 6:

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Correction page (Article 91) Patient (An) One week before drinking d

Blood glucose level (X) Blood glucose level (χ ₂ ) (X— X) d— 7

Al 11.0 6.7 4.3 2.566 6.584

A2 15.8 12.3 3.5 1.766 3.118

A3 11.3 10.8 0.5 -1.234 1.522

A4 9.7 8.8 0.9 -0.834 0.695

A5 12.3 8.8 3.5 1.766 3.118

A6 7.9 7.0 0.9 -0.834 0.695

A7 12.0 10.8 1.2 -0.534 0.285

A8 7.2 7.5 -0.3 -2.034 4.137

A9 9.7 7.6 2.1 0.366 0.133

A10 5.9 6.7 -0.8 -2.534 6.421

All 10.2 9.8 0.4 -1.334 1.779

A12 6.8 6.3 0.5 -1.234 1.522

A13 11.7 8.5 3.2 1.466 2.149

A14 8.9 5.9 3.0 1.266 1.602

A15 9.8 9.5 0.3 -1.434 2.056

A16 7.2 6.5 0.7 -1.034 1.069

A17 8.7 8.7 0 -1.734 3.006

A18 10.8 10.2 0.6 -1.134 1.258

A19 6.8 6.5 0.3 -1.434 1.602

A20 8.9 8.8 0.1 -1.634 2.669

A21 6.8 6.5 0.3 -1.434 1.602

A22 8.4 7.8 0.6 -1.134 1.258

A23 23.9 9.8 14.1 12.366 152.917 Total 231.7 (N = 23) 186.8.1 (N = 23) 39.9 201.251 Average 10.07 "x 8.078 Έ (1.734

According to the t test result, t = 3.161, when the degrees of freedom N = N-1 = 22-1 = 22, p = 0.05 t = 2.074, p = 0.01 t = 2.819, so the effect is extremely significant.

According to the analysis, the diabetic patients drink the invention, the longer the drinking time, the more obvious the effect, that is, drinking for one week is basically ineffective, drinking for two weeks shows a hypoglycemic effect, drinking for three weeks has a significant hypoglycemic effect, and drinking for four weeks is extremely significant .

2.2.3 Analysis of disease duration and drinking effect

The 23 diabetes patients drinking the present invention in Table 1 were divided into two groups: those who had been sick for more than 5 years as a group, and those who had been sick for less than 4 years as a group. Statistical analysis was performed, and the results were −

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Correction page (Article 91) .1, the analysis of the effect for more than 5 years is shown in Table 7

Table 7 Analysis of drinking effects for more than 5 years

t test result, t = 1.782, when the degrees of freedom N = N—1 = 13—1 = 12, t = 2.197 at p = 0.05, and t = 1.782 at p = 0.01, so the effect is not significant.

2.2.3.2. Table 8 shows the analysis of drinking effects for patients under 4 years of illness.

Table 8 Analysis of drinking effects after illness for 4 years

t test result, t = 2.966, when the degree of freedom N = N_ 1 = 10-1 = 9, p = 0.05 t = 2.262, p = 0.01 t = 3.250, so the effect is significant.

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Correction page (Article 91) 2.3 Conclusion

1. Amaranth has a significant effect on reducing blood sugar in patients with diabetes.

2. Patients with diabetes can take two weeks to take effect, and the effect is obvious around four weeks.

3. The disease is shorter (less than 4 years) longer than the time (more than 5 years).

The following examples further illustrate the preparation of the medicament of the present invention.

Example 1

Mangosteen water extract 2.0g, water 1000ml, mixed into 100 bottles, each 100ml, containing 20mg of mangosteen extract.

Example 2

15.0g of mangosteen and 485g of medicinal starch. The two are thoroughly mixed and filled into capsules to make 1000 capsules, each weighing 0.5g and containing 15mg of mangosteen.

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Correction page (Article 91)

Claims

Request for Rights

The application of maggot in the preparation of medicine for treating diabetes and improving its symptoms.

And hydrangea water extract in the preparation of medicine for treating diabetes and improving its symptoms

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Correction page (Article 91)