WO2016101324A1 - Native composition containing enzymes and use thereof in pharmacy - Google Patents

Abstract

Provided are a native composition containing enzymes and a use thereof in treating gout. The native composition containing enzymes comprises a therapeutically effective amount of enzymes, lycopene, grape seed extract and a pharmaceutically acceptable excipient; and the enzymes are one or more of papain, bromelain, trypsin, chymotrypsin, pancreatin, nattokinase, lumbrokinase or collagenase. The native composition of the present invention has obvious therapeutical effects on gout and cardiovascular diseases; also has effects of increasing immunity, preventing diabetes and cancers; and can be used for preparing drugs for treating gout, cardiovascular diseases, increasing immunnity, preventing diabetes and cancers.

Description

Natural composition containing enzyme and its application in pharmacy Technical field

The present invention relates to a natural composition containing an enzyme and uses thereof.

technical background

Gout is a crystal-associated joint disease caused by deposition of monosodium urate (MSU), which is directly related to hyperuricemia caused by a decrease in sputum metabolism and/or uric acid excretion, especially acute characteristic arthritis. Chronic tophi stone diseases, mainly including acute onset arthritis, tophus chronic arthritis, urate kidney disease and urinary acidic urinary calculi, severe joint disability and renal insufficiency. Gout is often associated with abdominal obesity, hyperlipidemia, hypertension, type 2 diabetes, and cardiovascular disease. Among them, acute gouty arthritis is the most serious damage to the body.

At present, the main drugs for treating gouty arthritis on the market are: non-steroidal anti-inflammatory drugs (NSAIDs), colchicine, glucocorticoids, uric acid-producing drugs (xanthine oxidase inhibitors), and uric acid-decomposing and excretion drugs. Although traditional Chinese medicine treatment of gout can dredge meridians, reduce swelling and relieve pain, and promote the benign circulation of blood in various joints, the compatibility of traditional Chinese medicine preparations is complicated, and it is inconvenient to eat, and some Chinese medicines are toxic and stimulating. The above drugs are not side effects or are not applicable to liver and kidney dysfunction, so they are more limited.

Summary of the invention

It is an object of the present invention to provide a natural composition containing an enzyme and its use in pharmaceuticals to overcome the deficiencies of the prior art.

The natural composition containing the enzyme of the present invention comprises a therapeutically effective amount of an enzyme, lycopene, grape seed extract and pharmaceutically acceptable excipients;

The enzyme is one or more of papain, bromelain, trypsin, chymotrypsin, trypsin, nattokinase, lumbrokinase or collagenase, but is not limited to the above varieties;

The auxiliary materials such as perfumes, sweeteners, liquid or solid fillers or diluents are commonly used as carrier materials, and are prepared into common pharmaceutical preparations such as tablets, capsules, powders, syrups and liquids by methods known in the art. The preparation, suspension, and preparation usually contain 35 to 60% by weight of an active ingredient, which is an enzyme, lycopene and grape seed extract.

The natural composition containing the enzyme comprises the following components by weight:

Preferred:

The papain can be used as a product of the German AB enzyme preparation company;

The bromelain can be used as a product of the German AB enzyme preparation company;

The trypsin may be a product of the German Union Enzyme Preparation Company;

The chymotrypsin is a proteolytic enzyme secreted by the pancreas, and is a product of the German Union Enzyme Preparation Company;

The trypsin is a mixture of trypsin, pancreatic amylase and pancreatic lipase, and is a product of the German AB enzyme preparation company;

The other enzymes such as nattokinase and lumbrokinase are products of the German Union Enzyme Preparation Company.

Grape seed extract can be used in literature: Wang Wei, Zheng Maoqiang, Wang Meng, Wang Siwei, Grape Seed Proanthocyanidins Separation and Purification Research, (Food and Food Industry, Vol. 16, 2009, No. 1) reported method preparation;

The excipients include medical and health food acceptable carriers such as diluents, excipients (such as water), fillers such as starch, sucrose, lactose, microcrystalline cellulose, etc., binders such as cellulose derivatives. , gelatin and polyvinylpyrrolidone, etc., wetting agent such as glycerin, surfactants such as cetyl alcohol, disintegrating agents such as calcium carbonate, crospovidone, sodium carboxymethyl starch, etc., lubricants such as talc And one or more of sodium stearyl fumarate, calcium stearate, and magnesium;

The preparation method of the present invention is conventional, and after mixing the components, the tablet is filled or filled by a method known in the art;

The test proves that the natural composition containing the enzyme of the invention has obvious therapeutic effects on gout and cardiovascular diseases, and has the effects of enhancing immunity, preventing diabetes and preventing cancer, and can be used for preparing gout drugs and cardiovascular diseases. Disease drugs, immune-enhancing drugs, diabetes prevention drugs, and cancer prevention drugs can also be used as natural nutritional compositions.

Preferably, the anti-inflammatory and anti-oxidation substances can also be combined with the natural composition containing the enzyme to have obvious curative effect on treating gout, and have auxiliary therapeutic effects on cardiovascular diseases, diabetes and hypertension. .

The natural composition containing the enzyme of the present invention can be orally administered to a patient in need of administration. In general, the dose is 20 mg to 50 mg/day/kg body weight, depending on the age of the patient, etc., depending on the physician.

The beneficial effects of the present invention are that the natural active substance is non-toxic and harmless, long-term use, and has no dependence, and is a safe and effective natural composition.

detailed description

Example 1

Preparation method: After mixing the components, the tablets are obtained by a method known in the art, and the tablets are obtained, and the weight of each tablet is 0.66 mg;

Clinical Observation:

(1) Clinical data

Clinical trials were conducted in 180 patients with gouty arthritis. These patients had varying degrees of joint pain and swelling, and the course of disease was 1-3 years. There were 120 males and 60 females. There were 104 patients in the treatment group and 76 patients in the control group.

(2) Treatment methods

The control group was routinely administered colchicine; the treatment group was orally administered the composition of the invention twice a day, 2 tablets each time; the cycle was 15 days

(3) Efficacy criteria:

Significant effect: no pain in the knee joint, no tenderness around the joint, no swelling of the joint, joint mobility 130°, X-ray examination of the joint is normal.

Effective: The knee joint is slightly painful, the skin around the joint is tender and tender, slightly swollen, and the joint mobility is 130°. X-ray examination of the joint space is mildly fuzzy.

Invalid: knee pain, swelling around the joints, tenderness, joint mobility less than 130°, X-ray examination of knee joint space narrowing, subchondral bone sclerosis.

(4) The clinical trial results are as follows:

clinical	Significant effect	effective	invalid	Total efficiency (%)
					therapy group	70	28	6	92.45
Control group	38	14	twenty four	68.42
					P value	<0.01			<0.01

In the subsequent long-term efficacy survey, there was almost no recurrence in the treatment group.

Example 2

Animal experiment

(1) Establishment of a model of hyperuricemia

Potassium oxonate is a uric acid enzyme inhibitor that acts as a chemical inducer to inhibit uric acid breakdown and increase serum uric acid levels in the body. The mice were intraperitoneally injected with oxonate potassium salt (Sigma) at a dose of 300 mg/kg 2 h before the blood sample was taken, and the normal control group was injected with an equal volume of 0.5% CMC-Na solution. Blood was collected from the posterior venous plexus of mice 2 h and 5 h after administration, and serum uric acid was determined by phosphomolybdic acid reduction method. The results showed that potassium oxonate can significantly increase serum uric acid level (P<0.001), resulting in a model of hyperuricemia in mice. The serum uric acid level of the model can be maintained for 5 hours. The method is sensitive, simple and reproducible, and has been widely used in the world to evaluate the antihyperuricemia and gout effects of drugs.

(2) Effect of nutritional composition on serum uric acid level in mice with hyperuricemia induced by potassium oxonate

60 Kunming mice, half male and half female, were randomly divided into 6 groups, 10 in each group. That is, the blank group, the hyperuricemia model group, the positive group (allopurinol 20 mg/kg) and the low, medium and high dose groups of nutritional composition (50 mg/kg, 100 mg/kg, 200 mg/kg). The mice were intraperitoneally injected with potassium oxonate at a dose of 300 mg/kg 2 hours before the blood was taken, and the blank group was injected with an equal volume of 0.5% CMC-Na solution; the administration group was intraperitoneally injected with the nutritional composition 1 hour before the blood was taken. The 嘌呤 group, the blank group and the model group were all injected with an equal volume of 0.5% CMC-Na solution. Blood was taken from each group of eyeballs, and the uric acid content in the serum of the mice was measured. The results are shown in the following table.

Effect of sample on hyperuricemia induced by potassium oxonate in mice

Note: **, p<0.01; *, p<0.05, compared with the model group at the same time point

▲ ▲, p < 0.01; compared with the positive group (all sterols);

It can be seen that the low, medium and high dose groups of the nutritional composition and the positive control group can significantly reduce the serum uric acid in hyperuricemia mice induced by potassium oxonate, and the dose-effect relationship is increased (P<0.01). There was no significant difference between the high dose group and the allopurin group (P>0.05).

Claims (7)

1. A natural composition comprising an enzyme comprising a therapeutically effective amount of an enzyme, lycopene, grape seed extract, and a pharmaceutically acceptable excipient;

   The enzyme is one or more of papain, bromelain, trypsin, chymotrypsin, trypsin, nattokinase, lumbrokinase or collagenase.
2. The natural composition containing an enzyme according to claim 1, which is a tablet, a capsule, a powder, a syrup, a liquid or a suspension.
3. The enzyme-containing natural composition according to claim 1, which comprises 35 to 60% by weight of an active ingredient, an enzyme, lycopene and grape seed extract.
4. An enzyme-containing natural nutritional composition characterized by comprising the following components by weight:

   
5. A natural composition comprising an enzyme characterized by comprising the following components by weight:

   

   
6. The use of the natural composition containing an enzyme according to any one of claims 1 to 5 for the preparation of a medicament for treating gout drugs, cardiovascular diseases, enhancing immunity drugs, preventing diabetes drugs and preventing cancer drugs.
7. The use according to claim 6, wherein the dose is from 20 mg to 50 mg per day per kg of body weight by oral administration to a patient in need of administration.