KR100516560B1 - Hypoglycemic and anagesic composition - Google Patents

Abstract

The present invention provides a simple and effective method for extracting and purifying extracts from Cardios crispus L. which have a strong hypoglycemic effect, excellent analgesic activity, and high safety using inexpensive organic solvents, The present invention relates to an antidiabetic, therapeutic adjuvant and therapeutic composition, and anti-inflammatory or antipyretic analgesic composition, which are used alone or in combination with other effective drugs, ingredients, and extracts, together with excipients or adjuvants that can be used functionally or functionally. The composition according to the present invention is expected to have excellent efficacy, high safety, and greatly reduce side effects when compared with drugs widely used as conventional diabetes treatment and analgesics.

Description

      Hypoglycemic and analgesic composition {Hypoglycemic and anagesic composition}

The present invention relates to a method for extracting and extracting extracts exhibiting hypoglycemic activity and analgesic activity from natural resources. More specifically, the present invention is an extract of the outpost (roots, leaves, stems and flower parts: especially flower parts) of the fin thistle ( Carduus crispus L.), which has a strong hypoglycemic activity and analgesic activity, hereinafter referred to as SJ -2101) and a method for extracting and extracting the extract.

The fin thistle ( Carduus crispus L.) is a biennial herb belonging to the genus Compositae, growing straight up to 60-100 cm, with wings on the main stem, with the tip of the spines of thorns. The leaves are regenerated, long oval, erupted, deeply and shallowly divided into pterygium, and the lateral side is dull, ending with thorns. Flowers bloom in June-August, purple to white, and fruity leaves in July-September. It is distributed throughout the country and grows in mountainous or wild areas. Their outposts or roots are called astringents or parenterals. It is also called as cotton, boxer, inertia, jatacho, and brain ball. Big wind. Colloquial. It has the effect of anti-inflammatory, and is mainly a sense of wind fever, wind fever, wind rash, skin ulceration, lobster, urethritis, Carbuncle, arthritis, vaginal injury. It is widely used for burns, hematuria, and hemostasis. However, as a result of a literature search for this plant, no specific efficacy studies have been conducted. Therefore, the present inventors have conducted an efficacy study for this plant extract, and as a result, the following invention has been completed.

      The present inventors conducted a drug search for natural resources to develop an antidiabetic and analgesic drug that is ideally used in the clinic, and among them, the extracts of fin thistle outposts or flower buds showed a strong hypoglycemic effect and analgesic effect. It was. The present inventors fractionated the extract of the fin thistle part by systematic organic solvent extraction and distribution method, and completed the present invention by confirming that the obtained organic solvent fraction exhibits strong blood sugar lowering action and analgesic activity. The present inventors have prepared the extract in an efficient and simple manner in extracting and extracting the red thistle thistle hatchery extract, which has a strong hypoglycemic and analgesic effect, and verified its physiological activity and safety through animal experiments.

      SJ-2101 showed excellent hypoglycemic activity, strong analgesic activity, and high safety. In addition, the SJ-2101 is an extract extracted from natural resources, and it is expected that side effects will be greatly reduced compared to synthetic compounds. SJ-2101 is a tablet, capsule, powder, oral solution, syrup, poultice, ointment, which is a pharmaceutical form commonly used in combination with conventional pharmaceutically used excipients or adjuvants, stabilizers, PH regulators, antioxidants, and It may be formulated and administered in the form of a conventional preparation such as an injection. The amount of SJ-2101 may vary depending on the patient's condition, age, sex, etc., but in general, the amount of 100-3000 mg may be divided and administered several times a day. This extract can also be used alone or in combination with other active drugs, ingredients and extracts.

      The present invention is explained in more detail by the following examples and experimental examples.

      In extracting and refining extracts with excellent hypoglycemic activity and analgesic activity from fin thistle buds, collect only thistle outpost or bristles, and then remove the fat-soluble substances using a nonpolar solvent and stir the remaining residue by adding lower alcohol. Then, the mixture was concentrated under reduced pressure, and the mixture was sufficiently shaken by distilled water, and then the organic solvent layer obtained by extracting and distributing by adding a halogen compound, a lower ether or a lower ketone and a hydrophilic lower acetate or butanol, etc. was combined, and dried under reduced pressure to lower the blood sugar level. It is characterized by purifying fin thistle extract with strong action, excellent analgesic activity and high safety. The present invention is described in more detail as follows.

      A fine fin thistle outpost or 5 Kg of firearms was added to an extractor, and 7 L of a non-polar solvent such as hexane and petroleum ether were added thereto, stirred at 60-80 ° C. for 3 hours, and filtered to obtain a residue of fin thistle. The residue was added to an extractor and 5 L of lower alcohol such as 50-100% methanol was added thereto, followed by stirring extraction at 60-90 ° C. for 2-8 hours. After extraction, the mixture was filtered and the filtrate was concentrated. To this was added a halogenated compound such as methyl chloride and 3 L of distilled water, followed by shaking sufficiently to obtain an organic solvent fraction. The obtained fractions were concentrated under reduced pressure below the boiling point to obtain an extract (hereinafter referred to as SJ-2101).

       The present invention is described in detail as examples and experimental examples as follows.

Example 1

      3 Kg of shredded fin thistles was added to the extractor, and 5 L of hexane was added thereto, followed by stirring at 60 ° C. for 6 hours, followed by filtration to obtain a fin thistle residue. The residue was added to an extractor, and 5 L of 80% methanol was added thereto, followed by extraction with stirring at 50 ° C for 6 hours. After the extraction was completed, the filtrate was concentrated, 2 L of distilled water was added thereto, the mixture was suspended, and extracted three times with 2 L of methylene chloride, and the obtained fraction extracts were combined, and the resultant was concentrated under reduced pressure to obtain SJ-2101. Got it.

Example 2

      After cutting 5 Kg of thistle fins into the extractor, it was added to 7 L of 80% ethanol, and extracted three times at 80 ° C for 3 hours. The extracts were combined and concentrated under reduced pressure at the boiling point to obtain a concentrated extract. . 1.5 L of distilled water was added to the extract, shaken and suspended in a water bath, followed by extraction and extraction three times by 1.5 L of hexane, 1.5 L of ether was added to the aqueous layer, and the extraction was performed three times. The extracted ether layers were combined and concentrated under reduced pressure below the boiling point to obtain SJ-2101.

Example 3

      3 Kg of shredded thistle outposts were placed in an extractor, and 5 L of hexane was added thereto, followed by stirring at 60 ° C. for 6 hours, followed by filtration to obtain a fin thistle residue. The residue was added to an extractor, and 5 L of 80% methanol was added thereto, followed by extraction with stirring at 50 ° C for 6 hours. After the extraction was completed, the filtrate was concentrated, 2 L of distilled water was added thereto, the mixture was suspended, and extracted three times with 2 L of methylene chloride, and the obtained fraction extracts were combined, and the resultant was concentrated under reduced pressure to obtain SJ-2101. Got it.

Example 4

      Cut 5 Kg of thistle outpost and put it in the extractor, add 7 L of 80% ethanol to it, extract it three times at 80 ° C for 3 hours, combine the extracts, and concentrate under reduced pressure to obtain a concentrated extract. . 1.5 L of distilled water was added to the extract, shaken and suspended in a water bath, followed by extraction and extraction three times by 1.5 L of hexane, 1.5 L of ether was added to the aqueous layer, and the extraction was performed three times. The extracted ether layers were combined and concentrated under reduced pressure below the boiling point to obtain SJ-2101.

Experimental Example 1

    Acute Toxicity Experiment

In the group of 10 male rats (23 ± 2 g) fasted from the evening before the experiment, SJ-2101 was administered orally and parenterally (abdominal injection) to observe abnormal behavior. LD ₅₀ values were calculated from the number of dead animals for 72 hours according to the methods of Lichfield J. and Wilcoxon F.

Acute Toxicity Experimental group LD ₅₀ (mg / kg) Route of administration     SJ-2101        > 3000> 2000        Oral cavity

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From the results of Table 1, the LD ₅₀ value of SJ-2101 was orally administered at 3000 mg / Kg or more, and intraperitoneal administration at 2000 mg / Kg or more.

Experimental Example 2

      Hypoglycemic action (hyperglycemic-induced mice)

      Male rats of 25 ± 2 g body weight (ICR) were divided into 10 groups and fasted for 16 hours, followed by intravenous administration of 75 mg / kg of aloxane, and blood glucose levels of 400 mg / kg after 48-72 hours. Diabetic rats with dl or more were selected and used for the experiment. SJ-2101 was dissolved in physiological saline (5% tween 80) and orally administered. After 120 minutes, blood was collected from the tail vein and glucose was measured by glucose oxidase method. .

Blood sugar measurement Experimental group Capacity (mg / kg, po ) Marisu Glucose content in serum (mg / dl) 0 hours 2 hours  %     Relative control group (aloxane) SJ-2101      --250500    10 10 10 10    143.9 ± 3.4 518.8 ± 15.6 511.2 ± 11.5 541.2 ± 13.8     140.5 ± 5.5 504.2 ± 19.9 357.6 ± 12.5 * 252.5 ± 15.1 **     2.3 2.8 30.0 53.3

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* p <0.05, ** p <0.01

      From the results of Table 2, it was confirmed that the hypoglycemic action of SJ-2101 in hyperglycemic mice is strongly dose-dependent.

Experimental Example 3

      Analgesic activity

The Way of the Whittle [ Brit. J. Pharmacol ., 22, 246 (1964)], 10 adult male seedlings (22 ± 2 g) fasted for one day, oral administration of the sample in a group, 0.7% acetic acid after 60 minutes 10 ml / kg of physiological saline was intraperitoneally injected, and 10 minutes later, the number of stretches was measured as a nociceptive index for 10 minutes. The anti-rising effect was determined by the inhibition rate of the sample administration group against the rising water of the control group.

Analgesic activity Experimental group Dose (mg / kg, po ) Marisu Rising Water % Inhibition      Control group SJ-2101       -200 400     10 10 10      12.7 ± 1.4 11.2 ± 0.8 * 8.5 ± 0.7 **        11.8 33.1

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* p <0.05, ** p <0.01

  From the results of Table 3, SJ-2101 showed significant analgesic activity in the 200, 400 mg / kg dose group.

      From the above experimental results, SJ-2101 of the present invention has a strong hypoglycemic action and excellent analgesic effect in hyperglycemic mice, and also shows high safety during oral and intraperitoneal administration in acute toxicity experiments. Therefore, it could be confirmed that SJ-2101 can be usefully used as an analgesic composition exhibiting excellent diabetes prevention, therapeutic supplements and therapeutic agents, and analgesic effects in terms of effectiveness and safety.

Claims (4)

1) extracting the outposts or flower beds of the fin thistle ( Carduus crispus L.) with hexane or petroleum ether and then filtering; 2) extracting the residue obtained in step 1) with methanol or ethanol; 3) distilled water and methylene chloride or ether are added to the filtrate obtained by filtration of the extract, followed by extractive distribution; And 4) extracts of the fin thistle, which are prepared by a method comprising the step of drying under reduced pressure the organic solvent layer obtained by extracting distribution and exhibiting hypoglycemic and analgesic action. 1) extracting the outpost or firewood of the fin thistle with hexane or petroleum ether and then filtering; 2) extracting the residue obtained in step 1) with methanol or ethanol; 3) distilled water and methylene chloride or ether are added to the filtrate obtained by filtration of the extract, followed by extractive distribution; And 4) A method for producing an extract of the fin thistle of claim 1, comprising the step of drying the organic solvent layer obtained by extraction and drying under reduced pressure. A composition for the treatment or prevention of diabetes, comprising the extract of the fin thistle of claim 1 as an active ingredient. An analgesic composition comprising the extract of the fin thistle of claim 1 as an active ingredient.