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Medical application of 1,2,3,4,6-O-pentagalloylglucose and composition thereof in preparation of demulcent medicaments

A technology of pentagalloyl glucose and its composition, which is applied in the field of preparing analgesic drugs, and can solve problems such as abnormal and allergic reactions, side effects that are difficult to eliminate, and adverse reactions

Inactive Publication Date: 2012-09-12
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among the current drugs for treating pain, although opioid receptor drugs such as morphine and pethidine have strong effects, they are prone to dependence and addiction, and once the side effects appear, it is difficult to eliminate
While reducing pain, non-steroidal analgesics such as indomethacin may cause obvious adverse reactions, such as gastrointestinal reactions, hematopoietic system abnormalities and allergic reactions
Existing analgesic drugs often have defects such as high dosage and large toxic and side effects. Therefore, there is an urgent market demand for analgesic drugs with high efficiency and low toxicity.

Method used

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  • Medical application of 1,2,3,4,6-O-pentagalloylglucose and composition thereof in preparation of demulcent medicaments
  • Medical application of 1,2,3,4,6-O-pentagalloylglucose and composition thereof in preparation of demulcent medicaments
  • Medical application of 1,2,3,4,6-O-pentagalloylglucose and composition thereof in preparation of demulcent medicaments

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0006] Inhibitory effect of PGG on visceral pain.

[0007] Blank control: 5% ethanol solution

[0008] Positive control: Indomethacin (2mg / kg)

[0009] Sample: sample PGG, after dissolving in ethanol, dilute to 5% ethanol solution, and prepare 2.4mg / kg, 1.6mg / kg, 0.8mg / kg, 0.4mg / kg solutions respectively. Indomethacin was made into a 2mg / kg solution with 5% ethanol solution.

[0010] Experimental method: 50 ICR mice, weighing 20±2g, were randomly divided into 5 groups, 10 mice in each group, and the drugs in each group were administered by intragastric administration. Concave, hind limbs straight, buttocks raised as indicators, record the number of writhing times of mice in each group within 15 minutes, and calculate the percentage of analgesic inhibition. Analgesic percentage (%)=(average number of writhing in the control group−average number of writhing in the treatment group) / average number of writhing in the control group×100%.

[0011] Experimental results: see Table ...

Embodiment 2

[0017] Effects of PGG on central and peripheral pain.

[0018] Blank control: 5% ethanol

[0019] Positive control: Indomethacin (2mg / kg)

[0020] Sample: sample PGG, after dissolving in ethanol, dilute to 5% ethanol solution, and prepare 2.4mg / kg, 1.6mg / kg, 0.8mg / kg solutions respectively. Indomethacin was made into a 2mg / kg solution with 5% ethanol solution.

[0021] experimental method:

[0022] Experimental method: 50 ICR mice, weighing 20±2g, were randomly divided into 5 groups, each group was administered by intragastric administration, and 20 μl of 2.5% formaldehyde solution was injected into the right hind foot of the mice 1 hour after the administration, and each time was recorded. The paw licking time of mice in the first phase (0-5min) and the second phase (15-35min).

[0023] Experimental results: see Table 2

[0024] Table 2 Effect of PGG on formaldehyde-induced pain mice

[0025]

[0026] *P<0.05, **P<0.01 compared with model group

[0027] Formaldeh...

Embodiment 3

[0030] Analgesic effect of PGG and SA combined in specific ratios.

[0031] Blank control: 5% ethanol solution

[0032] Positive control: Indomethacin (2mg / kg)

[0033] Sample: According to the baseline equal ratio increase and decrease method, under the premise of a constant total amount, take SA / PGG (3 / 2) as the baseline, expand to both sides, keep a distance, and finally expand to the pole, and divide it into several variable groups in the middle. During this period, the SA content decreased by 20%, and the PGG content increased by 20%. Conversely, the PGG content decreased by 20%, and the SA content increased by 20%, expanding to both sides.

[0034] Table 3 Dosage groups set according to the baseline proportional increase and decrease method

[0035]

[0036] Select (2:0, 4:1, 7:3, 3:2, 1:1, 2:3, 1:4, 0:2) from Table 3 (1, 3, 4, 5, 6, 7, 9, 11) groups.

[0037] Experimental method: 100 ICR mice, weighing 20±2g, were randomly divided into 10 groups. The drugs in eac...

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PUM

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Abstract

The invention relates to the fields of natural medicaments and medical health care, and in particular relates to medical application of 1,2,3,4,6-O-pentagalloylglucose (PGG) in preparation of demulcent medicaments. Animal experiments prove that the PGG has obvious demulcent activity for visceral pain, central pain and peripheral pain, and has low effective dose. The invention also discloses a composition of the PGG and ligustilide A (SA) in a specific ratio. The composition has a strong demulcent effect on the visceral pain, and has a broad application prospect.

Description

technical field [0001] The present invention relates to the fields of natural medicine and medical care, in particular to 1,2,3,4,6-O-pentagaloylglucose (PGG) and its combination with Ligustilide A (SA) in a specific ratio, which is used in the preparation of analgesic Uses in medicine. Background technique [0002] Pain is a complex physiological and psychological activity, and it is one of the most common clinical symptoms, which often brings great pain to patients. About 4 million patients in the world suffer from pain every day. Among the current drugs for treating pain, although opioid receptor drugs such as morphine and pethidine have strong effects, they are prone to dependence and addiction, and once the side effects appear, it is difficult to eliminate them. While reducing pain, non-steroidal analgesics such as indomethacin may cause obvious adverse reactions, such as gastrointestinal tract reactions, hematopoietic system abnormalities and allergic reactions. Exi...

Claims

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Application Information

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IPC IPC(8): A61K31/7024A61P29/00A61P25/04A61P25/00A61K31/365
Inventor 寇俊萍朱丹妮徐娅妮曹旦华
Owner CHINA PHARM UNIV
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