CN1569012A - Application of 20(R)-ginsenoside-Rg3 in the preparing process of medicine for treating or preventing hypertension - Google Patents
Application of 20(R)-ginsenoside-Rg3 in the preparing process of medicine for treating or preventing hypertension Download PDFInfo
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- CN1569012A CN1569012A CN 03132961 CN03132961A CN1569012A CN 1569012 A CN1569012 A CN 1569012A CN 03132961 CN03132961 CN 03132961 CN 03132961 A CN03132961 A CN 03132961A CN 1569012 A CN1569012 A CN 1569012A
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- ginsenoside
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Abstract
The invention provides the application of 20(R)-ginsenoside-Rg3 in the preparing process of medicine for treating or preventing hypertension, and the medicinal composition containing the 20(R)-ginsenoside-Rg3, wherein the medicinal composition can be administered through oral, tongue, subcutaneous, skin, urinary, vaginal or venous approaches.
Description
Technical field
The present invention relates to 20 (R)-ginsenoside-Rg
3Application in the medicine of preparation treatment or prophylaxis of hypertension.
Background technology
Along with the acceleration of aged tendency of population process and the change of life style, cardiovascular and cerebrovascular disease has become a global health problem, the mortality rate of coronary heart disease, apoplexy occupies the 1st, 3 respectively at world wide, and hypertension is considered to the main hazard factor of apoplexy always.The exploitation of novel and effective control hypertension disease medicament is very urgent.
20 (R)-ginsenoside-Rg
3It is the tetracyclic triterpenes panoxadiol type saponin monomer of separation and Extraction from Radix Ginseng.
20 (R)-ginsenoside-Rg
3Structural formula (R:-glu-o-glu; R
1:-CH
3R
2:-OH)
It is reported that Rg3 has antitumor, suppresses effects such as new vessels generation, antiinflammatory, but about 20 (R)-ginsenoside-Rg
3Effect with prevention or treatment hypertension does not appear in the newspapers; Given this, the inventor is surprised to find 20 (R)-ginsenoside-Rg by a large amount of experimentatioies
3Medical usage with prevention or treatment hypertension.
Summary of the invention
The invention provides 20 (R)-ginsenoside-Rg
3Application in the medicine of preparation treatment or prophylaxis of hypertension disease.
The invention provides and contain 20 (R)-ginsenoside-Rg
3The pharmaceutical composition of treatment hypertension.
20 (R)-ginsenoside-Rg
3Be used for the treatment of or during prophylaxis of hypertension its using dosage scope be 20mg～400mg, the preferred dose scope is 60mg～200mg.
20 (R)-ginsenoside-Rg that use among the present invention
3Can use separately or use with pharmaceutical compositions.Pharmaceutical composition comprises 20 (R)-ginsenoside-Rg as active component
3And pharmaceutical carrier.This pharmaceutical composition can be by oral, Sublingual, percutaneous, through muscle or subcutaneous, mucocutaneous, urethra, vagina or intravenous route administration.Pharmaceutical composition can exist with the form of tablet, pill, granule, capsule, suspension, solution, syrup, injection.Various pharmaceutical dosage form provided by the present invention all can be prepared from the pharmacy conventional method.
The inventor has confirmed that by following test 20 (R)-ginsenoside-Rg3 have the treatment or the effect of prophylaxis of hypertension disease, but is not limited to this test (the following examples are used for more detailed description the present invention, but and do not mean that the present invention only limits to this).Testing 20 used (R)-ginsenoside-Rg3 is provided by natural drug Engineering Technical Research Centre pharmaceutical chemistry research department, Shandong Province, and through HPLC detection level 90%, reference substance is provided by the natural drug Engineering Technical Research Centre chamber of analysis and research, Shandong Province.
The specific embodiment
Preparation embodiment 1: injection preparation prepares embodiment
Take by weighing 1.00g 20 (R)-ginsenoside-Rg
3, the propylene glycol that adds 20ml n-butyl alcohol and 30ml melts saponin fully, and the citric acid of 0.15g tetracaine hydrochloride, 0.02g is joined in the 40ml water for injection, makes dissolving fully, and above-mentioned aqueous solution is joined in the drug solution mix homogeneously; Regulating pH value with Borax and boric acid is 5.5 ± 1.0; 85 ℃ of insulations of the needle-use activated carbon of adding 0.1% 30 minutes, G
3Sintered glass funnel filters, the filtering with microporous membrane of 0.22um; Filtrate is sub-packed in the 7ml cillin bottle, and (directly tamponade of the injection that branch installs, jewelling cover into injection to every loading amount 2ml; Or make freeze-dried powder through the freeze dryer lyophilizing.)。
Test the influence of routine 1:20 (R)-ginsenoside-Rg3 to the experimental hypertension rat blood pressure
(1) material: 20 (R)-ginsenoside-Rg3: provide by natural drug Engineering Technical Research Centre pharmaceutical chemistry research department, Shandong Province.
Laboratory animal: regular grade Wistar rat, male, body weight 280g-350g, natural drug Engineering Technical Research Centre zoopery center, Shandong Province provides.The quality certification number: No. 200106005, Shandong kinoplaszm word.
(2) method and result: rat is divided into sham operated rats (waiting the capacity solvent) at random, model control group (waiting the capacity solvent), 20 (R)-ginsenoside-Rg3 small dose group (2mg/kg), dosage group (4mg/kg) among 20 (R)-ginsenoside-Rg3, the heavy dose of group of 20 (R)-ginsenoside-Rg3 (40mg/kg), 10 every group.After the fasting 12 hours, ip urethane (1.2g/kg) anesthesia, tracheal intubation, the abdomen position is in the constant temperature operating-table, outside the back of the body waist otch peritoneum of a left side, avoid the neural renal artery that separates of kidney, with the small artery folder of cover rubber tube, block the left renal artery blood flow fully, temporary transient closure of incisions, keep respiratory passage unblocked, the rectal temperature control is left standstill 4h at 37.5, changes dorsal position and fixes.In carotid artery intubate (PE50), write down arteriotony in Powerlab (8sp) through pressure transducer.Opening entry control basis blood pressure curve behind blocking-up kidney blood flow 4h, the renal artery folder is decontroled in stable back, and visible arteriotony rises gradually, about 3～6min tend towards stability (do not reach 14.5KPa as MAP and then abandon it).Each treated animal intravenous drip (injecting) relative medicine (administration volume 3ml, 30min drips off) of postoperative with infusion pump.The record administration before and administration after 1,5,10,15, the systolic pressure during 30min, diastolic pressure and changes in heart rate.
The result is shown in table 1, table 2, and 20 (R)-ginsenoside-Rg3 of various dose obviously reduce systolic pressure, the diastolic pressure of experimental hypertension rat, but changes in heart rate is not had influence.
Table 1 20 (R)-ginsenoside-Rg3 to the influence of experimental hypertension rat systolic pressure (X ± s, n=10)
Systolic pressure (mmHg)
Grouping
1min 5min 10min 15min 30min
Normal control group 125 ± 16 129 ± 18 126 ± 15 124 ± 15 126 ± 18
Model control group 193 ± 21
##196 ± 23
##195 ± 25
##194 ± 21
##196 ± 24
##
Heavy dose of group 186 ± 26 165 ± 15
*136 ± 16
*128 ± 28
*127 ± 18
*
Middle dosage group 197 ± 17 178 ± 28
*156 ± 26
*138 ± 28
*132 ± 28
*
Small dose group 189 ± 19 179 ± 19
*161 ± 16
*157 ± 18
*147 ± 19
*
Compare with model control group
*P＜0.05,
*P＜0.01; Compare with the normal control group
#P＜0.05,
##P＜0.01
Table 2 20 (R)-ginsenoside-Rg3 to the influence of experimental hypertension rat diastolic pressure (X ± s, n=10)
Diastolic pressure (mmHg)
Grouping
1min 5min 10min 15min 30min
Normal control group 85 ± 11 89 ± 12 86 ± 13 84 ± 12 86 ± 11
Model control group 132 ± 22
##136 ± 21
##135 ± 23
##134 ± 22
##136 ± 21
##
Heavy dose of group 116 ± 23
*106 ± 19
*97 ± 17
*88 ± 27
*81 ± 17
*
Middle dosage group 126 ± 13 117 ± 25
*106 ± 25
*92 ± 24
*83 ± 26
*
Small dose group 127 ± 14 117 ± 14
*107 ± 16
*102 ± 14
*98 ± 16
*
Compare with model control group
*P＜0.05,
*P＜0.01; Compare with the normal control group
#P＜0.05,
##P＜0.01
Test the vasodilator effect of routine 2:20 (R)-ginsenoside-Rg3
(1) material: 20 (R)-ginsenoside-Rg3: provide by natural drug Engineering Technical Research Centre pharmaceutical chemistry research department, Shandong Province.
Phenylephrine (PE) injection, Shanghai Hefeng Pharmaceutical Co., Ltd. produces; Except that specified otherwise, said medicine all is mixed with gradient dilution liquid with K-H liquid before experiment beginning standby.
Laboratory animal: rabbit is used in the experiment of growing up, and sex is regardless of, body weight 250kg～300kg, and natural drug Engineering Technical Research Centre zoopery center, Shandong Province provides.
(2) method: by [Li Anlong, Ye Yixin. the vasodilator effect of oxybenzene ammonia ketone and mechanism research thereof. Acta Pharmaceutica Sinica, 2002,37 (1): 10～3] described method, rabbit is impacted head, carotid artery sacrificed by exsanguination, get renal artery, insert in the K-H solution of oxygen enrichment.After removing blood vessel external fat and mucosa, be cut into the vascular strip of 5mm * 20mm continuously with helical form, an end is fixed in the 5ml bath bottom that contains K-H liquid, and the other end is fixed on the tonotransducer that range is 5g, whole vascular strip is soaked in the K-H liquid from start to finish, fills with 95%O continuously
2With 5%CO
2Gaseous mixture, bath is connected with water bath with thermostatic control, with (37.0 ± 0.5) recirculated water incubation.Transducer connects the Powerlab physiograph, adds the 1.5g preload, and balance 60～90min changes liquid 1 time every 15min.After antiotasis is stable, add variable concentrations 20 (R)-ginsenoside-Rg3, observe the influence of 20 (R)-ginsenoside-Rg3 normal vascular strip tension variation; Add 20 (R)-ginsenoside-Rg3 after adding blood vessel contracting agent phenylephrine (PE), observe the influence that 20 (R)-ginsenoside-Rg3 shrink vascular strip due to the PE.
(3) result:
A, 20 (R)-ginsenoside-Rg3 is to the influence of normal vascular strip tension variation
The result is as shown in table 3, and 20 (R)-ginsenoside-Rg3 of different final concentrations can reduce the vascular strip shrinkage amplitude, and vasodilator all has significant difference with blank group, solvent control group.
Table 3 20 (R)-ginsenoside-Rg3 to the influence of normal vascular strip tension variation (X ± s, n=6)
Concentration C shrinkage amplitude (g)
(mg/100ml) solvent 20 (R)-ginsenoside-Rg3
Blank group 1.6 ± 0.5 1.7 ± 0.6
0.5 1.6±0.3 1.5±0.6
1 1.5±0.5 1.2±0.6
*
2 1.4±0.5 1.0±0.5
**#
4 1.2±0.5 0.7±0.2
**#
8 1.2±0.3 0.3±0.1
**##
Compare with the blank group
*P＜0.05,
*P＜0.01; Compare with the solvent control group
#P＜0.05,
##P＜0.01
The blood vessel function that contracts of B, 20 (R)-ginsenoside-Rg3 antagonism PE
The result is as shown in table 4, and PE promotes vascular strip to shrink, the blood vessel function that contracts that 20 (R)-ginsenoside-Rg3 of different final concentrations can antagonism PE, and vasodilator relatively has significant difference with the PE matched group.
The blood vessel function that contracts of table 4 20 (R)-ginsenoside-Rg3 antagonism PE (X ± s, n=6)
Concentration C shrinkage amplitude (g)
(mg/100ml) solvent 20 (R)-ginsenoside-Rg3
Blank group 1.6 ± 0.5 1.7 ± 0.6
PE matched group 3.5 ± 1.8 3.6 ± 1.7
0.5 3.6±1.4 2.8±1.4
1 3.5±1.4 2.4±1.2
*
2 3.4±1.6 1.6±0.6
**
4 3.2±1.6 1.2±0.7
**
8 3.0±0.8 0.7±0.5
**
Compare with the PE matched group
*P＜0.05,
*P＜0.01
Claims (6)
1. the application of 20 (R)-ginsenoside-Rg3 in the medicine of preparation treatment or prophylaxis of hypertension disease.
2. application according to claim 1, the using dosage scope that it is characterized in that 20 (R)-ginsenoside-Rg3 is 20mg～400mg.
3. application according to claim 2 is characterized in that the using dosage of 20 (R)-ginsenoside-Rg3 is preferably 60mg～200mg.
4. contain being used for the treatment of or the pharmaceutical composition of prophylaxis of hypertension of 20 (R)-ginsenoside-Rg3.
5. pharmaceutical composition according to claim 4, said composition can be by oral, Sublingual, percutaneous, through muscle or subcutaneous, mucocutaneous, urethra, vagina or intravenous route administration.
6. according to claim 4 or 5 described pharmaceutical compositions, it is characterized in that compositions can exist with forms such as tablet, pill, granule, capsule, suspension, solution, syrup, injection, cream, ointment, spray, chewing agent or patches.
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| CN 03132961 CN1569012A (en) | 2003-07-24 | 2003-07-24 | Application of 20(R)-ginsenoside-Rg3 in the preparing process of medicine for treating or preventing hypertension |
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| CN 03132961 CN1569012A (en) | 2003-07-24 | 2003-07-24 | Application of 20(R)-ginsenoside-Rg3 in the preparing process of medicine for treating or preventing hypertension |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007134533A1 (en) * | 2006-05-22 | 2007-11-29 | Li Fu | 20(R)-GINSENOSIDE Rg3 MEDICINAL SOLUBLE INTERMEDIATE AND PROCESS THEREOF |
| WO2007134534A1 (en) * | 2006-05-22 | 2007-11-29 | Li Fu | WATER SOLUTION OF 20(R)-GINSENOSIDE Rg3 PHARMACEUTICAL COMPOSITION AND PROCESS THEREOF |
| CN103845280A (en) * | 2012-11-30 | 2014-06-11 | 富力 | 20(R)-ginsenoside Rg3 preparation for external use, preparing method thereof and applications thereof |
| CN104643058A (en) * | 2013-11-21 | 2015-05-27 | 富力 | Application of 20(R)-ginsenoside Rg3 in preparation of medicines for improving or/and treating liver cirrhosis diseases |
-
2003
- 2003-07-24 CN CN 03132961 patent/CN1569012A/en active Pending
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007134533A1 (en) * | 2006-05-22 | 2007-11-29 | Li Fu | 20(R)-GINSENOSIDE Rg3 MEDICINAL SOLUBLE INTERMEDIATE AND PROCESS THEREOF |
| WO2007134534A1 (en) * | 2006-05-22 | 2007-11-29 | Li Fu | WATER SOLUTION OF 20(R)-GINSENOSIDE Rg3 PHARMACEUTICAL COMPOSITION AND PROCESS THEREOF |
| JP2009537572A (en) * | 2006-05-22 | 2009-10-29 | 富力 | 20 (R) -Ginseng Saponin (Ginsenoside) Rg3 Medicinal Composition Aqueous Solution and Method for Preparing the Same |
| AU2007252183B2 (en) * | 2006-05-22 | 2013-07-11 | Dalian Fusheng Natural Medicine Development Co. Ltd | Water solution of 20(R)-ginsenoside Rg3 pharmaceutical composition and process thereof |
| US8487090B2 (en) | 2006-05-22 | 2013-07-16 | Dalian Fusheng Natural Medicine Development Co., Ltd. | Water solution of 20(R)-ginsenoside Rg3 pharmaceutical composition and process thereof |
| US9333215B2 (en) | 2006-05-22 | 2016-05-10 | Li Fu | Aqueous solution of 20(R)-ginsenoside RG3 pharmaceutical composition and process thereof |
| CN103845280A (en) * | 2012-11-30 | 2014-06-11 | 富力 | 20(R)-ginsenoside Rg3 preparation for external use, preparing method thereof and applications thereof |
| CN104643058A (en) * | 2013-11-21 | 2015-05-27 | 富力 | Application of 20(R)-ginsenoside Rg3 in preparation of medicines for improving or/and treating liver cirrhosis diseases |
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