CN101530453B - Method for preparing pterocarpus santalinus water extract used as direct vasodilation agent and applications of method - Google Patents
Method for preparing pterocarpus santalinus water extract used as direct vasodilation agent and applications of method Download PDFInfo
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- CN101530453B CN101530453B CN 200810084964 CN200810084964A CN101530453B CN 101530453 B CN101530453 B CN 101530453B CN 200810084964 CN200810084964 CN 200810084964 CN 200810084964 A CN200810084964 A CN 200810084964A CN 101530453 B CN101530453 B CN 101530453B
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Abstract
The invention relates to a method for preparing pterocarpus santalinus water extract used as a non-endothelium-dependent vasodilation agent and applications of the extract on the medicines or health products of non-endothelium-dependent vasodilation agent. The preparation method comprises the steps of extracting the pterocarpus santalinus powders thrice by 70% of water circumfluence of 6 times, 5 times and 3 times respectively for 2.5h, 2h and 1.5h, decompressing, concentrating, cooling and drying the extract, and finally obtaining the pterocarpus santalinus extract. Suitable auxiliary material is added into the obtained pterocarpus santalinus extract so as to prepare the medicines or health products such as powder injection, drops, troche, capsule, oral liquid, grain agents and the like.
Description
Technical field
The present invention relates to a kind of red sandalwood water extract as direct vasodilation, and this extract is in the medicine of the cardiovascular disease such as treatment hypertension or the application in the health product.
Background technology
Present stage is treated hypertensive vasodilation two large classes.One class is indirect vasodilator smooth muscle, comprises α receptor blocking agent, calcium antagonist and angiotensin converting enzyme inhibitor, is called indirect vasodilation.The another kind of vascular smooth muscle that directly acts on causes vasodilation, is called direct vasodilation.Vasodilation is the present clinically Novel blood pressure-reducing medicine of extensive use indirectly.And direct vasodilation especially extracts the vasodilation that obtains with natural drug, at present very rare also clinically.
The botanical term of " Lignum pterocarpi indici " is red sandalwood, is the pulse family Pterocarpus.Latin is called Pterocarpus santalinus L.F, and commodity are called red sanders, red sandal-wood.
Its timber can make body shrink, and augments and diaphoresis.The timber of pasty state is as cold therapy inflammation and headache.It is said that this is to help treat depression and dermatosis.The medicine of enduring out is as astringent cardiac tonic chronic dysentery bark powder gruel, is to be used for the treatment of diarrhoea.Drink and Lignum pterocarpi indici water every day be used for the treatment of diabetes twice.The locality is also referred to as rakthachandan.Other are with timber and the bark of generic, and Pterocarpus marsupium Roxb. P.marsupium is on record hypoglycemic activity.
Li Shizhen (1518-1593 A.D.) Compendium of Material Medica our department of the Ming Dynasty the 34 volume is said: " Lignum pterocarpi indici-one-tenth is slightly cold, and is nontoxic, energy and ying-qi detumescence poison.Available this sawdust is fried in shallow oil water and is smeared the affected part; And have relax through invigorate blood circulation, blood circulation promoting and antihypertensive effect.
But present stage is treated hypertensive medicine or health product with the red sandalwood water extract as vasodilation, yet there are no report.
Summary of the invention
1. the present invention has confirmed that the Lignum pterocarpi indici extract to the dilating effect without interior cutaneous vessel, has great clinical meaning to Cardiovarscular.
2. the present invention can obtain by following method: with the water reflux, extract, of 6 times, 5 times and 3 times three times, each time is respectively 2.5h, 2h and 1.5h respectively, concentrating under reduced pressure, and cool drying gets the Lignum pterocarpi indici extract.
3. the invention provides the Lignum pterocarpi indici extract and can make effective dosage of expanding without interior cutaneous vessel.
4. the Lignum pterocarpi indici extract among the present invention can be mixed and made into preparation mutually with pharmaceutically acceptable excipient, carrier, buffer agent and/or stabilizing agent.Comprise peroral dosage form, tablet, capsule, oral liquid, granule etc. are arranged, and injection type, injection and powder ampoule agent for injection etc. are arranged.
5. the invention provides the Lignum pterocarpi indici extract and can make route of administration without interior cutaneous vessel expansion, can be oral, injection or other approach.
6. the Lignum pterocarpi indici among the present invention is red sandalwood, India Lignum pterocarpi indici, Pterocarpus marsupium Roxb. or kiaat.
7. the invention provides medicine or the application of health product in treatment hypertension, coronary heart disease, apoplexy and myocardial infarction of the preparation of Lignum pterocarpi indici extract
The specific embodiment
Embodiment 1: the vasoconstrictor effects test method of the inhibition phyenlephrinium that the non-endothelium of the water extract of Lignum pterocarpi indici relies on:
The chest large artery trunks ring of mouse is adopted by present test.To prepare thing normal saline solution oxidation, then mix with following synthetic: 1. sodium chloride (119); 2. potassium chloride (4.7); 3. potassium dihydrogen phosphate (1.2); 4. magnesium sulfate (1.2); 5. sodium bicarbonate (25); 6. calcium chloride (1.6); 7. glucose (11) keeps 4 degrees centigrade temperature.Prepare two radicular arteries rings (every long 4 millimeters), remove endothelium, it is inner surperficial to rub gently with a smooth waddy, successfully removes interior micromicro and confirms by following method: large artery trunks ring and phyenlephrinium (1 μ M) lack the lax reaction to acetylcholine when meeting.The isometric stretching that the myograph system that processes with computer records the large artery trunks ring.After the balance through 90 minutes preloading of at least 1.5 grams (this is preloading best in our the previous test), twice challenge that arterial ring faces 60 milliliters potassium chloride in 30 minutes interval is to set up a contractile reaction baseline.
The contractility curve of the dependence concentration of the accumulation of vascular is also compressed, and the inhibitory action of the water extract of Lignum pterocarpi indici (15 mg/ml) can be prepared to test out by previous 30 minutes processing.The Lignum pterocarpi indici water extract significantly suppress vasoconstriction by suppressing phyenlephrinium.
Result of the test:
1, when phyenlephrinium is 10-5mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 120% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 40% of shrinkage degree that 60mM potassium chloride produces.
2, when phyenlephrinium is 10-6mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 110% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 38% of shrinkage degree that 60mM potassium chloride produces.
3, when phyenlephrinium is 10-7mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 80% of shrinkage degree that 60mM potassium chloride produces.And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 23% of shrinkage degree that 60mM potassium chloride produces.
4, when phyenlephrinium is 10-8mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 30% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 15% of shrinkage degree that 60mM potassium chloride produces.
5, when phyenlephrinium is 10-9mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 10% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 0% of shrinkage degree that 60mM potassium chloride produces.
Embodiment 2: the vasoconstrictor effects test method of the inhibition dopamine that the non-endothelium of the water extract of Lignum pterocarpi indici relies on:
The chest large artery trunks ring of mouse is adopted by present test.To prepare thing normal saline solution oxidation, then mix with following synthetic: 1. sodium chloride (119); 2. potassium chloride (4.7); 3. potassium dihydrogen phosphate (1.2); 4. magnesium sulfate (1.2); 5. sodium bicarbonate (25); 6. calcium chloride (1.6); 7. glucose (11) keeps 4 degrees centigrade temperature.Prepare two radicular arteries rings (every long 4 millimeters), remove endothelium, it is inner surperficial to rub gently with a smooth waddy, successfully removes interior micromicro and confirms by following method: large artery trunks ring and phyenlephrinium (1 μ M) lack the lax reaction to acetylcholine when meeting.The isometric stretching that the myograph system that processes with computer records the large artery trunks ring.After the balance through 90 minutes preloading of at least 1.5 grams (this is preloading best in our the previous test), twice challenge that arterial ring faces 60 milliliters potassium chloride in 30 minutes interval is to set up a contractile reaction baseline.
The contractility curve of the dependence concentration of the accumulation of vascular is also compressed, and the inhibitory action of the water extract of Lignum pterocarpi indici (15 mg/ml) can be prepared to test out by previous 30 minutes processing.The Lignum pterocarpi indici water extract significantly suppress vasoconstriction by suppressing dopamine.
Result of the test:
1, when dopamine is 10-3mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 105% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 15% of shrinkage degree that 60mM potassium chloride produces.
2, when dopamine is 10-4mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 90% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 20% of shrinkage degree that 60mM potassium chloride produces.
3, when dopamine is 10-5mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 80% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 18% of shrinkage degree that 60mM potassium chloride produces.
4, when dopamine is 10-6mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 30% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 5% of shrinkage degree that 60mM potassium chloride produces.
5, when dopamine is 10-7mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 5% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 0% of shrinkage degree that 60mM potassium chloride produces.
Embodiment 3: the vasoconstrictor effects of the varies in the inhibition blood that the non-endothelium of the water extract of Lignum pterocarpi indici relies on
Test method:
The chest large artery trunks ring of mouse is adopted by present test.To prepare thing normal saline solution oxidation, then mix with following synthetic: 1. sodium chloride (119); 2. potassium chloride (4.7); 3. potassium dihydrogen phosphate (1.2); 4. magnesium sulfate (1.2); 5. sodium bicarbonate (25); 6. calcium chloride (1.6); 7. glucose (11) keeps 4 degrees centigrade temperature.Prepare two radicular arteries rings (every long 4 millimeters), remove endothelium, it is inner surperficial to rub gently with a smooth waddy, successfully removes interior micromicro and confirms by following method: large artery trunks ring and phyenlephrinium (1 μ M) lack the lax reaction to acetylcholine when meeting.The isometric stretching that the myograph system that processes with computer records the large artery trunks ring.After the balance through 90 minutes preloading of at least 1.5 grams (this is preloading best in our the previous test), twice challenge that arterial ring faces 60 milliliters potassium chloride in 30 minutes interval is to set up a contractile reaction baseline.
The contractility curve of the dependence concentration of the accumulation of vascular is also compressed, and the inhibitory action of the water extract of Lignum pterocarpi indici (15 mg/ml) can be prepared to test out by previous 30 minutes processing.The obvious of Lignum pterocarpi indici water extract suppresses vasoconstriction by the varies that suppresses in the blood.
Result of the test:
When 1, the varies in blood is 10-4mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 125% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 75% of shrinkage degree that 60mM potassium chloride produces.
When 2, the varies in blood is 10-5mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 105% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 70% of shrinkage degree that 60mM potassium chloride produces.
When 3, the varies in blood is 10-6mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 55% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 15% of shrinkage degree that 60mM potassium chloride produces.
When 4, the varies in blood is 10-7mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 25% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 0% of shrinkage degree that 60mM potassium chloride produces.
When 5, the varies in blood is 10-8mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 10% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 0% of shrinkage degree that 60mM potassium chloride produces.
Embodiment 4: the vasoconstrictor effects of the inhibition dinoprost that the non-endothelium of the water extract of Lignum pterocarpi indici relies on
Test method:
The chest large artery trunks ring of mouse is adopted by present test.To prepare thing normal saline solution oxidation, then mix with following synthetic: 1. sodium chloride (119); 2. potassium chloride (4.7); 3. potassium dihydrogen phosphate (1.2); 4. magnesium sulfate (1.2); 5. sodium bicarbonate (25); 6. calcium chloride (1.6); 7. glucose (11) keeps 4 degrees centigrade temperature.Prepare two radicular arteries rings (every long 4 millimeters), remove endothelium, it is inner surperficial to rub gently with a smooth waddy, successfully removes interior micromicro and confirms by following method: large artery trunks ring and phyenlephrinium (1 μ M) lack the lax reaction to acetylcholine when meeting.The isometric stretching that the myograph system that processes with computer records the large artery trunks ring.After the balance through 90 minutes preloading of at least 1.5 grams (this is preloading best in our the previous test), twice challenge that arterial ring faces 60 milliliters potassium chloride in 30 minutes interval is to set up a contractile reaction baseline.
The contractility curve of the dependence concentration of the accumulation of vascular is also compressed, and the inhibitory action of the water extract of Lignum pterocarpi indici (15 mg/ml) can be prepared to test out by previous 30 minutes processing.The Lignum pterocarpi indici water extract significantly suppress vasoconstriction by suppressing dinoprost.
Result of the test:
1, when dinoprost is 10-5mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 130% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 25% of shrinkage degree that 60mM potassium chloride produces.
2, when dinoprost is 10-6mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 59% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 2% of shrinkage degree that 60mM potassium chloride produces.
3, when dinoprost is 10-7mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 30% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 0% of shrinkage degree that 60mM potassium chloride produces.
4, when dinoprost is 10-8mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 5% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 0% of shrinkage degree that 60mM potassium chloride produces.
5, when dinoprost is 10-9mol/L dosage, produce contractile response, do not use pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 3% of shrinkage degree that 60mM potassium chloride produces.
And with pterocarpus santalinus water extract pretreated without the endothelium aortic annulus, the contractile response of generation is equivalent to 0% of shrinkage degree that 60mM potassium chloride produces.
Claims (7)
1. Lignum pterocarpi indici or its belong to extract and the application in the direct vasodilation of preparation of the acceptable excipient of pharmacy, carrier, buffer agent and/or stabilizing agent of thing together, and wherein, extracting the used solvent of Lignum pterocarpi indici is water.
2. application as claimed in claim 1 is characterized in that, describedly belongs to all floristics that thing is the pulse family Pterocarpus together, and described floristics comprises India Lignum pterocarpi indici, Pterocarpus marsupium Roxb., kiaat.
3. application as claimed in claim 1 is characterized in that, the dosage form of described medicine adopts any dosage form of approving on the pharmaceutics.
4. such as each described application of claim 1～3, it is characterized in that described Lignum pterocarpi indici or its of being applied as belongs to the water extract of thing together as the application of unique active component in preparation treatment hypertension drug.
5. such as each described application of claim 1～3, it is characterized in that described Lignum pterocarpi indici or its of being applied as belongs to the water extract of thing together as the application of unique active component in preparation treatment medicaments for coronary disease.
6. such as each described application of claim 1～3, it is characterized in that described Lignum pterocarpi indici or its of being applied as belongs to the water extract of thing together as the application of unique active component in preparation prevention and treatment apoplexy medicine.
7. such as each described application of claim 1～3, it is characterized in that: described Lignum pterocarpi indici or its of being applied as belongs to the water extract of thing together as the application of unique active component at preparation prevention and treatment myocardial infarction Chinese medicine.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200810084964 CN101530453B (en) | 2008-03-11 | 2008-03-11 | Method for preparing pterocarpus santalinus water extract used as direct vasodilation agent and applications of method |
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| CN 200810084964 CN101530453B (en) | 2008-03-11 | 2008-03-11 | Method for preparing pterocarpus santalinus water extract used as direct vasodilation agent and applications of method |
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| CN101530453A CN101530453A (en) | 2009-09-16 |
| CN101530453B true CN101530453B (en) | 2013-03-27 |
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| CN 200810084964 Expired - Fee Related CN101530453B (en) | 2008-03-11 | 2008-03-11 | Method for preparing pterocarpus santalinus water extract used as direct vasodilation agent and applications of method |
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- 2008-03-11 CN CN 200810084964 patent/CN101530453B/en not_active Expired - Fee Related
Non-Patent Citations (2)
| Title |
|---|
| B. Kameswara Rao，et al.Effect of oral administration of bark extracts of Pterocarpus santalinus L. on blood glucose level in experimental animals.《Journal of Ethnopharmacology》.2001,第74卷69-74. * |
| 王玉芹摘.紫檀茎皮提取物对实验动物血糖水平的影响.《国外医药.植物药分册》.2002,第17卷(第1期),25. * |
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Inventor after: Chen Lihua Inventor after: Friede Murad Inventor after: Chen Zhenxing Inventor after: Zhao Yong Inventor before: Chen Lihua Inventor before: Friede Murad Inventor before: Bian *ka Inventor before: Chen Zhenxing Inventor before: Zhao Yong |
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