CN101040901A - Rosmarinus officinalis extract and its preparing process and application - Google Patents
Rosmarinus officinalis extract and its preparing process and application Download PDFInfo
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- CN101040901A CN101040901A CN 200710065802 CN200710065802A CN101040901A CN 101040901 A CN101040901 A CN 101040901A CN 200710065802 CN200710065802 CN 200710065802 CN 200710065802 A CN200710065802 A CN 200710065802A CN 101040901 A CN101040901 A CN 101040901A
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Abstract
The invention relates to a Rosmarinus officinalis extract, its preparing process and use, wherein the active constituents of the extract include carnosic acid 15-40%, carnosol 5-12% and ursolic acid 14-35%. The preparing process comprises drying the Rosmarinus officinalisl medicinal material in shade, cutting into chunks, charging solvent for extracting, cooling down the merged filtrate and filtrating, decolorizing with activated charcoal, drying and disintegrating. The extract can be used for preparing medicament for treating ischemic cardiovascular and cerebrovascular diseases.
Description
Technical field
The present invention relates to Herba Rosmarini Officinalis extract in application for the treatment of cardiac and cerebral vascular diseases and preparation method thereof.
Background technology
Cardiovascular and cerebrovascular disease has become worldwide one " modern popular disease " at present, and its M ﹠ M trend of rising mouth benefit is obvious, and the level of preventing and treating that improves cardiovascular and cerebrovascular disease is imperative.Along with the development of modern medicine, aspects such as the control of cardiovascular and cerebrovascular disease, diagnosis and treatment have all obtained certain progress.But because cardiovascular and cerebrovascular disease sickness rate height, cure rate is low, and complication is many, has brought certain difficulty for the preventing and controlling of cardiovascular and cerebrovascular disease.Traditional medicine and modern pharmacology show that a lot of Chinese medicines all have the effect of blood circulation promoting and blood stasis dispelling, good effect, and active strong, the characteristics that side effect is little have caused the concern of the world of medicine.
Herba Rosmarini Officinalis is a Labiatae Rosmarinus plant, and famous " dew of ocean " etc. is English by name: Rosemary, originate in Mediterranean Region, and be evergreen shrubs.All there is plantation in many areas, the whole world now.It is drought-enduring avoids waterlogging, likes the warm and humid climate environment.It is not tight to the requirement of soil, and adaptability is strong, but well reaches and slightly plant on the basic soil with dry, draining.At present, China just extensively plants, and cultivates successfully as ground such as Yunnan, Guizhou, Guangxi, Hainan and Xinjiang large tracts of land.Herba Rosmarini Officinalis mainly utilizes the position to be aerial parts, and to gather before the florescence to good, it is microscler, green that leaf is, and fragrant odour is rich in volatile oil in the former medicine leaf.Mainly containing terpenoid, flavonoid and a small amount of organic acid in the Herba Rosmarini Officinalis medical material becomes to grade.Herba Rosmarini Officinalis research emphasis in the past concentrates on antioxidant and the quintessence oil, and does not appear in the newspapers in the application aspect prevention and the treatment cardiovascular and cerebrovascular disease.
Summary of the invention
The purpose of this invention is to provide Herba Rosmarini Officinalis medical material effective site and preparation method thereof, and the application of Herba Rosmarini Officinalis effective site aspect prevention and treatment cardiovascular and cerebrovascular disease.
Herba Rosmarini Officinalis effective site active component provided by the invention is mainly by containing 15%～40% carnosic acid, 5%～12% carnosol and 14%～35% ursolic acid.
Herba Rosmarini Officinalis of the present invention the preparation method of effective site as follows:
1) pretreatment: the Herba Rosmarini Officinalis medical material after will gathering dry in the shade (drying) back cutting, the Herba Rosmarini Officinalis raw medicinal herbs that obtains is standby;
2) extract: the extracting solution that adds 5～12 times of crude drug amounts extracts each 1～3 hour 2～5 times; The extracting solution that merges is several times cooled to 20～60 ℃, remove by filter insoluble matter, the extraction filtrate of the green that obtains;
3) decolouring: extract filtrate at normal temperatures, by activated active carbon or kieselguhr or the kaolinic pillar that extracts amount of filtrate 0.04～10% is housed; Perhaps in extracting filtrate, add activated active carbon or kieselguhr or the kaolin that extracts amount of filtrate 0.05～20%, under 50 ℃, to stir 15～30 minutes, used decolorizing adsorbent is taken out in filtered while hot or centrifugalize, after decolouring, clarified, the medicinal liquid of transparent rufous;
4) concentrate: above-mentioned medicinal liquid is concentrated into dried, obtain after the pulverizing pale yellow powder Herba Rosmarini Officinalis effective site.
2) extracting solution described in the step is a kind of of ethanol, methanol of chloroform, dichloromethane, acetone, ethyl acetate, ether and different water cut concentration etc.
Herba Rosmarini Officinalis provided by the invention effective site can make various oral formulations and other pharmaceutical dosage forms; acute cerebral ischemia there is significant protective effect; can be made into the prevention and the medicine of ischemic cardio cerebrovascular diseases; can remove free radical, anticoagulant and thrombosis; ischemic diseasess such as ischemia apoplexy concurrent (apoplexy) and apoplexy sequela to angina pectoris, coronary heart disease, hypertension, arteriosclerosis etc. have a good curing effect; can be used for preventing senile dementia equally, have antidotal effect.
Below be Herba Rosmarini Officinalis effective site pharmacology, pharmacodynamic experiment result of study:
1) to the influence of MCAO rat delayed ischemic neurological deficits and cerebral infarction scope: after the rat MCAO modeling, the dyskinesia in various degree occurs, model group is compared significant difference with sham operated rats; In the Herba Rosmarini Officinalis effective site dosage group after surgery 6h, three dosage groups after surgery 24h can significantly improve the delayed ischemic neurological deficits of rat model.After the rat MCAO modeling, obviously infraction appears in ishemic part, and the brain coefficient has increase trend; Three dosage of Herba Rosmarini Officinalis effective site and positive control Herba Erigerontis tablet, nimodipine group all can obviously alleviate the cerebral infarction scope of rat model, but the brain coefficient not had obvious influence.
2) to the influence of inductive MCAO rat platelet aggregation of ADP and blood coagulation: after the rat MCAO modeling, platelet aggregation rate is compared with sham operated rats to some extent to be increased, and fibrinogen content has increase trend, and each administration group is compared with model group and be there is no significant difference.
3) to the influence of MCAO rat blood serum zymetology: model group rat blood serum AST and LDH activity are higher than sham operated rats, three dosage groups of Herba Rosmarini Officinalis effective site and positive control Herba Erigerontis tablet can significantly reduce the release of modeling rat LDH, and wherein Herba Rosmarini Officinalis effective site low dose group can also significantly reduce the AST activity.
4) to the influence of mice broken end cerebral hypoxia ischemia: Herba Rosmarini Officinalis effective site three dosage groups and positive control nimodipine group can obviously increase the number of times of panting of dehiscing of acute broken end cerebral ischemia mice; Nimodipine, Herba Erigerontis tablet, Herba Rosmarini Officinalis effective site 40mg/kg can also the significant prolongation decapitated mice dehisce the time of panting, all the other each groups only have effect trend and no difference of science of statistics.
5) influence that the mice thrombus in vivo is formed: mouse tail vein injection collagen and adrenalin derivant can activate thing hemiplegia and death because of thrombus in vivo forms; Herba Erigerontis tablet, three dosage groups of Herba Rosmarini Officinalis effective site and positive control ASP group can obviously reduce the animal dead rate due to the collagen and adrenalin, show the mice thrombus in vivo is formed with obvious inhibitory action.The anti-thrombosis function of Herba Rosmarini Officinalis effective site is better than Herba Erigerontis tablet 40mg/kg group.
6) acute toxicity testing result: the animal that takes off cervical vertebra execution after the observation period end is carried out gross anatomy observe, equal Non Apparent Abnormalities such as the volume of each tissue and organ, color, quality.
This research selects that ferric chloride causes the focal cerebral ischemia in rats model, the mice thrombus in vivo forms and the test of broken end cerebral hypoxia ischemia, observe with Herba Rosmarini Officinalis effective site relatively to the influence of ischemic cardio cerebrovascular diseases.The result shows that Herba Rosmarini Officinalis effective site can significantly be improved the delayed ischemic neurological deficits of MACO rat model, alleviates the cerebral infarction scope, reduces the release of LDH; Herba Rosmarini Officinalis effective site can reduce obviously all that thrombus in vivo forms mortality of mice due to the collagen and adrenalin, the dehisce time of panting and the increase that obviously the prolongs acute broken end cerebral ischemia mice number of times of panting of dehiscing.Result of study prompting Herba Rosmarini Officinalis effective site can make various oral formulations and other pharmaceutical dosage forms have significant protective effect to acute cerebral ischemia.
The technological process that preparation method of the present invention is simple to operate, yield is high, quality is good, production cost is low, and be detection method with HPLC, with carnosic acid, carnosol and content of ursolic acid serves as to detect index, can carry out quality control to whole process flow effectively.This method is suitable for suitability for industrialized production.
Description of drawings
Fig. 1 is that the high performance liquid chromatogram of Herba Rosmarini Officinalis effective site of the present invention detects collection of illustrative plates.Wherein peak 1 is a carnosol, and peak 2 is a carnosic acid, and peak 3 is a ursolic acid.
The specific embodiment
Embodiment 1:
The preparation of Herba Rosmarini Officinalis effective site: cutting after the Herba Rosmarini Officinalis medical material after will gathering dries in the shade, the ethyl acetate backflow that adds 10 times of crude drugs is extracted each 3 hours 2 times; The extracting solution that merges is cooled to 60 ℃, remove by filter insoluble matter, obtain the filtrate of green and brown color; Be concentrated into driedly, pulverize, obtain Herba Rosmarini Officinalis effective site of the present invention, it is the pistac powder, and yield is 11～14%.Wherein carnosic acid content is 22～26%, and carnosol content is 6～9%, and ursolic acid content is 23～27%.Shown in the detection collection of illustrative plates of the HPLC of Fig. 1.
Embodiment 2:
The preparation of Herba Rosmarini Officinalis effective site: cutting after the Herba Rosmarini Officinalis medical material after will gathering dries in the shade, the chloroform reflux, extract, of 12 times of crude drugs of adding 3 times, each 2 hours; The extracting solution that merges is cooled to 20 ℃, and the pillar of adorning by the activated active carbon that extracts amount of filtrate 0.1% (in 0.04～10% all can) is at normal temperatures clarified, the medicinal liquid of transparent rufous; Concentrated medicament is pulverized to doing, and obtains Herba Rosmarini Officinalis effective site of the present invention, and it is a pale yellow powder, yield 10～12%, and carnosic acid content is 21～25%, carnosol content 6～9%, ursolic acid 23～28%.
Embodiment 3:
The preparation of Herba Rosmarini Officinalis effective site: cutting after the Herba Rosmarini Officinalis medical material after will gathering dries in the shade, the acetone reflux, extract, of 8 times of crude drugs of adding 5 times, each 1 hour; The extracting solution that merges is cooled to 40 ℃, in extracting filtrate, add the activated active carbon (or kieselguhr or kaolin) that extracts liquid measure 10% (in 0.05～20% all can), under 50 ℃, stirred 15～30 minutes, used decolorizing adsorbent is taken out in filtered while hot or centrifugalize, after decolouring, clarified, the medicinal liquid of transparent rufous; Concentrated medicament is pulverized to doing, and obtains Herba Rosmarini Officinalis effective site of the present invention, and it is a pale yellow powder, and carnosic acid content is 21～25%, carnosol content 5～10%, ursolic acid 24～28%.
Embodiment 4:
The preparation of Herba Rosmarini Officinalis effective site: with organic solvent extraction Herba Rosmarini Officinalis effective sites such as dichloromethane or ether, method is the same, equally also can obtain mainly to contain the effective site of carnosic acid, ursolic acid, carnosol.
Claims (5)
1, a kind of Herba Rosmarini Officinalis effective site is characterized in that this extract active component mainly contains 15%～40% carnosic acid, 5%～12% carnosol and 14%～35% ursolic acid.
2, the preparation method of the described Herba Rosmarini Officinalis effective site of claim 1 is characterized in that carrying out according to the following steps:
1) pretreatment: cutting behind the Herba Rosmarini Officinalis medicinal material drying after will gathering, the Herba Rosmarini Officinalis crude drug that obtains is standby;
2) extract: the extracting solution that adds 5～12 times of crude drug amounts extracts 2～5 times, and each 1～3 hour, the extracting solution that merges is cooled to 20～60 ℃, remove by filter insoluble matter, obtain the filtrate of green and brown color;
3) drying: with step 2) filtrate that obtains be concentrated into dried, pulverize obtain Herba Rosmarini Officinalis effective site.
3, the preparation method of Herba Rosmarini Officinalis effective site according to claim 2, (3) before afterwards to it is characterized in that described processing step (2), increase bleaching process: merge solvent extraction filtrate, make it at normal temperatures, by activated active carbon, kieselguhr or the kaolinic pillar that extracts amount of filtrate 0.04～10% is housed; Perhaps in extracting filtrate, add the activated active carbon or kieselguhr or the kaolin that extract liquid measure 0.05～20%, under 50 ℃, stirred 15～30 minutes, used decolorizing adsorbent is taken out in filtered while hot or centrifugalize, after decolouring, is clarified, the medicinal liquid of transparent rufous.
4, the preparation method of Herba Rosmarini Officinalis effective site according to claim 2 is characterized in that described extracting solution is ethanol, the methanol of chloroform, dichloromethane, acetone, ethyl acetate, ether and different water cut concentration.
5, the described Herba Rosmarini Officinalis effective site of claim 1 application that can make various oral formulations and other pharmaceutical dosage forms, it is characterized in that being applied to the medicine of ischemic cardio cerebrovascular diseases, be used to remove the medicine of ischemic diseasess such as concurrent ischemia apoplexy such as free radical, anticoagulant and thrombosis, angina pectoris, coronary heart disease, hypertension, arteriosclerosis and apoplexy sequela, and can be used for preventing senile dementia, antidotal medicine.
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| CN102171217A (en) * | 2008-09-30 | 2011-08-31 | 帝斯曼知识产权资产管理有限公司 | Method of crystallizing carnosol |
| EP2440222A1 (en) * | 2009-06-12 | 2012-04-18 | Generex Pharmaceuticals, Inc. | Compositions and methods for prevention and treatment of brain diseases and conditions |
| CN102687627A (en) * | 2012-05-21 | 2012-09-26 | 中国科学院植物研究所 | Rosemary harvest method and preparation method of bacteriostatically active extract |
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| CN102861003A (en) * | 2011-07-05 | 2013-01-09 | 周应军 | Application of carnosic acid and its pharmaceutically acceptable salts in preparing medicines for preventing or treating cerebral infarction |
| CN103416165A (en) * | 2012-05-21 | 2013-12-04 | 中国科学院植物研究所 | Method for collecting rosemary and method for preparing rosemary antioxidant extractives |
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| US9950019B2 (en) | 2009-06-12 | 2018-04-24 | Generex Pharmaceuticals, Inc. | Compositions and methods for the prevention and treatment of brain diseases and conditions |
| EP2440222A1 (en) * | 2009-06-12 | 2012-04-18 | Generex Pharmaceuticals, Inc. | Compositions and methods for prevention and treatment of brain diseases and conditions |
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