CN101623294B - Composition for reducing blood pressure - Google Patents
Composition for reducing blood pressure Download PDFInfo
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- CN101623294B CN101623294B CN2009100130254A CN200910013025A CN101623294B CN 101623294 B CN101623294 B CN 101623294B CN 2009100130254 A CN2009100130254 A CN 2009100130254A CN 200910013025 A CN200910013025 A CN 200910013025A CN 101623294 B CN101623294 B CN 101623294B
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- berberine
- gastrodine
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- pressure lowering
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Abstract
The invention relates to a compound hypotensive preparation formed by raw medicines of berberine and gastrodin. The research of the invention proves that the combination of the berberine and the gastrodin has the blood pressure reduction effect which is obviously better than that of the berberine or the gastrodin which is singly used.
Description
Technical field
The present invention relates to a kind of blood pressure lowering composition, be specifically related to a kind of blood pressure lowering composition of forming by plant extract composition gastrodine and berberine, be field of pharmaceutical preparations.
Background technology
The Gastrodia orchid; it is the rare medicinal herbs of China; its property suffering; temperature; nontoxic; the function that suppressing the hyperactive liver to relieve the wind syndrome is arranged; be usually used in headache; dizzy; diseases such as body numbness; its chemical constituent has gastrodine; gastrodia elata genin; vanillyl alcohol; gastrodioside; hydroxy benzaldehyde; citric acid; succinic acid etc.; wherein the effective monomer component that active component content is the highest is a gastrodine; has multiple pharmacologically active; as has a tranquilizing soporific; convulsion; analgesia; the damage of protection anoxia brain cell; reduce peripheral vascular resistance etc., be commonly used to treat dizzy clinically; headache; the neurasthenia; diseases such as epilepsy also can be used to treat high blood pressure disease.
Berberine another name berberine, it is the alkaloid that from vegetable drugs such as plant Rhizoma Coptidis, Cortex Phellodendri, extracts, but also synthetic, berberine is a kind of spectrum antibiotic, inhibited to Gram-positive, negative bacterium, clinically commonly used advocate infections, a binding film inflammation etc., share, can strengthen other antibiotic antibacterial effect with some other antibiotic such as cyclosporin, fluoroquinolones, trimethoprim etc. with treatment.In recent years, more deep discovers, berberine also has blood pressure lowering, blood sugar lowering, arrhythmia, multiple new purposes such as anticancer, especially aspect cardiovascular, have special advantages, can be in order to heart failure, arrhythmia, treatment of diseases such as hypertension, hyperlipemia.
For the drug combination of the two, yet there are no the correlational study data.
Summary of the invention
The object of the present invention is to provide a kind of compound blood pressure reducing compositions of forming by berberine and gastrodine.
Research worker of the present invention combines use discovering through handsome choosing of a large amount of prescriptions and external pharmacology pharmacy with berberine and gastrodine, can play collaborative enhanced effect aspect blood pressure lowering.
Among the present invention, the two weight proportion of berberine and gastrodine is 2: 1～8: 1, is preferably 3: 1～5: 1.
Among the present invention, used berberine can be the berberine of synthetic, also can be from plants such as Rhizoma Coptidis, Cortex Phellodendri, Radix Berberidis, extract and natural berberine, in addition, can also be the extract that is rich in berberine that extracts from plant, wherein the weight percentage of berberine should be not less than 80% in the extract.
Among the present invention, used gastrodine can be the gastrodine of synthetic, also can be from the plant Rhizoma Gastrodiae, to extract and the gastrodine monomer component that obtains, certainly, can also be from the plant Rhizoma Gastrodiae, extract and the effective site that is rich in gastrodine and gastrodia elata genin, in this effective site, the weight percentage of gastrodine should be not less than 80%.
Among the present invention, used raw material berberine and gastrodine can be commercially available, also can be oneself refining or synthetic processing, and the method for preparation is not subjected to not invent restriction, so long as final raw material can obtain berberine, gastrodine just can; When extracting effective site, its method is not limit yet, and the weight percentage that in the final extract, the weight percentage that the berberine extract can reach berberine is not less than 80%, can reach gastrodine in the gastrodine extract is not less than 80% and gets final product.
Among the present invention, used gastrodine also can replace through the hydrolyzed product gastrodia elata genin with gastrodine.
Among the present invention, the preparation that contains crude drug berberine and gastrodine, can be according to different clinically needs, add acceptable proper supplementary material in the pharmacy, make needed preparation, as being oral formulations, also can be injection preparation, can also be percutaneous drug administration preparation, through duodenal administration preparation etc.
The preparation of oral administration mode can be tablet, capsule, pill or granule, and wherein tablet can be common plain sheet, also can be coated tablet, and coating can wrap with enteric coating, gastric solubleness clothing, extended release coatings, controlled release clothing etc.
Injection preparation can be injection liquid drugs injection, transfusion or powder pin; Percutaneous drug administration preparation can be a patch, spray etc.
Specific embodiment
Below from animal pharmacology test embodiment beneficial effect of the present invention is described.
One, to the hypotensive effect of renal hypertensive rat
The test material animal: 70 of healthy Wistar rats, body weight 250 ± 20g, male and female half and half are purchased in Shenyang medical experiment animal center, and licence is good: SCXK-(the Liao Dynasty) 2002-2006.Grouping and medicine: model control group, berberine extract group (is extracted from the plant Rhizoma Coptidis, self-control, 48mg/kg), gastrodine extract group (is extracted from Rhizoma Gastrodiae, self-control, 12mg/kg), present composition high dose group (berberine 48mg/kg+ gastrodine 12mg/kg), middle dosage group (berberine 24mg/kg+ gastrodine 6mg/kg), low dose group (berberine 48mg/kg+ gastrodine 12mg/kg), Captopril group (captopril sheet, Shandong XinHua Pharmacy stock Co., Ltd produces, and every contains captopril 25mg, lot number 20081109).
Test method: modelling: rat is through 1% pentobarbital sodium 30mg/kg intraperitoneal anesthesia, right lateral position is fixed on the Mus platform, the external left kidney of touching, cut off local 3cm * 3cm by hair, the Xiao Du drape, cut skin at palpation kidney and spinal column parallel direction, otch 1.5-2.0cm, successively separate subcutaneous fascia and muscle, push the perinephric fat capsule open with the saline cotton balls, strut with eye speculum and fully appear surgical field of view, the careful renal artery that separates behind peritoneum, trace kidney with finger, check errorless back at the autonomous aortic bifurcation of renal artery place placement standard steel wire, the silver brain clip clamp closes silver brain clip, takes out the standard steel wire then, successively close muscle, skin, preceding 3 standard deviations of postoperative 2 all hypertension Rhizoma Atractylodis Macrocephalae and be higher than 18.7kPa (140mmHg) and be model copy success.
According to above-mentioned grouping scheme and dosage, medicine is with distilled water wiring solution-forming or suspension, and model group gives isopyknic distilled water, continuous official position 15d, every day 1 time.
Blood pressure determination: utilize BP-6 non-invasive blood pressure instrument to adopt the arteria caudalis manometry to measure blood pressure to rat, the systolic pressure of 3d, 6d, 9d, 12d, 15d the results are shown in Table 1 behind the record successive administration.
Table 1 compound recipe of the present invention is to the influence of renal hypertensive rat systolic pressure (mmHg, n=10, x ± s)
Compare with model group,
*P＜0.05,
*P＜0.01; Compare with the gastrodine group,
#P＜0.05
From last table result as can be seen, berberine, gastrodine and berberine and gastrodine combination all have certain hypotensive effect, and the administration bleeding from anus presses off slowly decline of beginning.Compositions is compared with individually dosed, the antihypertensive effect of middle and high dosage group is all strong with berberine, gastrodine than independent, middle and high dosage group obviously is better than gastrodine group (P＜0.05) in the 6th day antihypertensive effect, shows that the two share, and the effect of mutual Synergistic is arranged.
Two, to the hemorheological influence of renal hypertensive rat
To the rat behind the above-mentioned administration 15d, 15d after administration gets blood with rat through the carotid artery intubate, detects hemorheology index in 4h: whole blood viscosity (height cuts, in cut, low cutting) and plasma viscosity.The results are shown in Table 2.
Table 2 compound recipe of the present invention is to the hemorheological influence of renal hypertensive rat (mPa.s, n=10, x ± s)
Compare with model group,
*P＜0.05,
*P＜0.01; Compare with the gastrodine group,
#P＜0.05.
Renal hypertensive rat is after the blood pressure lowering treatment, each dosage group has in various degree improvement effect to the ANOMALOUS VARIATIONS of above-mentioned hemorheological indexes, to hemorheological influence, the middle and high dosage group of compound recipe of the present invention is used the effective of berberine or gastrodine more separately, especially to low influence of cutting index and plasma viscosity index, the middle and high dosage group of drug combination has been compared significant difference (P＜0.05) than the gastrodine group, and uses the effect of berberine also stronger more separately.Point out the two to unite use, collaborative enhanced effect is arranged.
Formulation preparation embodiment
Below illustrate from formulation preparation embodiment and need to prove the preparation of preparation of the present invention that the preparation of enumerating not is a restriction dosage form of the present invention, but in order to say the present invention.
Embodiment 1
The preparation of tablet (1000 tablet recipe)
Berberine 300g, gastrodine 100g, lactose 80g, polyvidone 15g, magnesium stearate 5g, 70% ethanol is an amount of;
Get crude drug and adjuvant, pulverized 100 mesh sieves, berberine, gastrodine, lactose mix homogeneously are adhesive with the polyvidone that is scattered in advance in 70% ethanol, the preparation soft material is crossed the sieve series granule, 60 ℃ of dryings, granulate adds magnesium stearate, is pressed into 1000 promptly.
Embodiment 2
Capsular preparation (1000 capsule prescriptions)
Berberine 400g, gastrodine 50g, starch 50g
Get raw material and adjuvant, pulverize, mix homogeneously is loaded in 1000 hard capsules, promptly gets capsule.
Embodiment 3
The preparation of drop pill
Berberine 20g, gastrodine 5g, drop pill substrate common in the pharmacy is an amount of
With crude drug and drop pill substrate, the preparation technology according to drop pill in the pharmacy makes drop pill.
Embodiment 4
The preparation of injectable powder (1000 powder pin prescriptions)
Berberine 100g, gastrodine 50g, mannitol 150g, water for injection is an amount of
With berberine, gastrodine dissolved in distilled water, add mannitol, stir, be 8000 ultrafilter membrane ultrafiltration with molecular cut off, the collection ultrafiltrate is made powder injection formulation in freeze dryer.
Embodiment 5
The preparation of tablet (1000 tablet recipes, coated tablet)
Berberine 350g, gastrodine 70g, microcrystalline Cellulose 110g, polyvidone 15g, hydroxypropyl emthylcellulose 50g, Pulvis Talci 5g, 70% ethanol is an amount of;
Get crude drug and adjuvant, pulverized 100 mesh sieves, berberine, gastrodine, microcrystalline Cellulose mix homogeneously, with the polyvidone that is scattered in advance in 70% ethanol is adhesive, and the preparation soft material is crossed the sieve series granule, 60 ℃ of dryings, granulate adds Pulvis Talci, mix homogeneously, be pressed into 1000, in addition hydroxypropyl emthylcellulose be dissolved in an amount of ethanol, the sheet that suppresses is put in the coating pan, spray into hydroxypropyl emthylcellulose ethanol liquid coating, promptly.
Embodiment 6
The preparation of tablet (1000 tablet recipes, oral cavity disintegration tablet)
Berberine 350g, gastrodine 50g, microcrystalline Cellulose 70g, crospolyvinylpyrrolidone polyvidone 80g, polyvidone 15g, Pulvis Talci 6g, 70% ethanol is an amount of;
Get crude drug and adjuvant, pulverized 100 mesh sieves, berberine, gastrodine, microcrystalline Cellulose mix homogeneously, with the polyvidone that is scattered in advance in 70% ethanol is adhesive, the preparation soft material is crossed the sieve series granule, 60 ℃ of dryings, granulate, with whole good granule and crospolyvinylpyrrolidone mix homogeneously, add magnesium stearate again, mix homogeneously, be pressed into 1000, promptly get oral cavity disintegration tablet.
Claims (6)
1. a blood pressure lowering composition is characterized in that being made up of crude drug berberine and gastrodine, and the two weight proportion is 2: 1 to 8: 1.
2. blood pressure lowering composition according to claim 1, the weight proportion that it is characterized in that berberine and gastrodine is 3: 1 to 5: 1.
3. blood pressure lowering composition according to claim 1 and 2 is characterized in that described crude drug berberine is the synthetic berberine or extracts purified natural berberine from plant.
4. blood pressure lowering composition according to claim 1 and 2 is characterized in that described crude drug gastrodine extracts the refining natural gastrodine that obtains for artificial synthetic gastrodine or from the plant Rhizoma Gastrodiae.
5. claim 1 or 2 described blood pressure lowering compositions have application in the antihypertensive drugs in preparation.
6. claim 1 or the 2 described blood pressure lowering compositions application in preparation renal hypertension medicine.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009100130254A CN101623294B (en) | 2009-08-10 | 2009-08-10 | Composition for reducing blood pressure |
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| Application Number | Priority Date | Filing Date | Title |
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| CN2009100130254A CN101623294B (en) | 2009-08-10 | 2009-08-10 | Composition for reducing blood pressure |
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| CN101623294A CN101623294A (en) | 2010-01-13 |
| CN101623294B true CN101623294B (en) | 2011-05-04 |
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| CN2009100130254A Active CN101623294B (en) | 2009-08-10 | 2009-08-10 | Composition for reducing blood pressure |
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Effective date of registration: 20200102 Address after: 100124 1605, floor 13, building 3, No. 82, East Fourth Ring Middle Road, Chaoyang District, Beijing Patentee after: Beijing Huayao Kechuang Pharmaceutical Technology Development Co., Ltd Address before: 110179 Liaoning province Shenyang Hunnan New Long Street No. 10-1 Co-patentee before: Guan Yi Patentee before: Shenyang Yiling Medicine Technology Co., Ltd. |
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