CN101028328A - Production and use for kaki-leaf extract - Google Patents
Production and use for kaki-leaf extract Download PDFInfo
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- CN101028328A CN101028328A CN 200710034708 CN200710034708A CN101028328A CN 101028328 A CN101028328 A CN 101028328A CN 200710034708 CN200710034708 CN 200710034708 CN 200710034708 A CN200710034708 A CN 200710034708A CN 101028328 A CN101028328 A CN 101028328A
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- folium kaki
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- total flavones
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Abstract
An extract of persimmon leaf is prepared from persimmon leaf through pulverizing, extracting in water or alcohol, and separating. Said extract along with proper medicinal additives can be used to prepare tablet, mixture, capsule, particle, or injection for decreasing blood pressure and blood fat, and treating arrhythmia, and diabetes and its complications.
Description
Technical field
The present invention relates to the pure natural medical preparation of Folium Kaki extract as active ingredient, with and in the application of treatment hypertension, coronary heart disease, diabetes.
Background technology
Folium Kaki is the fresh or dried leaves of Ebenaceae calamander Fructus Kaki (Diospyros kaki L.).The present invention has carried out a large amount of research to this medicine; experiment is found; the arrhythmia that this product can significantly reduce rat blood pressure, increases coronary flow, impedance causes because of myocardial ischemia; obviously reduce rat fat; the blood glucose of diabetic mice due to sugared effect of the energy adrenergic liter of antagonism and the reduction streptozotocin can also obviously improve the disorderly situation of glycolipid in addition, increases secretion of insulin; protection and repair beta Cell of islet has bigger potential using value to the treatment of diabetes especially complication.
At present, still find no Folium Kaki water extract, ethanol extract, total flavones isoreactivity position are made preparation and be used for clinical report.
Summary of the invention
The objective of the invention is Folium Kaki water extract, ethanol extract are made pharmaceutical preparatioies such as tablet, mixture, capsule, granule, injection, be applied to hypertension, coronary heart disease, treatment of diabetes.
The technical solution used in the present invention:
The Folium Kaki coarse powder is carried out water extraction, alcohol extraction, extraction separation total flavones, add proper pharmaceutical excipients and make tablet, mixture, capsule, granule, injection, and carry out pharmacodynamic study.
1, the extraction of Folium Kaki water extract: the dry coarse powder of Folium Kaki, add 10 times of water gagings, boil 3 times, each 2h collects water cooking liquid, is condensed into thick paste.
2, the extraction of Folium Kaki ethanol extract: the dry coarse powder of Folium Kaki, add 10 times of amount 95% ethanol, reflux, extract, 3 times, each 2h, extracting solution reclaims ethanol, is condensed into thick paste.
3, the extraction separation of Folium Kaki total flavones: the Folium Kaki coarse powder, add 10 times of amount concentration 70% soak with ethanol 30min after, reflux, extract, 2h filters.Medicinal residues add 8 times of amount 70% ethanol again, and reflux, extract, 1h filters.Merge filtrate twice, the centrifugal (15min of 3000 γ/min).After reclaiming ethanol, collect extracting solution, concentrating under reduced pressure is used petroleum ether extraction 2 times, removes chlorophyll, abandons the ether phase, water ethyl acetate extraction 2 times, and combined ethyl acetate phase concentrate drying gets total flavones.
4, the preparation of preparation: Folium Kaki water extract, ethanol extract, total flavones add proper pharmaceutical excipients and make tablet, mixture, capsule, granule, injection.
5, the research of antihypertensive function: measure the influence that Folium Kaki water extract, ethanol extract, total flavones are pressed rat carotid artery with MS4000 bio signal quantified system analysis through the carotid artery intubate; Survey tail arterial blood pressure through gastric infusion with ALC-NIBP noinvasive tail arterial blood pressure measuring and analysis system, observe the influence of Folium Kaki water extract, ethanol extract, total flavones clear-headed rat blood pressure; To left ventricle, and insert right common femoral artery simultaneously from the right carotid intubate, measure the influence of Folium Kaki water extract, ethanol extract, total flavones cardiac hemodynamic indexs such as rat heart rate, myocardiac mechanics and myocardial oxygen need with MPA-cardiac function analytical system.
6, Folium Kaki water extract, ethanol extract, total flavones are to the influence of cardiac hemodynamic and coronary flow: be equipped with isolated rat heart with the Langendorff legal system, observe the myocardial contraction amplitude and also measure coronary flow.
7, Folium Kaki water extract, ethanol extract, total flavones are to the protective effect of rat myocardial ischemia and reperfusion damage: prepare MIRI model (pouring into 30min again behind the ligation coronary artery 5min) with the Wistar rat, observe the influence to lactic acid dehydrogenase (LDH), creatine phosphokinase (CK) active biochemical index in myocardial infarction area and cardiac muscular tissue's malonaldehyde (MDA) content, superoxide dismutase (SOD) vigor and the serum.
8, Folium Kaki is proposed the research of thing, ethanol extract, the effect of flavone in treating diabetes: (Streptozotocin STZ) causes the effect that diabetic mice model method research Folium Kaki water extract, ethanol extract, total flavones reduce hyperglycemia to adopt epinephrine to cause hyperglycemia mouse model and streptozotocin.
The present invention carries out discovery and arrangement to Guangxi national characters natural pharmaceutical resources, will provide new approaches for the deep development of Chinese herbal medicine, is significant to promoting China's Chinese herbal medicine industry modernization.For hypertension, coronary heart disease and treatment of diabetes provide a kind of new natural medicinal formulations.
The specific embodiment
1, the extraction of Folium Kaki water extract: the dry coarse powder of 1000g Folium Kaki, add 10L water, boil 3 times, each 2h collects water cooking liquid, is condensed into thick paste.Add corresponding adjuvant and make tablet, capsule, granule, injection, mixture.
2, the extraction of Folium Kaki ethanol extract: the dry coarse powder of 1000g Folium Kaki, add 10L95% ethanol, reflux, extract, 3 times, each 2h, extracting solution reclaims ethanol, is condensed into thick paste.Add corresponding adjuvant and make tablet, capsule, granule, injection, mixture.
3, the extraction separation of Folium Kaki total flavones: take by weighing Folium Kaki coarse powder 5.0g, after adding 70% ethanol 50ml and soaking 30min, reflux, extract, 2h filters.Medicinal residues add 70% ethanol 40ml again, and reflux, extract, 1h filters.Merge filtrate twice, the centrifugal (15min of 3000 γ/min).After reclaiming ethanol, collect extracting solution, concentrating under reduced pressure is used petroleum ether extraction 2 times, removes chlorophyll, abandons the ether phase, water ethyl acetate extraction 2 times, and combined ethyl acetate phase concentrate drying gets total flavones.Add corresponding adjuvant and make tablet, capsule, granule, injection, mixture.
Pharmacodynamic study
1, the research of antihypertensive function:
1.1 the observation that carotid artery is pressed
The Wistar rat is with urethane (1.2gkg
-1) intraperitoneal anesthesia, tracheal intubation, row carotid artery intubate connects BL bio signal analytical system, and record systolic pressure (SBP), diastolic pressure (DBP), mean pressure (MBP), heart rate (HR) write down limbs II simultaneously and lead the sign electrocardiogram.The femoral vein administration treats all that at every turn blood pressure returns to before the medicine rechallenge behind the horizontal 10min.SBP, DBP, MBP and HR situation of change before and after the record administration.The result shows that Folium Kaki water extract, ethanol extract, total flavones have obvious hypotensive effect through the femoral vein administration, and compares SBP, DBP, MBP before the medicine, and P＜0.05 or P＜0.01 is all arranged.
Table 1 Folium Kaki extract to the influence of Wistar rat blood pressure (x ± s, n=10)
| Group | Dosage | Mean blood pressure (mmHg) before the medicine | Mean blood pressure behind the medicine (mmHg) |
| Blank diltiazem persimmon leaf flavonoids persimmon leaf water extract high dose group low dose group persimmon leaf-alcohol extract high dose group low dose group | - 5mg·kg -1 25g·kg -1 25g·kg -1 12.5g·kg -1 25g·kg -1 12.5g·kg -1 | 121.9±16.9 115.4±14.8 117.7±14.3 119.5±19.2 120.0±10.2 122.3±13.4 116.0±18.7 | 120.0±16.7 96.7±11.2 ** 102.8±15.7 * 98.4±13.7 ** 103.7±10.8 * 99.9±10.7 * 100.7±18.1 * |
Annotate: with comparison before the medicine
*P＜0.05,
*P＜0.01.Flavone, water extract, ethanol extract are respectively organized dosage all with raw medicinal herbs (g crude drug/kg) calculate
1.2SHR the observation that tail is pressed
Measure clear-headed rat tail arterial blood pressure with ALC-NIBP noinvasive tail arterial blood pressure measuring and analysis system, observe administration front and back blood pressure situation.Found that the blood pressure that gives Folium Kaki water extract, ethanol extract, total flavones group rat has obvious decline, 40 days its hypotensive effects of administration are more obvious.
Table 2 Folium Kaki extract to the influence of SHR rat blood pressure (x ± s, n=10)
| Group | Dosage | Mean blood pressure (mmHg) before the medicine | Mean blood pressure behind the medicine (mmHg) |
| Blank diltiazem persimmon leaf flavonoids persimmon leaf water extract high dose group low dose group persimmon leaf-alcohol extract high dose group low dose group | - 5mg·kg -1 25g·kg -1 25g·kg -1 12.5g·kg -1 25g·kg -1 12.5g·kg -1 | 162.3±36.9 154.8±24.6 149.7±31.9 157.5±28.6 148.3±32.2 151.8±33.6 160.7±38.8 | 161.3±29.9 131.2±32.5 ** 133.7±30.5 * 130.8±29.8 ** 133.2±30.3 * 130.3±31.4 ** 150.3±39.9 * |
Annotate: with comparison before the medicine
*P＜0.05,
*P＜0.01.Flavone, water extract, ethanol extract are respectively organized dosage all with raw medicinal herbs (g crude drug/kg) calculate.
2, to the influence of cardiac hemodynamic and coronary flow
2.1 rat heart hemodynamics experiment
The Wistar rat is with 20% urethane 0.5mLkg
-1Intraperitoneal anesthesia, tracheal intubation, go into left ventricle from the right carotid intubate, separate the capable femoral arteriography of femoral artery, connect MPA-cardiac function analytical system, observe 10min, treat stable back recorded heart rate (HR), left ventricular systolic pressure (LVSP), left chamber EDP (LVEDP), left constant pressure rise maximum rate of change (dp/dtmax), left chamber descend maximum rate of change (myocardial contraction and diastole index such as dp/dtmax).From the femoral vein administration, treat all that at every turn blood pressure returns to before the medicine rechallenge behind the horizontal 10min.
The result shows, ((25g crude drug/kg), (dp/dtmax has shown negativity muscular strength and negative chronotropic action to total flavones to the Folium Kaki water extract generally for 25g crude drug/kg) can obviously reduce HR, LVSP for 25g crude drug/kg), ethanol extract.
Table 3 Folium Kaki extract to the hemodynamic influence of rat heart (x ± s, n=10)
| Index (unit) | Normal control | Diltiazem | Water extract | Flavone | Ethanol extract |
| HR(bpm) Lvsp(KPa) Lvedp(KPa) dp/dtmax(KPa.s-1) -dp/dtmax(KPa.s-1) | 389±62.3 18.1±1.48 2.45±0.46 638.9±58.2 -496.2±51.4 | 290±31.1 ** 13.3±1.73 ** 2.53±0.20 386.5±47.6 ** -488.2±38.9 | 340±27.3 * 13.9±1.18 ** 2.47±0.35 412.2±43.2 ** -471.6±50.89 | 346±25.1 * 15.1±1.37 ** 2.49±0.31 428.3±44.3 ** -484.5±11.34 | 339±62.9 * 14.8±1.48 * 2.42±0.22 436.6±26.43 ** -494.7±19.60 |
Annotate: compare with the blank group
*P＜0.05,
*P＜0.01.
2.2 isolated rat heart coronary flow determination experiment
With each isolated rat heart of Langendorff legal system, fix after pressure transducer connects MS4000 multimedia bio signal analytical system, record heart shrinkage amplitude, behind the perfusion 15min, 3 per minute coronary flows of METHOD FOR CONTINUOUS DETERMINATION (CF), the constant back of the value for the treatment of by the tee T administration, is measured administration front and back CF and heart shrinkage amplitude with peristaltic pump.
Found that Folium Kaki water extract, ethanol extract, total flavones can obviously alleviate myocardial ischemia-reperfusion and cause myocardial damage, dwindle myocardial infarct size, reduce MDA content, it is active and reduce the vigor of CK and LDH in the serum to improve SOD in the cardiac muscular tissue.
Table 4 Folium Kaki extract to the influence of rat heart coronary flow (x ± s, n=10)
| Group | Dosage | CF(ml/min) | Raising rate (%) | Myocardial contraction (cm) | Raising rate (%) |
| Normal control group water extract group ethanol extract group total flavones group diltiazem group | - 25g/kg 25g/kg 25g/kg 5mg/kg | 13.0±2.9 17.3±3.2 13.6±3.1 17.5±3.4 | 32.7±6.1 4.5±3.4 35.34±6.6 | 2.5±0.40 1.70±0.20 1.30±0.20 1.70±0.20 | 32.6±7.7 45.6±7.0 32.3±8.4 |
Annotate: compare with the blank group
*P＜0.05,
*P＜0.01.Flavone, water extract, ethanol extract are respectively organized dosage all with raw medicinal herbs (g crude drug/kg) calculate.
3, the protective effect that rat myocardial ischemia and reperfusion is damaged
Each organizes rat with urethane (1.2g/kg) intraperitoneal anesthesia, tracheal intubation, connect artificial respirator immediately after opening breast, it is dirty to core immediately after perfusion finishes again, weigh after freezing, be cut into the thick myocardium sheet of 0.1cm along coronary sulcus from the apex of the heart to heart base portion with ventricle, place 37 ℃ of water-bath temperature of 0.5%NBT solution to incubate 10min dyeing.Cut infarction part cardiac muscle along the infarction edge and weigh, represent myocardial infarct size with the percentage ratio (MI/LV * 100%) that infarcted myocardium and complete left chamber flesh are heavy.
The result shows that Folium Kaki water extract, ethanol extract, total flavones can obviously reduce myocardial infarct size.
4, the research of treatment diabetes effect:
(Streptozotocin STZ) causes the effect that diabetic mice model method research Folium Kaki water extract, ethanol extract, total flavones reduce hyperglycemia to adopt epinephrine to cause hyperglycemia mouse model and streptozotocin.Every morning is administered once, successive administration 15 days.Ordinary circumstances such as observed and recorded mice diet, drinking-water, body weight, defecation during this time, and after corresponding time, fasting glucose (FBG), medicine were measured in blood sampling 2h blood glucose (2hBG), triglyceride (TG), T-CHOL (TC), HDL-C (HDL-C), serum creatinine (Cr), carbamide (BU), uric acid (UA), glutamic oxaloacetic transaminase, GOT (AST), glutamate pyruvate transaminase indexs such as (ALT), and do pancreatic tissue and kidney pathology section examination.The result: administration is after 15 days; Folium Kaki water extract, ethanol extract, each dosage group energy inductive mice hyperglycemia of antagonism epinephrine (P＜0.01 or 0.05) of total flavones; and obviously reduce the blood glucose (P＜0.01 or 0.05) of diabetic mice due to the streptozotocin; improve the glycolipid metabolism disturbance state of diabetic mice; improve insulin level, protection is also repaired beta Cell of islet.Folium Kaki water extract, ethanol extract, total flavones can reduce change of serum C r, UA (P＜0.01 or 0.05) to some extent simultaneously; Rising Alb, TP (P＜0.01 or 0.05); Rising HDL-C and reduction TG, TC, ALT, AST there is certain trend.
Experimental result confirms; the blood glucose of diabetic mice due to Folium Kaki water extract, ethanol extract, the total flavones energy sugared effect of the adrenergic liter of antagonism and the reduction streptozotocin; can also obviously improve the disorderly situation of glycolipid in addition; increase secretion of insulin; protection and repair beta Cell of islet has bigger potential using value to the treatment of diabetes especially complication.
Table 5 Folium Kaki extract to the influence of normal mouse blood sugar (x ± s, n=10)
| Group | Dosage | FBG(mmol/L) |
| Dosage group low dose group in the dosage group low dose group persimmon leaf-alcohol extract high dose group in the blank glibenclamide persimmon leaf flavonoids persimmon leaf water extract high dose group | - 50mg·kg -1 12.5g·kg -1 25g·kg -1 12.5g·kg -1 6.25g·kg -1 25g·kg -1 12.5g·kg -1 6.25g·kg -1 | 5.62±1.12 4.45±0.83 * 5.63±1.08 5.70±1.46 5.71±1.31 5.67±0.70 5.83±2.13 5.79±1.45 5.78±1.27 |
Annotate: compare with the blank group
*P＜0.05,
*P＜0.01.Flavone, water extract, ethanol extract are respectively organized dosage all with raw medicinal herbs (g crude drug/kg) calculate.
Table 6 Folium Kaki extract to the influence of mice adrenal gland disposition hyperglycemia (x ± s, n=10)
| Group | Dosage | Epinephrine (μ g/kg) | Blood glucose (mmol/L) |
| Dosage group low dose group in the dosage group low dose group persimmon leaf-alcohol extract high dose group in the blank model group glibenclamide persimmon leaf flavonoids persimmon leaf water extract high dose group | - - 50mg·kg -1 12.5g·kg -1 25g·kg -1 12.5g·kg -1 6.25g·kg -1 25g·kg -1 12.5g·kg -1 6.25g·kg -1 | 300 300 300 300 300 300 300 300 300 | 5.62±1.12 △△ 19.64±5.46 ** 13.25±2.27 **△ 16.09±3.18 ** 14.97±2.34 ** 15.22±3.06 ** 17.19±2.29 ** 15.06±1.83 ** 16.61±3.10 ** 16.68±3.32 ** |
Annotate: compare with the blank group
*P＜0.05,
*P＜0.01.Flavone, water extract, ethanol extract are respectively organized dosage all with raw medicinal herbs (g crude drug/kg) calculate.
Table 7 Folium Kaki extract to the influence of streptozotocin blood glucose in diabetic mice (x ± s, n=10)
| Group | Dosage mgkg -1 | Blood glucose (mmol/L) before the medicine | The 5th day blood glucose (mmol/L) | The 10th day blood glucose (mmol/L) | The 15th day blood glucose (mmol/L) | The blood sugar lowering rate a (％) |
| Dosage group low dose group in the dosage group low dose group persimmon alcohol extracts from the leaves high dose group in the blank group model group glibenclamide persimmon leaf flavonoids persimmon leaf water extract high dose group | - - 50 12.5 25 12.5 6.25 25 12.5 6.25 | 3.95±0.76 △△ 17.36±2.00 ** 17.72±2.95 ** 19.83±3.53 ** 18.85±4.34 ** 19.21±3.28 ** 19.05±3.02 ** 19.06±4.64 ** 18.82±4.83 ** 19.16±4.42 ** | 4.52±0.84 △△ 17.95±1.64 ** 15.87±2.41 ** 18.09±4.38 ** 16.99±4.44 ** 17.57±3.40 ** 17.19±3.96 ** 17.53±4.82 ** 17.79±3.66 ** 18.35±4.72 ** | 4.51±0.82 △△ 18.91±2.44 ** 14.49±3.53 **△△ 17.69±3.88 ** 15.64±4.29 **△△ 16.85±4.18 ** 16.38±3.27 ** 16.37±4.36 **△ 16.92±4.52 ** 17.55±4.19 ** | 3.84±0.90 △△ 18.98±2.92 ** 12.96±3.13 **△△ 15.74±4.67 **△ 14.25±4.58 **△△ 15.20±3.98 **△ 15.63±3.83 **△ 14.58±4.76 **△△ 15.59±4.13 **△ 16.43±4.92 **△ | 26.86 20.63 24.39 20.86 17.96 23.50 17.16 14.25 |
Annotate: compare with the blank group:
*P＜0.05,
*P＜0.01; Compare with model group:
△P＜0.05,
△ △P＜0.01.
aThe 15th day blood sugar lowering rate.Flavone, water extract, ethanol extract are respectively organized dosage all with raw medicinal herbs (g crude drug/kg) calculate.
Table 8 Folium Kaki extract to streptozotocin diabetic mice medicine after 2h blood glucose influence (x ± s, n=10)
| Group | Dosage | FBG(mmol/L) | 2hBG(mmol/L) | Blood sugar lowering rate (%) |
| Dosage group low dose group in the dosage group low dose group persimmon leaf-alcohol extract high dose group in the blank group model group glibenclamide persimmon leaf flavone persimmon leaf water extract high dose group | - - 50mg·kg -1 12.5g·kg -1 25g·kg -1 12.5g·kg -1 6.25g·kg -1 25g·kg -1 12.5g·kg -1 6.25g·kg -1 | 3.84±0.91 △△ 18.70±3.22 ** 19.08±2.52 ** 18.35±3.27 ** 18.00±2.80 ** 18.35±3.27 ** 17.61±3.82 ** 18.00±2.80 ** 18.35±3.27 ** 17.61±3.82 ** | 4.30±1.50 △△ 21.73±5.32 ** 16.22±2.05 **△△ 17.36±3.19 **△ 16.68±3.28 **△ 17.36±3.19 **△ 16.72±3.73 **△ 16.68±3.28 **△ 17.36±3.19 **△ 16.72±3.73 **△ | 14.97 7.33 5.04 5.40 5.04 5.40 5.04 |
Compare with the blank group:
*P＜0.05,
*P＜0.01; Compare with model group:
△P＜0.05,
△ △P＜0.01.
Table 9 Folium Kaki extract to the influence of streptozotocin diabetic mice serum insulin levels (x ± s, n=10)
| Group | Dosage | Serum insulin (mIU/L) | Raising rate (%) |
| Dosage group low dose group in the dosage group low dose group persimmon leaf-alcohol extract high dose group in the blank model group glibenclamide persimmon leaf flavonoids persimmon leaf water extract high dose group | - - 50mg·kg -1 12.5g·kg -1 25g·kg -1 12.5g·kg -1 6.25g·kg -1 25g·kg -1 12.5g·kg -1 6.25g·kg -1 | 10.42±1.75 ** 4.67±1.53 △△ 6.55±0.93 **△△ 7.04±1.39 **△△ 7.09±1.38 **△△ 7.04±1.39 **△△ 6.33±1.10 **△ 7.09±1.38 **△△ 7.04±1.39 **△△ 6.33±1.10 **△ | 40.30 50.78 51.71 50.78 35.60 51.71 50.78 35.60 |
Compare with the blank group:
*P＜0.05,
*P＜0.01; Compare with model group:
△P＜0.05,
△ △P＜0.01.
Embodiment:
The extraction of embodiment 1, Folium Kaki water extract and the preparation of preparation thereof:
1.1 the preparation of Folium Kaki water extract: get the dry coarse powder 10kg of Folium Kaki, add 100L water, boil 3 times, each 2h filters, and collects water cooking liquid, is condensed into proportion and is 1.3 thick paste.
1.2 system water extract tablet: get the dry coarse powder 10kg of Folium Kaki, prepare thick paste with the 1.1st method, weigh and write down thick paste weight, adds 2 times and measure food starchs, and add 80% ethanol and be mixed, the granulation of sieving, 60 ℃ are dry down, granulate, add 3% Pulvis Talci, 4% carboxymethyl starch sodium, tabletting (plain sheet require for 0.3g/ sheet), sugar coating sheet (or Film coated tablets) is checked to get final product after up to specification.
1.3 controlling the water circulation is proposed the composite capsule agent: get the dry coarse powder 10kg of Folium Kaki, prepare thick paste, weigh and write down thick paste weight with the 1.1st method, add 2 times of amount food starchs, and adding concentration 80% ethanol is mixed the granulation of sieving, 60 ℃ dry down, and granulate divides the capsule (0.5g/) of packing into.
1.4 controlling the water circulation is proposed the composition granule agent: get the dry coarse powder 10kg of Folium Kaki, prepare thick paste with the 1.1st method, weigh and write down thick paste weight, add 1 times of amount dextrin and 1 times of Icing Sugar and mix, make and do wet suitable soft agglomerate, pressed 10 mesh sieve, granule is in 50～60 ℃ of dryings, the dry granule of crossing is got the granule pack sealing of sieving after 12～14 mesh sieves, and specification is the 10g/ bag.
1.5 system water extract mixture: get the dry coarse powder 10kg of Folium Kaki, prepare thick paste with the 1.1st method, weigh and write down thick paste weight, adds 5 times of amount dissolved in distilled water, autoclaving adds 0.1% benzoic acid, branch pack into (10ml/ bottle) in the bottle.
1.6 controlling the water circulation is carried composition injection: get the dry coarse powder 10kg of Folium Kaki, prepare thick paste, weigh and write down thick paste weight with the 1.1st method, add 10 times of amount distilled water stirring and dissolving, filter, filtrate adds 0.3% active carbon, boils 10min, decolouring, filter, the cooling back adds 0.2% Tween 80, stirs evenly after-filtration, in filtrate, add 1%～2% benzyl alcohol, mixing, reuse 10% sodium hydroxide is transferred about pH6.5, and 4～8 ℃ of preservations are spent the night, after coarse filtration, filter with 94 flint glass F degerming funnels, or by the degerming filter plate, as do not reach clarity and should refilter once, medicinal liquid after the degerming is promptly packed in the ampoule, seals.Ampoule is once more through steam sterilization.
The extraction of embodiment 2, Folium Kaki ethanol extract and the preparation of preparation thereof:
2.1 the preparation of Folium Kaki ethanol extract: get the dry coarse powder 1kg of Folium Kaki, add 10L concentration 95% ethanol, reflux, extract, 3 times, each 2h filters, and extracting solution reclaims ethanol, is condensed into proportion and is 1.3 thick paste.
2.2 system ethanol extract tablet: get the dry coarse powder 1kg of Folium Kaki, prepare thick paste with the 2.1st method, weigh and write down thick paste weight, adds 2 times and measure food starchs, and adding concentration 80% ethanol is mixed, the granulation of sieving, 60 ℃ are dry down, granulate, add 3% Pulvis Talci, 4% carboxymethyl starch sodium, tabletting (plain sheet requires to be the 0.2g/ sheet), sugar coating sheet (or Film coated tablets) gets final product after visual examination is up to specification.
2.3 system ethanol extract capsule: get the dry coarse powder 1kg of Folium Kaki, prepare thick paste, weigh and write down thick paste weight with the 2.1st method, add 2 times of amount food starchs, and adding concentration 80% ethanol is mixed the granulation of sieving, 60 ℃ dry down, and granulate divides the capsule (0.2g/) of packing into.
2.4 system ethanol extract granule: get the dry coarse powder 1kg of Folium Kaki, prepare thick paste with the 2.1st method, weigh and write down thick paste weight, add 1 times of amount dextrin and 1 times of Icing Sugar and mix, make and do wet suitable soft agglomerate, pressed 10 mesh sieve, granule is in 50～60 ℃ of dryings, the dry granule of crossing is got the granule pack sealing of sieving after 12～14 mesh sieves, and specification is the 1g/ bag.
2.5 system ethanol extract mixture: get the dry coarse powder 1kg of Folium Kaki, prepare thick paste with the 2.1st method, weigh and write down thick paste weight, adds 5 times of amount dissolved in distilled water, autoclaving adds 0.1% benzoic acid, branch pack into (10ml/ bottle) in the bottle.
2.6 system ethanol extract injection: get the dry coarse powder 1kg of Folium Kaki, prepare thick paste, weigh and write down thick paste weight with the 2.1st method, add 10 times of amount distilled water stirring and dissolving, filter, filtrate adds 0.3% active carbon, boils 10min, decolouring, filter, the cooling back adds 0.2% Tween 80, stirs evenly after-filtration, in filtrate, add 1%～2% benzyl alcohol, mixing, reuse 10% sodium hydroxide is transferred about pH6.5, and 4～8 ℃ of preservations are spent the night, after coarse filtration, filter with 94 flint glass F degerming funnels, or by the degerming filter plate, as do not reach clarity and should refilter once, medicinal liquid after the degerming is promptly packed in the ampoule, seals.Ampoule is once more through steam sterilization.
The extraction of embodiment 3, Folium Kaki total flavones and the preparation of preparation thereof:
3.1 the preparation of Folium Kaki total flavones: take by weighing Folium Kaki coarse powder 1kg, after adding 70% ethanol 10L and soaking 30min, reflux, extract, 2h filters.Medicinal residues add 70% ethanol 80L again, and reflux, extract, 1h filters.Merge filtrate twice, the centrifugal (15min of 3000 γ/min).After reclaiming ethanol, collect extracting solution, concentrating under reduced pressure is used petroleum ether extraction 2 times, removes chlorophyll, abandons the ether phase, water ethyl acetate extraction 2 times, and combined ethyl acetate phase concentrate drying gets total flavones.
3.2 system total flavones tablet: get the dry coarse powder 1kg of Folium Kaki, prepare total flavones with the 3.1st method, weigh and write down total flavones weight, adds 2 times and measure food starchs, and adding concentration 80% ethanol is mixed, the granulation of sieving, 60 ℃ are dry down, granulate, add 3% Pulvis Talci, 4% carboxymethyl starch sodium, tabletting (plain sheet requires to be the 0.1g/ sheet), sugar coating sheet (or Film coated tablets) gets final product after visual examination is up to specification.
3.3 system total flavone capsule agent: get the dry coarse powder 1kg of Folium Kaki, prepare total flavones, weigh and write down total flavones weight with the 3.1st method, add 2 times of amount food starchs, and adding concentration 80% ethanol is mixed the granulation of sieving, 60 ℃ dry down, and granulate divides the capsule (0.2g/) of packing into.
3.4 system total flavones granule: get the dry coarse powder 1kg of Folium Kaki, prepare total flavones with the 3.1st method, weigh and write down total flavones weight, add 1 times of amount dextrin and 1 times of Icing Sugar and mix, make and do wet suitable soft agglomerate, pressed 10 mesh sieve, granule is in 50～60 ℃ of dryings, the dry granule of crossing is got the granule pack sealing of sieving after 12～14 mesh sieves, and specification is the 0.5g/ bag.
3.5 system total flavones mixture: get the dry coarse powder 1kg of Folium Kaki, prepare total flavones with the 3.1st method, weigh and write down total flavones weight, adds 5 times of amount distilled water stirring and evenly mixings, autoclaving adds 0.1% benzoic acid, branch pack into (10ml/ bottle) in the bottle.
3.6 system injection of general flavone: get the dry coarse powder 1kg of Folium Kaki, prepare total flavones, weigh and write down total flavones weight with the 3.1st method, add 10 times of amount distilled water and transfer the pH7.2 stirring and dissolving with 10% sodium hydroxide, filter, filtrate adds 0.3% active carbon, boils 10min, decolouring, filter, the cooling back adds 0.2% Tween 80, stirs evenly after-filtration, in filtrate, add 1%～2% benzyl alcohol, mixing, reuse 10% sodium hydroxide is transferred about pH7.2, and 4～8 ℃ of preservations are spent the night, after coarse filtration, filter with 94 flint glass F degerming funnels, or by the degerming filter plate, as do not reach clarity and should refilter once, medicinal liquid after the degerming is promptly packed in the ampoule, seals.Ampoule is once more through steam sterilization.
Claims (7)
1, a kind of Folium Kaki water extract preparation for the treatment of hypertension, coronary heart disease, diabetes is characterized in that: the Folium Kaki water extract is to separate from Folium Kaki coarse powder water extraction to obtain, and adds corresponding pharmaceutic adjuvant and makes tablet, capsule, granule, injection, mixture.
2, Folium Kaki water extract preparation according to claim 1, it is characterized in that: Folium Kaki water extract preparation is used for the treatment of hypertension, coronary heart disease, diabetes.
3, a kind of Folium Kaki ethanol extract preparation for the treatment of hypertension, coronary heart disease, diabetes is characterized in that: the Folium Kaki ethanol extract is to separate with ethanol extraction from the Folium Kaki coarse powder to obtain, and adds corresponding pharmaceutic adjuvant and makes tablet, capsule, granule, injection, mixture.
4, Folium Kaki ethanol extract preparation according to claim 3, it is characterized in that: Folium Kaki ethanol extract preparation is used for the treatment of hypertension, coronary heart disease, diabetes.
5, a kind of Folium Kaki total flavones preparation for the treatment of hypertension, coronary heart disease, diabetes, it is characterized in that: the Folium Kaki total flavones is to obtain from Folium Kaki coarse powder extraction separation, adds corresponding pharmaceutic adjuvant and makes tablet, capsule, granule, injection, mixture.
6, Folium Kaki total flavones preparation according to claim 5, it is characterized in that: the preparation method of Folium Kaki total flavones is: the Folium Kaki coarse powder, add 10 times of amount concentration 70% soak with ethanol 30min after, reflux, extract, 2h filters; Medicinal residues add 8 times of amount 70% ethanol again, and reflux, extract, 1h filters; Merge filtrate twice, centrifugal, behind the recovery ethanol, collect extracting solution, concentrating under reduced pressure is used petroleum ether extraction 2 times, removes chlorophyll, abandons the ether phase, water ethyl acetate extraction 2 times, combined ethyl acetate phase concentrate drying gets total flavones.
7, Folium Kaki total flavones preparation according to claim 5, it is characterized in that: Folium Kaki total flavones preparation is used for the treatment of hypertension, coronary heart disease, diabetes.
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| CN 200710034708 CN101028328A (en) | 2007-04-06 | 2007-04-06 | Production and use for kaki-leaf extract |
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| Application Number | Priority Date | Filing Date | Title |
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| CN 200710034708 CN101028328A (en) | 2007-04-06 | 2007-04-06 | Production and use for kaki-leaf extract |
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103284148A (en) * | 2013-05-20 | 2013-09-11 | 国家林业局泡桐研究开发中心 | Processing method of persimmon leaf concentrated powder rich in natural vitamin C |
| CN104606276A (en) * | 2014-12-30 | 2015-05-13 | 桂林得坤生物科技股份有限公司 | Method for extracting micromolecular persimmon leaf flavones from persimmon leaves |
| CN105250508A (en) * | 2015-10-13 | 2016-01-20 | 六枝祥晖民族民间中医药开发研究所 | Medicine for treating diabetes and preparation method thereof |
| JP2018008924A (en) * | 2016-06-29 | 2018-01-18 | サンスター株式会社 | Tie2 active composition |
| CN108619217A (en) * | 2017-03-24 | 2018-10-09 | 北京致成生物医学科技有限公司 | A kind of persimmon leaf extract and its extracting method |
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2007
- 2007-04-06 CN CN 200710034708 patent/CN101028328A/en active Pending
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103284148A (en) * | 2013-05-20 | 2013-09-11 | 国家林业局泡桐研究开发中心 | Processing method of persimmon leaf concentrated powder rich in natural vitamin C |
| CN103284148B (en) * | 2013-05-20 | 2015-04-15 | 国家林业局泡桐研究开发中心 | Processing method of persimmon leaf concentrated powder rich in natural vitamin C |
| CN104606276A (en) * | 2014-12-30 | 2015-05-13 | 桂林得坤生物科技股份有限公司 | Method for extracting micromolecular persimmon leaf flavones from persimmon leaves |
| CN104606276B (en) * | 2014-12-30 | 2019-04-26 | 桂林得坤生物科技股份有限公司 | A method of extracting small molecule persimmon leaf flavone from persimmon leaf |
| CN105250508A (en) * | 2015-10-13 | 2016-01-20 | 六枝祥晖民族民间中医药开发研究所 | Medicine for treating diabetes and preparation method thereof |
| JP2018008924A (en) * | 2016-06-29 | 2018-01-18 | サンスター株式会社 | Tie2 active composition |
| CN108619217A (en) * | 2017-03-24 | 2018-10-09 | 北京致成生物医学科技有限公司 | A kind of persimmon leaf extract and its extracting method |
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