CN1637010A - Extraction and application of paeonol amygdaloside - Google Patents

Abstract

The present invention discloses the extraction and application of paeonol amygdaloside as one kind of organic compound. The compound may be used in preparing medicine for preventing and treating hypertension, hemicrania and other reacting source diseases.

Description

The extraction of paeonol amygdalin and application

Technical field

The present invention relates to a kind of organic chemistry composition paeonol (Paeonol) amygdalin (Amygdalin that extracts by Tree Peony Bark and peach kernel, VitaminB17, claim Vitamin B17 again) extraction and application, the particularly application in the medicine of reaction source kinds diseases such as preparation prevention and treatment, essential hypertension, migraine.

Background technology

Disease occurred frequently such as essential hypertension, migraine is a present world medicine class disease of the clear and definite cause of disease not as yet, can not etiological treatment, can only respite or mitigation symptoms and can not curing, but often repeatedly, become lifelong disease, and heavy then threat to life.We are through studying for a long period of time, from medical history, symptom, (reaction source place local subcutaneous is injected low dose of PROCAINE HCL, PHARMA GRADE or lignocaine for sign and clinical trial treatment, soup only can soak into the skin and the subcutis of 2～3 cm diameters, the local anaesthetics permeates cell membranes, the gate of the sodium-ion channel of side blocking-up within it, make the cell at reaction source place can not produce action potential and conduction of impulse, injected about 2 minutes, symptom and sign such as hypertension or pain can take a turn for the better, disappearance along with local anesthetic action, symptom and sign recovers again, and the pernicious stimulation of unusual bioenergy of reaction source is described, causes the symptom and sign of reaction source kinds disease to recover again.In the temporary transient elimination electricity of the local work of reaction source, magnetic treatment, the migraineur is wailing with pain, and gets final product pain relieving, Tears gave way to smiles.And all be pain relieving at triplicate at that time) in find, physics, chemistry or biology cause the variation of body local histocyte gene damage, can cause damaged cell variation and heredity, and can discharge bio signals such as unusual bioelectricity, hertzian wave, direct or pernicious reflectingly stimulation target tissue produces pathologic reaction and disease takes place, and this causes the pernicious stimulus of pathologic reaction, just be called the injury response source, be called for short reaction source.Cause the reaction source that a certain disease takes place, be called relevant reaction source, otherwise claim irrelevant reaction source.The disease that reaction source causes claims the reactinogenicity disease.For example, the hypertension that reaction source causes claims reactinogenicity hypertension, promptly is existing title essential hypertension or essential hypertension.The migraine that reaction source causes claims the reactinogenicity migraine; The psychosis that reaction source causes claims the reactinogenicity psychosis.The big class reactinogenicity disease that reaction source causes claims the reaction source kinds disease, is called for short the reaction source disease.This numerous reaction source kinds disease is that intensity, frequency and four parameters of target tissue of the unusual bio signal that discharged by the different sites of reaction source, reaction source are determined.According to the principle of reaction source, reaction source kinds diseases such as essential hypertension, migraine are checked, treated and prevent, be called the reaction source therapy and (draw certainly: Liu Jisheng, Liao Jianxian.The clinical observation of reaction source therapy for treating essential hypertension.The hypertension magazine.1995,3 (3): 218～220.) (because of a lot of reaction sources are arranged is at local skin at reaction source place local subcutaneous liquid medicine injection in the treatment of reaction source therapy, and subcutaneously have the high amount of drug can the fastest the most direct healing reaction source) or approach such as quiet, oral pharmaceutical treat, with control or elimination reaction source, the symptom and sign of disease just obtains taking a turn for the better or being completely recovered not recurring.

The organic chemistry composition paeonol of this extract, oneself know have calmness, hypnosis, ease pain, bring down a fever, antianaphylaxis, antibiotic, reduce vascular permeability and effect such as hypotensive, amygdalin is known to have anti-inflammatory, anticoagulation, antithrombotic formation, antianaphylaxis, and can effectively treat schistosomal cirrhosis, diseases such as posthepatitic cirrhosis, and anti-mutation, antitumor action are arranged.Become human oral VB ₁₇Powder 4g every day continues two weeks, or quiet administration one month, and visible toxic reaction, also can show as ECG T wave and change for see more with Digestive tract, and the room is early won, and after the drug withdrawal, above toxic reaction all can disappear.If dosage is kept to 0.6-1.2g every day, then can avoid toxic reaction (drawing) from " China's book on Chinese herbal medicine " 4 96 pages.

The organic chemistry composition of this reaction source medicine can thoroughly be cured and reaction source kinds diseases such as preventing hypertension disease, migraine; this composition has the effect of slight expansion blood vessel microcirculation improvement and Normocellular structure of protection and function; more significant feature is the anomalous structure of energy repair cell gene; close abnormal function; destroy and the superseded extra high cell of grade malignancy that can not repair, so the 26S Proteasome Structure and Function of cell on the throne is normal.This is because of the structures shape function.Thereby reaction source discharges the defunctionalization of pernicious unusual bio signal and cures and change healthy tissues into, and the reaction source kinds disease of original secondary along with recovery from illness gradually, did not recur yet.Cure relevant reaction source at premorbid, but just prophylactic response source class disease.

Put off until some time later the related problems of essential hypertension now.The cytogene textural anomaly at the relevant reaction source place of essential hypertension, cause cell to have the abnormal function that discharges unusual bioenergy, and the continuous generations of also genetic abnormality structure of the new cell of splitted of duplicating, also all has the abnormal function that discharges unusual bioenergy, so, after essential hypertension takes place, just can long term maintenance hypertension.It is more and more to be that the reaction source injury region changes the cell of anomalous structure into again, and the amount that discharges unusual bioenergy is just big more, and again if textural anomaly is serious more, it is just strong more to discharge unusual bioenergy, and the effect of pernicious stimulation is just big more, and essential hypertension is also just serious more.Thereby, long-term serious patients with hypertension, unusual at the cytogene at the relevant reaction source place of essential hypertension, just may become the inheritance of acquired characters to its filial generation, its children just may obtain the genetic predisposition of hereditary essential hypertension.Though reaction source kinds diseases such as essential hypertension are can be not hereditary, but owing to just being easier to the more sick reason reaction of susceptibility real estate after the region of interest local tissue damage with genetic predisposition, the gene structure that is damaging cells is easier to by normally changing into unusual, form reaction source, the intensity frequency that the also easier cell that makes the reaction source place discharges unusual bioenergy reaches and causes hypertensive scope, and essential hypertension takes place.Here it is, and its children of patients with hypertension suffer from the higher reason of morbidity of essential hypertension.Certainly, not having posteriori former local tissue damage with essential hypertension genetic predisposition region of interest is can not get essential hypertension.For example, there are a lot of father and mother to suffer from its children of essential hypertension and do not suffer from essential hypertension.Essential hypertension is not a heredopathia as from the foregoing.If be heredopathia, constantly heredity from generation to generation, human nearly several thousand history hands down by heredity, and the sickness rate of middle national trouble essential hypertension has surpassed more than 60% for a long time, and far more than until now 11.26%.A lot of in addition his last three generations of patients with hypertension do not suffer from essential hypertension.Observe from this EPDML angle, illustrated that also essential hypertension is not a heredopathia, but the reactinogenicity disease.Promptly be the reactinogenicity hypertension that is secondary to reaction source.So, at clinical commonly used now or new gene symptomatic treatment depressor, only when drug effect, just having temporary transient hypotensive effect, a drug withdrawal blood pressure raises again.PROCAINE HCL, PHARMA GRADE or lignocaine can only the temporary interruption reaction source discharge the effect of unusual bioenergy, and blood pressure only can temporarily descend, and after local anesthetic action rapidly disappeared, blood pressure went up rapidly again.So, have the medicine that can repair reaction source place cytogene anomalous structure only and could cure essential hypertension fully.This is because the pernicious stimulation pallium of the unusual bioenergy of release that the cell at reaction source place can continue for a long time, and cause the imbalance of corticocerebral excitement and process of inhibition for a long time, cause vasomotor center dysfunction under the cortex, make the vasoconstrictor centre that accounts for strong advantage cause that the periphery sympathetic excitability strengthens for a long time, and the long-term hyperfunction of periphery SNE just continues synthetic and discharge extraordinary a large amount of norepinephrines, cause the trickle artery of whole body and continue spastic contraction for a long time, peripheral vascular resistance increases, blood pressure essential hypertension just occurs along with rising.Do not cure and just become lifelong disease.This is the mechanism of the main conclusive generation development of essential hypertension.Essential hypertension is (as the cortin increase of source, inside and outside property, sodium retention etc.) in the presence that hypophysis internal secretion and body fluid change, and has aggravated the rising of blood pressure, just essential hypertension is more serious.

Catecholamine in the known blood plasma derives from adrenal medulla and SNE.Normal about 1000 times suprarenin and norepinephrine can be secreted even exceed to adrenal medulla in a large number in emergency reaction, both are about 4: 1 at content ratio.But adrenal medulla only has the basal secretion of certain trace in normal activity, participates in keeping normal arterial pressure.Patients with hypertension plasma epinephrine level does not have obviously and increases; but patients with hypertension has in various degree sympathetic activation (with drawing in the aftermentioned literary composition that Wang Yi encloses etc.); noradrenaline levels also has extraordinary increasing in various degree in the hyperamization slurry; and cause the generation blood pressure high and low different essential hypertension is arranged; increasing with adrenal medulla of noradrenaline levels has nothing to do in this explanation blood plasma, illustrates promptly that also medulliadrenal normal activity can not participate in the elevation of blood pressure of essential hypertension.SNE is because of making the methylated Phenylethanolamine nitrogen of norepinephrine position methyl translocase, and can not further synthesize suprarenin, only can synthesize and discharge norepinephrine.Therefore the extraordinary level that increases of noradrenaline cellulose content has directly reflected the periphery sympathetic hyperfunction in the blood plasma.In experimental observation patients with hypertension 24 hours blood pressure rhythm normal group (spoon type group) and unusual group (non-spoon type group) and the body in the relation of the most important blood vessel hormone that contracts that discharges by neuroendocrine, find the Angiotensin II that no obvious content increases in the blood plasma, suprarenin, endothelin and neuropeptide tyrosine do not have obvious influence to the change of the patients with hypertension diurnal blood pressure rhythm and pace of moving things of orthobiosis (promptly not causing the situation of emergency reaction), just illustrate that also Angiotensin II etc. does not play a major role to the elevation of blood pressure of essential hypertension, have that contents level significantly increases in the norepinephrine blood plasma only, the change of 24 hours blood pressure rhythm has been played significant feature (draws from Wang Yiwei, Sun Ningling, Lu Xining.The relation of neuroendocrine factor and essential hypertension ambulatory blood pressure curve.The hypertension magazine.2002，10(3)：224～225.)。This just illustrates that it is the major causes that cause the patients with hypertension elevation of blood pressure that the periphery SNE continues extraordinary a large amount of release norepinephrines.This Quantitative experimental study result has further illustrated reaction source and has caused the long-term functional disorder of pallium, pallium thereby the nerve impulse of biography pathologic reaction down, thereby cause that the periphery SNE continues hyperfunction, extraordinary a large amount of release norepinephrine, cause the long-term spastic contraction of the trickle artery of whole body, peripheral vascular resistance increases, and blood pressure is along with rising, and has produced the principle of essential hypertension.This experimental result and the clinical therapeutic trials such as checking liquid that is coated with at the relevant reaction source of head place can step-downs about fast 2 minutes, reduce to normally just no longer to descend, and the quick step-down phenomenon of gradually ging up again about 15 minutes matches.Behind coating, reaction source discharges the abnormal function of the unusual bioenergy of pernicious stimulation and is temporarily controlled, the former corticocerebral function that is subjected to pernicious stimulation to cause imbalance transfers to normally, just promptly stop to pass down the nerve impulse of pathologic reaction, former hyperfunction periphery SNE function transfers to normally, stops to synthesize and discharging extraordinary a large amount of norepinephrines immediately.Because the nerve impulse conduction rapidly, the transformation period of norepinephrine also only has about 20 seconds, so step-down fast.Angiotensin II production process and the time of all losing efficacy are all very long, this quick step-down phenomenon can not occur.What this elevation of blood pressure of adding bright essential hypertension played a major role is not Angiotensin II etc., but norepinephrine.Be again in the provincial scientific research task paper of " clinical observation of reaction source therapy for treating essential hypertension " as can be known, method by randomized, double-blind and placebo, only through 10～30 times in short-term the treatment 106 examples, systolic pressure and diastolic pressure are respectively 171 and 104mmHg before the treatment, be respectively 133 and 81mmHg after the treatment, obvious effective rate 84.9%, efficient is 96.2%.Two control groups are all invalid.After stopping treatment, need not any depressor, 91 people that can follow up a case by regular visits in first anniversary, wherein 56 people's blood pressures are still normal; Two anniversaries were visited 43 people, normal 34 people of blood pressure; Three anniversaries were visited 26 people, normal 21 people.This explanation clinical efficacy highly significant particularly has late result, this is only working from the different links of keeping blood pressure of all symptomatic treatments, just as solving on the non-source, only presses not comparability of the same temporary depressor by the water pipe precipitation that leaks.Have only the medicine of this class treatment cause of disease reaction source this safe and efficient effect far away just to be arranged, the excellent curative effect that does not just recur after curing fully.These results of study have confirmed that all reaction source is the cause of disease of essential hypertension.

Causing the reaction source of essential hypertension is thoroughly treating through this class medicine, the cytogene anomalous structure at reaction source place is all repaired, structure function is normal, become normal cell, no longer discharge the unusual bioenergy of virulent and stimulated pallium, pallium transfers to normal by excited with the process of inhibition imbalance, subcortical center causes that producing hypertensive pathologic reaction disappears, and the periphery SNE no longer continues extraordinary release norepinephrine, and trickle artery no longer continues to shrink, transfer standard state to, blood pressure just descends naturally, recovers normal, long-term stability, essential hypertension is just cured fully, does not recur.Cure relevant reaction source at premorbid, just can prevent reaction source kinds diseases such as essential hypertension.

Summary of the invention

The purpose of this invention is to provide a kind of Tree Peony Bark of disease such as reaction source kinds such as thoroughly healing and prevention of migraine, essential hypertension etc. and the co-extracted thing and the application thereof of peach kernel.The paeonol amygdalin of indication of the present invention is to be formed by Tree Peony Bark and peach kernel co-extracted, gets Tree Peony Bark 15-150g peach kernel 2-30g, extracts and makes the 100ml injection liquid.The prescription of long-acting sustained-release agent is Tree Peony Bark 3600g peach kernel 500g, extracts the 93ml concentrated solution.Manufacture process:

Former medicinal powder be broken into as sesame big → add the flour miscellany 17-180g → adding pure water 600-1000ml → distillation 40min of Tree Peony Bark and peach kernel → get distillate 300-500ml in the insoluble container in water-bath, redistillation 15min → get concentrated solution 100ml, add lignocaine 50mg, make every 1ml contain lignocaine 0.5mg (intravenous administration need not add) → filtration → embedding, 2ml/ props up (soup achromatism and clarity) → sterilization → shady and cool lucifuge place and preserves.

The making method of long-acting sustained-release agent: former medicinal powder be broken into as sesame big → add flour 4100g → adding pure water 10000ml → distillation 100min → get distillate 2000ml in the insoluble container in water-bath, redistillation 40min → get distillate 500ml, redistillation 30min → get distilled and concentrated solution 93ml is made into finished product behind the carrier of adding long-acting sustained-release agent and selective aggregation reaction source.

Usage and dosage: subcutaneous injection once a day, each 2-40ml

Intravenous drip once a day, each 10ml.

This class clinical drug is evident in efficacy, and in the safe treatment weight range, be applied to clinical, nontoxicity, non-evident effect, only the subcutaneous injection part has and swells and ache, but hot compress take a turn for the better, lump does not disappear can treat with reaction source then fade away.This lump reaction only appears at the reaction source place, and can play the ocular effect in favourable mark recognition reaction source.Not finding has detrimentally affect to hepatic and renal function.

The clinical efficacy of reaction source topical therapeutic and late result, first with whether accurately to have treated diseases induced whole relevant reaction source relevant, if the injection skew, soup fails to make reaction source all to soak into, can not make the cytogene anomalous structure reparation in total overall reaction source, then weak curative effect, easily recurrence.The 2nd, treatment number of times deficiency, the cytogene anomalous structure of reaction source is repaired fully, can only weaken rather than eliminate the abnormal function of reaction source, and then disease such as essential hypertension is not cured fully, easily recurs.To accurately control continuously more than 60 to 90 times, just can cure fully and not recur.

The possible related factors that reaction source kinds diseases such as essential hypertension are brought out or increased the weight of: head tans by the sun; Flu; Consume oil bar, fry in shallow oil hot dry irritable foods such as meat, ginger, beef, cock, dog meats; Tired; Insomnia; Nutrition and dysthymia and wound etc.In treatment, remove inducement, then can quicken to take a turn for the better.After if relevant reaction source cures fully, the above-mentioned related factors fall out effect that do not recur.

Embodiment

Embodiment one: former medicinal powder be broken into as sesame big → add flour → adding pure water 600ml → distillation 40min of Tree Peony Bark 15g and peach kernel 2g → get distillate 300ml in the insoluble container in water-bath, redistillation 15min → get concentrated solution 100ml adds lignocaine 50mg.Make every 1ml contain lignocaine 0.5mg → filtration → embedding, 2ml/ props up (soup achromatism and clarity) → sterilization → shady and cool lucifuge place and preserves.

Usage and dosage: subcutaneous injection once a day, each 2ml.

Embodiment two: former medicinal powder be broken into as sesame big → add flour → adding pure water 2000ml → distillation 80min of Tree Peony Bark 150 and peach kernel 20g → get distillate 1500ml redistillation 40min → get concentrated solution 1000ml in the insoluble container in water-bath, add lignocaine 500mg, make every 1ml contain lignocaine 0.5mg → filtration → embedding, 2ml/ props up (soup achromatism and clarity) → sterilization → shady and cool lucifuge place and preserves.

Usage and dosage: subcutaneous injection once a day, each 40ml.

Embodiment three: former medicinal powder be broken into as sesame big → add flour → adding pure water 1000ml → distillation 40min of Tree Peony Bark 150g peach kernel 30g → get distillate 500ml in the insoluble container in water-bath, redistillation 15min → get concentrated solution 100ml → filtration → embedding, 2ml/ props up (soup achromatism and clarity) → sterilization → shady and cool lucifuge place and preserves.

Usage and dosage: intravenous drip once a day, each 10ml.

Embodiment four: root bark of tree peony peach kernel powder be broken into as sesame big → add Tree Peony Bark 3600g peach kernel 500g → adding pure water 10000ml → distillation 100min → get distillate 2000ml in the insoluble container in water-bath, redistillation 40min → get distillate 500ml, redistillation 30min → get distilled and concentrated solution 93ml is made into finished product behind the carrier of adding long-acting sustained-release agent and selective aggregation reaction source.

Claims (3)

1, a kind of extracting method of paeonol amygdalin, it is characterized in that: former medicinal powder be broken into as sesame big → add Tree Peony Bark 15-150g in the insoluble container in water-bath, peach kernel 2-30g → adding pure water 600-1000ml → distillation 40min → get distillate 300-500ml, redistillation 15min → get concentrated solution 100ml, add lignocaine 50mg, make every 1ml contain lignocaine 0.5mg (intravenous administration need not add) → filtration → embedding, 2ml/ props up (soup achromatism and clarity) → sterilization → shady and cool lucifuge place and preserves.

2, a kind of making method of long-acting sustained-release agent of paeonol amygdalin: former medicinal powder be broken into as sesame big → add Tree Peony Bark 3600g in the insoluble container in water-bath, peach kernel 500g → adding pure water 10000ml → distillation 100min → get distillate 2000ml, redistillation 40min → get distillate 500ml, redistillation 30min → get distilled and concentrated solution 93ml is made into finished product behind the carrier of adding long-acting sustained-release agent and selective aggregation reaction source.

3, a kind of paeonol amygdalin purposes, it is characterized in that: the application of this composition in the medicine of reaction source kinds diseases such as preparation prevention and treatment essential hypertension, migraine.