CN105395646A

CN105395646A - Medicine composition for treating primary hypertension and preparation method thereof

Info

Publication number: CN105395646A
Application number: CN201510704176.XA
Authority: CN
Inventors: 邓凤桂
Original assignee: GUANGDONG JUZHICHENG TECHNOLOGY Co Ltd
Current assignee: GUANGDONG JUZHICHENG TECHNOLOGY Co Ltd
Priority date: 2015-10-27
Filing date: 2015-10-27
Publication date: 2016-03-16

Abstract

The invention belongs to the field of traditional Chinese medicine, and relates to a medicine composition for treating primary hypertension and a preparation method thereof. The medicine composition is mainly prepared from, by weight, 22-36 parts of folium mori, 10-20 parts of rhizomes of ligusticum wallichii, 8-16 parts of cape jasmine, 15-25 parts of clematis filamentosa, 12-18 parts of dutchmanspipe roots, 10-16 parts of rhizoma gastrodiae, 12-18 parts of eucommia ulmoides, 14-20 parts of Chinese yam, 8-14 parts of cortex moutan, 10-16 parts of ginkgo leaves, 6-12 parts of scutellaria baicalensis, 6-12 parts of cortex albiziae, 6-16 parts of spina date seeds and 8-18 parts of liquorice roots. The medicine composition is reasonable in formula and strong in synergistic effect; when used for treating primary hypertension, the medicine composition is significant in treatment effect, stable in medicine effect and small in side effect and has significant clinic promotion value.

Description

A kind of pharmaceutical composition for the treatment of essential hypertension and preparation method thereof

Technical field

The invention belongs to the field of Chinese medicines, particularly relate to a kind of pharmaceutical composition for the treatment of essential hypertension and preparation method thereof.

Background technology

By the standard of WHO, the blood pressure of human normal is systolic pressure 140mmHg and (or) diastolic pressure 90mmHg, and exceeding this scope can be diagnosed as hypertension.Hypertension is common cardiovascular disease, and it is defined as body and follows bad arterial pressure persistence and increase.The hypertension being secondary to kidney, endocrine and nervous system disease is called that secondary hypertension is sick, accounts for hyperpietic's 5% ~ 10%; And not yet illustrate the hypertension of its reason so far, be called essential hypertension.Essential hypertension accounts for hyperpietic's more than 90%, normal with organ functional or organic changes such as fat and sugar metabolism disorder and the heart, brain, kidney and retinas, it is the paathogenic factor of apoplexy (cerebral infarction and cerebral hemorrhage), coronary heart disease, retinopathy, kidney damage (glomerule infraction, renal failure), research shows, the M & M of cardiovascular and cerebrovascular disease and blood pressure to increase degree closely related.

The current research of doctor trained in Western medicine is thought, essential hypertension is the result of heredity, environment, anatomical structure, adaptability, nerve, endocrine, the many-sided comprehensive function of body fluid and hemodynamics, is that some congenital hereditary gene a kind of and many pathogenic supercharging factors and physiological reduce pressure factor interaction and the multi-factor disease that causes.Except foreign genetic element, high sodium low potassium meals in life, Bad Eating Habit and overweight, fat, the long-term psychentonia such as to drink, lack motion etc. and all likely bring out hypertension.So the cooperation outside Drug therapy and between non-drug therapy is focused in hypertensive treatment clinically, namely focuses on the cooperation between lifestyle modification and antihypertensive drug therapy.The antihypertensive drugs of the clinical frequent application of doctor trained in Western medicine mainly contains calcium ion antagonist (CaA), angiotensin-convertion enzyme inhibitor (ACEI), β body blocker, this four class of diuretic, secondly C receptor blocking agent, vasodilation etc. are also had, these medicines all can have larger side effect usually, also costly, toleration and the compliance of Drug safety and patient have much room for improvement price.

The most onset of hypertension is slow, progressive, as long as with arteriotony rising with lastingly for disease, also has dizziness in addition, has a headache, neck plate is tight, fatigue, cardio palmus shape.The traditional Chinese medical science belongs to the disease categories such as Chinese medicine is dizzy, headache to hypertensive elaboration, and its pathogenesis is due to negative and positive of qi and blood imbalance, makes brains hollow, and venation is lost and supported, or clear sun is not opened up, or fire is disturbed key clearly and created all diseases of hypertension.After hypertension is formed, internal injury is long-pending damages in stagnation of phlegm-damp in middle-JIAO, deficiency of qi and blood, deficiency of kidney yin, and the existence of intermediary's pathogenesis such as hyperactivity of YANG due to deficiency of YIN further develops, if qi and blood stagnation is in brain, then can become cerebral thrombosis and apoplexy, or stasis blocking in the heart be then the thoracic obstruction, angina pectoris.If QI and blood superinverse, hold expectorant under the arm and hold fire under the arm in clear key, then can occur cerebral hemorrhage apoplexy.Damage with the passing of time if internal injury is long-pending, hinder in kidney spleen, make kidney lose folding, board loses vaporization, and retention of water-damp in the body, namely the disease such as edema, renal failure occurs.

Chinese patent application 200710014082.5 discloses the hypertensive Chinese medicine composition of a kind of orally taken for curing, the crude drug of its effective ingredient mainly comprises: Ganoderma 6 ~ 9 grams, Radix Angelicae Sinensis 6 ~ 12 grams, Cordyceps 5 ~ 10 grams, Radix Gentianae 3 ~ 6 grams, Ramulus Uncariae Cum Uncis 3 ~ 12 grams, Folium Apocyni Veneti 6 ~ 12 grams, the Cortex Eucommiae 3 ~ 6 grams, Semen Cassiae 10 ~ 15 grams, Spica Prunellae 9 ~ 15 grams, Concha Margaritifera 10 ~ 20 grams, 4 ~ 8 grams, Radix Glycyrrhizae and Pheretima 5 ~ 10 grams.This traditional Chinese medicine composition for treating hypertension has determined curative effect, the advantage of non-relapse after healing, but crude drug cost is high, and drug price is expensive, is not easy to apply.

Current medical circle is thought, essential hypertension is a lifelong participation disease, and not yet report has any medicine thoroughly to cure hypertension at present, and patient needs long-term taking anti-hypertension treatment.Antihypertensive drugs needs to apply for a long time or all the life, the toleration of Drug safety and patient is very important, little and the efficacy stability of Traditional Chinese Medical on Treating Hypertension drug side effect, can long-term safety medication, has a extensive future, but it is not remarkable to there is effect in the hypertensive Chinese medicine of existing prevention and therapy, onset waits not enough slowly, seeks a kind of Be very effective, rapid-action, the pharmaceutical composition of taking convenience, has great importance to the clinical treatment of essential hypertension.

Summary of the invention

In order to make up the deficiencies in the prior art, first object of the present invention is to provide a kind of pharmaceutical composition for the treatment of essential hypertension, this pharmaceutical composition has effect of suppressing the hyperactive liver blood pressure lowering, blood circulation promoting and blood stasis dispelling, resolving stagnation for tranquilization, vital energy benefiting and the kidney invigorating, also possess the advantages such as rapid-action, therapeutic effect remarkable, efficacy stability, drug side effect are low simultaneously, can as the hyperpietic initial medication for the treatment of or long term maintenance medication, simultaneously low, the taking convenience of pharmaceutical composition cost of the present invention, is easy to apply.

Pharmaceutical composition of the present invention is prepared from primarily of the raw material of following parts by weight:

Folium Mori 22-36 part, Rhizoma Chuanxiong 10-20 part, Fructus Gardeniae 8-16 part, Clematis filamentosa Dunn 15-25 part, Radix Aristolochiae 12-18 part, Rhizoma Gastrodiae 10-16 part, Cortex Eucommiae 12-18 part, Rhizoma Dioscoreae 14-20 part, Cortex Moutan 8-14 part, Folium Ginkgo 10-16 part, Radix Scutellariae 6-12 part, Cortex Albiziae 6-12 part, Semen Ziziphi Spinosae 6-16 part and Radix Glycyrrhizae 8-18 part.

Further, described pharmaceutical composition is prepared from primarily of the raw material of following parts by weight:

22 parts, Folium Mori, Rhizoma Chuanxiong 10 parts, Fructus Gardeniae 8 parts, Clematis filamentosa Dunn 15 parts, Radix Aristolochiae 12 parts, 10 parts, Rhizoma Gastrodiae, the Cortex Eucommiae 12 parts, Rhizoma Dioscoreae 14 parts, Cortex Moutan 8 parts, Folium Ginkgo 10 parts, Radix Scutellariae 6 parts, Cortex Albiziae 6 parts, Semen Ziziphi Spinosae 6 parts and 8 parts, Radix Glycyrrhizae.

36 parts, Folium Mori, Rhizoma Chuanxiong 20 parts, Fructus Gardeniae 16 parts, Clematis filamentosa Dunn 25 parts, Radix Aristolochiae 18 parts, 16 parts, Rhizoma Gastrodiae, the Cortex Eucommiae 18 parts, Rhizoma Dioscoreae 20 parts, Cortex Moutan 14 parts, Folium Ginkgo 16 parts, Radix Scutellariae 12 parts, Cortex Albiziae 12 parts, Semen Ziziphi Spinosae 16 parts and 18 parts, Radix Glycyrrhizae.

28 parts, Folium Mori, Rhizoma Chuanxiong 16 parts, Fructus Gardeniae 12 parts, Clematis filamentosa Dunn 20 parts, Radix Aristolochiae 14 parts, 14 parts, Rhizoma Gastrodiae, the Cortex Eucommiae 16 parts, Rhizoma Dioscoreae 18 parts, Cortex Moutan 10 parts, Folium Ginkgo 13 parts, Radix Scutellariae 8 parts, Cortex Albiziae 10 parts, Semen Ziziphi Spinosae 12 parts and 14 parts, Radix Glycyrrhizae.

Source, the nature and flavor of pharmaceutical composition of the present invention Chinese crude drug used, return through and effect:

Folium Mori: this product is the dried leaves of moraceae plants Mulberry.Bitter in the mouth, sweet, cold nature; Return lung, Liver Channel; Wind and heat dispersing, liver heat removing and eyesight improving, cooling blood for hemostasis.

Rhizoma Chuanxiong: this product is the dry rhizome of samphire Rhizoma Chuanxiong; Acrid in the mouth, warm in nature; Return liver, gallbladder, pericardium channel; Blood-activating and qi-promoting, wind-expelling pain-stopping.

Fructus Gardeniae: this product is the fruit of Maguireothamnus speciosus Fructus Gardeniae; Bitter in the mouth, cold in nature; GUIXIN, lung, tri-jiao channel; Clearing away heat-damp and promoting diuresis, removing pathogenic heat from blood and toxic substance from the body, reducing swelling and alleviating pain.

Clematis filamentosa Dunn: this product is Ranunculaceae Clematis filamentosa Dunn, is used as medicine with leaf.Sweet in the mouth, slightly cool in nature; GUIXIN, Liver Channel; Clearing away liver-fire, mind calming god, blood pressure lowering, removing obstruction in the collateral to relieve pain.

Radix Aristolochiae: this product is the dry root of aristolochiaceae plant Fructus Aristolochiae.Acrid in the mouth, hardship, cold in nature; Attach to the lung and stomach meridians; Promoting the circulation of QI to relieve pain, removing toxic substances and promoting subsidence of swelling, suppressing the hyperactive liver blood pressure lowering.

Rhizoma Gastrodiae: this product is the dry tuber of orchid Rhizoma Gastrodiae.Sweet in the mouth, property is put down; Return Liver Channel; Endogenous wind stopping relieving convulsion, suppressing the hyperactive liver sun, dispelling wind and removing obstruction in the collateral.

The Cortex Eucommiae: this product is the dry bark of the Eucommiaceae plant Cortex Eucommiae.Sweet in the mouth, warm in nature; Return liver, kidney channel; Invigorating the liver and kidney, bone and muscle strengthening, antiabortive.

Rhizoma Dioscoreae: this product is the dry rhizome of Dioscoreaceae plant Rhizoma Dioscoreae.Sweet in the mouth, property is put down; Return spleen, lung, kidney channel; Spleen reinforcing nourishing the stomach, promote the production of body fluid lung benefiting, the kidney invigorating arresting seminal emission.

Cortex Moutan: this product is the dry root bark of ranunculaceae peony.Bitter in the mouth, pungent, cold nature; GUIXIN, liver, kidney channel; Clearing away heat and cooling blood, blood circulation promoting and blood stasis dispelling.

Folium Ginkgo: this product is the dried leaves of Ginkgoaceae plant Ginkgo biloba.Sweet in the mouth, hardship, puckery, property is put down; GUIXIN, lung meridian; Blood circulation promoting and blood stasis dispelling, removing obstruction in the collateral to relieve pain, astringes the lung and relievings asthma, and changes turbid blood fat reducing.

Radix Scutellariae: this product is the dry root of labiate Radix Scutellariae.Bitter in the mouth, cold in nature; Return lung, gallbladder, spleen, large intestine, small intestine meridian; Heat clearing and damp drying, eliminating fire and detoxication, hemostasis, antiabortive.

Cortex Albiziae: this product is the dry bark of leguminous plant Herba Albiziae.Sweet in the mouth, property is put down; GUIXIN, liver, lung meridian; Resolving stagnation for tranquilization, promoting blood circulation and detumescence.

Semen Ziziphi Spinosae: this product is the dry mature seed of Rhamnaceae plant Ziziphi Spinosae.Sweet in the mouth, acid, property is put down; Return liver, gallbladder, heart channel; Tonifying liver, mind calming, arresting sweating, promotes the production of body fluid.

Radix Glycyrrhizae: this product is the dry root of glycyrrhizic legume, Glycyrrhiza inflata Bat. or Glycyrrhiza glabra L..Sweet in the mouth, property is put down; GUIXIN, lung, spleen, stomach warp; Invigorating the spleen and replenishing QI, heat-clearing and toxic substances removing, expelling phlegm for arresting cough, relieving spasm to stop pain, coordinating the actions of various ingredients in a prescription.

The prescription analysis of medicament composing prescription of the present invention:

Medicament composing prescription of the present invention with Folium Mori, Rhizoma Chuanxiong and Clematis filamentosa Dunn for monarch drug, blood pressure lowering, clearing away liver-fire, blood-activating and qi-promoting; With Fructus Gardeniae, Radix Aristolochiae, Rhizoma Gastrodiae, the Cortex Eucommiae and Rhizoma Dioscoreae for ministerial drug, suppressing the hyperactive liver blood pressure lowering, liver and kidney tonifying, endogenous wind stopping relieving convulsion, dredging collateral, circulation of qi promoting; With Cortex Moutan, Folium Ginkgo, Radix Scutellariae, Cortex Albiziae and Semen Ziziphi Spinosae for adjuvant drug, blood circulation promoting and blood stasis dispelling, resolving stagnation for tranquilization, changes turbid blood fat reducing; With Radix Glycyrrhizae for making medicine, relieving spasm to stop pain, heat-clearing and toxic substances removing, coordinating the actions of various ingredients in a prescription, makes all medicines arrange in pairs or groups, synergism, jointly reaches suppressing the hyperactive liver blood pressure lowering, blood circulation promoting and blood stasis dispelling, resolving stagnation for tranquilization, effect of vital energy benefiting and the kidney invigorating, has very significant therapeutic effect to essential hypertension.

Second object of the present invention is to provide corresponding manufacturing process and is made and facilitate easy-to-use finished product preparation under the prerequisite ensureing curative effect by this Chinese medicine.

The preparation method of described pharmaceutical composition mainly comprises the following steps:

S1 gets Folium Mori, washes away impurity, 50 DEG C of hot air dryings 5 hours, and control moisture is 2-6%, pulverizes, and crosses 45-60 mesh sieve, obtains coarse powder; Coarse powder is sucked air-stream type ultrafine pulverizer and carry out micronizing, pulverize pressure 0.6MPa, charging rate is 28mg/s, carries out micronizing respectively after drying, crosses 800 mesh sieves, obtains Ultra-fine Powder of Mulberry Leaves;

S2 gets Rhizoma Chuanxiong, Fructus Gardeniae, Clematis filamentosa Dunn, Radix Aristolochiae, Rhizoma Gastrodiae, the Cortex Eucommiae, Rhizoma Dioscoreae, Cortex Moutan, Folium Ginkgo, Radix Scutellariae, Cortex Albiziae, Semen Ziziphi Spinosae and Radix Glycyrrhizae, clean, crushed after being dried, add the water soaking 2-4 hour of above-mentioned coarse powder total amount 8-12 times amount, then decoct 2-3 time, each 1-2 hour, filter, merging filtrate, filtrate is at 50-65 DEG C, vacuum is survey the clear paste that relative density is 1.10-1.20 under vacuum-concentrcted to 60 DEG C condition under the condition of 0.05-0.08MPa, cooling, slowly add ethanol while stirring and reach 40-60% to alcohol content, 4 DEG C of standing 12-24 hour, filter, obtain filtrate A and filtering residue,

It is the ethanol of 40-60% that the filtering residue obtained in step S2 is slowly added its weight 4-6 times amount volume fraction by S3 while stirring, 4 DEG C of standing 3-5 hour, filters, obtains liquor B and filtering residue; Filtering residue uses the washing with alcohol 2-3 time of 40-60% again, collects and merges cleaning mixture;

The liquor B that filtrate A and step S3 that step S2 obtains by S4 obtain and cleaning mixture mix, and survey the thick paste that relative density is 1.10-1.20, drying under reduced pressure under mixing final vacuum is evaporated to 60 DEG C of conditions, pulverize, cross 100-200 mesh sieve, the Ultra-fine Powder of Mulberry Leaves obtained with step S1 mixes, and to obtain final product.

Utilize modern general pharmaceutical composition technology, pharmaceutical composition of the present invention can be made into the finished product preparation of clinical needs, as dosage forms such as granule, pill, powder, tablet, capsule or oral liquids.

The present invention also discloses a kind of purposes of aforementioned pharmaceutical compositions, i.e. the purposes of aforementioned pharmaceutical compositions in preparation treatment essential hypertension medicine.Medicine composite for curing rat primary hypertension model test display of the present invention, pharmaceutical composition of the present invention is used for the treatment of essential hypertension and has the effect significantly reduced blood pressure, and also has certain effect of slowing down to the heart rate of rat simultaneously; Clinical trial also shows, drug regimen of the present invention is used for the treatment of essential hypertension, Be very effective, clinical symptoms such as dizzy, headache etc. common to essential hypertension also has significant improvement result, the average total effective rate for the treatment of essential hypertension reaches 95.00%, and its therapeutic effect is significantly higher than positive control drug.Medicine composite for curing Be very effective of the present invention, rapid-action, drug side effect is low, and can be used as the drug use for the treatment of essential hypertension, clinical generalization value is high.

Compared with prior art, pharmaceutical composition of the present invention has following technical advantage:

(1) compared with the Therapeutic Method of current essential hypertension, pharmaceutical composition of the present invention is natural pure pharmaceutical composition, toxic and side effects is little, the untoward reaction of medicine also can be avoided or reduce to long-term taking, and pharmaceutical composition efficacy stability of the present invention, easy to use, drug compliance is high, is applicable to the long-term treatment of essential hypertension.

(2) pharmacological evaluation display, pharmaceutical composition of the present invention as treatment essential hypertension drug use time, drug effect is comprehensive, have rapid-action, good effects etc. treat advantage significantly, effectively can reduce the generation of hypertension complication, improve the quality of life of patient.

(3) pharmaceutical composition preparation technology of the present invention is simple, and raw material is easy to get, and also has efficacy stability simultaneously, rapid-action, toxic and side effects is low and be easy to advantages such as applying.

Detailed description of the invention

Below will the present invention is described further by specific embodiment, it will be understood by those skilled in the art that the present invention also can make other similar changes and obtains similar result and do not depart from content of the present invention and scope except following examples.

Embodiment 1

The embodiment of the present invention 1 pharmaceutical composition is prepared from primarily of the raw material of following parts by weight:

Preparation method is as follows:

S1 gets Folium Mori, washes away impurity, 50 DEG C of hot air dryings 5 hours, and controlling moisture is 2%, pulverizes, and crosses 45 mesh sieves, obtains coarse powder; Coarse powder is sucked air-stream type ultrafine pulverizer and carry out micronizing, pulverize pressure 0.6MPa, charging rate is 28mg/s, carries out micronizing respectively after drying, crosses 800 mesh sieves, obtains Ultra-fine Powder of Mulberry Leaves;

S2 gets Rhizoma Chuanxiong, Fructus Gardeniae, Clematis filamentosa Dunn, Radix Aristolochiae, Rhizoma Gastrodiae, the Cortex Eucommiae, Rhizoma Dioscoreae, Cortex Moutan, Folium Ginkgo, Radix Scutellariae, Cortex Albiziae, Semen Ziziphi Spinosae and Radix Glycyrrhizae, clean, crushed after being dried, add the water soaking 2 hours of above-mentioned coarse powder total amount 8 times amount, then decoct 2 times, each 1 hour, filter, merging filtrate, filtrate is at 50 DEG C, vacuum is survey the clear paste that relative density is 1.10 under vacuum-concentrcted to 60 DEG C condition under the condition of 0.05MPa, cooling, slowly adds ethanol while stirring and reaches 40% to alcohol content, and 4 DEG C leave standstill 12 hours, filter, obtain filtrate A and filtering residue;

It is the ethanol of 40% that the filtering residue obtained in step S2 is slowly added its weight 4 times amount volume fraction by S3 while stirring, and 4 DEG C leave standstill 3 hours, filter, obtain liquor B and filtering residue; Filtering residue uses the washing with alcohol 2 times of 40% again, collects and merges cleaning mixture;

The liquor B that filtrate A and step S3 that step S2 obtains by S4 obtain and cleaning mixture mix, the thick paste that relative density is 1.10 is surveyed under mixing final vacuum is evaporated to 60 DEG C of conditions, drying under reduced pressure, pulverize, cross 100 mesh sieves, the Ultra-fine Powder of Mulberry Leaves obtained with step S1 mixes, and adds corresponding adjuvant, makes granule.

Embodiment 2

The embodiment of the present invention 2 pharmaceutical composition is prepared from primarily of the raw material of following parts by weight:

Preparation method is as follows:

S1 gets Folium Mori, washes away impurity, 50 DEG C of hot air dryings 5 hours, and controlling moisture is 4%, pulverizes, and crosses 50 mesh sieves, obtains coarse powder; Coarse powder is sucked air-stream type ultrafine pulverizer and carry out micronizing, pulverize pressure 0.6MPa, charging rate is 28mg/s, carries out micronizing respectively after drying, crosses 800 mesh sieves, obtains Ultra-fine Powder of Mulberry Leaves;

S2 gets Rhizoma Chuanxiong, Fructus Gardeniae, Clematis filamentosa Dunn, Radix Aristolochiae, Rhizoma Gastrodiae, the Cortex Eucommiae, Rhizoma Dioscoreae, Cortex Moutan, Folium Ginkgo, Radix Scutellariae, Cortex Albiziae, Semen Ziziphi Spinosae and Radix Glycyrrhizae, clean, crushed after being dried, add the water soaking 3 hours of above-mentioned coarse powder total amount 10 times amount, then decoct 2 times, each 1 hour, filter, merging filtrate, filtrate is at 60 DEG C, vacuum is survey the clear paste that relative density is 1.15 under vacuum-concentrcted to 60 DEG C condition under the condition of 0.06MPa, cooling, slowly add ethanol while stirring and reach 50% to alcohol content, 4 DEG C leave standstill 18 hours, filter, obtain filtrate A and filtering residue,

It is the ethanol of 50% that the filtering residue obtained in step S2 is slowly added its weight 5 times amount volume fraction by S3 while stirring, and 4 DEG C leave standstill 4 hours, filter, obtain liquor B and filtering residue; Filtering residue uses the washing with alcohol 2 times of 50% again, collects and merges cleaning mixture;

The liquor B that filtrate A and step S3 that step S2 obtains by S4 obtain and cleaning mixture mix, the thick paste that relative density is 1.15 is surveyed under mixing final vacuum is evaporated to 60 DEG C of conditions, drying under reduced pressure, pulverize, cross 140 mesh sieves, the Ultra-fine Powder of Mulberry Leaves obtained with step S1 mixes, and adds corresponding adjuvant, makes capsule.

Embodiment 3

The embodiment of the present invention 3 pharmaceutical composition is prepared from primarily of the raw material of following parts by weight:

Preparation method is as follows:

S1 gets Folium Mori, washes away impurity, 50 DEG C of hot air dryings 5 hours, and controlling moisture is 6%, pulverizes, and crosses 60 mesh sieves, obtains coarse powder; Coarse powder is sucked air-stream type ultrafine pulverizer and carry out micronizing, pulverize pressure 0.6MPa, charging rate is 28mg/s, carries out micronizing respectively after drying, crosses 800 mesh sieves, obtains Ultra-fine Powder of Mulberry Leaves;

S2 gets Rhizoma Chuanxiong, Fructus Gardeniae, Clematis filamentosa Dunn, Radix Aristolochiae, Rhizoma Gastrodiae, the Cortex Eucommiae, Rhizoma Dioscoreae, Cortex Moutan, Folium Ginkgo, Radix Scutellariae, Cortex Albiziae, Semen Ziziphi Spinosae and Radix Glycyrrhizae, clean, crushed after being dried, add the water soaking 4 hours of above-mentioned coarse powder total amount 12 times amount, then decoct 3 times, each 2 hours, filter, merging filtrate, filtrate is at 65 DEG C, vacuum is survey the clear paste that relative density is 1.20 under vacuum-concentrcted to 60 DEG C condition under the condition of 0.08MPa, cooling, slowly add ethanol while stirring and reach 60% to alcohol content, 4 DEG C leave standstill 24 hours, filter, obtain filtrate A and filtering residue,

It is the ethanol of 60% that the filtering residue obtained in step S2 is slowly added its weight 6 times amount volume fraction by S3 while stirring, and 4 DEG C leave standstill 5 hours, filter, obtain liquor B and filtering residue; Filtering residue uses the washing with alcohol 3 times of 60% again, collects and merges cleaning mixture;

The liquor B that filtrate A and step S3 that step S2 obtains by S4 obtain and cleaning mixture mix, the thick paste that relative density is 1.20 is surveyed under mixing final vacuum is evaporated to 60 DEG C of conditions, drying under reduced pressure, pulverize, cross 200 mesh sieves, the Ultra-fine Powder of Mulberry Leaves obtained with step S1 mixes, and adds corresponding adjuvant, makes tablet.

Pharmaceutical composition pharmacodynamic study of the present invention:

Test one: the experimentation of medicine composite for curing original hypertensive rat of the present invention

1, experimental animal: the Wistar rat of SPF level health 10,10 ~ 12 week age, body weight 180 ~ 220g, male, be set to Normal group.Original hypertensive rat (SHR) 50, SPF level, 10 ~ 12 week age, body weight 200 ~ 240g, male, be divided into 5 groups at random, be respectively model control group, positive controls, high dose group, middle dosage group and low dose group, often organize 10.

2, trial drug and dosage regimen:

Drug test group of the present invention: trial drug is the Chinese medicinal tablet of the present invention that the embodiment of the present invention 3 obtains, and grinds rear water into powder and is deployed into the solution that concentration is 0.6g/ml, 0.4g/ml and 0.2g/ml, for subsequent use.High dose group concentration is the drug solution of 0.6g/ml, middle dosage group concentration is the drug solution of 0.4g/ml, low dose group concentration is the drug solution of 0.2g/ml, high dose group (2.4g/kg), middle dosage group (1.6g/kg) and low dose group (0.8g/kg), according to dosage morning every day, late each gastric infusion are once, successive administration 30d.

Model control group: use isometric(al) normal saline every day early, late each gavage once, continuous gavage 30d.

Positive controls: positive control drug is kendir pressure-reducing sheet (the accurate word Z20093153 of traditional Chinese medicines, No. 2 TCM Factory), grind the solution that rear water is deployed into 0.6g/ml into powder, by dosage morning every day of 1.2g/kg, late each gastric infusion once, successive administration 30d.

Normal group: use isometric(al) normal saline every day early, late each gavage once, continuous gavage 30d.

3, the mensuration of blood pressure, heart rate: before first gastric infusion after 2h and last administration 2h, measure tail systolic arterial pressure and the heart rate of each group of rat.Before pressure measurement, rat is put into (37 ± 1) DEG C electrothermostat preheating 15min, survey 3 times continuously during pressure measurement, average as measured value.

4, result of the test: as shown in table 1.

Table 1 respectively group rat tail artery systolic pressure change

Group	Number of cases	Tail systolic arterial pressure (mmHg)	Heart rate (secondary/min)
				Normal group	10	108.28±10.66	390±26
Model control group	10	180.64±15.82 ^**	466±20 ^**
				Positive controls	10	148.66±11.80 ^△	410±20 ^△
Low dose group	10	135.12±10.12 ^△△	416±24 ^△
				Middle dosage group	10	125.70±9.04 ^△△#	394±20 ^△
High dose group	10	110.24±10.12 ^△△##	378±16 ^△△#

Note: compare with Normal group, ^*p0.01; Compare with model control group, ^△p0.05, ^{△ △}p0.01; Compare with positive controls, ^#p0.05, ^##p0.01.

5, conclusion (of pressure testing)

The experimentation display of medicine composite for curing original hypertensive rat of the present invention, pharmaceutical composition of the present invention significantly can reduce the blood pressure (P0.01) of essential hypertension rat model, and wherein the middle dosage group of pharmaceutical composition of the present invention and the antihypertensive effect of high dose group are all significantly better than positive controls (P0.05).Simultaneously, pharmaceutical composition of the present invention also possesses the effect of the essential hypertension rat model heart rate that slows down, the effect of low dose group and middle dosage group is suitable with positive controls, and the action effect of high dose group compares the difference (P0.05) with significance with positive controls.

To sum up, it is obvious that pharmaceutical composition of the present invention is used for the treatment of essential hypertension antihypertensive effect, and therapeutic effect is remarkable, has very large clinical value.

Test two: the clinical trial of pharmaceutical composition of the present invention

(1) diagnostic criteria and study subject are selected

The content of " diagnosis basis of hypertension " of reference " Chinese hypertension prevention and control guide " (revised edition in 2010) and " new Chinese medicine guideline of clinical investigations " is drafted.

1, Western medicine diagnose standard, in table 2.

The definition of table 2 blood pressure level and classification

When not using antihypertensive drugs, non-3 Measure blood pressures on the same day, systolic pressure >=140mmHg and/or diastolic pressure >=90mmHg, can be diagnosed as essential hypertension.

2, TCM syndrome diagnostic criteria

1) overabundant liver-fire syndrome

Primary symptom: dizzy, headache, being irritable and getting angry easily.

Secondary disease: flushing, conjunctival congestion, xerostomia, bitter taste, constipation, urinate red, red tongue with yellow fur, wiry and frequent pulse.

2) syndrome of hyperactivity of yang due to yin deficiency

Primary symptom: dizzy, headache, the soreness of waist, knee joint are soft, dysphoria with feverish sensation in the chest palms and soles.

Secondary disease: cardiopalmus, insomnia, tinnitus, the few tongue of forgetful, red tongue, stringy and thready pulse and counting.

3) phlegm-damp stops up Sheng card

Primary symptom: dizzy, headache, head as wrapped up in, uncomfortable in chest, vomiting expectorant birth.

Secondary disease: cardiopalmus, insomnia, tastelessness, lack of appetite, enlarged tongue greasy fur, rolling pulse.

4) deficiency syndrome of both YIN and YANG

Primary symptom: dizzy, headache, the soreness of waist, knee joint are soft, aversion to cold and cold limbs.

Secondary disease: tinnitus, cardiopalmus, breathe hard, nocturia frequency, pale tongue with white fur, deep pulse be thin and delicate.

Meet hypertension Western medicine diagnose standard and TCM syndrome diagnostic criteria, non-medication, or take hypertension drug but drug withdrawal after two weeks, obtained Informed Consent Form person, can include test case between 18 ~ 65 years old the age.

3, get rid of and reject case standard

1) secondary hypertension;

2) age is at under-18s or over-65s, trimester of pregnancy or women breast-feeding their children, or those who are allergic to this drug;

3) the severe primary diseases such as cardiovascular and cerebrovascular vessel, Liver and kidney and hemopoietic system are associated with, psychotic;

4) do not meet inclusive criteria, not by regulation medication, cannot judge that curative effect or data do not affect the treatment or safety judgement person entirely.

(2) clinical trial protocol

1, physical data

The clinical volunteers patient that 400 examples meet essential hypertension diagnostic criteria is obtained, man 220 example, female 180 example, 30 ~ 65 years old age, 50 years old mean age by diagnosis standard screening.Treatment A group, treatment B group, treatment C group and matched group four groups is divided into by random, double blinding, principle that is parallel, contrast, often organize each 100 examples, two groups of patients the influence factor such as sex, age, sick kind, state of an illness distribution, through statistical procedures, there was no significant difference, meets a point set condition.

2, trial drug and test method

Treatment group: respectively as treatment A, B, C group, treatment A group takes granule prepared by the embodiment of the present invention 1, treatment B group takes capsule prepared by the embodiment of the present invention 2, treatment C group takes tablet prepared by the embodiment of the present invention 3, one day three times, each 2g, was a course for the treatment of with 4 weeks, evaluates curative effect after 3 courses for the treatment of.

Matched group: control drug is kendir pressure-reducing sheet (the accurate word Z20093153 of traditional Chinese medicines, No. 2 TCM Factory), and one day three times, each 2g, was a course for the treatment of with 4 weeks, evaluates curative effect after 3 courses for the treatment of.

3, curative effect determinate standard

Effective: 1) diastolic pressure more than decline 10mmHg, and reach normal range; 2) though diastolic pressure is not down to normally but decline 20mmHg or more.Wherein 1 must be possessed.

Effective: 1) diastolic pressure declines not as good as 10mmHg, but reaches normal range; 2) diastolic pressure comparatively treats the front 10 ~ 19mmHg that declines, but does not reach normal range; 3) systolic pressure comparatively treats front more than decline 30mmHg.Wherein 1 must be possessed.

Invalid: not reach above standard person.

4, therapeutic outcome, as shown in table 3.

Table 3 therapeutic effect

Group	Number of cases	Effective (rate)	Effectively	Invalid	Total effective rate
						Matched group	100	52(52％)	32	16	84％
Treatment A group	100	79(79％)	16	5	95％
						Treatment B group	100	78(78％)	16	6	94％
Treatment C group	100	82(82％)	14	4	96％

5, conclusion (of pressure testing)

Clinical testing data shows, and pharmaceutical composition of the present invention is remarkable for essential hypertension therapeutic effect, and average obvious effective rate is 79.67%, and average total effective rate is 95.00%, and the total effective rate being significantly higher than contrast medicine is 84%.Treatment C group, the total effective rate of medicine composite for curing essential hypertension of the present invention that namely embodiment 3 prepares reaches 96%, is the optimal technical solution of pharmaceutical composition of the present invention.The clinical symptoms such as clinical observation finds, after taking two courses for the treatment of of pharmaceutical composition of the present invention, patients' blood obviously declines, dizzy, headache also obviously alleviate, and treatments period has no any untoward reaction.Clinical trial proves, pharmaceutical composition antihypertensive effect of the present invention is remarkable, and drug safety is high, and can be used as the drug use for the treatment of essential hypertension, clinical generalization value is high.

Claims

1. treat a pharmaceutical composition for essential hypertension, it is characterized in that, described pharmaceutical composition is prepared from primarily of the raw material of following parts by weight:

2. pharmaceutical composition as claimed in claim 1, it is characterized in that, described pharmaceutical composition is prepared from primarily of the raw material of following parts by weight:

3. pharmaceutical composition as claimed in claim 1, it is characterized in that, described pharmaceutical composition is prepared from primarily of the raw material of following parts by weight:

4. pharmaceutical composition as claimed in claim 1, it is characterized in that, described pharmaceutical composition is prepared from primarily of the raw material of following parts by weight:

5. the pharmaceutical composition as described in as arbitrary in claim 1-4, it is characterized in that, described pharmaceutical composition is granule, pill, powder, tablet, capsule or oral liquid.

6. the preparation method of the pharmaceutical composition as described in as arbitrary in claim 1-4, it is characterized in that, described preparation method comprises the following steps:

7. the purposes of pharmaceutical composition as claimed in claim 1 in preparation treatment essential hypertension medicine.