CN102283913A - Radix aconiti carmichaeli extract and application thereof - Google Patents
Radix aconiti carmichaeli extract and application thereof Download PDFInfo
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- CN102283913A CN102283913A CN2011102639410A CN201110263941A CN102283913A CN 102283913 A CN102283913 A CN 102283913A CN 2011102639410 A CN2011102639410 A CN 2011102639410A CN 201110263941 A CN201110263941 A CN 201110263941A CN 102283913 A CN102283913 A CN 102283913A
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- radix aconiti
- aconiti lateralis
- lateralis preparata
- decoction
- extract
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- Medicines Containing Plant Substances (AREA)
Abstract
The invention relates to a radix aconiti carmichaeli extract and application thereof. The radix aconiti carmichaeli extract is prepared by comprising the following steps of: sufficiently decocting raw radix aconiti carmichaeli by using water, and taking decoction liquid; continuously and sufficiently decocting residual decoction dreg by using acid water with the pH value of less than or equal to 4, and taking decoction liquid; mixing the decoction liquid in two steps, adding ethanol, standing after the alcohol volume proportion of the mixed liquid is up to 50-80%, carrying out solid-liquid separation, and removing ethanol in the liquid. According to the extract disclosed by the invention, no poisonous component of double ester type alkaloids exists; the extract not only has low toxicity but also is advantageous for stabilizing single ester type alkaloids of a main active component, reducing damaged loss and well playing the pharmacodynamic effect of the radix aconiti carmichaeli; and the extract can be widely applied in anti-inflammatory, analgesia or recuperation vitality pharmaceutical preparations prepared from effective pharmaceutical components of the radix aconiti carmichaeli, including the pharmaceutical preparations, such as traditional Shenfu decoction, Sini decoction, ginseng Sini decoction and the like.
Description
Technical field
The present invention relates to a kind of Radix Aconiti Lateralis Preparata extract and application thereof, can comprise that shenfu decoction, decoction for Resuscitation, Radix Ginseng decoction for Resuscitation and cold limbs class side etc. have extensive use in the pharmaceutical preparation of antiinflammatory, analgesia or recuperating depleted YANG and rescuing the patient from collapse effect.
Background technology
Radix Aconiti Lateralis Preparata be Ranunculaceae herbaceos perennial Aconitum carmichjaelii Debx. (
Aconitum carmichaeli Debx) processed goods of daughter root, the beginning is stated from Shennong's Herbal, acrid-sweet flavor, and extremely hot in nature, poisonous, GUIXIN, kidney, spleen channel are the representative of toxic herb.Have recuperating depleted YANG and rescuing the patient from collapse, mend effect fiery supporing yang, dispersing cold for relieving pain, be considered as mending the supporing yang key medicine of fire, also be described as " the recuperating depleted YANG and rescuing the patient from collapse first product medicine " by ancient Chinese medicine doctor.But fiery and forthright fast because of Radix Aconiti Lateralis Preparata, ancient Chinese medicine doctor and herbal works are all sayed Radix Aconiti Lateralis Preparata " poisonous ", " very toxic ", and be improper with it, is prone to serious toxic and side effects, and therefore, modern clinical decoction generally uses Radix Aconiti Lateralis Preparata, and fries in shallow oil attenuation for a long time.In the final drug preparation, generally also use Radix Aconiti Lateralis Preparata to be used as medicine, but in the Zhang Zhongjing treatise on Febrile Diseases cold limbs class side as the usefulness of all making a living of the Radix Aconiti Lateralis Preparata in the 8 first prescriptions such as zingiberis and Acniti Praeparatae Decoction, decoction for Resuscitation, Radix Ginseng decoction for Resuscitation.
Main poison/effect the composition of Radix Aconiti Lateralis Preparata is alkaloid, comprise diester-type alkaloids (as aconitine, mesaconitine, hypaconitine etc.), monoester alkaloid (as benzoyl aconine, Benzoylmesaconine, benzoyl hypo-aconine etc.) and hydramine type alkaloid (as aconine, new aconine, inferior aconine etc.), contain a spot of lipid alkaloid (lipo-alkaloid) in addition, as lipoaconitine, lipomesaconitine, lipohypaconitine etc.The white more report that waits adopts high performance liquid chromatography and electro spraying ionization-mass spectrometry technology, Analysis and Identification goes out 48 compositions from give birth to Radix Aconiti Lateralis Preparata, wherein diester-type alkaloids 8 (main component), 7 of monoester alkaloids, lipid alkaloid 29 (chemical journal, 2008,66 (2): 211-215).
Known now, the toxic component of Radix Aconiti Lateralis Preparata is mainly diester-type alkaloids, and its toxicity is directly related with the ester bond in the structure.This type of alkaloidal ester bond instability, heating hydrolysis can make its fracture.In the concocting process of Radix Aconiti Lateralis Preparata, at first be that the acetyl group that hydrolysis is fallen on 8 of the aconitines generates benzoyl aconine, its toxicity is 1/200 of aconitine; Further its benzoyl of 14 generation aconine is fallen in hydrolysis again, and its toxicity only is 1/2000 of aconitine; Also follow the generation deoxygenation simultaneously, generate talastisamine.Similar reaction also can take place in mesaconitine, hypaconitine.In addition, the acetyl group on 8 of the aconitine-type alkaloidses also can be generated the less lipid alkaloid (lipo-alkaloid) of toxicity by some fatty acyl groups displacements, and Radix Aconiti Lateralis Preparata makes alkaloid destroyed and run off in concocting process, thereby toxicity is reduced.
Radix Aconiti Lateralis Preparata is a toxic herb, can reach the purpose of attenuation by the above-mentioned process of preparing Chinese medicine.Experiment shows that Radix Aconiti Lateralis Preparata is through the above-mentioned process of preparing Chinese medicine, and the total alkaloids more than 80% can run off in the process of steeping, soaking, floating, and also can further make the diester-type alkaloids hydrolysis be converted into monoester type and hydramine type alkaloid through steaming again.Consequently, though toxicity reduces greatly, its pharmacologically active also weakens thereupon or disappears.Therefore, the process of preparing Chinese medicine of Radix Aconiti Lateralis Preparata has excessive suspicion.
Publication number CN1935201A Chinese patent has been reported a kind of Radix Aconiti Lateralis extract, gets the Radix Aconiti Lateralis pharmaceutical decocting piece, adds 9 ~ 11 times of water gagings for the first time, soaks 20 ~ 40 minutes, decocted 5.5 ~ 6.5 hours, and added 9 ~ 11 times of water gagings for the second time, decocted 3.5 ~ 4.5 hours, filter, concentrate, drying, promptly.
Wu Ping has reported a kind of extraction separation purification process (Chengdu University of Traditional Chinese Medicine's master thesis, 2007) of Radix Aconiti Lateralis Preparata alkaloid, with the Radix Aconiti Lateralis acid extraction, extracting solution adsorbs through macroporous resin column, wash decontamination earlier with water, reuse 60% ethanol elution is collected eluent, reclaim ethanol, medicinal liquid hydrolysis 2 hours under 120 ℃ and 0.2Mpa condition, medicinal liquid is regulated pH value to 10 ~ 11 with ammonia after the hydrolysis, uses ethyl acetate extraction, reclaim ethyl acetate, promptly get the Radix Aconiti Lateralis Preparata alkaloid extract.
Because Radix Aconiti Lateralis Preparata makes the total alkaloids loss of active ingredients can reach more than 80% in the processing concocting process, water miscible effective ingredient has lost totally substantially, pharmacologically active is weakened greatly, therefore there are many defectives in the use of the process of preparing Chinese medicine of Radix Aconiti Lateralis Preparata processing at present and Radix Aconiti Lateralis Preparata, makes the drug action as being used as medicine with Radix Aconiti Lateralis Preparata in the pharmaceutical preparatioies such as shenfu decoction (SHENFU ZHUSHEYE), Chinese Pharmacopoeia decoction for Resuscitation be subjected to influence.
Summary of the invention
At above-mentioned situation, the invention provides a kind of Radix Aconiti Lateralis Preparata extract that contains monoester alkaloid, do not contain hypertoxic composition diester-type alkaloids, not only toxicity is little, and can bring into play the drug action of Radix Aconiti Lateralis Preparata better.The pharmaceutical preparation with antiinflammatory, analgesia or recuperating depleted YANG and rescuing the patient from collapse effect that this extract can prepare at the active drug composition with Radix Aconiti Lateralis Preparata is included in the pharmaceutical preparatioies such as traditional shenfu decoction, decoction for Resuscitation, Radix Ginseng decoction for Resuscitation and is used widely.
Radix Aconiti Lateralis Preparata extract of the present invention is to prepare by following mode:
1': after the Radix Aconiti Lateralis water fully decocted, get decoction liquor.Radix Aconiti Lateralis wherein can be Radix Aconiti Lateralis pharmaceutical decocting piece or its coarse powder of routine;
2': after abundant decoction of sour water continuation of residue medicinal residues with pH value≤4, get decoction liquor;
3': merge last two step decoction liquor, add ethanol, make and left standstill after containing of mixed liquor, pure ratio reached 50% ~ 80%(v/v), solid-liquid separation, liquid concentrates after removing ethanol, is said Radix Aconiti Lateralis Preparata extract.
Said abundant decoction in the above-mentioned preparation method can be undertaken by mode currently reported and/or that use, for example according to the moisture degree of Radix Aconiti Lateralis, generally uses the decocting of 5 ~ 15 times of Radix Aconiti Lateralis weight to boil and gets final product in 1 ~ 4 hour.Radix Aconiti Lateralis fully decocts through water, can make wherein contained diester-type alkaloids hydrolysis be converted into monoester alkaloid, plays Attenuation.
As above-mentioned, fully soak back reuse decocting as first water before Radix Aconiti Lateralis decocts and boil, can shorten decocting time, the abundant stripping and the hydrolysis that help diester-type alkaloids transform, and also help the extraction of monoester alkaloid.Experiment shows that the immersion of Radix Aconiti Lateralis before decoction generally can be no more than 10 hours.For example can soak 1 ~ 4 hour in summer, winter, soak time can proper extension to 5 ~ 10 hour.
Above-mentioned Radix Aconiti Lateralis is soaked and/or decocts, when particularly decocting, generally should maintain enough water yields, but hypervolia also can increase the burden of subsequent treatment.Experiment shows, when immersion and/or decoction, preferably uses the decocting of 5 ~ 15 times of Radix Aconiti Lateralis weight to boil 1 ~ 4 hour.
Experiment shows, Radix Aconiti Lateralis through water fully decoct and solid-liquid separation after medicinal residues, the reuse sour water decocts, can not only make the further hydrolysis of lipid alkaloid in the Radix Aconiti Lateralis Preparata be converted into monoester alkaloid, and help the stable of monoester alkaloid, reduce to decoct and to be subjected to the failure loss of monoester alkaloid in the thermal process, thereby can extract and obtain more monoester alkaloid.Wherein preferred mode is to use the sour water of 5 ~ 15 times of Radix Aconiti Lateralis weight to decoct each 1 ~ 4 hour 1 ~ 2 time.The sour water of said pH value≤4 can wherein preferably use aqueous hydrochloric acid solution for the aqueous acids commonly used such as hydrochloric acid, sulphuric acid or citric acid that allow in the pharmacy to use, and conveniently is easy to get.
After the decoction liquor that decocting and sour water were fried in shallow oil for two steps merge, add ethanol and contain pure ratio, staticly settle after fully stirring, then through solid-liquid separation to said, can remove invalid components or impurity such as destarching, polysaccharide, extract effective active composition based on monoester alkaloid.Liquid after the solid-liquid separation, can regulate pH value earlier to 4-7 by acceptable usual manner in the pharmacy, decompression recycling ethanol is with concentrated again, and promptly obtaining with the monoester alkaloid is the said Radix Aconiti Lateralis Preparata extract of the present invention of main active (not containing diester-type alkaloids).
On this basis,, save ethanol consumption and convenient the processing, after water decoction and sour water decoction liquor merge, can add Ethanol Treatment by said mode again according to after handling needs and earlier the medicinal liquid that merges suitably being concentrated for reducing the medicine liquid volume when the Ethanol Treatment.Because the medicinal liquids after two steps, decoction liquor merged still are acid, experiment shows, helps effective ingredient such as monoester alkaloid under the acid condition and is subjected to thermally-stabilised.Being concentrated into relative density generally speaking is about 1.10 ~ 1.30 and gets final product.
Owing to do not contain hypertoxic composition diester-type alkaloids in the above-mentioned Radix Aconiti Lateralis Preparata extract of the present invention, not only toxicity is little, and preparation process helps monoester alkaloid stable of main active, reduced its ruined loss, can bring into play the drug action of Radix Aconiti Lateralis Preparata better.Thereby this extract comprises in the pharmaceutical preparatioies such as traditional shenfu decoction (Radix Ginseng, Radix Aconiti Lateralis Preparata), decoction for Resuscitation (Radix Aconiti Lateralis Preparata, Rhizoma Zingiberis, Radix Glycyrrhizae Preparata), Radix Ginseng decoction for Resuscitation (Radix Aconiti Lateralis Preparata, Rhizoma Zingiberis, Radix Glycyrrhizae Preparata, Radix Ginseng) and cold limbs class side and being used widely in the pharmaceutical preparation with antiinflammatory, analgesia or recuperating depleted YANG and rescuing the patient from collapse effect that the active drug composition with Radix Aconiti Lateralis Preparata prepares.
The specific embodiment by the following examples is described in further detail foregoing of the present invention again.But this should be interpreted as that the scope of the above-mentioned theme of the present invention only limits to following example.Do not breaking away under the above-mentioned technological thought situation of the present invention, various replacements or change according to ordinary skill knowledge and customary means are made all should comprise within the scope of the invention.
The specific embodiment
Embodiment 1
Get Radix Aconiti Lateralis decoction pieces 100kg, add 10 times in water, soaked 10 hours, decocted 1 hour, filter, decocting liquid is standby; Medicinal residues add 8 times of the aqueous hydrochloric acid solutions of pH 1 again, decoct each 4 hours 2 times, filter, merge decocting liquid, be concentrated into relative density and be about 1.2, adding ethanol makes and contains alcohol amount and reach 70%, fully stir, leave standstill solid-liquid separation, with sodium hydrate aqueous solution adjust pH to 4, decompression recycling ethanol concentrates, and promptly gets described Radix Aconiti Lateralis Preparata extract.
Embodiment 2
Get Radix Aconiti Lateralis and be ground into coarse powder 100kg, add 15 times in water, soaked 6 hours, decocted 1.5 hours, filter, decocting liquid is standby; Medicinal residues add 5 times of the aqueous hydrochloric acid solutions of pH 1.5 again, decoct each 3 hours 2 times, filter, merge decocting liquid, be concentrated into relative density and be about 1.1, adding ethanol makes and contains alcohol amount and reach 80%, fully stir, leave standstill solid-liquid separation, with sodium hydrate aqueous solution adjust pH to 6, decompression recycling ethanol concentrates, and promptly gets described Radix Aconiti Lateralis Preparata extract.
Embodiment 3
Get Radix Aconiti Lateralis decoction pieces 100kg, add 5 times in water, soaked 1 hour, decocted 3 hours, filter, decocting liquid is standby; Medicinal residues add respectively again pH 1 and pH 3 aqueous hydrochloric acid solution each 8 times, decoct each 2 hours 2 times, filter, merge decocting liquid, be concentrated into relative density and be about 1.3, adding ethanol makes and contains alcohol amount and reach 50%, fully stir, leave standstill solid-liquid separation, with sodium hydrate aqueous solution adjust pH to 7, decompression recycling ethanol concentrates, and promptly gets described Radix Aconiti Lateralis Preparata extract.
Embodiment 4
Get Radix Aconiti Lateralis and be ground into coarse powder 100kg, add 15 times in water, soaked 3 hours, decocted 2 hours, filter, decocting liquid is standby; Medicinal residues add 15 times of the aqueous hydrochloric acid solutions of pH 2 again, decoct 3 hours, filter, and merge decocting liquid, be concentrated into relative density and be about 1.25, add ethanol and make and contain alcohol amount and reach 60%, fully stir, leave standstill, solid-liquid separation, decompression recycling ethanol concentrates, and promptly gets described Radix Aconiti Lateralis Preparata extract.
Embodiment 5
Get Radix Aconiti Lateralis decoction pieces 100kg, add 8 times in water, decocted 4 hours, filter, decocting liquid is standby; Medicinal residues add respectively again pH 0.5 and pH 4 aqueous hydrochloric acid solution each 10 times, decoct each 1 hour 2 times, filter, merge decocting liquid, be concentrated into relative density and be about 1.2, adding ethanol makes and contains alcohol amount and reach 70%, fully stir, leave standstill solid-liquid separation, with the sodium hydrate aqueous solution adjust pH to 4-6, decompression recycling ethanol concentrates, and promptly gets described Radix Aconiti Lateralis Preparata extract.
Embodiment 6
Give birth to Radix Aconiti Lateralis Preparata 10kg, add 10 times in water, soaked 4 hours, decocted 2 hours, filter, decocting liquid is standby; Medicinal residues add respectively again pH 1 and pH 3 aqueous hydrochloric acid solution each 8 times, decoct each 2 hours 2 times, filter, merge decocting liquid, be concentrated into relative density and be about 1.2, adding ethanol makes and contains alcohol amount and reach 60%, fully stir, leave standstill solid-liquid separation, with sodium hydrate aqueous solution adjust pH to 5, decompression recycling ethanol concentrates, and promptly gets described Radix Aconiti Lateralis Preparata extract.
Embodiment 7
Give birth to Radix Aconiti Lateralis Preparata 10kg, add 10 times in water, soaked 4 hours, decocted 1 hour, filter, decocting liquid is standby; Medicinal residues add respectively again pH 1 and pH 3 aqueous hydrochloric acid solution each 8 times, decoct each 4 hours 2 times, filter, merge decocting liquid, be concentrated into relative density and be about 1.2, adding ethanol makes and contains alcohol amount and reach 60%, fully stir, leave standstill solid-liquid separation, with sodium hydrate aqueous solution adjust pH to 5, decompression recycling ethanol concentrates, and promptly gets described Radix Aconiti Lateralis Preparata extract.
Embodiment 8
Get Radix Ginseng (Radix Ginseng Rubra) 2.5 ~ 5kg, add 50% ~ 80% ethanol of 5 ~ 12 times of amounts of its weight, reflux, extract, 2 ~ 3 times, each 1 ~ 2 hour, filter, merge ethanol extraction, reclaim under reduced pressure eliminates ethanol, cross macroporous adsorptive resins (D101 or HPD-100), wash remove impurity earlier with water, reuse 50-70% ethanol elution, collect ethanol elution, decompression recycling ethanol concentrates, and promptly obtains Radix Ginseng extract.
Get the Radix Aconiti Lateralis Preparata extract (being equivalent to crude drug raw material 5kg) of embodiment 7, add above-mentioned Radix Ginseng extract, mix homogeneously, it is an amount of to add pharmaceutic adjuvant again, mixing, drying is pulverized, and makes capsule or tablet according to a conventional method, promptly obtains the attached pharmaceutical preparation of described ginseng.
Below be evaluation index by content of effective and drug action, further specify the beneficial effect that Radix Aconiti Lateralis Preparata extract of the present invention has.
Respectively with embodiment 6 and embodiment 7 Radix Aconiti Lateralis Preparata extract as preparation method of the present invention
IAnd Radix Aconiti Lateralis Preparata extract
IICarry out the detection and the efficacy trial of following effective ingredient.
The traditional preparation process method:
Get each 10kg of living Radix Aconiti Lateralis Preparata or Radix Aconiti Lateralis Preparata, add 10 times in water respectively, soaked 4 hours, decocted 2 hours, filter, decocting liquid is standby; Medicinal residues add 8 times in water more respectively, decoct 2 times, and each 2 hours, filter, merge decocting liquid, be concentrated into relative density and be about 1.2, add ethanol and make and contain alcohol amount and reach 60%, fully stir, leave standstill, solid-liquid separation, decompression recycling ethanol concentrates, and promptly gets Radix Aconiti Lateralis extract or Radix Aconiti Lateralis Preparata extract.
Bibliographical information method (publication number CN1935201A Chinese patent):
Give birth to Radix Aconiti Lateralis Preparata 10kg, add 10 times in water, soaked 40 minutes, decocted 6 hours, filter, decocting liquid is standby; Medicinal residues add 10 times in water again, decoct 4 hours, filter, and merge decocting liquid, concentrate, and promptly get the Radix Aconiti Lateralis Preparata extract of publication number CN1935201A Chinese patent.
1, content of effective is measured
With reference to the diester-type under 177 pages of Radix Aconiti Lateralis Preparata items of Chinese Pharmacopoeia version in 2010 and the detection method of monoester alkaloid, measure respectively Radix Aconiti Lateralis Preparata extract (
I)(embodiment 6), Radix Aconiti Lateralis Preparata extract (
II) (Embodiment 7), the Radix Aconiti Lateralis extract of traditional preparation process method, Radix Aconiti Lateralis Preparata extract, and the content of mesaconitine, aconitine, hypaconitine, Benzoylmesaconine, benzoyl aconine and benzoyl hypo-aconine in the Radix Aconiti Lateralis Preparata extract of bibliographical information method, the results are shown in Table 1.
Assay result (the gg of diester-type and monoester alkaloid in table 1 Radix Aconiti Lateralis Preparata extract
-1, in crude drug)
Annotate: "-" be not for detecting
2, analgesic experiment
Get 50 of mices, male and female half and half are divided into 5 groups, i.e. normal control group, Radix Aconiti Lateralis Preparata extract at random
IRadix Aconiti Lateralis extract group, the Radix Aconiti Lateralis Preparata extract group of group, Radix Aconiti Lateralis Preparata extract II group and traditional preparation process method.Dosed administration was 3 days during each group was pressed and shown, and 1h lumbar injection 1% sodium tartrate 0.2ml/ does not only observe it and turns round the body number of times after time administration, the results are shown in Table 2, shows that Radix Aconiti Lateralis Preparata extract of the present invention has better analgesic activity.
Table 2 Radix Aconiti Lateralis Preparata extract analgesic experiment result
| Group | Dosage (the g crude drug/Kg) | Test Mus number (only) | Turn round body number of times (inferior) |
| Normal control | ? | 10 | 30±10.5 |
| Radix Aconiti Lateralis Preparata extract I of the present invention | 12 | 10 | 13±7.9*** |
| Radix Aconiti Lateralis Preparata extract II of the present invention | 12 | 10 | 10±5.3*** |
| Tradition method for making Radix Aconiti Lateralis extract | 12 | 10 | 15±8.1** |
| Tradition method for making Radix Aconiti Lateralis Preparata extract | 12 | 10 | 18±9.8* |
Annotate: compare with matched group
*P＜0.05,
*P＜0.01,
* *P＜0.001.
3, antiinflammatory experiment
Get 50 of male mices, be divided into 5 groups at random, be i.e. Radix Aconiti Lateralis extract group, the Radix Aconiti Lateralis Preparata extract group of normal control group, Radix Aconiti Lateralis Preparata extract I group, Radix Aconiti Lateralis Preparata extract II group and traditional preparation process method.Dosed administration was 3 days during each group was pressed and shown, only evenly be coated with dimethylbenzene 0.05ml/ for mice left side ear in 40 minutes after the last administration, causing scorching back 30 minutes execution animals, with diameter is that the rustless steel punching pin of 8mm takes off left and right sides same area auricle, weigh, be calculated as follows swelling degree and inhibitory rate of intumesce, the results are shown in 3, show that Radix Aconiti Lateralis Preparata extract of the present invention has better antiinflammatory action.
Swelling degree=(left auricle Chong – auris dextra sheet is heavy)
Table 3 Radix Aconiti Lateralis Preparata extract antiinflammatory action experimental result
| Group | Dosage (the g crude drug/Kg) | Test Mus number (only) | Swelling degree (mg) | Suppression ratio (%) |
| Normal control | ? | 10 | 10.45±2.37 | — |
| Radix Aconiti Lateralis Preparata extract I of the present invention | 12 | 10 | 6.21±2.49 *** | 40.6 |
| Radix Aconiti Lateralis Preparata extract II of the present invention | 12 | 10 | 6.08±2.31 *** | 41.8 |
| Tradition method for making Radix Aconiti Lateralis extract | 12 | 10 | 7.16±2.53 ** | 31.5 |
| Tradition method for making Radix Aconiti Lateralis Preparata extract | 12 | 10 | 7.79±2.46 * | 25.5 |
Annotate: compare with matched group
*P＜0.05,
*P＜0.01,
* *P＜0.001.
4, cold resistance experiment
Reference literature (Li Liji etc., Pharmacology and Clinics of Chinese Materia Medica, 2005,21 (6): 31-33), 100 male and female half and half of mice, be divided into 5 groups at random, successive administration 5 days was put into freezer compartment of refrigerator in 1 hour after time administration,-10 ℃ of half an hour, observe its dead number of elements, the results are shown in Table 4, show that Radix Aconiti Lateralis Preparata extract of the present invention has better cold resistance effect.
Table 4 Radix Aconiti Lateralis Preparata extract is to the influence of mice cold resistant
| Group | Dosage (the g crude drug/Kg) | Test Mus number (only) | Dead Mus number (only) | Survival rate (%) |
| Contrast | ? | 20 | 13 | 35 |
| The Radix Aconiti Lateralis Preparata extract I | 10 | 20 | 4 | 75 |
| The Radix Aconiti Lateralis Preparata extract II | 10 | 20 | 5 | 80 |
| Tradition method for making Radix Aconiti Lateralis extract | 10 | 20 | 7 | 65 |
| Tradition method for making Radix Aconiti Lateralis Preparata extract | 10 | 20 | 10 | 50 |
5, anoxia enduring experiment
50 of mices, male and female half and half are divided into 5 groups at random, successive administration 5 days, after time administration 1 hour, the time of its mouth breathing of broken end observation, the results are shown in Table 5, show that Radix Aconiti Lateralis Preparata extract of the present invention has better resisting oxygen lack.
Table 5 Radix Aconiti Lateralis Preparata extract is to the influence of mice broken end mouth breathing time (x ± s)
| Group | Dosage (the g crude drug/Kg) | Test Mus number (only) | Breathing time (second) |
| Contrast | ? | 10 | 20.0±3.91 |
| Radix Aconiti Lateralis Preparata extract I of the present invention | 10 | 10 | 24.3±2.76 * |
| Radix Aconiti Lateralis Preparata extract II of the present invention | 10 | 10 | 25.2±3.35 ** |
| Tradition method for making Radix Aconiti Lateralis extract | 10 | 10 | 23.3±3.17 |
| Tradition method for making Radix Aconiti Lateralis Preparata extract | 10 | 10 | 22.1±3.04 |
Annotate: compare with matched group
*P＜0.05,
*P＜0.01.
6, control chronic heart failure test
6.1 animal grouping and modeling: get 85 SD rats, male and female half and half after adaptability is fed 3d, are got 10 (male and female half and half) at random as I number group (blank group), tail vein injection equal-volume normal saline.All the other 75 rats are used amycin (ADR) modeling, and every kg/ time/rat is used 4mg, injection in per 5 days 1 time, totally 3 times.Behind the last ADR administration 24h, 2 of picked at random model mouses, sacrificed by decapitation, take out heart, with pre-cooling 0.9% normal saline flushing, get left chamber cardiac muscle part, with 10% formaldehyde fixed, HE dyeing, after light microscopic is observed down and confirmed the modeling success, the more surplus rat of institute is divided at random II number group (heart failure model group), III number group (digoxin treatment group), IV number group (Radix Aconiti Lateralis Preparata extract I group), V number group (Radix Aconiti Lateralis Preparata extract II group), VI number group (traditional method for making Radix Aconiti Lateralis extract group), VII number group (traditional method for making Radix Aconiti Lateralis Preparata extract group).Each is organized equal concentrated feed and feeds, and freely drinks water.
6.2 medication: begin gastric infusion next day after III～VII group modeling, successive administration 21d, and Radix Aconiti Lateralis Preparata is to medicine group 5g crude drug/kg, and digoxin is pressed the 1.6mg/kg administration, and I, II group are irritated stomach with isopyknic normal saline.
6.3 experimental result
(1) general symptom: normal control group (I group) rat hair color gloss, physical agility, outward appearance is normal.The appearance activity successively behind the 1st～3 tail vein injection ADR of all the other 75 rats reduce, roll up, receive decreased food intake few, lose weight, ascites, oliguria loose stool, hypopnea, hair color be withered, lose hair or feathers, become thin etc., the 3rd ADR injects in back 75 rats dead 9, get 2 rats and do the modeling test, all the other 64 rats are divided into 6 groups at random, each 12 of II and VII groups, each 10 of III～VI groups, male and female half and half.Using the administration stage, II, III, IV, V, VI and VII group are distinguished dead 4,3,2,3,3,4 again.Experimental session subsequently, medication group rat are no longer dead, and except that the heart failure model group, other survival rats symptom all has improvement in various degree, and wherein, III～V group doing well,improving obviously is better than VI group and VII group, and heart failure model group symptom does not have obvious improvement.
(2) biochemical analysis and pathological examination: after the administration the 15th day, femoral vein was got blood, respectively with chemical method and put the method for exempting from and measure the level of respectively organizing NO in the rat plasma, serum TNF-α, the results are shown in Table 6 after the processing.Model group NO, TNF-alpha levels be apparently higher than normal control group and each treatment group (P＜0.01), and III～V group NO, TNF-alpha levels are starkly lower than VI group and VII group.
Last sacrificed by exsanguination rat is got left chamber cardiac muscle part, with 10% formaldehyde fixed, and routine paraffin wax embedding, pathological section, HE dyeing, om observation.As seen normal control group myocardial cell form, kytoplasm, a matter and horizontal stroke (indulging) stricture of vagina are all normal, but the heart failure model group exists myocardial cell horizontal stroke (indulging) stricture of vagina unclear, subregion myoplasm fibrolysis, in various degree inflammatory cell infiltration and interstitial edema pathological changes appear in the endochylema vacuolar degeneration.In the administration group, III～above pathological changes of V group has significantly than the heart failure model group and alleviates, and myocardial cell horizontal stroke (indulging) stricture of vagina exists, and obviously is better than VI group and VII group.
Above-mentioned experimental result fully shows, Radix Aconiti Lateralis Preparata extract of the present invention had both made Radix Aconiti Lateralis toxic composition diester-type alkaloids be converted into monoester alkaloid, and makes monoester alkaloid keep stable, has reduced the failure loss of monoester alkaloid.Further effect experiment shows that then Radix Aconiti Lateralis Preparata extract of the present invention has tangible drug action at aspects such as antiinflammatory, analgesia, recuperating depleted YANG and rescuing the patient from collapse, and produces the beyond thought effect that traditional water decocts extract that is better than, and has broad application prospects.
Table 6 I～VII group rat NO, TNF-alpha content change (x ± s)
| Group | n | NO | TNF-α |
| I number group | 10 | 9.46±0.25 | 0.72±0.29 |
| II number group | 8 | 63.37±0.94 | 1.52±0.16 |
| III number group | 7 | 11.83±0.31 *** | 0.84±0.30 *** |
| VI number group | 8 | 18.52±0.27 *** | 0.93±0.24 *** |
| V number group | 7 | 15.74±0.36 *** | 0.89±0.21 *** |
| IV number group | 7 | 31.35±0.54 *** | 0.97±0.28 ** |
| VII number group | 8 | 38.26±0.65 *** | 1.01±0.37 ** |
Annotate: compare with model group
*P＜0.01,
* *P＜0.001.
Claims (9)
1. Radix Aconiti Lateralis Preparata extract is characterized in that preparing by following mode:
1': after the Radix Aconiti Lateralis water fully decocted, get decoction liquor;
2': after abundant decoction of sour water continuation of residue medicinal residues with pH value≤4, get decoction liquor;
3': merge last two step decoction liquor, add ethanol, make and left standstill after containing of mixed liquor, pure volume ratio reached 50 ~ 80%, solid-liquid separation, liquid concentrates after removing ethanol, is said Radix Aconiti Lateralis Preparata extract.
2. Radix Aconiti Lateralis Preparata extract as claimed in claim 1, before the Radix Aconiti Lateralis that it is characterized in that 1' step decocted, first water fully soaked back reuse decocting and boils.
3. Radix Aconiti Lateralis Preparata extract as claimed in claim 2 is characterized in that said Radix Aconiti Lateralis soak time is≤10 hours.
4. as the described Radix Aconiti Lateralis Preparata extract of one of claim 1 to 3, it is characterized in that the decocting that the Radix Aconiti Lateralis in 1' step decocts with 5 ~ 15 times of its weight boiled 1 ~ 4 hour.
5. as the described Radix Aconiti Lateralis Preparata extract of one of claim 1 to 3, it is characterized in that 2' in the step sour water of pH value≤4 be aqueous hydrochloric acid solution.
6. Radix Aconiti Lateralis Preparata extract as claimed in claim 5 is characterized in that the 2' step decocts each 1 ~ 4 hour 1 ~ 2 time with the sour water of 5 ~ 15 times of Radix Aconiti Lateralis weight.
7. as the described Radix Aconiti Lateralis Preparata extract of one of claim 1 to 3, it is characterized in that decocting boil decoct two step decoction liquor and merge with sour water after, be concentrated into relative density 1.10 ~ 1.30 earlier after, add Ethanol Treatment again.
8. the application of the Radix Aconiti Lateralis Preparata extract of one of claim 1 to 7 in the pharmaceutical preparation that the active drug composition with Radix Aconiti Lateralis Preparata prepares with antiinflammatory, analgesia or recuperating depleted YANG and rescuing the patient from collapse effect.
9. application as claimed in claim 8 is characterized in that being used to prepare shenfu decoction, decoction for Resuscitation, Radix Ginseng decoction for Resuscitation and the pharmaceutical preparation of cold limbs class side.
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Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103405525A (en) * | 2013-08-09 | 2013-11-27 | 四川省中医药科学院 | Composition and medicine for strengthening heart and preventing and curing chronic heart failure and preparation method |
| CN105326925A (en) * | 2015-11-05 | 2016-02-17 | 西南科技大学 | Rapid extraction method of radix aconite lateralis preparata total alkaloids |
| CN109674793A (en) * | 2019-03-05 | 2019-04-26 | 上海市第一妇婴保健院 | Benzoylmesaconine, benzoyl aconine, benzoyl time aconine are preparing the application in cardiotonic agents |
| CN110448603A (en) * | 2019-08-05 | 2019-11-15 | 中国人民解放军总医院第五医学中心 | A kind of method for extraction and purification of monkshood |
| CN115944672A (en) * | 2023-02-09 | 2023-04-11 | 广东心宝药业科技有限公司 | Radix aconiti lateralis praeparata extract and application thereof |
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| CN1689593A (en) * | 2004-04-29 | 2005-11-02 | 哈药集团中药二厂 | Method for preparing ginseng and aconite powdered injection |
| CN1951432A (en) * | 2005-09-13 | 2007-04-25 | 山东绿叶天然药物研究开发有限公司 | Gingseng and aconite composition, its preparation, preparation process and usage |
| CN101357167A (en) * | 2008-09-12 | 2009-02-04 | 中国科学院长春应用化学研究所 | Method for increasing monoester alkaloid content in aconitum plant extract |
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Patent Citations (3)
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| CN1689593A (en) * | 2004-04-29 | 2005-11-02 | 哈药集团中药二厂 | Method for preparing ginseng and aconite powdered injection |
| CN1951432A (en) * | 2005-09-13 | 2007-04-25 | 山东绿叶天然药物研究开发有限公司 | Gingseng and aconite composition, its preparation, preparation process and usage |
| CN101357167A (en) * | 2008-09-12 | 2009-02-04 | 中国科学院长春应用化学研究所 | Method for increasing monoester alkaloid content in aconitum plant extract |
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| 李书华等: "附子中生物碱正交提取工艺和吸附树脂的筛选研究", 《中成药》 * |
Cited By (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103405525A (en) * | 2013-08-09 | 2013-11-27 | 四川省中医药科学院 | Composition and medicine for strengthening heart and preventing and curing chronic heart failure and preparation method |
| CN105326925A (en) * | 2015-11-05 | 2016-02-17 | 西南科技大学 | Rapid extraction method of radix aconite lateralis preparata total alkaloids |
| CN105326925B (en) * | 2015-11-05 | 2019-10-11 | 西南科技大学 | A kind of rapid extracting method of Radix Aconiti Lateralis Preparata total alkaloids |
| CN109674793A (en) * | 2019-03-05 | 2019-04-26 | 上海市第一妇婴保健院 | Benzoylmesaconine, benzoyl aconine, benzoyl time aconine are preparing the application in cardiotonic agents |
| CN110448603A (en) * | 2019-08-05 | 2019-11-15 | 中国人民解放军总医院第五医学中心 | A kind of method for extraction and purification of monkshood |
| CN115944672A (en) * | 2023-02-09 | 2023-04-11 | 广东心宝药业科技有限公司 | Radix aconiti lateralis praeparata extract and application thereof |
| CN115944672B (en) * | 2023-02-09 | 2023-06-30 | 广东心宝药业科技有限公司 | Radix aconiti lateralis extract and application thereof |
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| Publication number | Publication date |
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| CN102283913B (en) | 2013-03-27 |
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