CN109381514A - A kind of Baical Skullcap root P.E and combinations thereof and purposes for radiation injury protection - Google Patents
A kind of Baical Skullcap root P.E and combinations thereof and purposes for radiation injury protection Download PDFInfo
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- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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- A61K36/00—Medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicines
- A61K36/18—Magnoliophyta (angiosperms)
- A61K36/185—Magnoliopsida (dicotyledons)
- A61K36/53—Lamiaceae or Labiatae (Mint family), e.g. thyme, rosemary or lavender
- A61K36/539—Scutellaria (skullcap)
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- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/30—Extraction of the material
- A61K2236/33—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones
- A61K2236/333—Extraction of the material involving extraction with hydrophilic solvents, e.g. lower alcohols, esters or ketones using mixed solvents, e.g. 70% EtOH
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- A61K2236/30—Extraction of the material
- A61K2236/39—Complex extraction schemes, e.g. fractionation or repeated extraction steps
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- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/50—Methods involving additional extraction steps
- A61K2236/51—Concentration or drying of the extract, e.g. Lyophilisation, freeze-drying or spray-drying
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2236/00—Isolation or extraction methods of medicinal preparations of undetermined constitution containing material from algae, lichens, fungi or plants, or derivatives thereof, e.g. traditional herbal medicine
- A61K2236/50—Methods involving additional extraction steps
- A61K2236/53—Liquid-solid separation, e.g. centrifugation, sedimentation or crystallization
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Abstract
The invention belongs to technical field of traditional Chinese medicines, it is related to a kind of Baical Skullcap root P.E and combinations thereof and the purposes for radiation injury protection.The Baical Skullcap root P.E is using the method preparation included the following steps: (1) it is one or many that ethyl alcohol progress ultrasonic extraction being added in radix scutellariae；(2) merging filtrate after each ultrasonic extraction liquid of filtering；(3) combined filtrate is concentrated and dried, obtains the Baical Skullcap root P.E.Using Baical Skullcap root P.E and combinations thereof of the invention, there can be obvious better effect when for radiation injury protection.
Description
Technical field
The invention belongs to technical field of traditional Chinese medicines, it is related to a kind of Baical Skullcap root P.E and combinations thereof and is protected for radiation injury
Purposes.
Background technique
With the fast development of nuclear industry and Radiation Medicine, ionising radiation is increasingly taken seriously to the damage of human body.Greatly
Each system of Radiation On Human body of dosage is had damage, and wherein hemopoietic system and immune system are the most significant.Ionising radiation is non-spy
Opposite sex stimulation, acts on body and causes organ, tissue, lymphocyte, eventually leads to function of immune system decline.Due to hematopoiesis system
System and immune system are extremely sensitive to ionising radiation, enhance the protection right and wrong to hemopoietic system and immune system in radiation protection
It is often necessary.Traditional Chinese medicine has in the prevention and treatment of radiation injury to have certain effect.By years of researches, it has been found that have clear
Thermal detoxification, activating microcirculation and removing stasis medicinal, enriching the blood and tonifying qi, yin-nourishing rise white Chinese medicine and have different degrees of radiation resistance, and the traditional Chinese medicine medicinal herbs resource it is wide,
Toxicity is low, it is made to show big advantage and potentiality in the research of radioprotectant.
The mechanism of Chinese medicine Antiradiation injury mainly has the following aspects:
1, free radical and antioxidation are removed.Radiation causes water radiation solution reaction, generates free radicals, mainly has: .OH,
eaq-、O2 -、H2O2、HO2, indirect injury caused by radiation is mainly caused by the free radical that water radiolysis generates, wherein again with .OH
Effect it is most important, there is research to confirm, DNA damage 90% caused by low linear energy transfer ray is as caused by .OH.Therefore,
Radicals scavenging is an importance of anti-radiation research.
2, immune system is protected.Radio-induced immune function change is one of main performance of radiation insult, and leaching is immunized
Bar cell and its immunoregulatory internal organs are participated in, such as marrow, spleen, thymus gland are all high radiation sensitive cell groups.Radiation causes
Immune system damage be mainly manifested in the reduction of immunocyte, immune organ function lowers, so that it is special and non-to influence body
Specific immune function.
3, hemopoietic system is protected.Hematopoietic tissue is high radiation-sensitive tissue, candidate stem cell, grain system progenitor cells, red system ancestral
Cell is the Principle Target of radiation attack, and radiation often results in bone marrow suppression, microcirculation disorder, leucocyte decline and hematopoiesis micro-loop
Equivalent damage is destroyed in border.
Flavone compound scutelloside, baicalein, wogonoside and wogonin in radix scutellariae is because of its design feature,
With the activity for removing free radical.Baicalein and the scavenging hydroxyl of Determination of baicalin dependence, DPPH free radical and alkyl
Free radical, and wogonin and wogonoside are weaker to the scavenging effect of the above free radical.By removing free radical, anti-grease matter mistake
Oxidation and three in vitro tests of reducing power to metallic atom, compare the anti-oxidant energy of four kinds of flavone compounds in radix scutellariae
Power, baicalein show consistent antioxidation to three tests, and baicalein can protect lipid peroxidation；Scutelloside resists
Oxidability is weaker.
Summary of the invention
Primary and foremost purpose of the invention is to provide a kind of Baical Skullcap root P.E, can have when for radiation injury protection
Obvious better effect.
In order to achieve this, the present invention provides a kind of Baical Skullcap root P.E, and the radix scutellariae mentions in the embodiment on basis
Take object using the method preparation included the following steps:
(1) it is one or many that ethyl alcohol progress ultrasonic extraction is added in radix scutellariae；
(2) merging filtrate after each ultrasonic extraction liquid of filtering；
(3) combined filtrate is concentrated and dried, obtains the Baical Skullcap root P.E.
In a preferred embodiment, the present invention provides a kind of Baical Skullcap root P.E, wherein in step (1) ethyl alcohol body
Percent concentration is accumulated as 50-70%, the mass volume ratio of each ultrasonic extraction radix scutellariae and ethyl alcohol is 1:40-70.
In a preferred embodiment, the present invention provides a kind of Baical Skullcap root P.E, wherein ultrasonic extraction in step (1)
Temperature be 60-90 DEG C.
In a preferred embodiment, the present invention provides a kind of Baical Skullcap root P.E, wherein ultrasonic extraction in step (1)
Ultrasonic frequency be 10-30kHz.
In a preferred embodiment, the present invention provides a kind of Baical Skullcap root P.E, wherein ultrasonic extraction in step (1)
Number be 1-3 times.
In a kind of more preferred embodiment, the present invention provides a kind of Baical Skullcap root P.E, wherein in step (1) every time
The time of ultrasonic extraction is 0.5-1.5h.
A second object of the present invention is to provide a kind of pharmaceutical compositions of aforementioned Baical Skullcap root P.E, can be used for spoke
When penetrating injury protection, there is obvious better effect.
In order to achieve this, the present invention provides a kind of medicine group of aforementioned Baical Skullcap root P.E in the embodiment on basis
Object is closed, the pharmaceutically acceptable auxiliaries of a effective amount of Baical Skullcap root P.E and appropriate amount are protected containing radiation injury.
In a preferred embodiment, the present invention provides a kind of pharmaceutical composition of aforementioned Baical Skullcap root P.E, wherein
The dosage form of the pharmaceutical composition is capsule or granule.
Third object of the present invention is to provide a kind of aforementioned Baical Skullcap root P.Es or its pharmaceutical composition to be used to prepare radiation
The purposes of injury protection drug, can there is obvious better effect when for radiation injury protection.
In order to achieve this, the present invention provides a kind of aforementioned Baical Skullcap root P.E or its drug in the embodiment on basis
Composition is used to prepare the purposes of radiation injury protection medicine.
In a preferred embodiment, the present invention provides a kind of aforementioned Baical Skullcap root P.E or its pharmaceutical composition is used for
The purposes of radiation injury protection medicine is prepared, wherein the radiation injury is60The damage of gamma Rays caused by Co.
The beneficial effects of the present invention are can be used for using Baical Skullcap root P.E and its pharmaceutical composition of the invention
When radiation injury is protected, there is obvious better effect.
Baical Skullcap root P.E and its pharmaceutical composition Antiradiation injury significant effect of the invention, composition be easy, convenient to take,
It is highly-safe, adverse reaction is less, be easily accepted by patients.
Mouse is given in the preparatory stomach-filling of Baical Skullcap root P.E of the invention, small then through mouse high-dose irradiation survival experiment
Leukocyte counts and spleen and thymus gland coefficient determination, Mice water maze experiment etc. prove after mouse low dose exposure: the Huang
A kind of reed mentioned in ancient books extract can significantly improve survival rate of the mouse under high-dose irradiation；It is white under low dose exposure to dramatically increase mouse
Cell quantity and spleen, thymus gland coefficient have significant Antiradiation injury effect；Mouse can be significantly improved in low dose exposure
Under cognition dysfunction.Being indicated above the Baical Skullcap root P.E has significant Antiradiation injury to act on.
Specific embodiment
A specific embodiment of the invention is further illustrated with reference to embodiments.
Embodiment 1: the preparation (one) of Baical Skullcap root P.E
The Baical Skullcap root P.E for radiation injury protection is prepared with the following method.
Radix scutellariae 50g is taken, is shredded, the ethyl alcohol 60ml of 60% (v/v) is added according to every gram of medicinal material, under conditions of 70 DEG C,
It is extracted 2 times in 20kHz ultrasound, extracts 1h every time, stood, filtering.Filtrate is taken, is concentrated and dried to get the Baical Skullcap root P.E.
Embodiment 2: the preparation (two) of Baical Skullcap root P.E
The Baical Skullcap root P.E for radiation injury protection is prepared with the following method.
Radix scutellariae 50g is taken, is shredded, the ethyl alcohol 40ml of 70% (v/v) is added according to every gram of medicinal material, under conditions of 60 DEG C,
It is extracted 3 times in 10kHz ultrasound, extracts 0.5h every time, stood, filtering.Filtrate is taken, is concentrated and dried to get the Baical Skullcap root P.E.
Embodiment 3: the preparation (three) of Baical Skullcap root P.E
The Baical Skullcap root P.E for radiation injury protection is prepared with the following method.
Radix scutellariae 50g is taken, is shredded, the ethyl alcohol 70ml of 50% (v/v) is added according to every gram of medicinal material, under conditions of 90 DEG C,
It extracts 1 time, extraction time 1.5h, stands in 30kHz ultrasound, filtering.Filtrate is taken, is concentrated and dried to get the Baical Skullcap root P.E.
Embodiment 4: the high dose radiation injury protection survival rate zoopery of Baical Skullcap root P.E
(1) laboratory apparatus
50mL graduated centrifuge tube (Corning company), and animal irrigation stomach device (Beijing Ji'an get Er Science and Technology Ltd., No. 12
6cm)。
(2) experimental animal
Male ICR mouse (National Institute for Food and Drugs Control, production licence number: SCXK (capital) 2014-0013) 18
~22g.
(3) experimental drug
Trial drug: the Baical Skullcap root P.E of previous embodiment 1-3 preparation.
Positive control drug: amikacin srlfate injection (Dalian Merro Pharmaceutical Co., Ltd., lot number
53120502)。
(4) experimental method
After mouse adaptable fed 1 week, 6 groups are randomly divided into, every group 10, respectively (stomach-filling purifies blank control group
Water), model group (stomach-filling purified water), positive controls (intraperitoneal injection, 400mg/kg), (given low is embodiment 1-3 group
20mg/kg).Each mouse of positive controls and embodiment 1-3 group successive administration 14 days once a day；Blank control group and model
Each mouse stomach-filling purified water (2ml/100g) once a day of group, altogether stomach-filling 14 days.After last dose or stomach-filling purified water 1h, remove
Outside blank control group, remaining each group mouse is passed through60The disposable whole body uniform irradiation of Co gamma-rays, ource-skin Distance 80cm, exposure dose
9.0Gy, exposure dose rate 96.31cGy/min.It is radiated at the completion of affiliated hospital, Chinese Radiation Protection Research Inst radiotherapy department.Record
Survival condition in each group mouse 30 days.(5) experimental result
30 days survival rates: after observation irradiation in 30 days, the survival condition of groups of animals, and calculate 30 days survival rates, be averaged
Survival number of days and protective index.Wherein protective index=((ab+30c)/n)/((a ' b '+30c ')/n '), wherein a, a ' are respectively
The dead mouse average Survival number of days of administration group and model group；B, b ' is respectively the dead mouse number of administration group and model group；c,
C ' is respectively 30 days survival numbers of elements of administration group and model group mouse；N, n ' is respectively administration group and model group total mice.
30 days survival conditions: after 30 day observation period, the survival rate of blank control group animal is 100%, Average Survival
Number of days is 30 days；The survival rate of model group animal is 30%, and average Survival number of days are 13.6 days；The survival of positive controls animal
Rate is 70%, and average Survival number of days are 26.6 days, protective index 1.23；The survival rate of embodiment 1-3 group is respectively 70%,
80%, 80%, Average Survival is respectively 23.6 days, 27.2 days, 26.8 days, and protective index is respectively 1.18,1.28,1.24.
It is above-mentioned the experimental results showed that Baical Skullcap root P.E of the invention can greatly improve mouse by after large dosage of nuclear radiation
Survival rate.
Embodiment 5: the low dose radiation injury protection white blood cell count(WBC) and spleen of Baical Skullcap root P.E, thymus gland coefficient determination are dynamic
Object experiment
(1) laboratory apparatus
50mL graduated centrifuge tube (Corning company), and animal irrigation stomach device (Beijing Ji'an get Er Science and Technology Ltd., No. 12
6cm), the three full-automatic blood counting instruments (Nihon Kohden Corporation, MEK-6318K type) of classification, cellanalyzer are used
Dilution (Shanghai Photoelectricity Medical electron Instrument Co., Ltd., lot number 15050283).
(2) experimental animal
Male ICR mouse (National Institute for Food and Drugs Control, production licence number: SCXK (capital) 2014-0013) 18
~22g.
(3) experimental drug
Trial drug: the Baical Skullcap root P.E of previous embodiment 1-3 preparation.
Positive control drug: amikacin srlfate injection (Dalian Merro Pharmaceutical Co., Ltd., lot number
53120502)。
(4) experimental method
After mouse adaptable fed 1 week, 6 groups are randomly divided into, every group 10, respectively (stomach-filling purifies blank control group
Water), model group (stomach-filling purified water), positive controls (intraperitoneal injection, 400mg/kg), (given low is embodiment 1-3 group
20mg/kg).Each mouse of positive controls and embodiment 1-3 group successive administration 14 days once a day；Blank control group and model
Each mouse stomach-filling purified water (2ml/100g) once a day of group, altogether stomach-filling 14 days.After last dose or stomach-filling purified water 1h, remove
Outside blank control group, remaining each group mouse is passed through60The disposable whole body uniform irradiation of Co gamma-rays, ource-skin Distance 80cm, exposure dose
3.5Gy, exposure dose rate 96.31cGy/min.It is radiated at the completion of affiliated hospital, Chinese Radiation Protection Research Inst radiotherapy department.Irradiation
After the completion, all mouse in addition to blank control group continue administration or stomach-filling purified water 14 days, last dose or stomach-filling purified water
After 1h, weighing, eye socket takes blood, and then cervical dislocation is put to death, and wins spleen and thymus gland and weighs.
(5) experimental result
The white blood cell count(WBC) and spleen and thymus gland coefficient determination of every mouse pass through spss22.0 and carry out t inspection and variance
Analysis, is as a result expressed as average value ± standard deviation, is shown in Table 1,2 respectively.The results showed that
1) mouse immune system by accumulated dose 3.5Gy irradiation is seriously damaged, and is caused quantity of leucocyte to decline, is exempted from
Epidemic disease organ spleen and thymic factor D injection mitigate；
2) the embodiment of the present invention 1-3 group can dramatically increase quantity of leucocyte and dramatically increase the matter of spleen and thymus gland
Amount, and effect and positive drug are close.
Above-mentioned experimental result illustrates that Baical Skullcap root P.E of the invention has protection to make the radiation injury of mouse immune system
With.
Table 1ICR murine interleukin count results
Note: compared with dynamic with model group, P < 0.01 * P < 0.05, * *.
Table 2ICR mouse spleen and thymus gland coefficient determination result
Note: compared with dynamic with model group, P < 0.01 * P < 0.05, * *.
Embodiment 6: the cognitive function zoopery after the low dose radiation irradiation of Baical Skullcap root P.E
(1) laboratory apparatus
50mL graduated centrifuge tube (Corning company), and animal irrigation stomach device (Beijing Ji'an get Er Science and Technology Ltd., No. 12
6cm), rats and mice Morris water maze (Chinese Academy of Medical Sciences, model DMS-2).
(2) experimental animal
Male ICR mouse (National Institute for Food and Drugs Control, production licence number: SCXK (capital) 2014-0013) 18
~22g.
(3) experimental drug
Trial drug: the Baical Skullcap root P.E of previous embodiment 1-3 preparation.
Positive control drug: amikacin srlfate injection (Dalian Merro Pharmaceutical Co., Ltd., lot number 53120502).
(4) experimental method
After mouse adaptable fed 1 week, 6 groups are randomly divided into, every group 10, respectively (stomach-filling purifies blank control group
Water), model group (stomach-filling purified water), positive controls (intraperitoneal injection, 400mg/kg), (given low is embodiment 1-3 group
20mg/kg).Each mouse of positive controls and embodiment 1-3 group successive administration 14 days once a day；Blank control group and model
Each mouse stomach-filling purified water (2ml/100g) once a day of group, altogether stomach-filling 14 days.After last dose or stomach-filling purified water 1h, remove
Outside blank control group, remaining each group mouse is passed through60The disposable whole body uniform irradiation of Co gamma-rays, ource-skin Distance 80cm, exposure dose
3.5Gy, exposure dose rate 96.31cGy/min.It is radiated at the completion of affiliated hospital, Chinese Radiation Protection Research Inst radiotherapy department.Irradiation
After the completion, all mouse in addition to blank control group continue administration or stomach-filling purified water 14 days, in administration or stomach-filling purified water the
Start within 10 days to carry out water maze training, 4 times (orientation navigation test) of training, removed underwater platform in the 14th day and remembered daily
Aptitude tests (space search test).
(5) experimental result
The orientation navigation incubation period and space search last day, data incubation period that every mouse is trained 4 times a day lead to
It crosses spss22.0 and carries out t inspection and variance analysis, be as a result expressed as average value ± standard deviation, be shown in Table 3,4 respectively.Experimental result
Show:
1) mouse orientation navigation incubation period and space search incubation period after by radiation injury is longer, spanning platform
Number is less, has significant difference compared with blank control group；
2) mouse will affect its ability of learning and memory after by radiation injury, i.e. cognition dysfunction is impaired；
3) the embodiment of the present invention 1-3 group can significantly improve this symptom, and effect and positive drug are close.
Above-mentioned experimental result illustrates that Baical Skullcap root P.E of the invention has protection to make the radiation injury of cognitive function in mice
With.
The latency change result of 3 experimental mice of table
Note: compared to the blank group#p<0.05,##P < 0.01, * p < 0.05 compared with model group, * *.
p<0.01
The spanning platform number result of 4 experimental mice of table
Note: compared to the blank group#p<0.05,##P < 0.01, * p < 0.05 compared with model group, * *
p<0.01。
Above-described embodiment 4-6's the result shows that: the Baical Skullcap root P.E of ICR intragastric administration on mice embodiment 1-3, repeat administration 14 days
Afterwards, survival rate of the mouse under high dose radiation can be significantly improved；The Baical Skullcap root P.E of ICR intragastric administration on mice embodiment 1-3, weight
Can dramatically increase the quality of mouse quantity of leucocyte and spleen and thymus gland under low dose radiation after being administered 28 days again, and effect with
Positive drug is close.Thus illustrate that Baical Skullcap root P.E of the invention has protective effect to the radiation injury of mouse immune system；Energy
In the significant orientation navigation incubation period and space search incubation period for shortening mouse under low dose radiation, dramatically increase spanning platform
Number, illustrates that Baical Skullcap root P.E of the invention has protective effect to the radiation injury of cognitive function in mice.
Embodiment 7: the preparation of Baical Skullcap root P.E capsule
The Baical Skullcap root P.E 10g as made from embodiment 1-3 is respectively taken, it is each that 15g starch is added, it is uniformly mixed respectively, with appropriate
Ethanol wet, softwood processed cross the granulation of 30 meshes, in 70-80 DEG C of drying, cross 60 meshes, whole grain is packed into capsule, outer packing, difference
Capsule is made.
Embodiment 8: the preparation of Baical Skullcap root P.E granule
The Baical Skullcap root P.E 10g as made from embodiment 1-3 is respectively taken, each that 30g sucrose, 12.5g dextrin is added, mixing is equal respectively
It is even, it is soaked with ethanol in proper amount, softwood processed, crosses the granulation of 14 meshes, in 70-80 DEG C of drying, cross 60 meshes, whole grain, outer packing, difference
Granule is made.
Obviously, various changes and modifications can be made to the invention without departing from essence of the invention by those skilled in the art
Mind and range.If in this way, belonging to the model of the claims in the present invention and its equivalent technology to these modifications and changes of the present invention
Within enclosing, then the present invention is also intended to include these modifications and variations.Above-described embodiment or embodiment are only to the present invention
For example, the present invention can also be implemented with other ad hoc fashions or other particular form, without departing from of the invention
Main idea or substantive characteristics.Therefore, the embodiment of description is regarded as illustrative and non-limiting in any way.This
The range of invention should be illustrated that any variation equivalent with the intention and range of claim also should include by appended claims
Within the scope of the invention.
Claims (10)
1. a kind of Baical Skullcap root P.E, which is characterized in that the Baical Skullcap root P.E is using the method preparation included the following steps:
(1) it is one or many that ethyl alcohol progress ultrasonic extraction is added in radix scutellariae；
(2) merging filtrate after each ultrasonic extraction liquid of filtering；
(3) combined filtrate is concentrated and dried, obtains the Baical Skullcap root P.E.
2. Baical Skullcap root P.E according to claim 1, which is characterized in that the concentration of volume percent of ethyl alcohol in step (1)
For 50-70%, the mass volume ratio of each ultrasonic extraction radix scutellariae and ethyl alcohol is 1:40-70.
3. Baical Skullcap root P.E according to claim 1, it is characterised in that: the temperature of ultrasonic extraction is 60-90 in step (1)
℃。
4. Baical Skullcap root P.E according to claim 1, it is characterised in that: the ultrasonic frequency of ultrasonic extraction in step (1)
For 10-30kHz.
5. Baical Skullcap root P.E according to claim 1, it is characterised in that: the number of ultrasonic extraction is 1-3 in step (1)
It is secondary.
6. Baical Skullcap root P.E according to claim 5, it is characterised in that: the time of each ultrasonic extraction is in step (1)
0.5-1.5h。
7. the pharmaceutical composition of Baical Skullcap root P.E described in any one of -6 according to claim 1, it is characterised in that: described
Pharmaceutical composition contains the pharmaceutically acceptable auxiliaries that a effective amount of Baical Skullcap root P.E and appropriate amount are protected in radiation injury.
8. pharmaceutical composition according to claim 7, it is characterised in that: the dosage form of the pharmaceutical composition is capsule
Or granule.
9. Baical Skullcap root P.E described in any one of -6 or according to any one of claim 7-8 institute according to claim 1
The pharmaceutical composition for the Baical Skullcap root P.E stated is used to prepare the purposes of radiation injury protection medicine.
10. purposes according to claim 9, it is characterised in that: the radiation injury is60Gamma Rays caused by Co
Damage.
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| Publication number | Priority date | Publication date | Assignee | Title |
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| CN113768964A (en) * | 2021-09-14 | 2021-12-10 | 中国辐射防护研究院 | Astragalus extract and its medicinal composition and use |
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