CN106236764A - The application in preparation prevention or treatment decompression sickness medicine of the β aescine element - Google Patents
The application in preparation prevention or treatment decompression sickness medicine of the β aescine element Download PDFInfo
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- CN106236764A CN106236764A CN201610543650.XA CN201610543650A CN106236764A CN 106236764 A CN106236764 A CN 106236764A CN 201610543650 A CN201610543650 A CN 201610543650A CN 106236764 A CN106236764 A CN 106236764A
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- aescine
- decompression sickness
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7028—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages
- A61K31/7034—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin
- A61K31/704—Compounds having saccharide radicals attached to non-saccharide compounds by glycosidic linkages attached to a carbocyclic compound, e.g. phloridzin attached to a condensed carbocyclic ring system, e.g. sennosides, thiocolchicosides, escin, daunorubicin
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- Life Sciences & Earth Sciences (AREA)
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- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
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- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
The present invention relates to biomedicine technical field, it is provided that the application in preparation prevention or treatment decompression sickness medicine of the β aescine element.The present invention is administered through experiment in vivo display β aescine element can effectively reduce the M & M of rat decompression sickness, and extends incubation period and the life span of decompression sickness, illustrates that β aescine element can effectively prevent rat decompression sickness.
Description
Technical field
The present invention relates to pharmaceutical technology field, be specifically related to β-aescine element at preparation prevention or treatment decompression sickness medicine
In application.
Background technology
Diver enters under water, it is necessary to breathe the gases at high pressure of pressure equal with surrounding hydraulic pressure, physiological inertia therein
Gas (such as nitrogen, helium etc.) is internal by dissolving in a large number, for ensureing that these gas safeties excrete, and the rising decompression of diver
Must follow ad hoc rule, the most improper i.e. may form bubble in vivo, cause decompression sickness.Additionally, at job space (space
Extravehicular activity or fighter plane high-altitude are drawn high) in, being greatly lowered of ambient pressure also results in decompression sickness.The state of an illness of decompression sickness is multiple
Miscellaneous, progress is rapid, serious harm diver's life and health, it will usually bring serious consequence.Seek effectively to prevent and
One of measure focus being always decompression sickness area research for the treatment of decompression sickness.But there is no particularly effective for this disease at present
Preventive measure, existing measure mainly includes motion, nitric oxide releasing agents, hyperbaric oxygen pre-adaptation etc., but effect is the most not ideal enough,
Fail popularization and application.
Due to the particularity of the region of anatomy, blood vessel endothelium is highly prone to the damage of Ink vessel transfusing bubble, its biochemical effect caused
Should play an important role in decompression sickness development process, including platelet aggregation, lipoprotein degeneration, activated leukocyte, complement and
Kassinin kinins etc., cause a series of inflammation and Coagulation test.Current reduced pressure disease preventive measure such as statins, nitric oxide releasing agents
Etc. endothelial injury can be alleviated in various degree, thus it is speculated that protection of ecs measure can effectively play prevention and the effect for the treatment of decompression sickness, but
There is no direct protection of ecs measure at present for preventing and treating the research report of decompression sickness.
β-aescine element (English name β-escin, β-aescin) is (such as Aesculus hippocastanum L., day from Hippocastanaceae plant
This Aesculus chinensis Bunge, China's Aesculus) a kind of triterpene saponin containing ester bond of extracting in fruit is mainly having of the spirit that steps of clinical medicine
Effect composition.It has reduction vascular permeability, alleviates vessel wall damage, the increase effect such as venous return, antiinflammatory antioxidation.β-seven leaf
Saponin element is a kind of compound, and its chemical structural formula is as shown in formula I:
Wherein, R=tiglic acid (Tiglic acid) or angelic acid (Angelic acid).Tiglic acid, angelic acid are β-seven
Two groups of leaf saponin element, are equivalent to a part for β-aescine element, owing to linking on β-aescine each molecule of element
The two compound may be different, so β-aescine element is a kind of mixture.
Medicinal report currently, with respect to β-aescine element relates generally to the sides such as chronic venous insufficiency, hemorrhoid, edema
Face (Sirtori C R.Aescin:pharmacology, pharmacokinetics and therapeutic
profile.Pharmacological Research,2001,44(3):183-193.;Hou Minghua. the clinic of aescine
Application and analysis of adverse reactions. medicine, 2015 (8): 247-247.;Zhou Hua, Yang Yulan, Li Jiayi. beta-aescin sodium is clinical
Application general introduction. practical Chinese medicine magazine, 2013 (10): 881-883.), but there is no relevant β-aescine element and decompression sickness is prevented
The research pertinent literature report of effect.
Summary of the invention
It is an object of the invention to provide the application in preparation prevention or treatment decompression sickness medicine of the β-aescine element.
The present invention shows through experiment in vivo: β-aescine element be administered can effectively reduce rat decompression sickness sickness rate and
Mortality rate, and extend incubation period and the life span of decompression sickness, illustrate that β-aescine element can effectively prevent rat decompression sickness.
The invention provides the application in preparation prevention or treatment decompression sickness medicine of a kind of β-aescine element.
Described medicine is with β-aescine element as active ingredient, or comprises the pharmaceutical composition of β-aescine element.
In a preferred embodiment of the invention, described medicine is with β-aescine element for sole active composition.
The pharmaceutical composition of the described β of comprising-aescine element also includes excipient substance, and described adjuvant is selected from diluent, tax
One in shape agent such as normal saline etc., binding agent such as cellulose derivative etc., filler such as starch etc., flavouring agent, sweeting agent
Or it is several.
Described β-aescine element can make various dosage form by pharmaceutics routinely, and described dosage form includes tablet, capsule
One or more in agent, granule, suspensoid, Emulsion, solution, syrup or injection etc., can take oral or injection
One or more in (including one or more in intravenous injection, intravenous drip, intramuscular injection or subcutaneous injection etc.) etc. to
Medicine approach carries out the prevention of decompression sickness, protects or treat.By dosage form by the approach such as oral, intravenous injection be applied to
Body.Individuality can be human or animal.Dosage is generally 5~60mg/ days, specifically can become according to individual age, the state of an illness etc.
Change.
Compared to prior art, beneficial effects of the present invention is as follows:
The invention provides β-aescine element application in the medicine of prevention decompression sickness, β-aescine element can have
Effect ground prevention decompression sickness also blocks decompression sickness process, and the preventing and treating of decompression sickness is significant by this.And β-aescine element
Itself being a kind of plant extract active component, from the point of view of current data, side effect is less, and gastrointestinal reaction, head can occur once in a while
Dizzy, erythrocytolysis, phlebitis, therefore the highest as Drug safety, treat window width.
Accompanying drawing explanation
Fig. 1 is administration group and control rats decompression sickness M & M compares;
Fig. 2 is administration group and control rats decompression sickness invasioning delitescence compares;
Fig. 3 be administration group and control rats decompression sickness morbidity life span compare.
Detailed description of the invention
In conjunction with embodiment and accompanying drawing, the present invention is described in detail, but the enforcement of the present invention is not limited only to this.
The experimental technique of unreceipted actual conditions in the following example, generally according to normal condition, or according to manufacturer
Proposed condition.
Experimental data illustrates: rat decompression sickness sickness rate, mortality rate use Chi-square inspection, rat accumulation morbidity song
Line and survival curve use log-rank inspection, and P < 0.05 has statistical significance for difference.All of statistical analysis SPSS
11.5 software performs.Each group is compared and sees accompanying drawing, wherein: * P < 0.05,#P<0.05。
β in the present embodiment-aescine element is the most commercial commodity, purchased from Sigma-Aldrich company.
Embodiment:
Preparation β-aescine cellulose solution, process is as follows: weigh appropriate β-aescine element (purchased from Sigma-Aldrich
Company), it is dissolved in normal saline, makes 1.8mg/ml's.
Administration group gavage gives β-aescine cellulose solution (1.8mg/kg/ days, successive administration 7 days).
Saline control group gives same way and gives same dose normal saline the lasting identical time.
Administration prepares rat decompression sickness model after terminating, and process is as follows: administration terminates rear rat body weight and all controls at 300-
310g, puts into compression chamber by rat, is forced into 7ATA according to the slowest rear fast speed, maintains 90 minutes in 5 minutes, with
The speed of 2ATA/ minute at the uniform velocity reduces to normal pressure.Proceed to after going out cabin applicant's designed, designed electronic running rotating cage (application number:
CN200920077520.7, Publication No. CN201557446U, denomination of invention: a kind of pressure withstanding animal rotating cage running device), with
The speed of 3m/ minute is moved 30 minutes, the Behavioral change of close observation rat, treats that rapid breathing, difficulty in walking, front occurs in rat
During the performance such as limb/hind limb paralysis, tic, death, show to there occurs that (this standard is that the judgement rat generally acknowledged both at home and abroad subtracts to decompression sickness
Behavioristics's standard of pressure onste.Blatteau J E,Barre S,Pascual A,et al.Protective effects
of fluoxetine on decompression sickness in mice.PloS one,2012,7(11):e49069.)。
1, research β-aescine element impact on rat decompression sickness M & M
By recording each group of rat decompression sickness morbidity and dead number of cases, experimental result is as it is shown in figure 1, saline group rat is reduced pressure
Sick M & M is respectively 75%, 37.5%, administration group rat decompression sickness M & M is respectively 47.5%,
17.5%, compared with saline group, administration group rat decompression sickness sickness rate, mortality rate all have substantially reduction, and β-aescine is described
Element can reduce rat decompression sickness M & M.
2, research β-aescine element impact preclinical on rat decompression sickness
By recording the morbidity of each group of rat decompression sickness as rat invasioning delitescence, experimental result is as in figure 2 it is shown, administration group
Rat decompression sickness disease time-cumulative incidence rate curve is with saline group rat decompression sickness disease time-cumulative incidence rate curve ratio
Relatively there are notable difference, administration group rat invasioning delitescence to be obviously prolonged, illustrate that β-aescine element can extend rat decompression sickness
Incubation period.
3, research β-aescine element impact on rat decompression sickness life span
By recording each group of rat because of the decompression sickness death time, experimental result is as it is shown on figure 3, administration group rat decompression diease occurrence
Depositing curve to compare with saline group rat decompression sickness survival curve and have notable difference, the administration group surviving rats time is obviously prolonged, and says
Bright β-aescine element can extend rat decompression sickness life span.
The ultimate principle of the present invention, principal character and advantages of the present invention have more than been shown and described.The technology of the industry
Personnel, it should be appreciated that the present invention is not restricted to the described embodiments, simply illustrating this described in above-described embodiment and description
The principle of invention, the present invention also has various changes and modifications without departing from the spirit and scope of the present invention, and these become
Change and improvement both falls within scope of the claimed invention.Claimed scope by appending claims and
Equivalent defines.
Claims (4)
1. β-aescine element application in preparation prevention or treatment decompression sickness medicine.
The application in preparation prevention or treatment decompression sickness medicine of the β the most according to claim 1-aescine element, it is special
Levy and be: described medicine is with β-aescine element as active ingredient, or comprises the pharmaceutical composition of β-aescine element.
The application in preparation prevention or treatment decompression sickness medicine of the β the most according to claim 2-aescine element, it is special
Levy and be: described in comprise β-aescine element pharmaceutical composition also include excipient substance, described adjuvant is selected from diluent, figuration
One or more in agent, binding agent, filler, flavouring agent, sweeting agent.
The application in preparation prevention or treatment decompression sickness medicine of the β the most according to claim 1-aescine element, it is special
Levy and be: described β-aescine element pharmaceutics routinely makes various dosage form, described dosage form include tablet, capsule,
One or more in granule, suspensoid, Emulsion, solution, syrup, injection.
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Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN103948614A (en) * | 2014-04-18 | 2014-07-30 | 武汉爱民制药有限公司 | Novel application of aescin and salt thereof in pharmacy |
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- 2016-07-12 CN CN201610543650.XA patent/CN106236764A/en active Pending
Patent Citations (1)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CN103948614A (en) * | 2014-04-18 | 2014-07-30 | 武汉爱民制药有限公司 | Novel application of aescin and salt thereof in pharmacy |
Non-Patent Citations (1)
Title |
---|
唐文光等: "β-七叶皂苷钠治疗急性脑型减压病的疗效观察", 《华南国防医学杂志》 * |
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Application publication date: 20161221 |