CN107519178A - Therapeutic action of the 11 carbonyl β acetyl boswellic acids (AKBA) to peripheral nerve injury - Google Patents
Therapeutic action of the 11 carbonyl β acetyl boswellic acids (AKBA) to peripheral nerve injury Download PDFInfo
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- CN107519178A CN107519178A CN201710239070.6A CN201710239070A CN107519178A CN 107519178 A CN107519178 A CN 107519178A CN 201710239070 A CN201710239070 A CN 201710239070A CN 107519178 A CN107519178 A CN 107519178A
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- carbonyl
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- sciatic nerve
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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
- A61K31/56—Compounds containing cyclopenta[a]hydrophenanthrene ring systems; Derivatives thereof, e.g. steroids
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/02—Inorganic compounds
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
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- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
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Abstract
11 carbonyl β acetyl boswellic acids are an important activity composition in frankincense.A certain amount of 11 carbonyl β acetyl boswellic acids are weighed, is placed in the physiological saline of sterilizing, compound concentration 15mg/ml, is dissolved by ultrasonic oscillation, after 11 carbonyl β acetyl boswellic acids are completely dissolved, are sealed.During for treating Rats'Sciatic Nerve Injury, through intraperitoneal injection, dosage 5mg/kg, once a day, the next day be administered, successive administration 10 times.The histology reparation of the effector organ functional rehabilitation and sciatic nerve injury that are dominated by sciatic nerve carries out evaluation of clinical curative effect, the results showed that 11 carbonyl β acetyl perfume (or spice) lactic acid have good therapeutic action to Rats'Sciatic Nerve Injury, efficient up to 100%.In order to ensure 11 carbonyl β acetyl boswellic acids are to the clinical efficacy of peripheral nerve injury, reappearance test has been carried out.Result of the test shows twice：11 carbonyl β acetyl perfume (or spice) lactic acid formulations have therapeutic action through intraperitoneal injection to Rats'Sciatic Nerve Injury.
Description
This patent art and background technology
The invention belongs to natural medicine technical field, it is mainly used in treating the peripheral nerve injury of animal.
The resin that frankincense is olive subject plant Boswellia carterii and congener skin zone oozes out, acrid flavour, hardship are warm-natured, have promoting blood circulation
Analgesic, the effect of detumescence and promoting granulation.《Compendium of Materia Medica》Cloud：" frankincense perfume (or spice) is altered, and enters the heart channel of Hang-Shaoyin, analgesic therapy of invigorating blood circulation, therefore is ulcer epidemic disease ulcer, trusted subordinate
Pain key medicine." frankincense and its be used as medicine Shengji San, erosion prevention and muscle growing dissipate etc. prescription income《Chinese veterinary pharmacopoeia》.The main component of frankincense
For volatile oil, resin and natural gum, wherein resin content is 60%~70%, gum content 27%~35%, volatile oil 3%
~8%, remaining is impurity and moisture；Resin and volatile oil are its primary pharmacological activity composition.Resin is mainly five rings in frankincense
Triterpenes, tetracyclic triterpenes, macrocyclic diterpene class.Pentacyclic triterpene is that most types of compounds is distributed in Boswellia, most
Representative is masticinic acid and its derivative.Boswellic acids derivatives mainly include α-masticinic acid (α-boswellicacid,
α-BA), beta boswellic acid (β-boswellic acid, β-BA) and its derivative acetyl boswellic acid (aceboswellic acid,
), ABA 11- keto-β-boswellic acids (11-keto- β-tyl-boswellic acid, KBA) and acetyl group -11- ketone-β-frankincense
Sour (acetyl-11-keto- β-boswellicacid, AKBA) etc., wherein AKBA are that activity is most strong, study relatively broad change
Compound.
With the fast development of China's economy, the living standard of people improves constantly, and the raising pets using dog cat as representative turns into
A part for people's life.In toy, clinically dog cat peripheral nerve injury case is relatively conventional, due to perineural knot
Structure feature determines it compared with the injury repair of the tissues such as in general skin, muscle, and repair time is longer.When peripheral nerve damages
After wound, its effector organ miopragia dominated or forfeiture can be caused, the repairing of neural injury time is longer in addition, therefore, dog
Cat peripheral nerve injury case has become the clinical difficult and complicated cases of toy.At present, also it is used to treat dog cat week without exclusive
Enclose the medicine of neurotrosis.In order to develop the medicine for the treatment of peripheral nerve injury, our seminars look for from blood-activating and stasis-removing
Having arrived Olibanum extract has preferable clinical efficacy.Further study show that 11- keto-β-boswellic acids in Olibanum extract
(AKBA) it is its main active.AKBA belongs to the terpene micromolecular compound of three ring five, and it is anti-to be widely used in suppression inflammation
Should, promote the reparation of peripheral nerve injury, this conclusion is treated Rats'Sciatic Nerve Injury model by AKBA and confirmed.
The problem of existent technique is present
The medicine conventional currently used for treatment dog cat peripheral nerve injury is blood-activating stasis-removing kind Chinese medicine, because traditional Chinese medicine ingredients are answered
Miscellaneous, processing technology falls behind, and curative effect is not notable.
Product purpose
The object of the invention is by the repair of peripheral nerve injury in rats scale-model investigation AKBA peripheral nerve injuries
Develop the curative drug of dog cat peripheral nerve injury.
Product design main points
It is prepared by product：A certain amount of 11- carbonyl-beta-acetyls masticinic acid is accurately weighed, is placed in the physiological saline of sterilizing, matches somebody with somebody
The concentration of system is 15mg/ml, through ultrasonic oscillation 30 minutes, after 11- carbonyl-beta-acetyls masticinic acid all dissolving, is carried out close
Envelope preserves.
Curative effect：Using the Rats'Sciatic Nerve Injury model of preparation, by rat model be randomly divided into model control group,
Four groups of 11- carbonyl-beta-acetyl masticinic acids low dosage, middle dosage and high dose group.Control group administered physiological saline, test group is to 11-
Carbonyl-beta-acetyl masticinic acid.In operation the same day, through intraperitoneal injection, be administered once within 1st, the next day be administered once, continuously give
Medicine 10 times.
Therapeutic evaluation：The functional rehabilitation and sciatic nerve injury of the effector organ dominated by clinical observation and sciatic nerve
Histology reparation evaluation.Result of the test shows that 11- carbonyl-beta-acetyl perfume (or spice) lactic acid has well to Rats'Sciatic Nerve Injury
Therapeutic action.Optimal dosage is 5mg/kg.
Reappearance test：In order to ensure the accuracy of experiment, Curative effect does a replica test, as a result with the 1st time
Test consistent.
Technical scheme
Product is so found：Frankincense is drug for invigorating blood circulation and eliminating stasis, active, anti-inflammatory and antioxidation.Under study for action
Find that frankincense has the repair for promoting peripheral nerve injury in medicine compound preparation treatment wound repair.Utilize Olibanum extract
When treating Rats'Sciatic Nerve Injury, it was demonstrated that Olibanum extract peripheral nerve injury has a preferable repair.Pass through
To the experiment sieving of Olibanum extract active component, it was confirmed that to an important work of peripheral nerve injury repair in frankincense
Property composition is 11- carbonyl-beta-acetyl masticinic acids.
The preparation of product：A certain amount of 11- carbonyl-beta-acetyls masticinic acid is placed in the physiological saline of sterilizing, prepares 11-
Carbonyl-beta-acetyl frankincense acid concentration is 15mg/ml, through ultrasonic oscillation 30 minutes, treats 11- carbonyl-beta-acetyls masticinic acid whole
After dissolving, it is sealed.
The preparation of Rats'Sciatic Nerve Injury model：It is 180g or so rat 40 by body weight, is separated using surgical operation
Rat sciatic nerve, Rats'Sciatic Nerve Injury model is prepared using the method for clamp extruding.
Experiment packet and administration：Rat model is randomly divided into model control group, low dose of 11- carbonyl-beta-acetyl masticinic acids
Four groups of amount, middle dosage and high dose group, every group of 10 rats.Model control group is to physiological saline, dosage 5ml/kg；11- carbonyls
The basic, normal, high dosage group dosage of base-β-acetyl boswellic acid is 2.5mg/kg, 5mg/kg, 10mg/kg.
The course for the treatment of and therapeutic evaluation：In operation the same day, through intraperitoneal injection, be administered once within 1st, the next day be administered once,
Successive administration 10 times.The functional rehabilitation of effector organ and the group of sciatic nerve injury dominated by clinical observation, sciatic nerve
Knit and repair evaluation each group Rats'Sciatic Nerve Injury repairing effect, it is efficient up to 100%.
Reappearance test：In order to ensure the accuracy of experiment, will once be weighed by [0012] and [0013] operating process
Renaturation is tested, using [0014] course for the treatment of and therapeutic evaluation.As a result show that result of the test is consistent twice.
Conclusion：The functional rehabilitation of effector organ and the group of sciatic nerve injury dominated by clinical observation, sciatic nerve
Knit and repair evaluation, 11- carbonyl-beta-acetyl masticinic acids low dosage, middle dosage and high dose group sciatic nerve injury and repair are excellent
In model control group, wherein best as 5ml/kg 11- carbonyl-beta-acetyl masticinic acid dosage group repairing effects using concentration
Present invention solves the technical problem that and superiority
The following technical problem of the present invention：(1) frankincense is clinically mainly with water decoction or application of dispersant, due to special taste
Road, animal are orally difficult.(2) frankincense is clinically mainly complicated with water decoction or dispersion. formulation, influences facing for active component
Bed curative effect, therefore, water decoction or dispersant clinical efficacy are relatively slow slower.Product superiority：(1) it is refreshing around dog cat in recent years
Through damaging case in ascendant trend year by year, such as the peripheral nerve caused by interverbebral disc, waist dish outstanding, canine distemper complication and wound
Damage, veterinary clinic is also without corresponding medicine at present.The discovery of 11- carbonyl-beta-acetyl masticinic acids, has filled up animal and has faced
The blank of bed treatment peripheral nerve injury medicine.(2) 11- carbonyl-beta-acetyls masticinic acid is dissolved in water, beneficial to the exploitation of liquid drugs injection,
With the features such as convenient drug administration, drug absorption is fast, it is adapted to dog cat clinical application.(3) 11- carbonyl-beta-acetyls masticinic acid comes from day
The active component of right plant frankincense extraction, any toxicity and side effect are not shown in peripheral nerve injury in rats is treated.
Claims (3)
1.11- carbonyl-beta-acetyls masticinic acid has treatment peripheral nerve injury in rats effect.
It is prepared by 2.11- carbonyl-beta-acetyl masticinic acids injection：A certain amount of 11- carbonyl-beta-acetyls masticinic acid is weighed, is placed in and goes out
In the physiological saline of bacterium, the concentration of preparation is 15mg/ml, by ultrasonic oscillation, treats that 11- carbonyl-beta-acetyl masticinic acids are complete
After dissolving, it is sealed.
3. usage and dosage：When 11- carbonyl-beta-acetyls masticinic acid treats Rats'Sciatic Nerve Injury, through intraperitoneal injection, administration
Dosage is 5mg/kg, once a day, the next day be administered, general administration 10 times or so.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201710239070.6A CN107519178A (en) | 2017-04-13 | 2017-04-13 | Therapeutic action of the 11 carbonyl β acetyl boswellic acids (AKBA) to peripheral nerve injury |
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| CN201710239070.6A CN107519178A (en) | 2017-04-13 | 2017-04-13 | Therapeutic action of the 11 carbonyl β acetyl boswellic acids (AKBA) to peripheral nerve injury |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115282154A (en) * | 2022-08-15 | 2022-11-04 | 武汉科前生物股份有限公司 | Application of 11-carbonyl-beta-acetyl boswellic acid in preparation of medicine for treating feline abdominal distension |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101775058A (en) * | 2009-01-08 | 2010-07-14 | 凌沛学 | Preparation and application of pharmaceutic preparation of 11-carbonyl-betal- acetyl mastic acid and derivatives thereof extracted from frankincense |
-
2017
- 2017-04-13 CN CN201710239070.6A patent/CN107519178A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101775058A (en) * | 2009-01-08 | 2010-07-14 | 凌沛学 | Preparation and application of pharmaceutic preparation of 11-carbonyl-betal- acetyl mastic acid and derivatives thereof extracted from frankincense |
Non-Patent Citations (2)
| Title |
|---|
| 刘绍军等: "3-乙酰基-11-酮-β-乳香酸的抗炎作用及其衍生物的化学修饰", 《中国当代医药》 * |
| 郭鑫等: "周围神经损伤中P2Y12受体-p38MAPK通路的研究进展", 《现代生物医学进展》 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115282154A (en) * | 2022-08-15 | 2022-11-04 | 武汉科前生物股份有限公司 | Application of 11-carbonyl-beta-acetyl boswellic acid in preparation of medicine for treating feline abdominal distension |
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Application publication date: 20171229 |