CN106551897A - A kind of bulleyaconitine A liniment and preparation method and application - Google Patents
A kind of bulleyaconitine A liniment and preparation method and application Download PDFInfo
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- CN106551897A CN106551897A CN201510635186.2A CN201510635186A CN106551897A CN 106551897 A CN106551897 A CN 106551897A CN 201510635186 A CN201510635186 A CN 201510635186A CN 106551897 A CN106551897 A CN 106551897A
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Abstract
The invention discloses a kind of bulleyaconitine A liniment and preparation method and application.Described bulleyaconitine A liniment is made up of the triacetyl glycerine of the bulleyaconitine A of mass percent 0.1 ~ 1.0%, 4 ~ 25% Propylene Glycol, 0.2 ~ 2.5% azone and 74 ~ 95%.Preparation method is that bulleyaconitine A is ground sieving for standby；Sequentially add azone, the triacetyl glycerine of formulation ratio simultaneously in Propylene Glycol, be uniformly mixed so as to obtain mixed solvent；Mixed solvent is added in bulleyaconitine A, sonic oscillation obtains object bulleyaconitine A liniment.Treatment inflammation and/or the application in pain medication are being prepared using for described bulleyaconitine A liniment.The present invention is a kind of new bulleyaconitine A external preparation of acquisition of concentrating on studies through inventor, meets solvent by the solvent composition of optimized choice and helps the system of oozing so that drug absorption is fast, to no skin irritation and anaphylaxis.
Description
Technical field
The invention belongs to pharmaceutical technology field, and in particular to a kind of bulleyaconitine A liniment and preparation method and application.
Background technology
Bulleyaconitine A be the diterpene extracted from Yunnan Ranunculaceae aconitum plant tap Aconitum carmichjaelii Debx. than ester biological alkali, with stronger analgesic activity, also there is antiinflammatory action in addition.Its analgesic activity is central, be not found at present its have it is additive.
Bulleyaconitine A treating cancer late period pain, rheumatism and rheumatoid arthritiss, scapulohumeral periarthritis, shoulder brachialgia, stiff neck, osteoarthritis, benign arthralgia, waist and extremities joint are sprained, are dampened, lumbar muscle strain and lumbago and backache, sciatica, myofibrositis and costal chondritis, herpes zoster, headache due to common cold, toothache etc..
Dosage form the most frequently used at present is bulleyaconitine A tablet, and which can be used to treat rheumatic and rheumatoid arthritiss, lumbar muscle strain, scapulohumeral periarthritis, extremity are sprained, dampened, and is particularly useful in cure scapulohumeral periarthritis, osteoarthritis.Other dosage forms of bulleyaconitine A also have capsule, pill, oral administration solution etc..
However, peroral dosage form has very big restriction for treatment local inflammation and pain such as local arthritis, for example its slow, taking dose that works is big, and tablet dysphagia for old people, makes troubles to the use of patient.
In addition, there are the research and development of the preparation capable of permeating skin such as bulleyaconitine A patch at present, but as bulleyaconitine A has very strong stimulation, easily cause user allergy.Therefore not yet have safely and effectively bulleyaconitine A external preparation to be applied to clinic at present.
The content of the invention
The first object of the present invention is to provide a kind of bulleyaconitine A liniment；Second purpose is the preparation method of the bulleyaconitine A liniment for providing described；3rd purpose is the application of the bulleyaconitine A liniment for providing described.
The first object of the present invention is achieved in that described bulleyaconitine A liniment is made up of the triacetyl glycerine of the bulleyaconitine A of mass percent 0.1 ~ 1.0%, 4 ~ 25% Propylene Glycol, 0.2 ~ 2.5% azone and 74 ~ 95%.
The second object of the present invention is achieved in that and comprises the following steps：
A, bulleyaconitine A is ground into sieving for standby；
B, azone, triacetyl glycerine that formulation ratio is sequentially added in Propylene Glycol, are uniformly mixed so as to obtain mixed solvent；
C, the mixed solvent that step B is obtained is added to formulation ratio step A process bulleyaconitine A in, sonic oscillation obtains object bulleyaconitine A liniment.
The third object of the present invention is achieved in that described bulleyaconitine A liniment is preparing treatment inflammation and/or the application in pain medication.
The present invention is a kind of new bulleyaconitine A external preparation of acquisition of concentrating on studies through inventor, meets solvent by the solvent composition of optimized choice and helps the system of oozing so that drug absorption is fast, to no skin irritation and anaphylaxis.Bulleyaconitine A liniment of the present invention can Transdermal absorption, without skin irritation and anaphylaxis, being capable of topical application and inflammation or painful area, and have it is rapid-action, significantly improve compared with oral curative effect, the advantages of the whole body toxic and side effects as bulleyaconitine A causes in itself, duration of efficacy can be reduced extending.
Bulleyaconitine A of the present invention has advantages below：
1）By bulleyaconitine A external, it is to avoid take inconvenience, and be used directly for the position of inflammation or pain, it is to avoid whole body toxic and side effects；
2）Focus is directly acted on, it is rapid-action；
3）The vehicle system of optimization can avoid the anaphylaxiss of external.
Specific embodiment
With reference to embodiment, the present invention is further illustrated, but never in any form the present invention is any limitation as, based on present invention teach that any conversion for being made or replacement, belong to protection scope of the present invention.
Bulleyaconitine A liniment of the present invention, is made up of the triacetyl glycerine of the bulleyaconitine A of mass percent 0.1 ~ 1.0%, 4 ~ 25% Propylene Glycol, 0.2 ~ 2.5% azone and 74 ~ 95%.
Described bulleyaconitine A liniment is made up of the triacetyl glycerine of the bulleyaconitine A of mass percent 0.4%, 23% Propylene Glycol, 2.5% azone and 74.1%.
The preparation method of bulleyaconitine A liniment of the present invention, comprises the following steps：
A, bulleyaconitine A is ground into sieving for standby；
B, azone, triacetyl glycerine that formulation ratio is sequentially added in Propylene Glycol, are uniformly mixed so as to obtain mixed solvent；
C, the mixed solvent that step B is obtained is added to formulation ratio step A process bulleyaconitine A in, sonic oscillation obtains object bulleyaconitine A liniment.
Grinding described in step A is sieved to cross 60 ~ 80 mesh sieves.
The frequency of the sonic oscillation described in step C is 40KHz, and the time is
5~10min。
The application of bulleyaconitine A liniment of the present invention is that described bulleyaconitine A liniment is preparing treatment inflammation and/or the application in pain medication.
Described inflammation and/or pain are selected from rheumatism and rheumatoid arthritiss, scapulohumeral periarthritis, shoulder arm pain, stiff neck pain, osteoarthritis, benign arthralgia, waist and extremities joint are sprained, dampen pain, lumbar muscle strain and lumbago and backache, sciatica, myofibrositis and costal chondritis, herpes zoster pain, headache due to common cold, tenderness or cancer of late stage pain.
Embodiment is presented herein below, and the invention will be further described：
The preparation of 1 bulleyaconitine A liniment 1 of embodiment
Prescription：Bulleyaconitine A：4 g
Propylene Glycol：220 ml
Azone：25ml
Triacetyl glycerine：7751 ml
Preparation method：
1st, ground 80 mesh sieve, weighs 4 g of bulleyaconitine A, standby；
2nd, 220 ml of Propylene Glycol is measured, 1000 are placed in
In ml volumetric flasks, 25 ml of azone is added, triacetyl glycerine is subsequently adding to scale, is configured to clear and bright double solventss standby；
3rd, by the bulleyaconitine A after grinding, in adding another 1000 ml volumetric flask, and it is gradually added into 800 ml of obtained double solventss in above-mentioned steps 2, under the conditions of sonic oscillation, dissolve bulleyaconitine A, solution is clear and bright, is supplemented with above-mentioned mixed solvent to 1000 ml, obtains the bulleyaconitine A liniment 1 of the present invention after placement.
The preparation of 2 bulleyaconitine A liniment 2 of embodiment
Prescription：Bulleyaconitine A：1 g
Propylene Glycol：230 ml
Azone：20 ml
Triacetyl glycerine：749 ml
Preparation method：
1st, bulleyaconitine A 1g is weighed, ground 80 mesh sieve is standby；
2nd, Propylene Glycol 230ml is measured, be placed in 1000ml volumetric flasks, add azone 20ml, triacetyl glycerine is subsequently adding to scale, is configured to clear and bright mixed solvent standby；
3rd, by the bulleyaconitine A after grinding, in adding another 1000ml volumetric flask, and it is gradually added into obtained mixed solvent 800ml in above-mentioned steps 2, under the conditions of sonic oscillation, dissolve bulleyaconitine A, solution is clear and bright, is supplemented with above-mentioned mixed solvent to 1000ml, obtains the bulleyaconitine A liniment 2 of the present invention after placement.
The preparation of 3 bulleyaconitine A liniment 3 of embodiment
Prescription：Bulleyaconitine A：10 g
Propylene Glycol：40 ml
Azone：10 ml
Triacetyl glycerine：940 ml
Preparation method：
1st, 10 g of bulleyaconitine A is weighed, ground 80 mesh sieve is standby；
2nd, 40 ml of Propylene Glycol is measured, is placed in 1000ml volumetric flasks, add 10 ml of azone, triacetyl glycerine is subsequently adding to scale, is configured to clear and bright mixed solvent standby；
3rd, by the bulleyaconitine A after grinding, in adding another 1000ml volumetric flask, and it is gradually added into obtained mixed solvent 800ml in above-mentioned steps 2, under the conditions of sonic oscillation, dissolve bulleyaconitine A, solution is clear and bright, is supplemented with above-mentioned mixed solvent to 1000ml, obtains the bulleyaconitine A liniment 3 of the present invention after placement.
The preparation of 4 bulleyaconitine A liniment 4 of embodiment
Prescription：Bulleyaconitine A：10 g
Propylene Glycol：240 ml
Azone：2 ml
Triacetyl glycerine：748 ml
Preparation method：
1st, 10 g of bulleyaconitine A is weighed, ground 80 mesh sieve is standby；
2nd, 240 ml of Propylene Glycol is measured, 1000 are placed in
In ml volumetric flasks, 2 ml of azone is added, triacetyl glycerine is subsequently adding to scale, is configured to clear and bright mixed solvent standby；
3rd, by the bulleyaconitine A after grinding, in adding another 1000ml volumetric flask, and it is gradually added into obtained mixed solvent 800ml in above-mentioned steps 2, under the conditions of sonic oscillation, dissolve bulleyaconitine A, solution is clear and bright, is supplemented with above-mentioned mixed solvent to 1000ml, obtains the bulleyaconitine A liniment 4 of the present invention after placement.
5 pharmacodynamic experiment of embodiment
1.1 laboratory animal：
This experiment Wistar rats 36, male, 125 ~ 140g of body weight.
1.2 experimental drug：
Bulleyaconitine A standard substance, bulleyaconitine A liniment 1 prepared by embodiment 1, water for injection, Freund ' s Freund's complete adjuvants；PEG2, beta-endorphin ELISA kit, IFN-γ ELISA kit.
Hydrochloric acid is added in water for injection, the storing liquid of 1mg/mL is configured to（pH2~3）.And before experiment, Radix Aconiti Kusnezoffii formic acid standard substance are dissolved in above-mentioned hydrochloric acid storing solution, are diluted to 200 μ g/mL, the experimental solutions of pH5.
Foundation, packet and the treatment of 1.3 animal models：
Freund ' s Freund's complete adjuvant 0.1mL are injected in Wistar Rat Right metapedes plantars, secondary in the future whole rat paw injection site whole swelling reach peak, then begin to disappear day by day after 3-4 days.Primary inflammatory of this stage for rat.
Turn day after injection（d1）, rat is randomly divided into into 3 groups, 12 per group, Rat Right ankle Zhou Jing is measured respectively, the footpath value of right ankle week of each group is respectively 0.22 ± 0.09 cm, 0.23 ± 0.11 cm, 0.23 ± 0.07 cm.Turn day after injection（d1）Start once a day, continuous one week（d1~d7）, 3 groups of bulleyaconitine A standard substance for giving 50 μ g/mL respectively（A groups）, smear 2ml（3μg/mL）Bulleyaconitine A liniment 1 prepared by the embodiment of the present invention 1（B groups）, 100 μ L waters for injection of subcutaneous injection（C groups）.
1.4 observation index and method
1.4.1 footpath of right ankle joint week is evaluated
1 each group Rat Right ankle joint Zhou Jing of table
Interpretation of result：Apply bulleyaconitine A standard substance hydrochloric acid solution obvious with the Rat Right ankle swelling mitigation effect of bulleyaconitine A liniment, and the two effect is similar.Compared with water for injection, bulleyaconitine A standard substance started to manifest effect after second day with liniment, and swelling gradually started to be controlled at the 3rd day, and started within the 4th day detumescence.
1.4.2
Cytokines measurement
The 7th day after injection adjuvant（d7）Serum is left and taken, is illustrated according to ELISA kit, detect TNF-α, IFN-γ, PGE2, beta-endorphin level respectively, standard curve is drawn with the positive quality control product concentration of proportional dilution, corresponding cytokine levels are tried to achieve according to standard curve and test serum absorbance.
2 Cytokine data of table
Four index concentration are pg/mL
Data analysiss：
TNF-α can be detected in general arthritic's serum and joint fluid and IFN-γ content increases.TNF-α is a kind of proinflammatory factor, can cause a variety of inflammatory reactions.In two groups of A, B, TNF-α is substantially reduced, it was demonstrated that bulleyaconitine A can effectively suppress the growth of TNF-α.
IFN-γ is another kind of important inflammatory factor in arthritis, and which can be with activated mononuclear-macrophage so as to discharge the inflammatory factors such as IL-1, TNF-α.And in this experiment, in tri- groups of A, B, C, IFN-γ level is almost identical, it was demonstrated that it is more related to TNF-α level that bulleyaconitine A mitigates arthritis effect.
PGE2 is the inflammatory mediator with the scorching paroxysmal pain effect of cause that local organization is produced and discharged under pro-inflammatory cytokine effect.PGE2 can cause local vascular permeability to increase, and further increase inflammatory reaction, and promoting theca cell, fibroblast proliferation, angiogenesiss cause bone and cartilage destruction.Two groups of A, B is capable of the concentration of effective relatively low PGE2, it was demonstrated that the development to inflammation has certain inhibitory action.
Meanwhile, PGE2 can also be activated or sensitization periphery Pain receptor, transmit pain sensation signal, produce hyperalgesia, be important pain mediator.And beta-endorphin is acted on conversely, being the neuropeptide of stronger analgesic activity with PGE2.The factors such as inflammation, wound can activate maincenter endogenous opiatepeptide system, and beta-endorphin release increases, and is the stress of active countermeasures pain.And in this test, A, B group beta-endorphin has increase trend relative to C groups, it was demonstrated that bulleyaconitine A can improve beta-endorphin concentration, active countermeasures pain.
Two groups of A, B is compared, and cytokine concentrations are relatively, it was demonstrated that two kinds of preparations on therapeutic effect relatively.
Embodiment 6
Tested with embodiment 2,3,4 respectively, experimental technique is same as Example 5, as a result shown that treatment of the bulleyaconitine A liniment for preparing of the invention to inflammation and/or pain is effective.
Claims (7)
1. a kind of bulleyaconitine A liniment, it is characterised in that described bulleyaconitine A liniment is made up of the triacetyl glycerine of the bulleyaconitine A of mass percent 0.1 ~ 1.0%, 4 ~ 25% Propylene Glycol, 0.2 ~ 2.5% azone and 74 ~ 95%.
2. bulleyaconitine A liniment according to claim 1, it is characterised in that described bulleyaconitine A liniment is made up of the triacetyl glycerine of the bulleyaconitine A of mass percent 0.4%, 23% Propylene Glycol, 2.5% azone and 74.1%.
3. the preparation method of the bulleyaconitine A liniment described in a kind of claim 1 or 2, it is characterised in that comprise the following steps：
A, bulleyaconitine A is ground into sieving for standby；
B, azone, triacetyl glycerine that formulation ratio is sequentially added in Propylene Glycol, are uniformly mixed so as to obtain mixed solvent；
C, the mixed solvent that step B is obtained is added to formulation ratio step A process bulleyaconitine A in, sonic oscillation obtains object bulleyaconitine A liniment.
4. the preparation method of bulleyaconitine A liniment according to claim 3, it is characterised in that the grinding described in step A is sieved to cross 60-80 mesh sieves.
5. the preparation method of bulleyaconitine A liniment according to claim 3, it is characterised in that the frequency of the sonic oscillation described in step C is 40KHz, and the time is 5 ~ 10 min.
6. the application of the bulleyaconitine A liniment described in a kind of claim 1 or 2, it is characterised in that described bulleyaconitine A liniment is preparing treatment inflammation and/or the application in pain medication.
7. the application of bulleyaconitine A liniment according to claim 6, it is characterised in that described inflammation and/or pain are selected from rheumatism and rheumatoid arthritiss, scapulohumeral periarthritis, shoulder arm pain, stiff neck pain, osteoarthritis, benign arthralgia, waist and extremities joint are sprained, dampen pain, lumbar muscle strain and lumbago and backache, sciatica, myofibrositis and costal chondritis, herpes zoster pain, headache due to common cold, tenderness or cancer of late stage pain.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106943402A (en) * | 2017-05-13 | 2017-07-14 | 台州恩泽医疗中心(集团) | A kind of new application of bulleyaconitine A |
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| CN1041527A (en) * | 1989-11-21 | 1990-04-25 | 中国人民解放军军事医学科学院毒物药物研究所 | The preparation method of ftibamzone compound liniment |
| CN1965814A (en) * | 2006-11-03 | 2007-05-23 | 昆明制药集团股份有限公司 | Bulleyaconitionea cataplasma |
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2015
- 2015-09-30 CN CN201510635186.2A patent/CN106551897A/en active Pending
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1041527A (en) * | 1989-11-21 | 1990-04-25 | 中国人民解放军军事医学科学院毒物药物研究所 | The preparation method of ftibamzone compound liniment |
| CN1965814A (en) * | 2006-11-03 | 2007-05-23 | 昆明制药集团股份有限公司 | Bulleyaconitionea cataplasma |
Non-Patent Citations (1)
| Title |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN106943402A (en) * | 2017-05-13 | 2017-07-14 | 台州恩泽医疗中心(集团) | A kind of new application of bulleyaconitine A |
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