CN1535683A - Aconitum kusnezoffii methylsine aerosol and its preparation method - Google Patents
Aconitum kusnezoffii methylsine aerosol and its preparation method Download PDFInfo
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- CN1535683A CN1535683A CNA031176658A CN03117665A CN1535683A CN 1535683 A CN1535683 A CN 1535683A CN A031176658 A CNA031176658 A CN A031176658A CN 03117665 A CN03117665 A CN 03117665A CN 1535683 A CN1535683 A CN 1535683A
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- bulleyaconitine
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Abstract
The present invention provides an aconitum kusnezoffii methylsine aerosol and its preparation method. Every ml contains 0.01-0.8 mg of aconitum kusnezoffii methylsine, it can be made into the pharmaceutically-aceptable aerosol, and it can use methol or camphor, etc. which is 0.05-10% of main medicine content as medial permeation p romotor, and can use coumarinic lactone or vanillin, etc. which is 0.002-5% of main medicine content as medical perfume. Said invention has good stability, can be stored for 4 years at normal temp., is small in irritation, can be quickly absorbed and can quickly produce action, and can be used for relieving inflammation and stopping pain obviously.
Description
Technical field
The present invention relates to bulleyaconitine A aerosol of a kind of biologically active and preparation method thereof, belong to medical medicine.
Background technology
Bulleyaconitine A is to draw all from Ranunculaceae aconitum plant the western regions of the Yunnan Province that isolating new alkaloid (Aconitum BulleyanumDiels)---alkali first (Bulleyaconitine A) is all drawn in the western regions of the Yunnan Province.The preparation of bulleyaconitine A has injection, tablet, oral liquid, soft capsule at present.Exploitation is injection the earliest, is used for the treatment of clinically that rheumatic arthritis, rheumatoid arthritis, lumbar muscle strain, scapulohumeral periarthritis, extremity are sprained, contusion etc., has curative effect preferably; Also can be used for the pain that cancer, operation etc. produce; For herpes zoster etc. certain curative effect is arranged.But when producing this injection, because bulleyaconitine A has water insoluble and labile character, can only use organic solvents such as ethanol or propylene glycol, bring to the patient in when injection like this to have an intense pain and cause injection site redness etc., have a strong impact on the application of this injection.Publication number is CN 1107697 A, and denomination of invention is ' aconitum kusnezoffii oral tablets, a capsule ', and the patent No. is ZL 98 1 06595.3, and denomination of invention is ' radix aconiti kunsezoffii nail element soft capsule and a production method thereof '.Though overcome above-mentioned deficiency, exist onset to reach the defective of patient dependence differences such as mouth fiber crops when oral slowly, and can not spraining or dampening and implement rapid pain relieving extremity, strength portion.Therefore, be necessary prior art is improved.
Summary of the invention
The object of the present invention is to provide a kind of steady quality, energy analgesic high-quality bulleyaconitine A aerosol and preparation method thereof rapidly.
The present invention realizes by following technical proposal: every ml contains bulleyaconitine A 0.01～0.8mg, makes pharmaceutically acceptable aerosol.
In 0.05～10% Mentholum of the also available principal agent amount of the present invention or Camphora micromolecule terpenoid and/or Azone, CD, DMSO, muscone, the higher hydrocarbon alcohol one or more are as medical penetration enhancer.
0.002～5% the coumarin with certain ataralgesia effect of the also available principal agent amount of the present invention, in the vanillin one or more are as medical spice.
The present invention makes by following method:
1, under 10,000 grades of conditions, bulleyaconitine A is dissolved in the ethyl acetate below 10 times in advance fully;
2, add needed penetration enhancer, and note it is dissolved fully;
3, add flavouring agent as required, and after noting it is dissolved fully, get final product by common aerosol production.
For purpose of the present invention can clearly be described, now pharmacological experiments of the present invention is reported as follows:
1, the analgesic activity of bulleyaconitine A aerosol
Mouse writhing method:
30 of mices are divided into 3 groups at random, and 10 every group, the about 4cm of mouse back both sides unhairing
2, be administered twice midfeather 30min continuously at the unhairing position, each spray 2 times (～0.2mg), behind the administration 1h, inject 0.7% acetic acid 0.1ml/10g to mouse peritoneal, record 5～15min mouse writhing reaction times is calculated and comparable group differences significance, the results are shown in following table:
Group body weight dosage (mg/Kg) is turned round body number of times suppression ratio
Blank group 20 ± 1.1 equal-volumes 33.8 ± 4.50
Morphine group 20 ± 0.9 10 7.4 ± 2.51 90.5%
Test group 20 ± 1.2～0.2mg 18.6 ± 3.42 46.94%
Conclusion: the bulleyaconitine A aerosol has the effect of obvious inhibition mice pain, with the blank group difference of highly significant is arranged relatively.
2, the antiinflammatory action of bulleyaconitine A aerosol
Use the Whttle method, 30 of mices are divided into 3 groups at random, and 10 every group, the about 4cm of mouse back both sides unhairing
2Be administered twice at the unhairing position continuously, midfeather 30min, spray at every turn 2 times (～0.2mg), behind the administration 1h, the blue 0.2ml/ of mouse tail vein injection 0.5% ivens is the timely lumbar injection 0.7% acetic acid 0.2ml/10g in back only, puts to death mice behind the 15min, and intraperitoneal injection of saline 5ml gently rubs the back and extracts peritoneal fluid, centrifugal, supernatant is measured optical density value in the 620nm place, calculate and comparable group differences significance, the results are shown in following table:
Group body weight dosage (mg/Kg) optical density value suppression ratio
Blank group 20 ± 1.1 equal-volumes 0.28 ± 0.05
Aspirin 20 ± 1.3 200 0.11 ± 0.03 60.9%
Test group 20 ± 1.2 0.2 0.15 ± 0.05 58.8%
Conclusion: the bulleyaconitine A aerosol has the obvious anti-inflammatory and anti effect, with the blank group difference of highly significant is arranged relatively.
3, the irritation test of bulleyaconitine A aerosol
Get 4 of healthy rabbits, W:2.0～2.2kg, male and female half and half are divided into two groups, with the about 5 * 10cm of both sides, back unhairing
2, a depilation district does the normal skin test, is divided into administration district and check plot.Administration district administration 1 time (～0.1mg), check plot spray primary blank solvent.Another piece depilation district makes the injured skin irritation test, and with marking the scratch of " # " shape on the syringe needle depilation district skin, diameter 2cm to stab epidermis, does not hinder corium, and hyporrhea degree of being is arranged before the administration.Administrated method is the same with normal skin, and opposite side compares.Administration district administration 1 time (～0.1mg), check plot spray primary blank solvent.Behind the administration 24h, write down 1h, 24h, 48h, the erythema of 72h medicine-feeding part appearance and hemorrhage situation respectively, the stimulation degree is also estimated in the according to the form below scoring:
Skin irritation reaction standards of grading
| Erythema | Integration | Edema | Integration |
| The visible reluctantly obviously erythema moderate of no erythema has eschar to serious erythema purple erythema | ????0 ????1 ????2 ????3 ????4 | The slight edema cutaneous protuberance of no edema profile is known edema protuberance 1mm and expanded range | ????0 ????1 ????2 ????3 |
Skin irritation intensity standards of grading
Mean scores is estimated
0～0.49 nonirritant
0.5～2.99 slight zests
3.0～5.99 moderate zests
6.0～8.0 intense stimulus
The bulleyaconitine A aerosol is to normal skin irritant average response value
In the group number of animals integration and the average response value
1h???24h???48h???72h???1h???24h???48h???72h
Blank solvent 443001 0.75 00
Experimental group 45300 1.2 0.8 00
The result: the bulleyaconitine A aerosol is to the stimulation and the blank no significant difference of normal skin as can be seen from the table.
The average response value that the bulleyaconitine A aerosol stimulates injured skin
In the group number of animals integration and the average response value
1h????24h???48h???72h???1h???24h???48h??72h
Blank solvent 443001 0.75 00
Experimental group 45410 1.3 0.85 0.06 0
The result: the bulleyaconitine A aerosol is to the stimulation and the blank no significant difference of injured skin as can be seen from the table.
By above result, can draw and the invention has the advantages that:
1, good stability: can place at normal temperatures 2 years, product is reliable and stable, and every index is all qualified, meets the requirements fully;
2, zest is little: do irritant experiment with Cavia porcellus, zest is 0 grade, proves no significant change; Anti-inflammatory analgesic action is strong: this product and the bulleyaconitine A injection effect basically identical aspect anti-inflammatory analgesic, but analgesic effect is rapid, and can be within 1min.
Embodiment 1
Prescription:
Bulleyaconitine A 0.2g
F
11???????????????????????20000ml
Preparation technology: under 10,000 grades condition, bulleyaconitine A is dissolved in the ethyl acetate of (2ml) below 10 times earlier, and notes it is dissolved fully.Note it is dissolved fully, get final product by common aerosol production.Be distributed into 1000 bottles of every bottle of 20ml
Embodiment 2
Prescription:
Bulleyaconitine A 0.2g
Azone??????????????????????2ml
F
12???????????????????????20000ml
Preparation technology: under 10,000 grades condition, bulleyaconitine A and Azone are dissolved in the ethyl acetate of (2ml) below 10 times earlier, and note it is dissolved fully.Note it is dissolved fully, get final product by common aerosol production.Be distributed into 1000 bottles of every bottle of 20ml
Embodiment 3
Prescription:
Bulleyaconitine A 0.2g
Azone??????????????????????2ml
Muscone 0.5ml
Coumarin 1g
F
114??????????????????????20000ml
Preparation technology: under 10,000 grades condition, bulleyaconitine A and Azone, muscone, coumarin are dissolved in the ethyl acetate of (2ml) below 10 times earlier, and note it is dissolved fully.Note it is dissolved fully, get final product by common aerosol production.Be distributed into 1000 bottles of every bottle of 20ml.
Claims (4)
1, a kind of bulleyaconitine A aerosol is characterized in that every ml contains bulleyaconitine A 0.01～0.8mg, makes pharmaceutically acceptable aerosol.
2, bulleyaconitine A aerosol according to claim 1 is characterized in that with in 0.05～10% Mentholum of principal agent amount or Camphora micromolecule terpenoid and/or Azone, CD, DMSO, muscone, the higher hydrocarbon alcohol one or more as medical penetration enhancer.
3, bulleyaconitine A aerosol according to claim 1 is characterized in that 0.002～5% the coumarin with certain ataralgesia effect, in the vanillin one or more with the principal agent amount is as medical spice.
4, the preparation method of bulleyaconitine A aerosol according to claim 1 is characterized in that making by following method:
A, under 10,000 grades of conditions, bulleyaconitine A is dissolved in the ethyl acetate below 10 times in advance fully;
B, the above-mentioned medical penetration enhancer of adding, and it is dissolved fully;
C, add above-mentioned flavouring agent again, and after it is dissolved fully, make aerosol and get final product.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031176658A CN1535683A (en) | 2003-04-09 | 2003-04-09 | Aconitum kusnezoffii methylsine aerosol and its preparation method |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA031176658A CN1535683A (en) | 2003-04-09 | 2003-04-09 | Aconitum kusnezoffii methylsine aerosol and its preparation method |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1535683A true CN1535683A (en) | 2004-10-13 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA031176658A Pending CN1535683A (en) | 2003-04-09 | 2003-04-09 | Aconitum kusnezoffii methylsine aerosol and its preparation method |
Country Status (1)
| Country | Link |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100391457C (en) * | 2004-10-29 | 2008-06-04 | 余娟 | Novel bulleyaconitine A powder injection and its production method |
-
2003
- 2003-04-09 CN CNA031176658A patent/CN1535683A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN100391457C (en) * | 2004-10-29 | 2008-06-04 | 余娟 | Novel bulleyaconitine A powder injection and its production method |
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