CN101480393A - Application of bulleyaconitine A in preparing medicament for treating Nav1.7 ache disease - Google Patents
Application of bulleyaconitine A in preparing medicament for treating Nav1.7 ache disease Download PDFInfo
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- CN101480393A CN101480393A CNA2008100580088A CN200810058008A CN101480393A CN 101480393 A CN101480393 A CN 101480393A CN A2008100580088 A CNA2008100580088 A CN A2008100580088A CN 200810058008 A CN200810058008 A CN 200810058008A CN 101480393 A CN101480393 A CN 101480393A
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- bulleyaconitine
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- disease
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Abstract
The invention relates to an application of bulleyaconitine A used for preparing medicine for treating Nav1.7 pain, which belongs to medicine containing effective organic ingredients, in particular to medicine using the bulleyaconitine A for treating a disease. The medicine contains excipient which plays roles in padding, bond, disintegration and lubrication, the bulleyaconitine A and the excipient are mixed to be pressed into tablets, and each tablet of bulleyaconitine A contains 0.1mg to 0.5mg of the bulleyaconitine A. The invention has the characteristics of rapid absorption by oral administration, low content in the brain for the medicine distributed in a body, long half life period, little toxicity, and no tolerant phenomenon or addiction.
Description
Technical field
The invention belongs to the medicine that contains effective organic principle, particularly with the medicine of bulleyaconitine A as the treatment disease.
Background technology
Nav1.7 pain comprises erythromelalgia, paroxysmal severe pain disease.(Primary erythermalgia PE) is autosomal dominant inherited disease to primary erythermalgia.General onset is familial heredity in adolescence more, and its symptom is burnt sample pain, redness and temperature for the acra intermittence and raise, and is caused by slight thermostimulation or exercise-induced thermogenesis usually.But, generally raise limbs and maybe will suffer from limb and immerse relief of symptoms in the cold water, but the latter easily causes gangrene, severe patient even by amputation, the state of an illness brings very big injury badly for patient's body and mind.With ill saltant NaV1.7 transfection HEK293 cell, discover that the activation of the NaV1.7 passage of sudden change moves to left to hyperpolarization, activation threshold reduces, and the passage inactivation slows down simultaneously.Characteristics such as the sudden change passage easily activates, current amplitude increase, open hour prolongation cause neuron can respond to small stimulation and continue excited.Paroxysmal severe pain disease is a kind of rare autosomal dominant pain, and symptom is the sudden burning pain of no sign, and painful area generally is positioned at rectum, eyes and jaw portion.Gardiner etc. discover paroxysmal severe pain disease, sudden change has taken place patient's SCN9A gene can cause the unusual (GardinerMR of other pain, Keith AP, Moffatt LS, et al.SCN9Amutations in paroxysmal extreme pain disorder:allelic variants underliedistinct channel defects and phenotypes.Neuron, 2006,52:767～774).11 routine Inheritance sexually transmitted disease (STD) examples and 2 routine Sporadic cases are discovered: 8 places are positioned at the missense mutation on the SCN9A gene.External electrophysiologic study to wherein three kinds of sudden changes shows that sudden change concentrates on the zone of sodium-ion channel control inactivation, has hindered the rapid deactivation of valtage-gated property sodium channel, and the open hour are prolonged.Therefore, because the mutational site difference on SCN9A, make in these two kinds of pain the sodium channel changing function different, so that they all there are differences to clinical treatment from ill mechanism, analogue also occurs (George ALJr.Inherited disorders of voltage-gated sodium channels.J Clin Invest in other sodium-ion channel disease, 2005,115:1990～1999).Our test shows, under 50mV and certain low-frequency pulse condition, but the remarkable minimizing neuron sodium ion electric current that the bulleyaconitine A state relies on reduces the Nav1.7 electric current and surpasses 90%, therefore, bulleyaconitine A can become the medicine of a kind of treatment and Nav1.7 pain disease.
Summary of the invention
The present invention seeks to according to the bulleyaconitine A pharmacological mechanism, provide a kind of with the application of bulleyaconitine A as preparation treatment and Nav1.7 pain medication.
The object of the invention realizes in the following manner:
It has comprised the excipient of filling, bonding, disintegrate and lubrication, and bulleyaconitine A and mixed with excipients are pressed into tablet.
Described bulleyaconitine A tablet contains bulleyaconitine A 0.1mg～0.5mg/ sheet,
The oral usage of this tablet and consumption are an a slice, 2～3 times on the one.
Bulleyaconitine A has significant analgesia, antiinflammatory to all kinds of chronic pains and improves the effect of physical and chemical index.In the clinical or zooperal pharmacokinetics of other bulleyaconitine A, it is fast that bulleyaconitine A has oral absorption, and distribution brain content is very low in the body.Half-life is longer, and toxicity is little and do not produce the characteristics that tolerate phenomenon, no addiction, and therefore, we infer that this medicine still can have same characteristics for the present invention in treatment Nav1.7 pain disease.
The specific embodiment
Embodiment 1.
Contain the 0.1mg bulleyaconitine A and mixed with excipients is pressed into the bulleyaconitine A tablet with every.
Embodiment 2.
Contain the 0.3mg bulleyaconitine A and mixed with excipients is pressed into the bulleyaconitine A tablet with every.
Embodiment 3.
Contain the 0.5mg bulleyaconitine A and mixed with excipients is pressed into the bulleyaconitine A tablet with every.
The excipient that above-mentioned bulleyaconitine A tablet adds be filling, bonding, disintegrate and lubrication, not with medicine generation physical-chemical reaction, no physiological action, nontoxic, the common additional material that has no adverse reaction.
The oral usage of above-mentioned tablet and consumption are an a slice, 2～3 times on the one.
Points for attention comprise:
1. twice medication interval time should not be less than 6 hours, keeps blood drug level in treatment window level.
2. when untoward reaction occurring, but the intravenous injection atropine, decrement or stop using; The extremely heavy person of reaction handles by aconite poisoning, and drug withdrawal.
3. should ban use of when the medicine character changes.
4. this product allergy sufferers is forbidden.Cardiac, anemia of pregnant woman and women breast-feeding their children's forbidding.
Untoward reaction: cause after only a few patient's medication that transience is slightly nervous, feel sick, words are numb and cardiopalmus etc.
Claims (2)
1, bulleyaconitine A has comprised the excipient of filling, bonding, disintegrate and lubrication as the application of preparation treatment Nav1.7 antalgesic medicine, it is characterized in that bulleyaconitine A and mixed with excipients are pressed into the bulleyaconitine A tablet.
2, bulleyaconitine A according to claim 1 is characterized in that as the application of preparation treatment with the Nav1.7 pain medication bulleyaconitine A tablet contains bulleyaconitine A 0.1mg/ sheet～0.5mg/ sheet.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008100580088A CN101480393A (en) | 2008-01-07 | 2008-01-07 | Application of bulleyaconitine A in preparing medicament for treating Nav1.7 ache disease |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CNA2008100580088A CN101480393A (en) | 2008-01-07 | 2008-01-07 | Application of bulleyaconitine A in preparing medicament for treating Nav1.7 ache disease |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101480393A true CN101480393A (en) | 2009-07-15 |
Family
ID=40877786
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNA2008100580088A Pending CN101480393A (en) | 2008-01-07 | 2008-01-07 | Application of bulleyaconitine A in preparing medicament for treating Nav1.7 ache disease |
Country Status (1)
| Country | Link |
|---|---|
| CN (1) | CN101480393A (en) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102552254A (en) * | 2012-02-07 | 2012-07-11 | 云南昊邦制药有限公司 | Application of bulleyaconitine A used as state-independent sodium ion channel blocker to analgesia |
| CN103930437A (en) * | 2011-03-16 | 2014-07-16 | 安姆根有限公司 | Potent and selective inhibitors of Nav1.3 and Nav1.7 |
| CN110536895A (en) * | 2017-01-24 | 2019-12-03 | 奥利通公司 | SCN9A antisense anodyne |
-
2008
- 2008-01-07 CN CNA2008100580088A patent/CN101480393A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN103930437A (en) * | 2011-03-16 | 2014-07-16 | 安姆根有限公司 | Potent and selective inhibitors of Nav1.3 and Nav1.7 |
| CN102552254A (en) * | 2012-02-07 | 2012-07-11 | 云南昊邦制药有限公司 | Application of bulleyaconitine A used as state-independent sodium ion channel blocker to analgesia |
| CN110536895A (en) * | 2017-01-24 | 2019-12-03 | 奥利通公司 | SCN9A antisense anodyne |
| CN110536895B (en) * | 2017-01-24 | 2023-10-20 | 奥利通公司 | SCN9A antisense analgesic |
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Legal Events
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| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |
Open date: 20090715 |