CN106963763A - Compound and its medical usage - Google Patents
Compound and its medical usage Download PDFInfo
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- CN106963763A CN106963763A CN201710089611.1A CN201710089611A CN106963763A CN 106963763 A CN106963763 A CN 106963763A CN 201710089611 A CN201710089611 A CN 201710089611A CN 106963763 A CN106963763 A CN 106963763A
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- ritalin
- aplactan
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
- A61K31/4458—Non condensed piperidines, e.g. piperocaine only substituted in position 2, e.g. methylphenidate
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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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
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Abstract
The invention discloses a kind of compound, the compound includes：Ritalin and aplactan.By the above-mentioned means, the present invention can play effective reference function in terms of dizziness is prevented and treated, and then effective medicine effect may be further functioned as, and drug side-effect is relatively fewer.
Description
Technical field
The present invention relates to pharmaceutical technology field, more particularly to a kind of compound and its medical usage.
Background technology
Motion sickness betides people and takes the vehicles such as car and boat or carry out space flight, aviation or navigation operation, receives different
During normal vestibular stimulation and/or abnormal vision stimulation, mainly have pale complexion, cold sweat, salivation, indifferent, abdominal discomfort, dizziness,
The neuro-vegetative responses such as Nausea and vomiting.Documents and materials show that the navigation under severe sea condition, almost all occupant can be seasick；Space flight
During operation, although there is simulated training on ground, motion sickness incidence is still up to 60%-80%.Although leaving after movement environment
Motion sickness will progressively be eased, but it significantly affects the normal travelling of part sensitive subjects and in the spy such as Aeronautics and Astronautics and navigation
Operation under different environment.Meniere disease is based on the rotatory vertigo that breaks out, and with tinnitus, deafness, head or ear
The symptoms such as sensation of fullness are a kind of disease of inner ear of principal character, and the violent person of dizziness can be with symptoms such as Nausea and vomiting, cold sweats.
Meniere disease is often fallen ill urgency, is otorhinolaryngologic difficult treatment easily repeatedly.
Existing motion sickness drug species are various, and antihistamine dramamine is most commonly used that at present.For Meniere disease
Treatment, main at present using remedy measures such as anti-blooming, calmness, expansion blood vessel, dehydration and supporting treatments, expectant treatment is invalid
When, it is considered to operative treatment, such as endolymphatic sac decompression or bypass, neurotomy of vestibular nerve, lost damage or resection.
Present inventor has found in long-term R＆D process, the useful effect of above-mentioned anti-kinetosis Common drugs
Position is not known, and side effect is relatively strong, and the especially side effect such as CNS inhibition, eye-blurred can influence people in various spies
Operation under different environmental condition.Treatment method simultaneously for Meniere disease or therapeutic effect is had influence on, or brought
The even serious side effect such as hearing damage and vestibular function.
The content of the invention
The present invention solves the technical problem of a kind of compound is provided, it can be played in terms of dizziness is prevented and treated
The reference function of effect, and then effective medicine effect may be further functioned as, and drug side-effect is relatively fewer.
In order to solve the above technical problems, one aspect of the present invention is：A kind of compound is provided, it is described
Compound includes：Ritalin and aplactan.
In order to solve the above technical problems, another technical solution used in the present invention is：One kind is provided and prevents and treats motion sickness, plum
The sick medical composition of Buddhist nun angstrom, the medical composition includes the ritalin and brain for preventing and treating motion sickness, Meniere disease effective dose
Beneficial piperazine compound and pharmaceutically acceptable carrier.
In order to solve the above technical problems, another technical scheme that the present invention is used is：Ménière in a kind of preventing and treating is provided
Medical composition, the medical composition includes the ritalin and aplactan compound of Ménière effective dose in preventing and treating
And pharmaceutically acceptable carrier.
In order to solve the above technical problems, another technical scheme that the present invention is used is：A kind of doctor for preventing and treating dizziness is provided
Drug composition, the medical composition includes the ritalin and aplactan compound and medicine for preventing and treating dizziness effective dose
Upper acceptable carrier.
In order to solve the above technical problems, another technical scheme that the present invention is used is：A kind of ritalin and brain benefit are provided
Purposes of the piperazine compound in motion sickness, the preparation of the medicine of Meniere disease is prevented and treated.
In order to solve the above technical problems, another technical scheme that the present invention is used is：A kind of ritalin and brain benefit are provided
Purposes of the piperazine compound in the preparation of medicine of dizziness is prevented and treated.
The beneficial effects of the invention are as follows：Be different from the situation of prior art, compound of the present invention include ritalin and
Aplactan, ritalin is a kind of cerebral cortex excitant, it is possible to increase the arousal level of central nervous system.Aplactan is a kind of
Ménière has certain curative effect in calcium antagonist, confrontation.Ritalin and aplactan compatibility are used, respective anti-blooming is utilized respectively
Mechanism, makes the two play synergy, while respective anti-blooming effect is strengthened, and can also resist the unfavorable work in mutual part
With while the two toxic side effect produced is relatively fewer.Therefore, ritalin and aplactan compound can prevent and treat dizziness
Aspect plays effective reference function, and then may further function as effective medicine effect, and drug side-effect is relatively fewer.
Embodiment
First simply introduce the prior art scenario of correlation.
Motion sickness betides people and takes the vehicles such as car and boat or carry out space flight, aviation or navigation operation, receives different
During normal vestibular stimulation and/or abnormal vision stimulation, mainly have pale complexion, cold sweat, salivation, indifferent, abdominal discomfort, dizziness,
The neuro-vegetative responses such as Nausea and vomiting.Motion sickness research history for a long time, but its detailed pathogenesis is still not very clear,
Still lack the medicine efficiently having no side effect at present in terms of motion sickness preventing and treating.Existing motion sickness resistant medicament has a variety of, but this
A little medicine useful effect positions are unclear, and side effect is larger, and the especially side effect such as CNS inhibition, eye-blurred can influence people
Operation under various special environment conditions.
Meniere disease is the rotatory vertigo broken out, and is with symptoms such as sensations of fullness in tinnitus, deafness, head or ear
A kind of disease of inner ear of principal character, the violent person of dizziness can be with symptoms such as Nausea and vomiting, cold sweats.Meniere disease is ear nose
Larynx section common disease and frequently-occurring disease, are fallen ill common with monaural.Research for many years finds that Meniere disease and immune response, plant are refreshing
Relevant through the factor such as dysfunction or infection, these factors or interference inner ear microvascular function cause capillary and vein to return
Stream is obstructed, or blocks ductus endolymphaticus, endolymph fluid malabsorption, causes labyrintine hydrops, causes inner ear equilibrium function to be lacked of proper care.
Meniere disease is often fallen ill urgency, is otorhinolaryngologic difficult treatment easily repeatedly.For the treatment of Meniere disease, due to the cause of disease so far
Not yet get clear completely, at present clinic mainly for its pathophysiological process based on symptomatic treatment, using anti-blooming, calmness, expansion
The remedy measures such as blood vessel, dehydration and supporting treatment, when expectant treatment is invalid, it is considered to operative treatment：Endolymphatic sac decompression or shunting
Art, neurotomy of vestibular nerve, lost damage or resection etc..These methods or therapeutic effect is had influence on, or brought
The unnecessary serious side effect of even hearing damage and vestibular function etc..
The compound ritalin and aplactan of the present invention is respectively provided with anti-blooming effect, and toxic side effect is lighter, Ke Yiwei
Effective medicine effect is provided in terms of preventing and treating dizziness.
The technical scheme in the embodiment of the present invention will be clearly and completely described below, it is clear that described implementation
Example only a part of embodiment of the invention, rather than whole embodiments.Based on the embodiment in the present invention, the common skill in this area
The every other embodiment that art personnel are obtained under the premise of performing creative labour is not made, belongs to the model that the present invention is protected
Enclose.
The present invention provides a kind of compound, and the compound includes ritalin and aplactan.
Ritalin is a kind of cerebral cortex excitant for comparing mitigation, mainly by promoting dopamine and norepinephrine
Release, and suppress its reabsorption, improve the arousal level of central nervous system, thus reach excited spirit, eliminate suppress with
The melancholy, effect of relieving fatigue sense.There is slight excitation to cerebral cortex and subcortical center and respiratory center, it is also directly emerging
Put forth energy sympathetic nerve, so as to play a part of resisting dizziness.But using extensive central excitation can be caused during larger dose, even
Cause convulsions.But comparatively the effect to human body more relaxes, and toxic side effect is less, orally there are slight quickening heart rate and boosting
Effect.Ritalin is clinically mainly used in treatment attention deficit hyperactivity disorder, and (hyperkinetic syndrome, slight brain function is lost
Adjust), narcolepsy, central respiratory failure, various depression, and the central depressant such as barbiturates, chloraldurate
Stupor etc. caused by amount.
Aplactan be piperazines calcium antagonist, have direct dilating effect to vascular smooth muscle, can significantly improve Brain circlulation and
Coronary circulation, also prevents vascular sclerosis from acting on.In addition, aplactan also has antihistamine, medmain, anti-kassinin kinin activity and suppression
The effect of Complement C4 activation processed.Aplactan is clinically mainly used in treatment cerebral thrombosis, cerebral embolism, cerebral arteriovenous malformation, brain
Bleeding convalescence, subarachnoid hemorrhage convalescence, post-traumatic brain syndrome, coronary sclerosis and peripheral circulation is bad causes
Illness.Available for treatment chronic urticaria, the elderly's cutaneous pruritus, UGB, insomnia of the middle aged and elderly etc., Ke Yiyong
In Ménière in preventing and treating.Aplactan Ménière in preventing and treating is used relatively weak, but toxic side effect is less, occasionally have it is drowsiness,
The gastrointestinal reaction such as tired, fash and nausea, poor appetite, intravenous injection can make the of short duration decline of blood pressure.
Ritalin and aplactan compatibility are used to prevent and treat dizziness in the application, find that there is critically important practical value.
Ritalin is utilized respectively respective anti-blooming mechanism with aplactan when using, and the two is played synergy, and the two is strengthening respective
Anti-blooming effect while, can also resist mutual part detrimental effect, such as ritalin can resist brain benefit to a certain extent
The drowsiness side effect of piperazine.The toxic side effect that the two is produced is relatively fewer.Therefore, ritalin and aplactan compound can
Effective reference function is played in terms of dizziness is prevented and treated, and then effective medicine effect may be further functioned as, and medicine pair is made
With relatively fewer.
Wherein, the mass ratio of ritalin and aplactan is 2:5.
The present invention also provide it is a kind of prevent and treat motion sickness, the medical composition of Meniere disease, the medical composition includes preventing and treating
Motion sickness, the ritalin of Meniere disease effective dose and aplactan compound and pharmaceutically acceptable carrier.
Wherein, the effective dose ratio of ritalin and aplactan is 2:5.
The present invention also provides a kind of medical composition of Ménière in preventing and treating, and the medical composition includes Ménière in preventing and treating
The ritalin and aplactan compound of effective dose and pharmaceutically acceptable carrier.
Wherein, the effective dose ratio of ritalin and aplactan is 2:5.
The present invention also provides a kind of medical composition for preventing and treating dizziness, and the medical composition includes and prevents and treats dizziness effective dose
Ritalin and aplactan compound and pharmaceutically acceptable carrier.
Wherein, the effective dose ratio of ritalin and aplactan is 2:5.
The present invention also provides a kind of ritalin and aplactan compound and is preventing and treating motion sickness, the medicine of Meniere disease
Purposes in preparation.
Wherein, the effective dose ratio of ritalin and aplactan is 2:5.
The present invention also provides a kind of use of ritalin and aplactan compound in the preparation of medicine of dizziness is prevented and treated
On the way.
Wherein, the effective dose ratio of ritalin and aplactan is 2:5.
Hereinbefore ritalin and aplactan compound may make up the active component of medical composition, and generally can be with
The appropriate excipients or carrier suitably selected are mixed to be administered in the form of oral tablet or capsule.For example tablet, capsule, pill,
The dosage composition such as suppository and powder depends on predetermined administering mode, and it can pass through any acceptable approach.These administrations
Approach include by oral administration, intravenous injection (intravenous), intramuscular injection (intramuscular injection), (subcutaneous) etc. is subcutaneously injected.Can in a patient
To use one or more in these approach.In one embodiment, compound of the invention is used as oral dosage form administration
And can be combined with nontoxic pharmaceutically acceptable non-active carrier, such as water, glycerine, ethanol etc..Can also orally it mix
The inert excipient for being typically used as adhesive, disintegrant and colouring agent is added in compound.
When needing, the medical composition given also can include a small amount of innocuous substance, for example pH buffer, emulsifying agent,
Sodium acetate etc..Using the dosage of compound by depending on the species of patient, sex, body weight, age, medical condition, administration
The sanatory order of severity of approach and institute.Skilled medical practitioner can be readily determined to be had with the medicine of predetermined treatment disease
Imitate dosage.
Depending on the disease and situation of patient, terms used herein " treatment " includes curing treatment, palliative treatment and prevention
Property treatment in one or more.The exact dose that each reactive compound is applied will vary depending on a number of factors, these because
Element includes but is not limited to the type of patient and treats the type of morbid state, the age of patient and method of administration.
For above-mentioned therapeutical uses, institute's applied dose certainly can be with institute's method of application, required treatment and meaning
The disease shown and change.Total daily dose can be applied with single dose or fractionated dose.The present invention is also covered by slow releasing composition.
For example, medical composition can be in the form for being adapted to oral administration medicine supplying, such as tablet, capsule, pill, powder, slow
Release composite, solution.Medical composition can be in the unit dosage form for the single administration for being suitable for exact dose.Medicinal combination
Thing is by including conventional medical carrier and reactive compound.In addition, it may include other medicinal or medical agent, carrier, adjuvants etc..
Suitable medical carrier includes inert diluent or filler, water.If desired, medical composition can be included in addition
Composition, such as flavor enhancement, adhesive and analogous components.Therefore for being administered orally, containing the various excipient such as citric acid
Tablet can be with various disintegrants (such as starch, alginic acid and some composition silicates) and adhesive (such as sucrose, gelatin
And Arabic gum) be used together.In addition, the lubricant such as magnesium stearate, NaLS and talcum is frequently used for preparing
Tablet.The solid composite of similar type can also be used in soft hard-filled gelatin capsule.The useful constituent bag of these compositions
Include lactose or toffee and high molecular weight polyethylene glycol.When oral administration needs to use water suspension or elixir, activity therein
Compound can be with various sweeteners or flavor enhancement, pigment or dyestuff and optionally emulsifying agent or suspending agent and diluent
(such as water, ethanol, propane diols, glycerine) or its combination are combined.
The technical staff in the field knows or will become apparent from preparing various medical groups of the reactive compound with specified quantitative
The method of compound.
Listed dosage range is only exemplary herein, it is therefore intended that scope or the practice of composition are advocated in limitation.Lift
For example, dosage can be adjusted according to pharmacokinetics or pharmacodynamic parameter, pharmacokinetics or pharmacodynamic parameter
It may include clinical effect such as toxic effect and/or laboratory evaluation.Therefore, the present invention covers patient determined by those skilled in the art
Interior dosage escalation.It is determined that it is known in the related art using the suitable dose and scheme of chemotherapeutics, and once provide herein
Disclosed religious doctrine, it should be understood that covered by the technical staff in the field.
The medical composition of the present invention can be with bulk form, with single unit dosage form or with multiple single unit doses
Amount form is prepared, packs or sold." unit dose " used herein is the medical composition of the reactive compound comprising scheduled volume
Discrete amount.The amount of reactive compound, which is generally equal to, will be applied to the dosage or this dose of the reactive compound of subject
One convenient fraction, for example, for example, a half or thirds of this dose.
Reactive compound in medical composition of the present invention, pharmaceutically acceptable carrier and any other composition it is relative
Amount is by the identity according to treated subject, size and situation and is further changed according to the dosing way of composition.Citing
For, composition can include the active component between 0.1% and 100% (w/w).
In addition to the active compound, medical composition of the invention, which can further include, one or more other is as above begged for
The treatment active compounds of opinion.
Illustrate that complex composition ritalin and aplactan are provided effectively in terms of dizziness is prevented and treated with specific data below
Reference function.
The application has carried out related rotation test research of the relevant ritalin joint aplactan in terms of dizziness is prevented and treated, it was demonstrated that
Ritalin and aplactan compound have the effect for clearly resisting dizziness, are it as a kind of new combating vertigo medicine and its clinic
Using there is provided more complete experimental basis.Following each experiment, which is merely to illustrate ritalin and aplactan compound, has resistance dizziness
Effect, it is impossible to be considered as limiting the scope of the invention.Specifically：Respectively using beasle dog and male volunteers as research pair
As designing, different types of medicines and dosage group carry out rotation test, to determine that ritalin and aplactan compound are dizzy to preventing and treating
Dizzy effect.As a result show, compound treatment group is in nystagmus duration and the nystagmus average slow phase for suppressing rotatory stimulation induction
Ritalin and alone group of aplactan are superior in speed, both this explanations have certain synergy.In addition, compound treatment group
The incubation period and drop of the high dose group of middle dose group and compound treatment group salivation and vomiting after extension beasle dog rotatory stimulation
The low dose group and dramamine group of compound treatment group are superior on the average slow phase velocity of nystagmus of low rotatory stimulation induction, this
Illustrate that ritalin and aplactan compound also have a certain degree of influence on dosage on curative effect.Therefore, ritalin is combined
Aplactan is used, and is preventing and treating the especially interior Ménière of dizziness, will specifically be answered in motion sickness and Meniere disease with good
Use prospect.
The dramamine used in following experiments is produced by Huaihai Pharmaceuticla Factory, Shanghai, and ritalin is limited by the pharmacy of Suzhou the 1st
Company is produced, and aplactan is produced by Yan'an Pharmaceutical Plant, Shanghai.
Experiment 1
Ritalin extends salivation, the vomiting incubation period of rotatory stimulation induction with aplactan compound in beasle dog
20 beasle dogs are taken, wherein, male 13, female 7, body weight is 6~7kg.According to sex ratio, lattice will be compared
Dog is randomly divided into male 2-3 in 5 groups, every group, and only, female 1-2 is only.
Experiment is divided into 5 groups of progress：Control group, dramamine group, ritalin and aplactan compound low dose group, ritalin with
Aplactan compound middle dose group, ritalin and aplactan compound high dose group.
Control group：500mg starch is poured into capsule；
Dramamine group：Consumption is converted to obtain beasle dog consumption 8mg/6kg body weight by people 50mg, and 8mg medicines are poured into capsule,
Plus starch is to 500mg；
Ritalin and aplactan compound low dose group：Total drug dose be 3.5mg (ritalin 1mg, aplactan 2.5mg)/
6kg body weight, capsule is poured into by 3.5mg medicines, plus starch is to 500mg；
Ritalin and aplactan compound middle dose group：Total drug dose is 7mg (ritalin 2mg, aplactan 5mg)/6kg bodies
Weight, capsule is poured into by 7mg medicines, plus starch is to 500mg；
Ritalin and aplactan compound high dose group：Total drug dose is 14mg (ritalin 4mg, aplactan 10mg)/6kg
Body weight, capsule is poured into by 14mg medicines, plus starch is to 500mg.
Before drug test, to understand each beasle dog to the sensitiveness of rotatory stimulation, first give rotatory stimulation 1 time, do not give
Drug-treated, records each beasle dog salivation, the time of vomiting appearance, salivated between the beasle dog each group after rotatory stimulation, vomits
Telling incubation period does not have significant difference (p>0.05).Rest carries out drug study after 4 days.
Rotatory stimulation device is copied with reference to Crampton (Crampton) and Lv Ke (Lucot) (1985) report and formed.
During experiment by animal it is chainless be put into the lucite cage of rotating device, rotated around trunnion axis.Clockwise accelerate, slow down with
Accelerate counterclockwise, slow down alternately, 20s a cycles.Wherein, phase 7.5s, deceleration 2.5s are accelerated, adding during acceleration
Speed is 16 °/s2, acceleration during deceleration is -48 °/s2, 700 ° of rotational steps.Beasle dog stops rotation after there is vomiting
Turn, the time that the salivation of record beasle dog and vomiting occur.
Before experiment, each beasle dog is given rotatory stimulation is carried out after relative medicine, 1.5h respectively, and record salivation, vomiting occur
Time.If rotated after 30min, beasle dog still occurs without salivation and vomiting reaction, that is, stops the rotation, and represents that it flows with 30min
Saliva and vomiting incubation period.Each group of data represents that group difference uses the variance analysis of Group Design, two-by-two with mean ± standard deviation
Compare and examined using Scheffe method (Scheffe).
Wherein, during drug test, without notable when control animals salivation, vomiting time of occurrence are compared with preliminary experiment after rotatory stimulation
Property change (p>0.05)；Medicine refers to table 1 to being salivated after beasle dog rotatory stimulation and vomitting preclinical influence.
The medicine of table 1 is on salivating and vomitting preclinical influence (min, n=4) after beasle dog rotatory stimulation
Note：Vs control groups；⊿p<0.05,⊿⊿p<0.01, vs low dose group and dramamine group.
The result of table 1 shows that dramamine group, ritalin and aplactan compound low dose group animal salivate, vomiting incubation period
It increased compared with control group, but not statistically significant (p>0.05)；Ritalin is moved with aplactan compound middle dose group, high dose group
Logistics saliva, vomiting incubation period are obviously prolonged (p compared with control group<0.05 or 0.01).Meanwhile, ritalin and agent in aplactan compound
The salivation of amount group animal, vomiting incubation period are also longer than low dose group and dramamine group (p<0.05 or 0.01)；Ritalin and brain benefit
Piperazine compound middle dose group and high dose group animal salivate, (the p that compared that there was no significant difference between vomiting incubation period>0.05).This says
Bright ritalin can extend after beasle dog rotatory stimulation what is salivated and vomit with aplactan compound middle dose group and high dose group
Incubation period.
Experiment 2
The nystagmus that ritalin suppresses rotatory stimulation induction with aplactan compound is compared with the effect being used alone
8 male trial volunteers, the age is healthy at 22-27 Sui, and excludes and following may influence experimental result
Illness：Cardiovascular and cerebrovascular disease such as hypertension, coronary heart disease, the auditory disease of vestibular, spontaneous nystagmus and eye are dynamic abnormal, nerveous system
Disease of uniting and dysfunction, experiment is prohibited in first 48 hours to be taken sedative and Loratadine and forbids drinking, and experimental day is prohibited
Only smoking, coffee for drinking etc. have the beverage of excitation, avoid strenuous exercise.
8 male's trial volunteer's stochastic averaginas are divided into 4 groups of progress by experiment, are respectively：Control group, ritalin group, brain
Beneficial piperazine group, ritalin and aplactan compound group.
Control group：Use starch piece 2；
Ritalin group：Total drug dose is 1 10mg of ritalin piece, separately adds starch piece 1；
Aplactan group：Total drug dose is 1 25mg of stutgeron tablet, separately adds starch piece 1；
Ritalin and aplactan compound group：Total drug dose is the 10mg+ stutgeron tablets 1 of ritalin piece 1 25mg.
It is oral above.
The JKY-II types electric revolving chair produced using Beijing Aviation Institute for Medical Research carries out rotatory stimulation, and swivel chair presses 15 °/s2
120 °/s is accelerated to, 52s is rotated under this maximum angular rate, then the jerk in 0.5s.The RM- produced with Japanese photoelectricity company
Electronystagmograph after 6000 type polygraphs record swivel chair jerk.
Preliminary experiment shows the nystagmus Bilateral Symmetry that everybody subject rotatory stimulation induces.
Drug test is carried out 4 weeks using Latin―Square design order, and once in a week, 1h, 2h, 4h are each before medication and after medication
A rotatory stimulation is carried out, observation medicine is to nystagmus duration, the influence of average slow phase velocity.Each group of data is and medication
The preceding relative value (%) compared, is represented with mean ± standard deviation, and group difference uses the variance analysis of Group Design, compares two-by-two
Examined using Scheffe, experimental result is as shown in table 2, table 3.
Influence (%, n=8) of the medicine of table 2 to the nystagmus duration
Note：*p<0.05, * * p<0.01, vs control group；Vs ritalin groups；⊿p<0.05,⊿⊿p<
0.01, vs aplactan group.
Influence (%, n=8) of the medicine of table 3 to the average slow phase velocity of nystagmus
Note：*p<0.05, * * p<0.01, vs control group；Vs ritalin groups；⊿p<0.05,⊿⊿p<0.01, vs
Aplactan group.
The result of table 2 shows, ritalin group, aplactan group and ritalin and aplactan compound group each time after the tablet has been ingested
Point can suppress the nystagmus duration of rotatory stimulation induction, but can will become apparent from the effect of ritalin and aplactan compound group
It is most strong, act on still obvious after the 4h that even takes medicine.Meanwhile, table 3 show ritalin group, aplactan group and ritalin with
Each point in time can suppress the average slow phase velocity of nystagmus of rotatory stimulation induction to aplactan compound group after the tablet has been ingested, but with table 2
As a result consistent, ritalin and the effect of aplactan compound group are substantially most strong, act on still obvious after medication 4h.This explanation
Ritalin and aplactan compound have very strong cooperate with terms of reducing the nystagmus duration and suppressing the average slow phase velocity of nystagmus
Effect.
Experiment 3
Ritalin suppresses the nystagmus of rotatory stimulation induction and the effect ratio of positive control drug with aplactan various dose compound
Compared with
10 aspirations participate in the Male Students ' of experiment, age 19-21 Sui, healthy, and exclude following possible influence
The illness of experimental result：Cardiovascular and cerebrovascular disease such as hypertension, coronary heart disease, the auditory disease of vestibular, spontaneous nystagmus and eye move different
Often, the nervous system disease and dysfunction, experiment is prohibited in first 48 hours to be taken sedative and Loratadine and forbids drinking, real
Testing the same day, no smoking, coffee for drinking etc. has the beverage of excitation, avoids strenuous exercise.Preliminary experiment shows everybody subject rotation
The nystagmus Bilateral Symmetry of Induced by Stimulation.
10 male's trial volunteer's stochastic averaginas are divided into 5 groups of progress by experiment：Control group, positive control medicine group, profit
His woods and aplactan compound low dose group, ritalin and aplactan compound middle dose group, ritalin and aplactan compound high dose
Group.
Control group：Use starch piece 4；
Positive control medicine group：Total drug dose is 1 25mg of dimenhydrinate tablets, separately adds starch piece 3；
Ritalin and aplactan compound low dose group：Total drug dose is ritalin piece half 5mg, stutgeron tablet half
12.5mg, separately adds starch piece 3；
Ritalin and aplactan compound middle dose group：Total drug dose is 1 10mg of ritalin piece, stutgeron tablet 1
25mg, separately adds starch piece 2；
Ritalin and aplactan compound high dose group：：Total drug dose is 2 20mg of ritalin piece, stutgeron tablet 2
50mg。
Each medicine loads capsule above, orally.
Rotatory stimulation is carried out using JKY-II types electric revolving chair, swivel chair accelerates to 120 °/s by 15 °/s2, in this maximum angular
52s is rotated under speed, then the jerk in 0.5s.The nystagmus after swivel chair jerk is recorded with RM-6000 types polygraph
Electrograph.Drug test is carried out 5 weeks using Latin―Square design order, and once in a week, 2h is respectively carried out once before medication and after medication
Rotatory stimulation, observation medicine is to nystagmus leading indicator --- the influence of average slow phase velocity.All results are used before and after medication
Own control paired t-test.Experimental result is as shown in table 4.
Influence (mV/s, n=10) of the medicine of table 4 to the average slow phase velocity of nystagmus
Note：*p<Before 0.05, vs medication.
As shown in Table 4, rotatory stimulation induction can be reduced after the middle and high dosage group medication that ritalin is shared with aplactan
The average slow phase velocity of nystagmus；But, the low dose group and positive control medicine group that ritalin is shared with aplactan are without substantially work
With the synergy of this explanation ritalin and aplactan may be low relevant with dosage.
Embodiments of the present invention are the foregoing is only, are not intended to limit the scope of the invention, it is every to utilize this
Equivalent structure or equivalent flow conversion that description of the invention content is made, or directly or indirectly it is used in other related technology necks
Domain, is included within the scope of the present invention.
Claims (10)
1. a kind of compound, it is characterised in that the compound includes：Ritalin and aplactan.
2. compound according to claim 1, it is characterised in that
The mass ratio of the ritalin and aplactan is 2:5.
3. a kind of prevent and treat motion sickness, the medical composition of Meniere disease, it is characterised in that the medical composition is transported comprising preventing and treating
Dynamic disease, the ritalin of Meniere disease effective dose and aplactan compound and pharmaceutically acceptable carrier.
4. medical composition according to claim 3, it is characterised in that
The effective dose ratio of the ritalin and aplactan is 2:5.
5. the medical composition of Ménière in a kind of preventing and treating, it is characterised in that the medical composition includes Ménière in preventing and treating
The ritalin and aplactan compound of effective dose and pharmaceutically acceptable carrier.
6. medical composition according to claim 5, it is characterised in that
The effective dose ratio of the ritalin and aplactan is 2:5.
7. a kind of medical composition for preventing and treating dizziness, it is characterised in that the medical composition includes and prevents and treats dizziness effective dose
Ritalin and aplactan compound and pharmaceutically acceptable carrier.
8. medical composition according to claim 7, it is characterised in that
The effective dose ratio of the ritalin and aplactan is 2:5.
9. a kind of purposes of ritalin and aplactan compound in motion sickness, the preparation of the medicine of Meniere disease is prevented and treated.
10. a kind of purposes of ritalin and aplactan compound in the preparation of medicine of dizziness is prevented and treated.
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| 姜正林: "运动病发病机制与防治措施", 《交通医学》 * |
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