CN102872016A - Medicine combination - Google Patents
Medicine combination Download PDFInfo
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- CN102872016A CN102872016A CN2012103856556A CN201210385655A CN102872016A CN 102872016 A CN102872016 A CN 102872016A CN 2012103856556 A CN2012103856556 A CN 2012103856556A CN 201210385655 A CN201210385655 A CN 201210385655A CN 102872016 A CN102872016 A CN 102872016A
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- huperzine
- memantine
- pharmaceutical composition
- dementia
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Abstract
A medicine combination is prepared by mixing memantine hydrochloride, huperzine B, huperzine A and pharmaceutically acceptable auxiliary materials, wherein the memantine hydrochloride, the huperzine B and the huperzine A serve as active pharmaceutical ingredients. The medicine combination can be used for treating sequelae of brain infarction and various dementia.
Description
Technical field
The present invention relates to a kind of pharmaceutical composition and preparation method thereof, belong to medical technical field.
Background technology
Cerebral infarction sequela refers in the cerebral infarction morbidity after 1 year, if also there are the symptoms such as hemiplegia or aphasis or facial hemiparalysis, just be called cerebral infarction sequela, also be called the cerebral infarction sequela phase this period, compare with convalescent period, resume speed and degree are slower.Mainly contain hemiplegia (hemiplegia), half side physical handicaps, numb limbs and tense tendons, hemianopsia, aphasia.Perhaps crossed paralysis, contralateral sensory disturbance, ophthalmoplegia externa, nystagmus, dyslalia, aphasis, hypomnesis, facial hemiparalysis, dysphagia, choke food choke water, ataxia, dizziness headache etc.Basic reason is that the dysemias such as blood viscosity height, blood fat height, hypertension, blood glucose height, platelet aggregation appear in cerebrovascular inside, with vascular lesions such as atheromatous plaque formation, the thrombosis that is formed by two kinds of pathological changes combined effect results stops up due to the cerebral arteries, causes the blood flow of brain part to interrupt and the necrosis of cerebral tissue hypoxic-ischemic.
Dementia is by the course of disease syndrome due to the carrying out property cerebral disorders slowly.Feature is that multiple senior function of cortex is disorderly, relates to the many-sides such as memory, thinking, orientation, understanding, calculating, judgement, speech and learning capacity.Consciousness, the emotion self-control is poor, the decline of social activity or motivation, and normal and cognitive impairment accompanies, but sometimes can occur early than cognitive impairment.Mainly be divided into the dementia that the brain degenerative disease causes according to its cause of disease---dementia, mixed dementia three major types that Alzheimer dementia, cerebrovascular cause.
Alzheimer (Alzheimer disea se, AD) is one group of constitutional degeneration brain degenerative disease that the cause of disease is not bright.A lot of diseases are in the geratic period, the onset of hiding, and the course of disease is slow and irreversible, clinically take the intelligence infringement as main.Pathological change is mainly the cortex diffuse atrophy, and ditch returns broadening, and the ventricles of the brain enlarge, and neuron reduces in a large number, and visible senile plaque, the neurofibril knot) etc. pathological changes, choline acetylase and acetyl choline content significantly reduce.The Alzheimer main manifestations is the brain cell of the extensive death, particularly basal ganglia region of brain cell.Under normal circumstances, the Fiber Projections that basal ganglia region is sent is to the brain cortex relevant with memory and cognition, and it discharges acetylcholine.The formation of impermanent memory must have the participation of acetylcholine, and the patient compares acetylcholine transferase with the normal person content reduces 90% than the normal person.Be a kind of lethal neurodegenerative diseases that carries out sexual development, clinical manifestation constantly worsens for cognitive and memory function, and carrying out property of activity of daily living goes down, and various neuropsychic symptoms and behavior disorder are arranged.Prevalence studies show that 60 years old crowd's prevalence is 1%, and 85 years old crowd's prevalence is 30%.
Vascular dementia refers to the dementia due to the cerebrovascular blood supply disorder that a variety of causes causes.Age of onset is many at 50 ~ 60 years old, and take the male as many, patients more than half have hypertension, hyperlipemia, Atheromatosis history.This is because the vascular dementia generation is many after cardiovascular and cerebrovascular disease, and cardiovascular and cerebrovascular disease is take the male patient as many.The primary disease PD is rapid, and repeated multiple times apoplectic seizure is arranged in the medical history, how namely to occur soon dull-witted at post-stroke.The state of an illness is stage ladder sample progress.
Mixed dementia has the symptom of senile dementia and vascular dementia simultaneously.Add up according to European and American countries: the dementia that the brain degenerative disease causes---Alzheimer accounts for more than 50%, and the vascular dementia that cerebrovascular causes accounts for 15% ~ 20%.Statistics according to Japan: Alzheimer accounts for 33.7%, and vascular dementia accounts for 36.3%,
Mixed dementia accounts for 19.5%, the dementia that other reasons causes accounts for 10.5%.The reconnaissance information in 27 town and country of China shows: more than 60 years old the patient of old man's medium vessels dementia to lead be 3,24/,100,000 populations, Alzheimer is 2,38/,100,000 populations; The prevalence city of vascular dementia is higher than the rural area, Alzheimer antithesis, the rural area is more than the city.
Along with progressing into of Chinese aging society, treatment cerebral infarction sequela and senile dementia become a very important field.
Huperzine A (Huperzine A) is by Huperziaceae plant Herba Lycopodii serrati Huperzinaserrata (Thumb.)
A kind of alkaloid that extracts among the Trev is a potent acetylcholine esterase reversible inhibitor.True cholinesterase is had optionally inhibition, and inhibition strength is thousands of times of pseudocholinesterase; Suppressor mode is that competitive and noncompetitive mixed type suppresses, and has significantly different from the atomistic competition inhibitor; Easily enter maincenter by blood brain barrier, with maincenter and periphery therapeutical effect.
Huperzine B (HuperzineB) is a kind of alkaloid that extracts by among Huperziaceae plant Herba Lycopodii serrati Huperzinaserrata (Thumb.) Trev, has the function that suppresses cholinesterase activity and improve study, memory effect.Its action intensity is not as good as huperzine A; but effect is held time and is length than huperzine A, and untoward reaction than huperzine A still less has certain neuroprotective in addition; share the dose that can reduce huperzine A and take number of times with huperzine A, reduce untoward reaction.
Memantine is a noncompetitive 5HT3 receptor and nmda receptor antagonist, can with 5HT3 receptor and the preferential combination of nmda receptor antagonist.The treatment of antagonism glutamic acid, the deterioration that can slow down Alzheimer.
Memantine, huperzine B and huperzine A use in conjunction have good synergy, effectively reduce the generation of toxicity and untoward reaction, and good DEVELOPMENT PROSPECT is arranged.
Summary of the invention
The present invention is a kind of Pharmaceutical composition take memantine, huperzine B and huperzine A as active component, it is characterized in that, it is the active component that memantine, huperzine B and huperzine A form, and mixes the Pharmaceutical composition that forms with pharmaceutically acceptable adjuvant.
The consumption of described memantine is that per unit dosage is 1.5mg～30mg.Be preferably 3mg～15mg.The consumption of huperzine B is that per unit dosage is 0.02mg～0.8mg.Be preferably 0.05mg～0.2mg.The consumption of huperzine B is that per unit dosage is 0.02mg～0.8mg.Be preferably 0.05mg～0.2mg.
The weight ratio of described memantine, huperzine B and huperzine A is 1:0.001:0.001～1:0.5:0.5.The dosage ratio of memantine, huperzine B and huperzine A is (10mg+0.05mg+0.05mg, 10mg+0.1mg+0.1mg, 5mg+0.05mg+0.05mg, 5mg+0.1mg+0.1mg) in the preferred composite unit compound preparation.
Described a kind of Pharmaceutical composition take memantine, huperzine B and huperzine A as active component is characterized in that, can be made into tablet, capsule, drop pill etc.
Described Pharmaceutical composition take memantine, huperzine B and huperzine A as active component can be used for the treatment of cerebral infarction sequela and all kinds of dementias.
The specific embodiment
Embodiment 1 memantine, huperzine B and Huperzine-A Tablets, Tests for Uniformity
Prescription:
Preparation method:
Memantine, starch, microcrystalline Cellulose are crossed 80 mesh sieves, mix homogeneously, for subsequent use; Huperzine B, huperzine A are added in the pure water, fully stir and make dissolving, for subsequent use; Join in the mixed powder with the aqueous solution that is dissolved with medicine, granulate, drying adds magnesium stearate, film-making agent behind the mix homogeneously, and get final product.
Embodiment 2: memantine, huperzine B and huperzine A capsule agent
Prescription:
Preparation method:
Memantine, microcrystalline Cellulose are crossed respectively 80 mesh sieve mix homogeneously, for subsequent use; Huperzine B, huperzine A are added in 85% ethanol, fully stir and make dissolving, for subsequent use; Join in the mixed powder with the alcoholic solution that is dissolved with medicine, granulate, drying, granulate adds magnesium stearate, packing, and get final product.
Embodiment 3: memantine, huperzine B and huperzine dropping pills agent
Prescription
Preparation method:
Memantine, huperzine B and huperzine A are crossed 80 mesh sieves, for subsequent use; In addition with PEG6000, PEG8000 mixings post-heating extremely about 60 ℃ make melting; Memantine, huperzine B and huperzine A added in the fused solution stir, move in the dropping funnel, be incubated about 60 ℃, the regulating dropping head size take-25 ℃ dimethicones as the cooling phase, is carried out dripping, gets final product.
Embodiment 4:
The present invention also provides following pharmacological evaluation, further specifies Pharmaceutical composition of the present invention to the effect of dementia, the relevant disturbance of consciousness of cerebral infarction sequela and hypomnesis.
The grouping administration:
40 of laboratory animal Wistar rats.Adopt the method for lumbar injection scopolamine hydrobromide solution to prepare dementia animal model.Then the Model of Dementia Mus is divided into 4 groups at random, every group 1O: dull-witted blank model group (A); Huperzine A+huperzine B+memantine group (B), huperzine A group (C), memantine group (D).Begin medication behind the 30min, compound recipe memantine (proportioning of memantine and huperzine A, huperzine B is 50:1:1), huperzine A 0.4mg/kg, memantine 2mg/kg, every day 2 gavages; And by treatment time will be divided into again 30, three periods researchs of 60.9Od.
Experimental technique:
The learning capacity test: 4 groups of rats all need in experiment lumbar injection scopolamine hydrobromide on the same day, and dosage is 2
mg·kg-1。Behind the 30min mice is put in people's diving tower instrument, then energising, normal reaction after animal is shocked by electricity is that the rebound platform is to hide noxious stimulation, most animals may be again or is repeatedly skipped on the copper grid, platform snaps back again after being shocked by electricity, so training 5min records every Mus and reaches before required number of shocks (the being number of attempt) expression of continuous 1O correct response.Number of attempt surpasses 30 times rat with 30 countings.Memory ability test: behind the above-mentioned rat rest 48h up to standard, test its memory ability with same method.Record correct response number of times in every rat electric shock 10 times (namely more aobvious number of times) as the memory ability of rat.
The result: as seen from Table 1, in the test of rat learning and remembering ability, the improvement of the rat learning and remembering ability of memantine+huperzine A+huperzine B group significantly is better than other treatment group P＜0.05.
Table 1 treatment is rear in different time rat learning test number of times, the relative analysis of memory ability test reaction number of times
Claims (6)
1. a pharmaceutical composition is characterized in that, it is take memantine, huperzine B and huperzine A as active component, mixes the Pharmaceutical composition that forms with pharmaceutically acceptable adjuvant.
2. pharmaceutical composition as claimed in claim 1 is characterized in that, the consumption of described memantine is that per unit dosage is 1.5mg～30mg, is preferably 3mg～15mg; The consumption of huperzine B is that per unit dosage is 0.02mg～0.8mg, is preferably 0.05mg～0.2mg; The consumption of huperzine A is that per unit dosage is 0.02mg～0.8mg, preferred 0.05mg～0.2mg.
3. pharmaceutical composition as claimed in claim 1 is characterized in that, the weight ratio of described memantine, huperzine B and huperzine A is 1:0.001:0.001～1:0.5:0.5.The dosage ratio of memantine, huperzine B and huperzine A is (10mg+0.05mg+0.05mg, 10mg+0.1mg+0.1mg, 5mg+0.05mg+0.05mg, 5mg+0.1mg+0.1mg) in the preferred composite unit compound preparation.
4. pharmaceutical composition as claimed in claim 1 is characterized in that, can be made into tablet, capsule, drop pill etc.
5. pharmaceutical composition claimed in claim 1 is for the preparation of the application in the medicine for the treatment of cerebral infarction sequela.
6. pharmaceutical composition claimed in claim 1 is for the preparation of the application in the medicine for the treatment of dementia.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012103856556A CN102872016A (en) | 2012-03-22 | 2012-10-12 | Medicine combination |
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201210077622.5 | 2012-03-22 | ||
| CN201210077622 | 2012-03-22 | ||
| CN2012103856556A CN102872016A (en) | 2012-03-22 | 2012-10-12 | Medicine combination |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN102872016A true CN102872016A (en) | 2013-01-16 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2012103856556A Pending CN102872016A (en) | 2012-03-22 | 2012-10-12 | Medicine combination |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113842388A (en) * | 2020-06-28 | 2021-12-28 | 上海天慈生物谷生物工程有限公司 | Application of huperzine A in treating chronic ischemic cerebrovascular disease |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040044023A1 (en) * | 2002-08-30 | 2004-03-04 | Marc Cantillon | Compositions and methods for treating or preventing memory impairment |
| CN1644208A (en) * | 2004-11-26 | 2005-07-27 | 谢德隆 | China fir extracts with lycopodine A and B composition and their preparing method |
| CN101185648A (en) * | 2007-11-30 | 2008-05-28 | 北京润德康医药技术有限公司 | Pharmaceutical composition with memantine hydrochloride and huperzine A as active components and preparation method and use thereof |
| CN101234111A (en) * | 2008-01-09 | 2008-08-06 | 北京润德康医药技术有限公司 | Pharmaceutical composition containing memantine hydrochloride and huperzine A and preparation thereof |
-
2012
- 2012-10-12 CN CN2012103856556A patent/CN102872016A/en active Pending
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20040044023A1 (en) * | 2002-08-30 | 2004-03-04 | Marc Cantillon | Compositions and methods for treating or preventing memory impairment |
| CN1644208A (en) * | 2004-11-26 | 2005-07-27 | 谢德隆 | China fir extracts with lycopodine A and B composition and their preparing method |
| CN101185648A (en) * | 2007-11-30 | 2008-05-28 | 北京润德康医药技术有限公司 | Pharmaceutical composition with memantine hydrochloride and huperzine A as active components and preparation method and use thereof |
| CN101234111A (en) * | 2008-01-09 | 2008-08-06 | 北京润德康医药技术有限公司 | Pharmaceutical composition containing memantine hydrochloride and huperzine A and preparation thereof |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN113842388A (en) * | 2020-06-28 | 2021-12-28 | 上海天慈生物谷生物工程有限公司 | Application of huperzine A in treating chronic ischemic cerebrovascular disease |
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Application publication date: 20130116 |