CN103301464B - Pharmaceutical composition - Google Patents
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- CN103301464B CN103301464B CN201310254721.0A CN201310254721A CN103301464B CN 103301464 B CN103301464 B CN 103301464B CN 201310254721 A CN201310254721 A CN 201310254721A CN 103301464 B CN103301464 B CN 103301464B
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Abstract
The present invention relates to a kind of compositions for treating epilepsy, belong to pharmaceutical technology field.The present invention provides a kind of compound medicament compositions for treating epilepsy, which is characterized in that second propionyl ureas, imino group glycoside, the barbiturate compatibility of chlocibutamine and sodium channel inhibitor achieve unexpected synergistic effect in terms of epilepsy is treated.The present invention provides a kind of compositions, to improve the compliance of patient, achieve the purpose that control epileptic attack, while reduce the side effect of central nervous system depressant clinical application.A kind of safe and effective clinical application is provided for epileptic.
Description
Technical field：The present invention relates to a kind of compositions for treating epilepsy, belong to pharmaceutical technology field.
Background technology：Epilepsy is the chronic brain diseases caused by Different types of etiopathogenises, with cerebral neuron paradoxical discharge from
And transience central nervous system function is caused to be characterized extremely.There is document announcement, domestic epidemiological survey is shown, domestic insane
The incidence of epilepsy is close to 1 ‰, and illness rate is about 4 ‰~9 ‰.The existing epileptic in China up to more than 5,000,000 controls at present
The best approach of epileptic attack is still based on drug therapy, and medication purpose is to reduce or prevents breaking-out.At present, it there is no
The method of prevention and the healing of effect, therefore the treatment of epilepsy is often lifelong, and since most drugs are there are adverse reaction,
And some side effects or irreversible, long-time service enable patient be difficult to receive, therefore cause treatment interruption and the state of an illness repeatedly.
The object of the present invention is to provide a kind of compositions, improve the compliance of patient, reach control epileptic attack
Purpose, while reduce the generation of side effect.A kind of safe and effective clinical application is provided for epileptic.
Applicant has found through overtesting, second propionyl ureas, imino group glycoside, bar ratio of chlocibutamine and sodium channel inhibitor
Appropriate class compatibility of drugs achieves unexpected synergistic effect in terms of epilepsy is treated.
Technical solution：
A kind of compound medicament composition for treating epilepsy, which is characterized in that containing chlocibutamine and sodium channel inhibitor,
In, sodium channel inhibitor is selected from barbiturates, second propionyl ureas, imino group glycoside, phenyl triazines.
The present composition, which is characterized in that barbiturate is in amytal, phenobarbital, Primidone
One kind.
The present composition, barbiturate are also selected from aprobarbital, Phenallymal, brallobarbital, A Luoba
Than one kind in appropriate.
Second propionyl ureas includes：Dilantin sodium, Methoin, ethotoin etc..
Imino group glycoside includes：Carbamazepine, Oxcarbazepine.
Phenyl triazines include：Lamotrigine, Topiramate.
Currently preferred technical solution is：In the composition of unit dose, sodium channel inhibitor barbiturates, second propionyl
Ureas, imino group glycoside, phenyl triazines dosage be the half of routine clinical low dosage to high dose, chlocibutamine 75
~200mg.
Currently preferred technical solution is：7.5~45mg containing phenobarbital in the composition of unit dose, chlocibutamine
75~200mg.
Currently preferred technical solution is：15~75mg containing amytal in the composition of unit dose, chlorine osmanthus fourth
75~200mg of amine.
Currently preferred technical solution is：150~750mg containing Primidone in the composition of unit dose, chlocibutamine
90~150mg.
Currently preferred technical solution is：200~350mg containing Primidone in the composition of unit dose, chlocibutamine
90~130mg.
Currently preferred technical solution is：400mg containing Primidone in the composition of unit dose, chlocibutamine 100mg.
Currently preferred technical solution is：70~300mg containing Methoin in the composition of unit dose, chlocibutamine 75
~200mg.
Currently preferred technical solution is：80~150mg containing Methoin in the composition of unit dose, chlocibutamine 75
~150mg.
Currently preferred technical solution is：200~600mg containing carbamazepine in the composition of unit dose, chlorine osmanthus fourth
75~200mg of amine.
Currently preferred technical solution is：300~400mg containing carbamazepine in the composition of unit dose, chlorine osmanthus fourth
75~150mg of amine.
Currently preferred technical solution is：150~1200mg containing Oxcarbazepine in the composition of unit dose, chlorine osmanthus fourth
75~200mg of amine.
Currently preferred technical solution is：300~600mg containing Oxcarbazepine in the composition of unit dose, chlorine osmanthus fourth
100~150mg of amine.
Currently preferred technical solution is：50-200mg containing Lamotrigine in the composition of unit dose, chlocibutamine
75~200mg.
Currently preferred technical solution is：100mg containing Lamotrigine in the composition of unit dose, chlocibutamine
100mg。
Currently preferred technical solution is：50-200mg containing Topiramate in the composition of unit dose, chlocibutamine 75
~200mg.
Currently preferred technical solution is：90-150mg containing Topiramate in the composition of unit dose, chlocibutamine 100
~150mg.
The conventional amount used of the present composition is to take orally 1, twice a day.
It is prepared by the pharmaceutical preparation preparation method of the present composition routinely.
The present composition can also be prepared as sustained release preparation.
The present composition can be prepared as controlled release preparation.Unit dose is selected according to internal drug release situation.
The beneficial effects of the invention are as follows a kind of composition is provided, pass through the second third in chlocibutamine and sodium channel inhibitor
Ureide derivative, imino group glycoside, barbiturates, benzodiazepine reasonable compatibility, under the premise of therapeutic effect is ensured, energy
The side effect of sodium channel inhibitor clinical application is reduced, improves clinical therapeutic efficacy.
Embodiment 1, chlocibutamine 200g, phenobarbital 7.5g prepare 1000 according to a conventional method.
Embodiment 2, chlocibutamine 75g, phenobarbital 45g prepare 1000 according to a conventional method.
Embodiment 3, chlocibutamine 100g, phenobarbital 30g prepare 1000 according to a conventional method.
Embodiment 4, chlocibutamine 100g, amytal 45g prepare 1000 according to a conventional method.
Embodiment 5, chlocibutamine 200g, Methoin 70g prepare 1000 according to a conventional method.
Embodiment 6, chlocibutamine 75g, Methoin 300g prepare 1000 according to a conventional method.
Embodiment 7, chlocibutamine 100g, Methoin 100g prepare 1000 according to a conventional method.
Embodiment 8, chlocibutamine 100g, carbamazepine 350g prepare 1000 according to a conventional method.
Embodiment 9, chlocibutamine 75g, carbamazepine 600g prepare 1000 according to a conventional method.
Embodiment 10, chlocibutamine 200g, carbamazepine 200g prepare 1000 according to a conventional method.
Embodiment 11, Lamotrigine 50g, chlocibutamine 200g prepare 1000 according to a conventional method.
Embodiment 12, Lamotrigine 100g, chlocibutamine 100g prepare 1000 according to a conventional method.
Embodiment 13, Lamotrigine 200g, chlocibutamine 75g prepare 1000 according to a conventional method.
Embodiment 14, Topiramate 120g, chlocibutamine 100g prepare 1000 according to a conventional method.
Embodiment 15, Topiramate 50g, chlocibutamine 200g prepare 1000 according to a conventional method.
Embodiment 16, Topiramate 200g, chlocibutamine 75g prepare 1000 according to a conventional method.
Embodiment 17, Topiramate 50g, chlocibutamine 75g prepare 1000 according to a conventional method.
Embodiment 18, Lamotrigine 50g, chlocibutamine 75g prepare 1000 according to a conventional method.
Embodiment 19, chlocibutamine 75g, carbamazepine 200g prepare 1000 according to a conventional method.
Embodiment 20, chlocibutamine 75g, Methoin 70g prepare 1000 according to a conventional method.
Embodiment 21, chlocibutamine 75g, Primidone 150g prepare 1000 according to a conventional method.
Embodiment 22, chlocibutamine 75g, amytal 20g prepare 1000 according to a conventional method.
Test example 1：
Inclusion criteria：18 years old age or more meets epileptic attack class definition (1985)；There is no treatment history, epileptic attack
Frequency monthly 2 times or more；There are epileptiform discharges through EEG(electrocardiogram) examination confirmation；It is ready to participate in experiment and has preferable compliance.
Exclusion criteria：Non-epileptic seizures；It is associated with the serious diseases such as angiocarpy, liver, kidney and hemopoietic system；Have drug and
Alcohol abuse history；Prepare gestation or women breast-feeding their children；It affects the treatment with activity mental patient etc. or safety judgement person.
230, man 128, female 102.23 groups are randomly divided into, every group of 10 people, respectively chlocibutamine group, phenobarbital
Group, Primidone group, Methoin group, carbamazepine group, Lamotrigine group, Topiramate group, 1 group to 16 groups of embodiment.Continuous use 2
A month, during medication, the previous moon as adjustment period, took judgement of the breaking-out situation of the latter moon as therapeutic effect.
Observation index：The total inspection phase is 8 weeks.Observation is primary every 2 weeks and checks rehabilitation diary, every four weeks progress blood routine,
EEG(electrocardiogram) examination after treatment before routine urinalysis, Liver and kidney function and ECG examination and treatment, and with regard to epileptic attack number, drug agent
Amount, adverse reaction extremely degree record and curative effect evaluation are primary.
Chlocibutamine group takes chlocibutamine piece, and 200mg/ pieces, 2 times a day, 1 tablet once.
Phenobarbital group takes phenobarbital, and 30mg/ pieces, 1 tablet once, three times a day.
Primidone group takes Primidone, and 50mg starts, and is taken before sleeping, and is changed to 2 times a day, be changed to after a week daily after 3 days
3 times, start within 10th to be changed to 250mg (1), 3 times a day, total amount is no more than daily 1.5g (6)；Maintenance dose is generally
250mg (1), 3 times a day.
Methoin group takes Methoin, and 100mg/ pieces, 3 times a day, each 100mg/ pieces, 2 tablets once.
Carbamazepine group, takes carbamazepine, and 100mg/ pieces start one at a time, 3 times a day；Increase daily after second day
1, until 3 tablets once, 3 times a day.
Lamotrigine group, takes Lamotrigine, predose 50mg, one time a day, totally 2 weeks；Subsequent two weeks daily
100mg is taken in two divided doses.Hereafter, increased dose every 1-2 weeks, maximum incrementss are 100mg, until maintenance dose is
300mg/ days, divide 2 times and take.
Topiramate group, takes Topiramate, and since dosage adjustment should take 1 week, then, increase weekly taking orally 50mg every night
Add dosage 100mg, divide 2 times and take.Daily dose is 400mg/ days, divides 2 times and takes.
The tablet 2 times of 1 group of -16 group of embodiment daily corresponding embodiment, 1 tablet once.
Judgment criteria：Breaking-out control, without breaking-out in the observation period；Effective, attack times reduce 75%-99% in the observation period；
Effectively, observation period attack times are reduced between 74%-50%；Effect is poor, and observation period attack times reduce below 26%-49%；
In vain, observation period attack times reduce less than 25%；Deteriorate, attack times increase by more than 25%.
Data prove in table：The present composition treats the folk prescription medicine with obvious effects higher than control group of epilepsy, illustrates chlorine
The reasonable compatibility of osmanthus butylamine and central nervous system depressant is acted synergistically.
Test example 2, Lee, female, 38 years old, clinical definite was epileptic, and medical history 6 years once took phenobarbital, O'Casey
Equality drug, it is impossible to which effectively control breaking-out, patient and family are tormented deeply by the disease.Before this on-test, it is appropriate that patient takes first
English 100mg/ pieces, 2 tablets once, and three times a day, the moon breaks out 8 times or so.Take chlocibutamine 2 times a day, each 200mg/ pieces 2
3 months, the moon attack times do not improve.Through soliciting patient and family members' opinion, the phychology tried is had in arms, take implementation of the present invention
The composition of example 20, day take medicine 2 times, 1 time 1.Second month plays record number of incidences and breaks out 4 times for the moon.Patient is basic simultaneously
On eliminate because taking the drowsiness of other drugs appearance, headache, dizzy phenomenon, readme can feel good.
Test example 3, certain man, 48 years old, clinical definite was epileptic, and medical history 7 years once took a variety of antiepileptics, no
Breaking-out can be effectively controlled, patient and family are tormented deeply by the disease.Before this on-test, patient takes amytal 50mg/
Piece, 1 tablet once, and three times a day, the moon breaks out 9 times or so.Take chlocibutamine 2 times a day, each 200mg/ pieces 23 months, the moon
Attack times do not improve.Through soliciting patient and family members' opinion, the composition of the embodiment of the present invention 22 is taken, is taken medicine 2 times day, 1
Secondary 1.Second month plays record number of incidences and breaks out 4 times for the moon.Patient substantially eliminates to go out because taking other drugs simultaneously
Existing drowsiness, headache, dizzy phenomenon, readme can feel good.
Test example 4, it is high certain, man, 53 years old, clinical definite was epileptic, and medical history 12 years once took the medicines such as a variety of anti-epileptics
Object, it is impossible to effectively control breaking-out.Before this experiment, Primidone is taken, is taken orally：Each 0.3g, three times a day, the moon break out 8 times or so.Clothes
With chlocibutamine 2 times a day, each 200mg/ pieces 23 months, the moon attack times do not improve.Fix one's mind on through soliciting patient and family
See, take the composition of the embodiment of the present invention 21, day takes medicine 2 times, 1 time 1.Second month plays record number of incidences and breaks out for the moon
5 times.Patient is substantially eliminated because taking the drowsiness of other drugs appearance, headache, dizzy phenomenon simultaneously, and readme can feel good
It is good.
Test example 5, Mr. Wang, female, 48 years old, clinical definite was epileptic, and medical history 8 years once took the medicines such as a variety of anti-epileptics
Object, it is impossible to effectively control breaking-out.Before this experiment, carbamazepine is taken, is taken orally：Each 0.3g, three times a day, 2 tablets once, moon breaking-out
11 times or so.Take chlocibutamine 2 times a day, each 200mg/ pieces 23 months, the moon attack times do not improve.Suffer from through soliciting
Person and family members' opinion, take the composition of the embodiment of the present invention 19, and day takes medicine 2 times, 1 time 1.Second month plays record morbidity time
Number breaks out 5 times for the moon.Patient is substantially eliminated because taking the drowsiness of other drugs appearance, headache, dizzy phenomenon, readme simultaneously
It can feel good.
Test example 6, Zhang, female, 49 years old, clinical definite was epileptic, and medical history 8 years once took the medicines such as a variety of anti-epileptics
Object, it is impossible to effectively control breaking-out.Before this experiment, Lamotrigine is taken, is taken orally：Each 0.1g, three times a day, 1 tablet once, moon breaking-out
8 times or so.Take chlocibutamine 2 times a day, each 200mg/ pieces 23 months, the moon attack times do not improve.Suffer from through soliciting
Person and family members' opinion, take the composition of the embodiment of the present invention 18, and day takes medicine 2 times, 1 time 1, be carried out at the same time spirit and dredge.The
Number of incidences is recorded from two months to break out 5 times for the moon.Simultaneously patient substantially eliminate because take other drugs occur it is drowsiness,
Headache, dizzy phenomenon, readme can feel good.
Test example 7, Zhao, man, 38 years old, clinical definite was epileptic, and medical history 4 years once took the medicines such as a variety of anti-epileptics
Object, it is impossible to effectively control breaking-out.Before this experiment, Topiramate is taken, is taken orally：Each 0.1g, twice a day, 2 tablets once, moon breaking-out 11
It is secondary or so.Take chlocibutamine 2 times a day, each 200mg/ pieces 23 months, the moon attack times do not improve.Through soliciting patient
With family members' opinion, take the composition of the embodiment of the present invention 17, day takes medicine 2 times, 1 time 1.Second month plays record number of incidences
It breaks out 5 times for the moon.Patient is substantially eliminated because taking the drowsiness of other drugs appearance, headache, dizzy phenomenon, readme energy simultaneously
Feel good.
More than test example proves that the present composition has prominent synergy to treatment epileptic condition.Illustrate chlorine osmanthus fourth
The combination of amine and sodium channel inhibitor has unexpected Clinical practice effect.
Claims (6)
1. a kind of compound medicament composition for treating epilepsy, which is characterized in that in the composition of unit dose, containing Methoin 70~
300mg, 75~200mg of chlocibutamine.
2. a kind of compound medicament composition for treating epilepsy, which is characterized in that in the composition of unit dose, containing carbamazepine
200~600mg, 75~200mg of chlocibutamine.
3. a kind of compound medicament composition for treating epilepsy, which is characterized in that in the composition of unit dose, containing carbamazepine
150~400mg, 75~150mg of chlocibutamine.
4. a kind of compound medicament composition for treating epilepsy, which is characterized in that in the composition of unit dose, containing Lamotrigine
50-200mg, 75~200mg of chlocibutamine.
5. a kind of compound medicament composition for treating epilepsy, which is characterized in that in the composition of unit dose, containing Lamotrigine
100mg, chlocibutamine 100mg.
6. a kind of compound medicament composition for treating epilepsy, which is characterized in that in the composition of unit dose, 50- containing Topiramate
200mg, 75~200mg of chlocibutamine.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201310254721.0A CN103301464B (en) | 2013-06-15 | 2013-06-15 | Pharmaceutical composition |
Applications Claiming Priority (1)
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|---|---|---|---|
| CN201310254721.0A CN103301464B (en) | 2013-06-15 | 2013-06-15 | Pharmaceutical composition |
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| CN103301464B true CN103301464B (en) | 2018-06-12 |
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Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101991561A (en) * | 2010-11-11 | 2011-03-30 | 迪沙药业集团有限公司 | 3,4-dichlorophenyl-propenoyl-sec-butylamine composition |
-
2013
- 2013-06-15 CN CN201310254721.0A patent/CN103301464B/en not_active Expired - Fee Related
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101991561A (en) * | 2010-11-11 | 2011-03-30 | 迪沙药业集团有限公司 | 3,4-dichlorophenyl-propenoyl-sec-butylamine composition |
Non-Patent Citations (2)
| Title |
|---|
| 抗癫痫药物相关分子作用靶点的研究进展;何保明 等;《国际神经病学神经外科学杂志》;20081231;第35卷(第2期);第130页左栏3.1钠通道 * |
| 抗癫痫药物研究现状与新进展;应义 等;《中国药业》;20121020;第21卷(第20期);第110页左栏第1段，第110页右栏第1段-第111页右栏第2段 * |
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| CN103301464A (en) | 2013-09-18 |
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