CN102861022A - Hydrochloric acid vilazodone compound preparation - Google Patents
Hydrochloric acid vilazodone compound preparation Download PDFInfo
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- CN102861022A CN102861022A CN2012103912876A CN201210391287A CN102861022A CN 102861022 A CN102861022 A CN 102861022A CN 2012103912876 A CN2012103912876 A CN 2012103912876A CN 201210391287 A CN201210391287 A CN 201210391287A CN 102861022 A CN102861022 A CN 102861022A
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- hydrochloric acid
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- wella oxazolone
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Abstract
The invention discloses a hydrochloric acid vilazodone compound preparation which uses novel antidepressant hydrochloric acid vilazodone and vitamin B as the active ingredients, wherein the mass ratio of the hydrochloric acid vilazodone to the vitamin B is 1: (0.5-1), and the vitamin B is preferably B1, B2, B6 and B12. The hydrochloric acid vilazodone compound preparation is used for treating major depressive disorders, reduces side effects of sickness, nausea and insomnia caused by the hydrochloric acid vilazodone, has strong antidepressant activity and has good application prospect.
Description
Technical field
The invention belongs to drug world, be specifically related to a kind of hydrochloric acid Wella oxazolone compound preparation, the compound preparation of the Cure of depression that is formed by hydrochloric acid Wella oxazolone and vitamin B group.
Background technology
Depression (depression) is a kind of common mental sickness, clinical main manifestations is depressed, interest goes down but not forfeiture, pessimism, retardation of thinking, lack initiative, self-accusation is from crime, and the diet sleep is poor, worries oneself to suffer from various diseases, feel that the whole body many places are uncomfortable, suicidal thought and behavior can appear in severe patient.According to World Health Organization's statistics, global rate of depression is about 3.1%, and about developed country was near 6%, global patients with depression reached 1.2 hundred million, had become the fourth-largest disease that threatens human health.Along with rhythm of life day by day accelerate, compete increasingly sharpen, the sickness rate of depression is whole to be improved year by year.In 20 years old adult population, patients with depression increases with annual 11.3% speed, and World Health Organization (WHO) expects the year two thousand twenty, and depression will jump to world's second largest disease, be only second to ischemic heart desease.Almost among 7 adults 1 patients with depression is just arranged, so it is called as the flu in the psychiatry.The sickness rate of China's depression reaches 3%-5%, patient Yue Da 3,600 ten thousand people at present.
The new drug hydrochloric acid Wella oxazolone (Vilazodone HCl) of at present novel treatment major depressive disorder, being potent and the reuptake inhibitor of selectivity five hydroxytryptamine and 5-HT1A acceptor portion agonist of a kind of dual function, also is first indolyl amine novel antidepressant.Meet Americanism medical diagnosis on disease and statistic handbook [Diagnostic and Statistical Manual of Mental Disorders at heavy depression MDD, DSM-IV-TR] two 8 weeks of standard patient, multicenter, at random, double blinding, placebo-comparative study (18-70 year) in growing up determines that VIIBRYD is as the curative effect to major depressive disorder, in these researchs, the adjusting agent amount is to food dosage 40 mg VIIBRYD (n=436) or placebo (n=433) every day 1 time during 2 weeks.Be better than placebo when improving the depressive symptom with the mean change measurement VIIBRYD of the depressed quantitatively score of Montgomery-Asberg (MADRS) overall score from 8 weeks of baseline to the from baseline.Based on age (having small number of patients to surpass 65 years old), sex, and each subgroup crowd of race checks the evidence that does not disclose any clear reaction gender gap.
The routine of hydrochloric acid Wella oxazolone uses maintenance dose to be 40mg, and this dosage is incremented to maintenance dose 40mg from low dosage 10mg gradually to median dose 20mg, and as seen this maintenance dose is to the side effect of human body or sizable.The psychiatric system symptoms such as the gastrointestinal symptom such as the topmost side effect of hydrochloric acid Wella oxazolone is diarrhoea, feel sick, vomiting and insomnia.Therefore seek a kind of safely and effectively medicine and hydrochloric acid Wella oxazolone drug combination, can reduce in same curative effect the therapeutic dose of hydrochloric acid Wella oxazolone, can reduce again side effect that hydrochloric acid Wella oxazolone brings the particularly necessity that seems.
Vitamin B group is the water miscible vitamin of a class, comprise B1, B2, B3, B5, B6B1 B7, B9, B12, at present known vitamin B group can synergism, regulate metabolism, keep the health of skin and muscle, promote immune system and neural function, Promote cell's growth and division comprise promoting erythrocytic generation the generation of prevention anemia.The vitamin B group nutritious nerve that also is in the news is alleviated the effect of stress, and a large amount of report explanation vitamin B group have alleviating pain and stable neural effect.If the women takes can also releive premenstrual abdominal pain and menopause syndrome.Vitamin B group can obtain by daily diet, some avitaminous patients or need especially the crowd of vitimin supplement such as the anemia of pregnant woman just the special additional a certain amount of vitamin of needs with mitigate the disease.
Summary of the invention
The purpose of this invention is to provide the compound that is used for the treatment of depression, take hydrochloric acid Wella oxazolone and vitamin B group as active component, the benefit that vitamin B group associating hydrochloric acid Wella oxazolone uses together is, can reduce the using dosage of hydrochloric acid Wella oxazolone, the curative effect that when lower dose maintenance treatment produces high dose, produces, when low dosage, the corresponding side effect adverse reaction rate of hydrochloric acid Wella oxazolone and degree also decrease; Vitamin B group and hydrochloric acid Wella oxazolone drug combination can also reduce gastrointestinal tract and the neural side effect that produces with dosage hydrochloric acid Wella oxazolone.By following technical scheme can be complete item the present invention:
Hydrochloric acid Wella oxazolone compound preparation it is characterized in that the compound preparation that forms take hydrochloric acid Wella oxazolone and vitamin B group as active component.The mass ratio of hydrochloric acid Wella oxazolone and B group vitamin is 1:0.5～1; The dosage of hydrochloric acid Wella oxazolone is half of conventional maintenance dose in the present invention.
Described vitamin B group is one or more among vitamin B1, B2, B6, the B12.
The compound of Cure of depression among the present invention, its concrete dosage form is oral tablet or granule.This dosage form taking convenience, cost are also lower, safe.
Smooth for the preparation process that guarantees compound preparation, also in prescription, add filler, disintegrating agent, surfactant, lubricant and fluidizer composition.
Filler can be selected from one or more the combination in the following material: sugar alcohols, amylum pregelatinisatum, calcium phosphate, calcium hydrogen phosphate, calcium sulfate, microcrystalline Cellulose etc. are the acceptable material pharmaceutically.
Disintegrating agent is selected from starch, cross-linking sodium carboxymethyl cellulose, crospolyvinylpyrrolidone, low-substituted hydroxypropyl methylcellulose.
Surfactant is selected from polyoxyethylene sorbitan monoleate, poloxamer.
Lubricant and fluidizer are selected from stearic acid, magnesium stearate, calcium stearate, Pulvis Talci, sodium lauryl sulphate, colloidal silica.
Fluidizer is colloidal silica.
The consumption of above excipient can be the conventional amount used of ordinary preparation.
The method of the hydrochloric acid Wella oxazolone of preparation Cure of depression and B group vitamin compound preparation is conventional oral formulations preparation method, and those skilled in the art can realize easily.
Below come by specific embodiment the present invention is done more detailed description, but can't consist of any restriction to the present invention.Method is conventional method if no special instructions described in the following embodiment.
The specific embodiment
Hydrochloric acid Wella oxazolone and vitamin B group drug combination produce obvious synergistic experiment.
Male ICR mouse, secondary, 20-25g is available from Department Of Medicine, Peking University's Experimental Animal Center.Raising condition: 10 cages, 22 ± 1 ℃ of room temperatures, humidity 50% ± 10%, natural lighting, the drinking-water of freely ingesting.Adapting to 5 days in feeding environment after, all animals begin experiment, front fasting 12-16 hour of experiment, and drinking-water is freely.90 above-mentioned male mices are divided into 9 groups at random, 10 every group, be specially one group of matched group, give isopyknic normal saline; The high, medium and low dosage group of hydrochloric acid Wella oxazolone is respectively 40mg group, 20mg group, 10mg group; The vitamin B component is that high, medium and low dosage group is 5mg, 10mg, 20mg group; The drug combination group of hydrochloric acid Wella oxazolone and vitamin B group, one group is hydrochloric acid Wella oxazolone 20mg, vitamin B is 10mg; One group is hydrochloric acid Wella oxazolone 20mg, and vitamin B is 20mg.Come to 9 groups.Hydrochloric acid Wella oxazolone and vitamin B group drug combination group (also being combination group) are first gastric infusion vitamin B, gastric infusion hydrochloric acid Wella oxazolone again after 30 minutes, hydrochloric acid Wella oxazolone will be suspended in administration in the normal saline, the administration in normal saline of vitamin B stirring and dissolving in each group of trade company.
Adopt the antidepressant effect of forced swimming experimentation medicine: the behavioral despair experiment is also named in the forced swimming experiment, is a reliable depressed animal model, is widely used in the mechanism of action of screening antidepressants and research antidepressant drug.A large amount of studies show that this model is responsive to most antidepressants, comprises the medicines such as optionally 5-HT reuptake inhibitor, non-selective reuptake inhibitor and oxidase inhibitor.
The experiment of depression effect is by the forced swimming experiment confirm, concrete operations are as follows: tested front 24 hours, mice is placed in the glass circle cylinder of depth of water 10cm, 24 ℃ ± 1 ℃ of water temperature, do and forced swimming instruction 15 minutes, then force swimming 6 minutes under the same condition with again mice being placed after after each group mouse stomach administration 30 minutes, observe and record the dead time of mice in last 4 minutes.When mice stops to struggle, float over to keep motionless in the water, or only to do the time that some necessary mild action keep heads to float on the surface be non-swimming time that the antidepressant effect of shorter explanation of dead time is better, it is right to compare
Suppression ratio according to group is higher.Experimental result is as shown in the table:
Non-swimming time result (s)
Can be found out by above experimental result, when the drug combination of hydrochloric acid Wella oxazolone and vitamin B, inhibition will be significantly higher than individually dosed (P＜0.05) of any active component, and also is higher than the addition of two kinds of individually dosed effects of active component; Above result also shows, at hydrochloric acid Wella oxazolone during at low dosage (dosage is half of conventional therapy dosage), the simultaneously administration of associating vitamin B, antidepressant effect can be suitable with the individually dosed high dose group of hydrochloric acid Wella oxazolone, the administration of prompting vitamin B associating hydrochloric acid Wella oxazolone can guarantee greatly to reduce the dosage of hydrochloric acid Wella oxazolone under identical therapeutic effect prerequisite, dosage reduces simultaneously, the toxic and side effects and the untoward reaction that are proportionate with dosage have also just reduced accordingly, have improved the safety of medication.
Claims (3)
1. hydrochloric acid Wella oxazolone compound preparation, it is characterized in that comprising active component is hydrochloric acid Wella oxazolone and vitamin B group.
2. hydrochloric acid Wella oxazolone compound preparation as claimed in claim 1 is characterized in that described vitamin B group is one or more among vitamin B1, B2, B6, the B12.
3. hydrochloric acid Wella oxazolone compound preparation as claimed in claim 1 is characterized in that the mass ratio of described hydrochloric acid Wella oxazolone and B group vitamin is 1:0.5～1.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2012103912876A CN102861022A (en) | 2012-10-16 | 2012-10-16 | Hydrochloric acid vilazodone compound preparation |
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| Application Number | Priority Date | Filing Date | Title |
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| CN2012103912876A CN102861022A (en) | 2012-10-16 | 2012-10-16 | Hydrochloric acid vilazodone compound preparation |
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| CN102861022A true CN102861022A (en) | 2013-01-09 |
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| CN2012103912876A Pending CN102861022A (en) | 2012-10-16 | 2012-10-16 | Hydrochloric acid vilazodone compound preparation |
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Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004022043A1 (en) * | 2002-09-05 | 2004-03-18 | Pantarhei Bioscience B.V. | Use of a sri and vitamin b6 for the treatment of neurological and mental disorders |
| WO2004110417A2 (en) * | 2003-06-12 | 2004-12-23 | The Wwk Trust | Compositions for the enhanced treatment of depression |
| CN1633292A (en) * | 2002-01-25 | 2005-06-29 | 法玛西雅厄普约翰美国公司 | Cotherapy with an oxazolidinone and a vitamin B |
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2012
- 2012-10-16 CN CN2012103912876A patent/CN102861022A/en active Pending
Patent Citations (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN1633292A (en) * | 2002-01-25 | 2005-06-29 | 法玛西雅厄普约翰美国公司 | Cotherapy with an oxazolidinone and a vitamin B |
| WO2004022043A1 (en) * | 2002-09-05 | 2004-03-18 | Pantarhei Bioscience B.V. | Use of a sri and vitamin b6 for the treatment of neurological and mental disorders |
| WO2004110417A2 (en) * | 2003-06-12 | 2004-12-23 | The Wwk Trust | Compositions for the enhanced treatment of depression |
Non-Patent Citations (1)
| Title |
|---|
| 李赛: "维拉佐酮盐酸盐", 《中国药物化学杂志》 * |
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Application publication date: 20130109 |