CN101991577A - Novel mental medicinal composition - Google Patents
Novel mental medicinal composition Download PDFInfo
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- CN101991577A CN101991577A CN2009100905385A CN200910090538A CN101991577A CN 101991577 A CN101991577 A CN 101991577A CN 2009100905385 A CN2009100905385 A CN 2009100905385A CN 200910090538 A CN200910090538 A CN 200910090538A CN 101991577 A CN101991577 A CN 101991577A
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- agomelatine
- olanzapine
- compositions
- tablet
- medicinal composition
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Abstract
The invention relates to a novel mental medicinal composition, which is prepared from active ingredients of agomelatine and olanzapine and pharmaceutically acceptable auxiliary materials, and can be prepared into oral preparations, such as tablets, capsules, soft capsules, chewable tablets, orally disintegrating tablets, buccal tablets and pills, through a certain preparation process. The novel mental medicinal composition is used for treating mental diseases such as depression, Insomnia and anxiety, and schizophrenia.
Description
Technical field
The present invention is a kind of novel spiritual class pharmaceutical composition, belongs to medical technical field.
Background technology
Agomelatine is Melatonin receptor (MT1 and MT2) agonist, also is 5-hydroxy tryptamine 2C (5-HT2C) receptor blocking agent.Can be directly and the 5HT2C receptors bind of nerve synapse caudacoria, thereby bring into play its antidepressant curative effect, and do not increase the 5HT concentration between synapse, thereby do not have the common adverse effect of five hydroxytryptamine reuptake inhibitor class medicine and five hydroxytryptamine NRI class medicine.Another unique effect target spot of this medicine is at the MT receptor, by agonism to MT1 and MT2 receptor, can adjust the patient 24 circadian rhythm 24s, improve patient's sleep quality, thereby promote the improvement of patients with depression overall clinical situation.It is reported that 80% patients with depression is all with the sleep barrier.Animal experiment and clinical research show that this medicine has antidepressant, anxiety, adjustment sleep rhythm and regulates the biological clock effect, and untoward reaction is few.
Olanzapine is mainly used in the treatment of the schizophrenia positive symptom and negative symptoms, in addition, for the depression that is caused by schizophrenia, affective disorder such as manic mitigation is arranged.The effect of olanzapine and traditional anti-schizophrenia medicine have significant difference on the mechanism of action.The latter such as perphenazine mainly act on dopamine in the brain (DA) receptor, are used for reaching the effect of alleviating the schizophrenia positive symptom by suppressing hyperfunction central dopamine nervous system.And non-classical anti-schizophrenia medicine such as olanzapine not only suppresses dopamine receptor, simultaneously also can with 5-hydroxy tryptamine (5-HT) receptors bind, even the effect of itself and 5-HT receptor considerably beyond with the effect degree of DA receptor, so olanzapine has good therapeutical effect to negative symptoms.
Summary of the invention
The present invention relates to a kind of novel spiritual class pharmaceutical composition, it is to be active component with agomelatine and olanzapine, is combined to form with acceptable accessories.Wherein " agomelatine " also comprises its pharmaceutical salts, optical isomer and hydrate." olanzapine " also comprises its pharmaceutical salts, optical isomer and hydrate.
The average unit formulation input amount of described olanzapine is 1.0mg～100mg.Be preferably 5-20mg.The unit formulation content of agomelatine is 5mg～125mg.Be preferably 25mg～50mg.Can be by must preparation technology making oral formulations.Comprise tablet, capsule, soft capsule, chewable tablet, oral cavity disintegration tablet, buccal tablet, drop pill etc.Be used for the treatment of mental sickness such as depression, insomnia anxiety, schizophrenia.Compound recipe effect of the present invention is remarkable, and is more obvious than the effect of folk prescription.
The specific embodiment
Embodiment 1 compound recipe agomelatine sheet
Prescription;
Preparation method:
Crude drug is crossed 80 mesh sieves, standby; Take by weighing microcrystalline Cellulose, polyvinylpolypyrrolidone, colloidal silica, pregelatinized Starch, the magnesium stearate of recipe quantity, add principal agent, abundant mix homogeneously, direct powder compression, promptly.
Embodiment 2: compound recipe agomelatine capsule
Prescription:
Preparation method:
Principal agent is crossed 80 mesh sieves, standby.Get starch put 60 the degree baking ovens in the baking 6 hours, with the principal agent mix homogeneously, No. 2 capsules of fill, promptly.
Embodiment 3: compound recipe agomelatine chewable tablet
Prescription:
Preparation method:
Supplementary material is crossed 80 mesh sieves respectively, standby; Get principal agent, sorbitol, mannitol mix homogeneously, add the 5%PVP-k30 alcoholic solution, the system soft material, 16 mesh sieves are granulated, drying, 20 mesh sieve granulate add sucralose, essence mix homogeneously, tabletting, promptly.
Embodiment 4 compound recipe agomelatine oral cavity disintegration tablets
Prescription:
Preparation method:
Crude drug is crossed 80 mesh sieves, standby; Take by weighing the supplementary material of recipe quantity, abundant mix homogeneously, direct powder compression, promptly.Embodiment 5 compound recipe agomelatine buccal tablets
Prescription:
Preparation method:
Crude drug is crossed 80 mesh sieves, standby; Take by weighing the sorbitol and the mannitol of recipe quantity, with the principal agent mix homogeneously, the ethanol with 50% is binding agent, and the system soft material is crossed 16 eye mesh screens and granulated, 70 ℃ of oven dry, and 20 order granulate, tabletting, promptly.Embodiment 6 compound recipe agomelatine soft capsules
Prescription:
Preparation method:
Crude drug is crossed 80 mesh sieves, standby; Take by weighing Semen Maydis oil, add principal agent, fully stir into suspendible liquid, standby.Water intaking and glycerol are heated to 80 degree, add gelatin, and stirring is dissolved, and insulation.Produce with encapsulating machine, every loading amount is 0.3g, is coolant with the liquid paraffin, dries up, and washes ball, dries up, and selects ball, packing.
Embodiment 7 compound recipe agomelatine drop pill
Prescription:
Preparation method:
Crude drug is crossed 100 mesh sieves, standby; Take by weighing PEG6000, be heated to 70 degree and make fusion, add principal agent, fully mix homogeneously, and insulation, drop pill is a coolant with the liquid paraffin, is condensed into ball, promptly.
Embodiment 8 therapeutic evaluatioies experiment
1, estimates the effect of the high activeness of glutamic acid hypofunction schizophrenia disease mouse model due to the Zhuo Xiping maleate (MK-801) over the ground of compound recipe olanzapine agomelatine.
Method: get 40 model mices and be divided into 4 groups: normal saline blank group; Olanzapine group (5mg/ time); Agomelatine group (25mg/ time), olanzapine+agomelatine compound recipe group (30mg/ time), each organizes equal gastric infusion, and irritating the stomach volume is 10mL/kg.After 6 hours, single mice is put into the inspection box of autonomic activities video analytic system, the movable 30min of video recording mice writes down the mice event trace automatically, calculates the activity distance in the certain hour section.The activity distance of putting into the preceding 10min (being strange environment) of inspection box with mice is represented the exploratory behavior of mice, and on behalf of mice, the activity distance of back 20min get autonomic activities.
The result: each organizes the comparison of mice exploratory behavior and autonomic activities.By table 1 as seen, inquiry activity of compound recipe olanzapine agomelatine group mice and autonomic activities all obviously are less than matched group (P＜0.01).The autonomic activities of comparing with other administration groups also obviously reduces (P＜0.05), the high activeness that prompting compound recipe olanzapine agomelatine can obvious suppression schizophrenia disease mouse model.
The comparison that the total distance of table 1 pair mice exploratory behavior and autonomic activities changes (cm, x ± s)
2, the antidepressant effect of the desperate mice of behavior is studied
Method: get 40 mices and be divided into 4 groups: normal saline blank group; Olanzapine group (5mg/ time); Agomelatine group (25mg/ time), olanzapine+agomelatine compound recipe group (30mg/ time), each organizes equal gastric infusion, and irritating the stomach volume is 10mL/kg.Every day 1 time, 7d continuously.The experimental session animal is freely got food and drinking-water.Behind the last administration 1h, mouse tail is fixed with clip apart from the about 1cm of end place, it is hung upside down on the cross bar about the 15cm of distance ground, animal is for overcoming undesired position struggle activity, but after asking in the time of movable one section, it is motionless discontinuity to occur, shows disappointed state, and accumulative total is respectively organized the dead time in the 8min.
The result: in the mouse tail suspension depression model of classics, give relative medicine 7d continuously after, compound recipe olanzapine agomelatine can significantly shorten the mouse tail suspension dead time (P＜0.01), other positive control drug also shows same purpose (P＜0.05).See Table 2.Prompting compound recipe olanzapine agomelatine has significant antidepressant effect on this model,
The influence of table 2 pair mouse tail suspension experiment dead time (x ± s)
3, to the research of mice angst resistance effect
Method: mice cat ladder test: be that animal is excitatoty a kind of with reference to indication incubation period in the test of mice cat ladder, it is anxiety reaction indication that mouse hind leg is stood, when making the reaction of standing property of hind leg, medicine is reduced to the angst resistance effect positive, cat ladder number reaction animal behavior excitement (increase) and inhibition (minimizing).40 Kunming mouse groupings, dosage and medications are tested behind the administration 15min with above-mentioned embodiment.Test is carried out under the constant quiet environment of light, and the test ladder is made construction standardization, totally 5 steps by white plastic.Mice is placed the bottom of case, and the back of the body is towards stair, mice incubation period, cat ladder number and the number of standing in the record 3min.
The result: with the matched group comparison, compound recipe olanzapine agomelatine can make mouse hind leg stand several and the time of standing obviously reduces, and has effect antianxity preferably.
Table 3 matched group is to mice anxiety indication influence (x ± s) relatively
Claims (8)
1. novel spiritual class pharmaceutical composition is characterized in that, it is to be active component with agomelatine and olanzapine, is combined to form with acceptable accessories.
2. the described compositions of claim 1 is characterized in that, " agomelatine " also comprises its pharmaceutical salts, optical isomer and hydrate.
3. the described compositions of claim 1 is characterized in that, " olanzapine " also comprises its pharmaceutical salts, optical isomer and hydrate.
4. the described compositions of claim 1 is characterized in that, the average unit formulation input amount of described olanzapine is 1.0mg～100mg.Be preferably 5-20mg.
5. compositions as claimed in claim 1 is characterized in that, the unit formulation content of described agomelatine is 5mg～125mg.Be preferably 25mg～50mg.
6. the described compositions of claim 1 is characterized in that, can be made into oral formulations.
7. compositions as claimed in claim 6 is characterized in that described oral formulations comprises tablet, capsule, soft capsule, chewable tablet, oral cavity disintegration tablet, buccal tablet, drop pill etc.
8. the described compositions of claim 1 is used for the treatment of mental sickness such as depression, insomnia anxiety, schizophrenia.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009100905385A CN101991577A (en) | 2009-08-19 | 2009-08-19 | Novel mental medicinal composition |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009100905385A CN101991577A (en) | 2009-08-19 | 2009-08-19 | Novel mental medicinal composition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN101991577A true CN101991577A (en) | 2011-03-30 |
Family
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN2009100905385A Pending CN101991577A (en) | 2009-08-19 | 2009-08-19 | Novel mental medicinal composition |
Country Status (1)
| Country | Link |
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| CN (1) | CN101991577A (en) |
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102949360A (en) * | 2011-08-10 | 2013-03-06 | 瑟维尔实验室 | Solid pharmaceutical composition for buccal administration of agomelatine |
| CN107325011A (en) * | 2016-04-30 | 2017-11-07 | 陕西合成药业股份有限公司 | A kind of melatonin class compound and its production and use |
| CN109069437A (en) * | 2016-06-01 | 2018-12-21 | 浙江华海药业股份有限公司 | A kind of agomelatine soft capsule preparation |
| WO2020260725A1 (en) * | 2019-12-20 | 2020-12-30 | Lts Lohmann Therapie-Systeme Ag | Transmucosal therapeutic system containing agomelatine |
-
2009
- 2009-08-19 CN CN2009100905385A patent/CN101991577A/en active Pending
Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102949360A (en) * | 2011-08-10 | 2013-03-06 | 瑟维尔实验室 | Solid pharmaceutical composition for buccal administration of agomelatine |
| CN107325011A (en) * | 2016-04-30 | 2017-11-07 | 陕西合成药业股份有限公司 | A kind of melatonin class compound and its production and use |
| CN109069437A (en) * | 2016-06-01 | 2018-12-21 | 浙江华海药业股份有限公司 | A kind of agomelatine soft capsule preparation |
| WO2020260725A1 (en) * | 2019-12-20 | 2020-12-30 | Lts Lohmann Therapie-Systeme Ag | Transmucosal therapeutic system containing agomelatine |
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Application publication date: 20110330 |