CN103893180A - Pharmaceutical composition for treating insomnia - Google Patents
Pharmaceutical composition for treating insomnia Download PDFInfo
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- CN103893180A CN103893180A CN201210586524.4A CN201210586524A CN103893180A CN 103893180 A CN103893180 A CN 103893180A CN 201210586524 A CN201210586524 A CN 201210586524A CN 103893180 A CN103893180 A CN 103893180A
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- hydrochloric acid
- insomnia
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- disintegration tablet
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Abstract
The invention discloses use of a pharmaceutical composition in a medicament for treating insomnia. The study finds that a novel medicament vilazodone hydrochloride for treating a major depressive disorder generates sedative-hypnotic action and treats insomnia of animals at the dosage lower than the clinical recommended dose. The invention also discloses preparation forms of the pharmaceutical composition for treating insomnia, preferably orally disintegrating tablets, components of the disintegrating tablets, and a preparation method thereof. The clinical research shows that the medicament disclosed by the invention is free of obvious toxic and side effects, significant in effect on treatment of insomnia, quick to take effect, convenient to use, and easy to accept by a sufferer. A new choice is provided for treatment of insomnia, and the pharmaceutical composition has a broad market prospect.
Description
Technical field
The invention belongs to medicine field, be specifically related to the purposes of a kind of pharmaceutical composition in the medicine of Cure for insomnia, the purposes of the oral cavity disintegration tablet that designs more specifically a kind of hydrochloric acid Wella oxazolone in the medicine of Cure for insomnia.
Background technology
Insomnia refers to fall asleep and maybe cannot keep sleep state, causes not having enough sleep.Claim again DIMS (DIMS), often can not obtain a kind of disease of ortho sleep as feature, the difficulty falling asleep that caused by a variety of causes, Depth of sleep or frequently too short, early awakening and the length of one's sleep are not enough or of poor quality etc., and common the causing reason of having a sleepless night mainly contains environmental factors, individual factors, Physical factors, Nervous and Mental Factors, emotional factor etc.Along with the quickening of process of industrialization, the aggravation of operating pressure and social competition, night life and bad life habits, the reasons such as aged tendency of population, it is serious that sleep disorder problem more shows.Although countries in the world are more and more paid attention to sleep quality problem and are attempted various solutions, produce little effect.
Hydrochloric acid Wella oxazolone (Vilazodone HCl) is potent and the reuptake inhibitor of selectivity five hydroxytryptamine and 5-HT1A acceptor portion agonist of a kind of dual function, is also first indolyl amine novel antidepressant.From 2011, since U.S.'s listing, always as a kind of newtype drug for the treatment of major depressive disorder, the maintenance dose of its medication was at 10mg-40mg, and predose is 10mg, arrives the maintenance dose of 40mg through the transition dosage of 20mg.Also not studies have reported that at present hydrochloric acid Wella oxazolone at treatment of insomnia patients and improve the application progress aspect sleep quality.
In the present invention, having the first-selected dosage form of pharmaceutical composition of Cure for insomnia purposes is oral cavity disintegration tablet, in the hydrochloric acid Wella oxazolone oral cavity disintegration tablet of preparing Cure for insomnia, be insoluble in water in order to solve hydrochloric acid Wella oxazolone, the shortcoming that In Vitro Dissolution is low, in formulation and technology research, aspect two, improve: the one, hydrochloric acid Wella oxazolone is carried out to micronization processes, make the particle diameter of active component have 90% to be less than 20 microns, i.e. D
9020 microns of <; Make the tablet can disintegrate within 1 minute in saliva of buccal cavity by formula on the other hand, in formula, the ratio of water-soluble filler be more than or equal to 80%.More than the hydrochloric acid Wella oxazolone oral cavity disintegration tablet In Vitro Dissolution of preparation is rapid, and good mouthfeel, easy to use, confirms to have good Cure for insomnia through zoopery and clinical trial, improves the clinical effectiveness of sleep quality.
Summary of the invention
The object of this invention is to provide the purposes of a kind of pharmaceutical composition in the medicine of Cure for insomnia.In the time carrying out the pharmacological effect zoopery of hydrochloric acid Wella oxazolone, the unexpected medicine hydrochloric acid Wella oxazolone of finding treatment major depressive disorder can produce the effect that improves sleep therapy insomnia in the time of lower dosage, and the toxic and side effects of dosage correlation also reduces greatly simultaneously.In order to realize this purposes, hydrochloric acid Wella oxazolone need to be made and is applicable to the dosage form that insomniac uses, the present invention has chosen the fast oral cavity disintegration tablet dosage form of taking convenience rate of release, and by the means of micronised active ingredient and adjustment formula, improve the dissolution of slightly solubility composition hydrochloric acid Wella oxazolone; Improved mouthfeel by other preparation means, patient Geng Yi is accepted, the present invention, for Cure for insomnia provides a kind of new selection, has wide market prospect.The present invention can realize by following complete skill scheme:
The purposes of pharmaceutical composition in the medicine of Cure for insomnia, the active component of wherein said pharmaceutical composition is hydrochloric acid Wella oxazolone; Hydrochloric acid Wella oxazolone Cure for insomnia dosage be 5mg-10mg
The poorly water-soluble of hydrochloric acid Wella oxazolone, sees through the speed of buccal absorption in order to increase it, and the uncomfortable microgranule sense producing while reducing orally administer, and hydrochloric acid Wella oxazolone need to pass through micronization processes in advance, and index is granularity D
9020 microns of <, have the particle diameter of 90% hydrochloric acid Wella oxazolone to be less than 20 microns.
Because oral cavity disintegration tablet has other the incomparable advantage of fast-release tablet, quickly disintegrated fast dissolving dosage form equally, oral cavity disintegration tablet can be positioned in oral cavity, medicament is released in saliva and is taken after not needing extra liquid drug delivery or dissolving in advance dispersion medicine by the suitable taste of formula adjustment; And medicine is after Orally disintegrating, and a part enters in stomach through swallowing of patient, some without the effect that was subject to of liver, has reduced the efficient effect under low dosage that ensured that destroys directly by buccal absorption.Therefore the medicine composition dosage form of our Cure for insomnia purposes is oral cavity disintegration tablet.
In order to realize the smooth making of oral cavity disintegration tablet except the hydrochloric acid Wella oxazolone that comprises Cure for insomnia dosage, also comprise water-soluble filler 70%-80%, disintegrating agent 1%-5%, correctives 0.1%-1%.
Above-described water-soluble filler is selected from any one or more mixture in mannitol, xylitol, sorbitol, lactose, sucrose and glucose; Described disintegrating agent be crosslinked poly-dimension with in, carboxymethyl starch sodium, cross-linked carboxymethyl cellulose calcium, low-substituted hydroxypropyl methylcellulose any one or several.
Described correctives is sweeting agent, aromatic and the acidic flavoring agent pharmaceutically commonly used or their mixture.The pharmaceutically acceptable taste masking adjuvant such as conventional is glycyrrhizin, Aspartane, sucralose, saccharin sodium, cyclamate, various synthetic or natural fruit essence and vitamin C, citric acid.
In the preparation process of oral cavity disintegration tablet, also to add as required in addition a certain amount of binding agent, wetting agent, lubricant, fluidizer.Conventional binding agent has polyvidone, starch slurry, hydroxypropyl methylcellulose, microcrystalline Cellulose etc.; Wetting agent has the alcoholic solution of purified water or variable concentrations; Lubricant and fluidizer are often selected from one or more in magnesium stearate, stearic acid, sodium lauryl sulphate, Macrogol 4000 or polyethylene glycol 6000, micropowder silica gel, Pulvis Talci.The consumption of described binding agent, wetting agent, fluidizer is conventional amount used pharmaceutically.
In the present invention, for improving the preparation of hydrochloric acid Wella oxazolone of sleep quality matter, can take mode conventional in current preparation to prepare, such as wet granule compression tablet mode and direct compression mode, concrete operation is as follows:
1, wet granule compression tablet: by for subsequent use hydrochloric acid Wella oxazolone comminution by gas stream to 1 micron～20 microns (90% particle diameter will drop in the particle size range of requirement); The hydrochloric acid Wella oxazolone of getting recipe quantity is mixed homogeneously with the water-soluble filler, the disintegrating agent correctives that add in prescription, add binding agent wet granulation, dry, Extra Section disintegrating agent, lubricated fluidizer mix homogeneously, tabletting, makes hydrochloric acid Wella oxazolone oral cavity disintegration tablet.
2, direct compression mode: by for subsequent use hydrochloric acid Wella oxazolone comminution by gas stream to 1 micron～20 microns (90% particle diameter will drop in the particle size range of requirement); The hydrochloric acid Wella oxazolone of getting recipe quantity is mixed homogeneously with the water-soluble filler, disintegrating agent correctives and lubricant, the fluidizer that add in prescription, and direct compression, makes hydrochloric acid Wella oxazolone oral cavity disintegration tablet.
Detailed description of the invention
Below come by specific embodiment the present invention to do more detailed description, but can't form any restriction to the present invention
Embodiment 1
Preparation method: by for subsequent use hydrochloric acid Wella oxazolone comminution by gas stream to 1 micron～20 microns (90% particle diameter will drop in the particle size range of requirement); The hydrochloric acid Wella oxazolone of getting recipe quantity is mixed homogeneously with the xylitol, lactose, the cross-linking sodium carboxymethyl cellulose of interior dosage, Aspartane, the citric acid that add in prescription, add the appropriate wet granulation of purified water, dry, in dry granule, add cross-linking sodium carboxymethyl cellulose, the cherry essence mix homogeneously of outer dosage, tabletting, makes 1000 and get final product.
Embodiment 2
Preparation method is: by for subsequent use hydrochloric acid Wella oxazolone comminution by gas stream to 1 micron～20 microns (90% particle diameter will drop in the particle size range of requirement); The hydrochloric acid Wella oxazolone of getting recipe quantity is mixed homogeneously with the water-soluble filler, disintegrating agent correctives and lubricant, the fluidizer that add in prescription, and direct compression is made 1000 and get final product.
Embodiment 3 hydrochloric acid Wella oxazolone tranquilizing soporifics, improve the zoopery of sleep quality.
Experiment material: clean level male SD rat (SPF grade derives from Beijing Medical University's Experimental Animal Center), body weight 180-200g, raising condition: room temperature (22 ± 1) DEG C, humidity (50.4 ± 10) %, illumination in 12 hours-dark rhythmicity circulation, freely drinks water, takes food.
Experimental technique: administration is grouped into: normal saline blank group, basic, normal, high three the dosage groups of hydrochloric acid Wella oxazolone, dosage is 5mg/kg, 7.5mg/kg, 10mg/kg, and the hydrochloric acid Wella oxazolone of corresponding dosage is suspended in gastric infusion in appropriate normal saline.Record the time of every rat righting reflex loss and the time that righting reflex starts.Count Sleep latency from hydrochloric acid Wella oxazolone gavage to the time of righting reflex loss; The time that the time of righting reflex loss starts to occur to righting reflex is counted the length of one's sleep.The mensuration of the length of one's sleep must be carried out between 11:00-15:00 on the same day.
Improving sleep quality, to increase the experimental result of the length of one's sleep as shown in table 1 below:
The rat experiment result of table 1 hydrochloric acid Wella oxazolone sedative-hypnotic effect
| Average Sleep latency (min) | The average length of one's sleep (min) | |
| Normal saline blank | 3.60 | 93.5 |
| Hydrochloric acid Wella oxazolone low dose group | 2.98 | 104.7 |
| Dosage group in hydrochloric acid Wella oxazolone | 2.24 | 117.2 |
| Hydrochloric acid Wella oxazolone high dose group | 2.53 | 133.9 |
From above experimental result, the average Sleep latency time of hydrochloric acid Wella oxazolone dosage group and the average length of one's sleep increase than normal saline blank group, the Sleep latency of rat obviously shortens (P < 0.05), obviously extends (P < 0.05) length of one's sleep.Illustrate that hydrochloric acid Wella oxazolone can improve the sleep quality increase length of one's sleep of rat, has the physiologically active of Cure for insomnia.
Embodiment 4 hydrochloric acid Wella oxazolone oral cavity disintegration tablet mouthfeels and disintegrate experiment
Get the sample of embodiment 1 and embodiment 2, require to carry out the inspection of disintegration time according to 2010 editions two annex of Chinese Pharmacopoeia, measure disintegration time and the mouthfeel in oral cavity in volunteer oral cavity, result is as shown in table 2 below simultaneously:
Table 2 hydrochloric acid Wella oxazolone oral cavity disintegration tablet disintegrate experiment
| Embodiment | Disintegration (s) | The intraoral disintegration time (s) | Mouthfeel |
| Embodiment 1 | 15 | 20 | Well, be easy to accept |
| Embodiment 2 | 18 | 22 | Well, be easy to accept |
The human body effect of embodiment 5 hydrochloric acid Wella oxazolone oral cavity disintegration tablet Cure for insomnias
Experimental subject is that insomnia is the patient of unique symptom, and insomnia frequency is at least occurring weekly 3 times, and lasting more than one month; Insomnia causes significant worries, or ergasia decrease in efficiency, or hinders social function.Discharge standard: discharge physical disease or patient with phychlogical problems.
Therapeutic Method: patient gives embodiment 1 and the each a slice of embodiment 2 sample every night, and matched group gives placebo 10 people; Embodiment group 10 people, 2 group of 10 people of embodiment; One month course for the treatment of
Observation index: relatively sleep disorder scale (SDRS) scoring changes.
Curative effect determinate standard: to subtract point rate as curative effect index before and after SDRS total score treatment.Subtract a point rate=(the rear total score of total score-treatment before treatment) front total score of/treatment.Subtract point rate > 75% for recovery from illness, 50%-75% is effective, and 25%-49% is for taking a turn for the better, and < 25% is invalid.Experimental result is recorded into following table 3:
Efficacy result (%) before and after the treatment of table 3 hydrochloric acid Wella oxazolone oral cavity disintegration tablet
| Number of cases | Recovery from illness | Effective | Take a turn for the better | Invalid | Total effective rate | |
| Placebo group | 10 | 0（0） | 2（20） | 3（30） | 5（50） | 5（50） |
| 1 group of embodiment | 10 | 1（10） | 5（50） | 3（30） | 1（10） | 9（90%） |
| 2 groups of embodiment | 10 | 1（10） | 7（70） | 1（10） | 1（10） | 9（90%） |
More than in experiment, the total effective rate for the treatment of group and placebo group has been compared marked difference (P < 0.05), illustrates that hydrochloric acid Wella oxazolone can reach the effect that improves sleep quality Cure for insomnia in the time of dosage.
Claims (9)
1. the purposes of pharmaceutical composition in the medicine of Cure for insomnia, is characterized in that the active component of described pharmaceutical composition is hydrochloric acid Wella oxazolone.
2. purposes as claimed in claim 1, is characterized in that the dosage of hydrochloric acid Wella oxazolone in described pharmaceutical composition is 5mg-10mg.
3. purposes as claimed in claim 1, the granularity D of the hydrochloric acid Wella oxazolone described in it is characterized in that
9020 microns of <.
4. purposes as claimed in claim 1, the dosage form that it is characterized in that the pharmaceutical composition of narrating is oral cavity disintegration tablet.
5. oral cavity disintegration tablet as claimed in claim 4, is characterized in that comprising hydrochloric acid Wella oxazolone 5mg-10mg, water-soluble filler 70%-80%, disintegrating agent 1%-5%.
6. oral cavity disintegration tablet as claimed in claim 4, is characterized in that also comprising the correctives of 0.1%-1%.
7. oral cavity disintegration tablet as claimed in claim 4, is characterized in that described water-soluble filler is selected from any one or more mixture in mannitol, xylitol, sorbitol, lactose, sucrose and glucose; Described disintegrating agent be crosslinked poly-dimension with in, carboxymethyl starch sodium, cross-linked carboxymethyl cellulose calcium, low-substituted hydroxypropyl methylcellulose any one or several.
8. oral cavity disintegration tablet as claimed in claim 4, is characterized in that described correctives is sweeting agent, aromatic and the acidic flavoring agent pharmaceutically commonly used or their mixture.
9. the oral cavity disintegration tablet as described in claim 4-8, is characterized in that for improving the insomnia of sleep quality treatment human body.
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| Application Number | Priority Date | Filing Date | Title |
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| CN201210586524.4A CN103893180A (en) | 2012-12-30 | 2012-12-30 | Pharmaceutical composition for treating insomnia |
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| CN201210586524.4A CN103893180A (en) | 2012-12-30 | 2012-12-30 | Pharmaceutical composition for treating insomnia |
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Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105213334A (en) * | 2015-09-15 | 2016-01-06 | 万特制药(海南)有限公司 | A kind of vilazodone oral cavity disintegration tablet and preparation method thereof |
| CN106580895A (en) * | 2016-12-07 | 2017-04-26 | 万全万特制药（厦门）有限公司 | Orally disintegrating tablet containing vilazodone hydrochloride solid dispersions and preparation method thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102219783A (en) * | 2011-05-05 | 2011-10-19 | 天津市汉康医药生物技术有限公司 | Vilazodone hydrochloride and composition thereof |
-
2012
- 2012-12-30 CN CN201210586524.4A patent/CN103893180A/en active Pending
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102219783A (en) * | 2011-05-05 | 2011-10-19 | 天津市汉康医药生物技术有限公司 | Vilazodone hydrochloride and composition thereof |
Non-Patent Citations (1)
| Title |
|---|
| 钟静瑜等: "5 -羟色胺与睡眠的研究进展", 《医学综述》 * |
Cited By (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105213334A (en) * | 2015-09-15 | 2016-01-06 | 万特制药(海南)有限公司 | A kind of vilazodone oral cavity disintegration tablet and preparation method thereof |
| CN106580895A (en) * | 2016-12-07 | 2017-04-26 | 万全万特制药（厦门）有限公司 | Orally disintegrating tablet containing vilazodone hydrochloride solid dispersions and preparation method thereof |
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Application publication date: 20140702 |