CN101313903A - Medicament composition containing escitalopram - Google Patents
Medicament composition containing escitalopram Download PDFInfo
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- CN101313903A CN101313903A CN 200710099949 CN200710099949A CN101313903A CN 101313903 A CN101313903 A CN 101313903A CN 200710099949 CN200710099949 CN 200710099949 CN 200710099949 A CN200710099949 A CN 200710099949A CN 101313903 A CN101313903 A CN 101313903A
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- escitalopram
- pharmaceutical composition
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- microcrystalline cellulose
- mannitol
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Abstract
The invention relates to a medicine composition containing escitalopram, which comprises granules consisting of the escitalopram or other medicinal salts and disintegrants, and granules consisting of co-dried mannitol and microcrystalline cellulose, and simultaneously comprises sodium chloride. The composition conceals the strong bitterness of the escitalopram, and is used for treating the tristimania.
Description
Technical field
The present invention relates to contain the pharmaceutical composition of Escitalopram or its pharmaceutical salts, especially a kind of oral cavity disintegration tablet that contains this pharmaceutical composition.
Background technology
Depression belongs to the mental sickness class, has become a kind of disease of universality at present.According to statistics, the U.S. has 1,500 ten thousand adult to suffer from depression.Annual report that World Health Organization (WHO) announces not long ago shows: depression has occupied the 4th of the world's ten big diseases at present, expects the year two thousand twenty, will jump to the second, comes myocardial infarction afterwards before the cancer; In a year of future, will there be 5.8% man and 9.5% woman symptoms of depression can occur; In the global range, crowd's quantity of once experiencing certain spirit and neural aspect discomfort has in life reached 4.5 hundred million people at present, and wherein 5,000 ten thousand people suffer from epileptics, 2,400 ten thousand people suffer from schizophrenia, 1,0,000,000～2,0,000,000 people's suicide attempts, and have 1,000,000 people to implement suicide.
At present, along with the increase of patient amount, the antidepressant medicine development also enter a new stage.Clinical application is mostly based on injection, and antidepressant drug is mainly peroral dosage form in clinical use, the less use of other dosage forms.
Citalopram is one of commonplace antidepressants of current application, and citalopram is called as " the purest SSRIs ", and it is the highest in similar medicine to the relative selectivity that the 5-HT reuptake suppresses.CN01813752, CN02808468 all describe preparation citalopram preparation of compositions method in detail, and its enantiomer Escitalopram also has same advantage.CN02158181 disclose preparation citalopram enantiomer chemical compound preparation method and by its compositions that makes.And CN200380106377 mainly discloses the preparation method of the Escitalopram (S-citalopram) of hydrobromate form, relates generally to the preparation of the Escitalopram hydrobromate of amorphous or crystal form.CN1925844A discloses the preparation method of oxalates crystal grain particle diameter at least 20 μ m.
The effect of taking medicine for the patient that guarantees to suffer from depression, prepare and a kind ofly in the oral cavity, need not obey water, also need not to chew, place on the tongue, after meeting rapid dissolving of saliva or disintegrate, the Escitalopram oral cavity disintegration tablet of borrowing swallowing act to go into the stomach onset has realistic meanings.
When taking owing to oral cavity disintegration tablet simultaneously is disintegrate in the oral cavity, so adopt necessary method to cover the bad sense of taste that medicine produces in the oral cavity, patient can not produced conflict psychology to become research when medication and produce one of matter of utmost importance that oral cavity disintegration tablet institute must solution.Yet, taste beastly is arranged all for most drug.In the pharmaceutics field, mainly be by the beta-cyclodextrin inclusion compound effect, utilize solid dispersion technology or in compositions, add means such as correctives and reach the effect that medicine hides flavor.But those skilled in the art know when adopting beta-cyclodextrin inclusion compound effect and solid dispersion technology to hide flavor, and condition is wayward, and final products must verify that as X-diffraction, differential thermal analysis (DSC) etc., process is numerous and diverse through any special measures.
The method that adds correctives in compositions only is applicable to that also crude drug not have under the lighter situation of big zest and bitterness, and for the zest of some crude drug own especially greatly or bitterness when heavier, this method does not then have great role.
Summary of the invention
The purpose of this invention is to provide the simple oral solid drug composition of a kind of technology, the pharmaceutical composition that granule of being made up of Escitalopram or its officinal salt and disintegrating agent and the granule of being made up of exsiccant mannitol and microcrystalline Cellulose altogether and sodium chloride common combination form, said composition can be further used for preparing oral cavity disintegration tablet, and the intraoral disintegration time of oral cavity disintegration tablet is not had influence; This oral cavity disintegration tablet need not be obeyed water in the oral cavity, also need not to chew, and places on the tongue, after rapid dissolving of chance saliva or the disintegrate, borrows swallowing act to go into the stomach onset and gets final product.But the application of pharmaceutical composition of the present invention not only is confined to oral cavity disintegration tablet, also can be used in other oral formulations, as tablet, granule, capsule etc.
A kind of effective and technology is easy, be easy to the Orally disintegrating piece preparation method of molding in order to find to taste masking; the applicant is through discovering in a large number; behind Escitalopram and disintegrating agent dry granulation; behind the made granule mix homogeneously of mannitol and microcrystalline Cellulose PH101; again with the sodium chloride mix homogeneously; after adding an amount of other correctives, find to cover effectively the serious bitterness of Escitalopram pleasantly surprisedly, simultaneously the intraoral disintegration time of the oral cavity disintegration tablet of preparation is not had influence.This method also can be used for the medicine that other bitterness is heavier or zest is bigger.
Technical scheme of the present invention can with mannitol and the made granule mix homogeneously of microcrystalline Cellulose PH101, obtain the Escitalopram solid composite for behind Escitalopram and the disintegrating agent dry granulation, adds an amount of correctives, and this correctives is mainly sodium chloride.Above-mentioned composition all can further prepare the Escitalopram oral cavity disintegration tablet by adding other conventional adjuvant such as lubricant.
In said composition, the mannitol consumption is 2～8 times of principal agent Escitalopram; The correctives consumption is 0.04～0.2 times of Escitalopram; The microcrystalline Cellulose consumption is 1～4 times of Escitalopram; The consumption of disintegrating agent is 0.2～8 times of principal agent Escitalopram.
Correctives described in the said composition comprises one or more mixture in sucralose, acesulfame potassium, stevioside, the aspartame.
Disintegrating agent such as low-substituted hydroxypropyl cellulose, cross-linking sodium carboxymethyl cellulose, polyvinylpolypyrrolidone and carboxymethyl starch sodium.
Lubricant such as magnesium stearate, Pulvis Talci, calcium stearate, hydrogenated vegetable oil and light silicic acid anhydride.
Escitalopram Orally disintegrating piece preparation method of the present invention can for:
(1) with Escitalopram and disintegrating agent mix homogeneously, dry method is pressed large stretch of, crosses 30 order granulate.Get hybrid particles I.
(2) microcrystalline Cellulose and mannitol are granulated by common wet granulation technology, get hybrid particles II.
(3) with I and II mix homogeneously, add sodium chloride, other correctives, lubricant mixing, tabletting gets final product.
Embodiment
The present invention is further elaborated by following examples, but does not limit the scope of the invention.
Embodiment 1
| Escitalopram | 12.8 |
| Cross-linked carboxymethyl cellulose sodium | 10.0 |
| Mannitol | 51.4 |
| Microcrystalline Cellulose PH101 | 22.0 |
| Fructus Citri Limoniae essence | 0.10 |
| Sucralose | 0.10 |
| Mentholum | 1.00 |
| Sodium chloride | 0.60 |
| Magnesium stearate | 2.00 |
Preparation technology: with cross-linked carboxymethyl cellulose sodium mix homogeneously of recipe quantity Escitalopram and recipe quantity, it is large stretch of to adopt dry method to press, and granulates, and gets hybrid particles I; Recipe quantity mannitol and the microcrystalline Cellulose PH101 equivalent mix homogeneously that progressively increases, water system soft material, 24 mesh sieves are granulated, with 30 mesh sieve granulate, get hybrid particles II, granule 1 is pressed prescription mixed, sucralose, sodium chloride, Fructus Citri Limoniae essence, Mentholum, the magnesium stearate of other additional proportion amount, mix homogeneously with granule II; Measure drug content, determine that sheet is heavy, tabletting
Embodiment 2
| Escitalopram | 12.8 |
| Cross-linked carboxymethyl cellulose sodium | 8.0 |
| Mannitol | 53.4 |
| Microcrystalline Cellulose PH101 | 22.0 |
| Flavoring orange essence | 0.10 |
| Aspartame | 0.10 |
| Mentholum | 1.00 |
| Sodium chloride | 0.60 |
| Magnesium stearate | 2.00 |
Preparation technology: with cross-linked carboxymethyl cellulose sodium mix homogeneously of recipe quantity Escitalopram and recipe quantity, it is large stretch of to adopt dry method to press, and granulates, and gets hybrid particles I; Recipe quantity mannitol and the microcrystalline Cellulose PH101 equivalent mix homogeneously that progressively increases, water system soft material, 24 mesh sieves are granulated, with 30 mesh sieve granulate, get hybrid particles II, granule I and granule II are pressed prescription mixed, aspartame, sodium chloride, flavoring orange essence, Mentholum, the magnesium stearate of other additional proportion amount, mix homogeneously; Measure drug content, determine that sheet is heavy, tabletting
Embodiment 3
| Escitalopram | 12.8 |
| The low-substituted hydroxypropyl methylcellulose | 10.0 |
| Mannitol | 51.4 |
| Microcrystalline Cellulose PH101 | 22.0 |
| Fructus Citri Limoniae essence | 0.10 |
| Sucralose | 0.10 |
| Mentholum | 1.00 |
| Sodium chloride | 0.60 |
| Magnesium stearate | 2.00 |
Preparation technology: with the low-substituted hydroxypropyl methylcellulose mix homogeneously of recipe quantity Escitalopram and recipe quantity, it is large stretch of to adopt dry method to press, and granulates, and gets hybrid particles I; Recipe quantity mannitol and the microcrystalline Cellulose PH101 equivalent mix homogeneously that progressively increases, water system soft material, 24 mesh sieves are granulated, with 30 mesh sieve granulate, get hybrid particles II, granule I and granule II are pressed prescription mixed, aspartame, sodium chloride, flavoring orange essence, Mentholum, the magnesium stearate of other additional proportion amount, mix homogeneously; Measure drug content, determine that sheet is heavy, tabletting
Embodiment 4 (comparative example)
| Escitalopram | 12.8 |
| The low-substituted hydroxypropyl methylcellulose | 10.0 |
| Mannitol | 51.4 |
| Microcrystalline Cellulose PH101 | 22.0 |
| Fructus Citri Limoniae essence | 0.10 |
| Sucralose | 0.10 |
| Mentholum | 1.00 |
| Sodium chloride | 0.60 |
| Magnesium stearate | 2.00 |
Preparation technology: with recipe quantity Escitalopram and mannitol, the microcrystalline Cellulose mix homogeneously is granulated, and gets granule, adds the disintegrating agent of recipe quantity, correctives, magnesium stearate, mix homogeneously; Measure drug content, determine that sheet is heavy, tabletting
Select 6 volunteers that the sample of the various embodiments described above is carried out mouthfeel and Orally disintegrating time detecting, comprehensively its result, average, mouthfeel and Orally disintegrating time detecting the results are shown in Table 1.
The detection method of Orally disintegrating time is: select different experimenters, put into oral cavity disintegration tablet on the tongue and pick up counting, the slight friction of maxillary and tongue last slice is taken away the sheet surface by the part of saliva dissolves, stops timing in mouth when no solid or grittiness.
The mouthfeel of each embodiment of table 1 and mouth collapse the time limit
[notes] +++: it is fabulous, ++: good ,+: general ,-: it is relatively poor,--: poor,---: extreme difference
Conclusion: after Escitalopram and disintegrating agent granulation, mix with the interior granule that adds, add sodium chloride and other correctives, lubricant, the tablet mouthfeel that obtains is better, and disintegrate is very fast.Its preparation method is simple and easy to do simultaneously, and cost is low, has proved that said composition has excellent characteristic.
Claims (8)
1, a kind of oral solid drug composition is characterized in that comprising: the granule that Escitalopram or its officinal salt and disintegrating agent are formed, and by being total to granule and the sodium chloride that exsiccant mannitol and microcrystalline Cellulose are formed.
2, pharmaceutical composition as claimed in claim 1 is characterized in that the granule that described Escitalopram or its officinal salt and disintegrating agent are formed, and controls a method preparation by adopting dry method.
3, pharmaceutical composition as claimed in claim 1 is characterized in that the granule that described mannitol and microcrystalline Cellulose are formed, by adopting the wet granulation method preparation.
4,, it is characterized in that described two kinds of granules mix as each described pharmaceutical composition of claim 1-3.
5, pharmaceutical composition as claimed in claim 1 is characterized in that also comprising one or more lubricants, fluidizer and optional sweeting agent.
6, pharmaceutical composition as claimed in claim 1 is characterized in that existing with tablet, granule, Capsule form.
7, pharmaceutical composition as claimed in claim 1 is characterized in that existing with the form of oral cavity disintegration tablet.
8, pharmaceutical composition as claimed in claim 7 is characterized in that it is good less than 60 seconds and mouthfeel in intraoral disintegration time.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200710099949 CN101313903A (en) | 2007-06-01 | 2007-06-01 | Medicament composition containing escitalopram |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN 200710099949 CN101313903A (en) | 2007-06-01 | 2007-06-01 | Medicament composition containing escitalopram |
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| Publication Number | Publication Date |
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| CN101313903A true CN101313903A (en) | 2008-12-03 |
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Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN 200710099949 Pending CN101313903A (en) | 2007-06-01 | 2007-06-01 | Medicament composition containing escitalopram |
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102415992A (en) * | 2011-11-24 | 2012-04-18 | 福格森（武汉）生物科技有限公司 | Escitalopram oral liquid preparation |
-
2007
- 2007-06-01 CN CN 200710099949 patent/CN101313903A/en active Pending
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102415992A (en) * | 2011-11-24 | 2012-04-18 | 福格森（武汉）生物科技有限公司 | Escitalopram oral liquid preparation |
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Owner name: JIANGSU AVENTIS PHARMA. CO., LTD. Free format text: FORMER OWNER: DEZHONG WANQUAN PHARMACEUTICALS TECH. DEV. CO., LTD., BEIJING Effective date: 20120530 |
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Effective date of registration: 20120530 Address after: 225300 Taizhou City, Jiangsu Province medicine City Avenue, No. 1 Applicant after: Aventis Pharmaceutical (Jiangsu) Co., Ltd. Address before: 100097 Beijing city Haidian District Sijiqing Wanquan Zhuang 3 Building Applicant before: Dezhong Wanquan Pharmaceuticals Tech. Dev. Co., Ltd., Beijing |
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Open date: 20081203 |