CN102240270B - Blonanserin tablet and preparation method thereof - Google Patents
Blonanserin tablet and preparation method thereof Download PDFInfo
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- CN102240270B CN102240270B CN 201010170835 CN201010170835A CN102240270B CN 102240270 B CN102240270 B CN 102240270B CN 201010170835 CN201010170835 CN 201010170835 CN 201010170835 A CN201010170835 A CN 201010170835A CN 102240270 B CN102240270 B CN 102240270B
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Abstract
The invention provides a Blonanserin tablet and a preparation method thereof. The tablet contains Blonanserin, lactose and microcrystalline cellulose. Compared with present products and their preparation technologies, as the loss of active components during the direct compression process is very small, the Blonanserin tablet of the invention has a higher active component content and improved hardness, thus meeting the demands of commercial production and clinical medication.
Description
Technical field
The invention belongs to field of medicaments, be specifically related to a kind of Blonanserin tablet and preparation method thereof.
Background technology
In recent ten years, schizoid sickness rate shows ascendant trend.Take China as example, schizoid sickness rate by 5.69% of nineteen eighty-two rise in recent years 6.55%.According to Ministry of Public Health circular in 2002, China schizophrenia patient approximately had 8,000,000 people, and annual newly-increased patient 150,000 people, had been increased to 8,600,000 people to 2006.
Blonanserin is by the exploitation of SUMITOMO CHEMICAL Pharmaceutical Co., Ltd, the atypical antipsychotic in April, 2008 in Japan's listing.It belongs to 5-hydroxy tryptamine and dopamine antagonist, has the effect of blocking-up d2 dopamine receptor and 5-HT2A receptor.Compare with other resisting mental disease medicines in the market, the side effect reaction of its extrapyramidal system still less.
Yet the specification of existing blonanserin is 4mg, belong to low dose of specification, and wet granulation technology is adopted in the preparation of Blonanserin tablet usually in the prior art, there are following shortcoming in this technique and the Blonanserin tablet that makes thereof: 1) the active component loss is large in preparation process, is about 10-20%; 2) the used adhesive viscosities of granulating is inadequate, and the granule that makes is thinner, so be difficult to pressurization during tabletting, causes the hardness of tablet little.Therefore, need to improve for prescription and the preparation technology thereof of Blonanserin tablet, thereby develop a kind of new Blonanserin tablet and preparation technology thereof that can overcome above shortcoming.
Summary of the invention
One object of the present invention is to provide a kind of active component content and stability higher, and the Blonanserin tablet that is more suitable for of hardness.
Be used for realizing that above-mentioned technical purpose technical scheme is as follows:
A kind of Blonanserin tablet, this tablet comprises blonanserin, lactose and microcrystalline Cellulose.Preferably, count by weight, described tablet comprises 1 part of blonanserin; 10～20 parts of lactose, for example 15～20 parts; 9～15 parts of microcrystalline Cellulose, for example 10～12.5 parts.
Tablet of the present invention can also comprise adjuvant and/or additive commonly used on one or more pharmacopedicss.For example, this tablet can comprise cross-linking sodium carboxymethyl cellulose, and take 1 part of blonanserin as benchmark, the content of cross-linking sodium carboxymethyl cellulose can be 0.5～5 part.Tablet of the present invention can also comprise magnesium stearate, and take 1 part of blonanserin as benchmark, the content of magnesium stearate can be 0.5～5 part.In addition, tablet of the present invention can also comprise pregelatinized Starch, and take 1 part of blonanserin as benchmark, the content of described pregelatinized Starch can be 1～5 part.
For example, in a specific embodiments of tablet of the present invention, meter by weight, described tablet comprise 2.5 parts of 1 part of blonanserin, 15 parts of lactose, 12.5 parts of microcrystalline Cellulose, 1 part of cross-linking sodium carboxymethyl cellulose, 0.25 part of magnesium stearate and pregelatinized Starch.
For example, in another specific embodiments of tablet of the present invention, meter by weight, described tablet comprise 0.25 part of 1 part of blonanserin, 20 parts of lactose, 10 parts of microcrystalline Cellulose, 1 part of cross-linking sodium carboxymethyl cellulose and magnesium stearate.
Another object of the present invention is to provide the preparation method of above-mentioned Blonanserin tablet.
The invention provides the preparation method of above-mentioned Blonanserin tablet, in the preparation process of this preparation method the blonanserin loss little, and improved the hardness of tablet.
The preparation method of Blonanserin tablet provided by the invention may further comprise the steps:
1) each component is sieved mix homogeneously;
2) with step 1) granulating mixture that obtains, tabletting.
In above-mentioned preparation method, described step 1) preferred 60～80 mesh sieves that adopt that sieve in.
In order to solve the problem of the large and hardness deficiency of the active component loss that exists among existing Blonanserin tablet and the preparation technology thereof, on existing additive of tablet and preparation technology's basis, the present invention is through a large amount of screening and experimentation, finally adopt direct compression technique and with it corresponding prescription overcome above defective.Particularly, the present invention adopts compatibility test to confirm that the suitable adjuvant with the direct compression process using of blonanserin is compatible, directly mixed pressuring plate.The present invention further screens the adjuvant of direct compression process using again and compares, and has determined the suitable prescription of Blonanserin tablet.Compare with existing product and preparation technology thereof, because the active component loss is little in the preparation process of direct compression, the active component content of Blonanserin tablet of the present invention is higher, and hardness also is improved, and satisfies the needs of commodity production and clinical application.
The specific embodiment
Following examples only are used for explanation the present invention, and are not used in restriction the present invention.Unless otherwise indicated, the experiment condition in the embodiment of the invention is the experiment condition of this area routine.
Embodiment 1
Former, adjuvant compatibility test: investigate blonanserin and each vertical compression adjuvant and carrying out 60 ℃, the stability of accelerated test after 10 days of RH75%.
Sample treatment: the sample that forms shown in the table 1 is transferred in the 25ml volumetric flask, is diluted to scale with mobile phase, shake up, high-efficient liquid phase technique detects.
Table 1 compatibility test result
| The component kind | Component proportion (mg) | The content of acceleration environment active component after lower 10 days |
| Blonanserin: cellulose-lactose: pregelatinized Starch: cross-linking sodium carboxymethyl cellulose | 4.35∶99.93∶24.62∶4.01 | 99.2％ |
| Blonanserin: spray-dried lactose: microcrystalline Cellulose: cross-linking sodium carboxymethyl cellulose | 4.47∶98.28∶49.00∶4.45 | 97.8％ |
| Blonanserin accelerated test sample | 4.48 | 97.2％ |
| Blonanserin reference substance (do not carry out accelerated test, measure content and use) | 4.27 | 100％ |
Can find out by table 1 data, blonanserin raw material itself is very stable, and with the common compatibility of other vertical compression adjuvant the time, after the investigation under uniform temperature, the damp condition, content proves that without obvious decline they can mixed pressuring plate.
Embodiment 2
Prescription 1
Blonanserin 4.0g
Cellulose-lactose 110.0g
Cross-linking sodium carboxymethyl cellulose 4.0g
Magnesium stearate 1.0g
119g makes 1000
Preparation method: take by weighing each component by recipe quantity, cross 70 mesh sieves, fully mix homogeneously is granulated the single punch tablet machine tabletting.
Embodiment 3
Prescription 2
Blonanserin 4.0g
Spray-dried lactose 90.0g
Microcrystalline Cellulose 102 30.0g
Cross-linking sodium carboxymethyl cellulose 4.0g
Magnesium stearate 1.0g
129g makes 1000
Preparation method: take by weighing each component by recipe quantity, cross 60 mesh sieves, fully mix homogeneously is granulated the single punch tablet machine tabletting.
Embodiment 4
Prescription 3
Blonanserin 3.0g
Spray-dried lactose 45.0g
Optimization-type microcrystalline Cellulose 90 (PROSOLV SMCC90) 37.5g
Pregelatinized Starch 7.5g
Cross-linking sodium carboxymethyl cellulose 3.0g
Magnesium stearate 0.75g
96.75g, make 750
Preparation method: take by weighing each component by recipe quantity, cross 80 mesh sieves, fully mix homogeneously is granulated the single punch tablet machine tabletting.
Embodiment 5
Prescription 4
Blonanserin 3.0g
Spray-dried lactose 60.0g
Optimization-type microcrystalline Cellulose 90 (PROSOLV SMCC90) 30.0g
Cross-linking sodium carboxymethyl cellulose 3.0g
Magnesium stearate 0.75g
96.75g, make 750
Preparation method: take by weighing each component by recipe quantity, cross 70 mesh sieves, fully mix homogeneously is granulated the single punch tablet machine tabletting.
Embodiment 6
Optimization
Carrying out on the basis of former, adjuvant compatibility test above-mentioned prescription and preparation technology thereof being compared research.
The main technologic parameters of the tablet samples of table 2 embodiment 2～5 preparations
Data from table 2 can find out, the indices of prescription 3,4 meets the requirements.Therefore will write out a prescription 3 and prescription 4 carry out the technique amplification, adopt 12 stamping machine tablettings, mobility of particle and compressibility all meet the requirements as a result, can be used for the large production of commercialization.
Undertaken aluminum-plastic packagedly by the commercially available prod packaged form according to the samples of prescription 3,4 preparations, 40 ℃, RH75% and 60 ℃ are investigated 3 months under two kinds of acceleration environments of RH75%.Investigation result demonstration, content, the dissolution of prescription 3 and prescription 4 all obviously reduce, and be up to specification.
Claims (9)
1. Blonanserin tablet, this tablet comprises blonanserin, lactose and microcrystalline Cellulose, it is characterized in that, meter by weight, described tablet comprises 1 part of blonanserin; 10～20 parts of lactose; 9～15 parts of microcrystalline Cellulose; 0.5～5 part of cross-linking sodium carboxymethyl cellulose; 0.5～5 part of magnesium stearate.
2. tablet according to claim 1 is characterized in that, described lactose is 15～20 parts.
3. tablet according to claim 1 is characterized in that, described microcrystalline Cellulose is 10～12.5 parts.
4. each described tablet in 3 according to claim 1 is characterized in that, described tablet also comprises pregelatinized Starch.
5. tablet according to claim 4 is characterized in that, described pregelatinized Starch is 1～5 part.
6. a Blonanserin tablet is characterized in that, meter by weight, described tablet comprise 2.5 parts of 1 part of blonanserin, 15 parts of lactose, 12.5 parts of microcrystalline Cellulose, 1 part of cross-linking sodium carboxymethyl cellulose, 0.25 part of magnesium stearate and pregelatinized Starch.
7. a Blonanserin tablet is characterized in that, meter by weight, described tablet comprise 0.25 part of 1 part of blonanserin, 20 parts of lactose, 10 parts of microcrystalline Cellulose, 1 part of cross-linking sodium carboxymethyl cellulose and magnesium stearate.
8. the preparation method of each described tablet in 7 according to claim 1, this preparation method may further comprise the steps:
1) each component is sieved mix homogeneously;
2) granulating mixture that step 1) is made, tabletting.
9. preparation method according to claim 8 is characterized in that, described sieving adopted 60～80 mesh sieves.
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108392481A (en) * | 2018-05-21 | 2018-08-14 | 威海贯标信息科技有限公司 | A kind of Blonanserin tablet composition |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN104306345B (en) * | 2014-09-11 | 2017-07-21 | 丽珠医药集团股份有限公司 | A kind of oral slow-releasing preparation of blonanserin |
| CN104306346B (en) * | 2014-09-11 | 2017-07-21 | 丽珠医药集团股份有限公司 | A kind of sustained release preparation of blonanserin and preparation method thereof |
| CN107028903B (en) * | 2017-05-03 | 2020-03-10 | 深圳万和制药有限公司 | Blonanserin tablet pharmaceutical composition and preparation method thereof |
Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008050847A1 (en) * | 2006-10-25 | 2008-05-02 | Dainippon Sumitomo Pharma Co., Ltd. | Granular preparation prevented from caking |
| CN101530412A (en) * | 2008-03-10 | 2009-09-16 | 北京德众万全医药科技有限公司 | Pharmaceutical composition of blonanserin and preparation method thereof |
| CN101619039A (en) * | 2009-06-30 | 2010-01-06 | 严洁 | 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro-cycloocta[b]pyridine (blonanserin, Blonanserin) and composition thereof |
| CN101766626A (en) * | 2008-12-30 | 2010-07-07 | 严洁 | Blonanserin-contained oral preparation for treating schizophrenia |
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2010
- 2010-05-13 CN CN 201010170835 patent/CN102240270B/en active Active
Patent Citations (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2008050847A1 (en) * | 2006-10-25 | 2008-05-02 | Dainippon Sumitomo Pharma Co., Ltd. | Granular preparation prevented from caking |
| CN101530412A (en) * | 2008-03-10 | 2009-09-16 | 北京德众万全医药科技有限公司 | Pharmaceutical composition of blonanserin and preparation method thereof |
| CN101766626A (en) * | 2008-12-30 | 2010-07-07 | 严洁 | Blonanserin-contained oral preparation for treating schizophrenia |
| CN101619039A (en) * | 2009-06-30 | 2010-01-06 | 严洁 | 2-(4-ethyl-1-piperazinyl)-4-(4-fluorophenyl)-5,6,7,8,9,10-hexahydro-cycloocta[b]pyridine (blonanserin, Blonanserin) and composition thereof |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN108392481A (en) * | 2018-05-21 | 2018-08-14 | 威海贯标信息科技有限公司 | A kind of Blonanserin tablet composition |
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