CN101991555A - Quetiapine fumarate tablet and preparation method thereof - Google Patents
Quetiapine fumarate tablet and preparation method thereof Download PDFInfo
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- CN101991555A CN101991555A CN2009100564802A CN200910056480A CN101991555A CN 101991555 A CN101991555 A CN 101991555A CN 2009100564802 A CN2009100564802 A CN 2009100564802A CN 200910056480 A CN200910056480 A CN 200910056480A CN 101991555 A CN101991555 A CN 101991555A
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Abstract
The invention relates to a quetiapine fumarate tablet and a preparation method thereof. The tablet of the invention comprises quetiapine fumarate, a filler, a disintegrant, povidone and magnesium stearate in certain proportions. The preparation method comprises the following steps: granulating the quetiapine fumarate, the filler and the disintegrant by a wet method; then adding the povidone and granulating into a soft material; screening, drying and finishing the soft material; adding the magnesium stearate and mixing; measuring the content and calculating the tablet weight; and respectively tabletting and coating to obtain the quetiapine fumarate tablet. The tablet can be used for treating schizophrenia. By using the formula provided by the invention, the defect of poor particle mobility during granulating in the prior art is overcome.
Description
Technical field
The invention belongs to field of medicaments, relate to a kind of pharmaceutical preparation and preparation method thereof, be specifically related to a kind of quetiapine fumarate tablet and preparation method thereof.
Background technology
Quetiapine fumarate, its chemistry 11-[4-[2-(2-hydroxyl-oxethyl) ethyl by name]-the 1-piperazinyl] dibenzo [b, f] [1,4] sulfur azatropylidene hemifumarate, be a kind of atypical antipsychotic, its structure is similar with olanzapine to clozapine, and the various neurotransmitters receptor is had interaction.In brain, quetiapine fumarate is to serotonin (5HT
2) receptor has high affinity, and greater than the affinity to dopamine D 1 in the brain and d2 dopamine receptor.Quetiapine fumarate can have high-affinity by α 1 receptor equally to arteries and veins parathyrine on histamine's receptor and the kidney, and is low to adrenergic alpha-2 receptor affinity, but cholinergic muscarinic receptor or benzodiazepine receptors are not had affinity substantially.Clinically, the quetiapine fumarate treatment schizophrenia positive and negative symptoms are all effective.
The dosage form of listing has ordinary tablet and slow releasing tablet, slow releasing tablet complicated process of preparation, cost height at present.Ordinary tablet has the specification of 25mg, 100mg and 200mg.
The quetiapine fumarate ordinary tablet of AstraZeneca, commodity think of by name is auspicious
Its label is made up of active constituent, polyvidone, calcium hydrogen phosphate, microcrystalline Cellulose, Sodium Hydroxymethyl Stalcs, lactose and magnesium stearate, and coating material is made up of hydroxypropyl emthylcellulose, PEG and titanium dioxide.In the preparation of above-mentioned tablet, add lactose and make that particulate flowability is poor in the pelletization, the wayward quality of the pharmaceutical preparations, tabletting sheet weight instability.
Summary of the invention
Technical problem to be solved by this invention provides a kind of quetiapine fumarate tablet, and the prescription of described tablet mobility of particle in pelletization is good, is easy to carry out quality control.
The invention provides a kind of quetiapine fumarate tablet, form by following component:
A) quetiapine fumarate of 230 ± 10 weight portions,
B) filler of 220 ± 20 weight portions,
C) disintegrating agent of 35 ± 5 weight portions,
D) polyvidone of 15 ± 5 weight portions,
E) magnesium stearate of 5 ± 1 weight portions,
F) coating material of coating amount;
Described filler is selected from one or more in microcrystalline Cellulose, starch, soluble starch, dextrin or the calcium hydrogen phosphate, preferred starch, microcrystalline Cellulose and calcium hydrogen phosphate mixed;
Described disintegrating agent is selected from one or more in low hydroxypropyl cellulose, cross-linking sodium carboxymethyl cellulose, crosslinked carboxymethyl fecula sodium, Sodium Hydroxymethyl Stalcs, crosslinked Sodium Hydroxymethyl Stalcs, Carboxymethyl cellulose sodium, crosslinked Carboxymethyl cellulose sodium, polyvinylpolypyrrolidone or the pre-paying starch that replaces, preferred Sodium Hydroxymethyl Stalcs;
Described coating material is the gastric solubility coating material, preferred Opadry, more preferably Opadry 03B.
The Ka Er flow index of quetiapine fumarate raw material is 48, raw material itself mobile very poor, and account for 40% of label gross weight, heavily stable for guaranteeing the tabletting sheet, investigated the influence of the filler of different proportion to mobility of particle, tablet appearance, disintegration and dissolution, the result is as shown in the table.
| Prescription 1 (mg/ sheet) | Prescription 2 (mg/ sheets) | Prescription 3 (mg/ sheets) | |
| Quetiapine fumarate | 230.26 | 230.26 | ?230.26 |
| Microcrystalline Cellulose | 55 | 53 | ?50 |
| Starch | 100 | 160 | ?130 |
| Calcium hydrogen phosphate | 40 | 40 | ?40 |
| Sodium Hydroxymethyl Stalcs | 35 | 35 | ?35 |
| Polyvidone | 15 | 13 | ?13 |
| Magnesium stearate | 5 | 5 | ?5 |
| Mobility of particle | Ka Er index 30, mobile poor | Ka Er index 18, good fluidity | Ka Er index 8, good fluidity |
| Tablet appearance | Bright and clean | Bright and clean | Bright and clean |
| Disintegration | 1′23″～1′58″ | 1′53″～3′38″ | ?1′48″～2′31″ |
| Dissolution | Stripping fully in the 45min | Stripping fully in the 45min | Stripping fully in the 45min |
Above result shows that the tablet of prescription 3 has good mobility of particle, and the tablet of making has good disintegrate effect and qualified dissolution.
The present invention also provides a kind of quetiapine fumarate tablet, is made up of following component:
A) quetiapine fumarate of 230 ± 10 weight portions,
B) filler of 220 ± 20 weight portions,
C) Sodium Hydroxymethyl Stalcs of 35 ± 5 weight portions,
D) polyvidone of 15 ± 5 weight portions,
E) magnesium stearate of 5 ± 1 weight portions,
F) Opadry of coating amount;
Described filler is made up of starch, calcium hydrogen phosphate and microcrystalline Cellulose, and preferred filler is made up of the starch of 130 ± 5 weight portions, the calcium hydrogen phosphate of 40 ± 5 weight portions and the microcrystalline Cellulose of 50 ± 10 weight portions.
The present invention also provides a kind of quetiapine fumarate tablet, is made up of following component:
A) quetiapine fumarate of 230 weight portions,
B) filler of 220 weight portions,
C) Sodium Hydroxymethyl Stalcs of 35 weight portions,
D) polyvidone of 15 weight portions,
E) magnesium stearate of 5 weight portions,
F) Opadry of coating amount;
Described filler is made up of the starch of 130 weight portions, the calcium hydrogen phosphate of 40 weight portions and the microcrystalline Cellulose of 50 weight portions.
The present invention also provides a kind of preparation method of quetiapine fumarate tablet, may further comprise the steps:
1) quetiapine fumarate is crossed 80 mesh sieves, filler and disintegrating agent are crossed 24 mesh sieves respectively, and magnesium stearate is crossed 40 mesh sieves, and polyvidone is dissolved in the mixed, standby of ethanol, water or the two arbitrary proportion;
2) quetiapine fumarate, filler and the disintegrating agent with step 1) carries out wet granulation; Add povidone solution again and granulate, make soft material;
3) above-mentioned soft material is crossed 20 mesh sieves, and drying with 20 mesh sieve granulate, adds magnesium stearate and mixes evenly;
4) measure said mixture content, it is heavy to calculate sheet, tabletting, and coating promptly makes described tablet; Wherein filler, disintegrating agent as mentioned above, the concentration of above-mentioned povidone solution is 5～20%, under this concentration, granule is easy to granulate.The preferred Opadry 03B of coating material that coating is used.
The present invention also provides a kind of preparation method of concrete quetiapine fumarate tablet, may further comprise the steps:
1) quetiapine fumarate is crossed 80 mesh sieves, microcrystalline Cellulose, starch, calcium hydrogen phosphate and Sodium Hydroxymethyl Stalcs are crossed 24 mesh sieves respectively, and magnesium stearate is crossed 40 mesh sieves, and compound concentration is the ethanol or the aqueous solution of 5～20% polyvidone, and is standby;
2) quetiapine fumarate, starch, microcrystalline Cellulose, calcium hydrogen phosphate and the Sodium Hydroxymethyl Stalcs with step 1) carries out wet granulation; Add povidone solution again and granulate, make soft material;
3) above-mentioned soft material is crossed 20 mesh sieves, and drying with 20 mesh sieve granulate, adds magnesium stearate and mixes evenly;
4) measure said mixture content, it is heavy to calculate sheet, and tabletting uses Opadry 03B to carry out coating, promptly makes described tablet.
Following tablet provided by the invention can be used for the schizoid medicine of preparation treatment:
A) quetiapine fumarate of 230 ± 10 weight portions,
B) filler of 220 ± 20 weight portions,
C) Sodium Hydroxymethyl Stalcs of 35 ± 5 weight portions,
D) polyvidone of 15 ± 5 weight portions,
E) magnesium stearate of 5 ± 1 weight portions,
F) Opadry of coating amount;
Described filler is made up of starch, calcium hydrogen phosphate and microcrystalline Cellulose.
Quetiapine fumarate tablet provided by the invention has when granulating characteristics such as the heavily stable and easy disintegrating of particulate good fluidity, tabletting sheet.
The specific embodiment
The invention will be further described below in conjunction with embodiment, can make this area professional and technical personnel more fully understand the present invention, but not limit the present invention in any way.
Embodiment 1
Quetiapine fumarate sheet (by 1000 scales) by following component and recipe quantity: the quetiapine fumarate of 230.26g, the starch of 130.74g, the calcium hydrogen phosphate of 40.00g, 50.00g microcrystalline Cellulose, 35.00g Sodium Hydroxymethyl Stalcs, the polyvidone of 15.00g, the magnesium stearate of 5.00g.
The preparation of label:
1) quetiapine fumarate is crossed 80 mesh sieves, microcrystalline Cellulose, starch, calcium hydrogen phosphate and Sodium Hydroxymethyl Stalcs are crossed 24 mesh sieves respectively, and magnesium stearate is crossed 40 mesh sieves, and polyvidone is dissolved in 95% ethanol, and concentration is about 15%, and is standby;
2) quetiapine fumarate, starch, microcrystalline Cellulose, calcium hydrogen phosphate and the Sodium Hydroxymethyl Stalcs with step 1) carries out wet granulation; The alcoholic solution that adds polyvidone is again granulated, and makes soft material;
3) soft material is crossed 20 mesh sieves, drying, and it is qualified to be dried to moisture;
4), add magnesium stearate and mix evenly with 20 mesh sieve granulate;
4) measure said mixture content, it is heavy to calculate sheet, tabletting, and coating promptly makes described tablet.
Measuring mixture, to contain quetiapine fumarate (calculating with Quetiapine) be 0.403, and press the 0.2g specification, to calculate sheet heavy, carries out tabletting, measures hardness, the sheet of label weigh and hardness as follows:
Sheet is heavy: 496.3g
Hardness: 70～110N
The coating process:
Coating material prescription (by 1000 scales): Opadry 03B 20g, 95% ethanol 150g, purified water 30g; Label is carried out coating, promptly make the quetiapine fumarate sheet.
Tablet detects:
Outward appearance: bright and clean
Content: 100.9%
Related substance: 0.19%
Disintegration: 1 ' 53 "～2 ' 10 "
All strippings in dissolution: the 45min
Embodiment 2-3
The component of according to the form below and recipe quantity prepare the quetiapine fumarate sheet respectively, and preparation method is with embodiment 1.
Claims (9)
1. quetiapine fumarate tablet is characterized in that being made up of following component:
A) quetiapine fumarate of 230 ± 10 weight portions,
B) filler of 220 ± 20 weight portions,
C) disintegrating agent of 35 ± 5 weight portions,
D) polyvidone of 15 ± 5 weight portions,
E) magnesium stearate of 5 ± 1 weight portions;
F) coating material of coating amount;
Described filler is selected from one or more in microcrystalline Cellulose, starch, soluble starch, dextrin or the calcium hydrogen phosphate, preferred starch, microcrystalline Cellulose and calcium hydrogen phosphate mixed;
Described disintegrating agent is selected from one or more in low hydroxypropyl cellulose, cross-linking sodium carboxymethyl cellulose, crosslinked carboxymethyl fecula sodium, Sodium Hydroxymethyl Stalcs, crosslinked Sodium Hydroxymethyl Stalcs, Carboxymethyl cellulose sodium, crosslinked Carboxymethyl cellulose sodium, polyvinylpolypyrrolidone or the pre-paying starch that replaces;
Described coating material is the gastric solubility coating material.
2. tablet according to claim 1 is characterized in that being made up of following component;
A) quetiapine fumarate of 230 ± 10 weight portions,
B) filler of 220 ± 20 weight portions,
C) Sodium Hydroxymethyl Stalcs of 35 ± 5 weight portions,
D) polyvidone of 15 ± 5 weight portions,
E) magnesium stearate of 5 ± 1 weight portions,
F) Opadry of coating amount;
Described filler is made up of starch, calcium hydrogen phosphate and microcrystalline Cellulose.
3. tablet according to claim 2 is characterized in that described filler is made up of the starch of 130 ± 5 weight portions, the calcium hydrogen phosphate of 40 ± 5 weight portions and the microcrystalline Cellulose of 50 ± 10 weight portions.
4. tablet according to claim 2, it is to be made up of following component:
A) quetiapine fumarate of 230 weight portions,
B) filler of 220 weight portions,
C) Sodium Hydroxymethyl Stalcs of 35 weight portions,
D) polyvidone of 15 weight portions,
E) magnesium stearate of 5 weight portions,
F) Opadry of coating amount;
Described filler is made up of the starch of 130 weight portions, the calcium hydrogen phosphate of 40 weight portions and the microcrystalline Cellulose of 50 weight portions.
5. tablet according to claim 1 is characterized in that being made up of following component:
A) quetiapine fumarate of 230.26mg,
B) filler of 220.74mg,
C) Sodium Hydroxymethyl Stalcs of 35.00mg,
D) polyvidone of 15.00mg,
E) magnesium stearate of 5.00mg,
F) Opadry of coating amount;
Described filler is made up of the starch of 130.74mg, the calcium hydrogen phosphate of 40.00mg and the microcrystalline Cellulose of 50.00mg.
6. the preparation method of the described quetiapine fumarate tablet of claim 1 may further comprise the steps:
1) quetiapine fumarate is crossed 80 mesh sieves, filler and disintegrating agent are crossed 24 mesh sieves respectively, and magnesium stearate is crossed 40 mesh sieves, and polyvidone is dissolved in the mixed, standby of ethanol, water or the two arbitrary proportion;
2) quetiapine fumarate, filler and the disintegrating agent with step 1) carries out wet granulation; Add povidone solution again and granulate, make soft material;
3) above-mentioned soft material is crossed 20 mesh sieves, and drying with 20 mesh sieve granulate, adds magnesium stearate and mixes evenly;
4) measure said mixture content, it is heavy to calculate sheet, tabletting, and coating promptly makes described tablet;
Wherein filler, disintegrating agent are as mentioned above.
7. preparation method according to claim 6 may further comprise the steps:
1) quetiapine fumarate is crossed 80 mesh sieves, microcrystalline Cellulose, starch, calcium hydrogen phosphate and Sodium Hydroxymethyl Stalcs are crossed 24 mesh sieves respectively, and magnesium stearate is crossed 40 mesh sieves, and polyvidone is dissolved in the mixed, standby of ethanol, water or the two arbitrary proportion;
2) quetiapine fumarate, starch, microcrystalline Cellulose, calcium hydrogen phosphate and the Sodium Hydroxymethyl Stalcs with step 1) carries out wet granulation; Add povidone solution again and granulate, make soft material;
3) above-mentioned soft material is crossed 20 mesh sieves, and drying with 20 mesh sieve granulate, adds magnesium stearate and mixes evenly;
4) measure said mixture content, it is heavy to calculate sheet, tabletting, and coating promptly makes described tablet.
8. method according to claim 6 is characterized in that the coating material that the described coating of step 4) uses is Opadry 03B.
9. method according to claim 6, the concentration that it is characterized in that povidone solution in the step 1) is 5～20%.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009100564802A CN101991555A (en) | 2009-08-14 | 2009-08-14 | Quetiapine fumarate tablet and preparation method thereof |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2009100564802A CN101991555A (en) | 2009-08-14 | 2009-08-14 | Quetiapine fumarate tablet and preparation method thereof |
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| Publication Number | Publication Date |
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| CN101991555A true CN101991555A (en) | 2011-03-30 |
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| Application Number | Title | Priority Date | Filing Date |
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| CN2009100564802A Pending CN101991555A (en) | 2009-08-14 | 2009-08-14 | Quetiapine fumarate tablet and preparation method thereof |
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Cited By (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102406606A (en) * | 2011-11-29 | 2012-04-11 | 海南美大制药有限公司 | Solid quetiapine fumarate liposome preparation |
| CN102885305A (en) * | 2012-10-12 | 2013-01-23 | 中科乐仁（北京）科技发展有限公司 | Health food composition for enhancing immunity and preparation method thereof |
| CN109001353A (en) * | 2018-10-29 | 2018-12-14 | 湖南洞庭药业股份有限公司 | Quetiapine fumarate tablet pharmaceutical composition and preparation method |
| CN112516101A (en) * | 2020-11-19 | 2021-03-19 | 南京海纳医药科技股份有限公司 | Tablet containing quetiapine fumarate and preparation method thereof |
-
2009
- 2009-08-14 CN CN2009100564802A patent/CN101991555A/en active Pending
Cited By (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN102406606A (en) * | 2011-11-29 | 2012-04-11 | 海南美大制药有限公司 | Solid quetiapine fumarate liposome preparation |
| CN102885305A (en) * | 2012-10-12 | 2013-01-23 | 中科乐仁（北京）科技发展有限公司 | Health food composition for enhancing immunity and preparation method thereof |
| CN109001353A (en) * | 2018-10-29 | 2018-12-14 | 湖南洞庭药业股份有限公司 | Quetiapine fumarate tablet pharmaceutical composition and preparation method |
| CN112516101A (en) * | 2020-11-19 | 2021-03-19 | 南京海纳医药科技股份有限公司 | Tablet containing quetiapine fumarate and preparation method thereof |
| CN112516101B (en) * | 2020-11-19 | 2023-01-31 | 南京海纳医药科技股份有限公司 | Tablet containing quetiapine fumarate and preparation method thereof |
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Application publication date: 20110330 |