Oral quetiapine sustained-release tablet

A quetiapine and gentle technology, applied in the direction of medical preparations of non-active ingredients, organic active ingredients, nervous system diseases, etc., can solve the problems of low affinity and no affinity, so as to reduce drug resistance, increase release time, The effect of reducing volatility

Inactive Publication Date: 2012-01-11
TIANJIN DEXUAN MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Quetiapine also has strong affinity for histamine H receptors and adrenergic α1 receptors, but slightly lower affinity for α2 receptors and little affinity for muscarinic or benzodiazepine receptors

Method used

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  • Oral quetiapine sustained-release tablet
  • Oral quetiapine sustained-release tablet
  • Oral quetiapine sustained-release tablet

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Each 1000 tablets of quetiapine fumarate sustained-release tablets (200mg) contains:

[0019]

[0020] Prepared according to the following process:

[0021] (1) 230.26g of quetiapine fumarate, 32.32g of pregelatinized starch, 43.42g of microcrystalline cellulose, 8g of hypromellose and 75g of sodium citrate dihydrate were crushed and sieved as required, and mixed evenly , use 50% ethanol to make a suitable soft material, and granulate;

[0022] (2) Dry the wet granules, granulate, add 140g of polyoxyethylene N-12, 35g of polyoxyethylene N-60, 7g of magnesium stearate, 5g of stearic acid, 4g of talcum powder auxiliary materials and mix evenly during granulation.

[0023] (3) Tablets.

[0024] (4) Coating.

Embodiment 2

[0026] Each 1000 tablets of quetiapine fumarate sustained-release tablets (200mg) contains:

[0027]

[0028] Prepared according to the following process:

[0029] (1) 230.26g of quetiapine fumarate, 34.32g of pregelatinized starch, 34.32g of microcrystalline cellulose pH101, 75g of sodium citrate dihydrate and 8g of hypromellose E50 were crushed and sieved as required, Mix evenly, use 66g 50% ethanol to make a suitable soft material, and granulate;

[0030] (2) Dry the wet granules, granulate, add 124.1g of polyoxyethylene 1105, 60g of polyoxyethylene 303, 7g of magnesium stearate, 7g of silicon dioxide auxiliary materials and mix well during granulation.

[0031] (3) Shaped stamping sheet.

[0032] (4) Coating.

Embodiment 3

[0034] Each 1000 tablets of Quetiapine Fumarate Sustained Release Tablets (50mg) contains:

[0035]

[0036]

[0037] Prepared according to the following process:

[0038] (1) 57.6g of quetiapine fumarate, 60g of pregelatinized starch, 143.4g of microcrystalline cellulose, 36g of sodium citrate dihydrate and 8g of hypromellose E50 were crushed and sieved as required, and mixed evenly , use 60g 50% ethanol to make a suitable soft material, and granulate;

[0039] (2) Dry the wet granules, granulate, add 150g of polyoxyethylene 750, 35g of polyoxyethylene N-60, 5g of magnesium stearate, 5g of silicon dioxide auxiliary materials and mix evenly during granulation.

[0040] (3) Shaped stamping sheet.

[0041] (4) Coating.

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PUM

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Abstract

The technical problem solved by the invention is to provide an oral sustained-release tablet of quetiapine and its salts which can effectively and continuously release for more than 12 hours, is slow in medical effect release, can stably maintain the effective plasma concentration for 24 hours, is long in release period, less in toxic or side effect, and convenient for administration; the main components are quetiapine with active components, a skeletal material with sustained-release effect, and an excipient; the invention is characterized in that on a basis of the total weight of the tablet, the tablet comprises 5%-50% of quetiapine with active components, 5%-50% of skeletal material with sustained-release effect, and 20%-50% of excipients. Polyoxyethylene with one or several different models is selected as the skeletal material. The excipient comprises a proper amount of sodium citrate dihydrate compounds. Polyoxyethylene is selected which can prolong the sustained-release period; the release period is greatly increased; the medicinal effect is released stably and slowly; the plasma concentration is guaranteed; the disease condition is controlled stably; patients are provided with 24-hour effective treatment; and the invention is widely applicable to single-dosage quetiapine treatment.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a slow-release tablet for oral administration of quetiapine and its salts. Background technique [0002] Quetiapine (Quetiapine) is an atypical antipsychotic drug, which belongs to dibenzodiazepine derivatives, so it can retain the curative effect of clozapine and overcome its own adverse reactions of granulocytes. In the brain, the drug acts on serotonin (5-HT 2 ,), dopamine D1, and dopamine D2 have high affinity, mainly due to blocking central dopamine D2 receptors and 5-hydroxytryptamine (5-HT 2 ) receptors, and play an antipsychotic effect, so it has a significant effect on the treatment of schizophrenia, and has no obvious adverse reactions. Quetiapine also has a strong affinity for histamine H receptors and adrenergic α1 receptors, but slightly lower affinity for α2 receptors, and basically no affinity for muscarinic receptors or benzodiazepine receptors. Compa...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/22A61K47/34A61K31/554A61P25/18
Inventor 董坚强王浩苏鸿雁
Owner TIANJIN DEXUAN MEDICAL TECH
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