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Boletic acid quetiapine oral preparation and preparation method thereof

A technology for quetiapine fumarate and oral preparations, applied in the field of pharmaceutical preparations, can solve the problems of slow disintegration, slow drug absorption, and low bioavailability, and achieve good taste, fast absorption, and high bioavailability Effect

Inactive Publication Date: 2009-03-04
张宏宇
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] 1. Ordinary tablets disintegrate slowly, resulting in slow drug absorption and low bioavailability;
[0005] 2. Ordinary tablets are inconvenient to take and need to be swallowed with water. They are not suitable for those with dysphagia (especially elderly and children)

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Embodiment 1: Raw material ratio: quetiapine fumarate (in terms of quetiapine) 100g, sodium starch glycolate 20g, crospovidone 20g, mannitol 116g, aspartame 15g, micropowder silica gel 10g, Magnesium stearate 3g, essence 1g.

[0026] Preparation method: crush quetiapine fumarate, sieve, mix with aspartame and carboxymethyl starch sodium, make soft material with 5% povidone solution gastric humectant; granulate through 20 mesh sieve, and dry , use a 20-mesh sieve to sieve, add mannitol, crospovidone, micropowder silica gel, magnesium stearate, essence, mix well, measure the drug content, calculate the weight of the tablet, and press the tablet to obtain.

[0027] This orally disintegrating tablet has the following characteristics:

[0028] 1. Disintegration time limit inspection: all disintegrate into fine particles within 1 minute, and can pass through a 26-mesh sieve.

[0029] 2. Dissolution test: the dissolution rate is greater than 90% in 45 minutes.

[0030] Spec...

Embodiment 2

[0031] Embodiment 2: Raw material ratio: quetiapine fumarate (calculated as quetiapine) 25g, crospovidone 10g, microcrystalline cellulose 30g, sorbitol 30g, calcium hydrogen phosphate 5g, aspartame 6g , Micropowder silica gel 4g, magnesium stearate 2g.

[0032] The preparation method of the above quetiapine fumarate orally disintegrating tablets: take quetiapine fumarate and calcium hydrogen phosphate to pulverize respectively, and sieve; get the raw and auxiliary materials and mix, measure the drug content, calculate the tablet weight, and directly compress the tablet. Instantly.

[0033] The obtained orally disintegrating tablet has the following characteristics:

[0034] 1. Disintegration time limit inspection: all disintegrate into fine particles within 1 minute, and can pass through a 26-mesh sieve.

[0035] 2. Dissolution test: the dissolution rate is greater than 90% in 45 minutes.

Embodiment 3

[0036] Embodiment 3: Raw material proportioning: quetiapine fumarate coated granule (powder, counted in quetiapine) 100g, crospovidone 10g, microcrystalline cellulose 40g, lactose 50g, calcium hydrogen phosphate 15g, ammonium phosphate Saimi 7g, micronized silica gel 10g, sodium fumarate stearate 5g.

[0037] The preparation method of above quetiapine fumarate orally disintegrating tablet: get quetiapine fumarate fine powder, respectively with water, 0.5%-3% hypromellose solution or 1-30% povidone solution The wetting agent is granulated by a fluidized bed or a one-step granulator, dried, and granulated to obtain quetiapine fumarate granules. Take quetiapine fumarate granules, coat them with a coating solution until the coating weight increases by 2%-120%, stop coating, dry, and sieve for later use. The coating solution can be hypromellose solution, polyacrylic acid resin solution, or other polymer solutions or suspensions such as cellulose acetate or ethyl cellulose; the coa...

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PUM

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Abstract

The invention discloses a quetiapine fumarate oral preparation and a preparation method thereof. The quetiapine fumarate oral preparation is mainly prepared by raw materials with the following proportion by weight: 25-300 parts of quetiapine fumarate counted by quetiapine, 2-100 parts of disintegrating agent and 5-400 parts of filling agent. The preparation method of the oral preparation comprises the following process steps: (1) the quetiapine fumarate is taken, smashed, screened and evenly mixed with flavoring agent and the disintegrating agent, and wetting agent is added for preparing soft materials; (2) the soft materials are screen through a 20-mesh sieve for carrying out the granulation and the drying, the 20-mesh sieve is used for carrying out the size stabilization, the filling agent, an odor correcting agent, glidant and lubricant are added for even mixing; (3) the content of the drug which is evenly mixed is measured, the tablet weight is calculated, and the tablet pressing is carried out for the preparation. The oral preparation can be rapidly disintegrated in oral cavity without the use of water for the drug administration; the absorption is rapid and the bioavailability is high; and the taste is good.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to an oral preparation of quetiapine fumarate and a preparation method thereof. Background technique [0002] Quetiapine fumarate, 11-{4-[2-(2-(hydroxyethoxy)ethyl-1-piperazine])dibenzo[b,f][1,4]thiazepine {Zhuo}·1 / 2 fumarate is an atypical antipsychotic. Quetiapine fumarate is a diphenoxazepine drug, similar in structure to clozapine and olanzapine, and is an antagonist of multiple neurotransmitter receptors in the brain. Preclinical pharmacology studies have shown that quetiapine fumarate has similar pharmacological characteristics to clozapine, that is, it has a balanced regulation effect on 5HTergic and DAergic neural pathways, and is a 5HT / D2 receptor blocker. The drug has a greater affinity for 5HT2A than D2 receptors, and its pharmacological characteristics of selectively acting on the limbic system can explain its therapeutic effect on positive and negative symptoms and cogn...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/554A61K9/00A61K9/20A61P25/18
Inventor 张宏宇戴庆华杜军
Owner 张宏宇
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