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Solid quetiapine fumarate liposome preparation

A technology for quetiapine fumarate and solid preparations, applied in the field of pharmaceutical preparations, can solve problems such as unfavorable long-term storage, unsatisfactory drug stability, hidden dangers in clinical use and the like

Inactive Publication Date: 2013-01-23
HAINAN MEIDA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Although the above-mentioned quetiapine fumarate dosage form is prepared by screening specific auxiliary materials, it has certain advantages, but the stability of the drug is not ideal, it is not conducive to long-term storage, and the drug release rate and drug release process cannot or cannot be well controlled. It is also accompanied by a variety of adverse symptoms that inevitably occur frequently, and the bioavailability of quetiapine fumarate is low, thus bringing serious hidden dangers to clinical use

Method used

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  • Solid quetiapine fumarate liposome preparation
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  • Solid quetiapine fumarate liposome preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0061] Example 1 Preparation of quetiapine fumarate liposome tablets

[0062] The raw and auxiliary materials used are as follows:

[0063]

[0064] Adopt following production process to prepare quetiapine fumarate liposome tablet:

[0065] (1) 200g egg yolk lecithin, 120g cholesterol, 80g soybean sterol, 50g sorbitan stearate are dissolved in 1500ml acetone solvent, mix uniformly, remove organic solvent under reduced pressure on rotary evaporator, make phospholipid film;

[0066] (2) add 1500ml pH and be the phosphate buffer solution of 7.0, shake, stir to make phospholipid membrane fully hydrate, 3000rpm homogeneous emulsification, microporous membrane filtration, make blank liposome suspension;

[0067] (3) 100g of quetiapine fumarate was dissolved in the blank liposome suspension, filtered through a 0.45 μm microporous membrane, incubated at 59° C. for 30-40 minutes, and spray-dried to obtain a liposome solid;

[0068] (4) Mix quetiapine fumarate liposome solid with ...

Embodiment 2

[0070] Example 2 Preparation of quetiapine fumarate liposome tablets

[0071] The raw and auxiliary materials used are as follows:

[0072]

[0073] Adopt following production process to prepare quetiapine fumarate liposome tablet:

[0074] (1) 100g egg yolk lecithin, 60g cholesterol, 30g soy sterol, 45g sorbitan stearate are dissolved in 800ml acetone solvent, mix uniformly, remove organic solvent under reduced pressure on the rotary evaporator, make phospholipid film;

[0075] (2) Add 800ml of phosphate buffer solution with a pH of 7.0, shake and stir to fully hydrate the phospholipid membrane, homogeneously emulsify at 3000rpm, and filter through a microporous membrane to obtain a blank liposome suspension;

[0076] (3) 50g of quetiapine fumarate was dissolved in blank liposome suspension, filtered through a 0.45 μm microporous membrane, incubated at 59° C. for 30-40 minutes, and spray-dried to obtain a liposome solid;

[0077] (4) Mix quetiapine fumarate liposome so...

Embodiment 3

[0079] Example 3 Preparation of quetiapine fumarate liposome tablets

[0080] The raw and auxiliary materials used are as follows:

[0081]

[0082] Adopt following production process to prepare quetiapine fumarate liposome tablet:

[0083] (1) 50g egg yolk lecithin, 30g cholesterol, 20g soy sterol, 12g sorbitan stearate are dissolved in 400ml acetone solvent, mix uniformly, remove organic solvent under reduced pressure on rotary evaporator, make phospholipid film;

[0084] (2) Add 400ml pH of phosphate buffered saline solution of 7.0, shake and stir to make the phospholipid film fully hydrated, homogeneously emulsify at 3000rpm, and filter through a microporous membrane to obtain a blank liposome suspension;

[0085] (3) 25g of quetiapine fumarate was dissolved in the blank liposome suspension, filtered through a 0.45 μm microporous membrane, kept at 59° C. for 30-40 minutes, and spray-dried to obtain a liposome solid;

[0086] (4) Mix quetiapine fumarate liposome soli...

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Abstract

The invention provides a solid quetiapine fumarate liposome preparation and a preparation method thereof. According to the preparation method, quetiapine fumarate, yolk lecithin, cholesterol, soyasterol and sorbitam stearate are selected according to a specific weight ratio and prepared into high-quality quetiapine fumarate liposome, and the quetiapine fumarate liposome is prepared into a solid preparation according to a common preparation method. Compared with the traditional preparation, the preparation provided by the invention has the advantages of greatly improved stability, bioavailability and quality and reduced toxic and side effects.

Description

technical field [0001] The invention relates to a new solid preparation of quetiapine fumarate, a non-classic antipsychotic drug, in particular to a solid preparation of quetiapine fumarate liposome, belonging to the field of pharmaceutical preparations. Background technique [0002] Quetiapine Fumarate (Quetiapine Fumarate), the chemical name is 11-{4-[2-(2-hydroxyethoxy)ethyl]-1-piperazinyl}dibenzo[b,f][1 , 4] Thiazepine hemifumaric acid, molecular formula C 21 h 25 N 3 o 2 S 1 / 2C 4 h 4 o 4 , molecular weight: 441.54, structural formula: [0003] [0004] Quetiapine fumarate is an atypical antipsychotic that interacts with multiple neurotransmitter receptors. In the brain, quetiapine has a high affinity for serotonin (5HT2) receptors, greater than the affinity for dopamine D1 and dopamine D2 receptors in the brain. Quetiapine also has high affinity for histamine receptors and adrenergic α1 receptors, low affinity for adrenergic α1 receptors, but basically no af...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/127A61K9/20A61K31/554A61K47/28A61P25/18
Inventor 廖爱国公长春
Owner HAINAN MEIDA PHARMA
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