Quetiapine fumarate-containing tablet and preparation method thereof

Abstract

The invention relates to a quetiapine fumarate-containing tablet and a preparation method thereof. The quetiapine fumarate-containing tablet or a tablet core thereof comprises quetiapine fumarate as an active component, internally added auxiliary materials and externally added auxiliary materials. The preparation method comprises the following steps of firstly crushing the active component, uniformly mixing the crushed active component with one or more internally added auxiliary materials, adding a wetting agent, carrying out primary granulation, drying obtained wet granules, crushing the granules, sieving the crushed granules with a 50-15-mesh sieve, uniformly mixing the sieved granules with the rest internally added auxiliary materials, adding the wetting agent again, carrying out secondary granulation, and drying and straightening wet granules obtained again; and then mixing the dried granules with the externally added auxiliary materials, and performing tabletting, wherein the internally added auxiliary materials include a filling agent, an adhesive and an internally added disintegrating agent; and the externally added auxiliary materials are an externally added disintegratingagent and a lubricating agent. According to the invention, through simple twice granulation, the problems of low dissolution rate and incomplete end-point dissolution caused by static electricity, aggregation, adsorption and high surface energy after crushing of large-size insoluble preparation raw materials are significantly solved, and the dissolution rate and the bioavailability are significantly improved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a tablet containing quetiapine fumarate and a preparation method thereof. Background technique [0002] Quetiapine fumarate (Quetiapine Fumarate), its tablet was first successfully developed by British AstraZeneca Co., Ltd., FDA approved listing in 1997, trade name Listed in my country in 2001, the trade name For the treatment of various types of schizophrenia. This product is not only effective on the positive symptoms of schizophrenia, but also has a certain effect on the negative symptoms of schizophrenia, and can also alleviate the emotional symptoms related to schizophrenia, such as depression, anxiety and cognitive deficit symptoms. Currently, the dosage forms that have been approved for marketing worldwide include regular-release tablets and sustained-release tablets, and the regular-release tablets are available in specifications of 25mg, 100mg, 200mg and ...

AI Technical Summary

Problems solved by technology

[0006] Chinese patent application CN101991555A discloses a kind of quetiapine fumarate tablet and preparation method thereof, by wet granulation of raw and auxiliary materials earlier during wet granulation, and then Adding povidone solution to continue granulation improves the fluidity of the granules and the stability during tablet filling, but this superiority is based on a certain degree of over-granulation, which can easily cause the hardness of the granules to be relatively high, commonly known as "Dead granules", the inside of the granule is difficult to disintegrate, and the drug inside the granule is difficult to dissolve and release. Obviously, this preparation method only pays attention to the dissolution rate of 45 minutes, and it does not pay attention to the overall dissolution rate of the product

[0007] Chinese patent application CN107582534A discloses a kind of special quetiapine fumarate sheet preparation method, by quetiapine fumarate, stabilizer (surfactant ) and water are prepared into a nano-suspension through a high-pressure homogenizer, and then spray-dried to obtain a nano-suspension, and finally mixed with auxiliary materials for dry granulation, tablet compression, and coating, thereby solving the problem of poor dissolution and disintegration speed. slow, low bioavailability

[0009] Chinese patent application CN109001353A discloses a kind of preparation method of quetiapine fumarate tablet, in order to obtain better stripping effect, this patent uses each material All of them have been crushed to 120 meshes, which will undoubtedly change the properties of the materials. Because the crushed raw materials are relatively fine and have high surface energy, there will be obvious electrostatic aggregation, and they have not paid attention to this property of the raw materials. The problem of incomplete end-point dissolution brought about by the change, and a discriminative medium has not been found to evaluate the dissolution behavior, which will significantly increase the risk of insufficient bioavailability of the drug

[0010]Quetiapine Fumarate Tablets are relatively large in clinical application specifications, which are poorly soluble drugs and poorly soluble in water. In order to improve the dissolution rate and biological Utilization, the raw materials must be pulverized before use, but the pulverized raw materials have obvious electrostatic effects, which are characterized by aggregation, adsorption and high surface energy, resulting in low dissolution rate and incomplete dissolution of preparation products. At present, there is no A simple and effective method suitable for large-scale production solves this problem, and the dissolution method of quetiapine fumarate tablets currently recorded in the pharmacopoeia standards of various countries does not have a good ability to distinguish the advantages and disadvantages of preparation products, and it is necessary to find a method A discriminative medium for evaluating product quality

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