Novel preparation containing anticoagulant drug cilostazol and preparation method thereof

A technology of cilostazol and pharmacy, which is applied to the new preparation of anticoagulant drug cilostazol and its preparation field, and can solve the problems of low dissolution rate, uneven dissolution rate of sustained-release preparations, and difficulty in control.

Active Publication Date: 2022-05-27
许昌市中心医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008]Based on the basis of prior art, the present invention has overcome above-mentioned deficiency, has not only solved the problem that the dissolution rate of cilostazol poor water solubility causes is low, has made up for again The dissolution rate of sustained-release preparations is uneven and difficult to control. A double-layer tablet comprising a cilostazol immediate-release layer and a cilostazol sustained-release layer is provided. The immediate-release layer includes cilostazol, hydrophilic Sexual amino acids, pharmaceutically acceptable auxiliary materials; sustained-release layer includes cilostazol, sustained-release materials, pharmaceutically acceptable auxiliary materials
[0010] First, in order to solve the problem of poor water solubility of cilostazol, the inventor has carried out repeated and in-depth research and experiments, and found that combining cilostazol and hydrophilic Substances, especially hydrophilic amino acids, are mixed together and crushed or ground, which can increase the hydrophilic ability of cilostazol, thereby significantly promoting the dissolution of the drug

Method used

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  • Novel preparation containing anticoagulant drug cilostazol and preparation method thereof
  • Novel preparation containing anticoagulant drug cilostazol and preparation method thereof
  • Novel preparation containing anticoagulant drug cilostazol and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Embodiment 1 Cilostazol double-layer sustained-release tablets (1000 tablets)

[0037] Immediate release layer:

[0038]

[0039]

[0040] Slow release layer:

[0041]

[0042] Preparation:

[0043] (1) Preparation of immediate-release layer: mix cilostazol and hydrophilic amino acid, pulverize together at low temperature and evenly, add the auxiliary materials in the pulverized formula, and mix to obtain the mixture powder of immediate-release layer;

[0044] (2) Preparation of sustained-release layer: Mix cilostazol with the auxiliary materials in the formula evenly, add an appropriate amount of purified water, and granulate to obtain the mixture of sustained-release layer particles;

[0045] (3) Granulation: The immediate-release layer mixture powder obtained in step (1) and the slow-release layer mixture granules obtained in step (2) are placed in a double-layer tableting machine and compressed into a double-layer tablet.

Embodiment 2

[0046] Embodiment 2 Cilostazol double-layer sustained-release tablets (1000 tablets)

[0047] Immediate release layer:

[0048]

[0049] Slow release layer:

[0050]

[0051] The preparation method is the same as in Example 1.

Embodiment 3

[0052] Embodiment 3 Cilostazol double-layer sustained-release tablets (1000 tablets)

[0053] Immediate release layer:

[0054]

[0055]

[0056] Slow release layer:

[0057]

[0058] The preparation method is the same as in Example 1.

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Abstract

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to a novel preparation of an anticoagulant drug cilostazol and a preparation method of the novel preparation. The cilostazol preparation containing the double-layer sustained release tablet comprises a quick release layer and a sustained release layer, the quick release layer comprises cilostazol, hydrophilic amino acid and pharmaceutically acceptable auxiliary materials, and the sustained release layer comprises cilostazol, a sustained release material and pharmaceutically acceptable auxiliary materials. The cilostazol and the hydrophilic amino acid are co-crushed, the dissolution rate of the cilostazol is improved, a sustained-release material is preferably selected, the release of the cilostazol is accurately controlled, the in-vitro release can be as long as 24 hours, and the treatment effect of the cilostazol is prolonged.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a new preparation of an anticoagulant drug cilostazol and a preparation method thereof. Background technique [0002] Cilostazol is a typical intracellular cAMP PDE (cyclic AMP phosphodiesterase) inhibitor, and it has been known to inhibit platelet coagulation and dilate arteries by inhibiting PDE activity, in inhibition of blood coagulation, promotion of central blood circulation, anti-oxidative stress. It plays an important role in inflammatory and antiulcer effects, prevention and treatment of cerebral infarction, and improvement of cerebral circulation, and can also prevent diseases such as arteriosclerosis by inhibiting the growth of vascular smooth muscle cells that migrate to vascular endothelial cells. [0003] The current clinical use is mainly cilostazol ordinary tablets, and there are reports of other dosage forms. For example, Chinese p...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/24A61K47/18A61K47/46A61K47/38A61K31/4709A61P7/02
CPCA61K9/2086A61K9/2054A61K9/2013A61K31/4709A61P7/02
Inventor 翟华季张云飞
Owner 许昌市中心医院
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