Pharmaceutical composition containing nitroxoline lysine salt as well as preparation method and application of the pharmaceutical composition

A technology of nitroquinoline lysine salt and composition, which is applied in the field of pharmaceutical composition containing nitroquinoline lysine salt and its preparation and application, and can solve the problem of the absence of nitroquinoline lysine salt. The pharmaceutical composition and other issues, to achieve the effect of good dissolution properties

Inactive Publication Date: 2020-10-16
JIANGSU YAHONG MEDITECH CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in the prior art, there is no pharmaceutical composition containing nitroquinoline lysine salt, such as preparation

Method used

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  • Pharmaceutical composition containing nitroxoline lysine salt as well as preparation method and application of the pharmaceutical composition
  • Pharmaceutical composition containing nitroxoline lysine salt as well as preparation method and application of the pharmaceutical composition
  • Pharmaceutical composition containing nitroxoline lysine salt as well as preparation method and application of the pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Pass the active pharmaceutical ingredient and each auxiliary material through an 80-mesh sieve for subsequent use.

[0066] Accurately weigh each component respectively according to the above-mentioned first-layer prescription, 5-nitro-8-hydroxyquinoline L-lysine salt monohydrate, microcrystalline cellulose, crospovidone and sodium bicarbonate Mix thoroughly, then prepare soft material with 75wt% ethanol water solution (the consumption of 75wt% ethanol water solution is a conventional dosage, its quality accounts for 10%-30% of the total material quality of the first layer of prescription), pass through a 24 mesh sieve, Dry in a blast drying oven at 60°C for 2 hours, then use a 24-mesh sieve to sieve the granules, then add magnesium stearate and micro-powder silica gel, and mix well to obtain the first layer of granules.

[0067] Accurately weigh each component according to the above-mentioned second-layer prescription, and fully mix 5-nitro-8-hydroxyquinoline L-lysine ...

Embodiment 2

[0070] The first layer of particles and the second layer of particles were prepared according to the method of Example 1.

[0071] Weigh 166.67 mg of the first layer of granules and 333.33 mg of the second layer of granules for use (that is, the mass ratio of the two is 1:2). Pour the second layer of granules into the die ring of the tablet machine, lightly press it flat, and use it as the second layer. Then the first layer of granules is poured into the die ring of the tablet machine, and the first layer is pressed above the second layer to obtain the tablet of Example 2. The diameter of the punch of the tablet press is 11mm, and the pressure is controlled at 60-80N.

Embodiment 3

[0073] The first layer of particles and the second layer of particles were prepared according to the method of Example 1.

[0074] Weigh 333.33 mg of the first layer of granules and 166.67 mg of the second layer of granules for use (that is, the mass ratio of the two is 2:1). Pour the first layer of granules into the die ring of the tablet press, lightly press it flat, as the first layer; then pour the second layer of granules into the die ring of the tablet machine, and press the second layer above the first layer, Obtain the tablet of embodiment 3. The diameter of the punch of the tablet press is 11mm, and the pressure is controlled at 60-80N.

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PUM

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Abstract

The invention discloses a pharmaceutical composition containing nitroxoline lysine salt as well as a preparation method and application of the pharmaceutical composition. The pharmaceutical composition comprises a first layer and a second layer, wherein the first layer comprises 40%-70% of an active pharmaceutical ingredient, 10%-30% of a filling agent, 5%-12% of a disintegrating agent, 0.5%-2% ofa lubricating agent, 0.1%-1.5% of a flow aid and 10%-20% of an alkaline substance based on the total weight of the first layer; the second layer is prepared from the following components in percentage by total weight of the second layer: 40 to 70 percent of active pharmaceutical ingredient, 10 to 30 percent of filling agent, 10 to 35 percent of sustained-release material, 0.1 to 2 percent of lubricating agent and 0.1 to 2 percent of flow aid; and the active pharmaceutical ingredients are selected from one or more of nitroxoline lysine salt, a crystal form of the nitroxoline lysine salt and asolvate of the nitroxoline lysine salt. The pharmaceutical composition has a high dissolution property, and can achieve the purpose of suddenly releasing drugs in the early stage and continuously andslowly releasing drugs in the later stage.

Description

technical field [0001] The invention relates to a pharmaceutical composition containing nitroquinoline lysine salt, a preparation method and application thereof. Background technique [0002] Nitroxoline, whose chemical name is 5-nitro-8-hydroxyquinoline, was developed as an oral antibiotic drug in the 1960s, mainly for urinary system infections, and has a relatively safe history of use. The discovery and use of new antibiotics have been replaced. [0003] In recent years, new studies have found that nitroquinoline can simultaneously inhibit methionine aminopeptidase MetAP2 and silent information regulator 2-related enzymes SIRT1 in vascular endothelial cells, exerting a synergistic inhibitory effect on tumor angiogenesis, and at the same time inhibiting Inhibits the proliferation of tumor cells. Therefore, nitroquinoline has been redeveloped for the treatment of tumors including bladder cancer. [0004] However, how to improve the water solubility of nitroxyquinoline, th...

Claims

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Application Information

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IPC IPC(8): A61K9/22A61K9/36A61K47/38A61K47/36A61K31/47A61P31/00A61P35/00A61P13/02
CPCA61K9/209A61K9/2077A61K9/2095A61K9/2054A61K9/205A61K9/2866A61K31/47A61P31/00A61P35/00A61P13/02A61K9/2009A61K9/2059A61K9/2027A61K9/2086A61K9/5084A61K47/12A61K47/32A61K47/38
Inventor 刘江华潘柯郭玉申申帅孙继丽李丹丹陈杰
Owner JIANGSU YAHONG MEDITECH CO LTD
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