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Composition containing orlistat nanoparticles and protein kinase inhibitor

A protein kinase inhibitor, orlistat technology, applied in the field of medicine, can solve the problem of no orlistat, synergistic antibacterial effect of orlistat and protein kinase inhibitors, etc.

Inactive Publication Date: 2019-01-29
ZHONGSHAN WANHAN PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are literatures suggesting that fatty acid synthase plays a certain role in the physiological regulation of bacteria, but there is no technical teaching on orlistat for antibacterial in the prior art, and there is no orlistat and protein kinase inhibitors Combination produces synergistic antibacterial effect, not to mention the combination of orlistat nanoparticles and protein kinase inhibitors to produce synergistic antibacterial effect

Method used

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  • Composition containing orlistat nanoparticles and protein kinase inhibitor
  • Composition containing orlistat nanoparticles and protein kinase inhibitor
  • Composition containing orlistat nanoparticles and protein kinase inhibitor

Examples

Experimental program
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preparation example Construction

[0024] 3. Preparation and structure characterization of nanoparticles

[0025] The present invention adopts the solvent volatilization method well known to those of ordinary skill in the art to prepare the described orlistat nanoparticles, and its preparation method is as follows:

[0026] PLGA with various characteristic parameters was taken and dissolved in a mixed solvent of 0.5mL acetone and 0.5mL methylene chloride to prepare an oil phase matrix with a total carrier concentration of 20mg / mL. Take a certain amount of orlistat, disperse it in the oil phase matrix, and then sonicate at 300W for 30 seconds, add the obtained emulsion into 2mL of 3% (w / v) polyvinyl alcohol, and then sonicate at 300W for 100 seconds, That is, the complex milk emulsion is obtained. Add the double emulsion emulsion into 20 mL of 0.5% (w / v) polyvinyl alcohol under stirring, and distill off the remaining acetone and chloroform under reduced pressure to obtain the obtained product.

[0027] In the ...

Embodiment 1

[0086] Example 1 Preparation of capsules comprising orlistat nanoparticles and imatinib mesylate (molar ratio is 0.01:1)

[0087] Prescription (g)

[0088]

[0089] Preparation

[0090] Take orlistat nanoparticles, imatinib mesylate, sorbitol and sodium stearyl fumarate in the prescribed amount, mix them thoroughly, fill capsules, and subpackage.

Embodiment 2

[0091] Embodiment 2 Preparation of tablets comprising orlistat nanoparticles and gefitinib (molar ratio is 0.25:1)

[0092] Prescription (g)

[0093]

[0094] Preparation

[0095] Take orlistat nanoparticles, gefitinib, microcrystalline cellulose, and magnesium stearate in the prescribed amount, mix them thoroughly, and compress into tablets.

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PUM

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Abstract

On one hand, the invention provides a composition containing orlistat nanoparticles and a protein kinase inhibitor. The composition is characterized in that the orlistat nanoparticles contain orlistatand poly(lactose-glycolic acid), the protein kinase inhibitor is selected from one of imatinib, gefitinib, erlotinib, sunitinib, sorafenib, lapatinib, dasatinib, nilotinib, pazopanib, afatinib, bosutinib and crizotinib, or a pharmaceutically acceptable salt or a solvate of the selected one ingredient, or a solvate of the pharmaceutically acceptable salt. The in-vitro antibacterial experiment shows that the composition provided by the invention can generate a synergetic bacteriostasis effect for various bacteria including methicillin-resistant staphylococcus aureus.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a composition containing protein kinase inhibitors and orlistat nanoparticles. Background technique [0002] Infectious diseases are a large class of diseases caused by microbial infections such as bacteria, parasites, fungi, or viruses, and can be transmitted directly or indirectly between humans through various channels. Although a variety of anti-infective drugs, including antibiotics, antivirals, antifungals, and antiparasitics, are currently available for the treatment of infectious diseases, this disease remains one of the leading causes of illness or death worldwide. In 2010, approximately 15 million people worldwide died from infectious diseases. [0003] In 2001, the first protein kinase inhibitor imatinib was launched for the treatment of leukemia, which opened the prelude to the targeted therapy of tumors. As of October 2018, the FDA has approved more th...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K31/365A61K9/14A61K47/34A61P31/04A61K31/5377A61K31/506A61K31/517A61K31/44
CPCA61K9/146A61K31/365A61K31/44A61K31/506A61K31/517A61K31/5377A61K45/06A61P31/04A61K2300/00Y02A50/30
Inventor 向飞杜志博彭韪
Owner ZHONGSHAN WANHAN PHARM CO LTD