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Composition containing phosphodiesterase inhibitor nanoparticle and protein kinase inhibitor

A protein kinase inhibitor and phosphodiesterase technology, applied in the field of medicine, can solve the synergistic antibacterial effect of non-phosphodiesterase inhibitors, synergistic antibacterial effects of non-phosphodiesterase inhibitors and protein kinase inhibitors, etc. question

Inactive Publication Date: 2018-12-21
黄泳华
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Studies have shown that phosphodiesterase (PDE) is expressed in some bacteria and also regulates the toxicity of bacteria, but there is currently no phosphodiesterase inhibitor represented by sildenafil citrate ( PDEI) is used for the technical instruction of bacteriostasis, also does not have the instruction that phosphodiesterase inhibitor and protein kinase inhibitor combine to produce synergistic bacteriostatic effect, more does not have phosphodiesterase inhibitor nanoparticle and protein kinase inhibitor combination to produce synergy Bacteriostatic teaching

Method used

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  • Composition containing phosphodiesterase inhibitor nanoparticle and protein kinase inhibitor
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  • Composition containing phosphodiesterase inhibitor nanoparticle and protein kinase inhibitor

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preparation example Construction

[0027] 4. Preparation and structure characterization of nanoparticles

[0028] In the present invention, the phosphodiesterase inhibitor nanoparticles are prepared by a solvent evaporation method well known to those skilled in the art, and the preparation method is as follows:

[0029] Accurately weigh a certain mass ratio of the mixture of phosphodiesterase inhibitors and PLGA (total mass is 60g) and dissolve it in 200mL of ethanol, and ultrasonically sonicate for 2 minutes to fully dissolve to form an oil phase; Inject into 400mL polyvinyl alcohol aqueous solution with a concentration of 5mg / mL, stir at 2000rpm for 2min to form the first emulsion; then inject the first emulsion into 1000mL polyvinyl alcohol aqueous solution with a concentration of 5mg / mL, stir at 500rpm After 5 hours until the organic solvent evaporated completely, the second emulsion was formed; finally, it was centrifuged at 4000 rpm for 20 minutes, and washed twice with deionized water. The particles wer...

Embodiment 1

[0068] Example 1 Preparation of particles containing phosphodiesterase inhibitor nanoparticles and protein kinase inhibitors

[0069] prescription

[0070]

[0071]

[0072] Preparation

[0073] Accurately weigh a certain mass ratio of the mixture of phosphodiesterase inhibitors and PLGA (total mass is 60g) and dissolve it in 200mL of ethanol, and ultrasonically sonicate for 2 minutes to fully dissolve to form an oil phase; Inject into 400mL polyvinyl alcohol aqueous solution with a concentration of 5mg / mL, stir at 2000rpm for 2min to form the first emulsion; then inject the first emulsion into 1000mL polyvinyl alcohol aqueous solution with a concentration of 5mg / mL, stir at 500rpm After 5 hours until the organic solvent evaporated completely, the second emulsion was formed; finally, it was centrifuged at 4000 rpm for 20 minutes, and washed twice with deionized water. The particles were collected and vacuum-dried at room temperature for 12 hours to obtain white nanopa...

Embodiment 2

[0075] Example 2 Preparation of Capsules Containing Phosphodiesterase Inhibitor Nanoparticles and Protein Kinase Inhibitors

[0076] prescription

[0077]

[0078] Accurately weigh a certain mass ratio of the mixture of phosphodiesterase inhibitors and PLGA (total mass is 60g) and dissolve it in 200mL of ethanol, and ultrasonically sonicate for 2 minutes to fully dissolve to form an oil phase; Inject into 400mL polyvinyl alcohol aqueous solution with a concentration of 5mg / mL, stir at 2000rpm for 2min to form the first emulsion; then inject the first emulsion into 1000mL polyvinyl alcohol aqueous solution with a concentration of 5mg / mL, stir at 500rpm After 5 hours until the organic solvent evaporated completely, the second emulsion was formed; finally, it was centrifuged at 4000 rpm for 20 minutes, and washed twice with deionized water. The particles were collected and vacuum-dried at room temperature for 12 hours to obtain white nanoparticles, which were sealed and prot...

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Abstract

The invention provides a composition containing a phosphodiesterase inhibitor nanoparticle and a protein kinase inhibitor. The composition is characterized in that the nanoparticles contain the phosphodiesterase inhibitor and polylactose glycolic acid, the phosphodiesterase inhibitor and the protein kinase inhibitor are both products available in the market in China and other countries, and the composition has a synergetic antibacterial function (the drug combination index is less than 1) on multiple bacteria.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a composition containing phosphodiesterase inhibitor nanoparticles and protein kinase inhibitors. 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 h...

Claims

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Application Information

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IPC IPC(8): A61K45/06A61K31/506A61K31/517A61K31/44A61K31/519A61P31/04A61P31/10
CPCA61K31/44A61K31/506A61K31/517A61K31/519A61K45/06A61P31/04A61P31/10A61K2300/00
Inventor 向飞李强刘荣黄泳华
Owner 黄泳华
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