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Pharmaceutical composition containing papaverine and paeoniflorin and application of pharmaceutical composition

A composition and technology of papaverine, applied in the field of biomedicine, can solve problems such as unsatisfactory effects, and achieve the effects of inhibiting the release of inflammatory factors, inhibiting excessive activation, and accelerating repair

Pending Publication Date: 2021-12-03
三门峡市眼科医院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Previously, it was reported in the prior art that papaverine can inhibit the activation of microglial cells and reduce the inflammatory response, so it is expected to be used in the treatment of optic nerve damage such as glaucoma, but its effect is not satisfactory, and further improvement is needed

Method used

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  • Pharmaceutical composition containing papaverine and paeoniflorin and application of pharmaceutical composition
  • Pharmaceutical composition containing papaverine and paeoniflorin and application of pharmaceutical composition
  • Pharmaceutical composition containing papaverine and paeoniflorin and application of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Papaverine Concentration Screening

[0059] Experimental procedure

[0060] 1) BV2 cell culture

[0061] BV2 cells at 37 °C, 5% CO 2 Culture in an incubator, and the culture medium is DMED culture medium containing 10% FBS and 100U / mL penicillin / streptomycin double antibody. Well-grown cells were inoculated into 12-well cell culture plates (5.6 × 10 5 individual / mL) for later use.

[0062] 2) In the LPS group (group 1), 10ng / ml LPS was added to treat for 12h to induce the inflammatory response of BV2 cells;

[0063] 3) Add different concentrations of papaverine (0 μM, 0.4 μg / ml, 2 μg / ml, 10 μg / ml) for 4 hours.

[0064] 4) According to the ratio of 1:2000 (cells: microspheres), add 0.5um fluorescent microspheres to the medium, incubate at 37 degrees for 15 minutes, and rinse with PBS 3 times.

[0065] 5) The nuclei were stained with DAPI, and the phagocytosis of the beads by the cells was observed under a fluorescence microscope.

[0066] 6) Flow cytometry detects...

Embodiment 2

[0071] Drug combination screening.

[0072] 1. Experimental grouping

[0073] 1)LPS

[0074] 2) LPS + papaverine (10μg / ml)

[0075] 3) LPS+ papaverine (10μg / ml)+ paeoniflorin (200μM)

[0076] 4) LPS+ papaverine (10μg / ml)+ ferulic acid (10μM)

[0077] 5) LPS + papaverine (10μg / ml) + melatonin (10μM)

[0078] 6) LPS+ papaverine (10μg / ml)+ apigenin (30μM)

[0079] 2. Experimental steps

[0080] 1) BV2 cell culture

[0081] BV2 cells at 37 °C, 5% CO 2 Culture in an incubator, and the culture medium is DMED culture medium containing 10% FBS and 100U / mL penicillin / streptomycin double antibody. Well-grown cells were inoculated into 12-well cell culture plates (5.6 × 10 5 individual / mL) for later use.

[0082] 2) In the LPS group (group 1), 10ng / ml LPS was added to treat for 12h to induce the inflammatory response of BV2 cells;

[0083] 3) Groups 2 to 6 were treated with components of corresponding working concentration except LPS for 4 hours; group 1 was treated with the s...

Embodiment 3

[0093] Animal models verify the effectiveness of papaverine + paeoniflorin, papaverine + ferulic acid.

[0094] experiment process

[0095] 1. Surgical preparation of retinal injury model caused by unilateral optic nerve shearing in rats

[0096] Referring to the animal experiment standard of "Medical Experimental Zoology" edited by Qin Chuan and published by People's Medical Publishing House in 2008, the optic nerve crush injury model was established by the left eye optic nerve clamp method. The rats to be modeled were instilled with 0.25% chloramphenicol eye drops 3 times a day 3 days before the model was established. The rats were anesthetized by intraperitoneal injection of 3.5% chloral hydrate in the right lower abdomen, and the left eye of the rat was topically anesthetized with 1% proparacaine hydrochloride. After anesthesia, fix the rat on the animal operating table, cut the bulbar conjunctiva circularly along the temporal limbus of the left eye, separate the bulbar co...

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Abstract

The invention relates to the field of biomedicine, in particular to a pharmaceutical composition containing papaverine and paeoniflorin and an application of the pharmaceutical composition. According to the pharmaceutical composition containing the papaverine and the paeoniflorin and the application of the pharmaceutical composition, the composition has an obvious synergistic effect, can better inhibit excessive activation of microglial cells, inhibits release of inflammatory factors of the microglial cells, and accelerates repair of nerve injury.

Description

technical field [0001] The invention relates to the field of biomedicine, in particular to a pharmaceutical composition containing papaverine and paeoniflorin and application thereof. Background technique [0002] Microglia, also known as microglia, is a glial cell present in the brain and spinal cord, accounting for about 10% to 15% of the number of brain cells. As a macrophage group present in the central nervous system, microglia are the fastest responding and most important immune barrier in the central nervous system. The distribution area of ​​microglia in the central nervous system usually does not overlap with other glial cells such as astrocytes. Microglia are very important to maintain the normal function of the central nervous system: they can remove neuritic plaques, pathogens, and damaged or non-functional neurons and axons in the central nervous system. Microglia can sense small changes in the concentration of extracellular potassium ions through a special po...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K31/472A61P27/06A61P25/16A61P25/28A61P27/02A61P25/00A61P9/10
CPCA61K31/7048A61K31/472A61P27/06A61P25/16A61P25/28A61P27/02A61P25/00A61P9/10A61K2300/00
Inventor 党亚龙
Owner 三门峡市眼科医院
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