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Methylprednisolone delivery material based on epsilon-polylysine, preparation method of methylprednisolone delivery material, and kit

A technology of polylysine and polylysine hydrochloride is applied in the directions of non-active ingredient medical preparations, medical preparations containing active ingredients, anti-inflammatory agents, etc., to achieve simple preparation, improve bioavailability, The effect of good biodegradability

Pending Publication Date: 2021-01-08
SHANGHAI SIXTH PEOPLES HOSPITAL
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, there is currently no technical solution that can meet the above requirements at the same time.

Method used

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  • Methylprednisolone delivery material based on epsilon-polylysine, preparation method of methylprednisolone delivery material, and kit
  • Methylprednisolone delivery material based on epsilon-polylysine, preparation method of methylprednisolone delivery material, and kit
  • Methylprednisolone delivery material based on epsilon-polylysine, preparation method of methylprednisolone delivery material, and kit

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Experimental program
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Effect test

Embodiment 1

[0035] This embodiment provides a methylprednisolone delivery material based on ε-polylysine, which has a structure such as formula (I):

[0036]

[0037] Wherein, n is a positive integer, and 5≤n≤200, a and b are sets of positive integers and 0, and a+b=n;

[0038] R 1 for:

[0039]

[0040] R 2 for: -H or

[0041]

Embodiment 2

[0043] This embodiment provides the preparation method of the ε-polylysine-based methylprednisolone delivery material having the structure of formula (I) in the above embodiment 1:

[0044] Accurately weigh 0.475g (1mmol) methylprednisolone sodium succinate, 0.138g (1.2mmol) N-hydroxysuccinimide and 0.286g (1.5mmol) 1-ethyl-(3-dimethylaminopropyl) Carbodiimide hydrochloride was fully dissolved in 25 mL of dichloromethane, and stirred at 25°C for 2 hours. Subsequently, dichloromethane was evaporated at 200 Pa, 30° C., and the obtained solid powder was dissolved in 2 mL of dichloromethane. Finally, column chromatography separation is carried out, separation conditions: 200-300 mesh column chromatography silica gel, eluent is a mixed solvent of dichloromethane / petroleum ether with a volume ratio of 1:2, and a white powder active intermediate with the structure of formula (II) is obtained. Body 0.521g (0.912mmol), yield 91.2%.

[0045]

[0046] Accurately weigh 1 g of ε-polyl...

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Abstract

The invention discloses a methylprednisolone delivery material based on epsilon-polylysine, a preparation method of the methylprednisolone delivery material, and a kit. The methylprednisolone deliverymaterial can prolong the residence time of methylprednisolone in an articular cavity and prolong the half-life period of methylprednisolone, has cartilage permeability and cell membrane permeability,can permeate into cartilage tissue and stem cells and cartilage cells in the cartilage tissue in the form of an integral material. The methylprednisolone delivery material degrades under the action of intracellular enzymes to release methylprednisolone, so that the bioavailability of the methylprednisolone is improved. The methylprednisolone delivery material provided by the invention has excellent tissue and cell compatibility, does not cause toxic or side effects, and has good biodegradability, and degradation products do not have toxicity. Besides, the material is simple to prepare, the using process is very simple, and articular cavity injection administration can be directly performed.

Description

technical field [0001] The invention relates to the field of biological materials, in particular to a methylprednisolone delivery material based on ε-polylysine, a preparation method and a kit thereof. Background technique [0002] Osteoarthritis is a chronic joint disease characterized by degeneration of articular cartilage and secondary bone hyperplasia, clinically manifested as joint pain and mobility impairment. According to statistics, the prevalence rate of osteoarthritis can reach 50% among people over 60 years old in my country, and 80% among people over 75 years old, and the disability rate of this disease can be as high as 53%. Researchers predict that the number of people suffering from osteoarthritis in the world is expected to continue to increase in the next few decades. At present, interventions for osteoarthritis are mainly aimed at relieving pain and restoring function, and there is no clinical drug for improving the pathological manifestations of arthritis...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/64A61K31/573A61P29/00A61P19/02A61P19/08
CPCA61K47/645A61K31/573A61P29/00A61P19/02A61P19/08
Inventor 郑宪友杨云龙林俊卿
Owner SHANGHAI SIXTH PEOPLES HOSPITAL
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