Application of methotrexate and ABC inhibitor to preparation of medicament for treating psoriasis

A technology of methotrexate and inhibitors, which is applied in the field of external application in the treatment of psoriasis, and can solve the problems of large side effects of methotrexate

Active Publication Date: 2013-02-13
CENT SOUTH UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The curative effect of methotrexate in psoriasis is affirmative, and systemic application can relieve the condition in a short time, but the side effects of methotrexate are relatively large. Therefore, systemic methotrexate is generally not the first choice in the treatment of psoriasis

Method used

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  • Application of methotrexate and ABC inhibitor to preparation of medicament for treating psoriasis
  • Application of methotrexate and ABC inhibitor to preparation of medicament for treating psoriasis
  • Application of methotrexate and ABC inhibitor to preparation of medicament for treating psoriasis

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0014] Example 1 MRP-5 Inhibitor Research on MTX Efflux Inhibition

[0015] In this experiment, MRP-5 inhibitors were combined with MTX to study MRP-5 inhibitors blocking MRP-5-mediated MTX vesicular transport. The MRP-5 inhibitors used in this experiment are probenecid, MK571, triquinine, sildenafil, zaprinast, indomethacin, sulfinpyrazone, dipyridamole, pemetrexed , 5-FdUMP.

[0016] ABC transport pumps rely on ATP to uptake MTX and can be evaluated by membrane vesicle transport experiments. The membrane vesicles needed in this experiment can be obtained from HEK293 cells transfected with MRP-5.

[0017] The membrane vesicles were obtained by physically disrupting the cells under low temperature conditions. 20 μg of membrane vesicles were incubated with each inhibitor for 1 h on ice, and then incubated with 20 mM MgCl 2 , 4mM ATP or 4mM AMP-PNP, creatine phosphate and creatine kinase ATP buffer system. Add 100 μM [ 3 H]-MTX was incubated at 37°C for 10min. Add 3ml of st...

Embodiment 2A

[0019] Example 2 Study on the Inhibitory Effect of ABCG2 Inhibitors on MTX Efflux

[0020] The experiment combined ABCG2 inhibitors with MTX to study ABCG2 inhibitors blocking ABCG2-mediated MTX vesicular transport.

[0021] The inhibitory effect of tyrosine kinase inhibitors (TKIs) among ABCG2 inhibitors is particularly prominent. This experiment focuses on Nilotinib, Lapatinib, Erlotinib, and Sunitinib among tyrosine kinase inhibitors (TKIs), and FTC is used as a positive control.

[0022] In this experiment [ 3 The vesicle transport experiment of H]-MTX was determined by the method in Example 1. The membrane vesicles were incubated with various concentrations of inhibitors on ice for 1 h. Add 100 μM [ 3 H]-MTX was incubated at 37°C for 10min. Add 3ml of stop solution (0.25M sucrose, 100mM NaCl and 10mM Tris hydrochloride, pH7.5) to stop the reaction. Washing, inside the vesicle [ 3 H]-MTX was determined by liquid scintillation counting (Packard Instrument Company, Inc...

Embodiment 3

[0026] Embodiment 3 methotrexate gel

[0027] prescription composition

[0028] Ingredients Dosage

[0029] Methotrexate 500mg

[0030] Carbomer 1.0g

[0031] Triethanolamine 1.5g

[0032] DMSO 2ml

[0033] Distilled water up to 100g

[0034] Preparation

[0035] Soak the carbomer in water to make it fully swell, add glycerin, and drop triethanolamine to form a transparent gel. MTX is mixed with an appropriate amount of DMSO and then added to the gel, add water to a sufficient amount, and grind evenly.

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Abstract

The invention relates to application of an inhibitor combining methotrexate and ABC (ATP-binding cassette) to treatment of psoriasis. More specifically, the inhibitor combining the methotrexate and the ABC is applied in a local external use mode when used for treating the psoriasis.

Description

technical field [0001] The present invention relates to the medicinal approach of the medicine for treating psoriasis: specifically, the present invention relates to the external use of combined application of methotrexate and ABC inhibitor for treating psoriasis. Background technique [0002] Psoriasis is an immune abnormality disease under the background of polygenetic inheritance. Because of its high incidence and mainly affecting young adults, it has attracted much attention in the field of dermatology clinical and scientific research. Keratinocyte (KC) hyperproliferation, inflammatory cell infiltration, and neovascularization are the three elements of histopathology. Although there are very complex interactions and causal relationships between the three, it is generally believed that the accumulation and activation of T lymphocytes in the dermis Cells are the initiating factors for the occurrence of psoriatic lesions. Activated T cells can produce cells / chemokines such ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K45/00A61K31/519A61P17/06
Inventor 陈翔丁劲松匡叶红
Owner CENT SOUTH UNIV
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