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A kind of drug coating liquid for drug coating balloon, drug coating balloon

A technology of drug coating and coating liquid, applied in the directions of coatings, balloon catheters, catheters, etc., can solve the problems of inability to release paclitaxel, the disadvantage of rapid release, and the influence of blood vessel walls.

Active Publication Date: 2021-11-16
CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But the most fatal problem is that, as an excipient, shellac is slightly inferior in the critical step of quick release
During the short time when the balloon is in contact with the vessel wall, shellac cannot release a significant percentage of paclitaxel to the diseased vessel wall, but after the balloon is withdrawn, paclitaxel is wrapped in the blood flow and reaches the rest of the body to completely After the drug is released, it will not only reduce the absorption of the drug at the effective site, but also cause a certain systemic reaction of the drug, which will have a certain impact on the intact blood vessel wall

Method used

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  • A kind of drug coating liquid for drug coating balloon, drug coating balloon
  • A kind of drug coating liquid for drug coating balloon, drug coating balloon
  • A kind of drug coating liquid for drug coating balloon, drug coating balloon

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0081] Preparation of paclitaxel stock solution:

[0082] Use a 1.5 mL EP tube to weigh 6 mg of paclitaxel, add 400 μL of absolute ethanol to dissolve, vortex and sonicate until completely dissolved and clarified to obtain a paclitaxel stock solution with a concentration of 15 mg / mL, seal it with para film and store in a refrigerator at 4 °C.

[0083] Preparation of pectin colloid dispersion system:

[0084] Use a balance to weigh 1.9mg of powdered pectin for later use; take a 50mL eggplant bottle, in an oil bath at 40°C, under manual stirring, add the powdered pectin while adding water, the total volume of water added is 30mL, and finally add 72 μL of glycerol, and adjust the pH value to 7-7.5 with 2mol / L NaOH, stir well to form a light brown homogeneous liquid.

[0085] Pectin-RGDS-OCH 2 (CH 2 ) 6 CH 3 Preparation of colloidal dispersion system:

[0086] Add 19 mg of RGDS-OCH to the pectin colloidal dispersion system 2 (CH 2 ) 6 CH 3 Mix well to form a light brown ...

Embodiment 2

[0195] Preparation of paclitaxel stock solution:

[0196]Use a 1.5 mL EP tube to weigh 6 mg of paclitaxel, add 400 μL of absolute ethanol to dissolve, vortex and sonicate until completely dissolved and clarified to obtain a paclitaxel stock solution with a concentration of 15 mg / mL, seal it with para film and store in a refrigerator at 4 °C.

[0197] Preparation of pectin colloid dispersion system:

[0198] Use a balance to weigh 1.9mg of powdered pectin for later use; take a 50mL eggplant bottle, in an oil bath at 40°C, under manual stirring, add the powdered pectin while adding water, the total volume of water added is 30mL, and finally add 72 μL of glycerol, and adjust the pH value to 7-7.5 with 2mol / L NaOH, stir well to form a light brown homogeneous liquid.

[0199] Pectin-RGDS-OCH 2 (CH 2 ) 6 CH 3 Preparation of colloidal dispersion system:

[0200] Add 19 mg of RGDS-OCH to the pectin colloidal dispersion system 2 (CH 2 ) 6 CH 3 Mix well to form a light brown h...

Embodiment 3

[0206] Preparation of docetaxel stock solution:

[0207] Use a 1.5 mL EP tube to weigh 6 mg of docetaxel, add 400 μL of absolute ethanol to dissolve, vortex and sonicate until completely dissolved and clarified to obtain a stock solution of docetaxel with a concentration of 15 mg / mL, seal with para film and place in a 4 °C refrigerator save in .

[0208] Preparation of pectin colloid dispersion system:

[0209] Use a balance to weigh 1.9mg of powdered pectin for later use; take a 50mL eggplant bottle, in an oil bath at 40°C, under manual stirring, add the powdered pectin while adding water, the total volume of water added is 30mL, and finally add 72 μL of glycerol, and adjust the pH value to 7-7.5 with 2mol / L NaOH, stir well to form a light brown homogeneous liquid.

[0210] Pectin-RGDS-OCH 2 (CH 2 ) 6 CH 3 Preparation of colloidal dispersion system:

[0211] Add 19 mg of RGDS-OCH to the pectin colloidal dispersion system 2 (CH 2 ) 6 CH 3 Mix well to form a light br...

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Abstract

The invention provides a drug coating solution for a drug-coated balloon and a drug-coated balloon, which belong to the technical field of pharmacy. The drug coating liquid of the present invention uses pectin as the excipient of the drug coating balloon, and after being mixed with the active drug (paclitaxel or docetaxel), it helps the adhesion of the drug coating liquid to the blank balloon. When the drug-coated balloon reaches the lesion, pectin helps the active drug to be released from the surface of the balloon coating quickly and deposited on the surface of the blood vessel wall to reach an effective drug concentration. Arginine-glycine-aspartic acid (RGD) peptides are structural recognition motifs for cell surface integrins, including ανβ3 and α5β1, associated with the process of anchoring to the extracellular matrix. The present invention adds RGDS-OCH to the drug coating liquid 2 (CH 2 ) 6 CH 3 , can act as an integrin targeting vascular endothelial cells, enhance the absorption of active drugs, and reduce the loss of active drugs during delivery.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to a drug coating solution for a drug-coated balloon and a drug-coated balloon. Background technique [0002] With the increasing application of percutaneous transluminal coronary angioplasty (PTCA), many supporting equipment and technologies have also been continuously improved. Compared with stent implantation and second-generation drug-eluting The stent that has attracted much attention in recent years is the drug-coated balloon (DCB). DCB is an angioplasty balloon directly coated with an antiproliferatively active drug and an excipient (drug matrix or carrier) that facilitates the transfer of the drug to the lesion. The drug-coated balloon is delivered to the stenotic part of the blood vessel through the catheter, and the balloon inflates after inflation, and the drug coated on the surface of the balloon is released rapidly within a certain period of time. Paclitaxel cell cul...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61L29/08A61L29/16A61M25/10
CPCA61L29/08A61L29/085A61L29/16A61L2300/216A61L2300/416A61L2300/602A61M25/10A61M2025/105C08L5/06
Inventor 王玉记张启迪王彦明彭紫东阿依江冯琦琦
Owner CAPITAL UNIVERSITY OF MEDICAL SCIENCES
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