Preparation method of calcium phosphate-rapamycin compound drug, preparation method of drug-coated balloon, and drug-coated balloon

A technology of rapamycin and drug coating, which is applied in the field of preparation of calcium phosphate-rapamycin composite drug, can solve the limitation of clinical pharmacological application and biological effect of rapamycin drug-coated balloon, rapamycin The problem of low lipophilicity of rapamycin and difficulty in adhering to the surface of the balloon can be solved to achieve the effect of prolonging the penetration ability of rapamycin in tissues, increasing the solubility and stability, and improving the adhesion ability

Active Publication Date: 2022-03-22
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to (1) rapamycin’s low lipophilicity and (2) slow tissue absorption, it is difficult to adhere to the surface of the balloon, and it is difficult to use it as a coating drug
In addition, (3) the drug-coated balloon has a short residence time and is usually eluted within minutes to hours of administration. These deficiencies will greatly limit the clinical pharmacological application and The play of biological effects

Method used

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  • Preparation method of calcium phosphate-rapamycin compound drug, preparation method of drug-coated balloon, and drug-coated balloon
  • Preparation method of calcium phosphate-rapamycin compound drug, preparation method of drug-coated balloon, and drug-coated balloon
  • Preparation method of calcium phosphate-rapamycin compound drug, preparation method of drug-coated balloon, and drug-coated balloon

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Experimental program
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Effect test

Embodiment 1

[0054] A preparation method of calcium phosphate-rapamycin compound medicine of the present invention, comprises the following steps:

[0055] Step S1: adding rapamycin to DMEM culture solution so that the rapamycin content in the mixture of rapamycin and DMEM culture solution is 100 nmol / L, and fully equilibrating for 24 hours.

[0056] Step S2: Add 110 μL of CaCl with a concentration of 1 mol / L to the fully equilibrated solution in Step S1 2 A mineralization reaction is initiated to obtain a nanoparticle suspension. The entire reaction is performed in a cell culture environment. The reaction temperature was 37°C. Response environment CO 2 The content is 5%. Sodium citrate was added 0.5 hours after the reaction to terminate the reaction to control the size of nanoparticles in the nanoparticle suspension.

[0057] Implementation two:

[0058] A preparation method of calcium phosphate-rapamycin compound medicine of the present invention, comprises the following steps:

...

Embodiment 3

[0062] A preparation method of calcium phosphate-rapamycin compound medicine of the present invention, comprises the following steps:

[0063] Step S1: Add rapamycin to DMEM culture medium, so that the content of rapamycin in the mixture of rapamycin and DMEM culture medium is 102 nmol / L, and fully equilibrate for 28 hours.

[0064] Step S2: Add 200 μL of CaCl with a concentration of 1 mol / L to the fully equilibrated solution in Step S1 2 A mineralization reaction is initiated to obtain a nanoparticle suspension. The entire reaction is performed in a cell culture environment. The reaction temperature was 39°C. Response environment CO 2 The content is 6%. Two hours after the reaction, sodium citrate was added to terminate the reaction to control the size of nanoparticles in the nanoparticle suspension.

Embodiment 4

[0066] A method for preparing a calcium phosphate-rapamycin composite drug-coated balloon of the present invention comprises the following steps:

[0067] Step (1): Take the calcium phosphate-rapamycin nanoparticle suspension prepared by any one of the calcium phosphate-rapamycin composite drug preparation methods above.

[0068] Step (2): coating the calcium phosphate-rapamycin composite drug coating on the surface of the balloon by ultrasonic spraying.

[0069] The ultrasonic spraying method includes the following steps:

[0070] a) The calcium phosphate-rapamycin nanoparticle suspension is placed in a syringe pump and sprayed onto the surface of the balloon through an ultrasonic nozzle. The nanoparticle suspension passed through the ultrasonic nozzle at a speed of 0.08 mL / min. Ultrasonic output power is 1.5W. Ultrasonic frequency is 30kHz.

[0071] b) Vacuum drying at 37°C for 2 hours after spraying. The drying environment is a vacuum environment.

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Abstract

The invention discloses a method for preparing a calcium phosphate-rapamycin compound drug, a method for making a drug-coated balloon and a drug-coated balloon. The stability of the structure of rapamycin is conducive to its sustained release in the body, improving the adhesion ability of rapamycin on the balloon surface, the penetration ability of rapamycin in tissues and prolonging the residence time of the drug after administration, and improving its effect on cells. Inhibitory effect, thereby enhancing the therapeutic effect of rapamycin on vascular restenosis, the nanomaterial coating can increase the solubility and stability of the drug, thereby reducing the dosage of the drug, reducing or avoiding toxic and side effects; the slowing down of nanoparticles The release effect can eliminate the "peak-valley" phenomenon of blood drug concentration, maintain a certain therapeutic concentration, and effectively prevent adverse reactions caused by instantaneously high blood drug concentration; nanoparticles can prolong the residence time of drugs in the circulatory system and improve drug retention. level of treatment.

Description

【Technical field】 [0001] The invention relates to the technical field of pharmacy, in particular to the preparation method of calcium phosphate-rapamycin composite drug, the preparation method of drug-coated balloon and the technical field of drug-coated balloon. 【Background technique】 [0002] Cardiovascular disease (CVD) has become the number one killer threatening human health. According to the "China Cardiovascular Disease Report 2018", it is currently estimated that there are 290 million CVD patients in my country, and cardiovascular disease deaths account for more than 40% of the disease deaths among Chinese residents. Studies have shown that the number of patients with cardiovascular diseases in my country will continue to increase rapidly in the next 10 years, and the burden of cardiovascular diseases will increase day by day, which has become a major public health problem. Percutaneous coronary stenting (PTCA) has the characteristics of less trauma, less bleeding, ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K33/42A61K31/436A61P9/10A61L29/08A61L29/10A61L29/16A61M25/10
CPCA61K33/42A61K31/436A61P9/10A61L29/08A61L29/106A61L29/16A61M25/1029A61L2400/12A61L2400/18A61L2420/02A61L2420/04A61L2300/606A61L2300/602A61L2300/416A61M2025/1031A61M2025/105A61K2300/00
Inventor 傅国胜肖云林骏赵炎波
Owner ZHEJIANG UNIV
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