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Ultrasonic contrast agent and preparation method and application thereof

An ultrasonic contrast agent and stabilizer technology, applied in the field of ultrasonic contrast agent and its preparation, can solve the problems such as the inability to load active ingredients, the shell of the contrast agent is hard, and the contrast effect is not good, and achieves structural stability, improved mechanical index, and flexibility. Good results

Pending Publication Date: 2019-02-22
广州康臣药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] The purpose of the present invention is to overcome the above-mentioned deficiencies of the prior art, and provide an ultrasonic contrast agent and its preparation method to solve the problem that the existing contrast agent, especially the ultrasonic microbubble contrast agent of polymer material, has a relatively hard shell and relatively elastic shell. Poor, weak cavitation effect, technical problems of poor imaging effect
[0010] Another object of the present invention is to provide a pharmaceutical preparation to solve the technical problem that the active ingredient of the existing pharmaceutical preparation cannot be loaded by a contrast agent

Method used

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  • Ultrasonic contrast agent and preparation method and application thereof
  • Ultrasonic contrast agent and preparation method and application thereof
  • Ultrasonic contrast agent and preparation method and application thereof

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preparation example Construction

[0039] On the other hand, on the basis of the ultrasound contrast agent described above, the embodiment of the present invention also provides a preparation method of the ultrasound contrast agent. The preparation method process of the ultrasound contrast agent is as follows: figure 1 As shown, it includes the following steps:

[0040] S01: Dissolving biodegradable polymers and lipids in organic solvents to prepare an oil phase;

[0041] S02: performing a first emulsification treatment on the oily phase prepared in step S01 with water or an aqueous solution containing a substance that is easily decomposed to generate gas, to obtain a water-in-oil primary emulsion;

[0042] S03: performing a second emulsification treatment on the primary emulsion prepared in step S02 and the water phase to obtain a water-in-oil-in-water double emulsion;

[0043] S04: The organic solvent contained in the double emulsion prepared in step S03 is removed, the precipitate is collected, and the pre...

Embodiment 1

[0060] The embodiment of the present invention provides a DPPC-PLA ultrasonic contrast agent and a preparation method thereof. The DPPC-PLA ultrasonic contrast agent is a hollow microbubble structure, wherein the shell of the hollow microbubble structure includes a mixture of DPPC-PLA, and the hollow cavity of the hollow microbubble structure is coated with ammonium bicarbonate.

[0061] The preparation method of described DPPC-PLA ultrasonic contrast agent:

[0062] S11: Dissolve 0.1g PLA (number average molecular weight: 10,000) and 2.0mg DPPC in 1mL dichloromethane to prepare an oil phase;

[0063] S12: Add 0.2ml of 6wt% ammonium bicarbonate aqueous solution to the oil phase, mix thoroughly, and ultrasonicate for 240 seconds at a power of 190W to obtain a water-in-oil primary emulsion;

[0064] S13: At a stirring speed of 30,000 rpm, drop the primary emulsion obtained above into an aqueous solution of 4wt% polyvinyl alcohol (number average molecular weight: 30,000), and st...

Embodiment 2

[0067] The embodiment of the present invention provides a DSPE-PLC ultrasonic contrast agent and a preparation method thereof. The DSPE-PLC ultrasonic contrast agent is a hollow microbubble structure, wherein the shell of the hollow microbubble structure includes a mixture of DSPE-PLC, and the hollow cavity of the hollow microbubble structure is coated with ammonium bicarbonate.

[0068] The preparation method of the DSPE-PLC ultrasonic contrast agent:

[0069] S21: Dissolve 0.15g PLC (number average molecular weight: 5,000) and 1.5mg DSPE in 2mL dichloromethane to prepare an oil phase;

[0070] S22: Add 0.2ml of 6wt% ammonium bicarbonate aqueous solution to the oil phase, mix thoroughly, and ultrasonicate for 300 seconds at a power of 150W to prepare a water-in-oil primary emulsion;

[0071] S23: At a stirring speed of 40,000 rpm, drop the above-obtained primary emulsion into an aqueous solution of 5 wt% polyvinyl alcohol (number average molecular weight: 70,000), and stir a...

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Abstract

The invention provides an ultrasonic contrast agent and a preparation method and a pharmaceutical preparation thereof. The ultrasonic contrast agent is of a hollow microbubble structure. The shell ofthe hollow microbubble structure comprises a biodegradable polymer and lipids, wherein the lipids modify the biodegradable polymer. The ultrasonic contrast agent is prepared by taking the biodegradable polymer and lipids as an oil phase, preparing an oil-in-water-in-oil compound emulsion and finally removing a solvent out of the compound emulsion. The pharmaceutical preparation takes the ultrasonic contrast agent as a drug carrier. The shell of the hollow microbubble structure of the ultrasonic contrast agent has good flexibility and elasticity, so that the ultrasonic contrast agent is endowedwith good ultrasonic responsiveness and ultrasonic contrast effect, is stable in structure, can carry out ultrasonic detonation, and is safe and non-toxic and good in safety. The preparation method of the ultrasonic contrast agent is easy to control process condition and mild in condition, and can ensure that the prepared ultrasonic contrast agent is stable in structure and performance, preparation efficiency is high, and the production cost is lowered.

Description

technical field [0001] The invention relates to the technical field of medical detection reagents, in particular to an ultrasonic contrast agent and its preparation method and application. Background technique [0002] In recent years, molecular imaging technology has attracted extensive attention because it can provide important information for the diagnosis and monitoring of diseases in living tissues. Among many imaging modes, ultrasound imaging, as a non-invasive biomedical imaging mode, has important research value due to its advantages of safe and timely imaging and diagnosis, low price, lightness and quickness, and wide application. [0003] As the most commonly used method in medical imaging diagnosis at present, ultrasonic diagnostic technology uses the difference in the strength of reflection and scattering signals of ultrasonic waves at the interface of human tissue to display the normal and abnormal information of the structure and function of internal tissues an...

Claims

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Application Information

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IPC IPC(8): A61K49/22A61K9/50A61K47/34A61K47/24A61K31/704
CPCA61K49/223A61K9/5015A61K9/5031A61K31/704
Inventor 严飞于博陈彦梁杨标
Owner 广州康臣药业有限公司
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