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Medicine-carrying polylactic acid microcapsular ultrasound contrast agent and preparation method thereof

An ultrasound contrast agent, polylactic acid technology, which is applied in echo/ultrasonic imaging agents, pharmaceutical formulations, antitumor drugs, etc., can solve the problem that the particle size and distribution of microbubble drug carriers are difficult to control, difficult to encapsulate drugs, and the amount of drugs is limited. and other problems, to achieve a good sustained release effect, uniform and controllable particle size, and the effect of reducing the dosage of drugs

Inactive Publication Date: 2009-08-12
XIAMEN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] At present, the preparation of ordinary microbubble ultrasound contrast agents mostly adopts the double emulsion solvent evaporation method, and the film-forming materials (protein, lipid, etc.) and the encapsulating gas (air, fluorocarbon gas, etc.) Emulsification, etc., it is difficult to wrap the drug into the microbubbles in the process of microbubble preparation, it is easy to cause the particle size and distribution of the prepared microbubble drug carrier to be difficult to control, the amount of medicine carried by the microbubbles is limited, and the repeatability is poor. It has a great impact on both basic and clinical application research, limiting the application

Method used

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  • Medicine-carrying polylactic acid microcapsular ultrasound contrast agent and preparation method thereof
  • Medicine-carrying polylactic acid microcapsular ultrasound contrast agent and preparation method thereof
  • Medicine-carrying polylactic acid microcapsular ultrasound contrast agent and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] Dissolve 40 mg of hydroxycamptothecin powder in 10 mL of NaOH solution with a pH of 9.0 to make a HCPT solution with a concentration of 4 mg / mL, and use it as the inner water phase for later use; dissolve 250 mg of PDLLA powder in 10 mL of dichloromethane, and add 0.1 mL of dichloromethane Disc-80, mix well, as the outer oil phase; take 1g of PVA and heat it with distilled water to fully dissolve it, set the volume to 100mL, and make a PVA aqueous solution with a concentration of 1.0%, as the outer water phase, for later use; under the action of ultrasound (100W·10S·10 ) times, take 1mL of the inner water phase and add it into 10mL of the outer oil phase at a constant speed with a syringe to prepare a stable primary emulsion.

[0025] Transfer the primary emulsion into the pressure chamber of the SPG micro-membrane emulsifier, select the SPG membrane with a pore size of 1.1 μm, adjust the high-purity nitrogen pressure to 40kPa, pass the primary emulsion into the 100mL ex...

Embodiment 2

[0027] Dissolve 50 mg of hydroxycamptothecin powder in 10 mL of NaOH solution with a pH of 9.0 to make a HCPT solution with a concentration of 5 mg / mL, and use it as the inner water phase for later use; dissolve 250 mg of PDLLA powder in 10 mL of dichloromethane, and add 0.2 mL of dichloromethane Pan-80, mix well, as the external oil phase; 2g PVA, fully dissolved by heating with distilled water, and make the volume to 100mL to make a PVA aqueous solution with a concentration of 2.0%; as the external water phase, for standby; under the action of ultrasound (100W·10S·8) Once, take 1mL of the inner water phase and add it into 10mL of the outer oil phase at a constant speed with a syringe to prepare a stable primary emulsion.

[0028]Transfer the primary emulsion into the pressure chamber of the SPG micro-membrane emulsifier, select the SPG membrane with a pore size of 1.3 μm, adjust the high-purity nitrogen pressure to 40kPa, pass the primary emulsion into the 100mL external wate...

Embodiment 3

[0030] Dissolve 40 mg of hydroxycamptothecin powder in 10 mL of NaOH solution at pH 9.0 to make a HCPT solution with a concentration of 4 mg / ml, which is used as the inner water phase for later use; 300 mg of PDLLA powder is dissolved in 10 mL of dichloromethane, and then add 0.2 mL of Span- 60, mix evenly, as the external oil phase; 3.6g PVA, fully dissolved by heating distilled water, set the volume to 90mL, and make a PVA aqueous solution with a concentration of 4.0%; as the external water phase, for use; under the action of ultrasound (80W·10S·10) times , Take 1mL of the inner water phase and add it into 10mL of the outer oil phase at a constant speed with a syringe to prepare a stable primary emulsion.

[0031] Transfer the primary emulsion into the pressure chamber of the SPG micro-membrane emulsifier, select the SPG membrane with a pore size of 1.1 μm, adjust the high-purity nitrogen pressure to 45kPa, pass the primary emulsion through the SPG micro-membrane into 90mL of...

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Abstract

The invention provides a drug-loading polylactic acid microvesicle ultrasound contrast agent and a preparation method thereof, relating to a new preparation of antineoplastic drug. Specifically, the invention provides a drug-loading polylactic acid microvesicle ultrasound contrast agent with noticeable antineoplastic effect and a preparation method thereof. The drug-loading polylactic acid microvesicle ultrasound contrast agent comprises an adventitia material, a main drug and charge gas; wherein, the adventitia material is polylactic acid, the main drug is 10-hydroxycamptothecine and the charge gas is perfluoropropane; wherein, concentration of bulk main drug is 3-5mg / mL; the concentration of the adventitia material is 0.025-0.030g / mL. Under ultra audible sound, internal water phase containing hydroxycamptothecine is added to methylene dichloride containing polylactic acid to prepare initial emulsion; the initial emulsion is dispersed to external water phase containing polyvinyl alcohol by a membrane emulsifier to form diphase emulsion; low velocity stirring by magnetic force at constant temperature is carried out overnight to facilitate oil phase to volatize; the polylactic acid is solidified into envelope; microvesicle precipitation is collected and then is washed, cooled and dried; perfluoropropane is used to charge drug-loading microvesicle samples, thus obtaining the drug-loading microvesicle ultrasound contrast agent.

Description

technical field [0001] The present invention relates to a new preparation of antineoplastic drugs, in particular to a drug-loaded (10-hydroxycamptothecin, HCPT for short) polylactic acid microbubble ultrasound contrast agent for positioning and targeted drug release by means of ultrasound and its preparation method. Background technique [0002] Cancer is one of the major diseases that threaten human health. The treatment of malignant tumors is still dominated by chemotherapy to a large extent. Hydroxycamptothecin (10-HCTP) is a broad-spectrum antineoplastic drug, but the side effects of this drug are relatively large, mainly manifested as bone marrow suppression, leukopenia, gastrointestinal reactions, and urinary tract irritation. At the same time, 10-HCPT is insoluble in water, and the water-soluble preparation used clinically is its sodium salt preparation, which destroys the α-hydroxylactone ring of its anti-topoisomerase I active structure and reduces the anti-tumor a...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K49/22A61K31/4745A61K47/34A61P35/00
Inventor 张其清朱佩娟周春晓盘捷侯振清
Owner XIAMEN UNIV
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