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Norcantharidin derivative lipid microsphere injection and preparation method thereof

A technology of norcantharidin and lipid microspheres, applied in the field of medicine, can solve the problems of low drug loading and easy leakage of norcantharidin, achieve good chemical and physical stability, reduce toxic and side effects, and drug loading improved effect

Inactive Publication Date: 2015-04-01
辽宁正鑫药物研究有限公司
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0014] Purpose of the invention: the present invention provides a lipid microsphere injection of norcantharidin derivatives and a preparation method thereof, the purpose of which is to solve the problem of low drug loading of norcantharidin and easy leakage during sterilization and storage , reduce its toxicity and improve its efficacy

Method used

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  • Norcantharidin derivative lipid microsphere injection and preparation method thereof
  • Norcantharidin derivative lipid microsphere injection and preparation method thereof
  • Norcantharidin derivative lipid microsphere injection and preparation method thereof

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Embodiment approach

[0044] The main idea of ​​the present invention is to provide a lipid microsphere injection (composition of oil-in-water emulsion) containing N-alkyl derivative of norcantharidin imide, and provide a preparation method. The purpose is to reduce the irritation of the drug to blood vessels, prolong the action time of the drug in the body, and reduce its nephrotoxicity. At the same time, the lipid solubility of the derivative is used to solve the drug encapsulation caused by the high water solubility of sodium norcantharidate lipid microspheres. The rate is not high and the leakage problem.

[0045] The injection comprises: N-alkyl derivative of norcantharidinimide, fat-soluble medium, water and surfactant.

[0046] The formula of the present invention consists of: (in preparation mass),

[0047] Oil phase 5%~30%;

[0048] Norcantharidin imide N-alkyl derivatives 0.001%~5% (calculated as norcantharidin);

[0049] Surfactant 0.5%~7%;

[0050] Osmotic pressure regulator 1.0%~5%...

Embodiment 1

[0073] Example 1 The preparation process of the prescription of N-alkyl derivatives of norcantharidin imide (n=8-12) lipid microsphere injection.

[0074] The norcantharidin imide N-alkyl derivative R used in embodiment 1 is C 8-12 Saturated straight chain alkanes.

[0075] 【Prescription 1】Specification: 0.1mg / 10ml (calculated as norcantharidin)

[0076]

[0077]

[0078] Preparation method 1:

[0079](1) Glycerin for injection, polysorbate-80, EDTA, and sodium oleate are dispersed in an appropriate amount of water for injection, heated to 30-80°C in a magnetic stirrer, and stirred until completely dissolved, as the water phase;

[0080] (2) dissolving the norcantharidin amine derivatives of the prescription amount in the Brucea javanica oil for injection containing lecithin, putting in a magnetic stirrer and heating to 30-80° C. to mix uniformly, as the oil phase;

[0081] (3) Under stirring by a high-speed tissue disperser, add the water phase to the oil phase, firs...

Embodiment 2

[0103] Example 2 Preparation process of the prescription of norcantharidin imide N-alkyl derivatives (n=13-18) lipid microsphere injection

[0104] The norcantharidin imide N-alkyl derivative R used in embodiment 2 is selected from C 13-18 Saturated straight chain alkanes.

[0105] 【Prescription 4】Specification: 0.1mg / 10ml (calculated as norcantharidin)

[0106]

[0107] Preparation method 1:

[0108] (1) Disperse glycerin for injection, poloxamer 188, and EDTA in an appropriate amount of water for injection, heat to 30-80°C in a magnetic stirrer, and stir until completely dissolved, as the water phase;

[0109] (2) The norcantharidinimide N-alkyl derivative of prescription quantity and be dissolved in the safflower oil for injection containing lecithin and oleic acid, put in magnetic stirrer and be heated to 30-80 ℃ to Mix well, as the oil phase;

[0110] (3) Under stirring by a high-speed tissue disperser, add the water phase to the oil phase, first slowly and then qu...

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Abstract

The invention relates to norcantharidin derivative lipid microsphere injection and a preparation method thereof. The injection contains norcantharidin imide derivative, oil phase, water and surfactant; and the formula of the injection contains the following components by mass: 5 to 30 percent of oil phase, 0.001 to 1 percent of norcantharidin imide N-alkyl derivative, 0.5 to 7 percent of surfactant, 1 to 5 percent of osmotic pressure regulator, and the balance of injection water. Norcantharidin is connected with a long-chain saturated alkane group through amino, so that the lipid solubility of the injection is greatly improved, and the lipid solubility of the injection is improved together with increase of the chain length of the saturated alkane group. Lipid microspheres can carry medicaments with the granularity of more than 90 percent into lipid cores and (or) an interfacial film, so that the medicament loading capacity and the encapsulation efficiency are greatly improved, the vascular stimulation during injection is reduced, the physical and chemical stability of the medicaments and the lipid microsphere injection is improved, the in-vivo acting time of the medicaments is prolonged, the treatment effect is improved, and the toxic or side effect is reduced.

Description

[0001] Technical field: the present invention relates to a lipid microsphere of N-alkyl derivative of norcantharidinimide and a preparation method thereof, belonging to the technical field of medicine. Background technique: [0002] Malignant tumors, as one of the largest public health problems in the world, have greatly endangered human health and will become the number one killer of human beings in the new century. From a global perspective, there were 10.1 million new cancer cases and 6.2 million deaths in 2000, and 22.4 million cancer cases. In 2008, the number of cancer cases and deaths rose to 7.56 million. cases. At the same time, malignant tumors are no longer a serious disease in developed industrial countries, and developing countries are facing a greater disease burden. As a large developing country, our country is facing more and more serious situation of malignant tumors due to the problems of industrialization, urbanization and population aging. Therefore, the ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K31/407A61K47/44A61P35/00
Inventor 唐星蔡翠芳牛砚涛张宇
Owner 辽宁正鑫药物研究有限公司
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