Norcantharidin derivative lipid microsphere injection and preparation method thereof

A technology of norcantharidin and lipid microspheres, which is 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 improve curative effect Effect
CN102973503AInactive Publication Date: 2013-03-20辽宁正鑫药物研究有限公司
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
辽宁正鑫药物研究有限公司
Publication Date
2013-03-20
Estimated Expiration
Not applicable · inactive patent

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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.
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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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