Medical composition loaded with nimustine and synergist thereof

A technology of composition and synergist, which is applied in the direction of drug combination, antineoplastic drugs, liquid delivery, etc., can solve problems such as unclear effects, and achieve the effects of facilitating drug injection, reducing toxicity, and reducing drug concentration

Inactive Publication Date: 2010-12-22
SHANDONG LANJIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the effect of ACNU on other tumors is unclear

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0138] Put 70 mg of polylactic acid (PLA) with a molecular weight of 20,000-40,000 as a pharmaceutical excipient into a container, add 100 ml of organic solvent dichloromethane to dissolve and mix well, add 10 mg of nimustine and 20 mg of melphalan, and re-shake Dry in vacuo to remove the organic solvent. Shake again and dry in vacuo to remove the organic solvent. The dried drug-containing solid composition was frozen and pulverized to make a micropowder containing 10% nimustine and 20% melphalan, and then suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding Suspension-type sustained-release injection with a viscosity of 480cp-560cp (at 25°C-30°C). The subcutaneous release time is 35-45 days.

Embodiment 2

[0140] Put 75 mg of polylactic acid (PLA) with a molecular weight of 30,000-50,000 as a pharmaceutical excipient into a container, add 100 ml of organic solvent dichloromethane to dissolve and mix well, add 10 mg of nimustine and 15 mg of melphalan, and re-shake Dry in vacuo to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and then sterilized by radiation to obtain an anticancer in vivo implant for treating solid tumors with 10 mg of nimustine and 15 mg of melphalan. The subcutaneous release time is 40-45 days.

Embodiment 3

[0142] Put 80 mg of polylactic acid (PLA) with a molecular weight of 25,000-40,000 as a pharmaceutical excipient into a container, add 100 ml of organic solvent dichloromethane to dissolve and mix well, add 5 mg of nimustine and 15 mg of melphalan, and re-shake Dry in vacuo to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain an anticancer in vivo implant containing 5% nimustine and 15% melphalan for treating solid tumors. The subcutaneous release time is 30-40 days.

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PUM

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Abstract

The invention relates to a drug combination, namely, a slow-release injection, carrying nimustine and a synergistic agent thereof at the same time, which consists of slow-release accessories and active anti-cancer ingredients. The active anti-cancer ingredients comprise the nimustine and the synergistic agent thereof (vinorelbine, melphalan or mitomycin C) respectively. The viscosity of the slow-release injection is 10cp to 650cp (at the temperature of 20 DEG C to 30 DEG C). The active anti-cancer ingredients can also be prepared into a slow-release implant. The slow-release accessories are mainly biological soluble and degradable macromolecular polymerizers that can be absorbed. During the process of degradation and adsorption, the macromolecular polymerizers can slowly release the active anti-cancer ingredients to parts of tumors, thus obviously reducing the toxic reaction of the whole body as well as maintaining the concentration of effective drugs at the parts of the tumors. Putting the anti-cancer drug combination at the parts of the tumors can not only reduce the toxic reaction of the whole body active against cancer, but also selectively raise the drug concentration of the parts of the tumors and enhance the curative effect of nonspecific treatment, such as chemotherapy drugs and radiotherapy treatment, and the like. Solid tumors include glioma, osteoma sarcomatosum, lymphoma, lung cancer, intestinal cancer, oophoroma, and the like.

Description

(1) Technical field [0001] The invention relates to a pharmaceutical composition loaded with nimustine and its synergist, belonging to the technical field of medicines. Mainly sustained-release injections and sustained-release implants. (2) Background technology [0002] Although the research on cancer has made great progress, its mortality rate is still in the forefront of various common causes of death. In my country, about 1.6 million people suffer from cancer every year, and nearly 1.3 million people die of cancer, accounting for one-fifth of the total death toll. The incidence of cancer is increasing year by year and tends to be younger. Statistics show that in less than 20 years, the incidence of cancer in my country has increased by 69%, and the mortality rate has increased by 29.4%. According to the latest statistics from the World Health Organization, the global cancer incidence rate will increase by 50% by 2020, and the number of patients will increase to 15 mill...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/505A61K47/34A61K31/407A61K9/10A61P35/00
Inventor 刘恩祥孔庆忠邹会凤贺润平
Owner SHANDONG LANJIN PHARMA
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