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Nimustine slow release injection for treating extracranial noumenal tumour

A technology of slow-release injections and slow-release implants, which is applied in the direction of anti-tumor drugs, liquid delivery, emulsion delivery, etc., and can solve problems such as poor curative effect, many complications, and difficult operation

Inactive Publication Date: 2007-02-28
JINAN KANGQUAN PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, solid sustained-release implants (Chinese Patent No. ZL96115937.5; ZL97107076.8) and existing sustained-release microspheres for the treatment of brain tumors (ZL00809160.9) or U.S. Patent (US5,651,986) all have inadequacies. Easy operation, poor curative effect, many complications, etc.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0116] Put 90 mg of polylactic acid (PLA) with a molecular weight of 10,000 as a pharmaceutical excipient into a container, add 100 ml of organic solvent dichloromethane to dissolve and mix, add 10 mg of nimustine, re-shake, and then vacuum dry to remove the organic solvent. Shake again and dry in vacuo to remove the organic solvent. Freezing and pulverizing the dried drug-containing solid composition to make a micropowder containing 10% by weight of nimustine, and then suspending in physiological saline containing 1.5% sodium carboxymethylcellulose to obtain the corresponding suspension type Sustained-release injection with a viscosity of 380cp-460cp (at 25°C-30°C). The subcutaneous release time is 30-35 days.

Embodiment 2

[0118] Put 75 mg of polylactic acid (PLA) with a molecular weight of 20,000 as a pharmaceutical excipient into a container, add 100 ml of organic solvent dichloromethane to dissolve and mix, add 25 mg of nimustine, re-shake, and then vacuum dry 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 containing 25% by weight of nimustine for treating extracranial solid tumors. The subcutaneous release time is 35-40 days.

Embodiment 3

[0120] Put 95 mg of polylactic acid (PLA) with a molecular weight of 40,000 as a pharmaceutical excipient into a container, add 100 ml of organic solvent dichloromethane to dissolve and mix, add 5 mg of nimustine, re-shake, and then vacuum dry 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 containing 5% by weight of nimustine for treating extracranial solid tumors. The subcutaneous release time is 30-40 days.

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Abstract

Disclosed is a Nimustine slow release injection for treating extracranial solid tumours, which comprises effective anticancer dose of Nimustine or the combination of Nimustine and its synergists (such as 5-FU, cisplatin or 06-benzyl guanine). The viscosity of the slow release injection is 10-650cp (at 20-30 deg C), and the active anticancer constituents can also be made into slow release implanting agent. The slow release subsidiary materials mainly comprise bio-compactable and degradable macromolecular polymers, when locally dispensed on the tumor, the composition not only can lower down the whole body toxicity reaction of the anti-cancer medicament, but also can selectively increase the tumor local medicinal concentration, the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation can also be improved.

Description

(1) Technical field [0001] The invention relates to a nimustine sustained-release injection for treating extracranial solid tumors, and belongs 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 increas...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/505A61K47/34A61K31/513A61K31/282A61K31/52A61P35/00A61K47/38
Inventor 孔庆忠孙娟俞建江
Owner JINAN KANGQUAN PHARMA TECH
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