Slow-release anticarcinogen contg. carmustine and fluorouracil

A technology of carmustine and fluorouracil, which is applied in the field of anti-cancer sustained-release agents, can solve problems such as unclear effects, and achieve the effects of facilitating drug injection, reducing toxicity, and reducing drug concentration

Inactive Publication Date: 2007-07-18
SHANDONG LANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, the effect of ...

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0133] Put 90 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 carmustine, 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% carmustine by weight, and then suspending it in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension-type slow Release injection, the viscosity is 380cp-460cp (at 25°C-30°C). The subcutaneous release time is 30-35 days.

Embodiment 2

[0135] Put 75 mg of polylactic acid (PLGA, 50:50) with a molecular weight of 30,000-50,000 pharmaceutical excipients into a container, add 100 ml of organic solvent dichloromethane to dissolve and mix, add 25 mg of carmustine, re-shake and vacuum Dry to remove 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 carmustine for treating solid tumors. The subcutaneous release time is 35-40 days.

Embodiment 3

[0137] Put 90 mg of pharmaceutical excipient polyphenylpropane (p-carboxyphenylpropane: sebacic acid weight ratio is 50:50) into the container, add 100 ml of organic solvent dichloromethane to dissolve and mix, add 10 mg of carmustine , shake again and 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 containing 10% carmustine by weight for treating solid tumors. The subcutaneous release time is 15-20 days.

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Abstract

A slow-release anticancer medicine in the form of injection or implant contains carmustine and its synergist chosen from 5-FU, cisplatin and 06-benzylguanine. For said slow-release injection, it is composed of the slow-release microballs containing the active anticancer component and slow-releasing auxiliary and the special solvent containing suspending aid.

Description

(1) Technical field [0001] The invention relates to an anticancer slow-release agent loaded with carmustine and fluorouracil, 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 ...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/513A61K31/17A61K31/52A61K31/282A61K31/555A61K47/34A61P35/00
Inventor 孔庆忠张红军
Owner SHANDONG LANJIN PHARMA
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