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Controlled release agent of containing fluorouracil and synergis

A technology of synergist and sustained-release injection, applied in the field of medicine, can solve the problems of poor curative effect, difficult operation, many complications, etc., and achieve the effects of reducing toxicity, facilitating drug injection, and reducing complications

Inactive Publication Date: 2007-05-09
SHANDONG LANJIN PHARMA +1
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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

[0136] 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 5-FU and 20 mg of anastrozole, re-shake and dry in vacuum Remove organic solvents. 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% 5-FU and 20% anastrozole, 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

[0138] 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 5-FU and 15 mg of pemetrexed, re-shake and vacuum Dry to remove organic solvent. The dried solid composition was shaped immediately, subpackaged and then sterilized by radiation to obtain an anti-cancer in vivo implant for treating solid tumors with 10 mg of 5-FU and 15 mg of pemetrexed. The subcutaneous release time is 40-45 days.

Embodiment 3

[0140] 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 5-FU and 15 mg of edoxifene, 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 5% 5-FU and 15% edoxifene for treating solid tumors. The subcutaneous release time is 30-40 days.

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Abstract

A slowly-release anticancer medicine in the form of injection or implant is disclosed. Said slowly-release injection is composed of a special solvent containing suspending aid and the slowly-release microballs consisting anticance medicine, iterstitial hydrolyte and slowly-releasing auxiliary. Said anticancer medicine is chosen from 5-FU, triptoreline, etc. Said interstitial hydrolyte is chosen from collagenase, relaxin, etc. Said slowly-releasing auxiliary is chosen from biocompatible, biodegradable and absorptive high-molecular polymers, polyethanediol, etc.

Description

(1) Technical field [0001] The invention relates to a sustained-release agent containing fluorouracil (5-FU) and its synergist and a preparation method thereof, belonging to the technical field of medicines. Sustained-release preparations are mainly sustained-release injections and sustained-release implants. (2) Background technology [0002] As a commonly used chemotherapeutic drug, 5-fluorouracil (5-FU) has been widely used in the treatment of various malignant tumors, and the effect is more obvious. However, its unexpected neurotoxicity greatly limits the application of this drug. Blood vessels, connective tissue, matrix proteins, fibrin, and collagen in the tumor stroma not only provide scaffolds and essential nutrients for the growth of tumor cells, but also affect the penetration of chemotherapy drugs around the tumor and in the tumor tissue and diffusion (see Netti et al. "The influence of the status of the extracellular matrix on the delivery of drugs in solid tum...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K31/513A61K45/06A61K47/34A61P35/00
Inventor 孔庆忠俞建江
Owner SHANDONG LANJIN PHARMA
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