Sustained release agent containing fluorouracil and synergist thereof

A technology of fluorouracil and synergist, which is applied in the field of slow-release preparations of fluorouracil and its synergist and its preparation, can solve the problems of poor curative effect, many complications, and difficult operation, so as to reduce toxicity, reduce complications, The effect of facilitating drug injection

Inactive Publication Date: 2007-05-30
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

[0115] Put 70mg polyphenylene propane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) 20:80) copolymer into the container respectively, then add 100 ml of dichloromethane, dissolve and mix well, then add 15mg of 5-FU and 15mg of docetaxel were re-shaken and spray-dried to prepare microspheres for injection containing 15% of 5-FU and 15% of docetaxel. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection with a viscosity of 360cp-480cp (at 25°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 10-15 days, and the drug release time in mice subcutaneous is about 20-30 days.

Embodiment 2

[0117] Put 80mg of polyphenylpropane (p-CPP: 50:50 of sebacic acid (SA)) copolymer into the container respectively, then add 100ml of dichloromethane, dissolve and mix well, then add 5mg of 5-FU and 15mg of docetaxel were re-shaken and spray-dried to prepare microspheres for injection containing 5% of 5-FU and 15% of docetaxel. Then suspend the microspheres in physiological saline containing 1.5% carboxymethylcellulose sodium to prepare the corresponding suspension-type sustained-release injection with a viscosity of 380cp-460cp (at 25°C-30°C). The drug release time of the sustained release injection in physiological saline in vitro is 14-20 days, and the drug release time in mice subcutaneous is about 25-35 days.

Embodiment 3

[0119] The method steps for processing into sustained-release injections are the same as in Example 2, but the difference is that the anti-cancer active ingredients and their weight percentages are: 15% of 5-FU and 5% of docetaxel, suspension-type slow-release injections The viscosity of the release injection is 420cp-520cp (at 25°C-30°C). The drug release time of the slow-release injection in physiological saline in vitro is 15-25 days, and the drug release time in mice subcutaneous is about 25-35 days.

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Abstract

Disclosed is an anticancer slow release injection containing fluorouracil and synergistic agents, which comprises slow release micro-balloons and dissolvent, wherein the slow release microballoons comprise anti-cancer active constituents and slow release auxiliary materials, the dissolvent being specific dissolvent containing suspension adjuvant. The suspending agent is selected from sodium carboxymethylcellulose, mannitol, sorbitol, Tween-80 or their combination. The anticancer active constituents are the combination of 5-FU anddocetaxel, monohydric camptothecine, Etoposide as 5-FU synergistic agent. The slow release auxiliary materials are selected from polylactic acid, ethylene-vinylacetate copolymer, Polifeprosan, FAD, sebacic acid copolymer, polyglycolic acid and glycolic acid copolymer or their combination. The viscosity of the injection is 50-1000cp (at 20-30 deg C), The slow release microspheres can also be prepared into slow release implanting agent, when in-tumor or around-tumor injected or placed, the slow release agent can not only lower down the whole body toxicity reaction of the anti-cancer medicament, but also can selectively increase the tumor local medicinal concentration, and improve the treatment effect of the non-operative treatment methods such as chemotherapy, medicament and radiation.

Description

(1) Technical field [0001] The invention relates to a sustained-release agent of 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 tumors" "Ca...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/513A61K45/06A61K31/337A61K31/4745A61K31/7048A61K47/34A61P35/00A61K47/26A61K47/38
Inventor 孔庆忠苏红清
Owner SHANDONG LANJIN PHARMA
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