Fluorouracil slow release injection

A technology of slow-release injections and slow-release excipients, applied in the field of medicine, can solve problems such as many complications, poor curative effect, and difficult operation

Inactive Publication Date: 2006-10-04
JINAN SHUAIHUA 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

[0104] Put 90, 90 and 80mg polyphenylene propane (p-carboxyphenylpropane (p-CPP): sebacic acid (SA) is 20: 80) copolymer into three containers of A, B and C respectively, and then each Add 100ml of dichloromethane to it, dissolve and mix well, then add 10mg5-FU, 10mg colchicine, 10mg5-FU and 10mg colchicine respectively, re-shake and use spray drying method to prepare 10% 5-FU, 10% colchicine and 10% 5-FU and 10% colchicine microspheres for injection. Then suspend the microspheres in physiological saline containing 15% mannitol to prepare the corresponding suspension-type sustained-release injection. 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

[0106] The method step of being processed into sustained-release injection is the same as in Example 1, but the difference is that the contained anticancer active ingredients and their weight percentages are:

[0107] (1) 5-30% 5-FU;

[0108] (2) 5-30% of Cytochalasin, Mitochloramine, Mitopradone, Mitoguanidine Hydrazone, Mitonaphthamide, Mitohydrazine, Mitoquinone, Mitospor, Mitotane , Mitophenamine, Mitozolomide, Mitoransone, Colchicine Salicylate, Colchicine, Colchicine, Cytochalasin, Naphthol, α-Naphthol, β-Naphthol, Naphthol alpha-phosphate, alcodazole, procodazole, arsenic, giraladazole, or nocodazole; or

[0109] (3) 5-30% of 5-FU and 5-30% of Cytochalasin, Mitoclomin, Mitorapone, Mitoguanidine Hydrazone, Mitonaphthamide, Mitohydrazine, Mitoquinone , Mitospex, Mitotane, Mitonamamine, Mitozolomide, Mitoransone, Colchicine Salicylate, Colchicine, Colcemid, Cytochalasin, Naphthol, Alpha - a combination of naphthol, beta-naphthol, alpha-naphthol phosphate, alcodazole, pr...

Embodiment 3

[0111] Put 70 mg of polylactic acid (PLGA, 75:25) with a peak molecular weight of 25,000 into three containers of A, B, and C, respectively, and then add 100 ml of methylene chloride to each, dissolve and mix well, and pour into the three containers respectively. Add 30mg5-FU, 30mg cyclophosphamide, 15mg5-FU and 15mg cyclophosphamide, re-shake and use spray drying method to prepare 30% 5-FU, 30% cyclophosphamide, 15% 5-FU and 15% Cyclophosphamide microspheres for injection. The dried microspheres are suspended in physiological saline containing 1.5% sodium carboxymethylcellulose to prepare the corresponding suspension-type sustained-release injection. 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.

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PUM

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Abstract

Disclosed is a 5-FU slow release injection comprising slow release microballoons and dissolvent, wherein the slow release microballoons include anti-cancer active constituent and slow release adjuvant, the dissolvent being common dissolvent or dissolvent containing suspending agent selected from sodium carboxymethylcellulose, mannitol, sorbitol, Tween-80 or their combination. The anticancer active constituent being 5-FU and / or 5-FU synergistic agent selected from antimitotic drugs and / or alkyl agent, the slow release adjuvant being selected from polylactic acid, ethylene-vinyl acetate copolymer, Polifeprosan, FAD and sebacic acid copolymer, polyglycolic acid and glycollic acid copolymer or their combination.

Description

(1) Technical field [0001] The invention relates to a sustained-release injection containing fluorouracil (5-FU) and a preparation method thereof, belonging to the technical field of medicines. (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, fibrinoproteins, and collagen in the tumor stroma not only provide scaffolds and essential nutrients for the growth of tumor cells, but also affect the diffusion of chemotherapy drugs around the tumor and in the tumor tissue. Infiltration and diffusion (see Netti et al. "The influence of the status of the extracellular matrix on the drug delivery in solid tumors" "Cancer Research" 60 pp. 2497-503 (2000) (Netti PA, Cancer Res.2000, 60 (9 ): 2497-503)). Due ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/513A61K9/16A61K45/00A61K47/34A61P35/00A61K47/26
Inventor 孔庆霞
Owner JINAN SHUAIHUA PHARMA TECH
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