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Sustained-release injection containing methotrexate and synergist thereof

A technology for sustained-release injection and methotrexate, which is applied in the field of sustained-release injection and its preparation, and anti-cancer drug sustained-release preparation, can solve the problems of easy generation of drug resistance, poor sensitivity of anti-cancer drug methotrexate, and difficult operation.

Inactive Publication Date: 2009-04-01
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; ZL97107077.6) 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.
In addition, many solid tumors are less sensitive to anticancer drugs, including methotrexate, and are prone to drug resistance during treatment

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0106] Put 70mg of polyphenylpropane (p-CPP: sebacic acid (SA) 20:80) copolymer into a container, add 100ml of dichloromethane, dissolve and mix well, then add 20mg Methotrexate and 10 mg of cisplatin were re-shaken and spray-dried to prepare microspheres for injection containing 20% ​​methotrexate and 10% cisplatin. Then suspend the microspheres in physiological saline containing 1.5% sodium carboxymethylcellulose and 0.5% Tween 80 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

[0108] 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 are:

[0109] (1) 5-30% methotrexate; or

[0110] (2) Combination of 2-40% methotrexate and 1-30% cisplatin, carboplatin, omaplatin, dexomaplatin, heptaplatin, lobaplatin, nedaplatin or oxaliplatin.

Embodiment 3

[0112] Put 80mg polyphenylene propane (p-CPP: sebacic acid (SA) 20:80) copolymer into a container, add 100ml methylene chloride, dissolve and mix well, then add 10mg Methotrexate and 10 mg camptothecin were re-shaken and spray-dried to prepare microspheres for injection containing 10% methotrexate and 10% camptothecin. 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 15-25 days, and the drug release time in mice subcutaneous is about 30-40 days.

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Abstract

The invention relates to a sustained release injection containing methotrexate, consisting of sustained release microspheres and menstruum, wherein, the sustained release microspheres comprise effective anti-cancer component and sustained release auxiliary material; and the menstruum is ordinary menstruum or special menstruum containing suspending agent. The effective anti-cancer component is the combination of the methotrexate and the methotrexate synergist selected from platinum compound, topoisomerase inhibitor and / or tetrazine compound. The sustained release auxiliary material is selected from one or the combination of the copolymer of polylactic acid, polyglycolic acid and glycolic acid, ethylene vinyl acetate copolymer and the copolymer of polifeprosan, FAD and decanedioic acid. The suspending agent is selected from carboxymethyl cellulose, etc. The suspending agent is used for suspending the effective anti-cancer component or sustained release particle or microsphere containing the effective anti-cancer component, so as to be made into the sustained release injection. The sustained release injection is injected into tumor, which can not only reduce the general toxic reaction of the drug, but also improve the partial drug concentration at the tumour selectively and enhance the treatment effect of non-operative treatments, such as chemotherapeutic drug, radiotherapy, etc.

Description

(1) Technical field [0001] The invention relates to a slow-release injection containing methotrexate and its synergist and a preparation method thereof, belonging to the technical field of medicines. Specifically, the present invention provides a slow-release anticancer drug containing methotrexate and its synergist. (2) Background technology [0002] As a commonly used chemotherapeutic drug, methotrexate (Methotrexate, MTX) has been widely used in the treatment of various malignant tumors, and the effect is relatively 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 extracellula...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/08A61K31/519A61K45/00A61K47/30A61P35/00
Inventor 孙中先
Owner JINAN SHUAIHUA PHARMA TECH
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