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Slow-released injection containing methotrexate and its synergist

A slow-release injection, methotrexate technology, applied in the field of medicine, can solve the problems of many complications, easy generation of drug resistance, poor sensitivity of anticancer drug methotrexate, etc.

Inactive Publication Date: 2009-08-26
DASEN BIOLOGICAL PHARMA CO LTD
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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) at 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 of polyphenylpropane (p-CPP: sebacic acid (SA) at 20:80) copolymer into a container, add 100ml of dichloromethane, 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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PUM

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Abstract

The slow released anticancer injection containing methotrexate consists of slow released microballoon and solvent. The slow released microballoon includes effective anticancer component and slow releasing supplementary material, and the solvent is common solvent or special solvent containing suspending agent. The effective anticancer component is the composition of methotrexate and methotrexate synergist of platinum compound, topoisomerase inhibitor and / or tetrazine compound; the slow releasing supplementary material is PLA, PLGA, EVAc, etc or their composition; and the suspending agent is sodium carboxymethyl cellulose, etc for suspending the effective anticancer component or its slow released granule or microballoon to prepare slow released injection. Injecting the slow released preparation to local tumor part can lower the systematic toxic reaction of the medicine and raise the medicine concentration of local tumor part selectively to raise the treating effect.

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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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/10A61K45/00A61K47/32A61K47/34A61K47/38A61K31/5025A61P35/00A61K47/26
Inventor 孙中先
Owner DASEN BIOLOGICAL PHARMA CO LTD