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Anti-cancer sustained-released agent

A slow-release agent and sustained-release injection technology, which is applied in the direction of antineoplastic drugs, medical preparations of non-active ingredients, peptide/protein components, etc., can solve the problem of treatment failure, enhanced resistance of anticancer drugs, and limit the effective diffusion of drugs and other issues to achieve the effect of promoting penetration and diffusion

Inactive Publication Date: 2009-04-01
SHANDONG LANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above factors greatly limit the effective diffusion of drugs into solid tumors and tumors, thus constituting the main obstacle to tumor chemotherapy.
[0007] Not only that, the blood vessels in the tumor stroma are not sensitive to conventional chemotherapy drugs, which often leads to the enhancement of tumor cell resistance to anticancer drugs, and the result is treatment failure

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0101] Example 1. Comparison of local drug concentration after different application of neovascularization inhibitor (marimastat)

[0102] Taking rats as the test object, 2×10 5 Prostate tumor cells were subcutaneously injected into their ribs, and they were divided into groups after the tumors grew to a diameter of 1 cm. The dose of each group was 5 mg / kg marimastat. The drug content (%) in the tumor was measured at different times, and the results showed that the local drug concentration of marimastat was significantly different after being applied in different ways, and local administration could significantly increase and effectively maintain the effective drug concentration at the tumor site. Internal slow-release implants and intratumoral slow-release injections work best. However, intratumoral injection of sustained-release injections is the most convenient and easy to operate. This finding constitutes an important feature of the present invention. The following rel...

Embodiment 2

[0103] Example 2. Comparison of in vivo anti-tumor effect after different application of neovascularization inhibitor (fumagillin)

[0104] Taking rats as the test object, 2×10 5 A brain tumor cell was subcutaneously injected into its flank, and the tumors were divided into groups after the tumor grew to a diameter of 0.5 cm. The dose of each group was 10mg / kg fumagillin. On the 10th day after treatment, the tumor volume was measured, and the treatment effect was compared. The results showed that the tumor-inhibiting effect of fumagillin was significantly different after being applied in different ways. Local administration can significantly increase and effectively maintain the effective drug concentration at the tumor site. Delayed-release injections work best. However, intratumoral injection of sustained-release injections is the most convenient and easy to operate. Not only the curative effect is good, but also the side effects are small.

Embodiment 3

[0105] Embodiment 3, anti-tumor effect in vivo of neovascularization inhibitor and proteolytic enzyme (sustained-release injection)

[0106] Taking rats as the test object, 2×10 5 Pancreatic cancer tumor cells were subcutaneously injected into the ribs, and after 14 days of tumor growth, they were divided into the following 10 groups (see Table 1). The first group is the control group, and the 2nd to 10th groups are the treatment groups, and the drugs are injected into the tumor. The dose of neovascularization inhibitor was 7.5mg / kg, and the proteolytic enzyme was 2.5mg / kg. On the 20th day after treatment, the tumor volume was measured, and the treatment effects were compared (see Table 1).

[0107] Table 1

[0108] Test group (n) received treatment Tumor volume (cm 3 ) P value 1(6) control 62±10 2(6) proteolytic enzyme 40±5.0 <0.05

[0109] The above results show that neovascularization inhibitors (marimastat, fumagillin, SU5416, SU6668) an...

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Abstract

The invention relates to an anti-cancer sustained release injection, consisting of sustained release microspheres and menstruum, wherein, the sustained release microspheres comprise sustained release auxiliary material, angiogenesis inhibitor and / or proteolytic enzyme; and the menstruum contains suspending agent. The angiogenesis inhibitor is selected from gefitinib, erlotinib, lapatinib, vatalanib, pelitinib, endostatin, imatinib, semaxanib, dasatinib, avastin, sorafenib, sunitinib, telcyta or panitumumab; the proteolytic enzyme is selected from one or the combination of collagenase, hyaluronidase, relaxin and plasmase; the sustained release auxiliary material is selected from polifeprosan, decanedioic acid copolymer, EVAc, polylactic acid, the mixture or the copolymer thereof, and the like; and the suspending agent is selected from carboxymethyl cellulose and the like with the viscosity of 100cp to 3000cp (under the temperature of 25 DEG C to 30 DEG C). The injection can also be made into a sustained release implant. The sustained release injection is injected or arranged in or around the tumour and can improve the local drug concentration selectively, reduce the general reaction of the drug, inhibit the growth of tumour cell and blood vessel and enhance the treatment effect of non-operative treatments, such as radiotherapy, chemotherapy, etc.

Description

(1) Technical field [0001] The invention relates to an anticancer sustained-release agent, which belongs to the technical field of medicines. More specifically, it is an anti-solid tumor sustained-release agent, mainly sustained-release implants and injections. The anti-solid tumor slow-release agent can effectively inhibit or destroy tumor blood vessels and can inhibit tumor neovascularization; the anti-solid tumor slow-release implant also involves effectively reducing tension, interstitial pressure, and interstitial viscosity in the tumor, In turn, the conductivity of the interstitial fluid can be improved, which is conducive to the effective diffusion of drugs into solid tumors and in tumors. (2) Background technology [0002] Cancer treatment mainly includes surgery, radiotherapy and chemotherapy. Among them, surgical treatment cannot remove scattered tumor cells, so it often recurs or causes tumor cells to spread and metastasize due to surgical stimulation; radiother...

Claims

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Application Information

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IPC IPC(8): A61K9/10A61K38/43A61K47/34A61K47/30A61P35/00
Inventor 孔庆忠贺润平
Owner SHANDONG LANJIN PHARMA
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