An anticancer sustained releasing agent

A slow-release agent and slow-release injection technology, which is applied in the direction of anti-tumor drugs, medical preparations of non-active ingredients, peptide/protein components, etc., can solve the problems of treatment failure, tumor chemotherapy obstacles, and limit the effective diffusion of drugs, etc., to achieve Effects that promote penetration and diffusion

Inactive Publication Date: 2007-05-16
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

[0102] Example 1. Comparison of local drug concentration after different application of neovascularization inhibitor (marimastat)

[0103] 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

[0104] Example 2. Comparison of in vivo anti-tumor effect after different application of neovascularization inhibitor (fumagillin)

[0105] 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

[0106] Embodiment 3, anti-tumor effect in vivo of neovascularization inhibitor and proteolytic enzyme (sustained-release injection)

[0107] 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).

[0108] Table 1

[0109] Test group (n)

[0110] The above results show that neovascularization inhibitors (marimastat, fumagillin, SU5416, SU6668) and proteolytic enzymes (collagenase) have obvious inhibitory effects on the growth of various tumor cells when applied alone at ...

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Abstract

Disclosed is an anti-cancer slow release agent comprising slow release microspheres and dissolvent, wherein the slow release microspheres include slow release auxiliary materials, anti-angiogenesis agent and / or proteolytic enzyme, the dissolvent comprises suspension adjuvant. The anti-angiogenesis agent is selected from gefinitib, erlotinib, lapatinib, pelitinib, endostatin, imatinib, smasnib, avastin, sorafenib, sunitinib, oersted or panitoma, the proteolytic enzyme is selected from collagenase, hyaluronidase, relaxin and thrombase or the combination of them, the slow release auxiliary materials are selected from Polifeprosan, sebacylic acid copolymer, EVAc, polylactic acid and their mixture of copolymer, the viscosity of the suspension adjuvant is 100-3000cp (at 25-30 deg C), and is selected from sodium carboxymethylcellulose. The agent can also be prepared into implanting agent for injection or placement in or around tumor with the effects of selectively increasing local concentration, lowering general reaction of the drugs, suppressing growth of tumor cells and blood vessel, and improving the treatment effect of the non-operative treatment methods such as chemotherapy.

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): A61K9/00A61K45/06A61K38/46A61K47/34A61P35/00A61K47/26
Inventor 孔庆忠贺润平
Owner SHANDONG LANJIN PHARMA
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