Marseilledinun sustained-release implantation agent for curing entity tumour

A slow-release implant, masitinib technology, applied in the field of medicine, can solve problems such as unclear effects, systemic side effects that limit clinical application, etc.

Inactive Publication Date: 2008-05-21
SHANDONG LANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In vitro studies have shown that masitinib can inhibit vascular endothelial growth, however, the effect of monotherapy in other tumors is unclear
Although the combinati

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] Put 80 mg of sustained-release excipients (polylactic acid (PLA) with a molecular weight of 15,000-30,000) into a container, add a certain amount of organic solvent to dissolve and mix (subject to full dissolution), add 20 mg of masitinib, and re-shake After homogenization, the organic solvent was removed by vacuum drying. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a sustained-release implant containing 20% ​​masitinib. The release time of the sustained-release implant in physiological saline in vitro is 22-26 days, and the release time in mouse subcutaneous is 20-26 days.

Embodiment 2

[0079] Sustained-release implants were made according to the method described in Example 1, but the anti-cancer active ingredients contained were one of the following:

[0080] (A) 1% masitinib and 99% polylactic acid;

[0081] (B) 5% masitinib and 95% polylactic acid;

[0082] (C) 10% masitinib and 90% polylactic acid;

[0083] (D) 15% masitinib and 85% polylactic acid;

[0084] (E) 20% masitinib and 80% polylactic acid.

Embodiment 3

[0086] Put 85mg of sustained-release excipients (PLGA with a molecular weight of 15000-25000, 50:50) into the container, add a certain amount of organic solvent to dissolve and mix (subject to complete dissolution), add 15mg of masitinib, and shake again Then dry in vacuo to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a sustained-release implant containing 15% masitinib. The release time of the slow-release implant in physiological saline in vitro is 25-32 days, and the release time in mouse subcutaneous is 23-28 days.

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PUM

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Abstract

The invention relates to a masitinib sustained-release implant for the treatment of solid tumors, which is characterized in that the sustained-release implant contains anti-cancer effective amount of masitinib, sustained-release excipient and certain amount of sustained-release regulator. The solid tumors include lung cancer, esophageal cancer, stomach cancer, liver cancer, breast cancer, ovariancancer, prostate cancer, bladder cancer and colorectal cancer. The sustained-release excipient mainly comprises one or the combination of the copolymer of glycolic acid and hydroxyacetic acid, polifeprosan, poly (L-lactide-co-ethyl phosphate) and poly (L-lactide-co-propyl phosphate). The invention can slowly release the masitinib in the local part of the tumor during the degradation and absorption process, so the invention can maintain the effective drug concentration at the local part of the tumor at the same time of significantly reducing systemic toxic reaction. The sustained-release implant is arranged at the local part of the tumor, which can not only reduce the systemic toxic reaction of masitinib, but can also selectively improve the drug concentration at the local part of the tumor and strengthen the treatment effects of chemotherapy drugs, radiation therapy and other non-surgical therapies.

Description

(1) Technical field [0001] The invention relates to a masitinib slow-release implant for treating solid tumors, belonging to the technical field of medicines. (2) Background technology [0002] Malignant solid tumors account for more than 70% of all malignant tumors. However, unlike non-solid tumors such as hematological and lymphoid tumors, it is difficult for conventional chemotherapy to obtain long-term effective drug concentrations in solid tumors. Although spread occurs during tumor growth, expansive growth is still the dominant growth pattern in most malignant solid tumors. As a result, tissue pressures within tumors are significantly higher than in normal tissues. Not only that, the vascular disorder and intermittent blood flow caused by tumor growth often lead to the distribution of systemic chemotherapy drugs in other normal tissues and organs, and rarely enter solid tumors. Low concentrations of drugs not only cannot effectively kill cancer cells, but also promot...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/496A61K47/34A61P35/00
Inventor 孔庆忠刘玉燕
Owner SHANDONG LANJIN PHARMA
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