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Irinotecan sustained-release implant for treating solid tumor

A slow-release implant, irinotecan technology, applied in the field of medicine, can solve the problems of fast release and instability of sustained-release preparations

Inactive Publication Date: 2008-05-28
SHANDONG LANJIN PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the sustained-release preparations made by the existing methods release faster and unstable, so that they cannot bring into play their clinical effects well.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0065] Put the weighed (85 mg) sustained-release excipient (PLGA with a molecular weight of 15000-25000, 75:25) into the container, add a certain amount of organic solvent to dissolve and mix (subject to full dissolution), then add 10 mg of Iritinib Kang and 5mg mannitol, re-shake and vacuum-dry to remove organic solvents. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a slow-release implant containing 10% irinotecan. The release time of the sustained-release implant in physiological saline in vitro is 25-30 days, and the release time in mice subcutaneously is 26-32 days, without burst release.

Embodiment 2

[0067] 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:

[0068] (1) 1%-10% irinotecan and 90%-99% copolymer of glycolic acid and glycolic acid and 0.5%-15% sorbitol or mannitol;

[0069] (2) 10%-20% irinotecan and 80%-90% copolymer of glycolic acid and glycolic acid and 0.5%-10% sorbitol;

[0070] (3) 20%-30% irinotecan and 70%-80% copolymer of glycolic acid and glycolic acid and 0.5%-10% sodium chloride;

[0071] (4) 30%-40% irinotecan and 60%-70% copolymer of glycolic acid and glycolic acid and 0.25%-5% mannitol;

[0072] (5) 5% irinotecan and 93% copolymer of glycolic acid and glycolic acid and 2% sodium chloride;

[0073] (6) 10% irinotecan and 85% copolymer of glycolic acid and glycolic acid and 5% mannitol;

[0074] (7) 20% irinotecan and 75% copolymer of glycolic acid and glycolic acid and 5% mannitol;

[0075] (8) 30% irinotecan and 65% copolymer of glyc...

Embodiment 3

[0077] Put the weighed (80mg) sustained-release excipient (PLGA with a molecular weight of 20000-35000, 50:50) and 5mg of sodium chloride into the container, add a certain amount of organic solvent to dissolve and mix (subject to full dissolution) , add 15 mg of irinotecan, re-shake, and then vacuum-dry to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a slow-release implant containing 15% irinotecan. The release time of the sustained-release implant in physiological saline in vitro is 22-26 days, and the release time in mice subcutaneous is 22-28 days, without sudden release.

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PUM

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Abstract

An irinotecan sustained release implant includes effective dose of anticancer irinotecan, sustained release excipients and a certain quantity of sustained release moderator. Solid tumors include pancreatic cancer, lung cancer, liver cancer, breast cancer, cerebroma, ovarian cancer, prostatic carcinoma, esophageal carcinoma, lymphadenoma, osteosarcoma and colorectal cancer. Sustained release excipients are mainly one or combination of copolymer of glycolic acid and hydroxyacetic acid, polifeprosan, poly(L-lactide-co-ethyl phosphate), and poly (L-lactide-co-phosphoric acid propyl); in the process of decompression, irinotecanpto can be slowly and steadily released to local tumor, thus maintaining effective drug concentration of local tumor as well as significantly reducing overall toxic reaction. Being placed in local tumor, the sustained release implant not only reduces overall toxic reaction of irinotecan, but also selectively improves drug concentration in local tumor, enhancing the therapeutic effects of non-operative therapy such as chemotherapy drugs and radiotherapy.

Description

(1) Technical field [0001] The invention relates to an irinotecan slow-release implant for treating solid tumors, belonging to the technical field of medicines. (2) Background technology [0002] Recent studies have shown that the key reason for the failure of tumor chemotherapy is that the existing methods fail to obtain effective drug concentrations at the tumor site. Low-dose drug exposure not only fails to kill tumors, but also easily leads to tolerance. Simply increasing the administration concentration is limited by systemic toxicity. Therefore, selectively increasing the local drug concentration has become a hotspot of current research. [0003] Irinotecan Hydrochloride (CPT-11, Irinotecan Hydrochloride, CPT-11) is a derivative of semi-synthetic camptothecin, which can specifically inhibit DNA topoisomerase I. Irinotecan induces single-strand DNA damage, which blocks DNA replication forks, resulting in cytotoxicity. In vivo experiments, irinotecan showed broad-spe...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/4745A61K47/34A61P35/00
Inventor 孔庆忠赵传亮
Owner SHANDONG LANJIN PHARMA
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