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Estramustine sustained-release implantation agent for curing entity tumour

A technology of estradiol mustard and slow-release implants, which is applied in the field of medicine and can solve the problems of unclear effects, systemic toxic and 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

[0004] In vitro studies have shown that estradiol mustard (Estramustine) can inhibit the growth of vascular endothelium, but the effect of using it alone to treat other tumors is unclear
Although the combination with other anticancer drugs may have a certain effect on some tumors, the systemic side effects caused by conventional administration limit its clinical application

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0077] Put 80 mg of sustained-release excipient (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), then add 20 mg of estramustine, Shake again and dry in vacuo to remove the organic solvent. The dried solid composition is shaped immediately, subpackaged and sterilized by radiation to obtain a slow-release implant containing 20% ​​estramustine. The release time of the slow-release implant in physiological saline in vitro is 26-30 days, and the release time in mouse subcutaneous is 26-32 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% estramustine and 99% polylactic acid;

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

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

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

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

Embodiment 3

[0086] Put 85 mg of sustained-release excipient (PLGA with a molecular weight of 15000-25000, 50:50) into a container, add a certain amount of organic solvent to dissolve and mix (subject to complete dissolution), add 15 mg of estramustine, and re- Shake well and dry under vacuum 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% estramustine. The drug release time of the sustained-release implant in physiological saline in vitro is 27-34 days, and the drug release time in mice subcutaneously is 27-34 days

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Abstract

The invention relates to an estramustine sustained-release implant for the treatment of solid tumors, which is characterized in that the sustained-release implant contains anti-cancer effective amount of estramustine, sustained-release excipient and certain amount of sustained-release regulator. The solid tumors include lung cancer, esophageal cancer, stomach cancer, liver cancer, breast cancer, ovarian cancer, 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 estramustine in the local part of the tumor during the degradation and absorption process, so the invention can maintain 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 estramustine, 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 an estradiol mustard 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 al...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K31/566A61K47/34A61P35/00
Inventor 孔庆忠俞建江
Owner SHANDONG LANJIN PHARMA
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