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Controlled-release implanting preparation used for injecting LHRH (luteinizing hormone releasing hormone) antagonist

An antagonist and injection technology, applied in the field of sustained-release implant preparations, can solve the problems of increasing the dosage, affecting the penetration and diffusion of chemotherapy drugs, and difficult to form effective drug concentrations locally in tumors, so as to reduce systemic toxic reactions and prolong Effect of Local Drug Concentration

Inactive Publication Date: 2011-08-10
SHENZHEN JYMED TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] Blood vessels, connective tissue, matrix proteins, fibrin, and collagen in the tumor stroma not only provide scaffolds and essential nutrients for the growth of tumor cells, but also affect the penetration and diffusion of chemotherapy drugs around and within tumor tissues Due to the excessive expansion and hyperplasia of solid tumors, the interstitial pressure, tissue elastic pressure, fluid pressure and interstitial viscosity are all higher than those of the surrounding normal tissues. Therefore, it is difficult for conventional chemotherapy to form an effective drug concentration in the tumor. The dose is limited by the systemic response

Method used

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  • Controlled-release implanting preparation used for injecting LHRH (luteinizing hormone releasing hormone) antagonist
  • Controlled-release implanting preparation used for injecting LHRH (luteinizing hormone releasing hormone) antagonist
  • Controlled-release implanting preparation used for injecting LHRH (luteinizing hormone releasing hormone) antagonist

Examples

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Effect test

Embodiment 1

[0018] 10% Cetrorelix Acetate, 90% PLGA. Its preparation process is as follows:

[0019] Accurately weigh 600 mg of cetrorelix acetate, add 150 ml of acetone to a stoppered Erlenmeyer flask to dissolve it; precisely weigh 5400 mg of PLGA, add 150 ml of acetone to dissolve, mix the above two solutions, place them overnight at room temperature, and vortex to make It is fully mixed evenly, and the solution is a viscous transparent liquid. Pour it several times onto a clean horizontal glass template, heat in water at 40°C for 24 hours to fully volatilize the acetone, and form a white drug-containing PLGA film with a thickness of about 1 mm and a certain degree of elasticity. The film was completely removed, put into a mold, pressed into a cylindrical shape on a water bath at 50°C, left at room temperature for 2 days, and freeze-dried for more than 24 hours. After aliquoting, use cobalt 60 Sterilize. The resulting implant was cylindrical, with a diameter of 0.2 cm and a length ...

Embodiment 2

[0036] 15% Cetrorelix acetate, 85% PLCG. Its preparation process is as follows:

[0037] Accurately weigh 900 mg of cetrorelix acetate, add 230 ml of acetone to a stoppered Erlenmeyer flask to dissolve it; accurately weigh 5100 mg of PLCG, add 140 ml of acetone to dissolve, mix the above two solutions, and place at room temperature overnight. Vortex to make it fully mixed, the solution is a viscous transparent liquid. Pour it several times onto a clean horizontal glass template, and heat it in a water bath at 40°C for 24 hours to fully volatilize the acetone to form a white drug-containing PLCG film with a thickness of about 1 mm and a certain degree of elasticity. The film was completely removed, put into a mold, pressed into a cylindrical shape on a water bath at 50°C, left at room temperature for 2 days, and freeze-dried for more than 24 hours. After packing, drill 60 Sterilize. The resulting implant was cylindrical, with a diameter of 0.2 cm and a length of 1.0 cm.

...

Embodiment 3

[0054] 20% Cetrorelix Acetate, 80% PLA. Its preparation process is as follows:

[0055] Accurately weigh 1200 mg of cetrorelix acetate, add 300 ml of acetone to a stoppered Erlenmeyer flask to dissolve it; accurately weigh 4800 mg of PLA, add 100 ml of acetone to dissolve, mix the above two solutions, and place at room temperature overnight. Vortex to make it fully mixed, the solution is a viscous transparent liquid. Pour it several times onto a clean horizontal glass template, and heat it in a water bath at 40°C for 24 hours to fully volatilize the acetone to form a white drug-containing PLA film with a thickness of about 1 mm and a certain degree of elasticity. The film was completely removed, put into a mold, pressed into a cylindrical shape on a water bath at 50°C, left at room temperature for 2 days, and freeze-dried for more than 24 hours. After packing, drill 60 Sterilize. The resulting implant was cylindrical, with a diameter of 0.2 cm and a length of 1.0 cm.

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Abstract

The invention relates to a controlled-release implanting preparation used for injecting an LHRH (luteinizing hormone releasing hormone) antagonist. The invention is characterized in that the LHRH antagonist, namely cetrorelix acetate is loaded into a high polymer material carrier in a certain proportion, and then compressed into an implanting preparation of a certain shape so as to be used for implanting injection, thereby achieving the effect of long-acting controlled release. The controlled-release implanting preparation consists of the cetrorelix acetate with the effective dose for cancer resisting and controlled-release auxiliary materials, and the controlled-release auxiliary materials mainly comprise a biodegradable and biocompatible macromolecule copolymer; and the controlled-release implanting preparation is injected into tumors or around tumors, thereby being favorable for the effective diffusion of the medicament in the solid tumors, selectively improving the local medicament concentration of the tumors, reducing the injection times and the medicament tolerance, enhancing the compliance of patients and facilitating the clinical use and the medication for the patients.

Description

Technical field: [0001] The invention relates to the field of preparations, in particular to a slow-release implant preparation for LHRH antagonist injection. Background technique: [0002] The anticancer drug Cetrorelix is ​​a gonadotropin-releasing hormone (LHRH) antagonist developed by Germany's Asta Medica, which can control the stimulation of the ovary, prevent premature discharge of immature follicles, and help conception. Cetrorelix controls luteinizing hormone (LH) and follicle stimulating hormone (FSH) by competing with endogenous LHRH for membrane receptors on pituitary cells. As a newly synthesized LHRH antagonist, cetrorelix can treat, prevent and alleviate various diseases through three pathways: one is to inhibit the secretion of dependent hormones through the hypothalamus-pituitary-gonad pathway, and the other is to directly inhibit the proliferation of tumor cells and metastasis, and the third is to induce apoptosis of cancer cells. A large number of studie...

Claims

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Application Information

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IPC IPC(8): A61K38/08A61K9/00A61K9/16A61K9/70A61K47/42A61K47/34A61K47/36A61P35/00
Inventor 李新宇支钦姚志勇
Owner SHENZHEN JYMED TECH
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