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Preparation method of pamoic acid leuprorelin slow release preparation

A technology of leuprolide acetate and leuprolide, which is applied in directions such as pharmaceutical formulations, medical preparations without active ingredients, and medical preparations containing active ingredients, etc., can solve the problem of restricting the development of leuprolide microsphere industry, The problems of low product yield and long production cycle can achieve the effect of less pores, high product yield and simplified production process

Active Publication Date: 2016-07-27
ZHEJIANG SUNDOC PHARMA SCI & TECH CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The whole process is complex, with many steps, long production cycle and low product yield
In addition, gelatin is a protein derived from animals, which has the problem of allergenicity. These problems have long restricted the development of my country's leuprolide microsphere industry.

Method used

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  • Preparation method of pamoic acid leuprorelin slow release preparation
  • Preparation method of pamoic acid leuprorelin slow release preparation
  • Preparation method of pamoic acid leuprorelin slow release preparation

Examples

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Effect test

Embodiment 1

[0062] A preparation method of leuprolide pamoate sustained-release preparation, comprising the following steps:

[0063] (1) Salt formation and purification: Leuprolide acetate and pamoic acid disodium salt (4,4'-methylenebis(3-hydroxy-2-naphthoic acid) disodium salt, CAS: 6640-22 -8, commercially available) is the synthetic leuprolide pamoate of raw material, then leuprolide pamoate is purified;

[0064] The specific process steps of salt formation are:

[0065] a. Filtration to remove impurities: Leuprolide acetate crude product is dissolved in ultrapure water, prepared into a solution with a mass concentration of 5%, filtered through a 1 μm membrane stack to remove water-insoluble impurities to obtain a leuprolide acetate solution; pamoate disodium salt Dissolve in ultrapure water, prepare a solution with a mass concentration of 5%, and filter through a 1 μm membrane stack to remove water-insoluble impurities to obtain a pamoic acid disodium salt solution;

[0066] b. St...

Embodiment 2

[0083] A preparation method of leuprolide pamoate sustained-release preparation, comprising the following steps:

[0084] (1) Salt formation and purification: Leuprolide acetate and pamoic acid disodium salt (4,4'-methylenebis(3-hydroxy-2-naphthoic acid) disodium salt, CAS: 6640-22 -8, commercially available) is the synthetic leuprolide pamoate of raw material, then leuprolide pamoate is purified;

[0085] The specific process steps of salt formation are:

[0086] a. Filtration to remove impurities: Leuprolide acetate crude product is dissolved in ultrapure water, prepared into a solution with a mass concentration of 90%, filtered through a 1 μm membrane stack to remove water-insoluble impurities to obtain a leuprolide acetate solution; pamoate disodium salt Dissolve in ultrapure water, prepare a solution with a mass concentration of 90%, and filter through a 1 μm membrane stack to remove water-insoluble impurities to obtain a pamoic acid disodium salt solution;

[0087] b. ...

Embodiment 3

[0104] A preparation method of leuprolide pamoate sustained-release preparation, comprising the following steps:

[0105] (1) Salt formation and purification: Leuprolide acetate and pamoic acid disodium salt (4,4'-methylenebis(3-hydroxy-2-naphthoic acid) disodium salt, CAS: 6640-22 -8, commercially available) is the synthetic leuprolide pamoate of raw material, then leuprolide pamoate is purified;

[0106] The specific process steps of salt formation are:

[0107] a. Filtration to remove impurities: Leuprolide acetate crude product is dissolved in ultrapure water, prepared into a solution with a mass concentration of 50%, filtered through a 1 μm membrane stack to remove water-insoluble impurities to obtain a leuprolide acetate solution; pamoate disodium salt Dissolve in ultrapure water, prepare a solution with a mass concentration of 50%, and filter through a 1 μm membrane stack to remove water-insoluble impurities to obtain a pamoic acid disodium salt solution;

[0108] b. ...

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Abstract

The invention discloses a preparation method of a pamoic acid leuprorelin slow release preparation.The technology that leuprorelin acetate is prepared into indissoluble salt is adopted for the first time, and then a hot-melt extrusion technology is adopted; therefore, the production technologies are simplified, the pores on the surfaces of microspheres are few, the medicine packaging rate is high, the product yield is high, and the medicine burst release condition is significantly reduced.

Description

technical field [0001] The invention relates to the technical field of production of leuprolide sustained-release preparations, in particular to a preparation method of leuprolide pamoate sustained-release preparations. Background technique [0002] Luteinizing hormone-releasing hormone (LHRH) is secreted by the hypothalamus in a pulsatile manner. It acts on the pituitary gland, causing the pituitary gland to release luteinizing hormone (LH) and follicle-stimulating hormone (FSH), and LH and FSH then act on the sex organs, thereby regulating the function of the reproductive system. LHRH was identified as a decapeptide in 1997, and its chemical structure is as follows: pyroGlu-His-Trp-Ser-Tyr-Gly-Leu-Arg-Pro-Gly-NH 2 . [0003] The LHRH secreted by the hypothalamus of all mammals has this structure. But LHRH inactivates very quickly in the body, because Gly 6 -Leu 7 and Pro 9 -Gly 10 . The peptide bonds between them are easily decomposed and inactivated by peptide lya...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K38/09A61K47/12A61K47/34A61P35/00A61P15/00A61P5/04
CPCA61K9/0002A61K9/145A61K9/146A61K38/09
Inventor 丁多浩蒋朝军王代丰杜保国李娟娟朱精兵
Owner ZHEJIANG SUNDOC PHARMA SCI & TECH CO LTD
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