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Insoluble leuprorelin sustained-release preparation

A technology of leuprolide and sustained-release preparations, which is applied in the field of insoluble leuprolide sustained-release preparations, can solve the problems of restricting the development of leuprolide microsphere industry, long production cycle, and low product yield. The effect of high product yield, simplified production process, and uniform drug distribution

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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  • Insoluble leuprorelin sustained-release preparation
  • Insoluble leuprorelin sustained-release preparation
  • Insoluble leuprorelin sustained-release preparation

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0071] An insoluble leuprolide sustained-release preparation, prepared through the following steps:

[0072] (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 insoluble salt of raw material, then leuprolide insoluble salt is purified;

[0073] The specific process steps of salt formation are:

[0074] 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 to remove water-insoluble impurities to obtain a pamoic acid disodium salt solution;

[0075] b. Sterili...

Embodiment 2

[0102] An insoluble leuprolide sustained-release preparation, prepared through the following steps:

[0103] (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 insoluble salt of raw material, then leuprolide insoluble salt is purified;

[0104] The specific process steps of salt formation are:

[0105] a. Filtration to remove impurities: the crude product of leuprolide acetate is dissolved in ultrapure water, prepared into a solution with a mass concentration of 90%, and filtered through a 1 μm membrane to remove water-insoluble impurities to obtain leuprolide acetate solution; for disodium pamoate Dissolved in ultrapure water, prepared into a solution with a mass concentration of 90%, and filtered through a 1 μm membrane to remove water-insoluble impurities to obtain a pamoic acid disodium salt solution;

[0106]...

Embodiment 3

[0133] An insoluble leuprolide sustained-release preparation, prepared through the following steps:

[0134] (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 insoluble salt of raw material, then leuprolide insoluble salt is purified;

[0135] The specific process steps of salt formation are:

[0136] a, filter impurity removal: leuprolide acetate crude product is dissolved with ultrapure water, is mixed with the solution of mass concentration 50%, and 1 μm membrane filter removes water-insoluble impurity to obtain leuprolide acetate solution; Pamoate disodium salt is used Dissolved in ultrapure water, prepared into a solution with a mass concentration of 50%, and filtered through a 1 μm membrane to remove water-insoluble impurities to obtain a pamoic acid disodium salt solution;

[0137] b. Sterilization by fi...

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Abstract

The invention discloses an insoluble leuprorelin sustained-release preparation.Leuprorelin acetate is prepared into insoluble salt firstly, then emulsification is carried out through a single emulsion method, and leuprorelin microspheres are prepared through an in-liquid drying technology.The production process is simplified, there are few pores in the surfaces of the microspheres, the drug encapsulation rate is high, the product yield is high, and drug burst release is remarkably lowered.

Description

technical field [0001] The invention relates to the technical field of production of leuprolide sustained-release preparations, in particular to an insoluble leuprolide sustained-release preparation. 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 lyases. In order to se...

Claims

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Application Information

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IPC IPC(8): A61K38/09A61K9/50A61K47/34A61K47/32A61P5/04A61P15/00A61P35/00
CPCA61K9/0002A61K9/5026A61K9/5031A61K38/09
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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