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Long-acting leuprorelin acetate microsphere and preparation method thereof

A technology of leuprolide acetate and microspheres, which is applied in directions such as medical preparations without active ingredients, medical preparations containing active ingredients, and pharmaceutical formulas

Inactive Publication Date: 2016-02-03
北京博恩特药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the leuprolide acetate microspheres that have been approved for production in China are only products with a release period of one month, and the long-acting leuprolide acetate microspheres with a release period of three months have not yet been researched by relevant domestic units.

Method used

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  • Long-acting leuprorelin acetate microsphere and preparation method thereof
  • Long-acting leuprorelin acetate microsphere and preparation method thereof
  • Long-acting leuprorelin acetate microsphere and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0048] Experimental example 1: 90-day release study of 8 samples

[0049] In this method, 8 samples were prepared using the preparation method in Example 1, and different PLGA models were selected, and the drug loading and in vitro release rate of the microspheres were determined. PLGA is the key factor affecting the release rate. Long-term release requires a larger molecular weight and viscosity to achieve a better effect. This experiment mainly investigates the effect of different PLGA on the release rate. Its molecular weight is 20000-100000, intrinsic viscosity: 20-80g / ml.

[0050] Table 1: Experimental design of different models of PLGA

[0051]

[0052] Table 2: The release rate of each sample at each time point

[0053]

[0054] in conclusion:

[0055] 1. PLGA model 85155A, DL1A, DL4A, and DL5A microsphere release rate can meet the three-month release requirement, but PLGA75254A does not meet the requirement, especially 100DL4A, 5A is better, and the molecular ...

experiment example 2

[0056] Experimental example 2 investigates the impact of raw material and auxiliary material proportioning on yield

[0057] In this experiment, 4 groups of samples were prepared according to the method of Example 1. The difference between each group of samples was that the ratios of raw materials and auxiliary materials PLGA were respectively set (see Table 3 below). This experiment mainly investigated the ratio changes of raw materials and auxiliary materials PLGA.

[0058] Table 3 Experimental results:

[0059]

[0060] Summary: When the ratio is 11.25:85, the yield is the best, and the prepared microspheres can be released for three months, meeting the requirements.

experiment example 3

[0061] Experimental Example 3: Investigate the effect of PLGA concentration on release rate

[0062] In this experiment, three groups of samples were prepared by the method of Example 1. The only difference between each group of samples was that different concentrations of PLGA were set respectively. This experiment mainly investigated the influence of the concentration of PLGA on the yield of microspheres. (See Table 4)

[0063] Table 4: Experimental results

[0064] PLGA concentration

yield

Release

25％

52％

released for three months,

20％

64％

free for three months

15％

54％

Can be released for three months, slightly faster

[0065] Summarize:

[0066] 1. The concentration of PLGA has a certain influence on the yield of microspheres. The concentration of 20% is the best. The viscosity of 25% concentration is too high, which affects the yield. The concentration of 15% is too thin, which...

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Abstract

The invention relates to a chemical drug microsphere preparation and a preparation method thereof, in particular to long-acting leuprorelin acetate microsphere and a preparation method thereof. The raw materials of the leuprorelin acetate microsphere include leuprorelin acetate, a glycolide lactide copolymer, mannitol and gelatin. The microsphere and the preparation process provided by the invention select appropriate PLGA and unique production process parameters, thus developing the leuprorelin acetate microsphere with release time up to 3 months. And the release rate and yield of the microsphere provided by the invention are superior to the prior art.

Description

Technical field: [0001] The invention relates to a chemical drug microsphere preparation and a preparation method thereof, in particular to long-acting leuprolide acetate microspheres and a preparation method thereof. Background technique: [0002] Leuprorelin acetate (LeuprorelinAcetate) is a potent gonadotropin-releasing hormone agonist (GnRHa), which can stimulate the pituitary gland to secrete gonadotropins and induce reproductive organs to produce steroids. It is clinically used for endometriosis, uterine fibroids, central precocious puberty, and prostate cancer. Leuprolide acetate microspheres for injection are made by embedding leuprolide acetate in polymer materials to make the leuprolide acetate in the microspheres release slowly, so as to achieve therapeutic effect, especially suitable for life-long Patients taking medication, such as prostate cancer patients. Due to the high-tech characteristics of the preparation process of microsphere preparations, there are m...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K38/09A61K47/34A61K47/42A61K47/10A61P15/00A61P35/00
Inventor 郭光明黄似焕庞桂才岑振宁
Owner 北京博恩特药业有限公司
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