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Drug sustained release microsphere, preparation method and application thereof

A technology of slow-release microspheres and drugs, which is applied in drug combination, drug delivery, and pharmaceutical formulations. Solve the effect of poor repeatability

Active Publication Date: 2018-12-11
INST OF PROCESS ENG CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] (1) Since the gonadotropin-releasing hormone drug is a protein polypeptide substance, it is easy to diffuse to the outer water phase during the long-term curing process, resulting in a low encapsulation efficiency; (2) Due to the use of the inner water phase additive, it is easy to It makes it difficult to determine the residues in the later stage, and reduces the biological safety, making it difficult to achieve a good biological treatment effect

Method used

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  • Drug sustained release microsphere, preparation method and application thereof
  • Drug sustained release microsphere, preparation method and application thereof
  • Drug sustained release microsphere, preparation method and application thereof

Examples

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Embodiment 1

[0069] A preparation method for embedding triptorelin acetate long-acting sustained-release microspheres for injection, comprising the following steps (the schematic diagram of its preparation process is as follows: figure 1 shown):

[0070] The hydrophilic microporous membrane with a pore size of 80 μm is soaked in water to fully wet the porous membrane. 20mL concentration is 50mg / mL triptorelin aqueous solution as inner water phase W 1 , Dissolve 1 g of polylactic-co-glycolic acid (PLGA) with a molecular weight of 30,000 in 20 mL of acetone as oil phase O. Mix the inner water phase and the oil phase, homogeneously emulsify for 1 min, and get W 1 / O colostrum. The colostrum was added to 200 mL of 5% wt PVA aqueous solution W 2 , magnetic stirring at 600rpm for 1min to prepare W 1 / O / W 2 type pre-double emulsion, and then this pre-double emulsion is pressed through the microporous membrane device (such as figure 1 SPG film in ), get W 1 / O / W 2Type double emulsion, and...

Embodiment 2

[0081] A preparation method for embedding leuprolide long-acting sustained-release microspheres for injection, comprising the following steps (the schematic diagram of its preparation process is as follows: figure 1 shown):

[0082] The hydrophilic microporous membrane with a pore size of 32 μm was soaked in water to fully wet the porous membrane. 5 mL of 20 mg / mL leuprolide aqueous solution was used as the internal water phase, and 100 mg of polylactic-co-glycolic acid (PLGA) with a molecular weight of 10,000 was dissolved in 10 mL of ethyl acetate as the oil phase. Mix the inner water phase and the oil phase, homogeneously emulsify for 1 min, and get W 1 / O colostrum. The colostrum was added to 200 mL of 1% wt PVA aqueous solution W 2 , magnetically stirred at 500rpm for 2min to prepare W 1 / O / W 2 type pre-double emulsion, and then this pre-double emulsion is pressed through the microporous membrane device (such as figure 1 SPG film in ), get W 1 / O / W 2 Then the doub...

Embodiment 3

[0092] A preparation method for embedding leuprolide long-acting sustained-release microspheres for injection, comprising the following steps (the schematic diagram of its preparation process is as follows: figure 1 shown):

[0093] The hydrophilic microporous membrane with a pore size of 60 μm is soaked in water to fully wet the porous membrane. 10mL concentration of 10mg / mL leuprolide aqueous solution as the inner water phase W 1 , 100 mg of polylactic acid (PLA) with a molecular weight of 10,000 was dissolved in 10 mL of ethyl acetate as oil phase O. Mix the inner water phase and the oil phase, homogeneously emulsify for 30s, and get W 1 / O colostrum. This colostrum was added to 100 mL of 5% wt PVA aqueous solution W 2 In, magnetic stirring 300rpm stirs 30s to prepare pre-multiple emulsion, then this pre-multiplex emulsion is pressed through the microporous membrane device (such as figure 1 SPG film in ), get W 1 / O / W 2 Then the double emulsion was solidified at a va...

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Abstract

The invention provides a drug sustained release microsphere, a preparation method and an application thereof. The preparation method comprises the following steps: filtering an 'internal water phase / oil phase / external water phase' pre-emulsion solution with a micro-pore film, and then removing a solvent during a curing process, washing and drying, thereby acquiring the drug sustained release microsphere, wherein a gonadotrophin releasing hormone aqueous solution is served as the internal water phase. The preparation method provided by the invention is simple. The drug sustained release microsphere prepared according to the invention has uniform and controllable size, different batches of products are high in repeatability and the drug sustained release microsphere is easy for industrial production.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to a drug sustained-release microsphere and a preparation method and application thereof, in particular to a gonadotropin-releasing hormone-loaded sustained-release microsphere with uniform size, high encapsulation efficiency, and low burst release and its preparation method. Preparation methods and applications. Background technique [0002] Gonadotropin releasing hormone (GnRH), also known as luteinizing hormone releasing hormone (LHRH), is a decapeptide hormone secreted by the hypothalamus, which plays an important role in regulating sexual maturation and reproductive capacity of mammals . In addition, GnRH also plays an important regulatory role in tissues and organs outside the brain. Although the hypothalamic pituitary is the main tissue and target for the synthesis and secretion of GnRH, GnRH exists in tissues and organs outside the hypothalamus, and GnRH receptors ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K38/09A61K9/52A61P35/00A61P15/00
CPCA61K9/0002A61K9/5015A61K9/5026A61K9/5031A61K9/5089A61K38/09
Inventor 马光辉韦祎胡琳琳李勋樊素然周炜清
Owner INST OF PROCESS ENG CHINESE ACAD OF SCI
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