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Liraglutide sustained release microsphere composition and preparation method thereof

A technology of liraglutide and sustained-release microspheres, which is applied in the field of sustained-release microsphere compositions, can solve problems such as maintaining the effective therapeutic concentration of drugs, and achieve the effects of increasing drug loading, ensuring therapeutic effects, and high blood drug concentrations

Inactive Publication Date: 2019-10-25
浙江美华鼎昌医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0009] However, the liraglutide microsphere injection prepared by the above method has a drug loading of less than 10%, which cannot maintain the effective therapeutic concentration of the drug in the human body for a long time to achieve the desired therapeutic effect

Method used

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  • Liraglutide sustained release microsphere composition and preparation method thereof
  • Liraglutide sustained release microsphere composition and preparation method thereof
  • Liraglutide sustained release microsphere composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] This embodiment provides a preparation method of the above-mentioned liraglutide sustained-release microsphere composition, which includes the following steps:

[0031] 1) Grinding 0.3 g of liraglutide powder into an ultrafine powder with a D50 particle size of 2-3 microns by jet milling.

[0032] 2) Dissolve 0.7 g of glycolide-lactide copolymer (intrinsic viscosity: 1.5 dl / g, carboxyl-terminated, glycolide:lactide=15:85) in 14.0 g of dichloromethane.

[0033] 3) Add the liraglutide ultrafine powder obtained in step 1) into the organic solution in step 2), and shear at a high speed of 6000 rpm for 2 minutes to form a suspension.

[0034] 4) Stir the suspension in step 3) at 300 rpm and add 14.0 g of simethicone oil (viscosity: 350 cPa / s) at a constant speed within 3 minutes.

[0035] 5) The product of step 4) was poured into 2260 g of n-heptane and stirred at 500 rpm for 2 hours.

[0036] 6) The product of step 5) was filtered, and the obtained solid was freeze-dried ...

experiment example 1

[0048] Drug loading (%)=(drug content in microspheres / weight of microspheres)×100%

[0049] Encapsulation efficiency (%)=(drug content in microspheres / total weight of drug used)×100%

[0050] example Example 1 Comparative example 1 Drug loading(%) 23.5 2.4 Encapsulation rate (%) 84.6 63.6

[0051] It can be seen that the liraglutide sustained-release microspheres prepared in Example 1 have higher drug loading and encapsulation efficiency than those prepared in Comparative Example 1.

experiment example 2

[0053]The volume-average particle diameter of the liraglutide sustained-release microspheres prepared in Example 1 is 47 microns, which is suitable for injection administration.

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Abstract

The invention relates to a liraglutide sustained release microsphere composition and a preparation method thereof. The composition is composed of liraglutide and a glycolide-lactide copolymer. The composition is prepared by adopting a medicine superfine micro power direct packing method. The liraglutide sustained release microsphere prepared through the method has the high medicine carrying amount, and the high blood concentration can be maintained for a long time when the microsphere is released inside the human body to achieve the ideal treatment effect. Meanwhile, the microsphere has the proper grain size, and is suitable for the injection drug delivery route.

Description

technical field [0001] The invention relates to a sustained-release microsphere composition, in particular to a liraglutide sustained-release microsphere composition, and a preparation method of the liraglutide sustained-release microsphere composition. Background technique [0002] Diabetes is a group of metabolic diseases characterized by hyperglycemia. Diabetes is a chronic disease that requires long-term drug treatment. There are different parenteral antidiabetic drugs on the market, including human insulin and human glucagon-like peptide 1 (GLP-1) agonists. [0003] Liraglutide is a semi-synthetic / totally synthetic GLP-1 analogue. This medicine is used for the adjuvant treatment of type 2 diabetes. Liraglutide is a fatty acylated peptide drug that prevents it from being rapidly degraded in the human body. Its hypoglycemic effect is blood glucose dependent, and it is not easy to cause hypoglycemia in patients. [0004] However, the metabolic rate of liraglutide in t...

Claims

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Application Information

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IPC IPC(8): A61K9/52A61K38/26A61K47/34A61P3/10
CPCA61K9/0019A61K9/5031A61K38/26A61P3/10
Inventor 贾昕顾亚萍何书麟王传跃
Owner 浙江美华鼎昌医药科技有限公司
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