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A kind of exenatide sustained-release microsphere composition

A technology of exenatide and slow-release microspheres, applied in the field of medicine

Active Publication Date: 2016-05-18
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 method of preparing exenatide microspheres by combining two or more different PLGs has not been reported

Method used

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  • A kind of exenatide sustained-release microsphere composition
  • A kind of exenatide sustained-release microsphere composition
  • A kind of exenatide sustained-release microsphere composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0048] Example 1 Preparation of single PLG5% drug-loaded exenatide microspheres

[0049] Weigh 0.2g Exenatide Acetate and put it into a 5ml EP tube according to the dried and pure 0.2g Exenatide, weigh another 0.08g sucrose, put it into the EP Tube, add 2.4g Water for Injection, vortex to dissolve and put it in ice bath Save for later. Weigh 3.72g of PLG50504A (Evonik Industries AG, intrinsic viscosity 0.41dL / g, LA:GA50:50, weight average molecular weight about 55000Da), put it into a 50ml glass vial, and weigh 58.3g of dichloromethane, add it to the glass vial to dissolve, and put it in an ice bath Save for later. Using an ultrasonic cell breaker with a power of 1600W, under 40% amplitude ultrasonic, add the aqueous phase into the dichloromethane solution with a syringe, ultrasonic for 1 min, then stop for 1 min, and then ultrasonic for 2 min to form colostrum.

[0050] Place a 250ml beaker in a 3°C constant temperature water bath, transfer the colostrum into the beaker, an...

Embodiment 2

[0052] Example 2 Preparation of single PLG10% drug-loaded exenatide microspheres

[0053] Weigh 0.4g of exenatide after dehydration and purification, put it into a 5ml EP tube, weigh 0.16g of sucrose, put it into an EP tube, add 2.4g of water for injection, vortex to dissolve, and then ice-bath Save for later. Weigh 3.44g of PLG50504A (Evonik Industries AG, intrinsic viscosity 0.41dL / g, LA:GA50:50, weight average molecular weight about 55000Da), put it into a 50ml glass vial, and weigh 58.3g of dichloromethane, add it to the glass vial to dissolve, and put it in an ice bath Save for later. Using an ultrasonic cell breaker with a power of 1600W, under 40% amplitude ultrasonic, add the aqueous phase into the dichloromethane solution with a syringe, ultrasonic for 1 min, then stop for 1 min, and then ultrasonic for 2 min to form colostrum.

[0054] Place a 250ml beaker in a 3°C constant temperature water bath, transfer the colostrum into the beaker, and stir with a mechanical s...

Embodiment 3

[0056] Example 3 Preparation of two kinds of PLG10% drug-loaded exenatide microspheres

[0057] Weigh 0.42g of exenatide after dry and pure, put it into a 5ml EP tube, weigh another 0.16g of sucrose, put it into an EP tube, add 2.4g of water for injection, vortex to dissolve, and put it in ice bath Save for later. Weigh 0.855g PLG50501A (Evonik Industries AG, intrinsic viscosity 0.11dL / g, LA:GA50:50, weight average molecular weight about 5500Da), 2.565g PLG50504A (Evonik Industries AG, intrinsic viscosity 0.41dL / g, LA:GA50:50, weight average molecular weight about 55000Da ), put it into a 50ml glass vial, weigh another 58.3g of dichloromethane, add it into the glass vial to dissolve, and store it in an ice bath for later use. Using an ultrasonic cell breaker with a power of 1600W, under 40% amplitude ultrasonic, add the aqueous phase into the dichloromethane solution with a syringe, ultrasonic for 1 min, then stop for 1 min, and then ultrasonic for 2 min to form colostrum.

...

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Abstract

The invention aims to provide an exenatide controlled-release microsphere composition composed of exenatide or a salt thereof, a polymer blend and sucrose, wherein the weight content of the exenatide or the salt thereof is 10-20%, the weight content of the polymer blend is 76-89%, and the weight content of sucrose is 1-4%. The pharmaceutical composition exists in a microsphere form, has the property of long-term drug release, and can release exenatide in a time exceeding one month. The pharmaceutical composition has one characteristic that appropriate combination of two different PLGs is adopted in the pharmaceutical composition, the fluctuation of the exenatide concentration in plasma can be significantly reduced, and a release period is not delayed significantly. The pharmaceutical composition has another characteristic that the drug sudden release quantity is quite low under a high drug loading capacity situation. The exenatide microsphere composition has the drug loading quantity of not less than 10.0% and the sudden release quantity not exceeding 1.0%.

Description

technical field [0001] The invention belongs to the technical field of medicine and relates to an exenatide slow-release microsphere composition, which can be used in the preparation of hypoglycemic drugs or weight-controlling weight-loss drugs. Background technique [0002] According to the statistics of the International Diabetes Federation, in 2013, the global prevalence of diabetes among adults aged 20-79 was 8.3%, and the number of patients had reached 382 million. type diabetic patients. In 2013, the global diabetes medical expenditure was as high as 548 billion US dollars, accounting for 11% of the global medical expenditure. The development of effective and highly compliant diabetes drugs has great social and economic value. [0003] Glucagon-like peptide-1 (GLP-1) is a family of incretins, secreted by intestinal L cells, is a hormone secreted after meals, and helps control Blood glucose, the main metabolic response, is released with rising blood glucose levels af...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/22A61K9/16A61K47/34A61P3/04
Inventor 蒋朝军
Owner ZHEJIANG SUNDOC PHARMA SCI & TECH CO LTD
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