Low-sudden-release-rate semaglutide microspheres and preparation method thereof

A technology of semaglutide and microspheres, applied in the field of pharmaceutical preparations, can solve the problems of no obvious advantages of disease treatment cost, short half-life of exenatide, high dosage, to maintain the hypoglycemic effect, improve compliance and Quality of life, high encapsulation efficiency

Active Publication Date: 2019-08-09
QILU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Chinese patents CN 101065116B, CN 1968700A, CN 101291685A, etc. disclose the prescription composition and preparation process of exenatide microspheres. However, due to the short half-life of exenatide itself, exenatide microsphere injections that have been on the market need to be injected twice a day. times, exenatide microspheres need to be injected once a week
Chinese patents CN101133082A and CN104717972A disclose the chemical structure, synthesis and modification method, administration method, dosage, and pharmaceutical preparation form of semaglutide, but the oral preparation of semaglutide needs to be administered once a day and th

Method used

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  • Low-sudden-release-rate semaglutide microspheres and preparation method thereof
  • Low-sudden-release-rate semaglutide microspheres and preparation method thereof
  • Low-sudden-release-rate semaglutide microspheres and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Example 1 Preparation of 10g scale 6% drug-loaded semaglutide microspheres

[0046] First, 9.1 g of glycolide-lactide copolymer (Evonik, Select 5050DLG 4A) was dissolved in 175.75g of dichloromethane to obtain an oil phase; 0.6g of semaglutide and 0.3g of sucrose were added to 7.0g of water for injection to dissolve to form a water phase; the water phase was added to the oil phase in an ice bath , obtain the emulsion through ultrasonic dispersion by ultrasonic cell breaker; 316g coagulant simethicone (Dow Corning 360Medical Fluid, 350CST) is added in the above-mentioned emulsion, while stirring, to obtain the coacervate phase containing microspheres in a soft state; then the coacervate phase Transfer to 3505g quenching solvent (n-heptane / dehydrated alcohol mixed solution, weight ratio 80:20) and harden, collect the microsphere after hardening afterwards, n-heptane / ethanol / water for injection (weight ratio 80:15: 5) Continue washing, finally collect, vacuum dry for dry...

Embodiment 2

[0047] Example 2 Preparation of 10g scale 8% drug loading semaglutide microspheres

[0048] First, 8.8 g of glycolide-lactide copolymer (Evonik, Select 5050DLG 4A) was dissolved in 167.2g of dichloromethane to obtain an oil phase; 0.8g of semaglutide and 0.4g of sucrose were added to 10.4g of water for injection to dissolve to form a water phase; the water phase was added to the oil phase on ice , the emulsion was obtained by ultrasonic dispersion by an ultrasonic cell disruptor; 290g coagulant simethicone (Dow Corning 360Medical Fluid, 350CST) was added to the above-mentioned emulsion, and stirred at the same time to obtain a coacervate phase containing microspheres in a soft state; Transfer to 3344g quenching solvent (n-heptane / dehydrated alcohol mixed solution, weight ratio 80:20) and harden, collect the microsphere after hardening again, n-heptane / ethanol / water for injection (weight ratio 80:15: 5) Continue washing, finally collect, vacuum dry for drying.

Embodiment 3

[0049] Example 3 Preparation of 10g-scale 12% drug-loaded semaglutide microspheres

[0050] First, 8.8 g of glycolide-lactide copolymer (Evonik, Select 5050DLG 4A) was dissolved in 167.2g of dichloromethane to obtain an oil phase; 1.2g of semaglutide and 0.4g of sucrose were added to 15.0g of water for injection to dissolve to form a water phase; the water phase was added to the oil phase in an ice bath , the emulsion was obtained by ultrasonic dispersion with an ultrasonic cell disruptor; 250g coagulant simethicone (Dow Corning 360Medical Fluid, 350CST) was added to the above emulsion at a uniform speed, and stirred at the same time to obtain a coagulated phase containing microspheres in a soft state; Phase transfer is carried out in 3344g quenching solvent (n-heptane / dehydrated alcohol mixed solution, weight ratio 80:20) and harden, collect the microsphere after hardening afterwards, n-heptane / ethanol / water for injection (weight ratio 80:15 :5) Continue washing, finally co...

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Abstract

The invention provides low-sudden-release-rate semaglutide microspheres and a preparation method thereof. The preparation is a long-acting injection prepared from the active ingredient semaglutide with the weight being 1-20% of the weight of the microspheres, a biocompatible polymer substrate with the weight being 60-99% of the weight of the microspheres, and other pharmaceutically acceptable auxiliary materials with the weight being 0-20% of the weight of the microspheres. The semaglutide microspheres prepared by using the method are high in encapsulation efficiency, low in sudden release rate and capable of being slowly continuously released, the slow-release effect can last for 20-60 days, the effect on reducing blood sugar can last for at least 2-4 weeks, it only takes two weeks to onemonth or longer to conduct injection administration one time, the bioavailability of the polypeptide drug semaglutide is obviously improved, the metabolic half-life of the semaglutide is prolonged, the semaglutide administration frequency is further reduced, and the drug application compliance of a patient is further improved; because there are few drugs on the surface and the superficial layer of the preparation, the preparation is little released in the incipient administration stage, and therefore, the adverse drug sudden release effect is avoided.

Description

technical field [0001] The invention relates to a long-acting drug-loaded microsphere preparation, which belongs to the field of pharmaceutical preparations. Specifically, it relates to a semaglutide microsphere with sustainable release, low burst release rate and high safety and a preparation method thereof. Background technique [0002] Type 2 diabetes is a chronic metabolic disorder, accounting for more than 90% of diabetes, and has become a serious public health problem worldwide. Its main features are persistent hyperglycemia, positive urine glucose and impaired glucose tolerance. There are many types of diabetes treatment drugs currently on the market, and the treatment mechanisms are also different. However, the goal of diabetes treatment is to improve the blood sugar level of patients throughout the day and reduce it to the normal range. Due to their obvious side effects and other factors, the traditional hypoglycemic drugs limit the medication of diabetic patients...

Claims

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Application Information

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IPC IPC(8): A61K38/26A61K9/50A61P3/10
CPCA61K38/26A61K9/0019A61K9/5031
Inventor 孙彦华杨清敏赵树雍李延志陈曈张明会
Owner QILU PHARMA
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