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

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...

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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 the dosage is too large , Semaglutide injection needs to be injected once a week

CN 104203266A, CN 104203221A disclose the prescription composition and preparation process of semaglutide oral preparations, but no matter it is a tablet or a capsule, no matter the size of wet / dry granulation, no matter what the tablet preparation process is, what kind of excipients to choose (including disintegrants, adhesives, lubricants, etc.), the longest duration is only one day, and the oral effective dosage is as high as 40mg, compared with other antidiabetic drugs administered once a week, there is no obvious advantage and disease treatment must be expensive

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