Polypeptide medicament sustained release microsphere or microcapsule preparation with uniform grain size and preparation method thereof

Abstract

The invention discloses a polypeptide medicament sustained release microsphere or a microcapsule preparation with uniform grain size, a preparation method thereof and application. The average grain size of the microsphere or the microcapsule preparation is between 50 nanometers and 100 microns, and the grain size distribution coefficient CV value is less than 20 percent. The polypeptide medicament has a definite structure, has functions of therapy or adjuvant therapy of type-2 diabetes, and is preferably one or more of GLP-1, Exenatide, Exendin-4 and derivatives and analogs thereof. The microsphere or the microcapsule preparation uses a microsphere or a microcapsule with uniform grain size as a substrate to prepare the polypeptide medicament into a sustained release preparation through an embedding mode, and by changing the grain size of the microsphere or the microcapsule, the sustained release cycle is adjustable between one week and one month, and the microsphere or the microcapsule preparation can be applied to the therapy or the adjuvant therapy of the type-2 diabetes and body weight control. Besides, the microsphere or the microcapsule preparation has the advantages of simple preparation process and mild preparation course, and can protect the biological activity of the embedded polypeptide medicament.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations in medical technology, and is a polypeptide drug sustained-release microsphere or microcapsule preparation with uniform particle size and its preparation method and application. More specifically, it is a polymer microcapsule with uniform particle size. Ball or microcapsule materials, slow-release microsphere preparations for embedding peptide drugs such as Glucagon-like peptide-1 (GLP-1), Exendin-4, Exenatide and their derivatives and analogs Its preparation method and the use of the polypeptide drug sustained-release microsphere or microcapsule preparation in treating or assisting in treating diabetes or controlling body weight. Background technique [0002] Type 2 diabetes is a disease that seriously threatens human health and life. For a long time, people have mainly used drugs such as sulfonylureas and biguanides to treat type 2 diabetes, but these drugs have relatively large side ...

AI Technical Summary

Problems solved by technology

However, all three methods use a large amount of organic solvents, which can easily denature the drug.

[0016] Generally speaking, in terms of polypeptide drug slow-release microsphere preparations for the treatment of type 2 diabetes, the preparation of relevant carriers at home and abroad still adopts traditional methods, such as the preparation of emulsions by mechanical stirring, homogenization, ultrasonic crushing, spraying, etc., these Although the process conditions of the method are simple, the preparation repeatability is very poor, and there are large differences in the performance of different batches of products, and there are difficulties in scale-up production

Moreover, the particle size uniformity of the prepared microspheres is very poor, the drug embedding rate is low, and the particle size is difficult to control

The inhomogeneous particle size of the drug carrier can also cause the following problems: 1) Because the drug carriers with different particle sizes have different absorption sites and absorption mechanisms in the body, if the particle size is not uniform, the particle size and absorption site of the drug carrier cannot be adjusted. , and the relationship between the absorption mechanism; 2) When conducting in vivo and in vitro pharmacological experiments, since the particle size of the drug carrier directly affects the release rate of the encapsulated drug, if the particle size of the drug carrier is not uniform, it will lead to the experiment. The repeatability is poor, which directly affects the sustained and controlled release effect of the drug carrier; 3) Because the drug carriers with different particle sizes have different absorption sites in the body, the drug carrier will be absorbed by multiple parts in the body, causing certain toxic and side effects

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