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Smeglutide implant and preparation method thereof

An implant and organic solvent technology, applied in the field of drug preparation, can solve the problems of inconvenient drug storage, increased drug risk, tissue damage, etc., and achieve the effects of improving bioavailability, improving convenience, and increasing stability.

Pending Publication Date: 2022-05-13
兰州积石药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The current injection of semaglutide is packaged in the form of an injection pen, and the packaged volume of each injection pen is 4 doses. Although it is relatively convenient to inject, its dosage form needs to be stored at a low temperature of 2-8°C (i.e. in a refrigerator). ) to save
For some patients who need to travel frequently, this kind of storage method of drugs not only easily leads to the inconvenience of drug storage for patients during use, but also sometimes causes drug failure due to storage conditions and increases the risk of drug use.
In addition, long-term subcutaneous injection can also easily lead to tissue damage at the injection site

Method used

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  • Smeglutide implant and preparation method thereof
  • Smeglutide implant and preparation method thereof
  • Smeglutide implant and preparation method thereof

Examples

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preparation example Construction

[0031] The present invention provides a semaglutide implant and a preparation method thereof, and those skilled in the art can learn from the content of the present invention and appropriately improve process parameters to achieve. It should be particularly pointed out that all similar substitutions and modifications apparent to those skilled in the art are deemed to be included in the present invention. The method and application of the present invention have been described through the preferred embodiments, and it is obvious that relevant persons can make changes or appropriate changes and combinations of the methods and applications described herein without departing from the content, spirit and scope of the present invention to achieve and Apply the technology of the present invention.

[0032] The implant preparation provided by the present invention and the raw materials, auxiliary materials and reagents used in the preparation method and use thereof can be purchased fro...

Embodiment 1

[0034] Example 1: Preparation of Semaglutide Injection Subcutaneous Implant

[0035] The prescription of the present embodiment is as follows (1000):

[0036] Element Dosage Semaglutide sodium salt 4.005g (equivalent to semaglutide 4g) N-(8-(2-Hydroxybenzoyl)amino)octanoic acid (NAC) 10g PLA (M=20000 Daltons) 40g Poloxamer 188 120g Sorbitol 8g

[0037] PLA (M=20000) was completely dissolved in ethyl acetate to prepare a 5% ethyl acetate solution of PLA, and then semaglutide sodium salt and excipient N-(8-(2-hydroxybenzene) were added to it. Formyl)amino)caprylic acid (NAC) was fully stirred to prepare a PLA ethyl acetate solution containing semaglutide and N-(8-(2-hydroxybenzoyl)amino)octanoic acid (NAC) at 25°C. PLA microcapsules of semaglutide sodium were prepared by spray drying under the pressure of 0.5 MPa.

[0038] Take 20 ml of water for injection and cool it to 5°C, add poloxamer 188 at 2-10°C, mix well, and let it stand...

Embodiment 2

[0042] Example 2: Preparation of Semaglutide Injection Subcutaneous Implant

[0043] The prescription of the present embodiment is as follows (1000):

[0044] Element Dosage Semaglutide sodium salt 4.005g (equivalent to semaglutide 4g) N-(8-(2-Hydroxybenzoyl)amino)octanoic acid (NAC) 20g PLA (M=10000 Daltons) 40g Poloxamer 188 120g Mannitol 8g

[0045] PLA (M=10000) was completely dissolved in ethyl acetate to prepare a 5% PLA in ethyl acetate solution, and then semaglutide sodium salt and excipient N-(8-(2-hydroxybenzene) were added to it. Formyl)amino)octanoic acid (NAC), stir well, and prepare a PLA ethyl acetate solution containing semaglutide and excipient N-(8-(2-hydroxybenzoyl)amino)octanoic acid (NAC). The PLA microcapsules of semaglutide sodium were prepared by spray drying at 25° C. under a pressure of 1.0 MPa.

[0046] Take 20 ml of water for injection and cool it to 5°C, add poloxamer 188 at 2-10°C, mix well, and let...

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Abstract

The invention discloses a semeglutide implant and a preparation method thereof. The implant comprises semeglutide sodium salt, an auxiliary material N-(8-(2-hydroxybenzoyl) amino) caprylic acid, polylactic acid, a temperature-sensitive high-molecular polymer and a freeze-drying protective agent. The mass ratio of the semeglutide sodium salt to the auxiliary material N-(8-(2-hydroxybenzoyl) amino) caprylic acid to the polylactic acid to the temperature-sensitive high-molecular polymer to the freeze-drying protective agent is (0.5-5): (1-20): (2-10): (5-50): (0.5-10). The prepared semeglutide implant is a new dosage form of a sustained and controlled release preparation, and by adopting the implant, the clinical use frequency of injection of semeglutide once a week can be reduced to once a month, so that the medication convenience of a patient is greatly improved.

Description

technical field [0001] The invention belongs to the technical field of drug preparation, and particularly relates to a semaglutide implant and a preparation method thereof. technical background [0002] At present, the research and development of peptide drugs is a hot spot in the field of drug research, and the long-acting of peptide drugs is the current development trend of peptide drugs. [0003] For the long-acting of polypeptide drugs, in addition to improving the half-life of polypeptide molecules by chemical modification in structure, improving the dosage form of polypeptide preparations is also a very effective means of long-acting polypeptides. [0004] Semaglutide is a long-acting GLP-1 analog developed by Novo Nordisk. In 2017, its injection form was used to treat type 2 diabetes. It was first approved by the FDA and only requires subcutaneous injection once a week. Dosing. In June 2021, the indication of semaglutide injection for weight loss was approved by the...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K38/26A61K47/10A61K47/18A61K47/26A61K47/34A61P3/10
CPCA61K38/26A61K9/19A61K9/0019A61K47/34A61K47/26A61K47/183A61K47/10A61P3/10
Inventor 戴政清张凌云王宇恩马亚平
Owner 兰州积石药业有限公司
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