A pharmaceutical preparation containing glp-1 analogs and its preparation method

A drug and composition technology, applied in the field of polypeptide pharmaceutical preparations, can solve problems such as skin irritation and sensitization

Active Publication Date: 2018-06-26
HANGZHOU JIUYUAN GENE ENG +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0025] In general, propylene glycol is widely used and relatively safe, but it still has potential irritation and sensitization to the skin

Method used

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  • A pharmaceutical preparation containing glp-1 analogs and its preparation method
  • A pharmaceutical preparation containing glp-1 analogs and its preparation method
  • A pharmaceutical preparation containing glp-1 analogs and its preparation method

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0074] Example 1 Investigating the dissolution of liraglutide powder under different pH conditions

[0075] Dissolve an appropriate amount of liraglutide original powder in water for injection and disodium hydrogen phosphate buffer with different pH, and the dissolution conditions are shown in Table 1.

[0076] Table 1 Dissolution of the original powder in different pH solutions

[0077]

[0078]

[0079] From the above tests, it can be seen that the original powder of liraglutide does not dissolve under acidic and neutral conditions, but only dissolves under alkaline conditions.

Embodiment 2

[0080] Example 2 Investigate the osmotic pressure of solutions containing different osmotic pressure regulators

[0081] Dissolve different osmotic pressure regulators in 10 mM disodium hydrogen phosphate buffer solution, add liraglutide powder (6 mg / ml) while stirring, and then adjust the pH value to pH 8.15 with sodium hydroxide. Finally, the above solutions were filtered with 0.22 μm filters, respectively. The test results of the concentration and osmotic pressure of each solution isotonic agent are shown in Table 2:

[0082] Table 2 Concentration and osmotic pressure test results of isotonic agent

[0083] Isotonic agent

[0084] An isotonic solution has an osmolarity of about 0.285 to 0.310 osmol / L.

Embodiment 3

[0085] Example 3 Investigate the stability of formulation solutions containing different stabilizers

[0086] Dissolve the preservative, isotonic agent and buffer in water for injection, dissolve the original powder of liraglutide in the above solution while stirring slowly, and then adjust the pH to the required pH with sodium hydroxide and / or hydrochloric acid , respectively adding a certain amount of stabilizer. Finally, the above formulation solution was filtered with a 0.22 μm filter. The kind and consumption of adding stabilizer are shown in Table 3, and the composition of preparation is as follows:

[0087]

[0088] Table 3 Types and dosages of isotonic agents and stabilizers

[0089]

[0090] The above preparations were placed at 37°C, 25°C and 4°C for stability investigation, and the related substances of the samples were detected by HPLC (area normalization method). The specific results are as follows:

[0091] Table 4 Stability investigation results at 37°...

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Abstract

The invention discloses a pharmaceutical composition containing GLP-1 analogues, including GLP-1 analogues, buffers, stabilizers, isotonic regulators and preservatives. The advantage of the present invention is that by adding some ingredients acceptable to the human body, the stability of the physical, chemical and biological activities of the GLP-1 analog is enhanced, thereby preparing a preparation suitable for clinical multiple injections. This preparation can effectively prevent the active ingredient GLP‑1 analog from failing or crystallizing due to degradation, oxidation, precipitation and other factors, thereby facilitating transportation, long-term storage and clinical use.

Description

technical field [0001] The invention relates to the field of polypeptide pharmaceutical preparations, more specifically, the invention relates to a pharmaceutical preparation containing GLP-1 analogues and a preparation method thereof. Background technique [0002] In the 1960s, McIntyre (McIntyre) and Elrick (Elrick) and others found that oral glucose had a significantly higher effect on insulin secretion than intravenous injection, and this additional effect was called "incretin stimulation". Incretin effect". With the development of cell and molecular biology, studies have confirmed that incretin is a gut-derived hormone in the human body. After eating, this type of hormone can promote insulin secretion and exert a glucose concentration-dependent hypoglycemic effect. [0003] Incretins are mainly composed of glucagon-1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP), among which GLP-1 plays a more important role in the occurrence and development of type 2 diabe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/26A61K9/08A61K47/10A61P3/10
CPCA61K47/10A61K9/08A61K47/26A61K38/26A61P3/10A61K9/0019A61K47/02
Inventor 刘晓妮李寒星陈潮梁马国昌徐飞虎王同映孙汉栋
Owner HANGZHOU JIUYUAN GENE ENG
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