Pharmaceutical preparation for treating diabetes and preparation method thereof

A technology of drugs and compositions, applied in the field of polypeptide pharmaceutical preparations, can solve the problems of skin irritation and sensitization, and achieve the effects of convenient transportation and enhanced stability

Active Publication Date: 2014-07-02
HANGZHOU JIUYUAN GENE ENG +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0019] In general, propylene glycol is widely used and relatively saf

Method used

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  • Pharmaceutical preparation for treating diabetes and preparation method thereof
  • Pharmaceutical preparation for treating diabetes and preparation method thereof
  • Pharmaceutical preparation for treating diabetes and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0047] Example 1 Investigating the dissolution of liraglutide powder under different pH conditions

[0048] 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:

[0049] Table 1 Dissolution of the original powder in different pH solutions

[0050] The concentration of liraglutide Dissolution Water for Injection 6mg / ml insoluble 10mM Disodium Hydrogen Phosphate Buffer (pH7.00) 6mg / ml insoluble 10mM Disodium Hydrogen Phosphate Buffer (pH7.50) 6mg / ml Colorless and clear 10mM Disodium Hydrogen Phosphate Buffer (pH8.00) 6mg / ml Colorless and clear 10mM Disodium Hydrogen Phosphate Buffer (pH8.15) 6mg / ml Colorless and clear 10mM Disodium Hydrogen Phosphate Buffer (pH8.50) 6mg / ml Colorless and clear 10mM Disodium Hydrogen Phosphate Buffer (pH9.00) 6mg / ml Colorless and cl...

Embodiment 2

[0052] Example 2 Investigate the osmotic pressure of solutions containing different osmotic pressure regulators

[0053] Dissolve different osmotic pressure regulators in 10mM disodium hydrogen phosphate buffer solution, add liraglutide powder (6mg / ml) while stirring, and then adjust the pH value to pH8.15 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:

[0054] Table 2 Concentration and osmotic pressure test results of isotonic agent

[0055] Isotonic agent Osmolarity Negative control (no isotonic agent) 0.041 Methionine (15mg / ml) 0.141 Glycine (15mg / ml) 0.301 L-Arginine (25mg / ml) 0.322 Sodium chloride (8.6mg / ml) 0.307 Imported preparations 0.281

[0056] An isotonic solution has an osmolality of about 0.285-0.310 osmol / L.

Embodiment 3

[0057] Example 3 Investigate the stability of formulation solutions containing different stabilizers

[0058] Dissolve preservatives, isotonic agents and buffers 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:

[0059]

[0060] Table 3 Types and dosage of stabilizers

[0061] Preparation number Types of Stabilizers The amount of stabilizer 1 Polysorbate 80 0.02％ 2 Poloxamer 188 0.02％ 3 Polysorbate 80 + Poloxamer 188 0.01％＋0.01％ 4 Hydroxypropyl-β-cyclodextrin 2％ 5 Povidone K30 3% 6 PEG300 3% 7 Listed prescription for ...

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Abstract

The invention relates to a pharmaceutical preparation for treating diabetes and a preparation method thereof, and discloses a pharmaceutical composition containing a GLP-1 analogue. The pharmaceutical composition includes the GLP-1 analogue, a buffering agent, a stabilizer, an isoosmotic regulator and a preservative. The pharmaceutical composition has the advantages that through addition of some components which can be accepted by human bodies, the stability of physicochemical and biological activities of the GLP-1 analogue is enhanced, and thus the preparation suitable for clinical multi-injection is prepared. The preparation can effectively prevent the effective component GLP-1 analogue from failure or crystallization due to degradation, oxidation, precipitation and other factors, thereby being convenient for transportation, long-term preservation and clinical use.

Description

technical field [0001] The present invention relates to the field of polypeptide pharmaceutical preparations, more specifically, the present invention relates to a pharmaceutical preparation containing liraglutide. Background technique [0002] Liraglutide (liraglutide) chemical name Arg 34 , Lys 26 (N ε- (γ-Glu(N α -Hexadecanoyl))) GLP-1(7-37), is a fatty acid modified GLP-1 polypeptide analogue, and the modified drug has a plasma half-life of 13 hours after subcutaneous administration. The GLP-1 polypeptide chain sequence is similar to that of human GLP-1 (7-37), and the 34th lysine in the natural sequence of human GLP-1 is replaced by arginine, and its amino acid sequence is similar to glucagon-like Peptide-1 (GLP-1) has about 97% homology (Goke et al., J. Biol. Chem., 268:19650-55, 1993). The 16-carbon fatty acid is linked by a glutamic acid and the 26th lysine of the polypeptide, and its structure is as follows: [0003] [0004] As a GLP-1 analog, liraglutide ...

Claims

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Application Information

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IPC IPC(8): A61K38/26A61K47/34A61K47/02A61P3/10
Inventor 刘晓妮尚小广陈海红马国昌程睿
Owner HANGZHOU JIUYUAN GENE ENG
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