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Medicinal preparation containing exenatide

A technology of pharmaceutical preparations and exenatide, which is applied in the field of stable pharmaceutical preparations of exenatide, which can solve the problems of affecting the curative effect, changing the dosage, and the stability of exenatide cannot be guaranteed, etc.

Inactive Publication Date: 2013-01-16
HANGZHOU JIUYUAN GENE ENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Therefore, if the stability of exenatide during storage cannot be guaranteed, it will lead to changes in the dosage and affect the efficacy

Method used

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  • Medicinal preparation containing exenatide
  • Medicinal preparation containing exenatide
  • Medicinal preparation containing exenatide

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0070] Example 1: Screening of preservatives

[0071] In order to study the stability of exenatide under the condition of adding different preservatives, the following experiments were carried out. The method is as follows: first prepare different preservative solutions, each solution contains 3% methionine and 20mM pH4.5 Disodium hydrogen phosphate-citric acid buffer solution, then weigh exenatide, add it to different preservative solutions and dissolve it into an exenatide preparation solution of about 250 μg / ml, and then adjust the pH with NaOH or HCl to 4.5. After the preparation, put it into a 25°C incubator for accelerated testing. Samples were taken every 2 weeks and tested by HPLC to observe the degradation of the samples. The specific results are shown in the table below.

[0072] Byetta prescription: Exenatide 250μg / ml + m-cresol 2.2mg / ml + 4% mannitol + 30mM acetate buffer

[0073] Table 6: Addition of different preservatives

[0074]

[0075] Table 7: Content...

example 2

[0078] Example 2: Screening of different concentrations of sodium benzoate

[0079] First prepare sodium benzoate solutions containing different concentrations, each solution contains 3% methionine and 20mM pH4.5 disodium hydrogen phosphate-citric acid buffer, then weigh exenatide, add it to different Dissolve in the preservative solution to form about 250 μg / ml exenatide preparation solution, then adjust the pH to 4.5 with NaOH or HCl. After the preparation, put it into a 25°C incubator for accelerated testing. Samples were taken every 2 weeks and tested by HPLC to observe the degradation of the samples. The specific results are shown in the table below.

[0080] Table 8: Periodic reverse-phase detection of the content of related substances

[0081]

[0082] Can get from above-mentioned result: the sodium benzoate of 0.005%-5% (especially 0.2%-2.0%) has antiseptic effect preferably, but consider that preservatives generally have certain poisonous effect to human body, the...

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Abstract

The invention provides a medicinal preparation containing exenatide suitable for multi-administration, which contains exenatide, buffer solution, pharmaceutically acceptable accessory and preservative, wherein the buffer solution can keep the pH value of the preparation in an aqueous solution state at 3.0 to 7.0; the accessory may be one or combination of glucose, sucrose, methionine, mannitol or glycine; and the preservative is selected from benzoic acid, sodium benzoate, potassium sorbate or acetone chloroform. The medicinal preparation has the advantages that the stability of physicochemical and biological activities of the exenatide is enhanced by adding a few components capable of being accepted by the human body, and then a preparation suitable for clinical use, particularly injection use is prepared.

Description

field of invention [0001] The invention relates to a stable pharmaceutical preparation of exenatide, which can be used for the treatment of diabetic patients. technical background [0002] Exenatide (exenatide or exendin-4) was first isolated from the saliva secretion of giant monster lizard (Heloderm suspectum) (Eng, J. et al., J.Biol.Chem., 265:20259-62, 1990; Eng, J. et al., J.Biol.Chem., 267:7402-05, 1992), this is a 39-amino acid polypeptide whose amino acid sequence is similar to that of glucagon-like peptide-1 (GLP- 1) It has about 53% homology (Goke et al., J. Biol. Chem., 268:19650-55, 1993), and its amino acid sequence structure is as follows: [0003] His-Gly-Glu-Gly-Thr-Phe-Thr-Ser-Asp-Leu-Ser-Lys-Gln-Met-Glu-Glu-Glu-Ala-Val-Arg-Leu-Phe-Ile-Glu-Trp- Leu-Lys-Asn-Gly-Gly-Pro-Ser-Ser-GIy-Ala-Pro-Pro-Pro-Ser [0004] Pharmacological studies have found that exenatide has a similar effect to GLP-1, that is, it can stimulate pancreatic β cells to secrete insulin. Ex...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K38/17A61K9/08A61K9/19A61P3/10
Inventor 马国昌周哲程睿方井晋王同映
Owner HANGZHOU JIUYUAN GENE ENG
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