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Pharmaceutical preparation containing exenatide

The technology of a pharmaceutical preparation and exenatide is applied in the field of stable pharmaceutical preparations of exenatide, and can solve the problems of affecting the quality of the medicine, affecting the curative effect, and difficult to ensure low-temperature storage conditions, etc.

Inactive Publication Date: 2012-06-13
HANGZHOU JIUYUAN GENE ENG
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, there are still many problems in the actual use of the existing preparation forms. Due to stability problems, exenatide medicaments need to be stored at low temperature, and the existing multi-dose packaging forms are difficult to ensure low-temperature storage conditions on the way out, thereby affecting drug quality. , which in turn affects the curative effect; long-term use of products containing preservatives may bring a lot of potential harm, etc.

Method used

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  • Pharmaceutical preparation containing exenatide

Examples

Experimental program
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Effect test

example 1

[0072] Preparation of Injectable Pharmaceutical Preparations Containing Exenatide

[0073] Take a certain amount of exenatide bulk drug, and calculate the final volume (V1) of the preparation when diluting it to 50 μg / ml based on the weight of the existing exenatide. According to V1, an appropriate amount of methionine was weighed and added to an appropriate amount of sterile water to dissolve, so that the content of methionine in the final preparation was 3% (W / V). Then add an appropriate amount of high-concentration sodium hydrogen phosphate-citrate buffer solution with a pH of 4.5, so that the final concentration of the buffer solution in the preparation is 20 mmol / L. Then put the weighed exenatide bulk drug into dissolution, and adjust the pH to 4.5 with 1mol / l HCL or 10% NaOH. Finally, add an appropriate amount of sterile water for dilution to make the final volume of the preparation reach V1, and use a 0.22 micron filter membrane to carry out sterile filtration of the p...

example 2

[0075] Stability comparison of different formulations of water for injection containing exenatide.

[0076] 1) Preparation prescription 1 (refer to BYTTA, the preparation product of exenatide that has been developed and marketed according to US patents (US6902744 and US7115569) preparation prescription)

[0077] Weigh 40g of mannitol and 2.2g of m-cresol and add them into 700ml of sterile water to dissolve, add 150ml of 0.2M acetic acid-sodium acetate buffer solution with a pH of 4.5, add the weighed 50mg of exenatide raw material into the solution, and use 1mol / l HCL or 10% NaOH to adjust the pH to 4.5. Finally, an appropriate amount of sterile water was added for dilution to make the final volume of the preparation reach 1000 ml, and the final concentration of exenatide was 50 μg / ml. The formulation was sterile filtered using a 0.22 micron filter. Fill in 0.2ml / bottle into 1ml prefilled needles, and the batch number is batch 01.

[0078] 1000 ml of a preparation with a ...

example 3

[0090] Screening Experiment of Exenatide Injection Storage Containers

[0091] Fill exenatide injection with 0.2ml / bottle into 1ml prefilled needles, vials and ampoules, respectively, and place them at -20°C and 4°C for investigation for two weeks, and take samples every week once. The two indicators, the adsorption of exenatide injection by the container and the utilization rate of the liquid by the container, were investigated.

[0092] 1. The adsorption effect of the container on exenatide injection: use RP-HPLC to detect the peptide content, and calculate the adsorption rate of the container on exenatide injection.

[0093] 2. The usage rate of the container for the liquid medicine: take 20 exenatide injections in different containers, weigh their total weight (W1) first, and then weigh their total weight after the liquid medicine is dispensed (W2), the total weight of the medicine that can be used (W3=W1-W2), the weight of 20×0.2ml exenatide injection is W4, then the us...

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Abstract

The invention discloses a pharmaceutical preparation containing exenatide. Besides the active constituent exenatide, the pharmaceutical preparation further contains 10-100mm of buffer with pH being 3-7 and adjuvants for enhancing stability of the exenatide. The invention has the advantages of preparing an exenatide preparation which is applicable to clinical application, in particular to injection and can be stably kept by adding a plurality of human acceptable constituents.

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): A61K38/17A61K9/08A61K9/19A61K47/10A61K47/16A61K47/20A61K47/26A61P3/10
Inventor 马国昌王同映徐飞虎沈玲刘晓妮孙汉栋黄岩山
Owner HANGZHOU JIUYUAN GENE ENG
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