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Stability for injection solutions

a technology of stable solution and injection solution, which is applied in the direction of chemical treatment enzyme inactivation, drug composition, pharmaceutical packaging, etc., can solve the problems of shortened storage time and increased degradation, and achieve the effect of improving the stableness of low molecular weight thrombin inhibitors in solution

Inactive Publication Date: 2006-10-19
LUNDGREN ANNA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The present invention provides a solution for improving the stability of low molecular weight thrombin inhibitors in solution for injection. By using rubber material containing bromobutyl instead of chlorobutyl, the stability of the thrombin inhibitors can be significantly improved. The invention also provides a primary package containing the thrombin inhibitor solution, which can be sealed with a rubber stopper or plunger containing bromobutyl. The thrombin inhibitor can be a low molecular weight peptide-based thrombin inhibitor, such as inogatran or melagatran. The invention is useful for improving the stability of thrombin inhibitors in solution for injection.

Problems solved by technology

Solutions of low molecular weight thrombin inhibitors stored in vials, bottles, cartridges and prefilled syringes sealed by a stopper or plunger containing chlorobutyl rubber exhibits increased degradation, leading to shortened time of storage.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

example 2

[0030] This example is a comparison of melagatran in a water solution of HPβCD and melagatran in a water solution of NaCl. Both solutions are in direct contact with rubber plungers bromobutyl.

[0031] 3 plungers of the quality FM 257 (from Helvoet Pharma N.V.) were placed in each 3 ml glass vial together with 1 ml solution of melagatran (NaCl water solution and HPβCD water solution, respectively). Reference samples, that is melagatran in NaCl water solution and in HPβCD water solution having no contact with plunger material. The reference samples were treated in the same way as the other samples. The vials were stored at 50° C. for up to 3 months.

[0032] Compared to the study of Example 1 the ratio between solution exposed plunger surface and the quantity of melagatran solution is 16 times higher.

Manufacturing of Samples

Melagatran, 7.5 mg / ml, in HPβCD Water Solution (40% w / w), pH About 5.

[0033] Batch HF 839-2679

Melagatran928.8 mgHPβCD55.0 gHCl, 1 MqsNaOH, 1 Mqswater for inject...

example 3

[0054] This example shows a comparison of different kinds of stopper and plunger materials containing either bromobutyl rubber or chlorobutyl rubber in contact with a melagatran solution (NaCl, pH 5). Melagatran solution was filled in glass vials (3 ml) together with stoppers and plungers of different brands. 5 different rubber materials were used in the study. There were 3 different bromobutyl and 2 different chlorobutyl rubbers. As reference, NaCl water solution of melagatran was stored without any contact with stopper or plunger material.

[0055] The ratio between exposed plunger or stopper surface and melagatran in water solution is higher than in Example 1. A calculation has been made of exposed area of each tested plunger or stopper material. In the study the area ratio is 10-15 times higher compared to the area represented in Example 1. The vials were studied up to 19 days at a temperature of 50° C.

Manufacturing of Samples

Melagatran, 5 mg / ml, in Isotonic NaCl Solution, pH ...

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Abstract

A primary package containing a low molecular weight peptide-based thrombin inhibitors which package is sealed with a rubber stopper or plunger containing bromobutyl rubber.

Description

FIELD OF THE INVENTION [0001] The present invention relates to solutions of low molecular weight thrombin inhibitors stored in primary packages containing rubber components, such as vials, bottles, cartridges and prefilled syringes. The invention also relates to the medical use of such stored thrombin inhibitor solutions. BACKGROUND OF THE INVENTION [0002] Solutions for parentheral use of pharmaceutically active substances are normally stored in primary packages such as, vials, bottles, cartridges or in prefilled syringes. The primary packages are sealed by a rubber stopper or plunger. A commonly used rubber material contains chlorobutyl. Solutions of low molecular weight thrombin inhibitors stored in vials, bottles, cartridges and prefilled syringes sealed by a stopper or plunger containing chlorobutyl rubber exhibits increased degradation, leading to shortened time of storage. DISCLOSURE OF THE INVENTION [0003] It has now surprisingly been found that by using rubber material conta...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K38/54A61K31/724B65D85/42A61J1/00C12N9/99A61J1/05A61J1/06A61J1/14A61K9/00A61K9/08A61K38/02A61K38/55A61K47/40A61L33/14A61M5/31A61P43/00
CPCA61J1/05A61J1/062A61J2001/1468A61M5/3129A61K31/724A61K47/40A61K9/0019A61J1/1468A61P43/00
Inventor LUNDGREN, ANNASUNDGREN, MATS
Owner LUNDGREN ANNA
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