Pharmaceutical composition of piperazine derivatives

A composition and drug technology, applied in the direction of drug combination, drug delivery, pharmaceutical formulation, etc., can solve problems such as microbial contamination, and achieve the effect of avoiding dissolution

Active Publication Date: 2007-06-20
UCB FARCHIM
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, once the seal of the container is broken and the pharmaceutical composition is fully used for a period of time, each time the container is used and their lid is opened or closed, these pharmaceutical compositions are continuously exposed to environmental or Risk of microbial contamination in humans

Method used

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  • Pharmaceutical composition of piperazine derivatives

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040] Example 1. Antiseptic effect of cetirizine

[0041] Oral solutions and drops containing cetirizine are prepared. The composition is given in Table 1.

[0042] Table 1.- Cetirizine compositions

[0043] oral solution

drops

Cetirizine hydrochloride (mg)

1

10

70% sorbitol solution (mg)

450

-

Glycerin (mg)

200

250

Propylene Glycol (mg)

50

350

Sodium Saccharin (mg)

1

10

Banana spice (mg)

0.1754

-

Sodium acetate (mg)

4.2

10

Acetic acid

Add to pH 5

Add to pH 5

Purified water (ml)

add to 1

add to 1

[0044] Preservative efficacy tests of antimicrobial agents were carried out according to the European Pharmacopoeia (chapter 5.1.3.). Oral solution and drop samples were incubated with bacterial and yeast suspensions Pseudomonas aeruginosa ATCC 9027, Escherichia coli ATCC 8739, Staphylococcus aureus ATCC6538, Candida albican...

Embodiment 2

[0051] Example 2. Antiseptic effect of levocetirizine

[0052] Oral solutions and drops containing levocetirizine are prepared. The composition is given in Table 4.

[0053] Table 4.- Levocetirizine compositions

[0054] oral solution

[0055] Preservative efficacy tests of antimicrobial agents were carried out according to the European Pharmacopoeia (chapter 5.1.3.). Oral solution and drop samples were incubated with bacterial and yeast suspensions Pseudomonas aeruginosa ATCC 9027, Escherichia coli ATCC 8739, Staphylococcus aureus ATC C6538, Candida albicans ATCC 10231 and A. niger ATCC 16404. The number of viable microorganisms per ml of preparation is determined under the test conditions. The results are given in Tables 5 and 6.

[0056] Table 5.- Microorganism content in inoculated samples of oral solutions

[0057] time (days)

[0058] Table 6. Microbial content in the inoculated samples of the drops

[0059] time (days)

[0060] I...

Embodiment 3

[0061] Example 3. Antimicrobial preservative effect of parabens on aqueous solutions of cetirizine fruit

[0062] Oral solutions and drops containing cetirizine were prepared according to Example 1, but also containing a mixture of parabens (methylparaben / propylparaben in a weight ratio of 9 / 1) . The total amount of parabens was 0.15 mg / ml, 0.45 mg / ml, 0.75 mg / ml and 1.05 mg / ml. The antimicrobial preservation effect of these solutions and drops was determined according to the European Pharmacopoeia (Chapter 5.1.3.). The test results are given in Tables 7-14.

[0063] Table 7. Microorganism content in inoculated samples of oral solution containing 0.15 mg / ml paraben

[0064] time (days)

Pseudomonas aeruginosa fake sheet

Bacteria

Escherichia coli

bacillus

golden yellow

Staphylococcus

white rosary

bacteria

Aspergillus niger

Inoculum

5.5×10 5

4.6×10 5

4.0×10 5

3.7×10 5

2.3×10 6

0

5.1×1...

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PUM

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Abstract

The present invention relates to a liquid composition containing an active substance belonging to the family of substituted benzhydryl piperazines with reduced amounts of preservatives.

Description

Field of Invention [0001] The present invention relates to liquid pharmaceutical compositions comprising active substances such as cetirizine, levocetirizine and elerezine. Background of the Invention [0002] Many substances belonging to the substituted benzhydrylpiperazine family are known to have useful pharmacological properties. [0003] European Patent EP58146 in the name of UCB, S.A. describes substituted benzhydrylpiperazines having the following general formula, as well as pharmaceutically acceptable salts thereof: [0004] [0005] where L represents -OH or -NH 2 Group, X and X' represent hydrogen atom, halogen atom, C 1 or C 4 A linear or branched alkoxy group in position, or a trifluoromethyl group, m is equal to 1 or 2, and n is equal to 1 or 2. [0006] Among these compounds, 2-[2-[4-[(4-chlorophenyl)phenylmethyl]-1-piperazinyl]ethoxy]acetic acid (also known as cetirizine) and its two The antihistamine properties of the hydrochloride salt are also well ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K31/495
CPCA61K9/0048A61K31/495A61K9/0095A61K9/0043A61K47/14A61P37/08A61P43/00C07D487/04
Inventor D·法纳拉J·苏瓦尔特C·普兰M·迪勒斯
Owner UCB FARCHIM
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