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A suspension comprising benzimidazole carbamate and a polysorbate

A technology of benzimidazole carbamate and composition, applied in the field of suspension containing benzimidazole carbamate and polysorbate, capable of solving problems such as inability to administer drugs

Active Publication Date: 2012-11-21
INTERVET INT BV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] International patent application WO 95 / 16447 discusses anti-helminth compositions for oral administration comprising micronized particles of rafoxanide and fenbendazole, more than 98% of these particles having a particle size below 20 microns average particle size of , but the composition cannot be administered in the drinking water system

Method used

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  • A suspension comprising benzimidazole carbamate and a polysorbate
  • A suspension comprising benzimidazole carbamate and a polysorbate
  • A suspension comprising benzimidazole carbamate and a polysorbate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0108] Embodiment 1 Preparation of the fenbendazole composition of the present invention

[0109] A 0.2 g / ml fenbendazole (FBZ) drinking water suspension was prepared using the following three preparation steps: a) preparation of a premixed suspension (0.4 g / ml FBZ), b) wet milling of the premixed suspension and c) dilution The suspension was premixed to give the final product (0.2 g / ml FBZ).

[0110] Formulation of the final product (0.2g / ml FBZ suspension)

[0111] substance quantity Fenbendazole 20.0g Polysorbate 80 10.0g Benzyl alcohol 2.0g Simethicone Emulsion 0.5g water Add to 100ml

[0112] A. Preparation of Premixed Suspension

[0113] Mix the required amount of simethicone emulsion and polysorbate 80 in some water using a magnetic stirrer. In order to obtain a homogeneous mixture, it was heated moderately (less than 60°C). The required amount of fenbendazole and the remaining volume of water were then added under ...

Embodiment 2

[0122] Embodiment 2 Preparation of flubendazole composition of the present invention

[0123] A 0.2 g / ml flubendazole (FluBZ) drinking water suspension was prepared using the following three preparation steps: a) preparation of a premixed suspension (0.4 g / ml FluBZ), b) wet grinding of the premixed suspension and c) dilution The premixed suspension was triturated to give the final product (0.2 g / ml FluBZ).

[0124] Formulation of the final product (0.2g / ml FluBZ suspension)

[0125] substance quantity supplier Flubendazole 20.0g Transchem Polysorbate 80 10.0g Merck Benzyl alcohol 2.0g Fluka Simethicone Emulsion 0.5g Dow Corning pure water Add to 100ml -

[0126] A. Preparation of Premixed Suspension

[0127] Mix the required amount of simethicone emulsion and polysorbate 80 in some water using a magnetic stirrer. In order to obtain a homogeneous mixture, it was heated moderately (less than 60°C). The required am...

Embodiment 3

[0142] Example 3 Alternative Wet Milling by Recirculation of Premixed Suspension - Continuous Process

[0143] First, give A 0.6 L container of MILL KDL A was filled with 450 mL of 0.25-0.3 mm glass beads (supplier B. Braun Biotech International) and then 270 mL of the premixed suspension prepared in Step A of Example 1 or 2 was added.

[0144] The milling vessel was then connected to a pump to continuously feed the mill with the premixed suspension; the flow rate was set at about 1.3 L / h. One cycle of wet milling was completed after the premixed suspension in its intact form (500 mL) was passed through the mill, separated from the milling media by a 0.1 mm gap and drained into a new container. 6 milling cycles with polyurethane discs and 4200 rpm were applied to the suspension premix.

[0145] During wet milling, the product temperature was maintained below 50°C due to heat transfer using a double cooling jacket.

[0146] The particle size of the fenbendazole suspension ...

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Abstract

This invention is directed to a pharmaceutical composition for drinking water administration comprising benzimidazole carbamate particles having an effective average particle size of less than 450 nm and a Tween-type surfactant; a method for making the composition; use of the composition to make a medicament for controlling parasites; and use of said composition for the manufacture of a medicament or protecting an animal from a parasitic infection. The invention also provides a method for protecting an animal from a parasitic infection.

Description

field of invention [0001] The present invention generally relates to a pharmaceutical composition comprising a benzimidazole carbamate for administration using drinking water, a process for the preparation of the pharmaceutical composition, the use of the composition in the manufacture of a medicament for controlling parasites in animals and the use of the combination A method of preventing parasitic infections in animals. Background of the invention [0002] Benzimidazoles were originally developed as phytofungicides and subsequently as anthelmintics (eg, anthelmintics) for veterinary and human use. The family of benzimidazoles with antihelminth activity includes thiazolyl benzimidazoles and benzimidazole carbamates. Benzimidazoles exhibit a broad-spectrum activity especially against helminth parasites such as roundworms or tapeworms. [0003] Well-known benzimidazoles with antihelminthic activity are, for example, thiabendazole; cambendazole; and benzimidazole carbamates...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/415A61K9/00A61K9/10
CPCA61K9/10A61K9/0095
Inventor E·B·D·德斯查姆普斯C·施米特M·阿尔兰
Owner INTERVET INT BV