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Vermis expelling resinate and its preparation

A technology of anthelminth and resin, applied in the fields of praziquantel and exetel, which can solve the problems of strong sting, reluctance to eat, and high cost of capturing and injecting wild animals

Inactive Publication Date: 2004-09-22
ROHM & HAAS CO
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, injectable praziquantel has the disadvantage that the sting at the site of administration is so intense that it is common for animals to scratch the site of administration or howl immediately after injection
Capturing and injecting wild animals is very costly and not a viable option
Also, because of the bitter taste of praziquantel, wild animals are reluctant to consume food sources intentionally adulterated with praziquantel

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0057] The praziquantel is loaded on the cation exchange resin. - The resin used in this example is a weakly acidic methacrylic acid cation exchange resin with an exchange capacity of about 10.6 meq / g. Water (5.63 kg) and 95% ethanol (1.88 kg) were charged to a 10 liter flask equipped with a stirrer. The stirrer was started and resin (1.5 kg) was slowly added followed by praziquantel (175 g). When the praziquantel is fully dispersed, adjust the stirring speed to maintain the resin and praziquantel in a good suspension state. Stir overnight. After the stirring was stopped, the supernatant was removed by filtration. An additional 3.5 kg of water was added to the resin, the mixture was stirred for 5 minutes, and then the supernatant was removed by filtration. The washing step was repeated two more times. The resin is dried in a vacuum oven at 60-70 degrees Celsius until the water content is less than 5% w / w. The dried resin contained 9.9% w / w praziquantel based on mass bala...

Embodiment 2

[0059] Praziquantel release from resinate. - The resinate used in this example was prepared in a manner similar to Example 1 except that the resinate was not tested on drying. This resinate contained 9.3% w / w praziquantel (calculated on dry weight). To 10 ml of a solution containing the following components was added 273.3 mg of resinate:

[0060] 5.0% NaHCO 3

[0061] 2.35% NaCl

[0062] 0.75% KCl

[0063] Sufficient hydrochloric acid was added to adjust the pH to 7.0.

[0064] The mixture was shaken overnight. Observation of the mixture revealed the appearance of a white precipitate, which was confirmed to be praziquantel. Analysis of praziquantel in the supernatant revealed that the concentration of praziquantel was close to its saturation. This example shows that praziquantel is released from the resin at near neutral pH (resin is ionized).

Embodiment 3

[0066] Loading of praziquantel onto anion exchange resin. - The resin used in this example is a weakly basic anion exchange resin which exists in the free base form. This resin has an exchange capacity of about 10 meq / g. Add 100 mg of praziquantel to 15 g of 95% ethanol and shake until dissolved. Then 45 g of water were added thereto, followed by 3.1 g of resin (well hydrated). The mixture was shaken overnight at room temperature and filtered. The resulting resin contained 5.4% praziquantel (calculated on dry weight).

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PUM

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Abstract

The invention provides a pharmaceutical composition that includes a non-ionizable anthlemintic drug or derivative thereof loaded onto an anion exchange resin or a cation exchange resin. The non-ionizable anthlemintic is praziquantel, a praziquantel derivative, epsiprantel, or an epsiprantel derivative. The anthlemintic can also include Droncit, a derivative of Droncit, a precursor of Droncit, Drontal, a precursor of Drontal, a derivative of Drontal, Drontal Plus, a derivative of Drontal Plus, a precursor of Drontal Plus, a formulation comprising Praziquantel and Pyrantel Pamoate, and a formulation comprising Praziquantel, Pyrantel Pamoate and / or Febantel. In another variant, the invention includes a pharmaceutical composition including a basic anthlemintic drug loaded onto an anion exchange resin, or an acidic anthlemintic drug loaded onto a cation exchange resin, and a process for manufacturing the pharmaceutical composition.

Description

Background of the invention [0001] The present invention generally relates to compositions containing pharmacologically active anthelmintics loaded on ion exchange resins. In a particular variant, this patent application relates to a method of taste-masking of hexahydropyrazine derivatives, praziquantel and exetel, and taste-masked praziquantel and exetel. [0002] It is advantageous to use complexes of polymeric substances and anthelmintic active substances. These benefits include modification of the drug release rate, masking of the bitter taste of the drug, control of the site of administration, controlled release of flavoring substances and stabilization of labile substances. [0003] The preparation of the active material / ion exchange resin complex is called loading. Ion exchange resins compounded with active substances are called resinates. [0004] Basic drugs can be loaded onto cation exchange resins because basic molecules form cations, while acidic drugs can be lo...

Claims

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Application Information

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IPC IPC(8): A61K47/30A01N61/00A61K31/4985A61K31/55A61K45/00A61K47/48A61P33/10
CPCA61K47/48184A61K47/585A61P33/10A61P33/14A01N61/00
Inventor L·胡格斯W·A·齐亚诺
Owner ROHM & HAAS CO
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