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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AI-Extracted 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

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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.

Application Domain

BiocidePharmaceutical non-active ingredients +4

Technology Topic

EpsiprantelDrug +4

Examples

Experimental program(5)

Example Embodiment

[0056] Example 1

[0057] Load praziquantel on a cation exchange resin. -The resin used in this example is a weakly acidic methacrylic acid cation exchange resin with an exchange capacity of approximately 10.6 meq/g. Water (5.63 kg) and 95% ethanol (1.88 kg) were charged into a 10-liter flask equipped with a stirrer. The stirrer was started and the resin (1.5 kg) was slowly added, followed by praziquantel (175 g). When the praziquantel is fully dispersed, the stirring speed is adjusted to maintain the resin and praziquantel in a good suspension state. Stir overnight. After the stirring was stopped, the supernatant was removed by filtration. Then 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 cleaning step is repeated two more times. The resin is dried in a vacuum drying oven at 60-70 degrees Celsius to a moisture content of less than 5% w/w. Based on the mass balance calculation, the dried resin contains 9.9% w/w praziquantel.

Example Embodiment

[0058] Example 2

[0059] Praziquantel is released from the resinate. ——The resinate used in this example was prepared in a manner similar to that of Example 1, except that the resinate was not tested for drying. This resinate contains 9.3% w/w praziquantel (calculated by dry weight). Add 273.3mg of resinate to 10ml of the solution containing the following components:

[0060] 5.0% NaHCO 3

[0061] 2.35%NaCl

[0062] 0.75%KCl

[0063] Add enough hydrochloric acid to adjust the pH to 7.0.

[0064] The mixture was shaken overnight. Observing the mixture, a white precipitate can be seen, confirming that it is praziquantel. The praziquantel in the supernatant was analyzed, and it was found that the concentration of praziquantel was close to its saturation. This example shows that praziquantel is released from the resin under conditions close to neutral pH (the resin is ionized).

Example Embodiment

[0065] Example 3

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

PUM

Description & Claims & Application Information

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