preparation
A formulation, stabilizer technology, applied in the field of invasive injectable formulations, which can solve problems such as low bioavailability
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example 1
[0185] Hexaflumuron was studied as an example of a water-insoluble parasiticide.
[0186] The solubility of hexaflumuron in common solvents methanol, water and xylene has been investigated previously and the results are shown in Table 1. Hexaflumuron is not sufficiently soluble in these solvents for the purpose of producing a stable solution suitable for intraperitoneal injection.
[0187] Table 1
[0188] solvent Solubility of hexaflumuron (mg / ml) water 2.7x 10 -5
[0189] Tomlin, C.D.S. (ed.) The Pesticide Manual-World Compendium, 11th ed., British Crop Protection Council, Surrey, England 1997, p. 676.
[0190] To generate formulations in which hexaflumuron was present in a stable solution, the solubility of hexaflumuron in various other solvents was investigated. Solubility was determined by gradually adding each solvent to a specified mass of hexaflumuron until complete dissolution was observed. The resulti...
example 2
[0196] The safety of formulations of parasiticides prepared in polar solvents for intraperitoneal injection into Atlantic salmon was tested.
[0197] Juvenile Atlantic salmon (average size: 35.5 g) maintained in freshwater (17°C) were injected with one of 10 formulations containing DMSO as an example polar solvent, excipients containing propylene glycol (PG), dose and a certain amount of hexaflumuron ranging from 0 to 100 mg / ml (see Table 3). The 10 groups each contained 30 fish.
[0198] table 3
[0199]
[0200] figure 1 . Mortality of Atlantic salmon juveniles injected with the formulations shown in Table 3. .
[0201] Mortality in the injected group was recorded. Low to moderate mortality was observed in all groups injected with a volume of 0.05 ml, independent of hexaflumuron concentration. Mortality increased dramatically with injection volume, reaching >90% when the injection volume was 0.2ml. This mortality rate was independent of the presence of hexaflumuron ...
example 3
[0213] In Example 2, it was demonstrated that the unacceptable toxicity induced by the solution based formulation was due to the polar solvent (DMSO) in the formulation, not the parasiticide content. Replacing DMSO with other polar solvents did not address the toxicity challenge (see Table 5).
[0214] In view of this, in an attempt to produce a formulation with reduced toxicity, a formulation in which the proportion of the polar solvent in the formulation was decreased while increasing the proportion of the excipient PG was produced. PG was previously found to be safe following intraperitoneal injection in Atlantic salmon (see Table 5).
[0215] However, as shown in Table 2, the solubility of hexaflumuron in PG was found to be very low. It was therefore found impossible to adjust the relative proportions of PG and DMSO sufficiently to obtain a formulation in which the parasiticide is soluble and does not induce unacceptable levels of toxicity in fish.
[0216] This problem ...
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