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PHARMACEUTICAL COMPOSITION

IP.com Disclosure Number: IPCOM000173303D
Publication Date: 2008-Jul-30
Document File: 7 page(s) / 675K

Publishing Venue

The IP.com Prior Art Database

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PHARMACEUTICAL COMPOSITION

This disclosure describes pharmaceutical composition comprising compound of formula (I)

Compound (I) is a broad-spectrum insecticide that disrupts the insect's central nervous system and it is used to control cockroaches, ants, fleas, mole crickets, ticks, mites, subterranean termites, and agricultural pests. It is found in fleas and ticks treatments on cats and dogs and for fleas in their environment, and roach and ant bait traps for indoor use in both residential and commercial settings. Compound (I) may also be applied outdoors for ornamentals, lawns and on rice and corn crops.

Ingredients

Quantity (mg)

1

2

3

4

5

Compound (I)

100,00

100,00

100,00

100,00

100,00

Povidone

50,00

50,00

50,00

/

50,00

Ethanol

/

/

/

/

79

Polysorbate 80

50,00

50,00

50,00

/

50

Butyl hydroxytoluene (BHT)

0,10

0,10

0,10

0,10

0,1

Butyl hydroxyianisole (BHA)

0,20

0,20

0,20

0,20

0,2

Diethylene glycol monoethyl ether

/

/

/

/

up to

1 mL

Polyethylen glycol

/

50

/

50

/

Dimethyl sulfoxide

up to 1 mL

up to  1 mL

/

/

/

Glycerol

/

/

1 mL

1 mL

/

Manufacturing procedure is as follows:

Antioxidants (BHT, BHA) are dissolved in part of the solvent. Other ingredients are added and dissolved and as a final ingredient compound (I) is added and dissolved. In the last step the remaining solvent is added up to the final volume. In example 5 polyvinylpyrolidone is separately mixed and dissolved in ethanol and added to the solution with the other ingredients. The solution is mixed for a period of time (until all ingredients are dissolved). The final solution is filtered.

Compound (I) can be prepared by known methods such as methods disclosed in EP295117, EP668269, IN178903, WO0130760, CN1374298, WO 2004010785, WO2003064384, WO2000059862, WO2007069254, WO2007122440, WO2008055881, WO2008055882, WO2008055883, WO2008055884, US5232940, EP352944, IP156770. Compound (I) used in the preparation of  compositions described above can be in any crystal form such as crystal forms described in WO2007122440, WO2008055881, WO2008055882, WO2008055883, WO2008055884. Crystal form II and crystal form I are shown bellow.

XRPD pattern of compound (I) form II according to WO2007069254

No.

Pos. [°2Th.]

Rel. Int. [...