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Atovaquone with a particle size diameter range (D90) of greater than 3 [mu]m to about 10 [mu]m

A technology of atovaquone and particle size is applied in the treatment of disease states for which atovaquone is effective, and these compositions are prepared. Atovaquone is used as an active ingredient in the field of compositions, which can solve problems such as unsuccessful particles.

Inactive Publication Date: 2011-06-22
ALPHAPHARM PTY LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the teachings in the aforementioned documents found that conventional methods by reducing the particle size of atovaquone could not be successfully used to produce particles of the size required to improve bioavailability

Method used

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  • Atovaquone with a particle size diameter range (D90) of greater than 3 [mu]m to about 10 [mu]m
  • Atovaquone with a particle size diameter range (D90) of greater than 3 [mu]m to about 10 [mu]m
  • Atovaquone with a particle size diameter range (D90) of greater than 3 [mu]m to about 10 [mu]m

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0060] 30 mg of atovaquone was placed in 900 mL of purified water with 3 drops of polysorbate 80, and after ultrasonic treatment for 10 minutes at a stirring speed of 400 rpm, the particle size of atovaquone was measured by a Malvern laser particle size analyzer.

[0061] D. 90 The results are shown in Table 1:

[0062] Table 1

[0063] Stirring time (minutes)

Embodiment 2

[0065] 30 mg of atovaquone was placed in 900 mL of purified water with 3 drops of polysorbate 80, and after ultrasonic treatment for 10 minutes at a stirring speed of 400 rpm, the particle size of atovaquone was measured by a Malvern laser particle size analyzer.

[0066] D. 90 The results are shown in Table 2:

[0067] Table 2

[0068] Stirring time (minutes)

Embodiment 3

[0070] 30 mg of atovaquone was placed in 900 mL of purified water with 3 drops of polysorbate 80, and after ultrasonic treatment for 10 minutes at a stirring speed of 400 rpm, the particle size of atovaquone was measured by a Malvern laser particle size analyzer.

[0071] D. 90 The results are shown in Table 3:

[0072] table 3

[0073] Stirring time (minutes)

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Abstract

Atovaquone or a pharmaceutically acceptable salt thereof having a particle size diameter range with a D90 of between greater than 3 to about 10[mu]m.

Description

technical field [0001] The present invention relates to pharmaceutical compounds comprising atovaquone having a specific particle size, and compositions comprising such atovaquone as an active ingredient. Furthermore, the present invention relates to the use of such compositions for the manufacture of medicaments for the treatment of disease states for which atovaquone is effective, and to processes for the preparation of these compositions. Background technique [0002] The compound trans-2-[4-(4-chlorophenyl)cyclohexyl]-3-hydroxy-1,4-naphthalenedione, hereinafter referred to as atovaquone, is described in U.S. Patent No. 5,053,432 (referred to as Assigned to Wellcome Foundation) made public for the first time. Atovaquone is an anti-pneumocystis agent with the following structure: [0003] [0004] Atovaquone has been shown to be useful in the prevention of Plasmodium falciparum malaria and in the treatment of acute uncomplicated P. falciparum malaria. [0005] Atovaq...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C50/32A61K31/122C07C46/10A61K9/14A61P33/06A61K9/50C07C46/00
CPCA61K31/122A61K45/06A61K9/2866A61K9/2027A61P33/06Y10T428/2982Y02A50/30A61K2300/00
Inventor 布莱特·安东尼·穆尼帕纳吉奥塔斯·克莱米达斯
Owner ALPHAPHARM PTY LTD
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