Stable hydrated cephalosporin dry powder for oral suspension for

Details Stable hydrated cephalosporin dry powder for oral suspension for Stable hydrated cephalosporin dry powder for oral suspension for

1994-10-27

1997-02-04

Rose, Shep K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Particulate form

424485, 424488, 424489, 424490, 514202, 514782, A61K 910, A61K 914, A61K 31545, A61K 4700

Patent

active

055995578

DESCRIPTION:

BRIEF SUMMARY
This is a rule 371 application based on the priority date of PCT/US93/03856 filed Apr. 30, 1993.


BACKGROUND

This invention relates to a stable dry powder formulation of a hydrated cephalosporin, e.g., ceftibuten di-or trihydrate, which is suitable for use as a pharmaceutical composition in the form of an oral suspension product to treat bacterial infections..
U.S. Pat. No. 4,634,697 discloses ceftibuten, (+)-(6R,7R)-7-[(Z)-2-(2-amino-4-thiazolyl)-4-carboxycrotonamido]-8-oxo-5-t hia-1-azabicyclo[4.2.0]-oct-2-ene-2-carboxylic acid, a cephalosporin antimicrobial agent which exhibits antibacterial activity against a wide range of gram-negative and certain gram-positive bacteria.
U.S. Pat. Nos. 4,933,443 and 4,812,561 disclose that ceftibuten is stable in a (di-or-tri-)hydrate crystalline form and that a pharmaceutically effective amount of the (di or tri)hydrate can be incorporated into specially sealed hard gelatin capsules for oral administration.
There is still a need for a stable dry powder ceftibuten formulation suitable for suspension in water for oral administration. There is also a need for a simple efficient process for making such a stable dry powder ceftibuten formulation having an extended shelf life at temperatures of 25.degree. C. or less.


SUMMARY OF INVENTION

In accordance with the present invention there is provided a method of preparing a dry hydrated cephalosporin powder formulation which is resistant to air oxidation and dehydration is suitable for suspension in water to form a orally administerable product which comprises admixing at ambient temperature and humidity conditions a hydrated cephalosporin or a pharmaceutically acceptable salt thereof in the form of a dry solid powder with substantially dry pharmaceutically acceptable excipients selected from the group consisting of nonionic surfactants, suspending agents, thickening agents, opacificers, preservatives; and sweeteners to form a dry admixture, transferring the so-formed dry admixture to a sealable storage container opaque to incident visible radiation under an atmosphere containing no more than about 5 volume percent oxygen.
The present invention also provides a dry hydrated ceftibuten powder formulation suitable for constitution with a pharmaceutically acceptable carrier to form a pharmaceutical composition in a stable suspension oral dosage form comprising: about 7 to 14 weight percent water; oral dosage form selected from the group consisting of silicon dioxide and at least one of aluminum magnesium silicate, a mixture of microcrystalline cellulose and carboxymethyl cellulose in the ratio of 6:1 to 10:1 (w/w) and xanthan gum;
The present invention also provides a stable, dry hydrated ceftibuten powder formulation suitable for use as an oral suspension dosage form in water, which comprises:


______________________________________ Ingredients mg/g ______________________________________ (1) hydrated ceftibuten containing about About 65 to 7 to about 14.5% by weight about 150 of water (2) polysorbate 80 About 0.30 to about 0.50 (3) simethicone About 0.60 to about 1.0 (4) xanthan gum About 12 to about 20 (5) silicon dioxide About 8 to about 12 (6) titanium dioxide About 14 to about 22 (7) a water soluble preservative About 3 to 9 (8) a fruity flavoring agent, About 3 to 5 and (9) a sweetener or a sweetener q.s. to make composition 1 g ______________________________________
In a preferred embodiment, the present invention also provides a stable, dry hydrated ceftibuten powder formulation suitable for use as an oral suspension dosage form in water, which comprises:


______________________________________ Ingredients mg/g ______________________________________ (1) hydrated ceftibuten containing about 72-144 7 to about 14.5% by weight of water (2) polysorbate 80 About 0.4 (3) simethicone About 0.8 (4) xanthan gum About 16 (5) silicon dioxide About 10 (6) titanium dioxide About 18 (7) a water soluble preservative About 4 to 8 (8) a microencapsulated fru

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