Pharmaceutical forms for the oral administration of mesna

Details Pharmaceutical forms for the oral administration of mesna Pharmaceutical forms for the oral administration of mesna

1999-04-27

2001-11-27

Spear, James M. (Department: 1615)

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Tablets, lozenges, or pills

C424S465000, C424S474000, C424S489000, C424S490000

Reexamination Certificate

active

06322812

ABSTRACT:

This application is based on application no. 198 18 804.8 filed in Germany on Apr. 27, 1998, the content of which is incorporated hereinto by reference.
Mesna is a known antidote, which is employed for the prophylaxis of the urotoxicity of oxaphosphorines such as ifosphamide and cyclophosphamide. In addition to parenteral formulations, oral formulations are also already known.
Thus in U.S. Pat. No. 5,503,845, oral formulations in the form of tablets, pellets, capsules having an active compound content of up to >85% of mesna in combination with a preparation process of moist granulation with more than 30% of water, based on the amount of the solids employed, are described. Problems here are the long and uneconomical drying times to be expected as a result of the large amounts of water. Moreover, high amounts of water also lead to active compound instability.
Effervescent tablets with 10-80% of mesna are furthermore disclosed in U.S. Pat. No. 5,358,718. U.S. Pat. No. 5,262,169 describes tablets with 10-80% of mesna.
In both abovementioned patent specifications, the claimed composition is coupled with an alcoholic granulation process.
The use of organic liquids in granulation, however, is to be classified as problematical, since these substances are usually environmentally harmful, and moreover special arrangements are needed for employee protection.
EP 0468245 describes mesna tablets which contain 10-80% of mesna, in combination with various auxiliaries. Here too, a process for the production of these tablets by means of granulation in the presence of organic solvents is described. The same problems apply as with the abovementioned U.S. patents.
The object is thus to produce mesna tablets by means of a simple, economical production method and to do this, if possible, without the use of organic solvents.
Since mesna is administered in high doses, it is necessary for the oral mesna formulations to have an active compound content of over 80%.
Surprisingly, it was possible to achieve the object mentioned by producing pharmaceutical forms for oral administration in the form of tablets, film-coated tablets, pellets or granules comprising at least 88% of mesna, by granulation with up to 15% of water, based on the amount of solid employed, or pharmaceutical forms for oral administration in the form of tablets, film-coated tablets, pellets or granules comprising at least 80% of mesna by direct compression or compaction.
It is to be emphasized that the process for the production of pharmaceutical forms for oral administration in the form of tablets, film-coated tablets, pellets or granules by granulation, direct compression or compaction manages without the use of organic solvents.


REFERENCES:
patent: 5252341 (1993-10-01), Sauerbier et al.
patent: 5503845 (1996-04-01), Goede et al.
patent: 0 468 245 (1992-01-01), None

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