Tilidine dihydrogen orthophosphate, method of preparing it and p

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai

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560 48, A61K 31215, C07C21140

Patent

active

056936699

DESCRIPTION:

BRIEF SUMMARY
This is a 371 of PCT/EP93/02954 filed Oct. 25, 1993.


BACKGROUND OF THE INVENTION

The instant invention is for the new salt, tilidine dihydrogen orthophosphate, a process for its preparation and pharmaceutical trans-2-dimethylamino-1-phenyl-3-cyclohexene-trans-1-carboxylate)! is a commercially available analgesic which is enterally resorbed very quickly and is especially suitable for the treatment of very severe pains. For galenical compositions, salts of the basic active material are used since the base as such does not have sufficient stability over a comparatively long period of time. Until now for reasons of stability, even with the use of salts, it has not been possible to develop solid pharmaceutical forms, such as tablets or suppositories. Pat. No. 3,557,127!) has, in practice, proved to be useful as a salt for stable liquid compositions. It is commercially available in the form of a solution or of a portioned suspension in soft gelatin capsules under the trademark Valoron N. Because of its outstanding properties in combatting pain, Valoron N has become one of the leading analgesics in Germany. All endeavors to make available useful solid pharmaceutical forms of the active material tilidine have been unsuccessful because of the stability problems. There is a need for a useable solid galenical form of tilidine because only such a solid formulation can provide a controllable release of tilidine. Tilidine acts for a relatively short period of time and a uniform treatment of pain for a comparatively long period of time, with a single dose of active material is needed. Normal release, such as is provided by liquid compositions, is problematical. A sustained form would be a very great advance in the field of analgesics and especially where a uniform, high level of active material over a long period of time is required. Such a form would be useful in combatting chronic and severe painful conditions such as in the treatment of cancer and in the treatment of burns.


SUMMARY OF THE INVENTION

The present invention provides a tilidine salt which is stable in solid and sustained pharmaceutical compositions, especially in tablets, coated tablets, and suppositories. A process for the production of solid and sustained pharmaceutical compositions of this new salt is included.
The new salt is tilidine dihydrogen orthophosphate.
The invention covers a solid, sustained-release pharmaceutical composition comprising:
The pharmaceutical composition can also contain one or more agents for sustained release.
The composition is selected from: a tablet, a coated tablet, a capsule, a suppository, or a granulate.
Further, the invention involves a process for the preparations of tilidine dihydrogen orthophosphate comprising: water, and warming to from 30.degree.-50.degree. C., period of about 3 hours while adding seed crystals continuously,
A more preferred process for producing tilidine dihydrogen phosphate comprises: water, and warming to 35.degree.-45.degree. C., period of 3 hours while adding seed crystals continuously, with stirring, and L of 94% isopropanol.


BRIEF DESCRIPTION OF THE DRAWINGS



DETAILED DESCRIPTION

Surprisingly, we have now found that tilidine dihydrogen orthophosphate has outstanding stability and is the only salt suitable for the production of solid pharmaceutical compositions. In solid form, in combination with solid adjuvants, it undergoes practically no decomposition. Further, the new salt has surprising pharmaceutical-technological properties which are superior to the properties of other tilidine salts, such as, tilidine hydrogen sulfate or tilidine hydrogen fumarate. It can be prepared without special requirements as to the climate in the production rooms and the corrosion protection of the apparatus and tools used. Granulates, tablets, and suppositories can be produced which are storage stable not only chemically but also physically over a very long period of time.
In DE-1 923 619, (U.S. Pat. No. 3,649,628) it is mentioned in passing that basically substituted cyclohexenes can form salts wit

REFERENCES:
patent: 3557127 (1971-01-01), Satzinger et al.
patent: 4800083 (1989-01-01), Hom et al.
patent: 4933438 (1990-06-01), Bodor
patent: 5478577 (1995-12-01), Sackler et al.

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