Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Patent
1994-09-16
1996-09-17
Cintins, Marianne M.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
A61K 951, A61K 3119
Patent
active
055566383
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/DE92/01008, filed Dec. 4, 1992.
The invention relates to an immediate-effect medicament for the treatment of painful and/or inflammatory and febrile disorders, which contains flurbiprofen in addition to customary pharmaceutical excipients and auxiliaries, wherein the flurbiprofen is present in the form of a pharmaceutically administrable nanosol which, as excipient, essentially contains gelatin, a collagen hydrolyzate or a gelatin derivative, the nanosol
a) having an inner phase of flurbiprofen which has a particle size of 10-800 nm and possesses a surface charge,
b) an outer phase of gelatin, a collagen hydrolyzate or a gelatin derivative, which is oppositely charged, and
c) an approximately or completely isoionic charge state of the inner and outer phase and
d) being physiologically absorbable.
The invention furthermore relates such a medicament which is present partially as an immediate-effect form and partially as a sustained-release form, and the use of a pharmaceutically administrable nanosol of flurbiprofen, which is present to more than 50% as S- or R-flurbiprofen, for the preparation of an analgesic and/or antirheumatic and/or antipyretic having an immediate effect.
Nonsteroidal antirheumatics are proven substances in the therapy of rheumatic disorders and in the symptomatic therapy of pain and of fever. The common mechanism of action for analgesia, the anti-inflammatory action and the antipyretic action is based on the inhibition of prostaglandin synthesis.
The 2-arylpropionic acid derivative flurbiprofen (2-(2-fluoro-4-biphenylyl)propionic acid C.sub.15 H.sub.13 FO.sub.2) having the following structure ##STR1## is of particular importance as a representative of this indication group because of its relatively low individual dose of 50 or 100 mg compared with its structural relatives, such as e.g. ibuprofen. Fundamentally, it can be said that a development in the dose reduction trend also comprises an optimization of the medicament safety. The findings of pharmacological research verify that the effective potential of this substance can additionally be increased to an appreciable extent by the use of its optical antipodes:
To be precise, it was found that a pronounced analgesic action is to be ascribed to R-flurbiprofen and a marked anti-inflammatory action to S-flurbiprofen. This finding makes possible selective use in therapy. A further dose reduction accompanies this with the same activity, so that individual-dose immediate-effect forms containing 25, 50 and 100 mg of R- or S-flurbiprofen can be called the painkillers of the future.
In the customary, non-stereospecific synthesis flurbiprofen is formed as a racemate. It is known that the racemate has significant undesirable side effects. The use of the enantiomerically pure flurbiprofens also makes possible, in addition to the lowering of the dose, the reduction of undesirable effects. Since the introduction of large-scale production processes for the enantiomerically pure substances, nothing more now stands in the way of extensive therapeutic use.
The following interesting view is a point in the favor of the use of pseudoracemates of flurbiprofen:
A synthetic mixture (pseudoracemate, mixed from 50% each of the S- and the R-enantiomer) of flurbiprofen behaves with respect to its dissolution rate (release) in aqueous medium differently than the racemic flurbiprofen, consisting of 50% each of S- and R-enantiomer, obtained in the customary synthesis. Actually, the dissolution rate of the pseudoracemate is substantially higher than that of the racemate. As a result of this, investigations show that after administration of the pseudoracemate substantially higher blood levels were achieved than after administration of the racemate.
In spite of all efforts, however, there has still been no success in developing a pharmaceutical formulation for flurbiprofen which fulfills all requirements of an immediate-effect form having a rapid influx.
Racemic flurbiprofen having a solubility of 32.5 mg per liter of water, its enantio
REFERENCES:
patent: 4888178 (1989-12-01), Rotini et al.
Lukas Helmut
Schick Ursula
Schuster Otto
Wunderlich Jens-Christian
Alfatec Pharma GMBH
Cintins Marianne M.
MacMillan Keith
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