Immediate-effect ibuprofen-containing medicament and its use

Details Immediate-effect ibuprofen-containing medicament and its use Immediate-effect ibuprofen-containing medicament and its use

1995-12-01

2000-05-23

Page, Thurman K.

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Tablets, lozenges, or pills

424451, 424456, 424465, A61K 920, A61K 948, A61K 964

Patent

active

060663324

DESCRIPTION:

BRIEF SUMMARY
The invention relates to an immediate-effect medicament for the treatment of painful and/or inflammatory and febrile disorders, which contains ibuprofen in addition to customary pharmaceutical excipients and auxiliaries, wherein the ibuprofen is present in the form of a pharmaceutically administrable nanosol which, as excipient, essentially contains gelatin, a collagen hydrolyzate or a gelatin derivative.
The invention furthermore relates to such a medicament which contains ibuprofen as the immediate-effect form. The invention finally relates to the use of a pharmaceutically administrable nanosol of ibuprofen for the preparation of medicaments having an immediate analgesic and/or antirheumatic effect.
The different syndromes of the rheumatic type include, inter alia, disorders such as rheumatoid arthritis, osteoarthritis and rheumatic polymyalgia. Symptomatic therapy with nonsteroidal antirheumatics in this case primarily brings about the elimination of pain and furthermore the inhibition of inflammatory processes of the affected joints. The third activity component relates to the anti-inflammatory activity, which is accompanied by an improvement in mobility, and the stopping of the progressive course of the disease.
The nonsteroidal antirheumatics group includes a multiplicity of various classes of substance, to which mainly the acid character of the individual active compound is common.
Ibuprofen (2-(4-isobutylphenyl)propionic acid C.sub.13 H.sub.18 O.sub.2) of the following structure ##STR1## is a known painkiller and antirheumatic agent from the 2-arylpropionic acid group. Normally, ibuprofen is obtained during chemical synthesis as a racemate. It is known that the racemate has appreciable adverse side effects. Pharmacological research in recent years has verified that the use of the enantiomerically pure ibuprofens is accompanied by great advantages with respect to the reduction of undesired effects and a lowering of the dose. The newly developed large-scale preparation of pure enantiomers now makes possible for these substances not only extensive use in therapy, but also new possibilities in the combination of the enantiomers with one another. As modern painkillers and antirheumatic agents, the enantiomerically pure active compounds are increasingly gaining importance. Leading pharmacologists are making the demand to employ only the eutomer of racemic substance mixtures, i.e. the enantiomer having the desired effect, and to remove the distomer with undesired effect. In the case of ibuprofen both enantiomers can be ascribed specific effects: S-ibuprofen primarily has peripheral effect, while the enantiomer R-ibuprofen obviously possesses central activity.
A further interesting effect applies to the use of pseudoracemates of ibuprofen:
It is known of the structurally related 2-arylpropionic acid derivative flurbiprofen that an artificial mixture (pseudoracemate, mixed from 50% each of the S- and the R-enantiomers) behaves differently with respect to its rate of dissolution (release) in aqueous medium than the racemic flurbiprofen consisting of 50% each of S- and R-enantiomers and which is obtained in the customary synthesis. Actually, the rate of dissolution of the pseudoracemate is substantially higher than that of the racemate.
X-ray diffractometer investigations have shown for ibuprofen that the pure enantiomers in each case crystallize in different crystal lattices than the racemate. Furthermore, fairly large differences can be found in the melting point (racemate: 75-77.5.degree. C., S-ibuprofen: 51-52.degree. C.), in the solubility (racemate: 4.8 mg in 100 ml of water at 37.degree. C., in contrast to this under identical conditions S-ibuprofen 11.8 mg), and in the rate of solution between the racemates, the individual enantiomers and the pseudoracemates, such that the effect described above is even more greatly pronounced with ibuprofen than with flurbiprofen. As a result of this, investigations show that after administration of the pseudoracemate substantially higher blood levels were achieved t

REFERENCES:
patent: 5415871 (1995-05-01), Pankhania et al.

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