Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Capsules
Patent
1994-09-29
1996-10-01
Acquah, Samuel A.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Capsules
424455, 424456, 424458, 424462, 514513, 514568, A61K 948
Patent
active
055609244
DESCRIPTION:
BRIEF SUMMARY
This application is 371 of PCT/DE 92/01012 Dec. 4, 1992.
The invention relates to an immediate-effect medicament for the treatment of painful and/or inflammatory, and also febrile, disorders which as active compound contains a 2-arylpropionic acid derivative in the form of a pharmaceutically administrable nanosol and as excipient essentially contains gelatin, a collagen hydrolyzate or a gelatin derivative in addition to customary pharmaceutical auxiliaries.
The invention furthermore relates to the use of a pharmaceutically administrable nanosol of a 2-arylpropionic acid derivative for the preparation of medicaments having immediate analgesic and/or antirheumatic, and also antipyretic, effect..
The invention finally relates to a process for the preparation of a colloidally disperse system of a 2-arylpropionic acid derivative.
Nonsteroidal antirheumatics (NSAR), such as, for example, the active compounds from the substance class of the salicylic acid derivatives (acetylsalicylic acid), indolylacetic acid derivatives (indometacin), phenylacetic acid derivatives (diclofenac) and oxicams (piroxicam) are employed for the symptomatic therapy of disorders of the rheumatic type. These include, inter alia, rheumatoid arthritis, degenerative forms such as arthroses and spondyloses, and also rheumatic polymyalgia. A differentiation is essentially made between two principal effects: on the one hand the analgesic and antipyretic effect and on the other hand the pronounced antirheumatic/anti-inflammatory effect, which are both based on inhibition of prostaglandin synthesis. With such a therapy, the quality of life of the patients, first and foremost the freedom from pain and the conservation of or improvement in the mobility as well as the chronic progressive course of the disease are favorably affected.
Recently, the pharmacologically active NSAR from the 2-arylpropionic acid derivatives group have gained increasing importance as modern painkillers and antirheumatic agent. Thus in 1987 the painkiller ibuprofen 2-(4-isobutylphenyl)propionic acid or .alpha.-methyl-(2-methylpropyl)phenlacetic acid, C.sub.13 H.sub.18 O.sub.2 already had a 13% share in the total world analgesics market in the non-prescription area alone. Furthermore, the consumption of ibuprofen-containing medicaments rose distinctly in Germany after release from prescription status and ibuprofen is today already described as the painkiller of the 90s.
In addition to ibuprofen, in the coming years the analgesic and antirheumatic structurally related compounds which all possess an asymmetric carbon atom, such as e.g. flurbiprofen, 2-(2-fluoro-4-biphenylyl)propionic acid C.sub.15 H.sub.13 FO.sub.2, whose racemate is already given in anti-rheumatic therapy at a distinctly lower dose (recommended daily dose 150-200 mg) than racemic ibuprofen (up to 2400 mg daily), ketoprofen, 2- (3-benzoylphenyl)propionic acid C.sub.16 H.sub.14 O.sub.3, and tiaprofen acid, 2-(5-benzoyl-2-thienyl)propionic acid C.sub.14 H.sub.12 O.sub.3 S, will become the focus of interest. S-Naproxen, (S)-2-(6 -methoxy-2-naphthyl)propionic acid C.sub.14 H.sub.14 O.sub.2, is today already successfully employed in therapy as an enantiomerically pure active compound from this class of substance.
A difficult problem of this active compound group for the pharmacist is to be seen in their poor solubility, because according to the theory of passive transport active compounds are only absorbed in dissolved and undissociated form. In general, by comminuting the active compound (micronizing) it is attempted according to the Noyes-Whitney equation to achieve an increase in the effective substance surface area A, which leads to an increase in the rate of solution. This, in turn, results in an improvement in the bioavailability. Micronized powders are therefore preferably employed today for poorly soluble analgesics/antirheumatics which are to be administered orally.
The technique of micronization is energy-consuming and expensive and problems occur with the very fine dusts, such as e.g. the danger of a dust
REFERENCES:
patent: 4880634 (1989-11-01), Speiser
patent: 5430021 (1995-07-01), Rudnic et al.
Freidenreich Jurgen
Lukas Helmut
Schick Ursula
Schuster Otto
Werry Jurgen
Acquah Samuel A.
Alfatec-Pharma GmbH
PAZ Arzneimittelentwicklungsgesell schaft mbH
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