Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Tablets – lozenges – or pills
Patent
1994-10-07
1997-01-28
Spear, James M.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Tablets, lozenges, or pills
424489, 424400, 514937, 514974, A61K 914, A61K 920
Patent
active
055975836
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/GB93/00702 filed Apr. 2, 1993.
This invention relates to a pharmaceutical composition containing ibuprofen, a process for its preparation, and a palatable formulation thereof suitable for oral consumption. In particular, the invention relates to an ibuprofen-cyclodextrin clathrate complex suitable for formulation in aqueous solution as a hot drink.
Ibuprofen, (.+-.)-2-(p-isobutylphenyl)propionic acid, belongs to the group of non-steroidal antiinflammatory agents (NSAIDs) and is widely indicated for the relief of pain and inflammation in disease states such as arthritis and for treatment of symptoms associated with the common cold and flu. Formulation of the drug into a preparation suitable for oral administration, in particular into a water-soluble form suitable for liquid dosing is complicated by its poor water solubility, its irritating odour and its unpleasant taste. It is an object of the present invention to provide a palatable pharmaceutical composition containing ibuprofen formulated for oral dosing as an aqueous solution.
The ability of drug-cyclodextrin complexes to enhance water solubility and to mask unpleasant taste and odour has been known for many years. In this respect, ibuprofen has proved to be very suitable as a candidate for complexation with cyclodextrins.
Japanese patent publication, JP 56-46837 (Kowa Yakuhin Kogyo) discloses a method for the preparation of an ibuprofen-.beta.-cyclodextrin clathrate complex involving the combination of ibuprofen with .beta.-cyclodextrin in water at elevated temperature and isolation of the clathrate by spray-drying. This method is reported to yield a product containing a high percentage of ibuprofen with a molar ratio of ibuprofen to .beta.-cyclodextrin in excess of 0.7. The increase in water solubility of the drug is considerable, being raised more than 8-fold from 10.44mg per 100 ml to 89.38 mg per 100 ml at 27.degree. C.
The water solubility achieved by complexation with .beta.-cyclodextrin, although significant, is not considered sufficient to permit formulation of ibuprofen as a soluble dosage form for oral administration in liquid form wherein ibuprofen is present at a therapeutic dosage level (100-600 mg) in a suitable volume of water (120-250 ml).
European patent publication 274 444 (Bristol Myers) describes the preparation of ibuprofen-cyclodextrin complexes using .alpha.-cyclodextrin, .gamma.-cyclodextrin or a methylated .beta.-cyclodextrin in place of .beta.-cyclodextrin. The water solubility of the ibuprofen-cyclodextrin complex is further enhanced to levels of practical utility using these forms of cyclodextrin, but the high cost of these materials, reflected in the cost of medicinal products containing them, is unlikely to promote their widespread use in analgesic products, more particularly in products available for self medication for the treatment of minor aches and pains and the symptomatic relief of colds and flu.
United Kingdom patent publication GB 2,219,585 (Reckitt & Colman) discloses a complex of .beta.-cyclodextrin with the sodium, potassium, ammonium, magnesium, calcium, arginine, glycine or lysine salt of ibuprofen, having a molar ratio of ibuprofen to .beta.-cyclodextrin in the range 1:0.2 to 1:0.75 and possessing good water solubility. These complexes are not entirely suitable for incorporation into formulations intended for oral consumption in liquid form since, on solution in water, they confer a somewhat unpleasant, soapy taste, typical of an alkaline solution.
The present invention provides an ibuprofen-cydodextrin complex which is suitable for administration as an aqueous solution, which is palatable and yet which is relatively simple and inexpensive to manufacture in comparison with prior art ibuprofen-cyclodextrin complexes.
According to the present invention there is provided the use of an ibuprofen-.beta.-cyclodextrin complex for the manufacture of a medicament for oral consumption as an aqueous solution, characterised in that the complex is administered in a solution comprising hot
REFERENCES:
patent: 5019563 (1991-05-01), Hunter et al.
patent: 5024997 (1991-06-01), Motola et al.
Kanagy James M.
King William T.
Lentz Edward T.
SmithKline Beecham p.l.c.
Spear James M.
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