Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Food or edible as carrier for pharmaceutical
Patent
1995-04-11
1997-01-14
Spear, James M.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Food or edible as carrier for pharmaceutical
424440, 424441, 424465, 424489, 514974, A61K 920
Patent
active
055936857
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/EP93/02763 filed Oct. 11, 1993.
The present invention relates to improvements in the formulation of the histamine H.sub.2 -receptor antagonist ranitidine, particularly for oral administration.
Ranitidine, N-[2-[[5-[(dimethylamino)methyl]-2-furanylmethyl]-thio]ethyl]-N'-methyl-2- nitro-1,1-ethenediamine, and its physiologically acceptable salts are described and claimed in British Patent Specification No. 1565966, and a particular crystalline form of ranitidine hydrochloride is described and claimed in British Patent Specification No. 2084580B. In both these specifications there is reference to formulations for oral administration, which may take the form of for example tablets, capsules, granules, powders, solutions, syrups, suspensions, or tablets or lozenges for buccal administration. Oral preparations of ranitidine are also disclosed in British Patent Specification Nos. 2142820, 2198352, 2218336, 2219940, 2222772 and 2229094.
Oral administration constitutes a preferred route for administering ranitidine. Ranitidine, however, in common with many drug substances, has an inherently bitter taste, and this constitutes a disadvantage with certain types of oral preparation. Moreover, it is well known that patients may not complete a necessary course of medicine if they are prescribed an oral presentation which is particularly unpleasant to taste. The problems resulting from the bitter taste of ranitidine are particularly acute in formulations such as chewable tablets.
Chewable tablets are a particularly convenient form of oral presentation for patients who prefer not to take swallowable tablets, or find difficulty in swallowing them.
We have now discovered a chewable tablet formulation which effectively masks the bitter-taste of ranitidine and which also exhibits particularly advantageous bioavailability.
Thus the present invention provides a chewable ranitidine tablet comprising ranitidine, or a physiologically acceptable salt thereof, a chewable base selected from sucrose, glucose, lactose, maltose, or a mixture thereof, a flavouring and, optionally, an intense sweetener.
Chewable ranitidine tablets containing sucrose are described in GB2222772. However, these tablets contain alginic acid and sodium bicarbonate as essential components of the formulation and such tablets are excluded from the present invention.
Thus according to a further aspect the present invention provides a chewable ranitidine tablet consisting essentially of ranitidine, or a physiologically acceptable salt thereof, a chewable base selected from sucrose, glucose, lactose, maltose, or a mixture thereof, a flavouring and, optionally, an intense sweetener.
According to a further aspect the present invention provides a composition consisting essentially of ranitidine, or a physiologically acceptable salt thereof, a chewable base selected from sucrose, glucose, lactose, maltose, or a mixture thereof, a flavouring and, optionally, an intense sweetener.
Ranitidine may be employed in the tablets according to the invention in the form of either its free base or a physiologically acceptable salt. Such salts include salts with inorganic or organic acids such as the hydrochloride, hydrobromide, sulphate, acetate, maleate, succinate, citrate, tartrate, fumarate and ascorbate salts. A particularly preferred salt of ranitidine is the hydrochloride.
The bitter-taste of ranitidine is effectively masked in the chewable tablets according to the invention when ranitidine is employed in conventional form. However, coated or encapsulated forms of ranitidine may be used in the tablets according to the invention. Suitable coated and encapsulated forms are described in, for example, EP538034, EP523847. WO92/21328, EP473431, EP459695, EP349103, CA2068366 and U.S. Pat. No. 5,084,278. Ranitidine resin adsorbates as described in UK2218333 may also be incorporated into the tablets according to the present invention.
Preferably ranitidine and its salts are used in conventional form.
The chewable base in the tablets according to the inve
REFERENCES:
patent: 5075114 (1991-12-01), Roche
patent: 5084278 (1992-01-01), Mehta
Bye Alan
Evans Jill
Huckle Paul D.
Lacey Laurence F.
Rue Peter J.
Glaxo Group Limited
Spear James M.
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