Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Food or edible as carrier for pharmaceutical
Patent
1995-04-12
1997-06-03
Rose, Shep K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Food or edible as carrier for pharmaceutical
424484, 424490, 424497, 424498, A61K 928, A61K 916
Patent
active
056352000
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/EP93/02832 filed on Oct. 14, 1993 published as WO94/08576 Apr. 28, 1994.
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, granules, powders, solutions or suspensions. To some extent, the bitter taste may be masked by the use of sweetening and/or flavouring agents, although this is not entirely satisfactory, and an unpleasant after-taste may still remain in the mouth. In addition, there may be circumstances in which it is undesirable or inappropriate to use a sweetening and/or flavouring agent.
Various methods of taste-masking ranitidine have been described. For example, British Patent Specification No. 2218333 describes complexes formed between ranitidine and an ion exchange resin to give a resin adsorbate which is substantially free of the bitter taste associated with ranitidine.
Other methods of taste-masking ranitidine are described in EP349103, EP459695, EP473431 and U.S. Pat. No. 5084278.
We have now found that the bitter taste of ranitidine may be masked by coating the drug substance with a suitable lipid.
One of the factors that governs the degree of taste masking obtained by lipid coating is the water solubility of the input drug substance. Thus, for forms of ranitidine which are only poorly soluble in water (e.g. less soluble salts of rantidine), the bitter taste associated with ranitidine may be satisfactorily masked by simple lipid coating of the drug substance. In the case of forms of ranitidine which are soluble in water to an appreciable extent (e.g. ranitidine base and certain of its salts), the degree of taste masking achieved by simple lipid coating of the drug substance may not be entirely satisfactory, particularly if the product is to be formulated in an aqueous medium or the product comes into contact with the wet environment of the mouth. We have found that the degree of taste masking achieved by coating the drug substance with a suitable lipid, especially when the ranitidine is in a form having an appreciable solubility in water, can be significantly enhanced if the drug substance is incorporated into a core prior to being coated with the lipid.
The resulting lipid coated particles, containing an inner core if required, are substantially insoluble in water but break down on contact with gastrointestinal fluid, such that the bitter taste associated with ranitidine is masked on oral administration, with subsequent release of the drug substance, by dispersion or dissolution, in the gastrointestinal tract.
Thus according to one aspect the present invention provides a composition which is substantially free of the bitter taste associated with ranitidine and comprises physiol
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Douglas Stephen J.
Evans Jill
Brink Robert H.
Glaxo Group Limited
Rose Shep K.
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