Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1995-07-14
1997-01-28
Henley, III, Raymond
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
A61K 31415
Patent
active
055978444
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/EP93/03272 filed Nov. 22, 1993.
This invention relates to granules of cimetidine which are useful in the preparation of pharmaceutical compositions having an improved flavour.
Cimetidine is a histamine H.sub.2 -antagonist and has been described in UK. Patent Specification 1,397,436. Cimetidine has been shown to be useful in the treatment of duodenal, gastric, recurrent and stomal ulceration, and reflux oesophagitis and in the management of patients who are at high risk from haemorrhage of the upper gastrointestinal tract.
Cimetidine is known to have a pronounced bitter taste. This is not usually a problem when the dosage form employed is a capsule or a tablet designed to be swallowed, thereafter to disintegrate upon reaching the stomach. However, such dosage toms can be impractical when it is desired to administer a large amount of active ingredient, or to co-administer a relatively bulky second active ingredient such as an antacid or alginate. Moreover many individuals have difficulty in swallowing a solid dosage form.
A conventional approach to administering relatively large amounts of active ingredient is by means of a suspension or a chewable tablet, i.e. a tablet which disintegrates in the mouth upon being chewed.
It will be appreciated that a major requirement of such dosage forms is that they must be palatable, since an unpalatable formulation increases the risk of a patient neglecting to take a medicament. Such non-compliance with the dosing regimen will in turn delay or prevent the patient's recovery from the condition under treatment.
A further requirement of such compositions is that once the formulation reaches the stomach, the individual particles should release the active ingredient rapidly and completely in order to ensure that substantially all of the active ingredient is absorbed; that is to say the formulation should be bioavailable.
In the case of cimetidine, because of its bitterness, the provision of such dosage forms represents a considerable problem.
EP-A-257823 describes a stable aqueous suspension of cimetidine wherein at least 90% of the cimetidine is in the polymorphic B form. It is disclosed that the use of polymorph B overcomes the problem of polymorphic interconversion found in the case of polymorph A suspensions of relatively low viscosity which tend to result in lumpy and non homogeneous suspensions.
EP-A-322048 describes a pharmaceutical granule composition comprising cimetidine and an ester of a polyhyctroxy compound, in particular a glycerol ester selected from: triglyceride content of less than 30% by weight, and point of less than 40.degree. C.
It is disclosed that such cimetidine containing granules are useful in the preparation of chewable tablets.
Coated cimetidine granules have now been discovered which have improved flavour. They can be presented in a variety of pharmaceutical forms, e.g., as a chewable tablet, a constitutable powder, or as a sprinkle powder, i.e., a powder that can be sprinkled, for example, onto food before consumption.
In a first aspect the present invention provides a pharmaceutical composition comprising cimetidine granules coated with a partially hydrogenated vegetable oil or a chemical equivalent thereof, in an amount corresponding to at least 20%, suitably from 25% to 200%, by weight relative to the cimetidine.
More suitably the partially hydrogenated vegetable oil is present in an amount from 50% to 150%, preferably 75% to 125%, particularly 100% by weight relative to the cimetidine.
The cimetidine can exist in any form, for example, polymorph A, B, C or Z or any mixture thereof, preferably polymorph A.
Partially hydrogenated vegetable oils are derived from natural products and generally comprise a mixture of glycerides of C.sub.14-20 fatty acids, in particular palmitic and stearic acids, said raixmre suitably having an iodine value of less than 10 and a melting point greater than 40.degree. C. Preferably said mixture has an iodine value less than 5 and a melting point between 45.degree. and 75.degree. C.
S
REFERENCES:
patent: 5229137 (1993-07-01), Wolfe
Buehler John
Chauhan Sushil
France Gordon
Dinner Dara L.
Henley III Raymond
Lentz Edward T.
Venetianer Stephen
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