Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Food or edible as carrier for pharmaceutical
Patent
1995-02-15
1996-11-26
Spear, James M.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Food or edible as carrier for pharmaceutical
424497, 424482, 424464, A61K 922, A61K 932, A61K 958
Patent
active
055783163
DESCRIPTION:
BRIEF SUMMARY
This invention relates to a composition and method for taste masking bitter, unpleasant tasting medicaments and provides for an immediate release of the medicament after ingestion. More specifically, the invention relates to medicament cores coated with methacrylate ester copolymers which masks the bitter and unpleasant taste of the medicament. A method of preparing dosage units such as chewable tablets, employing the coated medicament is also described.
In a preferred embodiment of this invention, the composition comprises a chewable tablet containing cimetidine coated with separate layers of methacrylate ester copolymers. The tablets do not exhibit the bitter taste of cimetidine and provides for an immediate release of the cimetidine.
BACKGROUND OF THE INVENTION
Cimetidine is a histamine H.sub.2 -antagonist which has been shown to be useful in the treatment of duodenal, gastric, recurrent and stomal ulceration. It is also employed in the management of patients who are at high risk from hemorrhage of the upper gastrointestinal tract.
Cimetidine is known to be one of many medicaments 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 forms 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 in a solid dosage form is by means of a chewable tablet, i.e., a tablet which disintegrates in the mouth upon being chewed. Such a tablet also circumvents the problem of a solid dosage being difficult to swallow.
It will be appreciated that a major requirement of such a dosage form is that it must be palatable, since an unpalatable formulation increases the risk of a patient neglecting to take the tablet. 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 a composition is that once the disintegrated tablet 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 readily bioavailable.
In the case of cimetidine, because of its bitterness and solubility characteristics, the provision of such a dosage form represents a considerable problem.
Several solutions to the problem of taste masking pharmaceutical compositions have been attempted. For example, cimetidine granules have been coated with various compositions such as ethylcellulose and polyvinyl and acrylic polymers. One such proposal is disclosed in U.S. Pat. No. 4,800,087 wherein a polymer mixture coating is employed. The mixture comprises a high temperature film forming copolymer of polymethyacrylic acid ester and acrylic acid ester and a low temperature film forming copolymers consisting of methacrylic acid ester and styrene acrylate. U.S. Pat. No. 4,892,740 discloses pharmaceutical preparations having improved flavouring characteristics obtained by the drug being coated by a polymeric substance which is soluble in gastic juice.
DESCRIPTION OF THE INVENTION
In accordance with this invention it has been unexpectedly discovered that when bitter, unpleasant tasting medicaments are coated with separate layers of specific methacrylate ester copolymers a core results which is palatable and has good dissolution characteristics in the stomach. The coated core results in a taste masked medicament without reducing its bioavailability.
The core particles which are to be coated can be composed of pure granular drug material or drug granules prepared in the conventional manner employing appropriate binding agents. The particle size of the
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Bhardwaj Sanjay
Hayward Marshall
King William T.
Lentz Edward T.
SmithKline Beecham Corporation
Spear James M.
Suter Stuart R.
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