Oral dosage form for treating migraine

Details Oral dosage form for treating migraine Oral dosage form for treating migraine

1995-01-31

1999-01-26

Venkat, Jyothsna

Drug, bio-affecting and body treating compositions

Preparations characterized by special physical form

Tablets, lozenges, or pills

424464, 424465, 424475, A61K 936

Patent

active

058635599

DESCRIPTION:

BRIEF SUMMARY
The present invention relates to a pharmaceutical composition containing as active ingredient particular a composition for oral administration. may be represented by the formula (I) ##STR1## and its physiologically acceptable salts and solvates are disclosed in UK Patent Specification No. 2162522. The compound of formula (I) exhibits selective vasoconstrictor activity and is useful in the treatment of migraine.
Oral administration constitutes the generally preferred route for administration of pharmaceuticals since this route is particularly convenient and acceptable to patients. Unfortunately oral compositions may be associated with certain disadvantages in the treatment of conditions associated with cephalic pain. For example, such conditions, particularly migraine are associated with gastrointestinal dysfunction in the form of delayed gastric emptying. This leads to both a delay and an impairment of drug absorption and it is generally accepted that oral formulations of drugs for the treatment of such conditions should be administered in the form of a liquid preparation.
Numerous clinical studies have demonstrated the effectiveness of the compound of formula (I) in migraineurs. Hitherto, the drug has always been administered either by parenteral injection or in the form of a dispersible tablet which is dispersed in drinking water prior to oral administration. This mode of oral administration was believed to minimise the potential problems associated with gastrointestinal dysfunction in migraineurs.
However, it has been found that the compound of formula (I) has a particularly unpleasant taste. When the compound of formula (I) is administered orally this unpleasant taste may exacerbate the nausea and vomiting associated with migraine.
The present invention provides a particularly advantageous formulation suitable for oral administration of the compound of formula (I).
There is thus provided according to the invention a pharmaceutical composition for oral administration comprising a film-coated solid dosage N-methyl-1H-indole-5-methanesulphonamide or a pharmaceutically acceptable salt or solvate thereof as active ingredient.
As used herein the term "film-coated solid dosage form" means a solid core comprising the active ingredient, which solid core is substantially covered with a film coating.
The compositions of the invention may comprise, for example, granules, tablets or capsules. Preferably the compositions of the invention will comprise tablets, most preferably compressed tablets.
There is provided in a preferred aspect of the invention a film coated tablet comprising a tablet core containing an effective amount of pharmaceutically acceptable salt or solvate thereof as active ingredient and a film coat on the tablet core.
We have found that the unpleasant taste associated with oral administration of the compound of formula (I) is substantially eliminated by the formulations of the present invention. The film coating also makes the formulations easier to handle and reduces potentially hazardous dust formation occurring during the packaging or administration of the drug. Surprisingly these advantages are attained without any significant loss in the bioavailability of the compound of formula (I) when compared to aqueous solutions or dispersible tablet formulations for oral administration to migraineurs Film-coated tablets according to the invention are therefore surprisingly effective in the treatment of migraine.
It is preferred that should be employed in the compositions of the invention in the form of a physiologically acceptable salt. Such salts include salts of inorganic or organic acids such as hydrochloride, hydrobromide, sulphate, nitrate, phosphate, formate, mesylate, citrate, benzoate, fumarate, maleate, tartrate and succinate salts. Most preferably be employed in the compositions of the invention in the form of its succinate (1:1) salt.
The film coating comprises a polymer. Suitable polymers include cellulose ethers, for example, hydroxypropyl methylcellulose, hydroxypropyl cellulose or methyl

REFERENCES:
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patent: 4894387 (1990-01-01), Butina et al.
patent: 5037845 (1991-08-01), Oxford
Remingtons pharmaceutical Sciences (17th edition) pp. 1605-1606 (1985).
The Bantam Medical Dictionary by John Wiley & Sons pp. 196, 320 (1990).
King; Remington's Pharmaceutical Sciences; Fifteenth Edition, 1975; 89; pp. 1576-1577.
Wilkinson; Cephalalgia, vol. 3, 1983; pp. 61-67.
Volans; Chemical Pharmacokinetics 3: 1978; pp. 313-318.
Patten; J. Neurol (1991); 238: S62-S65.
Hussey; Clin. Pharm. Ther. (1991), 49(2), Abs. pp. 1-46.

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