Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Particulate form
Patent
1997-02-11
1998-11-10
Webman, Edward J.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Particulate form
424488, 424499, 424494, 424495, 424497, 424470, 424458, 424461, 424462, A61K 916, A61K 926, A61K 956, A61K 958
Patent
active
058340211
DESCRIPTION:
BRIEF SUMMARY
The present invention relates to the use of prednisolone metasulphobenzoate and pharmacologically acceptable salts thereof, especially the sodium salt, in the treatment of inflammatory bowel disease. In particular, it provides a solid enteric pharmaceutical composition having relatively rapid dissolution at pH 6.5 of the prednisolone metasulphobenzoate from an excipient matrix and dosage forms containing pellets (or granules) of the composition unless it is clear from the context that the free ester is intended, the terms "Prednisolone metasulphobenzoate" and "PRED-MSB" are used herein to include pharmacologically acceptable salts of prednisolone metasulphobenzoate as well as the free ester.
Steroids are widely used to treat severe cases of inflammation of the large bowel, especially ulcerative colitis and Crohn's disease. Usually, they are administered orally or parenterally to provide a systemic effect or rectally by enema to provide a topical effect. Relatively high doses of steroids are required to treat severe cases of inflammatory bowel disease. However, systemic absorption produces serious side effects and, although absorption is lower with rectal administration, the use of enemas is inconvenient.
The most commonly used steroid in the oral treatment of inflammatory bowel disease is prednisolone (17,21-dihydroxypregna-1,4-diene-3, 11,20-trione) in the form of the free alcohol or an ester thereof, usually the acetate. Daily doses of 15 to 60 mg (calculated as the free alcohol) are required to treat severe cases of inflammatory bowel disease but absorption at these doses is harmful. Accordingly, present treatment with prednisolone is limited in both dosage and duration of therapy.
FR-A-5083M discloses compositions comprising a corticosteroid, enzyme, salicylate and a vitamin. Exemplified corticosteroids include PRED-MSB but no excipients are specified and there is no reference to the treatment of inflammatory bowel disease.
FR-A-8106M discloses combinations of corticosteroids with cobalamines. The exemplified corticosteroids include PRED-MSB but no excipients are specified and there is no reference to the treatment of inflammatory bowel disease.
U.S. Pat. No. 3,424,842 discloses a process for manufacturing tablets directly from a dry powder containing 1 to 10 wt % of a powdery polyethylene glycol, gelatin or non-starch polysaccharide. Prednisolone is amongst a lengthy list of therapeutically active compounds which can be present in the tablets but there is no mention of PRED-MSB or of the treatment of inflammatory bowel disease.
GB-A-1578850 discloses solid pharmaceutical formulations for oral administration comprising 5 to 80 wt % steroid, 1 to 8 wt % sodium starch glycolate and the remainder conventional oral excipients. The only exemplified formulations are blends in gelatin capsules. It is reported that the presence of the sodium starch glycolate enhances disintegration of the tablets in 0.1N HCl. Reference is made to prednisolone but there is no reference to PRED-MSB or of the treatment of inflammatory bowel disease.
WO 87/05804 discloses the use of super-disintegrants in amounts of greater than 10% to enhance the disintegration of compressed tablets or capsules and has particular, but not exclusive, application to tablets containing glucocorticoid steroids. "Super-disintegrants" are defined to be those disintegrants which can be used in a fractional amount of normal disintegrants, such as corn starch, to obtain the same effect. Specified super-disintegrants include modified starches (especially sodium starch glycolate), croscarmellose sodium, and crospovidone. The super-disintegrants can be used in compositions containing microcrystalline cellulose and/or lactose as excipients. Exemplified steroids include methyl-prednisolone and prednisone but there is no reference to prednisolone or PRED-MSB. Further, there is no reference to the treatment of inflammatory bowel disease.
It is stated in WO 87/05804 that rapid dissolution of a pharmaceutical agent from a tablet or capsule requires rapid disintegr
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