DE2260384

• Main Authors: ROSS, GERHARD., 6237 LIEDERBACH, TILLMANN, WALTER, 6230 FRANKFURT, CERESA, FRANCESCO, , TURIN (ITALIEN)
• Format: Patent
• Language: English
• Published: 12.04.1979
• Edition: 2
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES

1458676 Corticosteroid compositions HOECHST AG 10 Dec 1973 [9 Dec 1972] 57090/73 Heading A5B A controlled release unit dosage pharmaceutical composition for oral administration comprises at least two layers, the word "layer" including a core in its meaning (e.g. drageÚ cores), each comprising a corticosteroid in the form of the free alcohol or an ester or salt thereof and each having different release properties. The corticosteroid may be hydrocortisone, cortisone, prednisone, prednisolone, methylprednisolone, or esters or salts thereof. Each layer may contain the same or different corti- 'costeroids, e.g. prednisolone in one layer and its acetate in another, or cortisone acetate in one layer and prednisolone in another. The preferred form is a dregÚe core such as a pressed tablet as the one corticosteroid-containing layer, having an enteric coat (e.g. cellulose acetate phthalate) resistant to gastric juice but soluble in the dudodenum, and an outer dragÚe coating containing corticosteroid, this coating being freely soluble in gastric juice to liberate its active ingredient for absorption in the stomach. The compositions are intended to enable the corticosteroid to be administered in such a way that its absorption rate and action is synchronised with the circadian rhythm of physiological ACTH secretion, and accordingly, the preferred form provides a small steroid dose immediately (i.e. from the outer, soluble layer), and a larger dose some hours later (i.e. from the inner, enterically coated layer), the dosage form being intended to be taken early in the morning. The invention includes a pack comprising a card carrying at least one pair of inventive unit dosage forms together with instruction that one unit is to be taken at about breakfast time and the other unit is to be taken between midafternoon and bed-time.