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TABLETS WITH REGULATED BY LOCATION AND TIME RELEASE OF A GLUCOCORTICOID IN THE GASTROINTESTINAL TRACT
TABLETS WITH REGULATED BY LOCATION AND TIME RELEASE OF A GLUCOCORTICOID IN THE GASTROINTESTINAL TRACT
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机译：胃肠道中糖皮质激素的位置和时间释放对片剂的影响
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摘要
1. A method of manufacturing a tablet that releases the active ingredient glucocorticoid at a predetermined location in the gastrointestinal tract, which includes:! - determination of the location of the gastrointestinal tract to which glucocorticoid must be delivered; ! - the formation of a coated tablet having a core comprising a glucocorticoid and a swelling adjuvant, and an inert outer coating that does not swell and does not undergo erosion; and! - compressing the coating of said tablet at a pressure selected so that it releases the glucocorticoid at the indicated predetermined location, namely, applying a pressing pressure of up to 600 kg ensures the release of glucocorticoid in the upper intestines, and a pressing pressure above 600 kg ensures the release of glucocorticoid in the lower sections of the intestine. ! 2. The method of claim 1, wherein the glucocorticoid is rapidly released when the core is in contact with gastrointestinal fluids, and wherein said coating is capable of preventing a substantial release of glucocorticoid within a certain period of time after taking the dosage form. ! 3. The method according to claim 1, in which the core further comprises a disintegrant. ! 4. The method according to any one of claims 1 to 3, in which the glucocorticoid is released in the upper intestines from about 2 to 6 hours after ingestion, where systemic exposure occurs in vivo by the release of glucocorticoid in the upper intestines, and in which the coating is applied by pressure pressing 250-600 kg. ! 5. The method according to any one of claims 1 to 3, in which the glucocorticoid is released in the lower intestine during the period
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