Utilization of dialkylfumarates
A dialkyl fumarate, application technology, applied in the direction of medical preparations containing active ingredients, ester active ingredients, anhydride/acid/halide active ingredients, etc., can solve the unknown exact properties of TNF-α, etc. problems, resulting in improved absorption, gastrointestinal irritation and reduced side effects
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Embodiment 1
[0045] Prepared in capsules containing 120.0 mg dimethyl fumarate, equivalent to 96 mg Enteric coated microtablets of malic acid
[0046] Taking the necessary precautions (masks, gloves, protective clothing, etc.), 12.000 kg of dimethyl fumarate are crushed, mixed and homogenized with a sieve 800. An excipient mixture was then prepared with the following composition: 17.50 kg starch derivative (STA-RX® 1500), 0.30 kg microcrystalline cellulose (Avicel® PH 101), 0.75 kg PVP (Kollidon® 120), 4.00 kg Primogel® . 0.25 kg of colloidal silicic acid (Aerosil(R)). The active ingredient is added to the entire powder mixture, mixed, homogenized with a sieve 200, processed in a conventional manner with a 2% aqueous solution of polyvinylpyrrolidone (Kollidon® K25) to obtain binder granules, which are then combined in the dry state with the external phase mix. The external phase consisted of 0.50 kg of magnesium stearate and 1.50 kg of talc.
[0047] The powder mixture is then compr...
Embodiment 2
[0052] Prepared in capsules containing 120.0 mg dimethyl fumarate, equivalent to 96 mg fumarate Acid enteric coated microtablets
[0053] 12.000 kg of dimethyl fumarate were crushed and homogenized as above. An excipient mixture was then prepared with the following composition: 23.20 kg microcrystalline cellulose (Avicel® PH 200), 3.00 kg Croscarmellose sodium (AC-Di-SOL-SD-711), 2.50 kg talc, 0.10 kg anhydrous silicon dioxide (Aerosil(R) 200) and 1.00 kg magnesium stearate. The active ingredient is then added to the entire powder mixture and mixed uniformly. The powder mixture was then compressed by direct compression into convex tablets with a gross weight of 10.0 mg and a diameter of 2.00 mm.
[0054] Then, a solution of 0.94 Eudragit(R) in isopropanol was prepared which also contained 0.07 kg of dibutyl phthalate. Spray this solution onto the tablet core. Next, a suspension of a mixture of 17.32 kg of Eudragit(R) LD-55 and 2.80 kg of microtalc, 2.00 kg of Macrogol ...
Embodiment 3
[0057] Prepared in capsules containing 50.0 mg dimethyl fumarate, equivalent to 40 mg fumaric acid pellets
[0058] 5.000 kg of dimethyl fumarate were crushed and homogenized as above. In addition, 2 liters of a 20% (m / v) polyvinylpyrrolidone ethanol solution (Kollidon K-30) was prepared. 7.250 kg of nonpareilles pellets in the coating pan were sprayed with a portion of the Kollidon K-30 solution until slightly wet. The active ingredient is then added in portions until the pellets are dry. This wetting / drying process continues until all of the active ingredient mixture has been added. The pellets were then shaken until completely dry.
[0059] Afterwards, the pellets were filled into hard gelatin capsules (126.5 mg pellets / capsule).
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