Modified dosage forms of tacrolimus
A tacrolimus and release agent technology, applied in the field of regulated release tacrolimus formulations, can solve problems such as impact, incomplete absorption, and low bioavailability
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Embodiment 1
[0103] According to the present invention, dosage forms are prepared which contain an immediate release component and a release modifying component. The procedure consisted of dissolving a hydrophilic surfactant (vitamin E TPGS), tacrolimus and a lipophilic surfactant (glycerol monooleate) in a suitable solvent (isopropanol) and coating a blank sphere core. These obtained pellets are divided into two parts, using suitable coating equipment, to form one part of the immediate release dosage unit, which is further coated with a film-forming polymer solution to form the second part of the delayed release dosage unit, using The compositions given in Table 1 were coated with enteric material. Pellets of the immediate and delayed release components corresponding to their required amounts are then filled into capsules. In some formulations, the second portion of the composition forming the delayed release dosage unit may be coated with the film coating composition prior to enteric co...
Embodiment 2
[0112] According to the present invention, dosage forms are prepared which contain an immediate release component and a release modifying component. The steps include dissolving a hydrophilic surfactant (sodium lauryl sulfate, sodium dioctyl sulfosuccinate), tacrolimus, a water-soluble carrier in a suitable solvent (ethanol, dichloromethane or a mixture thereof) and other excipients to obtain a clear solution. The solution obtained above was coated on blank pellet cores. These obtained pellets are divided into two parts, using suitable coating equipment, to form one part of the immediate release dosage unit, which is further coated with a film-forming polymer solution to form the second part of the delayed release dosage unit, using Composition given in Table 3, coated with enteric material. Pellets of the immediate and delayed release components corresponding to their required amounts are then filled into capsules. In some formulations, the second portion of the dosage for...
Embodiment 3
[0120] Embodiment 3: pharmacokinetic research:
[0121] (a) The study was designed in a small group of healthy human volunteers to evaluate the pharmacokinetic profile of single-dose oral administration of tacrolimus compositions E and J (one dose per day, 5 mg) of the present invention; 1 and T 2 , and compared it to the reference product (R), a conventional immediate-release product available (2.5mg, administered twice a day) compared.
[0122] Study Design: Open-label, randomized, fasting, single-dose pharmacokinetic study. Healthy human volunteers fasted overnight prior to dosing. Individual volunteers took the formulation with 250 ml of water. Collect pre-dose and after predetermined time intervals (post-dose 0.5, 1.0, 1.5, 2.0, 4.0, 8.0, 9.0, 10.0, 11.0, 12.0, 12.5, 13.0, 13.5, 14.0, 16.0, 20.0, 22.0, 24.0, 36.0 hours) of blood samples. Volunteers were given a standard diet during the study. Plasma analysis using validated analytical methods for determination of ...
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