MANUFACTURE OF CAFFEINE PELLETS BY EXTRUSION-SPHERONIZATION FOR A "COCKTAIL" TEST SYSTEM

Cocktail" test systems are used for phenotyping the metabolic activity of human cytochrome P450 isoenzymes. The vast majority of "cocktails" for phenotyping include caffeine, based on data on the metabolism of which the activity of the CYP1A2 isoenzyme is determined. The use of pellets as a dosage form consisting of many particles for "cocktail" test systems makes it easy to change the composition and dosage of the test system depending on the needs of CYP research, and also provides easier acceptance of the test system by the patient in geriatric studies. Aim. Development of pellets containing caffeine for a "cocktail" test system using the methodology of a complete factor experiment. Materials and methods. Pellets containing caffeine (Shandong Xinhua Pharmaceutical Co., Ltd., China) were manufactured by extrusion-spheronization in the ESI 25 apparatus (Tofflon, China). The obtained pellets were subjected to technological tests in accordance with the GF of the Russian Federation XV. The quality of the pellets obtained and their dissolution profile were evaluated. Results and discussion. With the help of a complete factorial experiment, the optimal composition of pellets was selected, the optimal amount of granulating liquid was selected, and the parameters of the extrusion-spheronization process were worked out. Conclusion. As a result of the conducted research, the composition and technology of production of caffeine pellets for the cocktail test system were developed using a complete factorial experiment. A technological scheme for the production of pellets has been developed. Optimal conditions for humidification of the pellet mass were selected for the extrusion-spheronization technology.