Paper
FENG Zhong, WEI Ruixia, JIA Junwei, CHEN Mengyu, YAN Jiyong, ZHANG Guimin
Enteric-coated pellets of esomeprazole magnesium were prepared by bottom spray fluid bed process. First, the blank sugar pellets were coated with a 15%-solid-content liquid containing 2% hydroxypropyl methylcellulose E5 LV, 0.3% talc and the bulk drug. Then, the drug-coated pellets were coated with a 10%-solid-content liquid containing the mixture of hydroxypropyl cellulose LF and talc(1∶2), and the weight gain of this isolation layer was (23±2)%. After that, the above pellets were coated with a 15%-solid-content liquid containing Eudragit L30D-55, triethyl citrate and Tween-80 (28∶4∶5). The final enteric pellets were obtained when the weight gain of enteric layer reached 45% - 50%. Finally, the title tablets were obtained by blending with microcrystalline cellulose(with ratio of MCC 101 to MCC 102 of 40∶60), crospovidone and sodium stearyl fumarate, compression and coating with a film layer. The results showed that the content uniformity, acid resistance and release of the coated tablets met the requirements of Chinese pharmacopoeia 2020. A method for determination of esomeprazole in Beagle dog plasma by LC-MS was established. Under fasting condition, cmax of the self-made pellet-based tablets and reference preparation were (287.16±13.37) and (290.34±12.42)ng/ml, tmax were (1.34±1.37) and (1.41±2.37)h, respectively. The oral relative bioavailability of the selfmade preparation was (98.5±6.7)%. Under feeding condition, AUC and cmax obviously decreased for both self-made and reference preparations. This process could solve the acid instability problem of esomeprazole magnesium.