兰索拉唑肠溶微丸型口崩片的制备研究

Study on the Preparation of Lansoprazole Enteric-coated Pellets Orally Disintegrating Tablets

目的:制备兰索拉唑肠溶微丸并压制成口崩片,评价耐酸性和释放度。方法:采用流化床包衣法制备兰索拉唑肠溶微丸,考察了丙烯酸树脂L30D-55和丙烯酸树脂NE30D配比、增塑剂用量和压片主压力对兰索拉唑肠溶微丸型口崩片的耐酸性和释放度的影响,并采用f_2相似因子法评价了自制兰索拉唑肠溶微丸型口崩片与市售制剂的体外释放相似性。结果:选用微晶纤维素丸芯平均粒径为150~180μm载药,隔离层增重为10%,丙烯酸树脂L30D-55和丙烯酸树脂NE30D配比为8∶2,肠溶衣包衣增重为30%,增塑剂用量为20%,压片主压力为10~16 kN,制备的兰索拉唑肠溶微丸在压片过程中肠溶衣膜未发生破裂,表现出良好的耐酸性,与市售制剂的体外释放度相比f_2相似因子值大于50,说明两种制剂体外释放行为相似。结论:本研究制备的兰索拉唑肠溶微丸型口崩片的耐酸性较好,与市售制剂相比体外释放相似性较高,可进一步放大生产。

Objective： To prepare lansoprasole enteric-coated pellets and compress them into orally disintegrating tablets, and e- valuate the acid resistance in the acid stage and the in vitro dissolution in the buffer stage. Methods： Lansoprazole enteric-coated pel- lets were prepared by fluid bed coating technology, and the effects of the ratio of methacrylic acid copolymer dispersion to ethyl acrylate - methyl methacrylate copolymer dispersion, the concentration of triethyl citrate and the main pressure on the acid resistance in the acid stage and the in vitro dissolution in the buffer stage were evaluated. The similarity of the self-prepared orally disintegrating tablets and the reference preparation was evaluated by using f2 similarity factor method. Results： The average particle size of microcrystalline cellulose core was 150-180 μm, the ratio of methacrylic acid copolymer dispersion to ethyl acrylate - methyl methacrylate copolymer dispersion was adjusted to 8： 2, the enttetic-coated weight was 30%, 20% triethyl citrate was used and the main pressure was controlled within the range of 10-16 kN. Lansoprazole enteric-coated pellets had sufficiently flexibility and stability against the compression force. The enteric coating did not break, showing good acid resistance. The dissolution similarity factor of the self-prepared orally disintegra- ting tablets and the reference preparation was greater than 50. Conclusion： Lansoprazole enteric-coated pellets orally disintegrating tablets have good acid resistance and high similarity for the in vitro dissolution, which can be further amplified.