미세결정셀룰로오스와 호화전분을 이용한 암로디핀말레이트 정제의 수분에 대한 안정성 개선

Abstract

The aim of the study was to formulate the stable amlodipine maleate tablet by selecting and combining of suitable ingredients. Amlodipine tablets were designed by using different manufacturing methods or formulations. Dissolution rate at 30 min of newly formulated tablets was over 98% in 0.1 M HCl medium. After 4 months storage under accelerated condition, the changes of appearance, loss on drying, content and total impurity were investigated. For long-term stability tests, two formulations of K017 (direct compressed tablets consisting of microcrystalline cellulose and pregelatinized starch) and K018 (wet granulated tablets by OpadryAMB) were stored under , 60% RH for 24 months. Under the accelerated condition, moisture content in K017 formulation was increased as 5.96% for 4 months, while other formulations with anhydrous monobasic phosphoric potassium or by wet granulation showed higher increase in moisture content compared to K017. In addition, K017 formulation showed a low decrease in contents and total relative substance as 0.8% and 0.7%, respectively. Similar stability of amlodipine in K017 was obtained under the long-term stability test. These results indicate that the K017 combined with microcrystalline cellulose and pregelatinized starch as ingredients is very stable formulation to protect active substance from moisture contact and sustain stability. Therefore, suitable combination of ingredients such as microcrystalline cellulose and pregelatinized starch could attribute to enhance the stability of moisture-labile drug such as amlodipine maleate.