坎地沙坦酯自微乳软胶囊的制备和溶出度评价

Study on preparation and dissolution of candesartan cilexetile self-microemulsifying soft capsules

目的研制坎地沙坦酯自微乳软胶囊,并对其溶出度进行评价。方法制备坎地沙坦酯自微乳软胶囊,并按药典方法考察自微乳软胶囊与普通胶囊在三种不同溶出介质(水、0.1mol/L盐酸和pH6.8的缓冲溶液)中的溶出度。结果坎地沙坦酯自微乳释药系统处方为乙酸乙酯:聚氧乙烯氢化蓖麻油RH40:聚乙二醇400为9∶14∶7。坎地沙坦酯自微乳受溶出介质的影响小,且溶出速率高于普通胶囊。结论自微乳软胶囊能显著提高坎地沙坦酯的体外溶出。

Objective To prepare candesartan cilexetile self-microemulsifying soft capsules and evaluate its dissolution. Methods The candesartan cilexetile self-microemulsifying soft capsules were prepared. The dissolution of soft capsules and common capsule were investigated in three different dissolution medium （water, 0.1 mol/L hydrochloric acid and pH 6.8 buffer solution） in accordance with the pharmacopoeia. Results The self-microemulsifying drug delivery system was composed of acetic ether （as oil）： RH40 （as emulsifier）： PEG400 （as co-emulsifier） = 9 ∶ 14 ∶ 7. The dissolution release of soft capsule was not influenced by the different dissolution medium. And the drug release rate of soft capsule was faster than the common capsule. Conclusion The dissolution of candesartan cilexetile soft capsule was remarkably improved.