Goto S, Kawata M, Suzuki T, Kim N S, Ito C
Faculty of Pharmaceutical Sciences, Kyushu University, Fukuoka, Japan.
J Pharm Sci. 1991 Oct;80(10):958-61. doi: 10.1002/jps.2600801011.
New organogels containing salicylic acid, sodium salicylate, procaine, and ketoprofen were prepared by using Eudragit L and S, and propylene glycol. The physical properties (e.g., penetration and extensibility) of the organogels were affected considerably by the incorporation of a basic drug, such as procaine, rather than an acidic drug, such as salicylic acid. In in vivo evaluation using rabbits, it was found that 30% Eudragit L organogels containing 1.25% (w/w) salicylic acid or 2.5% (w/w) ketoprofen showed sustained plasma salicylic acid or ketoprofen levels and almost the same AUC as compared with Witepsol H-15 suppositories containing these drugs. Furthermore, the relative bioavailability for salicylic acid and ketoprofen released from 30% Eudragit L organogels, with 10% (w/w) linolic acid or oleic acid as absorption enhancer, increased to 1.55-1.75- and 1.46-1.85-fold, respectively, compared with 30% Eudragit L organogels without these unsaturated fatty acids.
采用尤特奇L和S以及丙二醇制备了含有水杨酸、水杨酸钠、普鲁卡因和酮洛芬的新型有机凝胶。有机凝胶的物理性质（如渗透性和延展性）受碱性药物（如普鲁卡因）而非酸性药物（如水杨酸）的掺入影响很大。在使用兔子的体内评估中发现，含有1.25%（w/w）水杨酸或2.5%（w/w）酮洛芬的30%尤特奇L有机凝胶显示出血浆水杨酸或酮洛芬水平持续，与含有这些药物的Witepsol H - 15栓剂相比，AUC几乎相同。此外，与不含这些不饱和脂肪酸的30%尤特奇L有机凝胶相比，以10%（w/w）亚油酸或油酸作为吸收促进剂的30%尤特奇L有机凝胶释放的水杨酸和酮洛芬的相对生物利用度分别提高到1.55 - 1.75倍和1.46 - 1.85倍。
