氨苄青霉素缓释直肠胶囊剂的研制

Delayed release rectal capsule of ampicillin

氨苄青霉素缓释直肠胶囊剂系根据硬胶囊可在直肠中迅速崩解,而膜包衣胶囊可延缓崩解的性能,经正交设计选择有效的直肠吸收促进剂和符合设计要求的缓释膜而制成。本制剂在正常受试者体内实现了一次给药可达到两次有效峰浓度及违释与缓释部分的达峰时相距3h以上的目的。用于婴幼儿可解决小儿口服及注射给药难的问题,给药次数减少,副作用减轻。

The delayed-release rectal capsule ofampicillin (DRRCA) was prepared according tothe rapid disintegration of the capsule and de-layed disintegration of the capsule coated witha delayed-release membrane in the rectus. For-mulations of the preparation and the delayed-release membrane were confirmed by orthogo-nal design L_4: (2~3) and L-9 (3~4). DRRCA wasgiven to four healthy volunteers and its serumconcentration determined by microbial assay.Double peaks of its serum level were observedas follows: 2.48±0.75μg/ml at 0.63±0.25hand 0.8±0.20μg/ml at 3.63±0.63h respec-tively (n=4). DRRCA provides a new route ofampicillin administration for children or re-duces the chances of adminiatration.