氨苄青霉素具有良好的抗菌活力和安全性,得到广泛使用。过去对婴幼儿感染采用口服或注射给药。但口服时的苦味会使患儿拒绝服药或发生呕吐,使给药不能保证,肌肉注射给药可发生肌肉萎缩,静脉注射则很难保护血管。抗生素栓剂,在欧美早已开发,但日本仅有红霉素,然而其生物利用度低,这对于维持血浓度来说未必满意。最近日本京都药品工业研究所发现癸酸钠具有促进直肠吸收β内酰胺类抗生素的良好作用,可将其加入基质中制成氨苄青霉素栓剂。氨苄青霉素钠能作用于细菌细胞膜中的青霉素结合蛋白而抑制细菌细胞壁的合成,从而产生杀菌作用。特别是已知它对于金黄色葡萄球菌、链球菌属(肠球菌除外)、肺炎球菌、流感杆菌具有良好的抗菌作用。 Ampicillin has good antibacterial activity and safety, has been widely used. In the past, infants and young children were infected by oral or injection. However, oral bitterness will make children refuse medication or vomiting, so that medication can not be guaranteed, intramuscular injection can occur muscle atrophy, intravenous injection is difficult to protect the blood vessels. Antibiotic suppositories, already developed in Europe and the United States, but Japan only erythromycin, however, its low bioavailability, which is not necessarily satisfied with the maintenance of blood concentration. Recently, Japan’s Kyoto Pharmaceutical Industry Institute found that sodium caprate has a good effect of rectal absorption of β-lactam antibiotics, which can be added to the matrix ampicillin suppository. Ampicillin sodium can act on the bacterial cell membrane in the penicillin binding protein and inhibit bacterial cell wall synthesis, resulting in bactericidal effect. In particular, it is known to have a good antibacterial action against Staphylococcus aureus, Streptococcus (except Enterococcus), pneumococcus, and Influenza bacilli.