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由于β-内酰胺类抗生素分子结构中连接羧基,具有亲水性,通常口服和直肠给药难以吸收。盐酸氨苄青霉素甲戊酯(BAPC)是氨苄青霉素(ABPC)的前药,它的脂溶性比母体药物(ABPC)显著增强,因此BAPC口服后有较好的吸收。那么BAPC能否直肠给药呢?基于这个问题,作者以Witepsol H- 15为基质,将BAPC制成了栓剂,并且对BAPC的直肠,口服和静脉给药进行了兔体内生物利用度的研究。高压液相色谱法测不出血样的BAPC,而只能检出BAPC的母体药物(ABPC),因此以静脉注射等克分子的ABPC作为计算
Due to the carboxyl group attached to the molecular structure of β-lactam antibiotics, it is hydrophilic and is usually absorbed orally and rectally. Ampicillin methylpenate hydrochloride (BAPC) is a prodrug of ampicillin (ABPC), its fat-soluble than the parent drug (ABPC) was significantly enhanced, so after oral administration of BAPC better absorption. So BAPC rectal administration it? Based on this problem, the authors of Witepsol H-15 as a matrix, the BAPC made suppositories, and BAPC rectal, oral and intravenous administration of rabbit bioavailability studies. High-pressure liquid chromatography can not detect blood BAPC, but only the parent drug BAPC (ABPC) was detected, so the intravenous injection of other molecules of ABPC as a calculation