| 摘要 |
<p><P>PROBLEM TO BE SOLVED: To permit transdermal administration (topical application) ofβ-lactam antibiotic substances through skin barrier by increasing permeability of theβ-lactam antibiotic substances. <P>SOLUTION: Novel positively-charged prodrugs of theβ-lactam antibiotic substances represented by a structure 4 are designed. Positively-charged amino groups of the prodrugs not only make a drug water-soluble but also combine with negative charges on phosphate head groups of a membrane. The combination disturbs the membrane to a minor extent and may produce a certain quantity of space for lipophilic parts of the prodrugs. The prodrugs diffuse through human skin, blood-brain barrier and blood-milk barrier 100 times quicker than theβ-lactam antibiotic substances. In blood plasma, the prodrugs in an amount of more than 90% of the blood plasma are changed in a few minutes and can be returned to parent drug. The prodrugs can be pharmaceutically used for treatment in a state being able to undergoβ-lactam antibiotic treatment in human or animal. Transdermal administration of the prodrugs is permitted for any kind of drug treatment. <P>COPYRIGHT: (C)2013,JPO&INPIT</p> |
