The present invention relates to a method and an improved composition for improving the absorption of an ester prodrug in a subject. The method includes co-administering to the subject an effective amount of the ester prodrug or a pharmaceutical acceptable salt thereof, and a sufficient amount of adjuvant to impede a carboxylesterase-mediated hydrolysis of the ester prodrug in vivo, wherein the adjuvant is selected from the group consisting of triacetin, triethyl citrate and a combination of both. The present invention also relates to a method for impeding carboxylesterase-mediated hydrolysis of esters, including ester prodrugs.本發明有關於用以改善個體體內酯類前驅藥吸收率的方法與改良之藥學組合物。上述方法包含一併對個體投予治療有效量的酯類前驅藥或其藥學上可接受鹽類,以及足量的佐劑,以阻礙酯類前驅藥於活體內經脫羧醣酯酶媒介而水解;上述佐劑為三乙酸甘油酯、檸檬酸三乙酯或兩者的混合物。本發明亦有關於用以阻礙酯類(包括酯類前驅藥)經脫羧醣酯酶媒介而水解的方法。
