Takahashi K, Matsumoto T, Kimura T, Sakano H, Mizuno N, Yata N
Institute of Pharmaceutical Sciences, Mukogawa Women's University School of Pharmacy, Hyogo, Japan.
Biol Pharm Bull. 1996 Jun;19(6):893-6. doi: 10.1248/bpb.19.893.
The effects of a series of polyol fatty acid esters (sefsols) on diclofenac permeation through rat skin were investigated using in vitro and in vivo methods. Four monoesters and one diester of sefsol were selected as a vehicle components. The effects of each sefsol on in vitro diclofenac permeation were compared at a concentration of 5% sefsol in water. Monoesters of sefsol, except the glyceryl monoester, enhanced the percutaneous permeation of diclofenac. The highest enhancement was observed in propylene glycol monocaprylate. The plasma concentration of diclofenac was increased dramatically by the addition of 10% propylene glycol monocaprylate when applying the diclofenac sodium suspension to abdominal rat skin in vivo. These results suggest that the monoesters of polyol fatty acid are potential candidates to enhance the transdermal absorption of diclofenac sodium.
采用体外和体内方法研究了一系列多元醇脂肪酸酯(sefsols)对双氯芬酸透过大鼠皮肤的影响。选择了四种sefsol单酯和一种双酯作为载体成分。在水中sefsol浓度为5%时,比较了每种sefsol对体外双氯芬酸渗透的影响。除甘油单酯外,sefsol单酯均增强了双氯芬酸的经皮渗透。在丙二醇单辛酸酯中观察到最高的增强效果。当在体内将双氯芬酸钠混悬液应用于大鼠腹部皮肤时,添加10%的丙二醇单辛酸酯可使双氯芬酸的血浆浓度显著增加。这些结果表明,多元醇脂肪酸单酯是增强双氯芬酸钠透皮吸收的潜在候选物。