正烷基羧酸在离体猪口腔黏膜中的渗透性研究

Permeability of N-alkyl Carboxylates through ex Vivo Porcine Buccal Mucosa

目的:研究正烷基羧酸的理化性质对其经离体猪口腔黏膜渗透性的影响。方法:选择正烷基羧酸中的乙酸、正丁酸、正己酸和正辛酸作为模型药物,采用Franz扩散池进行离体猪口腔黏膜渗透试验,用气相色谱法测定各样品浓度并计算渗透系数,同时与经人体皮肤的渗透系数文献值比较。结果:乙酸、正丁酸、正己酸和正辛酸透过猪口腔黏膜的渗透系数分别为2.05×10-5、3.03×10-5、1.66×10-4、1.19×10-4cm.s-1,人体皮肤渗透系数的文献值分别为9.77×10-8、3.47×10-7、3.80×10-6、6.61×10-6cm.s-1。结论:正烷基羧酸的猪口腔黏膜渗透性大于人体皮肤;该类化合物的脂溶性和分子体积等理化参数对其口腔黏膜渗透性的影响明显小于对人体皮肤。

OBJECTIVE： To study the effect of the physico - chemistical property of n - alkyl carboxylates on its permeability through ex vivo porcine buccal mucosa of pig. METHODS： Acetic acid, butanoic acid, hexanoic acid and caprylic acid were used as model drugs. The permeability of them through ex vivo porcine buccal mucosa of pig was studied using modified Franz diffusion cell; The concentrations of different samples were determined by gas chromatography （GC） and the permeability coefficients（P） of different samples were computed, which were compared with the P through human skin reported in literature. RESULTS： The P of acetic acid, butanoie acid, hexanoic acid and caprylic acid through porcine buecal mucosa were 2.05× 10^-5, 3.03× 10^-5, 1.66× 10^-4 and 1.19× 10^-4 cm.s^-1, respectively, and the P of which though human skin reported in literature were 9.77× 10^-8, 3.47× 10^-7, 3.80×10^-8 and 6.61× 10^-6 cm.s^-1, respectively. CONCLUSION： The permeability of carboxylates through porcine buecal mucosa of pig was greater than that through human skin. The liposolubility and the molecular volume （physico- chemistical parameters） of this kind of compounds had much less impact on the permeability of carboxylates through porcine buccal mucosa of pig than through human skin.