蒋新国, 陆翔, 崔景斌, 邱亮, 奚念朱. 药物的油—水分配系数与鼻腔吸收研究J. 药学学报, 1997, 32(6): 458-460.
引用本文: 蒋新国, 陆翔, 崔景斌, 邱亮, 奚念朱. 药物的油—水分配系数与鼻腔吸收研究J. 药学学报, 1997, 32(6): 458-460.
XG Jiang, X Lu, JB Cui, L Qiu , NZ Xi, . STUDIES ON OCTANOL-WATER PARTITION COEFFICIENT AND NASAL DRUG ABSORPTIONJ. Acta Pharmaceutica Sinica, 1997, 32(6): 458-460.
Citation: XG Jiang, X Lu, JB Cui, L Qiu , NZ Xi, . STUDIES ON OCTANOL-WATER PARTITION COEFFICIENT AND NASAL DRUG ABSORPTIONJ. Acta Pharmaceutica Sinica, 1997, 32(6): 458-460.

药物的油—水分配系数与鼻腔吸收研究

STUDIES ON OCTANOL-WATER PARTITION COEFFICIENT AND NASAL DRUG ABSORPTION

  • 摘要: 以油—水分配系数作为药物理化性质的一个指标,研究其与鼻腔吸收的关系。以脂溶性不同的盐酸地尔硫和对乙酰氨基酚为模型药物,用大鼠鼻腔在体重循环法研究了它们在不同pH条件下的鼻粘膜吸收速度常数,同时也测定了相应条件下的辛醇—水分配系数。结果表明,药物透鼻粘膜能力与其油—水分配系数有良好的相关性(γ=0.9761,n=9),提示鼻腔粘膜的性质与多数生物膜相似,脂溶性大的药物容易通过,而亲水性药物的通透性则较低。

     

    Abstract: In order to find out the quantitative relationship between physicochemical properties of drugs and their nasal absorption, diltiazem hydrochloride and paracetamol were selected as model drugs and their octanolwater partition coefficient was determined. In situ nasal recirculation method at different pH values was used to estimate the rate constant of nasal drug absorption in rats. Results showed that quantitative relationship existed between partition coefficient and nasal absorption constant, with correlation coefficient being 0.9761(n=9). Besides methods of partition coefficient determination, the in situ nasal recirculation manipulation was also improved.

     

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