栀子环烯醚萜苷鼻腔给药的吸收特性

Absorption Characteristics of Nasal Drug Delivery of Gardenia Iridoid Glycoside

关键词:  栀子环烯醚萜苷  栀子苷  鼻腔给药  鼻腔循环灌流实验

Key words:  gardenia iridoid glycoside  geniposide  nasal drug delivery  nasal circulatory perfusion test

摘要:

目的 研究栀子环烯醚萜苷类成分鼻腔给药的吸收特性，为其鼻腔给药制剂设计提供依据。方法 采用Franz扩散池，选用新鲜猪鼻黏膜为渗透屏障，以栀子苷为测定指标，HPLC测定含量，进行渗透试验；采用大鼠鼻腔循环灌流实验，以PBS溶液(pH7.4)作为鼻腔循环液，HPLC测定栀子苷，进行在体鼻黏膜吸收试验。结果 栀子苷表观渗透系数Papp 为(2.01±0.23)×10^-5 cm^-2·s^-1；药物稳态流量Jss为(1.61±0.18)×10^-4 μg·cm^-2·s^-1，透黏膜扩散属于以膜两侧浓度差为动力的被动扩散。栀子苷大鼠在体鼻黏膜吸收动力学方程lnC=1.165 7-0.001 6t，r=0.991 4，k=(1.6±0.021)×10^-3 min^-1。结论 栀子环烯醚萜苷可经鼻吸收，可制成经鼻给药的新制剂用于脑部疾病的防治。

Abstract:

OBJECTIVE To study the absorption characteristics of a nasal drug delivery of gardenia iridoid glycoside, so as to provide some technicial consults of its nasal drug delivery system. METHODS Using Franz diffusion cell, the fresh nasal mucosa of pig was used for permeability barrier, the geniposide was determined by HPLC as indexs. Using medicated PBS(pH=7.4) for nasal liquid circulation, the geniposide was determined by HPLC with using rat nasal circulatory perfusion experiments(in situ). RESULTS The apparent permeability coefficient (Papp) of geniposide was (2.01±0.23)×10^-5 cm^-2·s^-1, the steady state flow (Jss) of geniposide was (1.61±0.18)×10^-4 μg·cm^-2·s^-1, the diffusion through mucosa was a passive diffusion with concentration difference of both mucosal sides. The absorption kinetics equation of geniposide in rat nasal mucosa(in vivo) was lnC=1.165 7-0.001 6t, r=0.991 4, k=(1.6±0.021)×10^-3 min^-1. CONCLUSION Gardenia iridoid glycoside can be absorbed through nasal mucosa, which can be made into new nasal preparations for the prevention and treatment of brain diseases.