Studies on Asthmatic Chinese Medicine Ⅱ Effect of Geniposide on Tracheal Permeability of Guinea Pigs and Its Pharmacokinetics

• Main Authors: Chao, Yen-Chin, 趙彥欽
• Other Authors: Liaw, Jiahorng
• Format: Others
• Language: zh-TW
• Published: 1995
• Online Access: http://ndltd.ncl.edu.tw/handle/55374278184704764146

碩士 === 台北醫學大學 === 生藥學研究所 === 83 === Asthma is a common disease of airway inflammation, and smite one of the important pathological manifestation is increased airway epithelial permeability. Due to the penetration of the allergens from airway lumen through tracheal epithelia, it causes mucus plugging and eosinophil infiltration by release mediators of as well as the damage to airway epithelial tissue. Therefore decreasing epithelial permeability, it could improve asthmatic tissue injuries and reduce asthmatic symptoms. Geniposide, a major component from Gardenia jasminoides Ellis, has been used an antiphlogisic, a diurtic and a chalaogues in Chinese medicine. We have investigated the anti-inflammatory of geniposide effect on guinea pig trachea by introduction of inhaled ovalbumin challenge-induced. The data showed that 10mM of geniposide had protective effect on the asthmatic tracheal permeability. In addition, using aerosol dosage form of 50mM geniposide, it could improve the integrity of asthmatic tissues and preserve the tight junction structure. In order to understand the bioavailability of geniposide, we investigated the parameters of IV basic pharmacokinetics. A high- performance liquid chromatographic method used for the determination of geniposide in rabbit serum was developed. Geniposide in rabbit serum was extracted under methanoi denaturation condition and then injected into a reverse-phase column, it could be detected at UV 240nm using H20-CH3CN-THF=90 : 8 : 2 as the mobile phase. The results showed that the effect of geniposide could be fit into a two compartment model in vivo of rabbit and the average α (distribution-half life was 2.945±0.251 minutes, β (elimination-half life was 16.305 ±1.435 minutes, overall the central volumn of distribution(V1) was 0.210 ±0.021 liter/kg, and the clearance rate was 0.027±0.012 liter/min/kg. In the model model, the mean residence time was calculated to be 17.514 ±0.382 minutes.