Experimental Studies Of Absorption Of Jinlingzi Powder In Different Compatibilities

1 ObjectiveThe compatibility of prescription in traditional Chinese medicine (TCM) is the special feature and superiority of Chinese Material, and it is the significance guidance for clinical prescription to understand the rule of compatibility. The oral administration is the main form of Chinese Herbs, and the intestinal absorption is one of the important factors to contribute the bioavailability and the pharmaco-dynamic. According to orthogonal design, Jinlingzi powder is used as a case to investigate the absorption of the represents compounds in intestinal. Some representative constituents such as Toosendanin (TSN), d-Corydaline (CDL) and Tetrahydropalmatine (THP) are monitored. Three index including difference number, difference dose and difference proportion of Jinlingzi powder are used to describe their dynamic variety regulation and calculate the influence degree and modality of the prescripted drugs. Some mathematics equations and illustrations are presented to describe all the above results. At last the principle and signification of the compatibility of prescription in Chinese Material Medical is discussed.2 Method and Result2.1 Research the absorption of Jinlingzi powder in the single herbs and difference compatibility in the everted gut sacsMethod:The experiment employs the Lg(34) orthogonal design, which the Toosendanin extract and corydalis extract are used as two factors and difference dosage as three levels. The absorbance of nine compatibility and corresponding single herbs are studied by the means of the everted gut seas. Three representative composition of Jinlingzi powder, TSN, CDL and THP, were detected by HPLC and K values were calculated. The statistics is carried out by One-way ANOVA, the general linear model and normalization synthetic weighted mark method.Result:The absorption of TSN,CDL and THP in intestines is the zero order rate process, R2>0.95. The K of TSN, CDL and THP display the passive absorption. The absorption trend in different intestines of jejunum, ileum or colon is similar and the absorbed dose in colon is less. The intestinal absorption of THP is between 40% and 80%. The intestinal absorption of CDL or TSN and less 20%.The absorption dynamics of 3 compounds are distinct in Jinlingzi powder with the difference compatibility in orthogonal design. It is showed that the same compounds have the similar absorption trend in different intestine, and the different compounds are various in the absorption. The optimal absorption compatibility of 3 compounds are as follows:TSN (4:3), CDL (4:3). THP (1:3).The optimal proportion of the prescription compatibility is obtained by employing the multicriteria orthogonal analysis. The result shows the Toosendanin extract made the greater contribution in different intestine and the optimization of the compatibility is 4:3(Toosendanin extract /corydalis extract).2.2 Research the absorption of Jinlingzi powder in single herbs and the optimization compatibility in the Caco-2 cell monolayerMethod:the absorption of Caco-2 cell monolayer is similar with the small intestine epithelium, which can investigate the uptake and transport of extract of Chinese herbs and their compatibility. In the uptake experiment, The Caco-2 cells are seeded 24 pore plates, and add the drugs. One hour later, the cells are homogenate and the compounds content in cells are determined. In the transport experiment, the Caco-2 cells are seeded the Millicell, and twenty-one days later, the cells complete the differentiation and can be used to transport. Add drugs in AP or BL, and detect the receptor compounds.Result: The alKline phosphates in AP is over double BL at 21 day (P<0.05), which shows the cells already come into being polarity, and complete the differentiation. The transmissivity of the fluoresce in sodium is less than 1% in two hours. TEER is over 500Ω-cm2 that means the good integration and could use for transport experiment.The experiment of Caco-2 cells showed the passive absorption of TSN, CDL and THP, and the Pb-a/Pa-b is about 1. The uptake and excretion of TSN, CDL and THP in single herbs and the optimization compatibility are different. The uptake, absorption and excretion of CDL is decrease.But the uptake and excretion of THP is increased(P < 0.05). And it of TSN is similar. 3 ConclusionThe experiment is to research the intestinal absorption of the represents in the single herbs and the difference compatibility of Jinlingzi powder in the everted gut sacs and Caco-2 cells monolayer, which to elucidate the regularity and scientification of the compatibility of prescription. The mechanism of absorption of the represents in Jinlingzi powder is different, and the absorption has a change in the different compatibility. The optimal compatibility in absorption is 4:3(Toosendanin extract /corydalis extract).And the Toosendanin extract makes the greater influence which is the monarch, and the corydalis extract is a bit lower that make them minister.