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Wysłany: Czw 14:42, 24 Lut 2011 Temat postu: asics shoes online Kampo drug interactions (8) rat |
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Kampo drug interactions (8): The intestinal CYP3A activity of microsomes
Results show that even in the same botanical origin of Curcuma herbs, and other factors due to the different origin of the inhibition varied significantly. Therefore, in taking health food products containing these ingredients should be careful. 139 Schisandra composition on the inhibition of CYP3A4 [Japanese] / Iwata macro ... of 83 Crude Drug inhibition of CYP3A4 and CYP2D6, which inhibit the CYP3A4 Schisandra significant role, this time its active ingredients were selected. Methods: Schisandra extract powder ether soluble fraction separated by HPLC to detect the various parts of the CYP3A4 inhibition. From commercial human liver microsomes as the enzyme source, erythromycin as a substrate in the presence of NADPH generating system by solid phase column extraction and separation of radioactive demethylation reaction of HCHO, calculated based on radioactivity of the metabolic activity of CYP3A4, and separation suppression components, the pharmacokinetic analysis. Results and Discussion: Extract from Schisandra 4 inhibition of isolated components,[link widoczny dla zalogowanych], the spectral analysis to determine the structure of these inhibitory components, which inhibit the activity of the strongest components were identified as high-Missing C, the inhibition of CYP3A4 metabolic activity constants (Ki values) for the 0.0491aM, under the same conditions ketoconazole Ki value 0.0701aM. These results indicate that Schisandra extract contains powerful ingredients inhibit CYP3A4. Schisandra compatibility with Kampo medicine prescription and use, due to inhibition of CYP3A4 metabolism of Schisandra, it may cause drug interactions. 140 Kampo drug interactions (8): rat small intestine microsomal CYP3A activity [Japanese] / Matsumoto just ... to mushroom diltiazem (DTZ) as a CYP3A substrate,[link widoczny dla zalogowanych], of a single oral dose given to 25 kinds of Kampo formulas on the microsomes derived from intestinal CYP3A activity. Methods: Experimental animals Male Wistar rats 9 weeks of age, * 125 * given a single dose of oral prescription of various Kampo extract suspension (10 times the clinical dose or amount of his), 3h after the small intestine, according to often the legal system of the small intestine microsomes. In the presence of NADPH generating system,[link widoczny dla zalogowanych], the microsomes (300gg) and DTZ (251aM) and incubated at 37 ~ C 5min,[link widoczny dla zalogowanych], detection DTZN a demethylation activity, and compared with the control group. Results and Discussion: In addition to Chaihuguizhi soup, the other formula (1O times the clinical dose volume) have shown that enhanced intestinal microsomal CYP3A activity trends. Especially Fangjihuangqi soup, soup ephedra, Ginseng, Banxiabaizhutianma soup, and Chai Ling, Gui Zhi Tang Ginseng significantly increased CYP3A activity. Thus indicating that some kind of Kampo Formula and DTZ Western CYP3A substrate and used, may make the initial permeability of the small intestine of the metabolic changes in medicine. 141 N Xiaoqinglongtang leather and hydrochloric acid drug interactions between Sting [Japanese] / Inagaki your margin ... the anti-histamine drug hydrochloride nitrogen mushroom Sting (Az) Xiao Qing Long Tang combined with a significant effect, this study has two drug interactions. Methods: SD rats (female, 9 weeks old) given orally every 12h Xiao Qing Long Tang extract powder, administered 4 times per O. 1g or lg / kg. 1h after the last oral administration (10mg/kg) or intravenous administration (0.5mg/kg) AZ. Blood following a time to LC / MS detection of blood levels of AZ, the pharmacokinetic analysis. Results and Discussion: Xiao Qing Long Tang Duijing pulse taking the time to give AZ had no effect on the body dynamics; and use low-dose Xiao Qing Long Tang (approximately 2 times the human dose used),[link widoczny dla zalogowanych], the dynamics of AZ had no effect on the body; high dose Xiao Qing Long Tang ( dose of about 2O times were used), the significantly lower (P <0.05) AZ's largest concentration of the blood (Cmax), significantly increased (P <O.05) mean residence time (MRT). But no significant effect on AUC and half-life therefore speculated that Xiao Qing Long Tang has no effect on the metabolism of AZ, the high dose because the formation of insoluble salts and the influence of physical factors, delaying the absorption of AZ. That if used by clinical doses, AZ asked Xiao Qing Long Tang and no pharmacokinetic interaction. (Yiyue Excerpt) (to be continued) '
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