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Dr. Kai Lv Yexin Sun Lanyin Sun Zengquan Wei Prof. Huiyuan Guo Jinwei Wu Prof. Mingliang Liu 《ChemMedChem》2012,7(7):1300-1300
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《Drug development and industrial pharmacy》2013,39(6):724-734
Purpose: This study was aimed at investigating the possible relationship between the physical properties and the permeation of S-amlodipine and RS-amlodipine and studying the possible enantioselectivity of permeation of amlodipine in the presence and absence of enhancers, such as terpene enhancers and ethanol. Method: The solubility of S-amlodipine and RS-amlodipine was measured using the shake-flask method. The thermodynamic properties were investigated by differential scanning calorimetry (DSC). The type of racemate amlodipine was investigated by DSC and Fourier transform infrared spectroscopy (FTIR). The permeability of racemate and enantiomers of amlodipine through rat epidermis in vitro was investigated using the modified Franz diffusion cell. Results: The aqueous solubility of S-amlodipine was higher than that of RS-amlodipine. The melting temperature and enthalpy of fusion of S-amlodipine were lower than those of RS-amlodipine. RS-amlodipine was a racemic compound. The permeation of the enantiomers of amlodipine from RS-amlodipine reservoir showed no significant differences in the presence and absence of enhancers, but the permeation of S-amlodipine from S-amlodipine reservoir was significantly higher than that of RS-amlodipine from RS-amlodipine reservoir 30% ethanol, 50% ethanol, and terpene enhancers could not influence the difference in permeation between S-amlodipine and RS-amlodipine, but 75% ethanol could reduce the difference. Conclusion: These results suggested that there was no enantioselectivity of the enantiomers of amlodipine from RS-amlodipine reservoir in the presence and absence of enhancers, but the differences in physical properties between S-amlodipine and RS-amlodipine led to the difference in permeation across rat skins. 相似文献
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Mark L. Winston Keith N. Slessor Michael J. Smirle Ali A. Kandil 《Journal of chemical ecology》1982,8(10):1283-1288
The effect of enantiomers of the queen-produced substance, 9-hydroxy-(E)-2-decenoic acid (9HDA) on swarm clustering behavior of the honeybeeApis mellifera was studied. Caged queens were removed from the swarms at the start of each test and were replaced with small Petri dishes containing one of the following treatments: 100 gS(+) enantiomer of 9HDA, 100 gR(-) enantiomer of 9HDA, 200 g racemic (R, S) 9HDA, and a vehicle-treated control. Each swarm was considered to have dispersed when it had lost 50% of its starting weight. All treatments with 9HDA resulted in significantly longer swarm aggregation when compared with the control. Enantiomers were not shown to have different effects at theP 0.05 level of significance. However, observations on swarm behavior indicated that theR(-) enantiomer was the most active in retarding swarm dispersal. 相似文献
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