The influence of chirality, physicochemical properties, and permeation enhancers on the transdermal permeation of amlodipine across rat skin
The influence of chirality, physicochemical properties, and permeation enhancers on the transdermal permeation of amlodipine across rat skin
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手性、理化性质和渗透促进剂对氨氯地平大鼠皮肤透皮渗透的影响
DOI：
10.3109/03639040903460438
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发表时间：
2010-05
影响因子：
3.4
通讯作者：
Qiang Fu
中科院分区：
文献类型：
--
作者：
Changhe Wang;Guangde Yang;Aiguo Zeng;Bingxiang Yuan;Qiang Fu
目的：本研究的目的是调查的物理性质之间的可能的关系和渗透的S-ESTA和RS-ESTA和研究可能的对映体选择性的渗透在存在和不存在的促进剂，如萜烯促进剂和乙醇的ESTA。方法：采用摇瓶法测定S-山梨醇和RS-山梨醇的溶解度。用差示扫描量热法（DSC）研究了其热力学性质。用DSC和FTIR对产物的结构进行了表征。采用改进的Franz扩散池研究了氨氯地平外消旋体和对映体体外透过大鼠表皮的渗透性。结果：S-羟丙基甲基纤维素的水溶性大于RS-羟丙基甲基纤维素。S-β的熔融温度和熔融焓低于RS-β。RS-125是一种外消旋化合物。在有无促渗剂的情况下，RS-120对映体的渗透无显著性差异，但S-120对映体的渗透显著高于RS-120对映体的渗透，30%乙醇、50%乙醇对S-120和RS-120对映体的渗透无显著性差异，萜类促渗剂对S-120和RS-120对映体的渗透无显著性影响。而75%乙醇可降低差异。结论：这些结果表明，在存在和不存在促进剂的情况下，从RS-C18储库中的C18对映体不存在对映体选择性，但是S-C18和RS-C18之间的物理性质的差异导致了通过大鼠皮肤的渗透的差异。
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.
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影响因子：
3.8
作者：
K. Midha;G. Mckay;M. Rawson;J. Hubbard
通讯作者：
K. Midha;G. Mckay;M. Rawson;J. Hubbard
影响因子：
1.7
作者：
K. Miyazaki;F. Kaiho;A. Inagaki;M. Dohi;N. Hazemoto;M. Haga;H. Hara;Y. Kato
通讯作者：
K. Miyazaki;F. Kaiho;A. Inagaki;M. Dohi;N. Hazemoto;M. Haga;H. Hara;Y. Kato
影响因子：
1.7
作者：
HATANAKA, T;INUMA, M;MORIMOTO, Y
通讯作者：
MORIMOTO, Y
DOI：
10.1016/s0378-4347(97)00394-0
发表时间：
1997-12-05
影响因子：
3
作者：
Luksa, J;Josic, D;Milutinovic, S
通讯作者：
Milutinovic, S
影响因子：
3.8
作者：
Kommuru, TR;Khan, MA;Reddy, IK
通讯作者：
Reddy, IK