Topical penetration of commercial salicylate esters and salts using human isolated skin and clinical microdialysis studies.

作者: Sheree E. Cross , Chris Anderson , Michael S. Roberts

DOI: 10.1046/J.1365-2125.1998.00045.X

关键词:

摘要: Aims The penetration of active ingredients from topically applied anti-inflammatory pharmaceutical products into tissues below the skin is basis their therapeutic eYcacy. There still controversy as to whether these agents are capable direct by diVusion through or redistribution in systemic circulation responsible for tissue deposition application site. Methods extent salicylate commercial ester and salt formulations dermal subcutaneous human volunteers was determined using technique cutaneous microdialysis. We also examined diVerences hydrolysis methylester vitro cells full-thickness epidermal membranes. Results present study showed that whilst significant levels could be detected dermis treated with methylsalicylate formulation, negligible were seen following triethanolamine formulation. formulation approx. 30-fold higher than plasma concentrations. absorption concentration profiles indicative not solely blood supply.

参考文章(23)
J. A. Fraser Roberts, Some Practical Applications Springer, Boston, MA. pp. 164- 171 ,(1965) , 10.1007/978-1-4899-6580-6_13
James Boehnlein, Adel Sakr, J. Leon Lichtin, Robert L. Bronaugh, Characterization of esterase and alcohol dehydrogenase activity in skin. Metabolism of retinyl palmitate to retinol (vitamin A) during percutaneous absorption. Pharmaceutical Research. ,vol. 11, pp. 1155- 1159 ,(1994) , 10.1023/A:1018941016563
M S Roberts, P Singh, Local deep tissue penetration of compounds after dermal application: structure-tissue penetration relationships. Journal of Pharmacology and Experimental Therapeutics. ,vol. 279, pp. 908- 917 ,(1996)
M S Roberts, P Singh, Skin permeability and local tissue concentrations of nonsteroidal anti-inflammatory drugs after topical application. Journal of Pharmacology and Experimental Therapeutics. ,vol. 268, pp. 144- 151 ,(1994)
S. E. Cross, M. S. Roberts, Zhenyu Wu, The effect of protein binding on the deep tissue penetration and efflux of dermally applied salicylic acid, lidocaine and diazepam in the perfused rat hindlimb. Journal of Pharmacology and Experimental Therapeutics. ,vol. 277, pp. 366- 374 ,(1996)
Asher Pardo, Yoseph Shiri, Sasson Cohen, Kinetics of transdermal penetration of an organic ion pair: physostigmine salicylate. Journal of Pharmaceutical Sciences. ,vol. 81, pp. 990- 995 ,(1992) , 10.1002/JPS.2600811006
Markus Müller, Rainer Schmid, Oswald Wagner, Bettina v. Osten, Houshang Shayganfar, Hans G Eichler, In vivo characterization of transdermal drug transport by microdialysis Journal of Controlled Release. ,vol. 37, pp. 49- 57 ,(1995) , 10.1016/0168-3659(95)00063-E
Lutz Hegemann, Christa Forstinger, Bernhard Partsch, Irmgard Lagler, Sabine Krotz, Klaus Wolff, Microdialysis in Cutaneous Pharmacology: Kinetic Analysis of Transdermally Delivered Nicotine Journal of Investigative Dermatology. ,vol. 104, pp. 839- 843 ,(1995) , 10.1111/1523-1747.EP12607019
A. Danon, S. Ben-Shimon, Z. Ben-Zvi, Effect of exercise and heat exposure on percutaneous absorption of methyl salicylate. European Journal of Clinical Pharmacology. ,vol. 31, pp. 49- 52 ,(1986) , 10.1007/BF00870985