Long-Term Permeation Kinetics of Estradiol: (III) Kinetic Analyses of the Simultaneous Skin Permeation and Bioconversion of Estradiol Esters
作者： Kirti H. Valia , Kakuji Tojo , Yie W. Chien
DOI: 10.3109/03639048509059861
关键词:
摘要: AbstractThe skin permeation system developed earlier in this laboratory was utilized to study the kinetics of simultaneous and bioconversion 5 estradiol esters. The equilibrium solubility esters lipophilic silicone fluid hydrophilic PEG 400/saline solution found be dependent upon alkyl chain length Estradiol-3,17-diacetate had a greater lower than estradiol-17-acetate. (skin/silicone fluid) partition coefficients were observed decrease as increased length. During course permeation, metabolized by esterase regenerate estradiol. rate appearance from ester concentration on stratum corneum surface follow order of: diacetate > valerate heptanoate cypionate acetate. From dermal uptake metabolism s...
informapharmascience.com参考文章(21)
R.J. Scheuplein, I.H. Blank, G.J. Brauner, Dorothy J. Macfarlane, Percutaneous Absorption of Steroids* Journal of Investigative Dermatology. ,vol. 52, pp. 63- 70 ,(1969) , 10.1038/JID.1969.9
Francis N. Marzulli, John F. Callahan, D.W.C. Brown, Chemical Structure and Skin Penetrating Capacity of a Short Series of Organic Phosphates and Phosphoric Acid**From the Dermal Toxicity Branch, DP, Bureau of Scientific Research, Food and Drug Administration, Washington, D.C. and the Field Toxicology Branch, Toxicology Division, Chemical Research & Development Laboratories, Edgewood Arsenal, Maryland. Journal of Investigative Dermatology. ,vol. 44, pp. 339- 344 ,(1965) , 10.1038/JID.1965.59
Birgitte Møllgaard, Annie Hoelgaard, Hans Bundgaard, Pro-drugs as drug delivery systems XXIII. Improved dermal delivery of 5-fluorouracil through human skin via N-acyloxymethyl pro-drug derivatives International Journal of Pharmaceutics. ,vol. 12, pp. 153- 162 ,(1982) , 10.1016/0378-5173(82)90115-6
Irvin H. Blank, Robert J. Scheuplein, Dorothy J. Macfarlane, Mechanism of Percutaneous Absorption Journal of Investigative Dermatology. ,vol. 49, pp. 582- 589 ,(1967) , 10.1038/JID.1967.184
A. NIMROD, K. J. RYAN, Aromatization of androgens by human abdominal and breast fat tissue. The Journal of Clinical Endocrinology and Metabolism. ,vol. 40, pp. 367- 372 ,(1975) , 10.1210/JCEM-40-3-367
Dale E. Wurster, Sherman F. Kramer, Investigation of some factors influencing percutaneous absorption Journal of Pharmaceutical Sciences. ,vol. 50, pp. 288- 293 ,(1961) , 10.1002/JPS.2600500403
DAVID T. BAIRD, AMELIA GUEVARA, Concentration of unconjugated estrone and estradiol in peripheral plasma in nonpregnant women throughout the menstrual cycle, castrate and postmenopausal women and in men. The Journal of Clinical Endocrinology and Metabolism. ,vol. 29, pp. 149- 156 ,(1969) , 10.1210/JCEM-29-2-149
K.B. Sloan, N. Bodor, Hydroxymethyl and acyloxymethyl prodrugs of theophylline: enhanced delivery of polar drugs through skin International Journal of Pharmaceutics. ,vol. 12, pp. 299- 313 ,(1982) , 10.1016/0378-5173(82)90101-6
S. S. C. YEN, P. L. MARTIN, A. M. BURNIER, N. M. CZEKALA, M. O. GREANEY, M. R. CALLANTINE, Circulating Estradiol, Estrone and Gonadotropin Levels Following the Administration of Orally Active 17β-Estradiol in Postmenopausal Women The Journal of Clinical Endocrinology and Metabolism. ,vol. 40, pp. 518- 521 ,(1975) , 10.1210/JCEM-40-3-518
Hans Bundgaard, Annie Hoelgaard, Birgitte Møllgaard, Leaching of hydrolytic enzymes from human skin in cutaneous permeation studies as determined with metronidazole and 5-fluorouracil pro-drugs International Journal of Pharmaceutics. ,vol. 15, pp. 285- 292 ,(1983) , 10.1016/0378-5173(83)90162-X