Study on Transdermal Compound Levonorgestrel and Estradiol Patch
WANG Qiao，CHEN Guo-shen
Author information+
Institute of Materia Medica，Zhejiang Academy of Medical Sciences，Hangzhou 310013，China
{{custom_zuoZheDiZhi}}
{{custom_authorNodes}}
{{custom_bio.content}}
{{custom_bio.content}}
{{custom_authorNodes}}
Collapse
History+
Received
Revised
Published
2008-10-12
2008-10-12
2008-10-12
Issue Date
2009-04-10
Abstract
OBJECTIVE To investigate the permeation of transdermal compound levonorgestrel(LNG) and estradiol(E2) patch.METHODS Transdermal permeability of LNG and E2 were carried out by using Valia-Chien double-compartment permeation cell and the permeation amounts of LNG and E2 within 168 h in vitro were examined by HPLC.RESULTS The LNG and E2 permeated through the human skin with different rates at 65 and 43 μg·d-1 respectively while the enhancers were composed of 8% azone,30% propylene glycol and 4% polyethylene glycol and the contents of LNG and E2 in patch were 4 and 2.5 mg·20 cm-2 respectively.The adhesiveness of patch was good.CONCLUSION The human skin permeation rates of LNG and E2 can meet the requirement of contraception.
WNG Qio;CHEN Guo-shen.
Study on Transdermal Compound Levonorgestrel and Estradiol Patch [J]. Chinese Pharmaceutical Journal, 2009, 44(08): 598-601
{{custom_sec.title}}
{{custom_sec.title}}
{{custom_sec.content}}
References
[1] SHULMAN L P. 17 Beta-estradiol/levonorgestrel transdermal system for the management of the symptomatic menopausal woman[J]. Expert Opin Pharmacother，2004，5(12)：2559-2566.
[2] VON HOLST T，SALBACH B. Efficacy of a new 7-day transdermal sequential estradiol/levonorgestrel patch in women[J]. Maturitas，2002，41(3)：231-242.
[3] CHEN G S，KIM D D，CHIEN Y W. Dual-controlled transdermal
delivery of levonorgestrel and estradiol：enhanced permeation and modulated delivery[J]. J Controlled Release，1995，34：129-143.
[4] FRIEND D，CATZ P，HELLER J，et al. Transdermal delivery of levonorgestrel I: Alkanols as permeation enhancers in vitro[J]. J Controlled Release，1988，7：243-250.
[5] FRIEND D R，CATZ P，HELLER J，et al．Transdermal delivery of levonorgestrel IV：Evaluation of membranes[J]．J Pharm Sci，1989，78(6)：477-480.
[6] LANDGREN B M，AEDO A R，JOHANNISSON E，et al. Studies on a vaginal ring releasing levonorgestrel at an initial rate of 27 micrograms/24 h when used alone or in combination with transdermal systems releasing estradiol[J]. Contraception，1994，50(1)：87-100.
[7] FRIEND D R，CATZ P，PHILLIPS S. Transdermal delivery of levonorgestrel. VII. In vivo studies[J]. Contraception，1989，40(1)：73-80.
[8] FRIEND D R. Transdermal delivery of levonorgestrel[J]. Med Res Rev，1991，11(1)：49-80.
[9] CHEN G S，ZHANG M Y，WANG Q，et al. The pharmacokinetics and pharmacodynamics of compound levonorgestrel transdermal delivery system on human[J]．Chin J Family Planning(中国计划生育杂志)，1997，31(5)：263-264,269.
[10] WANG Q，SHAO B，CHEN G S. Effects of EVAc membrane and enhancers on levonorgestrel permeation rate through human skin[J]. Chin Pharm J (中国药学杂志)，1998，33(11)：665-668.
[11] CHEN G S，GONH S J，DU J，et al. Transdermal permeability of estradiol through human skin of different body regions in vitro[J]. Acta Pharmacol Sin(中国药理学报)，1990，11(1)：57-59.
[12] CHEN G S，GONG S J，WANG Q，et al. Mechanism of controlled release of estradiol transdermal drug delivery system[J]. Chin J Pharm(中国医药工业杂志)，1994，25(1)：8-10.
[13] CHIEN Y W，CHIEN T Y，BAGDON R E，et al. Transdermal dual-controlled delivery of contraceptive drugs: formulation development，in vitro and in vivo evaluations，and clinical performance[J]. Pharm Res，1989，6(12)：1000-1010.
