摘要
目的考察研制的复方左炔诺孕酮/雌二醇(LNG/E2)透皮吸收贴片的渗透性。方法采用Valia-Chien双室渗透池进行体外经皮渗透实验,以HPLC测定药物浓度求算168h内的渗透量。结果8%月月月月酮、30%丙二醇、4%聚乙二醇400为混合促进剂,LNG和E2的含量分别为4mg·20cm-2,2.5mg·20cm-2时,研制的LNG/E2透皮贴片能使LNG和E2分别以65和43μg·d-1的速率透过人离体皮肤,黏着性较好。结论LNG和E2的体外人体皮肤渗透率可达避孕贴片设计要求。
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.
关键词
左炔诺孕酮 /
雌二醇 /
贴片 /
透皮给药系统
{{custom_keyword}} /
Key words
levonorgestrel /
estradiol /
patch /
transdermal delivery system
{{custom_keyword}} /
王俏;陈国神.
复方左炔诺孕酮/雌二醇透皮吸收贴片的研制[J]. 中国药学杂志, 2009, 44(08): 598-601
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}}
参考文献
[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.
{{custom_fnGroup.title_cn}}
脚注
{{custom_fn.content}}
基金
浙江省计划生育委员会项目
{{custom_fund}}
