• 中国精品科技期刊
  • 中国高校百佳科技期刊
  • 中国中文核心期刊
  • 中国科学引文数据库核心期刊
Advanced Search
GAO Yan-li, XIAO Yan, LIANG Jin-ying, ZHU Xuan-xuan, LI Ying, LIU Jian-ping. Double-layer patch containing gestodene and ethinylestradiol:preparation and in vitro/in vivo characterization[J]. Journal of China Pharmaceutical University, 2009, 40(5): 416-420.
Citation: GAO Yan-li, XIAO Yan, LIANG Jin-ying, ZHU Xuan-xuan, LI Ying, LIU Jian-ping. Double-layer patch containing gestodene and ethinylestradiol:preparation and in vitro/in vivo characterization[J]. Journal of China Pharmaceutical University, 2009, 40(5): 416-420.

Double-layer patch containing gestodene and ethinylestradiol:preparation and in vitro/in vivo characterization

More Information
  • Aim :To prepare a novel contraceptive patch containing gestodene(GEST) and ethinylestradiol(EE),and to study the in vitro characterization and in vivo contraceptive effect. Methods :Double-layer technique was applied to sustain steady 7-day permeation flux of drugs.Polariscope examination was carried out to observe the drug distribution behavior in the patch.Uniformity,adhesion,skin irritation,release and permeation tests were conducted to evaluate in vitro characterization.Anti-implantation and anti-fertility experiments were carried out to investigate its contraceptive effect. Results :The in vitro release profiles of both drugs were in accordance with Higuchi equation.The daily permeated amount of GEST per 10 cm2 patch was about 75 μg while the amount of EE was 30 μg.The in vitro transdermal permeation of both drugs from the patches displayed a zero-order process.Permeation rate constants were 0.377 μg/(cm2 ·h) for GEST,and 0.092 μg/(cm2 ·h) for EE,respectively.After transdermal administration,the embryonic number of the test groups was zero,and the uterus coefficients of those groups were significantly reduced compared with those of the control group (P<0.01). Conclusion :Double-layer transdermal drug delivery system(TDDS) could allow the steady 7-day permeation flux of drugs when the drug ratio between the immediate-release layer and the reservoir layer was 1∶4.In vivo characterization demonstrated its contraceptive effects.The prepared novel patch might be a promising non-oral contraceptive preparation.
  • Related Articles

    [1]WU Yang-yang, GAO Yan-li, LIU Jian-ping, SUN Jian-guo, WANG Guang-ji. In vitro permeation and in vivo pharmacokinetics of once-weekly contraceptive patch containing gestodene and ethinlyestradiol[J]. Journal of China Pharmaceutical University, 2012, 43(1): 35-42.
    [3]Effect of 3,5 Diisopropylsalicylic Acid and Its Copper Complex on Glutathione Chemical Modulation and Metabolism in the Cytosolic Fraction of Human Blood[J]. Journal of China Pharmaceutical University, 1997, (5): 49-52.
    [4]Enhancing Effect of Geraniol on the Permeation of 5 Fluorouracil Through Excised Rat Skin[J]. Journal of China Pharmaceutical University, 1997, (4): 16-19.
    [5]Gas Chromatographic-Mass Spectrometric Method for Determination of Metandienone and Its Metabolites in Urine[J]. Journal of China Pharmaceutical University, 1991, (5): 282-285.
    [6]STUDY OF PREPARATION ON CONTRACEPTIVE CREAM AND ITS PERCUTANEOUS ABSORPTION[J]. Journal of China Pharmaceutical University, 1987, (4): 247-250.
    [7]Hu Yuzhu, Yu Rugu. DETERMINATION OF ETHINYL ESTRADIOL IN TABLETS BY FLUORESCENCE SPECTROPHOTOMETRY[J]. Journal of China Pharmaceutical University, 1983, (3): 9-15.
    [8]Dong Shanshi, Yang Jingrong, An Dengkui. DETERMINATION OF NONOXYNOL-9 IN THE CAPSHAPED CONTRACEPTIVE FILMS BY ORTHOGONAL POLYNOMIAL SPECTROPHOTOMETRY[J]. Journal of China Pharmaceutical University, 1982, (3): 57-58.
    [9]Dong Shanshi, Yang Zhongyuan, An Dengkui. Comparative Study of the Determination of Nonyl phenoxy-polyoxyethylethanol in Contraceptive Film.[J]. Journal of China Pharmaceutical University, 1980, (2): 64-70.
    [10]Yang Zhongyuan, Dong Shanshi, An Dengkui. Determination of Nonylphenoxylpolyoxyethylethanol in Contraceptive Films by Orthogonal Functions Method[J]. Journal of China Pharmaceutical University, 1980, (1): 54-57.

Catalog

    Article views (1305) PDF downloads (1391) Cited by()

    /

    DownLoad:  Full-Size Img  PowerPoint
    Return
    Return