U.S. patents available from 1976 to present.
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Estradiol transdermal delivery system

Patent 4906475 Issued on March 6, 1990. Estimated Expiration Date: Icon_subject February 16, 2008. Estimated Expiration Date is calculated based on simple USPTO term provisions. It does not account for terminal disclaimers, term adjustments, failure to pay maintenance fees, or other factors which might affect the term of a patent.

Patent References

3249109

3426754

3464413

3472931

3527864

3598122

3598123

3632740

3641237

3699963

More ...

Inventor

Assignee

Application

No. 156266 filed on 02/16/1988

US Classes:

424/449, Transdermal or percutaneous424/447, Bandages with incorporated medicaments424/448Pressure sensitive adhesive means

Examiners

Primary: Robinson, Ellis P.
Assistant: Horne, Leon R.

Attorney, Agent or Firm

Foreign Patent References

  • 0764422 BE 08/13/1971
  • 0930668 CA 07/13/1973
  • 144486 EP. 06/13/1985
  • 3333240 DE. 03/13/1985
  • 2224126 FR 10/13/1974
  • 2224140 FR 10/13/1974
  • 2437830 FR. 04/13/1980
  • 0537493 JP. 03/13/1978
  • 139011 JP. 08/13/1982
  • 058913 JP. 06/13/1983
  • 87/03490 WO. 06/13/1987
  • 1001949 GB. 01/13/1965
  • 1108837 GB. 04/13/1968
  • 2021950 GB. 12/13/1979
  • 2158355 GB. 11/13/1985

International Class

A61F 013/00

Abstract

The present invention is directed to a transdermal delivery system for an active substance. The active substance is estrogen or its derivatives and preferably is 17-beta-estradiol. The system comprises an impermeable backing layer and a matrix affixed thereto. The matrix comprises, on a weight percentage basis, from about 60 to about 95% of an adhesive polymer, from about 5 to about 20% of a solvent, from about 0.2 to about 4% of a skin penetration enhancer, and from about 0.5 to about 5% of the active substance. The system is free of any discrete permeable, polymeric, diffusion-controlling membrane.

Other References

  • Cooper, E. R., "Increased Skin Permeability for Lipophilic Molecules", J. Pharm. Sci., Aug. 1984, vol. 73, No. 8, pp. 1153-1156
  • F. S. Kilmer MacMillan, et al., "The Antiperspirant Action of Topically Applied Anticholinergics", The Journal of Investigative Dermatology, vol. 43, pp. 363-377, 1964
  • A. S. Michaels et al., Drug Permeation Through Human Skin: Theory and in vitro Experimental Measurement, American Institute of Chemical Engineers Journal, vol. 21, No. 5, pp. 985-996, 1975
  • Dow Corning, New Product Information Brochure, Silastic.RTM. Q7-4840 A/B Medical Grode Liquid Silicone Rubber (LSR) 1981
  • Valia, et al. "Transdermal Controlled Administration of Estradiol Derviates and Structure-Kinetic Relationships", Dissertaton Abstracts Intn'l vol. 46, No. 2, 8/85
  • Chein, et al., "Long Term Permeation Kinetics of Estradiol", Drug Development and Industrial Pharmacy, vol. 11, Nos. 6 & 7, pp. 1195-1212, 1985
  • Guy et al., "Interpretation and Prediciton of the Kinetics of Transdermal Drug Delivery: oestradiol, hyoscine and timolol", Intn'l J. of Pharmaaceutics, vol. 32, pp. 159-163 (1986)
  • Acharya, et al., "Observations on 17-B-Hydroxysteriod Dehydrogenase in the Broad Patch of House Sparrow", Current Sci., vol. 53, No, 3, pp. 160-162, 2/1984
  • Judd, "Efficacy of Transdermal Estradiol", Am. J. Obstet Gynecol, May 1987
  • Jones, et al., "Incubation Patch of the Chicken", Gen. and Comp Endocr. vol. 15, pp. 398-403, 1970
  • Hutchinson, et al., "The Effects of Estrogen Progesterone and Prolactin on Brood Patch Formation in Ovariectomized Canaries", J. Endocr., vol. 39, pp. 379-385 (1967)
  • Hohn, "Failure to Induce Incubation Behavior . . . " Gen. and Comp. Endocr., vol. 44, pp. 396-399 (1981)
  • Padwick et al., "Efficacy, Acceptability, and Metabolic Effects of Transdermal Estradiol . . . ", Am J. Obstet Gyncol., p. 1085 et seq. 8/1985
  • Chetkowski, et al., "Biological Effects of Transdermal Estradiol"; New Eng. J. of Med. vol. 314, No. 25, p. 1615 et seq., Jun. 1986
  • Selby, et al., "The Effect of Transermal Oestrogen Bone . . . ", Clin. Endocr., vol. 25, pp. 543-547, 1986
  • Tojo, et al., "Bioconversion of Estradiol Esters in Hairless Mouse Skin in Vitro", Chemical Eng. J., vol. 33, B63-B67, 1986
  • Baker, et al., "Patients in Transermal Drug Delivery", Drug Delivery Systems, pp. 26-31 (1987)
  • CTFA-Cosmetic Ingredient Dictionary, 1st ed., The Cosmetic, Toiletry, and Fragrance Assocation, Inc., Washington, D.C. 1973, pp. 126-127
  • Idson, B., "Perculaneous Absorption", Journal of Pharm. Sci., Jun. 1975, pp. 901-924
  • Higuchi, T., "Rate of Release of Medicaments from Ointment Bases Containing Drugs in Suspension," J. of Pharm. Sci., Oct. 1961, pp. 874-875
  • "Cases Where the Rate Controlling Step is in the Applied Phase", J. of Soc. of Cosmetic Chemists, pp. 94-97
  • Haleblian, J. et al., "Steroid Release from Silicone Elastomer Containing Excess Drug in Suspension", J. Pharm. Sci., Apr. 1971, pp. 541-545
  • Bottari, F. et al., "Influence of Drug Concentration on In Vitro Release of Salicyclic Acid from Ointment Bases", J. Pharm. Sci., Nov. 1974, pp. 1779-1783
  • Higuchi, T., "Physical Chemical Analysis of Percutaneous Absorption Process from Creams and Ointments", J. soc. Cosmetic Chemists, pp. 85-93, Sep. 1959
  • Chandrasekaran, S. K. et al., "Scopolomine Permation Through Human Skin in Vitro", AlChE J., Sep. 1976, pp. 828-83
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