U.S. patents available from 1976 to present.
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Methods and compositions for treating urinary incontinence using optically pure (S)-oxybutynin

Patent 5736577 Issued on April 7, 1998. Estimated Expiration Date: Icon_subject June 28, 2016. 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.

Inventors

Assignee

Application

No. 671976 filed on 06/28/1996

US Classes:

514/617, R contains benzene ring424/449, Transdermal or percutaneous424/451, Capsules (e.g., of gelatin, of chocolate, etc.)424/464, Tablets, lozenges, or pills514/540Nitrogen in Y moiety

Examiners

Primary: Rollins, John W.

Attorney, Agent or Firm

Foreign Patent References

  • 940540 GB. 07/13/1961
  • 92/20377 WO. 05/13/1992

International Classes

A61K 031/165
A61K 009/70
A61K 009/66
A61K 009/46

Abstract

A method for treating urinary incontinence while avoiding concomitant liability of adverse effects associated with racemic oxybutynin is disclosed. The method comprises administering a therapeutically effective amount of (S)-oxybutynin, or a pharmaceutically acceptable salt thereof, substantially free of its R enantiomer. Pharmaceutical compositions comprising (S)-oxybutynin, or a pharmaceutically acceptable salt thereof, substantially free of its R enantiomer, and a pharmaceutically acceptable carrier are also disclosed.

Other References

  • Lish et al. "Oxybutynin--A Musculotropic Antispasmodic Drug . . ." Arch. int. Pharmacodyn. 156, 456-488 (1965)
  • Hock "Clinical Evaluation of Oxybutynin Chloride" Current Therapeutic Research 9, 437-440 (1967)
  • Fredericks et al. "A Study of the Anticholinergic and Antispasmodic Activity of Oxybutynin . . ." Investigative Urology 12, 317-319 (1975)
  • Nilvebrant et al. "Dicyclomine, Benzhexol and Oxybutynine Distinguish . . ." Europ. J. Pharmacol. 123, 133-143 (1986)
  • Tonini et al. "Depressant Action of oxybutynin on the contractility . . ." J. Pharm. Pharmacol. 39, 103-107 (1986)
  • Kachur et al. "R and S Enantiomers of Oxybutynin: Pharmacological Effects . . ." J. Pharm. Exper. Ther. 247, 867-872 (1988)
  • Noronha-Blob et al. "Muscarinic Receptors: Relationships Among Phosphoinositude . . ." J. Pharm Exper. Ther. 249, 843-851 (1989)
  • Noronha-Blob et al. "The Anticholinergic Activity of Agents Indicated for Urinary . . ." J. Pharm. Exper. Ther. 251, 586-593 (1989)
  • Peterson et al. "In Vivo Crystometrogram Studies in Urethane-Anesthetized and Conscious Guinea Pigs" J. Pharm. Methods 21, 231-241 (1989)
  • Guarneri et al. "Effects of Oxybutynin, Terodiline, and Nifedipine . . ." Pharm. Research 24, 263-272 (1991)
  • Noronha-Blob et al. "Enantiomers of Oxybutynin: In Vitro Pharmacological Characterization . . ." J. Pharm. Exp. Ther. 256, 562-567 (1990)
  • Lowe et al. "Effect of extracellular Ca2+ on cholinergic, KCl and phorbol ester-mediated . . ." Eur. J. Pharm. 195, 273-279 (1991)
  • Massad et al. "The Pharmacokinetics of Intravesical and Oral Oxybutynin Chloride" J. Urology 148, 595-597 (1992)
  • Angelico et al. "In Vivo Effects of Different Antispasmodic Drugs on the Rat Bladder Contractions" J. Pharm. Methods 27, 33-39 (1992)
  • Guarneri et al. "Effects of Drugs Used in the Therapy of Detrusor Hyperactivity . . ." Pharm. Research 27, 173-187 (1993)
  • Lindeke et al. "Metabolism of Oxybutynin: establishment of desethyloxybutynin and Oxybutynin N-Oxide formation in Rat Liver Preparations using Deuterium Substitution and Gas Chromatographic Mass Spectrometric Analysis" Biomedical Mass Spectrometry, vol. 8, No. 10, 506-513 (1981)
  • Kasama et al. "Preparation of Substituted Glycolic acid 4-alkyl-amino-2-butynyl Esters as Antispasmodics and for Regulation of Urination" Chemical Abstracts, vol. 113:23118k, 586 (1990
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