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US Patent 5942543 - Topical anesthetic comprising lidocaine, adrenaline, and tetracaine, and its method of use

US Patent Issued on August 24, 1999
Estimated Patent Expiration Date: Icon_subject December 16, 2016Estimated 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.
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Abstract

A topical anesthetic includes about 1-10% by weight lidocaine hydrochloride, about 0.01-0.10% by weight adrenaline, and about 0.25-4% by weight tetracaine hydrochloride, preferably in an aqueous base with about 2% benzyl alcohol or in a gel including about 3% hydroxyethyl cellulose. The topical anesthetic has been found to be at least as effective as TAC (tetracaine hydrochloride, adrenaline, cocaine), but with fewer harmful side effects and at a greatly reduced cost (about 1/10 of the cost of TAC).

Other References

  • Adriani et al., "Fatalities following topical application of local anesthetics to mucous membranes", JAMA 1956; 162 (17): 1527-1530
  • Campbell et al., "Absorption of local anethetics", JAMA 1958; 168(7): 873-877
  • Adriani, "The clinical pharmacology of local anesthetics" Clinical Pharmacology and Therapeutics, vol. I, No. 5, 645-673 (1960)
  • Adriani et al., "Clinical effectiveness of drugs used for topical anesthesia",. JAMA 1964; 188(8): 711-716
  • DiFazio, "Local anesthetics: Action, metabolism and toxicity", Otolaryngologic Clinics of North America, 1981; 14(3): 515-519
  • Mofenson et al., "Lidocaine toxicity from topical mucosal application", Clinical Pediatrics, Mar. 1983; 22(3): 190-192
  • Beyer et al., "Systemic Toxicity from Tetracaine Pharyngeal Anesthesia", Digestive Diseases and Sciences, vol. 35, No. 2 (Feb. 1990), p. 280
  • Wase et al., "XAP--an Alternative to Cocaine for Topical Anesthesia", Annals of Emergency Medicine, 22:11 (Nov. 1993), pp. 1776-1777
  • Schilling, C.G. et al., "Tetracaine, Epinephrine, Cocaine (TAC) vs Lidocaine, Epinephrine, Tetracaine (LET) for Anesthesia of Lacerations in Children", American Journal of Diseases of Children, (Apr. 1993), p. 427, No. 48
  • Schilling, C.G. et al., "Tetracaine, Epinephrine, Cocaine (TAC) vs Lidocaine, Epinephrine, Tetracaine (LET) for Anesthesia of Lacerations in Children", Annals of Emergency Medicine, (Feb. 1995), p. 203
  • Ernst, Amy A. et al., "Lidocaine Adrenaline Tetracaine Gel Versus Tetracaine Adrenaline Cocaine Gel for Topical Anesthesia in Linear Scalp and Facial Lacerations in childres Aged 5 to 17 Years", Pediatrics, (Feb. 1995), pp. 255-258
  • Ernst, Amy A. et al., "LAT (Lidocaine-Adrenaline-Tetracaine) Versus TAC (Tetracaine-Adrenaline-Cocaine) for Topical Anesthesia in Face and Scalp Lacerations", American Journal of Emergency Medicine, (Mar. 1995) pp. 151-15

Inventor

Application

No. 766994 filed on 12/16/1996

US Classes:

514/537, With an additional active ingredient514/535, The nitrogen of the Z radical is directly bonded to a benzene ring which is directly bonded to the C(=O) group514/536, With an agent to enhance topical absorption or with a stabilizing agent514/626, Nitrogen in R514/817ANESTHETIC, TOPICAL

Field of Search

514/537, With an additional active ingredient514/536, With an agent to enhance topical absorption or with a stabilizing agent514/535, The nitrogen of the Z radical is directly bonded to a benzene ring which is directly bonded to the C(=O) group514/626, Nitrogen in R514/817ANESTHETIC, TOPICAL

Examiners

Primary: Burn, Brian M.

Attorney, Agent or Firm

US Patent References

3868445, 3898339, 3957996, Pharmaceutical local anesthetic compositions
Issued on: 05/18/1976
Inventor: Adams ,   et al.
4006218, Potentiated medicaments
Issued on: 02/01/1977
Inventor: Sipos
4029794, Pharmaceutical local anesthetic composition
Issued on: 06/14/1977
Inventor: Adams ,   et al.
4057582, Aminotetralins and use in inducing anesthesia
Issued on: 11/08/1977
Inventor: Dunnigan ,   et al.
4105760, Local anaesthetic salts of chondroitinsulfate compounds
Issued on: 08/08/1978
Inventor: Szejtli ,   et al.
4200098, Osmotic system with distribution zone for dispensing beneficial agent
Issued on: 04/29/1980
Inventor: Ayer ,   et al.
4285987, Process for manufacturing device with dispersion zone
Issued on: 08/25/1981
Inventor: Ayer ,   et al.
4320759, Dispenser with diffuser
Issued on: 03/23/1982
Inventor: Theeuwes
4474751, Ophthalmic drug delivery system utilizing thermosetting gels
Issued on: 10/02/1984
Inventor: Haslam ,   et al.
4562060, Local anesthetic mixture for topical application, process for its preparation, as well as method for obtaining local anesthesia
Issued on: 12/31/1985
Inventor: Broberg ,   et al.
4668506, Sustained-release formulation containing and amino acid polymer
Issued on: 05/26/1987
Inventor: Bawa
4861760, Ophthalmological composition of the type which undergoes liquid-gel phase transition
Issued on: 08/29/1989
Inventor: Mazuel ,   et al.
4945084, Method and composition for topically treating anorectal or other dermal wounds
Issued on: 07/31/1990
Inventor: Packman
4966773, Topical ophthalmic compositions containing microfine retinoid particles
Issued on: 10/30/1990
Inventor: Gressel, et al.
5077033, Ophthalmic drug delivery with thermo-irreversible gels of polxoxyalkylene polymer and ionic polysaccharide
Issued on: 12/31/1991
Inventor: Viegas, et al.
5147294, Therapeutic method for reducing chronic pain in a living subject
Issued on: 09/15/1992
Inventor: Smith, et al.
5149320, Composite anesthetic article and method of use
Issued on: 09/22/1992
Inventor: Dhaliwal, et al.
5196405, Compositions and methods of treating hemorrhoids and wounds
Issued on: 03/23/1993
Inventor: Packman
5234957, Compositions and methods for topical administration of pharmaceutically active agents
Issued on: 08/10/1993
Inventor: Mantelle
5252318, Reversible gelation compositions and methods of use
Issued on: 10/12/1993
Inventor: Joshi, et al.
5261903, Composite anesthetic article and method of use
Issued on: 11/16/1993
Inventor: Dhaliwal, et al.
5563153, Sterile topical anesthetic gel
Issued on: 10/08/1996
Inventor: Mueller, et al.
5635540Stabilized topical pharmaceutical preparations
Issued on: 06/03/1997
Inventor: Edlich, et al.

International Class

A61K 031/24

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