Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Web – sheet or filament bases; compositions of bandages; or...
Patent
1988-06-07
1990-09-11
Page, Thurman K.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Web, sheet or filament bases; compositions of bandages; or...
424447, A61F 1340
Patent
active
049561812
ABSTRACT:
Method and device for treating angina pectoris and preventing tolerance to nitrate drugs which takes into account the frequent need to provide the patient with relief from or prevention of pre-waking or early morning angina. The treatment comprises administering a daily unit dose of the nitrate before bedtime in a dosage form that (1) provides a washout period of 3 to 12 hours by sufficiently retarding delivery of the nitrate to the patient during the washout period so as to provide a rate of delivery of nitrate from the patch that is so low as to be insufficient to cause tolerance to said nitrate in said patient; (2) at the end of the washout period and at least 30 minutes before the patient expects to awaken, initiates an effective delivery period during which the dosage form provides an initial effective delivery rate sufficient to provide an antianginally effective concentration of nitrate in the blood stream of the patient; and (3) thereafter, during a ramp-up delivery period, delivers the nitrate at an increasing rate until a final delivery rate is achieved, which is from 125% to 1,000% of the initial effective delivery rate. At the end of the ramp-up period, delivery is exhausted or otherwise terminated. A new unit dose is administered at bedtime, and the cycle is repeated. A preferred transdermal patch for carrying out the treatment is provided.
REFERENCES:
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patent: 4725272 (1988-02-01), Gale
patent: 4752478 (1988-06-01), Bondi et al.
Ho-Leung Fung, Ph.D., "Pharmacokinetic Determinants of Nitrate Action," The American Journal of Medicine, 6/22/84, pp. 22-26.
Steven Corwin, MD, James A. Reiffel, MD, "Nitrate Therapy for Angina Pectoris," Arch. Intern. Med., vol. 145, Mar., 1985, pp. 538-543.
Johathan Abrams, MD, "Pharmacology of Nitroglycerine and Long-Acting Nitrates," Am. J. Cardiol., 1985, vol. 56, pp. 12A-18A.
John O. Parker, MD, "Nitrate Tolerance," Am J. Cardiol., 1985, vol. 56, pp. 281-311.
John T. Flaherty, MD, "Hemodynamic Attenuation and the Nitrate-Free Interval: Alternative Dosing Strataegies for Transdermal Nitroglycerine," Am. J. Cardiol, vol. 56, pp. 321-371.
Bayer Gerald W.
Diamantopoulos Paul A.
Osterhoudt Hans W.
Schmit Paul F.
Eastman Kodak
Horne Leon R.
Page Thurman K.
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