US4921695A — Antianginal plate for treating ischemic heart dis…

Claim 1

Independent Claim 374 words

A method for treating ischemic heart disease in a patient subject to anginal pectoris comprising the step of adhering to a chosen site of the mouth mucosa an antianginal film composition in plate form useful for treating ischemic heart diseases in patients subject to anginal pectoris and which is capable of adherence to a selected site of the mouth mucosa for rapid arresting or prevention of anginal pectoris attacks whereby said composition when highly adhered remains fixed and glued to a chosen site of the mouth mucosa and insures immediate, uniform and sustained delivery of an antianginal nitrate, in an amount effective for an average of about 5 hours per plate, directly into the blood circulation system through the mouth mucosa, with the great advantage that it is possible to control and easily discontinue the nitrate uptake by removing the unresolved film in cases where it becomes necessary or, on the contrary, to renew the therapy, said antianginal composition comprising from about 3 to 30 weight percent of an antianginal nitrate in a complex labile bond with from about 70 to 97 weight percent of a mouth mucosa soluble, swellable and resolvable polymeric film-forming carrier, in which solutions of the biologically resolvable soluble polymer carrier and the active substance were mixed, and a film cast and dried until the residual amount of the solvent does not exceed about 10 percent by weight; said film-forming carrier having the ability to: (a) form labile complex bonds with said anti-anginal coronary vasodilating nitrate; (b) remain highly adhered to the mouth mucosa, but can be removed to interrupt or discontinue treatment; and (c) release the active principle of said coronary vasodilator nitrate immediately, and thereafter at such a sustained rate and for a period of time that the pharmacodynamic effects as expressed by the mean data of the repeated individual selected standard physical loads with treadmill in combination with ECG-monitoring (i) are detectable practically instantaneously after affixing to the mouth mucosa, (ii) confirm the presence of a continuous therapeutic concentration of said active principle in the patient's blood during resolution of said carrier, and (iii) confirm a bioavailability of said active principle in an amount substantially greater than that obtained with a sublingual nitroglycerin tablet as the standard.

Claim 2

Independent Claim 374 words

A method for treating ischemic heart disease in a patient subject to anginal pectoris comprising the step of adhering to a chosen site of the mouth mucosa an antianginal film composition in plate form useful for treating ischemic heart diseases in patients subject to anginal pectoris and which is capable of adherence to a selected site of the mouth mucosa for rapid arresting or prevention of anginal pectoris attacks whereby said composition when highly adhered remains fixed and glued to a chosen site of the mouth mucosa and insures immediate, uniform and sustained delivery of an antianginal nitrate, in an amount effective for an average of about 5 hours per plate, directly into the blood circulation system through the mouth mucosa, with the great advantage that it is possible to control and easily discontinue the nitrate uptake by removing the unresolved film in cases where it becomes necessary or, on the contrary, to renew the therapy, said antianginal composition comprising from about 3 to 30 weight percent of an antianginal nitrate in a complex labile bond with from about 70 to 97 weight percent of a mouth mucosa soluble, swellable and resolvable polymeric film-forming carrier, in which solutions of the biologically resolvable soluble polymer carrier and the active substance were mixed, and a film cast and dried until the residual amount of the solvent does not exceed about 10 percent by weight; said film-forming carrier having the ability to: (a) form labile complex bonds with said anti-anginal coronary vasodilating nitrate; (b) remain highly adhered to the mouth mucosa, but can be removed to interrupt or discontinue treatment; and (c) release the active principle of said coronary vasodilator nitrate immediately, and thereafter at such a sustained rate and for a period of time that the pharmacodynamic effects as expressed by the mean data of the repeated individual selected standard physical loads with treadmill in combination with ECG-monitoring (i) are detectable practically instantaneously after affixing to the mouth mucosa, (ii) confirm the presence of a continuous therapeutic concentration of said active principle in the patient's blood during resolution of said carrier, and (iii) confirm a bioavailability of said active principle in an amount substantially greater than that obtained with a sublingual nitroglycerin tablet as the standard.

Claim 3

Dependent Claim 23 words

The method of claim 1 wherein said antianginal nitrate is selected from the group consisting of glycerol trinitrate, pentaerythritol tetranitrate, and isosorbide dinitrate.

Claim 4

Dependent Claim 40 words

The method of claim 1 wherein from about 3 to about 30% by weight of a dispersed solid fat melting at temperatures of from 30° to 50° C. is present based on the total weight of said nitrate and carrier.

Claim 5

Dependent Claim 27 words

The method of claim 3 where said solid fat is selected from the group consisting of cocoa butter, hydrogenized cotton seed oil, glycerol laurate, and glycerol phthalate.

Claim 6

Dependent Claim 65 words

The method of claim 1 wherein said polymer carrier has the ability to form labile complex bonds with said antianginal coronary vasodilating nitrates, said nitrates having been prepared by mixing solvent solutions of said labile complex bond-forming polymer and said antianginal nitrate, removing air from the solution in vacuum at room temperature, casting a film and drying the film at temperatures up to 40° C.

Claim 7

Dependent Claim 17 words

The method of claim 1 wherein said film is from about 0.1 to about 1.5 mm thick.

Claim 8

Independent Claim 391 words

A method for treating ischemic heart disease in a patient subject to anginal pectoris comprising the step of adhering to a chosen site of the mouth mucosa and antianginal film composition in plate form useful for treating ischemic heart diseases in patients subject to anginal pectoris and which is capable of adherence to a selected site of the mouth mucosa for rapid arresting or prevention of anginal pectoris attacks whereby said composition when highly adhered remains fixed and glued to a chosen site of the mouth mucosa and insures immediate, uniform and sustained delivery of an antianginal nitrate directly into the blood circulation system through the mouth mucosa, in an effective sustained amount for an average of about 5 hours per plate, and with the great advantage that it is possible to control and easily discontinue the nitrate uptake by removing the unresolved film in cases where it becomes necessary or, on the contrary, to renew the therapy, said antianginal composition comprising from about 3 to 30 weight percent of an antianginal nitrate in a complex labile bond with from about 70 to 97 weight percent of a mouth mucosa soluble, swellable and resolveable polymer film-forming carrier selected from the group consisting of homopolymers of acrylamide and vinylpyrrolidone and their copolymers with acrylates, in which solutions of the biologically resolvable soluble polymer carrier and the active substance were mixed, and a film cast and dried until the residual amount of the solvent does not exceed about 10 percent by weight; said film-forming carrier having the ability to: (a) form labile complex bonds with said anti-anginal coronary vasodilating nitrate; (b) remain highly adhered to the mouth mucosa, but can be removed to interrupt or discontinue treatment, and (c) release the active principle of said coronary vasodilator nitrate immediately, and thereafter at such a sustained rate and for a period of time that the pharmacodynamic effects as expressed by the mean data of the repeated individual selected standard physical loads with treadmill in combination ECG-monitoring (i) are detectable practically instantaneously after affixing to the mouth mucosa, (ii) confirm the presence of a continuous therapeutic concentration of said active principle in the patient's blood during resolution of said carrier, and (iii) confirm a bioavailability of said active principle in an amount substantially greater than that obtained with a sublingual nitroglycerin tablet as the standard.

Claim 9

Independent Claim 391 words

A method for treating ischemic heart disease in a patient subject to anginal pectoris comprising the step of adhering to a chosen site of the mouth mucosa and antianginal film composition in plate form useful for treating ischemic heart diseases in patients subject to anginal pectoris and which is capable of adherence to a selected site of the mouth mucosa for rapid arresting or prevention of anginal pectoris attacks whereby said composition when highly adhered remains fixed and glued to a chosen site of the mouth mucosa and insures immediate, uniform and sustained delivery of an antianginal nitrate directly into the blood circulation system through the mouth mucosa, in an effective sustained amount for an average of about 5 hours per plate, and with the great advantage that it is possible to control and easily discontinue the nitrate uptake by removing the unresolved film in cases where it becomes necessary or, on the contrary, to renew the therapy, said antianginal composition comprising from about 3 to 30 weight percent of an antianginal nitrate in a complex labile bond with from about 70 to 97 weight percent of a mouth mucosa soluble, swellable and resolveable polymer film-forming carrier selected from the group consisting of homopolymers of acrylamide and vinylpyrrolidone and their copolymers with acrylates, in which solutions of the biologically resolvable soluble polymer carrier and the active substance were mixed, and a film cast and dried until the residual amount of the solvent does not exceed about 10 percent by weight; said film-forming carrier having the ability to: (a) form labile complex bonds with said anti-anginal coronary vasodilating nitrate; (b) remain highly adhered to the mouth mucosa, but can be removed to interrupt or discontinue treatment, and (c) release the active principle of said coronary vasodilator nitrate immediately, and thereafter at such a sustained rate and for a period of time that the pharmacodynamic effects as expressed by the mean data of the repeated individual selected standard physical loads with treadmill in combination ECG-monitoring (i) are detectable practically instantaneously after affixing to the mouth mucosa, (ii) confirm the presence of a continuous therapeutic concentration of said active principle in the patient's blood during resolution of said carrier, and (iii) confirm a bioavailability of said active principle in an amount substantially greater than that obtained with a sublingual nitroglycerin tablet as the standard.

Annuity Stage	Window Opens	Payment Deadline	Surcharge Period Until	Estimated Fee	Status
3.5 Years (Year 4)	1993-04-30	1993-10-30	1994-05-01	$2000.00	Window Closed / Lapsed
7.5 Years (Year 8)	1997-04-30	1997-10-30	1998-05-01	$3760.00	Window Closed / Lapsed
11.5 Years (Year 12)	2001-04-30	2001-10-30	2002-05-01	$7700.00	Window Closed / Lapsed

Antianginal plate for treating ischemic heart disease

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