Antianginal film and method of treating ischemic heart disease
원문보기
IPC분류정보
국가/구분
United States(US) Patent
등록
국제특허분류(IPC7판)
A61K-031/04
A61K-009/22
출원번호
US-0799210
(1985-11-19)
발명자
/ 주소
Babaian Eduard A. (Moscow SUX) Gerasimova Galina A. (Moscow SUX) Davydov Anatoly B. (Moscow SUX) Utyamyshev Rustam I. (Moscow SUX) Khromov Gennady L. (Moscow SUX) Metelitsa Vladimir I. (Moscow SUX) V
출원인 / 주소
Vsesojuny Kardiologichesky Nauchny Tsentr Adkaemii Meditsinski Nauk SSSR (Moscow SUX 07) Vsesojuzny Nauchno-Issledovatelsky I Ispytateiny Institut Meditsinskoi Tekhniki (Moscow SUX 07)
인용정보
피인용 횟수 :
43인용 특허 :
3
초록▼
The antianginal film is a plate, 0.1 to 1.5 thick, consisting of a biologically soluble and resolvable carrier, which is a hompolymer of acrylamide or vinylpyrrolidone, or a copolymer thereof with acrylate, containing from 99 to 70 percent by weight of acrylamide with vinylpyrrolidone and from 1 to
The antianginal film is a plate, 0.1 to 1.5 thick, consisting of a biologically soluble and resolvable carrier, which is a hompolymer of acrylamide or vinylpyrrolidone, or a copolymer thereof with acrylate, containing from 99 to 70 percent by weight of acrylamide with vinylpyrrolidone and from 1 to 30 percent by weight of acrylate having a molecular mass from 50,000 to 1,000,000, and the active principle having antianginal action, the components being taken in the following proportions, in percent by weight: active substance having antianginal action 3.0-30.0 biologically soluble and resolvable carrier 70.0-97.0 The method of treating ischemic heart disease with the proposed antianginal film by individual doses, consists in that a biologically soluble and resolvable film without any active substance is first applied to a selected site of the mouth mucosa and the time during which this film is fully resolved is determined, this time being characteristic of the period during which the active substance is delivered into the patient\s body. Next a medicinal film containing the active substance in the quantity which should be delivered into the patient\s body during the time of the film resolution is selected. Finally the film containing the required quantity of the antianginal preparation is applied once or several times, to the selected site of the mouth mucosa to ensure continuous and optimal therapeutic effect during the entire period of the full resolution of the proposed film.
대표청구항▼
In the method of treating ischemic heart disease in patients subject to anginal pectoris by placing anti-anginal coronary vasodilating nitrates buccally for rapid arresting of anginal pectoris attacks, the improvement whereby said buccally placed coronary vasodilating nitrates are highly adhered and
In the method of treating ischemic heart disease in patients subject to anginal pectoris by placing anti-anginal coronary vasodilating nitrates buccally for rapid arresting of anginal pectoris attacks, the improvement whereby said buccally placed coronary vasodilating nitrates are highly adhered and remain fixed and glued to a chosen site of the mouth mucosa to insure uniform delivery of said anti-anginal nitrate 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, which comprises placing at a selected site of the mouth mucosa of said patient, an anti-anginal effective amount of said anti-angle nitrate admixed and dissolved in film form with a selected 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 resolvable, polymeric film forming carrier having been evaluated to determine its ability to provide immediate, uniform and substained release of a safe but adequate dose of said anti-anginal nitrate, for a particular patient, by: (i) first applying a film of said soluble and resolvable carrier polymer containing no active anti-anginal ingredient, to a chosen site of the mouth mucosa of the patient in the region of the upper gum above the canine or premolars. (ii) determining the time of full resolution of the film, and (iii) preparing a film containing that dose of the active principle which should be given to the patient during the time required for full resolution of the film, thereby insuring continuous and optimal therapeutic effect during the entire period of dissolution of the film once the film containing the required amount of the anti-anginal preparation is applied to the chosen site of the mouth mucosa of the patient; 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 tha presence of a continous 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.
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