# US 6,294,197 B1 · Solid oral dosage forms of valsartan > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 6,294,197 B1 - Document ID: US6294197B1 - Status: Granted - Kind: B1 - Application number: 09/202,805 - Filed: 1999-05-07 - Granted: 2001-09-25 - Earliest claimed: 1996-06-27 - Assignees: Novartis AG - Inventors: Robert Frank Wagner; Yoshimitsu Katakuse; Takashi Taike; Fujiki Yamato; Manfred Kohlmeyer - Web page: https://patentgrep.com/patent/US6294197B1 ## CPC - A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca - A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates} - A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 31/41: having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole - A61K 31/54: having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame - A61P 3/10: for hyperglycaemia, e.g. antidiabetics - A61P 9/00: Drugs for disorders of the cardiovascular system - A61P 9/04: Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure - A61P 9/10: for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis - A61P 9/12: Antihypertensives - A61P 9/14: Vasoprotectives; Antihaemorrhoidals; Drugs for varicose therapy; Capillary stabilisers - A61P 13/12: of the kidneys - A61P 21/00: Drugs for disorders of the muscular or neuromuscular system - A61P 25/04: Centrally acting analgesics, e.g. opioids - A61P 25/28: for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia - A61P 43/00: Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00 - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS ## Abstract The present invention is concerned with solid dosage forms comprising a) valsartan and optionally HCTZ, and b) pharmaceutically acceptable additives suitable for the preparation of solid oral dosage forms by compression methods. ## Claims ### Claim 1 A compressed solid dosage form comprising a) an active agent containing an effective amount of valsartan or a pharmaceutically acceptable salt thereof; and, b) at least one pharmaceutically acceptable additive wherein the active agent is present in an amount of more than 35% by weight based on the total weight of the compressed solid dosage form. ### Claim 2 (depends on 1) A solid oral dosage form according to claim 1 wherein the active agent is present in an amount of more than 50% by weight. ### Claim 3 (depends on 1) A compressed solid dosage form according to claim 1 wherein the active agent is present in an amount ranging from 57 to 62% by weight. ### Claim 4 (depends on 1) A compressed solid dosage form according to claim 1 wherein the active agent consists entirely of valsartan or a pharmaceutically acceptable salt thereof in a dosage of from between about 10 and 250 mg. ### Claim 5 (depends on 1) A compressed solid dosage from according to claim 1 wherein the dosage range is from 40 to 160 mg. ### Claim 6 (depends on 1) A compressed solid dosage from according to claim 1 wherein the dosage is 40 mg, 80 mg or 160 mg. ### Claim 7 (depends on 1) A compressed solid dosage form according to claim 1 wherein the active agent consists of an effective amount of valsartan or a pharmaceutically acceptable salt thereof and an effective amount of hydrochlorothiazide (HCTZ). ### Claim 8 A compressed solid dosage form which comprises an effective amount of valsartan or a pharmaceutically acceptable salt thereof; an effective amount of HCTZ; and, at least one pharmaceutically acceptable additive. ### Claim 9 (depends on 8) A compressed solid dosage form according to claim 8 comprising a unit dose of about 10 to 250 mg of valsartan or a pharmaceutically acceptable salt thereof and a unit dose of about 6 to 60 mg HCTZ. ### Claim 10 (depends on 8) A compressed solid dosage form according to claim 8 comprising a unit dose of about 50 to 100 mg of valsartan or a pharmaceutically acceptable salt thereof and a unit dose of about 10 to 30 mg of HCTZ. ### Claim 11 (depends on 8) A compressed solid dosage form according to claim 8 comprising a unit dose of about 80 to 160 mg of valsartan or a pharmaceutically acceptable salt thereof and a unit dose of about 12.5 mg or 25 mg of HCTZ. ### Claim 12 (depends on 8) A compressed solid dosage form according to claim 8 which comprises microcrystalline cellulose as a pharmaceutically acceptable additive. ### Claim 13 (depends on 8) A compressed solid dosage form according to claim 8 which comprises crosslinked polyvinylpyrrolidone (PVP) as a pharmaceutically acceptable additive. ### Claim 14 (depends on 12) A compressed solid dosage from according to claim 12 wherein the microcrystalline cellulose is present in an amount of from 15 to 25% by weight. ### Claim 15 (depends on 13) A compressed solid dosage form according to claim 13 wherein the crosslinked PVP is present in an amount of from 10 to 30% by weight. ### Claim 16 (depends on 8) A compressed solid dosage form according to claim 8 in the form of a tablet. ### Claim 17 (depends on 8) A compressed solid dosage form according to claim 8 in the form of a dragee. ### Claim 18 A process of forming a compressed solid dosage form containing more than 35% by weight of valsartan or a pharmaceutically acceptable salt thereof and at least one pharmaceutically acceptable additive wherein the process comprises the steps of: i) blending the valsartan and at least one pharmaceutically acceptable additive to form a mixture; ii) subjecting the mixture to compression to form a coprimate; iii) converting the coprimate into a granulate; and, iv) compressing the granulate to form the compressed solid dosage form. ### Claim 19 (depends on 18) A process according to claim 18 wherein the compression step ii) is carried out using roller compaction or slugging techniques. ### Claim 20 (depends on 18) A process according to claim 18 wherein step iii) is carried out by screening or milling the coprimate. ### Claim 21 (depends on 18) A process according to claim 18 wherein the granulate is compressed without first being sized. ### Claim 22 (depends on 18) A process according to claim 18 wherein the granulate is formed under a pressure of from about 25 to about 65 kN. ### Claim 23 (depends on 19) Coprimates obtained by roller compaction or slugging according to claim 19. ### Claim 24 (depends on 18) Granulate obtained according to the process according to claim 18. ### Claim 25 (depends on 18) A compressed solid dosage form produced according to the process as defined in claim 18. ### Claim 26 (depends on 1) A method of treating hypertension, congestive heart failure, angina, myocardial infarction, arteriosclerosis, diabetic nephropathy, diabetic cardiac myopathy, renal insufficiency, peripheral vascular disease, left ventricular hypertrophy, cognitive dysfunction, headache, or chronic heart failure, wherein the method comprises administering a solid oral dosage form as defined in claim 1 to a host in need of said treatment. ### Claim 27 (depends on 1) A compressed solid dosage form according to claim 1 in the form of a tablet. ### Claim 28 (depends on 1) A compressed solid dosage form according to claim 1 in the form of a dragee. ### Claim 29 A process of forming a compressed solid dosage from containing more than 35% by weight of valsartan or a pharmaceutically acceptable salt thereof, an effective amount of HCTZ and at least one pharmaceutically acceptable additive wherein the process comprises the steps of: i) blending the valsartan, HCTZ and at least one pharmaceutically acceptable additive to form a mixture; ii) subjecting the mixture to compression to form a coprimate; iii) converting the coprimate into a granulate; and, iv) compressing the granulate to form the compressed solid dosage form. ### Claim 30 (depends on 29) A process according to claim 29 wherein the compression step ii) is carried out using roller compaction or slugging techniques. ### Claim 31 (depends on 29) A process according to claim 29 wherein step iii) is carried out by screening or milling the coprimate. ### Claim 32 (depends on 29) A process according to claim 29 wherein the granulate is compressed without first being sized. ### Claim 33 (depends on 29) A process according to claim 29 wherein the granulate is formed under a pressure of from about 25 to about 65 kN. ### Claim 34 (depends on 30) Coprimates obtained by roller compaction or slugging according to claim 30. ### Claim 35 (depends on 29) Granulate obtained according to the process according to claim 29. ### Claim 36 (depends on 29) A compressed solid dosage form produced according to the process as defined in claim 29. ### Claim 37 (depends on 8) A method of treating hypertension, congestive heart failure, angina, myocardial infarction, arteriosclerosis, diabetic nephropathy, diabetic cardiac myopathy, renal insufficiency, peripheral vascular disease, stroke, left ventricular hypertrophy, cognitive dysfunction, headache, or chronic heart failure, wherein the method comprises administering a compressed solid dosage form as defined in claim 8 to a host in need of such treatment. ### Claim 38 (depends on 1) A compressed solid dosage form according to claim 1 wherein the dimension ratio of the dosage forms length:width:height is 2.5-5.0:0.9-2.0:1.0. ### Claim 39 (depends on 1) A compressed solid dosage form according to claim 1 wherein the dosage form has a length of approximately 10 to 11 mm, a width of approximately 5.0-6.0 mm and a height of approximately 3.0-4.0 mm. ### Claim 40 (depends on 1) A compressed solid dosage form according to claim 1 wherein the dosage form has a length of approximately 15.0-16.0 mm, a width of approximately 6.0-7.0 mm and a height of approximately 3.5 to 5.0 mm. ### Claim 41 (depends on 1) A compressed solid dosage form according to claim 1 wherein the dosage form has a diameter of about 8 to 8.5 mm and a depth of about 3 to 3.5 mm. ### Claim 42 (depends on 1) A compressed solid dosage form according to claim 1 wherein the dosage form has a diameter of about 16 mm and a depth of about 6 mm. ### Claim 43 (depends on 8) A compressed solid dosage form according to claim 8 wherein the dimension ratio of the dosage forms length:width:height is 2.5-5.0:0.9-2.0:1.0. ### Claim 44 (depends on 8) A compressed solid dosage form according to claim 8 wherein the dosage form has a length of approximately 10 to 11 mm, a width of approximately 5.0-6.0 mm and a height of approximately 3.0-4.0 mm. ### Claim 45 (depends on 8) A compressed solid dosage form according to claim 8 wherein the dosage form has a length of approximately 15.0-16.0 mm, a width of approximately 6.0-7.0 mm and a height of approximately 3.5 to 5.0 mm. ### Claim 46 (depends on 8) A compressed solid dosage form according to claim 8 wherein the dosage form has a diameter of about 8 to 8.5 mm and a depth of about 3 to 3.5 mm. ### Claim 47 (depends on 8) A compressed solid dosage form according to claim 8 wherein the dosage form has a diameter of about 16 mm and a depth of about 6 mm. ### Claim 48 (depends on 18) The process according to claim 18 wherein the blending step includes grinding. ### Claim 49 (depends on 29) The process according to claim 29 wherein the blending step includes grinding. ### Claim 50 (depends on 18) The process of claim 18 wherein the coprimate is formed by compression in the absence of water. ### Claim 51 (depends on 29) The process of claim 29 wherein the coprimate is formed by compression in the absence of water. ### Claim 52 (depends on 26) A method of treating according to claim 26 wherein the compressed solid dosage form is orally administered to the host. ### Claim 53 (depends on 37) A method of treating according to claim 37 wherein the compressed solid dosage form is orally administered to the host.