AR080683A1 - PHARMACEUTICAL COMPOSITIONS OF ALISKIREN AND METHODS OF ADMINISTRATION - Google Patents
PHARMACEUTICAL COMPOSITIONS OF ALISKIREN AND METHODS OF ADMINISTRATIONInfo
- Publication number
- AR080683A1 AR080683A1 ARP110100850A ARP110100850A AR080683A1 AR 080683 A1 AR080683 A1 AR 080683A1 AR P110100850 A ARP110100850 A AR P110100850A AR P110100850 A ARP110100850 A AR P110100850A AR 080683 A1 AR080683 A1 AR 080683A1
- Authority
- AR
- Argentina
- Prior art keywords
- pharmaceutical composition
- weight
- amount
- sodium
- composition
- Prior art date
Links
- 239000008194 pharmaceutical composition Substances 0.000 title abstract 21
- UXOWGYHJODZGMF-QORCZRPOSA-N Aliskiren Chemical group COCCCOC1=CC(C[C@@H](C[C@H](N)[C@@H](O)C[C@@H](C(C)C)C(=O)NCC(C)(C)C(N)=O)C(C)C)=CC=C1OC UXOWGYHJODZGMF-QORCZRPOSA-N 0.000 title abstract 7
- 229960004601 aliskiren Drugs 0.000 title abstract 7
- 238000000034 method Methods 0.000 title abstract 4
- -1 medium chain fatty acid salt Chemical class 0.000 abstract 11
- 239000000203 mixture Substances 0.000 abstract 8
- 239000007787 solid Substances 0.000 abstract 7
- 150000003839 salts Chemical class 0.000 abstract 6
- 239000003814 drug Substances 0.000 abstract 5
- 229940124597 therapeutic agent Drugs 0.000 abstract 5
- 229920002125 Sokalan® Polymers 0.000 abstract 4
- 230000002209 hydrophobic effect Effects 0.000 abstract 4
- NIXOWILDQLNWCW-UHFFFAOYSA-N Acrylic acid Chemical compound OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 abstract 3
- 239000004372 Polyvinyl alcohol Substances 0.000 abstract 3
- 206010012601 diabetes mellitus Diseases 0.000 abstract 3
- 229920000642 polymer Polymers 0.000 abstract 3
- 229920002451 polyvinyl alcohol Polymers 0.000 abstract 3
- 239000003381 stabilizer Substances 0.000 abstract 3
- 239000004094 surface-active agent Substances 0.000 abstract 3
- 239000000725 suspension Substances 0.000 abstract 3
- ULQISTXYYBZJSJ-UHFFFAOYSA-N 12-hydroxyoctadecanoic acid Chemical compound CCCCCCC(O)CCCCCCCCCCC(O)=O ULQISTXYYBZJSJ-UHFFFAOYSA-N 0.000 abstract 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 abstract 2
- 102000015427 Angiotensins Human genes 0.000 abstract 2
- 108010064733 Angiotensins Proteins 0.000 abstract 2
- RTZKZFJDLAIYFH-UHFFFAOYSA-N Diethyl ether Chemical compound CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 abstract 2
- 206010020772 Hypertension Diseases 0.000 abstract 2
- TWRXJAOTZQYOKJ-UHFFFAOYSA-L Magnesium chloride Chemical compound [Mg+2].[Cl-].[Cl-] TWRXJAOTZQYOKJ-UHFFFAOYSA-L 0.000 abstract 2
- 108090000028 Neprilysin Proteins 0.000 abstract 2
- 102000003729 Neprilysin Human genes 0.000 abstract 2
- 229920003171 Poly (ethylene oxide) Polymers 0.000 abstract 2
- 239000007864 aqueous solution Substances 0.000 abstract 2
- 229960001631 carbomer Drugs 0.000 abstract 2
- 235000014113 dietary fatty acids Nutrition 0.000 abstract 2
- 239000000194 fatty acid Substances 0.000 abstract 2
- 229930195729 fatty acid Natural products 0.000 abstract 2
- 125000003976 glyceryl group Chemical group [H]C([*])([H])C(O[H])([H])C(O[H])([H])[H] 0.000 abstract 2
- 239000003112 inhibitor Substances 0.000 abstract 2
- 229910052751 metal Inorganic materials 0.000 abstract 2
- 239000002184 metal Substances 0.000 abstract 2
- 229920000036 polyvinylpyrrolidone Polymers 0.000 abstract 2
- 239000001267 polyvinylpyrrolidone Substances 0.000 abstract 2
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 abstract 2
- 239000000843 powder Substances 0.000 abstract 2
- JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical compound OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 abstract 1
- WCDDVEOXEIYWFB-VXORFPGASA-N (2s,3s,4r,5r,6r)-3-[(2s,3r,5s,6r)-3-acetamido-5-hydroxy-6-(hydroxymethyl)oxan-2-yl]oxy-4,5,6-trihydroxyoxane-2-carboxylic acid Chemical class CC(=O)N[C@@H]1C[C@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](C(O)=O)O[C@@H](O)[C@H](O)[C@H]1O WCDDVEOXEIYWFB-VXORFPGASA-N 0.000 abstract 1
- LDVVTQMJQSCDMK-UHFFFAOYSA-N 1,3-dihydroxypropan-2-yl formate Chemical group OCC(CO)OC=O LDVVTQMJQSCDMK-UHFFFAOYSA-N 0.000 abstract 1
- IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical group CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 abstract 1
- 229940114072 12-hydroxystearic acid Drugs 0.000 abstract 1
- JVKUCNQGESRUCL-UHFFFAOYSA-N 2-Hydroxyethyl 12-hydroxyoctadecanoate Chemical compound CCCCCCC(O)CCCCCCCCCCC(=O)OCCO JVKUCNQGESRUCL-UHFFFAOYSA-N 0.000 abstract 1
- FHVDTGUDJYJELY-UHFFFAOYSA-N 6-{[2-carboxy-4,5-dihydroxy-6-(phosphanyloxy)oxan-3-yl]oxy}-4,5-dihydroxy-3-phosphanyloxane-2-carboxylic acid Chemical class O1C(C(O)=O)C(P)C(O)C(O)C1OC1C(C(O)=O)OC(OP)C(O)C1O FHVDTGUDJYJELY-UHFFFAOYSA-N 0.000 abstract 1
- 206010001580 Albuminuria Diseases 0.000 abstract 1
- 229940123338 Aldosterone synthase inhibitor Drugs 0.000 abstract 1
- QGZKDVFQNNGYKY-UHFFFAOYSA-O Ammonium Chemical compound [NH4+] QGZKDVFQNNGYKY-UHFFFAOYSA-O 0.000 abstract 1
- 206010002383 Angina Pectoris Diseases 0.000 abstract 1
- 206010003210 Arteriosclerosis Diseases 0.000 abstract 1
- 229940127291 Calcium channel antagonist Drugs 0.000 abstract 1
- 206010007558 Cardiac failure chronic Diseases 0.000 abstract 1
- 206010007559 Cardiac failure congestive Diseases 0.000 abstract 1
- 229920002307 Dextran Polymers 0.000 abstract 1
- 102000002045 Endothelin Human genes 0.000 abstract 1
- 108050009340 Endothelin Proteins 0.000 abstract 1
- 108090000790 Enzymes Proteins 0.000 abstract 1
- 102000004190 Enzymes Human genes 0.000 abstract 1
- 206010019233 Headaches Diseases 0.000 abstract 1
- 206010019280 Heart failures Diseases 0.000 abstract 1
- 208000007177 Left Ventricular Hypertrophy Diseases 0.000 abstract 1
- WHXSMMKQMYFTQS-UHFFFAOYSA-N Lithium Chemical compound [Li] WHXSMMKQMYFTQS-UHFFFAOYSA-N 0.000 abstract 1
- 208000021642 Muscular disease Diseases 0.000 abstract 1
- 201000009623 Myopathy Diseases 0.000 abstract 1
- 108090000854 Oxidoreductases Proteins 0.000 abstract 1
- 208000018262 Peripheral vascular disease Diseases 0.000 abstract 1
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 abstract 1
- 239000002202 Polyethylene glycol Substances 0.000 abstract 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 abstract 1
- 208000001647 Renal Insufficiency Diseases 0.000 abstract 1
- 229920001304 Solutol HS 15 Polymers 0.000 abstract 1
- 208000006011 Stroke Diseases 0.000 abstract 1
- 239000002170 aldosterone antagonist Substances 0.000 abstract 1
- 229940083712 aldosterone antagonist Drugs 0.000 abstract 1
- 150000001413 amino acids Chemical group 0.000 abstract 1
- 239000002333 angiotensin II receptor antagonist Substances 0.000 abstract 1
- 239000005557 antagonist Substances 0.000 abstract 1
- 208000011775 arteriosclerosis disease Diseases 0.000 abstract 1
- 239000003833 bile salt Substances 0.000 abstract 1
- 239000011575 calcium Substances 0.000 abstract 1
- 239000000480 calcium channel blocker Substances 0.000 abstract 1
- 239000002775 capsule Substances 0.000 abstract 1
- 230000000747 cardiac effect Effects 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 239000003599 detergent Substances 0.000 abstract 1
- 239000002934 diuretic Substances 0.000 abstract 1
- 229940030606 diuretics Drugs 0.000 abstract 1
- 238000001035 drying Methods 0.000 abstract 1
- 230000009977 dual effect Effects 0.000 abstract 1
- ZUBDGKVDJUIMQQ-UBFCDGJISA-N endothelin-1 Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CC(O)=O)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(O)=O)NC(=O)[C@H]1NC(=O)[C@H](CC=2C=CC=CC=2)NC(=O)[C@@H](CC=2C=CC(O)=CC=2)NC(=O)[C@H](C(C)C)NC(=O)[C@H]2CSSC[C@@H](C(N[C@H](CO)C(=O)N[C@@H](CO)C(=O)N[C@H](CC(C)C)C(=O)N[C@@H](CCSC)C(=O)N[C@H](CC(O)=O)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H](CCC(O)=O)C(=O)N2)=O)NC(=O)[C@@H](CO)NC(=O)[C@H](N)CSSC1)C1=CNC=N1 ZUBDGKVDJUIMQQ-UBFCDGJISA-N 0.000 abstract 1
- 239000002532 enzyme inhibitor Substances 0.000 abstract 1
- 150000002148 esters Chemical class 0.000 abstract 1
- 150000002191 fatty alcohols Chemical class 0.000 abstract 1
- 229930182470 glycoside Natural products 0.000 abstract 1
- 231100000869 headache Toxicity 0.000 abstract 1
- 229940014041 hyaluronate Drugs 0.000 abstract 1
- FZWBNHMXJMCXLU-BLAUPYHCSA-N isomaltotriose Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1OC[C@@H]1[C@@H](O)[C@H](O)[C@@H](O)[C@@H](OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C=O)O1 FZWBNHMXJMCXLU-BLAUPYHCSA-N 0.000 abstract 1
- 208000017169 kidney disease Diseases 0.000 abstract 1
- 201000006370 kidney failure Diseases 0.000 abstract 1
- 235000010445 lecithin Nutrition 0.000 abstract 1
- 229940067606 lecithin Drugs 0.000 abstract 1
- 239000000787 lecithin Substances 0.000 abstract 1
- 229910052744 lithium Inorganic materials 0.000 abstract 1
- UEGPKNKPLBYCNK-UHFFFAOYSA-L magnesium acetate Chemical compound [Mg+2].CC([O-])=O.CC([O-])=O UEGPKNKPLBYCNK-UHFFFAOYSA-L 0.000 abstract 1
- 229910001629 magnesium chloride Inorganic materials 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 150000004667 medium chain fatty acids Chemical class 0.000 abstract 1
- 208000010125 myocardial infarction Diseases 0.000 abstract 1
- 125000001421 myristyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 abstract 1
- 229960000502 poloxamer Drugs 0.000 abstract 1
- 229920001983 poloxamer Polymers 0.000 abstract 1
- 239000004584 polyacrylic acid Chemical class 0.000 abstract 1
- 239000008389 polyethoxylated castor oil Substances 0.000 abstract 1
- 229920001223 polyethylene glycol Polymers 0.000 abstract 1
- 229910052700 potassium Inorganic materials 0.000 abstract 1
- 239000011591 potassium Substances 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- BTURAGWYSMTVOW-UHFFFAOYSA-M sodium dodecanoate Chemical compound [Na+].CCCCCCCCCCCC([O-])=O BTURAGWYSMTVOW-UHFFFAOYSA-M 0.000 abstract 1
- UDWXLZLRRVQONG-UHFFFAOYSA-M sodium hexanoate Chemical group [Na+].CCCCCC([O-])=O UDWXLZLRRVQONG-UHFFFAOYSA-M 0.000 abstract 1
- BYKRNSHANADUFY-UHFFFAOYSA-M sodium octanoate Chemical compound [Na+].CCCCCCCC([O-])=O BYKRNSHANADUFY-UHFFFAOYSA-M 0.000 abstract 1
- JAJWGJBVLPIOOH-IZYKLYLVSA-M sodium taurocholate Chemical compound [Na+].C([C@H]1C[C@H]2O)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(=O)NCCS([O-])(=O)=O)C)[C@@]2(C)[C@@H](O)C1 JAJWGJBVLPIOOH-IZYKLYLVSA-M 0.000 abstract 1
- FIWQZURFGYXCEO-UHFFFAOYSA-M sodium;decanoate Chemical compound [Na+].CCCCCCCCCC([O-])=O FIWQZURFGYXCEO-UHFFFAOYSA-M 0.000 abstract 1
- NMTDPTPUELYEPL-UHFFFAOYSA-M sodium;heptanoate Chemical compound [Na+].CCCCCCC([O-])=O NMTDPTPUELYEPL-UHFFFAOYSA-M 0.000 abstract 1
- LTOCMXUTASYUOC-UHFFFAOYSA-M sodium;nonanoate Chemical compound [Na+].CCCCCCCCC([O-])=O LTOCMXUTASYUOC-UHFFFAOYSA-M 0.000 abstract 1
- JUQGWKYSEXPRGL-UHFFFAOYSA-M sodium;tetradecanoate Chemical compound [Na+].CCCCCCCCCCCCCC([O-])=O JUQGWKYSEXPRGL-UHFFFAOYSA-M 0.000 abstract 1
- JZVZOOVZQIIUGY-UHFFFAOYSA-M sodium;tridecanoate Chemical compound [Na+].CCCCCCCCCCCCC([O-])=O JZVZOOVZQIIUGY-UHFFFAOYSA-M 0.000 abstract 1
- ZOOPHYLANWVUDY-UHFFFAOYSA-M sodium;undecanoate Chemical compound [Na+].CCCCCCCCCCC([O-])=O ZOOPHYLANWVUDY-UHFFFAOYSA-M 0.000 abstract 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/30—Macromolecular organic or inorganic compounds, e.g. inorganic polyphosphates
- A61K47/32—Macromolecular compounds obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. carbomers, poly(meth)acrylates, or polyvinyl pyrrolidone
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/16—Amides, e.g. hydroxamic acids
- A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/12—Carboxylic acids; Salts or anhydrides thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/16—Agglomerates; Granulates; Microbeadlets ; Microspheres; Pellets; Solid products obtained by spray drying, spray freeze drying, spray congealing,(multiple) emulsion solvent evaporation or extraction
- A61K9/1605—Excipients; Inactive ingredients
- A61K9/1617—Organic compounds, e.g. phospholipids, fats
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/14—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles
- A61K9/19—Particulate form, e.g. powders, Processes for size reducing of pure drugs or the resulting products, Pure drug nanoparticles lyophilised, i.e. freeze-dried, solutions or dispersions
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P13/00—Drugs for disorders of the urinary system
- A61P13/02—Drugs for disorders of the urinary system of urine or of the urinary tract, e.g. urine acidifiers
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
- A61P9/12—Antihypertensives
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Engineering & Computer Science (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Oil, Petroleum & Natural Gas (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Inorganic Chemistry (AREA)
- Biophysics (AREA)
- Molecular Biology (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
Reivindicacion 1: Una composicion farmacéutica que comprende una suspension que comprende una mezcla de un medio hidrofobo y una forma solida, donde la forma solida comprende una cantidad terapéuticamente eficaz de aliskirén, y opcionalmente, un segundo agente terapéutico, y en forma opcional, un tercer agente terapéutico, y por lo menos una sal de un ácido graso de cadena media. Reivindicacion 8: La composicion farmacéutica de la reivindicacion 7, donde la sal de ácido graso de cadena media es hexanoato sodico, heptanoato sodico, octanoato sodico, nonanoato sodico, decanoato sodico, undecanoato sodico, dodecanoato sodico, tridecanoato sodico o tetradecanoato sodico, o una correspondiente sal de potasio, litio o amonio, o una de sus combinaciones. Reivindicacion 10: La composicion farmacéutica de cualquiera de las reivindicaciones 1-9, donde la sal de ácido graso de cadena media se presenta en la composicion en una cantidad del 11% al 40% en peso, preferentemente, 12% a 18% en peso, con mayor preferencia, de alrededor del 15% en peso. Reivindicacion 11: La composicion farmacéutica de cualquiera de las reivindicaciones 1-10, donde la sal de ácido graso de cadena media se presenta en la forma solida en una cantidad de 50% a 90% en peso, preferentemente, en una cantidad de 70% a 80% en peso. Reivindicacion 12: La composicion farmacéutica de cualquiera de las reivindicaciones 1-11, donde el polímero formador de matriz se presenta en la composicion en una cantidad de alrededor del 0,5% al 15% en peso, preferentemente, de alrededor del 1% al 10% en peso. Reivindicacion 13: La composicion farmacéutica de cualquiera de las reivindicaciones 1-12, donde el polímero formador de matriz se selecciona del grupo que consiste en polivinilpirrolidona, carbomero (por ejemplo, polimero Carbopol), alcohol polivinílico, dextrano, sal de alginato, sal de hialuronato y sal de ácido poliacrílico, o una de sus combinaciones. Reivindicacion 15: La composicion farmacéutica de la reivindicacion 14, donde la polivinilpirrolidona es, preferentemente, PVP-12, y, preferentemente, tiene un peso molecular de alrededor de 3000, y se presenta en la composicion en una cantidad de alrededor de 2% a alrededor de 20% en peso, preferentemente, en una cantidad de alrededor de 5% a alrededor de 15% en peso, con mayor preferencia, en una cantidad de alrededor de 10% en peso. Reivindicacion 16: La composicion farmacéutica de la reivindicacion 14, donde el carbomero es, preferentemente, Carbopol 934P, y se presenta en la composicion en una cantidad de alrededor de 0,1% a alrededor de 6% en peso, preferentemente, en una cantidad de alrededor de 0,5% a alrededor de 4% en peso, con mayor preferencia, en una cantidad de alrededor de 1% en peso. Reivindicacion 17: La composicion farmacéutica de la reivindicacion 14, donde el alcohol polivinílico es, preferentemente, alcohol polivinílico de un peso molecular de alrededor de 27.000 Da, y se presenta en la composicion en una cantidad de 4% en peso, con mayor preferencia, en una cantidad de alrededor de 1-2% en peso. Reivindicacion 20: La composicion farmacéutica de cualquiera de las reivindicaciones 1-19, que comprende, además, un surfactante. Reivindicacion 22: La composicion farmacéutica de la reivindicacion 20, donde el surfactante es lecitina o una sal biliar (por ejemplo, taurocolato sodico), o un detergente, o una de sus combinaciones. Reivindicacion 23: La composicion farmacéutica de la reivindicacion 20, donde el surfactante es un monoglicérido, un cremoforo, un éter de alcohol graso de polietilenglicol, un éster de ácido graso de sorbitano, un éster de ácido graso de polioxietileno sorbitano, Solutol HS15 (ésteres de polioxietileno de ácido 12-hidroxiesteárico), un alquil-sacárido (por ejemplo, octil glicosido, tetra decil maltosida) o un poloxámero, o una de sus combinaciones. Reivindicacion 32: La composicion farmacéutica de cualquiera de las reivindicaciones 1-31, donde componente principal en peso del medio hidrofobo es gliceril tricaprilato. Reivindicacion 36: La composicion farmacéutica de cualquiera de las reivindicaciones 1-35, que además comprende un estabilizador de aliskirén. Reivindicacion 37: La composicion farmacéutica de la reivindicacion 36, donde el estabilizador de aliskirén es un aminoácido. Reivindicacion 40: La composicion farmacéutica de la reivindicacion 36, donde el estabilizador de aliskirén es una sal metálica. Reivindicacion 42: La composicion farmacéutica de la reivindicacion 41, donde la sal metálica se selecciona del grupo que consiste en MgCl2, ZnCI2, CaCI2, acetato de Zn, acetato de Mg y acetato de Ca. Reivindicacion 47: La composicion farmacéutica de cualquiera de las reivindicaciones 1-45, donde el medio hidrofobo consiste esencialmente en gliceril tricaprilato. Reivindicacion 61: Un proceso para la produccion de una composicion farmacéutica, que comprende la preparacion de una solucion acuosa que comprende una cantidad terapéuticamente eficaz de aliskirén; opcionalmente, un segundo agente terapéutico; y en forma opcional, un tercer agente terapéutico; y una sal de ácido graso de cadena media; el secado de la solucion acuosa, de modo de obtener un polvo solido; y la suspension del polvo solido en un medio hidrofobo, a fin de producir una suspension que contiene, en forma solida, el aliskirén y la sal de ácido graso de cadena media, de manera de producir la composicion farmacéutica. Reivindicacion 112: Una cápsula que contiene la composicion de cualquiera de las reivindicaciones 1-60 y 108. Reivindicacion 116: Un método para el tratamiento de hipertension, hipertension con diabetes, insuficiencia cardíaca congestiva, angina de pecho, infarto de miocardio, arterioesclerosis, nefropatía diabética, miopatía cardíaca diabética, insuficiencia renal, albuminuria, enfermedad vascular periférica, hipertrofia ventricular izquierda, disfuncion cognitiva, accidente cerebrovascular, cefalea e insuficiencia cardiaca cronica, donde dicho método comprende la administracion de una cantidad terapéuticamente eficaz de una forma farmacéutica oral solida de cualquiera de las reivindicaciones 109-110, a un paciente que lo necesita. Reivindicacion 118: La composicion de cualquiera de las reivindicaciones 1-60 y 108, donde el segundo o el tercer agente terapéutico se selecciona del grupo que consiste en antagonistas del receptor AT1, inhibidores de la HMG-Co-A reductasa, inhibidores de la enzima convertidora de la angiotensina (ECA), bloqueadores del canal de calcio, inhibidores de la aldosterona sintasa, antagonistas de la aldosterona, inhibidores duales de la enzima convertidora de la angiotensina/endopeptidasa neutra (ACE/NEP), antagonistas de la endotelina y diuréticos.Claim 1: A pharmaceutical composition comprising a suspension comprising a mixture of a hydrophobic medium and a solid form, wherein the solid form comprises a therapeutically effective amount of aliskiren, and optionally, a second therapeutic agent, and optionally, a third therapeutic agent, and at least one salt of a medium chain fatty acid. Claim 8: The pharmaceutical composition of claim 7, wherein the medium chain fatty acid salt is sodium hexanoate, sodium heptanoate, sodium octanoate, sodium nonanoate, sodium decanoate, sodium undecanoate, sodium dodecanoate, sodium tridecanoate or sodium tetradecanoate, or a corresponding salt of potassium, lithium or ammonium, or one of its combinations. Claim 10: The pharmaceutical composition of any of claims 1-9, wherein the medium chain fatty acid salt is presented in the composition in an amount of 11% to 40% by weight, preferably 12% to 18% by weight , more preferably, about 15% by weight. Claim 11: The pharmaceutical composition of any of claims 1-10, wherein the medium chain fatty acid salt is presented in the solid form in an amount of 50% to 90% by weight, preferably, in an amount of 70% at 80% by weight. Claim 12: The pharmaceutical composition of any of claims 1-11, wherein the matrix-forming polymer is presented in the composition in an amount of about 0.5% to 15% by weight, preferably about 1% by weight. 10% by weight Claim 13: The pharmaceutical composition of any of claims 1-12, wherein the matrix-forming polymer is selected from the group consisting of polyvinylpyrrolidone, carbomer (for example, Carbopol polymer), polyvinyl alcohol, dextran, alginate salt, salt of hyaluronate and polyacrylic acid salt, or one of its combinations. Claim 15: The pharmaceutical composition of claim 14, wherein the polyvinylpyrrolidone is preferably PVP-12, and preferably has a molecular weight of about 3000, and is presented in the composition in an amount of about 2% at about 20% by weight, preferably, in an amount of about 5% to about 15% by weight, more preferably, in an amount of about 10% by weight. Claim 16: The pharmaceutical composition of claim 14, wherein the carbomer is preferably Carbopol 934P, and is presented in the composition in an amount of about 0.1% to about 6% by weight, preferably in an amount from about 0.5% to about 4% by weight, more preferably, in an amount of about 1% by weight. Claim 17: The pharmaceutical composition of claim 14, wherein the polyvinyl alcohol is preferably polyvinyl alcohol with a molecular weight of about 27,000 Da, and is presented in the composition in an amount of 4% by weight, more preferably, in an amount of about 1-2% by weight. Claim 20: The pharmaceutical composition of any of claims 1-19, further comprising a surfactant. Claim 22: The pharmaceutical composition of claim 20, wherein the surfactant is lecithin or a bile salt (for example, sodium taurocholate), or a detergent, or one of its combinations. Claim 23: The pharmaceutical composition of claim 20, wherein the surfactant is a monoglyceride, a cremophor, a polyethylene glycol fatty alcohol ether, a sorbitan fatty acid ester, a sorbitan polyoxyethylene fatty acid ester, Solutol HS15 (esters of 12-hydroxystearic acid polyoxyethylene), an alkyl saccharide (eg, octyl glycoside, tetra decyl maltoside) or a poloxamer, or one of its combinations. Claim 32: The pharmaceutical composition of any of claims 1-31, wherein the main component by weight of the hydrophobic medium is glyceryl tricaprilate. Claim 36: The pharmaceutical composition of any of claims 1-35, further comprising an aliskiren stabilizer. Claim 37: The pharmaceutical composition of claim 36, wherein the aliskiren stabilizer is an amino acid. Claim 40: The pharmaceutical composition of claim 36, wherein the aliskiren stabilizer is a metal salt. Claim 42: The pharmaceutical composition of claim 41, wherein the metal salt is selected from the group consisting of MgCl2, ZnCI2, CaCI2, Zn acetate, Mg acetate and Ca acetate. Claim 47: The pharmaceutical composition of any of the claims 1-45, wherein the hydrophobic medium consists essentially of glyceryl tricaprilate. Claim 61: A process for the production of a pharmaceutical composition, comprising the preparation of an aqueous solution comprising a therapeutically effective amount of aliskiren; optionally, a second therapeutic agent; and optionally, a third therapeutic agent; and a medium chain fatty acid salt; the drying of the aqueous solution, so as to obtain a solid powder; and the suspension of the solid powder in a hydrophobic medium, in order to produce a suspension containing, in solid form, the aliskiren and the medium-chain fatty acid salt, so as to produce the pharmaceutical composition. Claim 112: A capsule containing the composition of any of claims 1-60 and 108. Claim 116: A method for the treatment of hypertension, hypertension with diabetes, congestive heart failure, angina pectoris, myocardial infarction, arteriosclerosis, nephropathy diabetic, diabetic cardiac myopathy, renal failure, albuminuria, peripheral vascular disease, left ventricular hypertrophy, cognitive dysfunction, stroke, headache and chronic heart failure, where said method comprises the administration of a therapeutically effective amount of a solid oral pharmaceutical form of any of claims 109-110, to a patient in need. Claim 118: The composition of any of claims 1-60 and 108, wherein the second or third therapeutic agent is selected from the group consisting of AT1 receptor antagonists, HMG-Co-A reductase inhibitors, enzyme inhibitors angiotensin converting (ACE), calcium channel blockers, aldosterone synthase inhibitors, aldosterone antagonists, dual angiotensin / neutral endopeptidase converting enzyme (ACE / NEP) inhibitors, endothelin antagonists and diuretics.
Applications Claiming Priority (1)
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| US31439810P | 2010-03-16 | 2010-03-16 |
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| ARP110100850A AR080683A1 (en) | 2010-03-16 | 2011-03-16 | PHARMACEUTICAL COMPOSITIONS OF ALISKIREN AND METHODS OF ADMINISTRATION |
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| TW (1) | TW201136582A (en) |
| WO (1) | WO2011116115A1 (en) |
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| US20150283163A1 (en) * | 2014-04-04 | 2015-10-08 | Organic Medical Ventures, L.L.C. | Muscle treatment composition and method making same |
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| US5508272A (en) | 1993-06-15 | 1996-04-16 | Bristol-Myers Squibb Company | Compounds containing a fused bicycle ring and processes therefor |
| DE69426698T2 (en) | 1993-08-18 | 2001-08-16 | Banyu Pharmaceutical Co., Ltd. | CONDENSED HETEROAROMATIC CYCLOPENTE DERIVATIVES WITH ENDOTHELINE-ANTAGONISTIC ACTIVITY |
| MY119161A (en) | 1994-04-18 | 2005-04-30 | Novartis Ag | Delta-amino-gamma-hydroxy-omega-aryl-alkanoic acid amides with enzyme especially renin inhibiting activities |
| US5612359A (en) | 1994-08-26 | 1997-03-18 | Bristol-Myers Squibb Company | Substituted biphenyl isoxazole sulfonamides |
| US6083955A (en) | 1995-12-20 | 2000-07-04 | Yamanouchi Pharmaceutical Co., Ltd. | Arylethenesulfonamide derivatives and drug composition containing the same |
| IT1277737B1 (en) | 1995-12-28 | 1997-11-12 | Zambon Spa | TIOLIC DERIVATIVES FOR METALLOPEPTIDASE INHIBITIVE ACTIVITY |
| WO1997027314A1 (en) | 1996-01-23 | 1997-07-31 | Shionogi & Co., Ltd. | Process for producing oleanolic acid analogs by culturing hairy root |
| SK130098A3 (en) | 1996-04-04 | 1999-05-07 | Banyu Pharma Co Ltd | Method of treating heart failure with endothelin antagonists |
| PE20050596A1 (en) * | 2003-12-19 | 2005-10-18 | Novartis Ag | MICROEMULSION INCLUDING A RENIN INHIBITOR |
| BRPI0817586A2 (en) | 2007-09-28 | 2015-03-31 | Novartis Ag | Galenic formulations of organic compounds |
| PL2205279T3 (en) * | 2007-09-28 | 2011-09-30 | Novartis Ag | Pharmaceutical combination of aliskiren and valsartan |
| AR066168A1 (en) * | 2007-09-28 | 2009-07-29 | Novartis Ag | GALENIC FORMULATIONS OF ORGANIC COMPOUNDS |
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| TW201136582A (en) | 2011-11-01 |
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