IL138345A - Composition comprising eprosartan and its use in the preparation of medicaments for blocking angiotensin ii receptors and for treating hypertension, congestive heart failure and renal failure - Google Patents
Composition comprising eprosartan and its use in the preparation of medicaments for blocking angiotensin ii receptors and for treating hypertension, congestive heart failure and renal failureInfo
- Publication number
- IL138345A IL138345A IL13834599A IL13834599A IL138345A IL 138345 A IL138345 A IL 138345A IL 13834599 A IL13834599 A IL 13834599A IL 13834599 A IL13834599 A IL 13834599A IL 138345 A IL138345 A IL 138345A
- Authority
- IL
- Israel
- Prior art keywords
- eprosartan
- composition
- preparation
- salt
- medicament
- Prior art date
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 59
- 239000002080 C09CA02 - Eprosartan Substances 0.000 title claims abstract description 34
- 229960004563 eprosartan Drugs 0.000 title claims abstract description 34
- OROAFUQRIXKEMV-LDADJPATSA-N eprosartan Chemical compound C=1C=C(C(O)=O)C=CC=1CN1C(CCCC)=NC=C1\C=C(C(O)=O)/CC1=CC=CS1 OROAFUQRIXKEMV-LDADJPATSA-N 0.000 title claims abstract description 34
- 206010020772 Hypertension Diseases 0.000 title claims abstract description 10
- 206010007559 Cardiac failure congestive Diseases 0.000 title claims abstract description 8
- 206010019280 Heart failures Diseases 0.000 title claims abstract description 8
- 208000001647 Renal Insufficiency Diseases 0.000 title claims abstract description 8
- 201000006370 kidney failure Diseases 0.000 title claims abstract description 8
- 102000008873 Angiotensin II receptor Human genes 0.000 title claims abstract description 7
- 108050000824 Angiotensin II receptor Proteins 0.000 title claims abstract description 7
- 238000002360 preparation method Methods 0.000 title claims description 13
- 239000003814 drug Substances 0.000 title claims description 12
- 230000000903 blocking effect Effects 0.000 title claims description 5
- 150000003839 salts Chemical class 0.000 claims abstract description 27
- 239000012453 solvate Substances 0.000 claims abstract description 16
- 238000000034 method Methods 0.000 claims abstract description 9
- 239000002245 particle Substances 0.000 claims description 22
- 150000001875 compounds Chemical class 0.000 claims description 17
- 238000003801 milling Methods 0.000 claims description 13
- 239000011324 bead Substances 0.000 claims description 10
- 239000002775 capsule Substances 0.000 claims description 8
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 8
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 8
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 8
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical group OC1C(O)C(OC)OC(CO)C1OC1C(O)C(O)C(OC2C(C(O)C(OC3C(C(O)C(O)C(CO)O3)O)C(CO)O2)O)C(CO)O1 UFVKGYZPFZQRLF-UHFFFAOYSA-N 0.000 claims description 8
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 8
- 239000002934 diuretic Substances 0.000 claims description 7
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 7
- 238000009826 distribution Methods 0.000 claims description 6
- 230000001882 diuretic effect Effects 0.000 claims description 6
- 239000008194 pharmaceutical composition Substances 0.000 claims description 6
- 238000001694 spray drying Methods 0.000 claims description 6
- 238000001238 wet grinding Methods 0.000 claims description 6
- 238000011049 filling Methods 0.000 claims description 5
- FBPFZTCFMRRESA-KVTDHHQDSA-N D-Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 claims description 4
- 229930195725 Mannitol Natural products 0.000 claims description 4
- 239000000594 mannitol Substances 0.000 claims description 4
- 235000010355 mannitol Nutrition 0.000 claims description 4
- 239000000843 powder Substances 0.000 claims description 4
- 239000005541 ACE inhibitor Substances 0.000 claims description 3
- JZUFKLXOESDKRF-UHFFFAOYSA-N Chlorothiazide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC2=C1NCNS2(=O)=O JZUFKLXOESDKRF-UHFFFAOYSA-N 0.000 claims description 3
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims description 3
- 229960000573 eprosartan mesylate Drugs 0.000 claims description 3
- DJSLTDBPKHORNY-XMMWENQYSA-N eprosartan methanesulfonate Chemical compound CS(O)(=O)=O.C=1C=C(C(O)=O)C=CC=1CN1C(CCCC)=NC=C1\C=C(C(O)=O)/CC1=CC=CS1 DJSLTDBPKHORNY-XMMWENQYSA-N 0.000 claims description 3
- 229960002003 hydrochlorothiazide Drugs 0.000 claims description 3
- RVTZCBVAJQQJTK-UHFFFAOYSA-N oxygen(2-);zirconium(4+) Chemical compound [O-2].[O-2].[Zr+4] RVTZCBVAJQQJTK-UHFFFAOYSA-N 0.000 claims description 3
- 239000002461 renin inhibitor Substances 0.000 claims description 3
- 229940086526 renin-inhibitors Drugs 0.000 claims description 3
- 229910001928 zirconium oxide Inorganic materials 0.000 claims description 3
- 101710129690 Angiotensin-converting enzyme inhibitor Proteins 0.000 claims description 2
- 101710086378 Bradykinin-potentiating and C-type natriuretic peptides Proteins 0.000 claims description 2
- 229920002678 cellulose Polymers 0.000 claims description 2
- 239000001913 cellulose Substances 0.000 claims description 2
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims 1
- 229910052791 calcium Inorganic materials 0.000 claims 1
- 239000011575 calcium Substances 0.000 claims 1
- 239000000725 suspension Substances 0.000 description 13
- 238000009472 formulation Methods 0.000 description 12
- 239000003826 tablet Substances 0.000 description 12
- 239000007921 spray Substances 0.000 description 11
- 150000004677 hydrates Chemical class 0.000 description 9
- 239000012530 fluid Substances 0.000 description 6
- 239000011230 binding agent Substances 0.000 description 5
- 239000007884 disintegrant Substances 0.000 description 5
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 description 5
- -1 4-carboxyphenyl Chemical group 0.000 description 4
- 239000000945 filler Substances 0.000 description 4
- 239000012729 immediate-release (IR) formulation Substances 0.000 description 4
- 238000002156 mixing Methods 0.000 description 4
- 230000036470 plasma concentration Effects 0.000 description 4
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 4
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 4
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 4
- 239000004094 surface-active agent Substances 0.000 description 4
- 239000008186 active pharmaceutical agent Substances 0.000 description 3
- 239000012736 aqueous medium Substances 0.000 description 3
- 238000007796 conventional method Methods 0.000 description 3
- 229940088679 drug related substance Drugs 0.000 description 3
- 238000005469 granulation Methods 0.000 description 3
- 230000003179 granulation Effects 0.000 description 3
- 239000000314 lubricant Substances 0.000 description 3
- 239000000463 material Substances 0.000 description 3
- GUBGYTABKSRVRQ-XLOQQCSPSA-N Alpha-Lactose Chemical compound O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-XLOQQCSPSA-N 0.000 description 2
- 206010003210 Arteriosclerosis Diseases 0.000 description 2
- 208000037260 Atherosclerotic Plaque Diseases 0.000 description 2
- 229940127291 Calcium channel antagonist Drugs 0.000 description 2
- 241000282472 Canis lupus familiaris Species 0.000 description 2
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 2
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 2
- 229920002472 Starch Polymers 0.000 description 2
- 239000007900 aqueous suspension Substances 0.000 description 2
- 239000000480 calcium channel blocker Substances 0.000 description 2
- 239000000969 carrier Substances 0.000 description 2
- YKGMKSIHIVVYKY-UHFFFAOYSA-N dabrafenib mesylate Chemical compound CS(O)(=O)=O.S1C(C(C)(C)C)=NC(C=2C(=C(NS(=O)(=O)C=3C(=CC=CC=3F)F)C=CC=2)F)=C1C1=CC=NC(N)=N1 YKGMKSIHIVVYKY-UHFFFAOYSA-N 0.000 description 2
- 239000003085 diluting agent Substances 0.000 description 2
- 201000010099 disease Diseases 0.000 description 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 2
- 229940079593 drug Drugs 0.000 description 2
- 239000003937 drug carrier Substances 0.000 description 2
- 239000008187 granular material Substances 0.000 description 2
- 239000001863 hydroxypropyl cellulose Substances 0.000 description 2
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 description 2
- 239000008101 lactose Substances 0.000 description 2
- 238000011068 loading method Methods 0.000 description 2
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 2
- 230000002265 prevention Effects 0.000 description 2
- AQHHHDLHHXJYJD-UHFFFAOYSA-N propranolol Chemical compound C1=CC=C2C(OCC(O)CNC(C)C)=CC=CC2=C1 AQHHHDLHHXJYJD-UHFFFAOYSA-N 0.000 description 2
- 239000008213 purified water Substances 0.000 description 2
- 239000007787 solid Substances 0.000 description 2
- 239000008107 starch Substances 0.000 description 2
- 229940032147 starch Drugs 0.000 description 2
- 235000019698 starch Nutrition 0.000 description 2
- 239000007916 tablet composition Substances 0.000 description 2
- 230000001225 therapeutic effect Effects 0.000 description 2
- 239000000080 wetting agent Substances 0.000 description 2
- YNGDWRXWKFWCJY-UHFFFAOYSA-N 1,4-Dihydropyridine Chemical compound C1C=CNC=C1 YNGDWRXWKFWCJY-UHFFFAOYSA-N 0.000 description 1
- 206010002383 Angina Pectoris Diseases 0.000 description 1
- 102000005862 Angiotensin II Human genes 0.000 description 1
- 101800000733 Angiotensin-2 Proteins 0.000 description 1
- 208000019901 Anxiety disease Diseases 0.000 description 1
- 229920002785 Croscarmellose sodium Polymers 0.000 description 1
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 description 1
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 description 1
- 208000007342 Diabetic Nephropathies Diseases 0.000 description 1
- 206010012689 Diabetic retinopathy Diseases 0.000 description 1
- 229940097420 Diuretic Drugs 0.000 description 1
- 108010061435 Enalapril Proteins 0.000 description 1
- 208000010412 Glaucoma Diseases 0.000 description 1
- 208000016988 Hemorrhagic Stroke Diseases 0.000 description 1
- CZGUSIXMZVURDU-JZXHSEFVSA-N Ile(5)-angiotensin II Chemical compound C([C@@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](CC=1C=CC=CC=1)C([O-])=O)NC(=O)[C@@H](NC(=O)[C@H](CCCNC(N)=[NH2+])NC(=O)[C@@H]([NH3+])CC([O-])=O)C(C)C)C1=CC=C(O)C=C1 CZGUSIXMZVURDU-JZXHSEFVSA-N 0.000 description 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 description 1
- 206010061216 Infarction Diseases 0.000 description 1
- 235000017858 Laurus nobilis Nutrition 0.000 description 1
- 208000007177 Left Ventricular Hypertrophy Diseases 0.000 description 1
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 1
- 229920000881 Modified starch Polymers 0.000 description 1
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- CZMRCDWAGMRECN-UGDNZRGBSA-N Sucrose Chemical compound O[C@H]1[C@H](O)[C@@H](CO)O[C@@]1(CO)O[C@@H]1[C@H](O)[C@@H](O)[C@H](O)[C@@H](CO)O1 CZMRCDWAGMRECN-UGDNZRGBSA-N 0.000 description 1
- 229930006000 Sucrose Natural products 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-L Sulfate Chemical compound [O-]S([O-])(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-L 0.000 description 1
- 235000005212 Terminalia tomentosa Nutrition 0.000 description 1
- 244000125380 Terminalia tomentosa Species 0.000 description 1
- 229940121792 Thiazide diuretic Drugs 0.000 description 1
- TVXBFESIOXBWNM-UHFFFAOYSA-N Xylitol Natural products OCCC(O)C(O)C(O)CCO TVXBFESIOXBWNM-UHFFFAOYSA-N 0.000 description 1
- DPXJVFZANSGRMM-UHFFFAOYSA-N acetic acid;2,3,4,5,6-pentahydroxyhexanal;sodium Chemical compound [Na].CC(O)=O.OCC(O)C(O)C(O)C(O)C=O DPXJVFZANSGRMM-UHFFFAOYSA-N 0.000 description 1
- 239000013543 active substance Substances 0.000 description 1
- 238000002399 angioplasty Methods 0.000 description 1
- 229950006323 angiotensin ii Drugs 0.000 description 1
- 239000005557 antagonist Substances 0.000 description 1
- 230000036506 anxiety Effects 0.000 description 1
- 239000008365 aqueous carrier Substances 0.000 description 1
- 230000009286 beneficial effect Effects 0.000 description 1
- 102000015005 beta-adrenergic receptor activity proteins Human genes 0.000 description 1
- 108040006818 beta-adrenergic receptor activity proteins Proteins 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000008280 blood Substances 0.000 description 1
- 210000004369 blood Anatomy 0.000 description 1
- 230000036765 blood level Effects 0.000 description 1
- 235000021152 breakfast Nutrition 0.000 description 1
- 229960000830 captopril Drugs 0.000 description 1
- FAKRSMQSSFJEIM-RQJHMYQMSA-N captopril Chemical compound SC[C@@H](C)C(=O)N1CCC[C@H]1C(O)=O FAKRSMQSSFJEIM-RQJHMYQMSA-N 0.000 description 1
- 235000014633 carbohydrates Nutrition 0.000 description 1
- 150000001720 carbohydrates Chemical class 0.000 description 1
- 208000015114 central nervous system disease Diseases 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000003920 cognitive function Effects 0.000 description 1
- 239000003086 colorant Substances 0.000 description 1
- 239000013065 commercial product Substances 0.000 description 1
- 238000007906 compression Methods 0.000 description 1
- 230000006835 compression Effects 0.000 description 1
- 238000011109 contamination Methods 0.000 description 1
- 238000013270 controlled release Methods 0.000 description 1
- 229960001681 croscarmellose sodium Drugs 0.000 description 1
- 229960000913 crospovidone Drugs 0.000 description 1
- 235000010947 crosslinked sodium carboxy methyl cellulose Nutrition 0.000 description 1
- 230000007850 degeneration Effects 0.000 description 1
- 230000003111 delayed effect Effects 0.000 description 1
- 238000013461 design Methods 0.000 description 1
- 208000033679 diabetic kidney disease Diseases 0.000 description 1
- 150000004683 dihydrates Chemical class 0.000 description 1
- 229940030606 diuretics Drugs 0.000 description 1
- 239000002552 dosage form Substances 0.000 description 1
- 238000001035 drying Methods 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 229960000873 enalapril Drugs 0.000 description 1
- GBXSMTUPTTWBMN-XIRDDKMYSA-N enalapril Chemical compound C([C@@H](C(=O)OCC)N[C@@H](C)C(=O)N1[C@@H](CCC1)C(O)=O)CC1=CC=CC=C1 GBXSMTUPTTWBMN-XIRDDKMYSA-N 0.000 description 1
- 239000002702 enteric coating Substances 0.000 description 1
- 238000009505 enteric coating Methods 0.000 description 1
- 239000000796 flavoring agent Substances 0.000 description 1
- 238000009477 fluid bed granulation Methods 0.000 description 1
- 229960003883 furosemide Drugs 0.000 description 1
- ZZUFCTLCJUWOSV-UHFFFAOYSA-N furosemide Chemical compound C1=C(Cl)C(S(=O)(=O)N)=CC(C(O)=O)=C1NCC1=CC=CO1 ZZUFCTLCJUWOSV-UHFFFAOYSA-N 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 239000007903 gelatin capsule Substances 0.000 description 1
- 230000007574 infarction Effects 0.000 description 1
- 238000010902 jet-milling Methods 0.000 description 1
- 239000000832 lactitol Substances 0.000 description 1
- 235000010448 lactitol Nutrition 0.000 description 1
- VQHSOMBJVWLPSR-JVCRWLNRSA-N lactitol Chemical compound OC[C@H](O)[C@@H](O)[C@@H]([C@H](O)CO)O[C@@H]1O[C@H](CO)[C@H](O)[C@H](O)[C@H]1O VQHSOMBJVWLPSR-JVCRWLNRSA-N 0.000 description 1
- 229960003451 lactitol Drugs 0.000 description 1
- 229960001375 lactose Drugs 0.000 description 1
- 239000002171 loop diuretic Substances 0.000 description 1
- 235000019359 magnesium stearate Nutrition 0.000 description 1
- 239000011159 matrix material Substances 0.000 description 1
- 238000005259 measurement Methods 0.000 description 1
- 239000002609 medium Substances 0.000 description 1
- HEBKCHPVOIAQTA-UHFFFAOYSA-N meso ribitol Natural products OCC(O)C(O)C(O)CO HEBKCHPVOIAQTA-UHFFFAOYSA-N 0.000 description 1
- 229920000609 methyl cellulose Polymers 0.000 description 1
- 239000001923 methylcellulose Substances 0.000 description 1
- 235000010981 methylcellulose Nutrition 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 239000007912 modified release tablet Substances 0.000 description 1
- 239000003607 modifier Substances 0.000 description 1
- 229960001597 nifedipine Drugs 0.000 description 1
- HYIMSNHJOBLJNT-UHFFFAOYSA-N nifedipine Chemical compound COC(=O)C1=C(C)NC(C)=C(C(=O)OC)C1C1=CC=CC=C1[N+]([O-])=O HYIMSNHJOBLJNT-UHFFFAOYSA-N 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 238000000643 oven drying Methods 0.000 description 1
- 239000008188 pellet Substances 0.000 description 1
- 230000002572 peristaltic effect Effects 0.000 description 1
- 229920000642 polymer Polymers 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 1
- 230000009862 primary prevention Effects 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 239000000047 product Substances 0.000 description 1
- 229960003712 propranolol Drugs 0.000 description 1
- 230000002685 pulmonary effect Effects 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
- 230000009863 secondary prevention Effects 0.000 description 1
- 230000035945 sensitivity Effects 0.000 description 1
- 239000000377 silicon dioxide Substances 0.000 description 1
- 235000012239 silicon dioxide Nutrition 0.000 description 1
- 239000011734 sodium Substances 0.000 description 1
- 229910052708 sodium Inorganic materials 0.000 description 1
- 229920003109 sodium starch glycolate Polymers 0.000 description 1
- 229940079832 sodium starch glycolate Drugs 0.000 description 1
- 239000008109 sodium starch glycolate Substances 0.000 description 1
- 239000008279 sol Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 229960002920 sorbitol Drugs 0.000 description 1
- 238000000528 statistical test Methods 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 229960004793 sucrose Drugs 0.000 description 1
- 229910021653 sulphate ion Inorganic materials 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 238000001356 surgical procedure Methods 0.000 description 1
- 238000013268 sustained release Methods 0.000 description 1
- 239000012730 sustained-release form Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 238000012360 testing method Methods 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- 239000003451 thiazide diuretic agent Substances 0.000 description 1
- 230000002110 toxicologic effect Effects 0.000 description 1
- 231100000759 toxicological effect Toxicity 0.000 description 1
- 238000009827 uniform distribution Methods 0.000 description 1
- 239000001993 wax Substances 0.000 description 1
- 239000000811 xylitol Substances 0.000 description 1
- 229960002675 xylitol Drugs 0.000 description 1
- 235000010447 xylitol Nutrition 0.000 description 1
- HEBKCHPVOIAQTA-SCDXWVJYSA-N xylitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)CO HEBKCHPVOIAQTA-SCDXWVJYSA-N 0.000 description 1
Classifications
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
- A61K31/4164—1,3-Diazoles
- A61K31/4178—1,3-Diazoles not condensed 1,3-diazoles and containing further heterocyclic rings, e.g. pilocarpine, nitrofurantoin
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/38—Heterocyclic compounds having sulfur as a ring hetero atom
- A61K31/381—Heterocyclic compounds having sulfur as a ring hetero atom having five-membered rings
-
- 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
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
-
- 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
- A61K9/141—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers
- A61K9/146—Intimate drug-carrier mixtures characterised by the carrier, e.g. ordered mixtures, adsorbates, solid solutions, eutectica, co-dried, co-solubilised, co-kneaded, co-milled, co-ground products, co-precipitates, co-evaporates, co-extrudates, co-melts; Drug nanoparticles with adsorbed surface modifiers with organic macromolecular compounds
-
- 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
- A61P13/12—Drugs for disorders of the urinary system of the kidneys
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- 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
- A61P9/04—Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
-
- 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
- A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
-
- 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)
- General Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Urology & Nephrology (AREA)
- Vascular Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Plural Heterocyclic Compounds (AREA)
- Steroid Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US7766098P | 1998-03-11 | 1998-03-11 | |
| PCT/US1999/004651 WO1999045779A1 (en) | 1998-03-11 | 1999-03-11 | Novel compositions of eprosartan |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL138345A0 IL138345A0 (en) | 2001-10-31 |
| IL138345A true IL138345A (en) | 2004-12-15 |
Family
ID=22139347
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL13834599A IL138345A (en) | 1998-03-11 | 1999-03-11 | Composition comprising eprosartan and its use in the preparation of medicaments for blocking angiotensin ii receptors and for treating hypertension, congestive heart failure and renal failure |
Country Status (21)
| Country | Link |
|---|---|
| EP (1) | EP1061803B1 (cs) |
| JP (1) | JP2002506010A (cs) |
| KR (1) | KR20010041796A (cs) |
| CN (1) | CN1299235A (cs) |
| AT (1) | ATE508633T1 (cs) |
| AU (1) | AU757547B2 (cs) |
| BR (1) | BR9908691A (cs) |
| CA (1) | CA2323363C (cs) |
| CY (1) | CY1111738T1 (cs) |
| CZ (1) | CZ303067B6 (cs) |
| DK (1) | DK1061803T3 (cs) |
| ES (1) | ES2366394T3 (cs) |
| HU (1) | HU228574B1 (cs) |
| IL (1) | IL138345A (cs) |
| NO (1) | NO331207B1 (cs) |
| NZ (1) | NZ506700A (cs) |
| PL (1) | PL192545B1 (cs) |
| SI (1) | SI1061803T1 (cs) |
| TR (1) | TR200002646T2 (cs) |
| WO (1) | WO1999045779A1 (cs) |
| ZA (1) | ZA991922B (cs) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP0810853B1 (en) | 1995-02-24 | 2004-08-25 | Elan Pharma International Limited | Aerosols containing nanoparticle dispersions |
| CN1198591C (zh) * | 1998-07-20 | 2005-04-27 | 史密丝克莱恩比彻姆公司 | 在口服固体剂型中包含依普沙坦的生物利用度提高的制剂 |
| US7521068B2 (en) | 1998-11-12 | 2009-04-21 | Elan Pharma International Ltd. | Dry powder aerosols of nanoparticulate drugs |
| CN1422152A (zh) * | 2000-04-12 | 2003-06-04 | 诺瓦提斯公司 | 有机化合物的联合形式 |
| DE10230272A1 (de) * | 2002-07-05 | 2004-01-22 | Solvay Pharmaceuticals Gmbh | AT1-Rezeptorantagonisten zur Prävention von Folgeschlaganfällen |
| EP1382334A1 (en) * | 2002-07-11 | 2004-01-21 | Université de Picardie Jules Verne | Use of angiotensin II AT1-receptor blockers (ARB), alone or combined with thiazide or angiotensin II for the treatment of stroke |
| US7232828B2 (en) * | 2002-08-10 | 2007-06-19 | Bethesda Pharmaceuticals, Inc. | PPAR Ligands that do not cause fluid retention, edema or congestive heart failure |
| AU2004206109A1 (en) * | 2003-01-21 | 2004-08-05 | Ranbaxy Laboratories Limited | Co-precipitated amorphous losartan and dosage forms comprising the same |
| BRPI0406987A (pt) | 2003-01-31 | 2006-01-10 | Sankyo Co | Medicamento para a prevenção e/ou tratamento de arteriosclerose, medicamentos para a inibição de proliferação de células do músculo liso vascular, de formação de neoìntima dos vasos sanguìneos e de remodelação vascular, medicamento para a prevenção de restenose que segue intervenção coronária percutânea, e, medicamentos para a profilaxia e/ou tratamento de hipertensão ou doenças causadas por hipertensão ou doenças causadas por hipertensão, de doenças cardìacas, de angina do peito, de infarto miocárdico, de arritmia, de morte súbita, de insuficiência cardìaca, de hipertrofia cardìaca, de doenças renais, de nefropatia diabética, de glomerulonefrite, de nefrosclerose, de doenças cerebrovasculares, de infarto cerebral, e de hemorragia cerebral |
| AU2005256634B2 (en) * | 2004-06-23 | 2010-12-09 | Solvay Pharmaceuticals Gmbh | Pharmaceutical compositions comprising NEP-inhibitors, inhibitors of the endogenous endothelin producing system and AT1-receptor antagonists |
| US20060099230A1 (en) * | 2004-11-10 | 2006-05-11 | Chin-Chih Chiang | Novel formulations of eprosartan with enhanced bioavailability |
| WO2006136916A2 (en) * | 2005-06-20 | 2006-12-28 | Glenmark Pharmaceuticals Limited | Substantially pure micronized particles of telmisartan and pharmaceutical compositions containing same |
| KR100715355B1 (ko) * | 2005-09-30 | 2007-05-07 | 주식회사유한양행 | 프란루카스트를 함유하는 분무-건조 과립 및 그의 제조방법 |
| WO2009013760A2 (en) * | 2007-07-25 | 2009-01-29 | Hetero Drugs Limited | Eprosartan mesylate crystalline particles and a process for preparing pure eprosartan |
| EP2108365A1 (en) * | 2008-04-09 | 2009-10-14 | LEK Pharmaceuticals d.d. | Single dosage pharmaceutical formulation comprising eprosartan mesylate |
| CN103705510A (zh) * | 2013-12-27 | 2014-04-09 | 华润赛科药业有限责任公司 | 一种阿齐沙坦固体组合物的制备方法 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4107288A (en) * | 1974-09-18 | 1978-08-15 | Pharmaceutical Society Of Victoria | Injectable compositions, nanoparticles useful therein, and process of manufacturing same |
| DE3013839A1 (de) * | 1979-04-13 | 1980-10-30 | Freunt Ind Co Ltd | Verfahren zur herstellung einer aktivierten pharmazeutischen zusammensetzung |
| JPS587609B2 (ja) | 1979-06-17 | 1983-02-10 | フロイント産業株式会社 | 粉体薬剤のコ−テング法 |
| US5185351A (en) * | 1989-06-14 | 1993-02-09 | Smithkline Beecham Corporation | Imidazolyl-alkenoic acids useful as angiotensin II receptor antagonists |
| JP2642486B2 (ja) | 1989-08-04 | 1997-08-20 | 田辺製薬株式会社 | 難溶性薬物の超微粒子化法 |
| US5145684A (en) * | 1991-01-25 | 1992-09-08 | Sterling Drug Inc. | Surface modified drug nanoparticles |
| EA001958B1 (ru) | 1996-03-29 | 2001-10-22 | Смитклайн Бичам Корпорейшн | Дигидрат эпросартана и способ его получения и готовая препаративная форма |
| NZ502644A (en) * | 1997-08-06 | 2002-03-01 | Smithkline Beecham Corp | Eprosartan arginyl charge-neutralization-complex useful for treating diseases where blockade of the angiotensin II receptor is indicated |
-
1999
- 1999-03-10 ZA ZA9901922A patent/ZA991922B/xx unknown
- 1999-03-11 HU HU0101243A patent/HU228574B1/hu not_active IP Right Cessation
- 1999-03-11 ES ES99909780T patent/ES2366394T3/es not_active Expired - Lifetime
- 1999-03-11 WO PCT/US1999/004651 patent/WO1999045779A1/en not_active Ceased
- 1999-03-11 TR TR2000/02646T patent/TR200002646T2/xx unknown
- 1999-03-11 SI SI9931058T patent/SI1061803T1/sl unknown
- 1999-03-11 AU AU28909/99A patent/AU757547B2/en not_active Ceased
- 1999-03-11 KR KR1020007010070A patent/KR20010041796A/ko not_active Ceased
- 1999-03-11 EP EP99909780A patent/EP1061803B1/en not_active Expired - Lifetime
- 1999-03-11 CN CN99805844A patent/CN1299235A/zh active Pending
- 1999-03-11 AT AT99909780T patent/ATE508633T1/de active
- 1999-03-11 CZ CZ20003288A patent/CZ303067B6/cs not_active IP Right Cessation
- 1999-03-11 CA CA002323363A patent/CA2323363C/en not_active Expired - Fee Related
- 1999-03-11 DK DK99909780.1T patent/DK1061803T3/da active
- 1999-03-11 NZ NZ506700A patent/NZ506700A/xx not_active IP Right Cessation
- 1999-03-11 BR BR9908691-3A patent/BR9908691A/pt not_active Application Discontinuation
- 1999-03-11 JP JP2000535205A patent/JP2002506010A/ja not_active Ceased
- 1999-03-11 PL PL343411A patent/PL192545B1/pl not_active IP Right Cessation
- 1999-03-11 IL IL13834599A patent/IL138345A/en not_active IP Right Cessation
-
2000
- 2000-09-08 NO NO20004502A patent/NO331207B1/no not_active IP Right Cessation
-
2011
- 2011-07-25 CY CY20111100730T patent/CY1111738T1/el unknown
Also Published As
| Publication number | Publication date |
|---|---|
| AU757547B2 (en) | 2003-02-27 |
| EP1061803B1 (en) | 2011-05-11 |
| NO20004502D0 (no) | 2000-09-08 |
| SI1061803T1 (sl) | 2011-09-30 |
| KR20010041796A (ko) | 2001-05-25 |
| CY1111738T1 (el) | 2015-10-07 |
| WO1999045779A1 (en) | 1999-09-16 |
| EP1061803A1 (en) | 2000-12-27 |
| AU2890999A (en) | 1999-09-27 |
| ATE508633T1 (de) | 2011-05-15 |
| IL138345A0 (en) | 2001-10-31 |
| PL343411A1 (en) | 2001-08-13 |
| NZ506700A (en) | 2003-03-28 |
| NO20004502L (no) | 2000-11-07 |
| CN1299235A (zh) | 2001-06-13 |
| HUP0101243A1 (hu) | 2002-05-29 |
| ES2366394T3 (es) | 2011-10-19 |
| EP1061803A4 (en) | 2007-12-26 |
| ZA991922B (en) | 1999-09-13 |
| CA2323363A1 (en) | 1999-09-16 |
| HU228574B1 (en) | 2013-04-29 |
| JP2002506010A (ja) | 2002-02-26 |
| CA2323363C (en) | 2008-09-30 |
| NO331207B1 (no) | 2011-10-31 |
| CZ303067B6 (cs) | 2012-03-21 |
| TR200002646T2 (tr) | 2001-01-22 |
| HUP0101243A3 (en) | 2005-09-28 |
| BR9908691A (pt) | 2000-12-26 |
| CZ20003288A3 (cs) | 2001-03-14 |
| PL192545B1 (pl) | 2006-11-30 |
| DK1061803T3 (da) | 2011-08-29 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| EP1039909B1 (en) | Method of production and composition of an oral preparation of itraconazole | |
| CA2338256C (en) | Bioenhanced formulations comprising eprosartan in oral solid dosage form | |
| EP1061803B1 (en) | Compositions of eprosartan | |
| JP2022510732A (ja) | ニロチニブの医薬組成物 | |
| US20020098241A1 (en) | High drug load immediate and modified release oral dosage formulations and processes for their manufacture | |
| EP0889880B1 (en) | Eprosartan dihydrate and a process for its production and formulation | |
| KR20160113294A (ko) | 안드로겐 수용체 길항제의 고체 제약 조성물 | |
| EA015108B1 (ru) | Способ получения твердой фармацевтической композиции, содержащей валсартан | |
| CA2310028C (en) | High drug load immediate and modified release oral dosage formulations and processes for their manufacture | |
| US20030022928A1 (en) | Novel compositions of eprosartan | |
| KR101931489B1 (ko) | 칼슘 길항약/안지오텐신 ii 수용체 길항약 함유 의약 제제의 제조 방법 | |
| JP6141580B2 (ja) | ラノラジンおよびドロネダロンの医薬組成物 | |
| US11260055B2 (en) | Oral pharmaceutical composition of lurasidone and preparation thereof | |
| MXPA00008888A (en) | Novel compositions of eprosartan | |
| JP2009538905A (ja) | 感湿性薬物を含んで成る安定性製剤及びその製造方法 | |
| ZA200406553B (en) | Pharmaceutical compositions comprising 2-(4-ethoxy-phenyl)-3-(4-methanesulfonyl-phenyl)-pyrazoloÄ1,5-bÜpyridazine in nanoparticulate form. | |
| MXPA00006574A (en) | Method and composition of an oral preparation of itraconazole |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FF | Patent granted | ||
| KB | Patent renewed | ||
| KB | Patent renewed | ||
| KB | Patent renewed | ||
| MM9K | Patent not in force due to non-payment of renewal fees |