CA2605183A1 - Compositions ameliorees biologiquement - Google Patents
Compositions ameliorees biologiquement Download PDFInfo
- Publication number
- CA2605183A1 CA2605183A1 CA002605183A CA2605183A CA2605183A1 CA 2605183 A1 CA2605183 A1 CA 2605183A1 CA 002605183 A CA002605183 A CA 002605183A CA 2605183 A CA2605183 A CA 2605183A CA 2605183 A1 CA2605183 A1 CA 2605183A1
- Authority
- CA
- Canada
- Prior art keywords
- composition
- agent
- valsartan
- solubility enhancing
- arb
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
- 239000000203 mixture Substances 0.000 title claims abstract description 151
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 78
- 230000002708 enhancing effect Effects 0.000 claims abstract description 70
- 238000004090 dissolution Methods 0.000 claims abstract description 51
- 238000000034 method Methods 0.000 claims abstract description 48
- 230000001965 increasing effect Effects 0.000 claims abstract description 12
- 102000008873 Angiotensin II receptor Human genes 0.000 claims abstract description 3
- 108050000824 Angiotensin II receptor Proteins 0.000 claims abstract description 3
- 239000004072 C09CA03 - Valsartan Substances 0.000 claims description 125
- 229960004699 valsartan Drugs 0.000 claims description 114
- -1 lauryl macrogol Chemical compound 0.000 claims description 32
- 229920000642 polymer Polymers 0.000 claims description 23
- 229920001223 polyethylene glycol Polymers 0.000 claims description 21
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 20
- 239000008108 microcrystalline cellulose Substances 0.000 claims description 20
- 229940016286 microcrystalline cellulose Drugs 0.000 claims description 20
- 235000019813 microcrystalline cellulose Nutrition 0.000 claims description 20
- 239000002202 Polyethylene glycol Substances 0.000 claims description 19
- 235000019333 sodium laurylsulphate Nutrition 0.000 claims description 19
- 239000004094 surface-active agent Substances 0.000 claims description 19
- 229960003511 macrogol Drugs 0.000 claims description 16
- 238000010521 absorption reaction Methods 0.000 claims description 15
- 239000002775 capsule Substances 0.000 claims description 13
- 210000001035 gastrointestinal tract Anatomy 0.000 claims description 13
- 238000002156 mixing Methods 0.000 claims description 13
- 239000002904 solvent Substances 0.000 claims description 12
- 229940030600 antihypertensive agent Drugs 0.000 claims description 11
- 239000002220 antihypertensive agent Substances 0.000 claims description 11
- 239000001768 carboxy methyl cellulose Substances 0.000 claims description 11
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 10
- 206010020772 Hypertension Diseases 0.000 claims description 10
- 239000011575 calcium Substances 0.000 claims description 10
- 229910052791 calcium Inorganic materials 0.000 claims description 10
- 239000004359 castor oil Substances 0.000 claims description 10
- 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 9
- 239000003524 antilipemic agent Substances 0.000 claims description 9
- 239000002876 beta blocker Substances 0.000 claims description 9
- 229940097320 beta blocking agent Drugs 0.000 claims description 9
- 235000019438 castor oil Nutrition 0.000 claims description 9
- 125000005456 glyceride group Chemical group 0.000 claims description 9
- ZEMPKEQAKRGZGQ-XOQCFJPHSA-N glycerol triricinoleate Natural products CCCCCC[C@@H](O)CC=CCCCCCCCC(=O)OC[C@@H](COC(=O)CCCCCCCC=CC[C@@H](O)CCCCCC)OC(=O)CCCCCCCC=CC[C@H](O)CCCCCC ZEMPKEQAKRGZGQ-XOQCFJPHSA-N 0.000 claims description 9
- 239000004041 inotropic agent Substances 0.000 claims description 9
- 150000003839 salts Chemical class 0.000 claims description 9
- 238000013268 sustained release Methods 0.000 claims description 9
- 239000012730 sustained-release form Substances 0.000 claims description 9
- 229920002153 Hydroxypropyl cellulose Polymers 0.000 claims description 8
- 239000001863 hydroxypropyl cellulose Substances 0.000 claims description 8
- KDYFGRWQOYBRFD-UHFFFAOYSA-L succinate(2-) Chemical compound [O-]C(=O)CCC([O-])=O KDYFGRWQOYBRFD-UHFFFAOYSA-L 0.000 claims description 8
- SMZOUWXMTYCWNB-UHFFFAOYSA-N 2-(2-methoxy-5-methylphenyl)ethanamine Chemical compound COC1=CC=C(C)C=C1CCN SMZOUWXMTYCWNB-UHFFFAOYSA-N 0.000 claims description 7
- NIXOWILDQLNWCW-UHFFFAOYSA-N 2-Propenoic acid Natural products OC(=O)C=C NIXOWILDQLNWCW-UHFFFAOYSA-N 0.000 claims description 7
- CERQOIWHTDAKMF-UHFFFAOYSA-N Methacrylic acid Chemical compound CC(=C)C(O)=O CERQOIWHTDAKMF-UHFFFAOYSA-N 0.000 claims description 7
- WPMWEFXCIYCJSA-UHFFFAOYSA-N Tetraethylene glycol monododecyl ether Chemical compound CCCCCCCCCCCCOCCOCCOCCOCCO WPMWEFXCIYCJSA-UHFFFAOYSA-N 0.000 claims description 7
- 239000008139 complexing agent Substances 0.000 claims description 7
- 201000010099 disease Diseases 0.000 claims description 7
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 7
- 235000010977 hydroxypropyl cellulose Nutrition 0.000 claims description 7
- 235000010979 hydroxypropyl methyl cellulose Nutrition 0.000 claims description 7
- 239000001866 hydroxypropyl methyl cellulose Substances 0.000 claims description 7
- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 7
- UFVKGYZPFZQRLF-UHFFFAOYSA-N hydroxypropyl methyl cellulose Chemical compound 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 7
- 208000017169 kidney disease Diseases 0.000 claims description 7
- 239000011159 matrix material Substances 0.000 claims description 7
- 229940113116 polyethylene glycol 1000 Drugs 0.000 claims description 7
- 229920005862 polyol Polymers 0.000 claims description 7
- 150000003077 polyols Chemical class 0.000 claims description 7
- RMMXLENWKUUMAY-UHFFFAOYSA-N telmisartan Chemical compound CCCC1=NC2=C(C)C=C(C=3N(C4=CC=CC=C4N=3)C)C=C2N1CC(C=C1)=CC=C1C1=CC=CC=C1C(O)=O RMMXLENWKUUMAY-UHFFFAOYSA-N 0.000 claims description 7
- 239000005541 ACE inhibitor Substances 0.000 claims description 6
- 229920002134 Carboxymethyl cellulose Polymers 0.000 claims description 6
- 229920000663 Hydroxyethyl cellulose Polymers 0.000 claims description 6
- 229920000881 Modified starch Polymers 0.000 claims description 6
- 239000004372 Polyvinyl alcohol Substances 0.000 claims description 6
- DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims description 6
- 239000004141 Sodium laurylsulphate Substances 0.000 claims description 6
- 229940044094 angiotensin-converting-enzyme inhibitor Drugs 0.000 claims description 6
- 229920001400 block copolymer Polymers 0.000 claims description 6
- 235000010948 carboxy methyl cellulose Nutrition 0.000 claims description 6
- 239000008112 carboxymethyl-cellulose Substances 0.000 claims description 6
- 229940105329 carboxymethylcellulose Drugs 0.000 claims description 6
- 239000000314 lubricant Substances 0.000 claims description 6
- 229920002503 polyoxyethylene-polyoxypropylene Polymers 0.000 claims description 6
- 229920002451 polyvinyl alcohol Polymers 0.000 claims description 6
- 229940068984 polyvinyl alcohol Drugs 0.000 claims description 6
- XZIIFPSPUDAGJM-UHFFFAOYSA-N 6-chloro-2-n,2-n-diethylpyrimidine-2,4-diamine Chemical compound CCN(CC)C1=NC(N)=CC(Cl)=N1 XZIIFPSPUDAGJM-UHFFFAOYSA-N 0.000 claims description 5
- 229920000858 Cyclodextrin Polymers 0.000 claims description 5
- 239000004354 Hydroxyethyl cellulose Substances 0.000 claims description 5
- 239000005913 Maltodextrin Substances 0.000 claims description 5
- 229920002774 Maltodextrin Polymers 0.000 claims description 5
- 229920003171 Poly (ethylene oxide) Polymers 0.000 claims description 5
- 229920002125 Sokalan® Polymers 0.000 claims description 5
- 229920002472 Starch Polymers 0.000 claims description 5
- 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 claims description 5
- 239000000883 anti-obesity agent Substances 0.000 claims description 5
- 239000003472 antidiabetic agent Substances 0.000 claims description 5
- 229940125708 antidiabetic agent Drugs 0.000 claims description 5
- 229940125710 antiobesity agent Drugs 0.000 claims description 5
- 239000011230 binding agent Substances 0.000 claims description 5
- 239000000378 calcium silicate Substances 0.000 claims description 5
- 229910052918 calcium silicate Inorganic materials 0.000 claims description 5
- OYACROKNLOSFPA-UHFFFAOYSA-N calcium;dioxido(oxo)silane Chemical compound [Ca+2].[O-][Si]([O-])=O OYACROKNLOSFPA-UHFFFAOYSA-N 0.000 claims description 5
- JAUGGEIKQIHSMF-UHFFFAOYSA-N dialuminum;dimagnesium;dioxido(oxo)silane;oxygen(2-);hydrate Chemical compound O.[O-2].[O-2].[Mg+2].[Mg+2].[Al+3].[Al+3].[O-][Si]([O-])=O.[O-][Si]([O-])=O.[O-][Si]([O-])=O JAUGGEIKQIHSMF-UHFFFAOYSA-N 0.000 claims description 5
- 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 claims description 5
- 150000002148 esters Chemical class 0.000 claims description 5
- 239000000945 filler Substances 0.000 claims description 5
- 235000019447 hydroxyethyl cellulose Nutrition 0.000 claims description 5
- 229940035034 maltodextrin Drugs 0.000 claims description 5
- 238000007909 melt granulation Methods 0.000 claims description 5
- 229920000609 methyl cellulose Polymers 0.000 claims description 5
- 235000010981 methylcellulose Nutrition 0.000 claims description 5
- 239000001923 methylcellulose Substances 0.000 claims description 5
- 239000004584 polyacrylic acid Substances 0.000 claims description 5
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 5
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 5
- 229940035044 sorbitan monolaurate Drugs 0.000 claims description 5
- 239000008107 starch Substances 0.000 claims description 5
- 235000019698 starch Nutrition 0.000 claims description 5
- 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 claims description 4
- 239000002083 C09CA01 - Losartan Substances 0.000 claims description 4
- 239000002080 C09CA02 - Eprosartan Substances 0.000 claims description 4
- 239000002053 C09CA06 - Candesartan Substances 0.000 claims description 4
- 239000005537 C09CA07 - Telmisartan Substances 0.000 claims description 4
- 229920001661 Chitosan Polymers 0.000 claims description 4
- 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
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims description 4
- 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 claims description 4
- 229930195725 Mannitol Natural products 0.000 claims description 4
- 229920001800 Shellac Polymers 0.000 claims description 4
- 229920002494 Zein Polymers 0.000 claims description 4
- 235000001465 calcium Nutrition 0.000 claims description 4
- 229960000932 candesartan Drugs 0.000 claims description 4
- 150000001720 carbohydrates Chemical class 0.000 claims description 4
- 229920001577 copolymer Polymers 0.000 claims description 4
- 229960004563 eprosartan Drugs 0.000 claims description 4
- 150000004676 glycans Chemical class 0.000 claims description 4
- 239000000017 hydrogel Substances 0.000 claims description 4
- 230000003165 hydrotropic effect Effects 0.000 claims description 4
- 239000008101 lactose Substances 0.000 claims description 4
- FPYJFEHAWHCUMM-UHFFFAOYSA-N maleic anhydride Chemical compound O=C1OC(=O)C=C1 FPYJFEHAWHCUMM-UHFFFAOYSA-N 0.000 claims description 4
- 239000000594 mannitol Substances 0.000 claims description 4
- 235000010355 mannitol Nutrition 0.000 claims description 4
- 229920000765 poly(2-oxazolines) Polymers 0.000 claims description 4
- 229920000233 poly(alkylene oxides) Polymers 0.000 claims description 4
- 229920002401 polyacrylamide Polymers 0.000 claims description 4
- 229920001444 polymaleic acid Polymers 0.000 claims description 4
- 229920001282 polysaccharide Polymers 0.000 claims description 4
- 239000005017 polysaccharide Substances 0.000 claims description 4
- 229920002635 polyurethane Polymers 0.000 claims description 4
- 239000004814 polyurethane Substances 0.000 claims description 4
- 229920002689 polyvinyl acetate Polymers 0.000 claims description 4
- HFHDHCJBZVLPGP-UHFFFAOYSA-N schardinger α-dextrin Chemical class O1C(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC(C(O)C2O)C(CO)OC2OC(C(C2O)O)C(CO)OC2OC2C(O)C(O)C1OC2CO HFHDHCJBZVLPGP-UHFFFAOYSA-N 0.000 claims description 4
- 229940113147 shellac Drugs 0.000 claims description 4
- ZLGIYFNHBLSMPS-ATJNOEHPSA-N shellac Chemical compound OCCCCCC(O)C(O)CCCCCCCC(O)=O.C1C23[C@H](C(O)=O)CCC2[C@](C)(CO)[C@@H]1C(C(O)=O)=C[C@@H]3O ZLGIYFNHBLSMPS-ATJNOEHPSA-N 0.000 claims description 4
- 239000004208 shellac Substances 0.000 claims description 4
- 235000013874 shellac Nutrition 0.000 claims description 4
- 229920003179 starch-based polymer Polymers 0.000 claims description 4
- 239000004628 starch-based polymer Substances 0.000 claims description 4
- 229920002554 vinyl polymer Polymers 0.000 claims description 4
- 239000005019 zein Substances 0.000 claims description 4
- 229940093612 zein Drugs 0.000 claims description 4
- 206010003210 Arteriosclerosis Diseases 0.000 claims description 3
- 239000002947 C09CA04 - Irbesartan Substances 0.000 claims description 3
- 208000002249 Diabetes Complications Diseases 0.000 claims description 3
- 206010012655 Diabetic complications Diseases 0.000 claims description 3
- 208000012902 Nervous system disease Diseases 0.000 claims description 3
- 239000005480 Olmesartan Substances 0.000 claims description 3
- 239000005477 Pratosartan Substances 0.000 claims description 3
- 208000011775 arteriosclerosis disease Diseases 0.000 claims description 3
- 229960002198 irbesartan Drugs 0.000 claims description 3
- 208000028867 ischemia Diseases 0.000 claims description 3
- 229960004773 losartan Drugs 0.000 claims description 3
- 208000010125 myocardial infarction Diseases 0.000 claims description 3
- VTRAEEWXHOVJFV-UHFFFAOYSA-N olmesartan Chemical compound CCCC1=NC(C(C)(C)O)=C(C(O)=O)N1CC1=CC=C(C=2C(=CC=CC=2)C=2NN=NN=2)C=C1 VTRAEEWXHOVJFV-UHFFFAOYSA-N 0.000 claims description 3
- 229960005117 olmesartan Drugs 0.000 claims description 3
- KCTFTBCZZUBAKN-UHFFFAOYSA-N pratosartan Chemical compound CCCC1=NC=2CCCCC(=O)C=2N1CC(C=C1)=CC=C1C1=CC=CC=C1C1=NN=NN1 KCTFTBCZZUBAKN-UHFFFAOYSA-N 0.000 claims description 3
- 229950005649 pratosartan Drugs 0.000 claims description 3
- 238000001694 spray drying Methods 0.000 claims description 3
- 229960005187 telmisartan Drugs 0.000 claims description 3
- 208000024827 Alzheimer disease Diseases 0.000 claims description 2
- 208000000044 Amnesia Diseases 0.000 claims description 2
- 208000031091 Amnestic disease Diseases 0.000 claims description 2
- 206010002383 Angina Pectoris Diseases 0.000 claims description 2
- 208000019901 Anxiety disease Diseases 0.000 claims description 2
- 208000020446 Cardiac disease Diseases 0.000 claims description 2
- 206010065929 Cardiovascular insufficiency Diseases 0.000 claims description 2
- 206010012289 Dementia Diseases 0.000 claims description 2
- 206010018364 Glomerulonephritis Diseases 0.000 claims description 2
- 206010020571 Hyperaldosteronism Diseases 0.000 claims description 2
- 206010053159 Organ failure Diseases 0.000 claims description 2
- 208000001647 Renal Insufficiency Diseases 0.000 claims description 2
- 208000017442 Retinal disease Diseases 0.000 claims description 2
- 206010038923 Retinopathy Diseases 0.000 claims description 2
- 208000006011 Stroke Diseases 0.000 claims description 2
- 230000006986 amnesia Effects 0.000 claims description 2
- 206010007776 catatonia Diseases 0.000 claims description 2
- 201000006549 dyspepsia Diseases 0.000 claims description 2
- 208000019622 heart disease Diseases 0.000 claims description 2
- 201000006370 kidney failure Diseases 0.000 claims description 2
- 230000002093 peripheral effect Effects 0.000 claims description 2
- 201000009395 primary hyperaldosteronism Diseases 0.000 claims description 2
- 238000000935 solvent evaporation Methods 0.000 claims description 2
- SJSNUMAYCRRIOM-QFIPXVFZSA-N valsartan Chemical compound C1=CC(CN(C(=O)CCCC)[C@@H](C(C)C)C(O)=O)=CC=C1C1=CC=CC=C1C1=NN=N[N]1 SJSNUMAYCRRIOM-QFIPXVFZSA-N 0.000 claims 18
- 241000965481 Darksidea alpha Species 0.000 claims 3
- 239000002461 renin inhibitor Substances 0.000 claims 3
- 229940086526 renin-inhibitors Drugs 0.000 claims 3
- 241000124008 Mammalia Species 0.000 claims 1
- 206010039710 Scleroderma Diseases 0.000 claims 1
- SGZAIDDFHDDFJU-UHFFFAOYSA-N candesartan Chemical compound CCOC1=NC2=CC=CC(C(O)=O)=C2N1CC(C=C1)=CC=C1C1=CC=CC=C1C1=NN=N[N]1 SGZAIDDFHDDFJU-UHFFFAOYSA-N 0.000 claims 1
- YCPOHTHPUREGFM-UHFFFAOYSA-N irbesartan Chemical compound O=C1N(CC=2C=CC(=CC=2)C=2C(=CC=CC=2)C=2[N]N=NN=2)C(CCCC)=NC21CCCC2 YCPOHTHPUREGFM-UHFFFAOYSA-N 0.000 claims 1
- KJJZZJSZUJXYEA-UHFFFAOYSA-N losartan Chemical compound CCCCC1=NC(Cl)=C(CO)N1CC1=CC=C(C=2C(=CC=CC=2)C=2[N]N=NN=2)C=C1 KJJZZJSZUJXYEA-UHFFFAOYSA-N 0.000 claims 1
- 239000003087 receptor blocking agent Substances 0.000 claims 1
- 238000009472 formulation Methods 0.000 abstract description 48
- 239000007962 solid dispersion Substances 0.000 abstract description 30
- 230000002378 acidificating effect Effects 0.000 abstract description 22
- 238000000338 in vitro Methods 0.000 abstract description 19
- 239000002552 dosage form Substances 0.000 abstract description 16
- 239000012729 immediate-release (IR) formulation Substances 0.000 abstract description 14
- 239000006104 solid solution Substances 0.000 abstract description 2
- 238000013270 controlled release Methods 0.000 abstract 1
- 239000008137 solubility enhancer Substances 0.000 abstract 1
- ACWBQPMHZXGDFX-QFIPXVFZSA-N valsartan Chemical compound C1=CC(CN(C(=O)CCCC)[C@@H](C(C)C)C(O)=O)=CC=C1C1=CC=CC=C1C1=NN=NN1 ACWBQPMHZXGDFX-QFIPXVFZSA-N 0.000 description 107
- 229940125364 angiotensin receptor blocker Drugs 0.000 description 59
- 241001553178 Arachis glabrata Species 0.000 description 41
- 239000003814 drug Substances 0.000 description 26
- 229940079593 drug Drugs 0.000 description 23
- 239000002333 angiotensin II receptor antagonist Substances 0.000 description 18
- HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 18
- 239000000194 fatty acid Substances 0.000 description 17
- 239000003826 tablet Substances 0.000 description 17
- 235000014113 dietary fatty acids Nutrition 0.000 description 16
- 229930195729 fatty acid Natural products 0.000 description 16
- 239000000546 pharmaceutical excipient Substances 0.000 description 14
- GHOSNRCGJFBJIB-UHFFFAOYSA-N Candesartan cilexetil Chemical compound C=12N(CC=3C=CC(=CC=3)C=3C(=CC=CC=3)C3=NNN=N3)C(OCC)=NC2=CC=CC=1C(=O)OC(C)OC(=O)OC1CCCCC1 GHOSNRCGJFBJIB-UHFFFAOYSA-N 0.000 description 12
- 238000005070 sampling Methods 0.000 description 12
- 229920003084 Avicel® PH-102 Polymers 0.000 description 11
- 229940074619 diovan Drugs 0.000 description 11
- 229960000573 eprosartan mesylate Drugs 0.000 description 11
- 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 description 11
- 229920001983 poloxamer Polymers 0.000 description 11
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerine Chemical compound OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 description 9
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 description 9
- 239000002253 acid Substances 0.000 description 9
- 239000012738 dissolution medium Substances 0.000 description 9
- 235000019359 magnesium stearate Nutrition 0.000 description 9
- 230000008569 process Effects 0.000 description 9
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 description 8
- DNIAPMSPPWPWGF-UHFFFAOYSA-N Propylene glycol Chemical compound CC(O)CO DNIAPMSPPWPWGF-UHFFFAOYSA-N 0.000 description 8
- AOBORMOPSGHCAX-UHFFFAOYSA-N Tocophersolan Chemical compound OCCOC(=O)CCC(=O)OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C AOBORMOPSGHCAX-UHFFFAOYSA-N 0.000 description 8
- 229960000913 crospovidone Drugs 0.000 description 8
- 239000006185 dispersion Substances 0.000 description 8
- 235000013809 polyvinylpolypyrrolidone Nutrition 0.000 description 8
- 239000000047 product Substances 0.000 description 8
- 239000007787 solid Substances 0.000 description 8
- 229920002690 Polyoxyl 40 HydrogenatedCastorOil Polymers 0.000 description 7
- 239000008280 blood Substances 0.000 description 7
- 210000004369 blood Anatomy 0.000 description 7
- 239000000872 buffer Substances 0.000 description 7
- 230000002496 gastric effect Effects 0.000 description 7
- 239000004615 ingredient Substances 0.000 description 7
- 239000008194 pharmaceutical composition Substances 0.000 description 7
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 7
- GVJHHUAWPYXKBD-UHFFFAOYSA-N (±)-α-Tocopherol Chemical compound OC1=C(C)C(C)=C2OC(CCCC(C)CCCC(C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-UHFFFAOYSA-N 0.000 description 6
- 239000004480 active ingredient Substances 0.000 description 6
- 229960004349 candesartan cilexetil Drugs 0.000 description 6
- 238000007922 dissolution test Methods 0.000 description 6
- 229920000191 poly(N-vinyl pyrrolidone) Polymers 0.000 description 6
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 6
- 239000007909 solid dosage form Substances 0.000 description 6
- 238000005063 solubilization Methods 0.000 description 6
- 230000007928 solubilization Effects 0.000 description 6
- 229910002016 Aerosil® 200 Inorganic materials 0.000 description 5
- RVGRUAULSDPKGF-UHFFFAOYSA-N Poloxamer Chemical compound C1CO1.CC1CO1 RVGRUAULSDPKGF-UHFFFAOYSA-N 0.000 description 5
- 229930182558 Sterol Chemical class 0.000 description 5
- 239000008187 granular material Substances 0.000 description 5
- 229960002003 hydrochlorothiazide Drugs 0.000 description 5
- 229940071676 hydroxypropylcellulose Drugs 0.000 description 5
- 239000007788 liquid Substances 0.000 description 5
- 230000036470 plasma concentration Effects 0.000 description 5
- 229920001992 poloxamer 407 Polymers 0.000 description 5
- 229940044476 poloxamer 407 Drugs 0.000 description 5
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 5
- 150000003432 sterols Chemical class 0.000 description 5
- 235000003702 sterols Nutrition 0.000 description 5
- 239000007916 tablet composition Substances 0.000 description 5
- JVKUCNQGESRUCL-UHFFFAOYSA-N 2-Hydroxyethyl 12-hydroxyoctadecanoate Chemical compound CCCCCCC(O)CCCCCCCCCCC(=O)OCCO JVKUCNQGESRUCL-UHFFFAOYSA-N 0.000 description 4
- 229920001304 Solutol HS 15 Polymers 0.000 description 4
- 239000008186 active pharmaceutical agent Substances 0.000 description 4
- 239000011248 coating agent Substances 0.000 description 4
- 238000000576 coating method Methods 0.000 description 4
- 229940075614 colloidal silicon dioxide Drugs 0.000 description 4
- 239000007884 disintegrant Substances 0.000 description 4
- 238000010348 incorporation Methods 0.000 description 4
- 238000012360 testing method Methods 0.000 description 4
- 230000001225 therapeutic effect Effects 0.000 description 4
- 102100033350 ATP-dependent translocase ABCB1 Human genes 0.000 description 3
- 102000005862 Angiotensin II Human genes 0.000 description 3
- 101800000733 Angiotensin-2 Proteins 0.000 description 3
- LYCAIKOWRPUZTN-UHFFFAOYSA-N Ethylene glycol Chemical compound OCCO LYCAIKOWRPUZTN-UHFFFAOYSA-N 0.000 description 3
- 206010019280 Heart failures Diseases 0.000 description 3
- SHBUUTHKGIVMJT-UHFFFAOYSA-N Hydroxystearate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OO SHBUUTHKGIVMJT-UHFFFAOYSA-N 0.000 description 3
- 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 3
- KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 description 3
- 108010047230 Member 1 Subfamily B ATP Binding Cassette Transporter Proteins 0.000 description 3
- 229920002675 Polyoxyl Polymers 0.000 description 3
- 229930003427 Vitamin E Natural products 0.000 description 3
- 230000009471 action Effects 0.000 description 3
- 150000001413 amino acids Chemical class 0.000 description 3
- 229950006323 angiotensin ii Drugs 0.000 description 3
- 125000002843 carboxylic acid group Chemical group 0.000 description 3
- 230000000052 comparative effect Effects 0.000 description 3
- 150000004665 fatty acids Chemical class 0.000 description 3
- WIGCFUFOHFEKBI-UHFFFAOYSA-N gamma-tocopherol Natural products CC(C)CCCC(C)CCCC(C)CCCC1CCC2C(C)C(O)C(C)C(C)C2O1 WIGCFUFOHFEKBI-UHFFFAOYSA-N 0.000 description 3
- 229920001477 hydrophilic polymer Polymers 0.000 description 3
- 230000002209 hydrophobic effect Effects 0.000 description 3
- 229940072106 hydroxystearate Drugs 0.000 description 3
- 239000003112 inhibitor Substances 0.000 description 3
- YOSHYTLCDANDAN-UHFFFAOYSA-N irbesartan Chemical compound O=C1N(CC=2C=CC(=CC=2)C=2C(=CC=CC=2)C=2NN=NN=2)C(CCCC)=NC21CCCC2 YOSHYTLCDANDAN-UHFFFAOYSA-N 0.000 description 3
- PSIFNNKUMBGKDQ-UHFFFAOYSA-N losartan Chemical compound CCCCC1=NC(Cl)=C(CO)N1CC1=CC=C(C=2C(=CC=CC=2)C=2NN=NN=2)C=C1 PSIFNNKUMBGKDQ-UHFFFAOYSA-N 0.000 description 3
- 239000002609 medium Substances 0.000 description 3
- GHBFNMLVSPCDGN-UHFFFAOYSA-N rac-1-monooctanoylglycerol Chemical compound CCCCCCCC(=O)OCC(O)CO GHBFNMLVSPCDGN-UHFFFAOYSA-N 0.000 description 3
- 239000000126 substance Substances 0.000 description 3
- 235000000346 sugar Nutrition 0.000 description 3
- 235000019165 vitamin E Nutrition 0.000 description 3
- 239000011709 vitamin E Substances 0.000 description 3
- 229940046009 vitamin E Drugs 0.000 description 3
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 3
- VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 2
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.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 WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 description 2
- 108090000746 Chymosin Proteins 0.000 description 2
- 108010038807 Oligopeptides Chemical class 0.000 description 2
- 102000015636 Oligopeptides Human genes 0.000 description 2
- 229920001213 Polysorbate 20 Polymers 0.000 description 2
- 235000004443 Ricinus communis Nutrition 0.000 description 2
- 239000013543 active substance Substances 0.000 description 2
- 125000000129 anionic group Chemical group 0.000 description 2
- 235000011175 beta-cyclodextrine Nutrition 0.000 description 2
- 230000036772 blood pressure Effects 0.000 description 2
- 210000004204 blood vessel Anatomy 0.000 description 2
- 229960003340 calcium silicate Drugs 0.000 description 2
- 235000012241 calcium silicate Nutrition 0.000 description 2
- 125000002091 cationic group Chemical group 0.000 description 2
- 210000000170 cell membrane Anatomy 0.000 description 2
- 238000010668 complexation reaction Methods 0.000 description 2
- 238000007906 compression Methods 0.000 description 2
- 230000006835 compression Effects 0.000 description 2
- 238000007796 conventional method Methods 0.000 description 2
- 229920001531 copovidone Polymers 0.000 description 2
- 239000002285 corn oil Substances 0.000 description 2
- 235000005687 corn oil Nutrition 0.000 description 2
- 239000006184 cosolvent Substances 0.000 description 2
- 206010012601 diabetes mellitus Diseases 0.000 description 2
- 238000012377 drug delivery Methods 0.000 description 2
- 239000007903 gelatin capsule Substances 0.000 description 2
- 235000021472 generally recognized as safe Nutrition 0.000 description 2
- RZRNAYUHWVFMIP-HXUWFJFHSA-N glycerol monolinoleate Natural products CCCCCCCCC=CCCCCCCCC(=O)OC[C@H](O)CO RZRNAYUHWVFMIP-HXUWFJFHSA-N 0.000 description 2
- 239000008172 hydrogenated vegetable oil Substances 0.000 description 2
- 229960001021 lactose monohydrate Drugs 0.000 description 2
- 239000000787 lecithin Chemical class 0.000 description 2
- 235000010445 lecithin Nutrition 0.000 description 2
- 239000011777 magnesium Substances 0.000 description 2
- 238000004519 manufacturing process Methods 0.000 description 2
- 238000012986 modification Methods 0.000 description 2
- 230000004048 modification Effects 0.000 description 2
- 230000007935 neutral effect Effects 0.000 description 2
- 239000006186 oral dosage form Substances 0.000 description 2
- 239000012466 permeate Substances 0.000 description 2
- 239000008177 pharmaceutical agent Substances 0.000 description 2
- 239000008363 phosphate buffer Substances 0.000 description 2
- 239000006069 physical mixture Substances 0.000 description 2
- 235000010486 polyoxyethylene sorbitan monolaurate Nutrition 0.000 description 2
- 239000000256 polyoxyethylene sorbitan monolaurate Substances 0.000 description 2
- 229920001184 polypeptide Chemical class 0.000 description 2
- 238000002360 preparation method Methods 0.000 description 2
- 108090000765 processed proteins & peptides Chemical class 0.000 description 2
- 102000004196 processed proteins & peptides Human genes 0.000 description 2
- 230000009467 reduction Effects 0.000 description 2
- APSBXTVYXVQYAB-UHFFFAOYSA-M sodium docusate Chemical class [Na+].CCCCC(CC)COC(=O)CC(S([O-])(=O)=O)C(=O)OCC(CC)CCCC APSBXTVYXVQYAB-UHFFFAOYSA-M 0.000 description 2
- 229920003109 sodium starch glycolate Polymers 0.000 description 2
- 239000008109 sodium starch glycolate Substances 0.000 description 2
- 229940079832 sodium starch glycolate Drugs 0.000 description 2
- 239000000243 solution Substances 0.000 description 2
- 229940032147 starch Drugs 0.000 description 2
- 210000002784 stomach Anatomy 0.000 description 2
- 239000007939 sustained release tablet Substances 0.000 description 2
- 229940124597 therapeutic agent Drugs 0.000 description 2
- 238000005809 transesterification reaction Methods 0.000 description 2
- NWUYHJFMYQTDRP-UHFFFAOYSA-N 1,2-bis(ethenyl)benzene;1-ethenyl-2-ethylbenzene;styrene Chemical compound C=CC1=CC=CC=C1.CCC1=CC=CC=C1C=C.C=CC1=CC=CC=C1C=C NWUYHJFMYQTDRP-UHFFFAOYSA-N 0.000 description 1
- WECGLUPZRHILCT-GSNKCQISSA-N 1-linoleoyl-sn-glycerol Chemical compound CCCCC\C=C/C\C=C/CCCCCCCC(=O)OC[C@@H](O)CO WECGLUPZRHILCT-GSNKCQISSA-N 0.000 description 1
- OVYMWJFNQQOJBU-UHFFFAOYSA-N 1-octanoyloxypropan-2-yl octanoate Chemical compound CCCCCCCC(=O)OCC(C)OC(=O)CCCCCCC OVYMWJFNQQOJBU-UHFFFAOYSA-N 0.000 description 1
- RZRNAYUHWVFMIP-KTKRTIGZSA-N 1-oleoylglycerol Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OCC(O)CO RZRNAYUHWVFMIP-KTKRTIGZSA-N 0.000 description 1
- 239000000263 2,3-dihydroxypropyl (Z)-octadec-9-enoate Substances 0.000 description 1
- OIQOAYVCKAHSEJ-UHFFFAOYSA-N 2-[2,3-bis(2-hydroxyethoxy)propoxy]ethanol;hexadecanoic acid;octadecanoic acid Chemical compound OCCOCC(OCCO)COCCO.CCCCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCCCCCC(O)=O OIQOAYVCKAHSEJ-UHFFFAOYSA-N 0.000 description 1
- GHHURQMJLARIDK-UHFFFAOYSA-N 2-hydroxypropyl octanoate Chemical compound CCCCCCCC(=O)OCC(C)O GHHURQMJLARIDK-UHFFFAOYSA-N 0.000 description 1
- RZRNAYUHWVFMIP-GDCKJWNLSA-N 3-oleoyl-sn-glycerol Chemical compound CCCCCCCC\C=C/CCCCCCCC(=O)OC[C@H](O)CO RZRNAYUHWVFMIP-GDCKJWNLSA-N 0.000 description 1
- QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 1
- 235000019489 Almond oil Nutrition 0.000 description 1
- 229920001450 Alpha-Cyclodextrin Polymers 0.000 description 1
- 244000144725 Amygdalus communis Species 0.000 description 1
- 235000011437 Amygdalus communis Nutrition 0.000 description 1
- 235000017060 Arachis glabrata Nutrition 0.000 description 1
- 244000105624 Arachis hypogaea Species 0.000 description 1
- 235000010777 Arachis hypogaea Nutrition 0.000 description 1
- 235000018262 Arachis monticola Nutrition 0.000 description 1
- 229940127291 Calcium channel antagonist Drugs 0.000 description 1
- 206010007559 Cardiac failure congestive 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
- 235000019739 Dicalciumphosphate Nutrition 0.000 description 1
- 239000001116 FEMA 4028 Substances 0.000 description 1
- 101000830701 Homo sapiens Tubulin polyglutamylase complex subunit 1 Proteins 0.000 description 1
- 229920003091 Methocel™ Polymers 0.000 description 1
- UQGKUQLKSCSZGY-UHFFFAOYSA-N Olmesartan medoxomil Chemical compound C=1C=C(C=2C(=CC=CC=2)C2=NNN=N2)C=CC=1CN1C(CCC)=NC(C(C)(C)O)=C1C(=O)OCC=1OC(=O)OC=1C UQGKUQLKSCSZGY-UHFFFAOYSA-N 0.000 description 1
- 239000008118 PEG 6000 Substances 0.000 description 1
- 235000019483 Peanut oil Nutrition 0.000 description 1
- 229920002584 Polyethylene Glycol 6000 Polymers 0.000 description 1
- HDSBZMRLPLPFLQ-UHFFFAOYSA-N Propylene glycol alginate Chemical compound OC1C(O)C(OC)OC(C(O)=O)C1OC1C(O)C(O)C(C)C(C(=O)OCC(C)O)O1 HDSBZMRLPLPFLQ-UHFFFAOYSA-N 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- 229930006000 Sucrose Natural products 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
- 102100024600 Tubulin polyglutamylase complex subunit 1 Human genes 0.000 description 1
- 206010047139 Vasoconstriction Diseases 0.000 description 1
- FOLJTMYCYXSPFQ-CJKAUBRRSA-N [(2r,3s,4s,5r,6r)-6-[(2s,3s,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)-2-(octadecanoyloxymethyl)oxolan-2-yl]oxy-3,4,5-trihydroxyoxan-2-yl]methyl octadecanoate Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](COC(=O)CCCCCCCCCCCCCCCCC)O[C@@H]1O[C@@]1(COC(=O)CCCCCCCCCCCCCCCCC)[C@@H](O)[C@H](O)[C@@H](CO)O1 FOLJTMYCYXSPFQ-CJKAUBRRSA-N 0.000 description 1
- 239000008351 acetate buffer Substances 0.000 description 1
- 125000002252 acyl group Chemical class 0.000 description 1
- 239000000654 additive Substances 0.000 description 1
- 230000001476 alcoholic effect Effects 0.000 description 1
- 150000001298 alcohols Chemical class 0.000 description 1
- 125000005210 alkyl ammonium group Chemical group 0.000 description 1
- 150000005215 alkyl ethers Chemical class 0.000 description 1
- 150000008051 alkyl sulfates Chemical class 0.000 description 1
- 235000020224 almond Nutrition 0.000 description 1
- 239000008168 almond oil Substances 0.000 description 1
- HFHDHCJBZVLPGP-RWMJIURBSA-N alpha-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO HFHDHCJBZVLPGP-RWMJIURBSA-N 0.000 description 1
- 229940043377 alpha-cyclodextrin Drugs 0.000 description 1
- 229940053200 antiepileptics fatty acid derivative Drugs 0.000 description 1
- 238000003556 assay Methods 0.000 description 1
- 229940058087 atacand Drugs 0.000 description 1
- 229940000201 avapro Drugs 0.000 description 1
- 238000000498 ball milling Methods 0.000 description 1
- 229940055053 benicar Drugs 0.000 description 1
- WHGYBXFWUBPSRW-FOUAGVGXSA-N beta-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO WHGYBXFWUBPSRW-FOUAGVGXSA-N 0.000 description 1
- 229960004853 betadex Drugs 0.000 description 1
- 230000015572 biosynthetic process Effects 0.000 description 1
- 239000000480 calcium channel blocker Substances 0.000 description 1
- 239000001506 calcium phosphate Substances 0.000 description 1
- 239000007963 capsule composition Substances 0.000 description 1
- LDVVMCZRFWMZSG-UHFFFAOYSA-N captan Chemical compound C1C=CCC2C(=O)N(SC(Cl)(Cl)Cl)C(=O)C21 LDVVMCZRFWMZSG-UHFFFAOYSA-N 0.000 description 1
- 150000001732 carboxylic acid derivatives Chemical group 0.000 description 1
- 229960004203 carnitine Drugs 0.000 description 1
- 239000007795 chemical reaction product Substances 0.000 description 1
- 230000001684 chronic effect Effects 0.000 description 1
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical class OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 1
- 238000005056 compaction Methods 0.000 description 1
- 239000000599 controlled substance Substances 0.000 description 1
- 238000001816 cooling Methods 0.000 description 1
- 229940097499 cozaar Drugs 0.000 description 1
- 230000001186 cumulative effect Effects 0.000 description 1
- 150000003950 cyclic amides Chemical class 0.000 description 1
- 229940097362 cyclodextrins Drugs 0.000 description 1
- GHVNFZFCNZKVNT-UHFFFAOYSA-M decanoate Chemical compound CCCCCCCCCC([O-])=O GHVNFZFCNZKVNT-UHFFFAOYSA-M 0.000 description 1
- KXGVEGMKQFWNSR-LLQZFEROSA-N deoxycholic acid Chemical compound C([C@H]1CC2)[C@H](O)CC[C@]1(C)[C@@H]1[C@@H]2[C@@H]2CC[C@H]([C@@H](CCC(O)=O)C)[C@@]2(C)[C@@H](O)C1 KXGVEGMKQFWNSR-LLQZFEROSA-N 0.000 description 1
- 229960003964 deoxycholic acid Drugs 0.000 description 1
- 230000001419 dependent effect Effects 0.000 description 1
- 238000011161 development Methods 0.000 description 1
- NEFBYIFKOOEVPA-UHFFFAOYSA-K dicalcium phosphate Chemical compound [Ca+2].[Ca+2].[O-]P([O-])([O-])=O NEFBYIFKOOEVPA-UHFFFAOYSA-K 0.000 description 1
- 229940038472 dicalcium phosphate Drugs 0.000 description 1
- 229910000390 dicalcium phosphate Inorganic materials 0.000 description 1
- MTHSVFCYNBDYFN-UHFFFAOYSA-N diethylene glycol Chemical compound OCCOCCO MTHSVFCYNBDYFN-UHFFFAOYSA-N 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 238000007907 direct compression Methods 0.000 description 1
- 238000011978 dissolution method Methods 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 229940088679 drug related substance Drugs 0.000 description 1
- 238000007908 dry granulation Methods 0.000 description 1
- 239000008157 edible vegetable oil Substances 0.000 description 1
- 230000000694 effects Effects 0.000 description 1
- 150000002170 ethers Chemical class 0.000 description 1
- 238000001125 extrusion Methods 0.000 description 1
- 235000020937 fasting conditions Nutrition 0.000 description 1
- 150000002191 fatty alcohols Chemical class 0.000 description 1
- IECPWNUMDGFDKC-MZJAQBGESA-N fusidic acid Chemical class O[C@@H]([C@@H]12)C[C@H]3\C(=C(/CCC=C(C)C)C(O)=O)[C@@H](OC(C)=O)C[C@]3(C)[C@@]2(C)CC[C@@H]2[C@]1(C)CC[C@@H](O)[C@H]2C IECPWNUMDGFDKC-MZJAQBGESA-N 0.000 description 1
- GDSRMADSINPKSL-HSEONFRVSA-N gamma-cyclodextrin Chemical compound OC[C@H]([C@H]([C@@H]([C@H]1O)O)O[C@H]2O[C@@H]([C@@H](O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O[C@H]3O[C@H](CO)[C@H]([C@@H]([C@H]3O)O)O3)[C@H](O)[C@H]2O)CO)O[C@@H]1O[C@H]1[C@H](O)[C@@H](O)[C@@H]3O[C@@H]1CO GDSRMADSINPKSL-HSEONFRVSA-N 0.000 description 1
- 229940080345 gamma-cyclodextrin Drugs 0.000 description 1
- 125000002791 glucosyl group Chemical group C1([C@H](O)[C@@H](O)[C@H](O)[C@H](O1)CO)* 0.000 description 1
- YQEMORVAKMFKLG-UHFFFAOYSA-N glycerine monostearate Natural products CCCCCCCCCCCCCCCCCC(=O)OC(CO)CO YQEMORVAKMFKLG-UHFFFAOYSA-N 0.000 description 1
- SVUQHVRAGMNPLW-UHFFFAOYSA-N glycerol monostearate Natural products CCCCCCCCCCCCCCCCC(=O)OCC(O)CO SVUQHVRAGMNPLW-UHFFFAOYSA-N 0.000 description 1
- 229940075529 glyceryl stearate Drugs 0.000 description 1
- 238000005469 granulation Methods 0.000 description 1
- 230000003179 granulation Effects 0.000 description 1
- 239000012943 hotmelt Substances 0.000 description 1
- 150000004677 hydrates Chemical class 0.000 description 1
- 239000012728 immediate-release (IR) tablet Substances 0.000 description 1
- 230000006872 improvement Effects 0.000 description 1
- 238000001727 in vivo Methods 0.000 description 1
- 239000003456 ion exchange resin Substances 0.000 description 1
- 229920003303 ion-exchange polymer Polymers 0.000 description 1
- 239000002563 ionic surfactant Substances 0.000 description 1
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical class CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 1
- 229960001375 lactose Drugs 0.000 description 1
- 125000003473 lipid group Chemical group 0.000 description 1
- 238000005461 lubrication Methods 0.000 description 1
- 238000012792 lyophilization process Methods 0.000 description 1
- 230000014759 maintenance of location Effects 0.000 description 1
- 229960001855 mannitol Drugs 0.000 description 1
- 230000001404 mediated effect Effects 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 229940101564 micardis Drugs 0.000 description 1
- RZRNAYUHWVFMIP-UHFFFAOYSA-N monoelaidin Natural products CCCCCCCCC=CCCCCCCCC(=O)OCC(O)CO RZRNAYUHWVFMIP-UHFFFAOYSA-N 0.000 description 1
- 210000003205 muscle Anatomy 0.000 description 1
- 239000002736 nonionic surfactant Substances 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
- 239000003921 oil Substances 0.000 description 1
- 235000019198 oils Nutrition 0.000 description 1
- 229940049964 oleate Drugs 0.000 description 1
- 239000004006 olive oil Substances 0.000 description 1
- 235000008390 olive oil Nutrition 0.000 description 1
- 239000008184 oral solid dosage form Substances 0.000 description 1
- 239000003002 pH adjusting agent Substances 0.000 description 1
- 239000003346 palm kernel oil Substances 0.000 description 1
- 235000019865 palm kernel oil Nutrition 0.000 description 1
- 235000020232 peanut Nutrition 0.000 description 1
- 239000000312 peanut oil Substances 0.000 description 1
- WXZMFSXDPGVJKK-UHFFFAOYSA-N pentaerythritol Chemical compound OCC(CO)(CO)CO WXZMFSXDPGVJKK-UHFFFAOYSA-N 0.000 description 1
- 230000035699 permeability Effects 0.000 description 1
- 150000003904 phospholipids Chemical class 0.000 description 1
- 229940093429 polyethylene glycol 6000 Drugs 0.000 description 1
- 229920000193 polymethacrylate Polymers 0.000 description 1
- 229920005606 polypropylene copolymer Polymers 0.000 description 1
- 235000019422 polyvinyl alcohol Nutrition 0.000 description 1
- 229920000523 polyvinylpolypyrrolidone Polymers 0.000 description 1
- 230000003389 potentiating effect Effects 0.000 description 1
- 229940069328 povidone Drugs 0.000 description 1
- 239000000843 powder Substances 0.000 description 1
- 238000012545 processing Methods 0.000 description 1
- 235000010409 propane-1,2-diol alginate Nutrition 0.000 description 1
- 239000000770 propane-1,2-diol alginate Substances 0.000 description 1
- 239000008213 purified water Substances 0.000 description 1
- 230000002441 reversible effect Effects 0.000 description 1
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical class OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 1
- 239000008299 semisolid dosage form Substances 0.000 description 1
- 238000007613 slurry method Methods 0.000 description 1
- 210000000813 small intestine Anatomy 0.000 description 1
- OABYVIYXWMZFFJ-ZUHYDKSRSA-M sodium glycocholate 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)NCC([O-])=O)C)[C@@]2(C)[C@@H](O)C1 OABYVIYXWMZFFJ-ZUHYDKSRSA-M 0.000 description 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 description 1
- 239000012453 solvate Substances 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 230000000087 stabilizing effect Effects 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000000758 substrate Substances 0.000 description 1
- 239000005720 sucrose Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 208000019270 symptomatic heart failure Diseases 0.000 description 1
- 238000003786 synthesis reaction Methods 0.000 description 1
- 150000003899 tartaric acid esters Chemical class 0.000 description 1
- 229940078806 teveten Drugs 0.000 description 1
- 239000003451 thiazide diuretic agent Substances 0.000 description 1
- 150000003626 triacylglycerols Chemical class 0.000 description 1
- 239000010913 used oil Substances 0.000 description 1
- 230000025033 vasoconstriction Effects 0.000 description 1
- 235000015112 vegetable and seed oil Nutrition 0.000 description 1
- 239000008158 vegetable oil Substances 0.000 description 1
- 229940088594 vitamin Drugs 0.000 description 1
- 229930003231 vitamin Natural products 0.000 description 1
- 235000013343 vitamin Nutrition 0.000 description 1
- 239000011782 vitamin Substances 0.000 description 1
- 150000003722 vitamin derivatives Chemical class 0.000 description 1
- 238000005550 wet granulation Methods 0.000 description 1
- 239000002888 zwitterionic surfactant Substances 0.000 description 1
- GVJHHUAWPYXKBD-IEOSBIPESA-N α-tocopherol Chemical compound OC1=C(C)C(C)=C2O[C@@](CCC[C@H](C)CCC[C@H](C)CCCC(C)C)(C)CCC2=C1C GVJHHUAWPYXKBD-IEOSBIPESA-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
- A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
- A61K31/35—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom
- A61K31/352—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having six-membered rings with one oxygen as the only ring hetero atom condensed with carbocyclic rings, e.g. methantheline
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- 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
-
- 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
- A61K9/145—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 compounds
-
- 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
- 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
- A61K9/20—Pills, tablets, discs, rods
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2072—Pills, tablets, discs, rods characterised by shape, structure or size; Tablets with holes, special break lines or identification marks; Partially coated tablets; Disintegrating flat shaped forms
- A61K9/2077—Tablets comprising drug-containing microparticles in a substantial amount of supporting matrix; Multiparticulate tablets
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
-
- 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
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4866—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
- A61P17/00—Drugs for dermatological disorders
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/22—Anxiolytics
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/24—Antidepressants
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system 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
-
- 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
- A61P9/04—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)
- Life Sciences & Earth Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Urology & Nephrology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Dermatology (AREA)
- Pain & Pain Management (AREA)
- Inorganic Chemistry (AREA)
- Vascular Medicine (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| IN477MU2005 | 2005-04-18 | ||
| IN477/MUM/2005 | 2005-04-18 | ||
| IN0315/MUM/2006 | 2006-03-06 | ||
| IN315MU2006 | 2006-03-06 | ||
| PCT/US2006/014422 WO2006113631A2 (fr) | 2005-04-18 | 2006-04-18 | Compositions ameliorees biologiquement |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2605183A1 true CA2605183A1 (fr) | 2006-10-26 |
Family
ID=37115820
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002605183A Abandoned CA2605183A1 (fr) | 2005-04-18 | 2006-04-18 | Compositions ameliorees biologiquement |
Country Status (8)
| Country | Link |
|---|---|
| EP (1) | EP1877042A4 (fr) |
| JP (1) | JP2008536929A (fr) |
| KR (1) | KR20080042039A (fr) |
| AU (1) | AU2006236497A1 (fr) |
| CA (1) | CA2605183A1 (fr) |
| IL (1) | IL186721A0 (fr) |
| MX (1) | MX2007012947A (fr) |
| WO (1) | WO2006113631A2 (fr) |
Families Citing this family (32)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090123543A1 (en) * | 2006-01-02 | 2009-05-14 | Rubicon Research Private Limited | Pharmaceutical compositions |
| AU2007293727A1 (en) * | 2006-09-05 | 2008-03-13 | Astrazeneca Ab | Pharmaceutical composition comprising candesartan cilexetil |
| AU2007312233B2 (en) * | 2006-10-20 | 2012-09-20 | Abbvie B.V. | Micellar nanoparticles of chemical substances |
| US7923026B2 (en) | 2006-10-20 | 2011-04-12 | Solvay Pharmaceuticals B.V. | Embedded micellar nanoparticles |
| WO2008064338A2 (fr) * | 2006-11-22 | 2008-05-29 | Rubicon Research Pvt. Ltd. | Formulation de valsartan pour administration pulsatile |
| WO2008065097A2 (fr) * | 2006-11-28 | 2008-06-05 | Laboratorios Liconsa, S.A. | Composition pharmaceutique solide stabilisee de candesartan cilexetil |
| PE20081443A1 (es) * | 2006-12-05 | 2008-12-23 | Novartis Ag | Formas de dosificacion en microemulsion de valsartan, y metodos para elaborarlas |
| US20080152717A1 (en) * | 2006-12-14 | 2008-06-26 | Isp Investments, Inc. | Amorphous valsartan and the production thereof |
| WO2008084504A2 (fr) * | 2007-01-12 | 2008-07-17 | Rubicon Research Private Limited | Composition pharmaceutique d'inhibiteurs du récepteur de l'angiotensine ii |
| CA2685261A1 (fr) * | 2007-04-25 | 2008-11-06 | Teva Pharmaceutical Industries Ltd. | Complexe d'excipient pharmaceutique |
| EP2167047A2 (fr) * | 2007-06-06 | 2010-03-31 | Dexcel Ltd. | Procédé de formation de formes posologiques orales solides dans des antagonistes du récepteur de l'angiotensine ii |
| JP2010535212A (ja) * | 2007-08-01 | 2010-11-18 | テバ ファーマシューティカル インダストリーズ リミティド | 改良されたカンデサルタンの製剤 |
| CA2701695A1 (fr) * | 2007-10-09 | 2009-04-16 | Novartis Ag | Formulation pharmaceutique de valsartan |
| KR20100090689A (ko) * | 2007-10-19 | 2010-08-16 | 애보트 게엠베하 운트 콤파니 카게 | Ｎ―아릴 우레아계 화합물을 함유하는 고체 분산액 생성물 |
| JP5222550B2 (ja) * | 2007-12-27 | 2013-06-26 | 財團法人工業技術研究院 | 徐放性組成物およびその製造方法 |
| WO2009084040A1 (fr) * | 2007-12-28 | 2009-07-09 | Rubicon Research Private Limited | Formule d'antagonistes des récepteurs de l'angiotensine administrée une fois par jour |
| US20110028526A1 (en) * | 2008-02-28 | 2011-02-03 | Amol Matharu | Valsartan solid oral dosage forms and methods of making such formulations |
| CN102046154A (zh) * | 2008-06-03 | 2011-05-04 | 诺瓦提斯公司 | 缬沙坦的脉冲释放 |
| ATE533474T1 (de) | 2008-09-17 | 2011-12-15 | Helm Ag | Durch nassgranulation hergestellte stabile und fertig gelöste zusammensetzungen aus candesartan- cilexetil |
| DE102008047910A1 (de) | 2008-09-19 | 2010-03-25 | Molkerei Meggle Wasserburg Gmbh & Co. Kg | Tablettierhilfsstoff auf Laktose- und Cellulosebasis |
| EP2446879B1 (fr) * | 2009-06-25 | 2014-02-12 | Jin Yang Pharm. Co., Ltd. | Composition pharmaceutique contenant du carboxy-losartan et son procede de production |
| WO2011028016A2 (fr) * | 2009-09-04 | 2011-03-10 | 한올바이오파마주식회사 | Préparation pharmaceutique comprenant des agents bêtabloquants et des agents bloquants du récepteur de l'angiotensine ii |
| EP2812074B1 (fr) * | 2012-02-08 | 2023-05-10 | Supernus Pharmaceuticals, Inc. | Formulations de liberation modifiée du viloxazine |
| WO2014088123A1 (fr) | 2012-12-05 | 2014-06-12 | Sawai Pharmaceutical Co., Ltd. | Préparation contenant du candésartan cilexétil |
| JP6379043B2 (ja) | 2013-01-30 | 2018-08-22 | 沢井製薬株式会社 | カンデサルタンシレキセチル含有医薬組成物 |
| WO2016005994A2 (fr) * | 2014-07-06 | 2016-01-14 | Gattefosse India Pvt. Ltd. | Composition pharmaceutique comprenant une dispersion solide de médicaments de classe ii bcs avec gelucires |
| US9675585B1 (en) | 2016-03-24 | 2017-06-13 | Ezra Pharma | Extended release pharmaceutical formulations |
| US9687475B1 (en) | 2016-03-24 | 2017-06-27 | Ezra Pharma Llc | Extended release pharmaceutical formulations with controlled impurity levels |
| KR20200062270A (ko) | 2017-10-04 | 2020-06-03 | 셀진 코포레이션 | 시스-4-[2-｛[(3s,4r)-3-플루오로옥산-4-일]아미노｝-8-(2,4,6-트리클로로아닐리노)-9h-퓨린-9-일]-1-메틸시클로헥산-1-카르복스아미드의 조성물 및 이용 방법 |
| CN109350609A (zh) * | 2018-11-14 | 2019-02-19 | 常州大学 | 一种壳聚糖包裹玉米醇溶蛋白纳米粒的制备及负载金合欢素钠盐的应用 |
| CN113933472B (zh) * | 2020-06-29 | 2024-07-09 | 武汉武药科技有限公司 | 测定替米沙坦固体制剂溶出度的溶出介质及其应用 |
| CN112516105A (zh) * | 2020-12-10 | 2021-03-19 | 成都恒瑞制药有限公司 | 一种氯沙坦钾口服制剂及其制备方法 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6248363B1 (en) * | 1999-11-23 | 2001-06-19 | Lipocine, Inc. | Solid carriers for improved delivery of active ingredients in pharmaceutical compositions |
| US20030236236A1 (en) * | 1999-06-30 | 2003-12-25 | Feng-Jing Chen | Pharmaceutical compositions and dosage forms for administration of hydrophobic drugs |
| US20030180352A1 (en) * | 1999-11-23 | 2003-09-25 | Patel Mahesh V. | Solid carriers for improved delivery of active ingredients in pharmaceutical compositions |
| US20030152622A1 (en) * | 2001-10-25 | 2003-08-14 | Jenny Louie-Helm | Formulation of an erodible, gastric retentive oral diuretic |
| JP3751287B2 (ja) * | 2002-03-27 | 2006-03-01 | バイエル薬品株式会社 | 小型化されたニフェジピン有核錠剤 |
| CN1726030A (zh) * | 2002-12-18 | 2006-01-25 | 诺瓦提斯公司 | 缬沙坦与cox－2抑制剂的组合 |
| US20050096365A1 (en) * | 2003-11-03 | 2005-05-05 | David Fikstad | Pharmaceutical compositions with synchronized solubilizer release |
| HRP20031029A2 (en) * | 2003-12-12 | 2005-08-31 | Belupo - Lijekovi I Kozmetika D.D. | Process for production of inclusion complexes of valsartan with?-cylodextrin |
-
2006
- 2006-04-18 WO PCT/US2006/014422 patent/WO2006113631A2/fr active Application Filing
- 2006-04-18 CA CA002605183A patent/CA2605183A1/fr not_active Abandoned
- 2006-04-18 JP JP2008507777A patent/JP2008536929A/ja active Pending
- 2006-04-18 EP EP06750455A patent/EP1877042A4/fr not_active Withdrawn
- 2006-04-18 MX MX2007012947A patent/MX2007012947A/es unknown
- 2006-04-18 AU AU2006236497A patent/AU2006236497A1/en not_active Abandoned
- 2006-04-18 KR KR1020077026647A patent/KR20080042039A/ko not_active Application Discontinuation
-
2007
- 2007-10-17 IL IL186721A patent/IL186721A0/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| JP2008536929A (ja) | 2008-09-11 |
| AU2006236497A1 (en) | 2006-10-26 |
| WO2006113631A3 (fr) | 2006-12-14 |
| EP1877042A4 (fr) | 2011-03-02 |
| KR20080042039A (ko) | 2008-05-14 |
| EP1877042A2 (fr) | 2008-01-16 |
| WO2006113631A2 (fr) | 2006-10-26 |
| IL186721A0 (en) | 2008-02-09 |
| MX2007012947A (es) | 2008-04-09 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CA2605183A1 (fr) | Compositions ameliorees biologiquement | |
| EP1750717B1 (fr) | Compositions pharmaceutiques a liberation controlee presentant une meilleure biodisponibilite | |
| WO2008084504A2 (fr) | Composition pharmaceutique d'inhibiteurs du récepteur de l'angiotensine ii | |
| RU2570752C2 (ru) | Способы лечения сердечно-сосудистых нарушений | |
| CA2720658C (fr) | Formulations ameliorees pour des ingredients pharmaceutiques actifs faiblement permeables | |
| EP2359830A1 (fr) | Préparations à libération contrôlée d'oxcarbazépine disposant d'un profil à libération sigmoïdale | |
| US20110136883A1 (en) | Granulation of active pharmaceutical ingredients | |
| WO2005070398A2 (fr) | Compositions pharmaceutiques de candesartan cilexetil stabilisees par des co-solvants | |
| US20090123543A1 (en) | Pharmaceutical compositions | |
| WO2009084040A1 (fr) | Formule d'antagonistes des récepteurs de l'angiotensine administrée une fois par jour | |
| CA2644179C (fr) | Composition pharmaceutique inedite comprenant une matrice de desintegration | |
| CA2801020A1 (fr) | Preparation pharmaceutique stable contenant du telmisartan et de l'hydrochlorothiazide | |
| AU2009256423A1 (en) | Pulsatile release of valsartan | |
| CN101217942A (zh) | 生物增强组合物 | |
| WO2013175494A2 (fr) | Formulations pharmaceutiques à libération contrôlée d'inhibiteurs directs de la thrombine | |
| ES2663721T3 (es) | Formulaciones de olmesartán | |
| US20100119607A1 (en) | Bioenhanced compositions | |
| KR101460783B1 (ko) | 안정성이 개선된 칸데사르탄 실렉세틸을 함유하는 약제학적 조성물 및 이의 제조방법 | |
| WO2019130277A1 (fr) | Formulations pharmaceutiques d'azilsartan médoxomil | |
| WO2008064338A2 (fr) | Formulation de valsartan pour administration pulsatile | |
| EP2438911A1 (fr) | Compositions pharmaceutiques comprenant du secrétagogue d'insuline de classe suphonylurée et huile de ricin à base de glycol de polyéthylène | |
| EP2153822A1 (fr) | Granulation d'ingrédients pharmaceutiques actifs | |
| WO2006119779A2 (fr) | Composition pharmaceutique comprenant un antagoniste de l'aldosterone | |
| WO2008068727A2 (fr) | Composition pharmaceutique comprenant du candésartan cilexétil | |
| CN101132782A (zh) | 氯沙坦的口服药物剂型 |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FZDE | Discontinued |