AP1192A - Solubilized sertraline compositions. - Google Patents

Solubilized sertraline compositions. Download PDF

Info

Publication number: AP1192A
Authority: AP; ARIPO
Prior art keywords: composition; sertraline; matter; solubilizing agent; acid
Prior art date: 1997-07-01

Application number

APAP/P/1998/001280A

Other languages

English (en)

Other versions

AP9801280A0 (en

Inventor

Dwayne Thomas Friesen

Scott Max Herbig

Ravi Mysore Shanker

James Blair West

Original Assignee

Pfizer Prod Inc

Priority date (The priority date 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 date listed.)

1997-07-01

Filing date

1998-06-25

Publication date

2003-07-23

Family has litigation

First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=21971159&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AP1192(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.

1998-06-25 Application filed by Pfizer Prod Inc filed Critical Pfizer Prod Inc

1998-06-30 Publication of AP9801280A0 publication Critical patent/AP9801280A0/xx

2003-07-23 Application granted granted Critical

2003-07-23 Publication of AP1192A publication Critical patent/AP1192A/en

Links

VGKDLMBJGBXTGI-SJCJKPOMSA-N sertraline Chemical compound C1([C@@H]2CC[C@@H](C3=CC=CC=C32)NC)=CC=C(Cl)C(Cl)=C1 VGKDLMBJGBXTGI-SJCJKPOMSA-N 0.000 title claims abstract description 133
229960002073 sertraline Drugs 0.000 title claims abstract description 126
239000000203 mixture Substances 0.000 title claims abstract description 75
239000002904 solvent Substances 0.000 claims abstract description 85
VEXZGXHMUGYJMC-UHFFFAOYSA-M Chloride anion Chemical compound [Cl-] VEXZGXHMUGYJMC-UHFFFAOYSA-M 0.000 claims abstract description 31
239000002552 dosage form Substances 0.000 claims description 49
KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 31
150000007524 organic acids Chemical class 0.000 claims description 31
FAPWRFPIFSIZLT-UHFFFAOYSA-M Sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims description 29
GHBFNMLVSPCDGN-UHFFFAOYSA-N rac-1-monooctanoylglycerol Chemical compound CCCCCCCC(=O)OCC(O)CO GHBFNMLVSPCDGN-UHFFFAOYSA-N 0.000 claims description 29
CIWBSHSKHKDKBQ-JLAZNSOCSA-N Ascorbic acid Chemical compound OC[C@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-JLAZNSOCSA-N 0.000 claims description 26
VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 26
150000003839 salts Chemical class 0.000 claims description 26
238000012360 testing method Methods 0.000 claims description 23
125000005456 glyceride group Chemical group 0.000 claims description 21
238000000034 method Methods 0.000 claims description 18
229940093915 gynecological organic acid Drugs 0.000 claims description 16
235000005985 organic acids Nutrition 0.000 claims description 16
229920001223 polyethylene glycol Polymers 0.000 claims description 16
238000013270 controlled release Methods 0.000 claims description 14
239000011780 sodium chloride Substances 0.000 claims description 14
229910000019 calcium carbonate Inorganic materials 0.000 claims description 13
230000003381 solubilizing effect Effects 0.000 claims description 13
235000010323 ascorbic acid Nutrition 0.000 claims description 12
-1 organic acid salts Chemical class 0.000 claims description 12
ARIWANIATODDMH-UHFFFAOYSA-N rac-1-monolauroylglycerol Chemical compound CCCCCCCCCCCC(=O)OCC(O)CO ARIWANIATODDMH-UHFFFAOYSA-N 0.000 claims description 12
239000011668 ascorbic acid Substances 0.000 claims description 11
235000015165 citric acid Nutrition 0.000 claims description 11
239000002202 Polyethylene glycol Substances 0.000 claims description 10
229960005070 ascorbic acid Drugs 0.000 claims description 10
CKLJMWTZIZZHCS-REOHCLBHSA-N aspartic acid group Chemical group N[C@@H](CC(=O)O)C(=O)O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims description 10
150000002334 glycols Chemical class 0.000 claims description 10
239000012729 immediate-release (IR) formulation Substances 0.000 claims description 10
229960005261 aspartic acid Drugs 0.000 claims description 9
235000003704 aspartic acid Nutrition 0.000 claims description 9
OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims description 9
239000003795 chemical substances by application Substances 0.000 claims description 9
238000001727 in vivo Methods 0.000 claims description 9
WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims description 8
235000010216 calcium carbonate Nutrition 0.000 claims description 8
230000000052 comparative effect Effects 0.000 claims description 8
230000036961 partial effect Effects 0.000 claims description 8
WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims description 7
229960002989 glutamic acid Drugs 0.000 claims description 7
229940087068 glyceryl caprylate Drugs 0.000 claims description 7
VSGNNIFQASZAOI-UHFFFAOYSA-L calcium acetate Chemical compound [Ca+2].CC([O-])=O.CC([O-])=O VSGNNIFQASZAOI-UHFFFAOYSA-L 0.000 claims description 6
239000001639 calcium acetate Substances 0.000 claims description 6
235000011092 calcium acetate Nutrition 0.000 claims description 6
229960005147 calcium acetate Drugs 0.000 claims description 6
229960003563 calcium carbonate Drugs 0.000 claims description 6
150000002148 esters Chemical class 0.000 claims description 6
235000013922 glutamic acid Nutrition 0.000 claims description 6
239000004220 glutamic acid Substances 0.000 claims description 6
229940068939 glyceryl monolaurate Drugs 0.000 claims description 6
JNYAEWCLZODPBN-JGWLITMVSA-N (2r,3r,4s)-2-[(1r)-1,2-dihydroxyethyl]oxolane-3,4-diol Chemical class OC[C@@H](O)[C@H]1OC[C@H](O)[C@H]1O JNYAEWCLZODPBN-JGWLITMVSA-N 0.000 claims description 5
230000000694 effects Effects 0.000 claims description 5
229920000056 polyoxyethylene ether Polymers 0.000 claims description 5
229920001451 polypropylene glycol Polymers 0.000 claims description 5
229920000136 polysorbate Polymers 0.000 claims description 5
150000005846 sugar alcohols Polymers 0.000 claims description 5
150000005323 carbonate salts Chemical class 0.000 claims description 4
229960004106 citric acid Drugs 0.000 claims description 4
DBMJMQXJHONAFJ-UHFFFAOYSA-M Sodium laurylsulphate Chemical compound [Na+].CCCCCCCCCCCCOS([O-])(=O)=O DBMJMQXJHONAFJ-UHFFFAOYSA-M 0.000 claims 4
239000000783 alginic acid Substances 0.000 claims 4
235000010443 alginic acid Nutrition 0.000 claims 4
229920000615 alginic acid Polymers 0.000 claims 4
229960001126 alginic acid Drugs 0.000 claims 4
150000004781 alginic acids Chemical group 0.000 claims 4
239000008159 sesame oil Substances 0.000 claims 4
235000011803 sesame oil Nutrition 0.000 claims 4
239000001509 sodium citrate Substances 0.000 claims 4
NLJMYIDDQXHKNR-UHFFFAOYSA-K sodium citrate Chemical compound O.O.[Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O NLJMYIDDQXHKNR-UHFFFAOYSA-K 0.000 claims 4
235000011083 sodium citrates Nutrition 0.000 claims 4
235000019333 sodium laurylsulphate Nutrition 0.000 claims 4
235000019483 Peanut oil Nutrition 0.000 claims 3
239000000312 peanut oil Substances 0.000 claims 3
229920003171 Poly (ethylene oxide) Polymers 0.000 claims 1
239000003921 oil Substances 0.000 claims 1
235000019198 oils Nutrition 0.000 claims 1
239000000243 solution Substances 0.000 description 41
239000000546 pharmaceutical excipient Substances 0.000 description 33
JVTAAEKCZFNVCJ-UHFFFAOYSA-M Lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 description 24
239000011248 coating agent Substances 0.000 description 18
238000000576 coating method Methods 0.000 description 18
229940079593 drug Drugs 0.000 description 14
239000003814 drug Substances 0.000 description 14
238000009472 formulation Methods 0.000 description 14
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 13
239000008101 lactose Substances 0.000 description 13
239000002253 acid Substances 0.000 description 11
URAYPUMNDPQOKB-UHFFFAOYSA-N triacetin Chemical compound CC(=O)OCC(OC(C)=O)COC(C)=O URAYPUMNDPQOKB-UHFFFAOYSA-N 0.000 description 10
238000004090 dissolution Methods 0.000 description 9
239000000499 gel Substances 0.000 description 9
XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 9
150000007513 acids Chemical class 0.000 description 8
239000011575 calcium Substances 0.000 description 8
238000001879 gelation Methods 0.000 description 8
238000013268 sustained release Methods 0.000 description 8
239000012730 sustained-release form Substances 0.000 description 8
230000008901 benefit Effects 0.000 description 7
239000012528 membrane Substances 0.000 description 7
230000003204 osmotic effect Effects 0.000 description 7
239000012085 test solution Substances 0.000 description 7
GLQPTZAAUROJMO-UHFFFAOYSA-N 4-(3,4-dimethoxyphenyl)benzaldehyde Chemical compound C1=C(OC)C(OC)=CC=C1C1=CC=C(C=O)C=C1 GLQPTZAAUROJMO-UHFFFAOYSA-N 0.000 description 6
DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Chemical compound NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 description 6
ZMANZCXQSJIPKH-UHFFFAOYSA-N Triethylamine Chemical compound CCN(CC)CC ZMANZCXQSJIPKH-UHFFFAOYSA-N 0.000 description 6
239000012530 fluid Substances 0.000 description 6
238000000338 in vitro Methods 0.000 description 6
HQKMJHAJHXVSDF-UHFFFAOYSA-L magnesium stearate Chemical compound [Mg+2].CCCCCCCCCCCCCCCCCC([O-])=O.CCCCCCCCCCCCCCCCCC([O-])=O HQKMJHAJHXVSDF-UHFFFAOYSA-L 0.000 description 6
239000011159 matrix material Substances 0.000 description 6
229960003660 sertraline hydrochloride Drugs 0.000 description 6
238000003756 stirring Methods 0.000 description 6
VBICKXHEKHSIBG-UHFFFAOYSA-N 1-monostearoylglycerol Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCC(O)CO VBICKXHEKHSIBG-UHFFFAOYSA-N 0.000 description 5
RFVNOJDQRGSOEL-UHFFFAOYSA-N 2-hydroxyethyl octadecanoate Chemical compound CCCCCCCCCCCCCCCCCC(=O)OCCO RFVNOJDQRGSOEL-UHFFFAOYSA-N 0.000 description 5
QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 5
229930091371 Fructose Natural products 0.000 description 5
239000005715 Fructose Substances 0.000 description 5
RFSUNEUAIZKAJO-ARQDHWQXSA-N Fructose Chemical compound OC[C@H]1O[C@](O)(CO)[C@@H](O)[C@@H]1O RFSUNEUAIZKAJO-ARQDHWQXSA-N 0.000 description 5
239000002775 capsule Substances 0.000 description 5
239000001087 glyceryl triacetate Substances 0.000 description 5
235000013773 glyceryl triacetate Nutrition 0.000 description 5
230000007246 mechanism Effects 0.000 description 5
239000000843 powder Substances 0.000 description 5
239000002244 precipitate Substances 0.000 description 5
230000002829 reductive effect Effects 0.000 description 5
239000007787 solid Substances 0.000 description 5
229960002622 triacetin Drugs 0.000 description 5
QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 description 4
QTBSBXVTEAMEQO-UHFFFAOYSA-M Acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 description 4
CIWBSHSKHKDKBQ-DUZGATOHSA-N D-araboascorbic acid Natural products OC[C@@H](O)[C@H]1OC(=O)C(O)=C1O CIWBSHSKHKDKBQ-DUZGATOHSA-N 0.000 description 4
VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 4
ZTHYODDOHIVTJV-UHFFFAOYSA-N Propyl gallate Chemical compound CCCOC(=O)C1=CC(O)=C(O)C(O)=C1 ZTHYODDOHIVTJV-UHFFFAOYSA-N 0.000 description 4
229920001400 block copolymer Polymers 0.000 description 4
150000001875 compounds Chemical class 0.000 description 4
230000003111 delayed effect Effects 0.000 description 4
235000010350 erythorbic acid Nutrition 0.000 description 4
WNLRTRBMVRJNCN-UHFFFAOYSA-N hexanedioic acid Natural products OC(=O)CCCCC(O)=O WNLRTRBMVRJNCN-UHFFFAOYSA-N 0.000 description 4
239000000463 material Substances 0.000 description 4
150000003904 phospholipids Chemical class 0.000 description 4
239000000126 substance Substances 0.000 description 4
GTZCVFVGUGFEME-UHFFFAOYSA-N trans-aconitic acid Natural products OC(=O)CC(C(O)=O)=CC(O)=O GTZCVFVGUGFEME-UHFFFAOYSA-N 0.000 description 4
VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 4
239000001124 (E)-prop-1-ene-1,2,3-tricarboxylic acid Substances 0.000 description 3
IIZPXYDJLKNOIY-JXPKJXOSSA-N 1-palmitoyl-2-arachidonoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCC\C=C/C\C=C/C\C=C/C\C=C/CCCCC IIZPXYDJLKNOIY-JXPKJXOSSA-N 0.000 description 3
CTXGTHVAWRBISV-UHFFFAOYSA-N 2-hydroxyethyl dodecanoate Chemical compound CCCCCCCCCCCC(=O)OCCO CTXGTHVAWRBISV-UHFFFAOYSA-N 0.000 description 3
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 description 3
CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
WEVYAHXRMPXWCK-UHFFFAOYSA-N Acetonitrile Chemical compound CC#N WEVYAHXRMPXWCK-UHFFFAOYSA-N 0.000 description 3
239000004471 Glycine Substances 0.000 description 3
VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 3
QAQJMLQRFWZOBN-LAUBAEHRSA-N L-ascorbyl-6-palmitate Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](O)[C@H]1OC(=O)C(O)=C1O QAQJMLQRFWZOBN-LAUBAEHRSA-N 0.000 description 3
239000011786 L-ascorbyl-6-palmitate Substances 0.000 description 3
229920002562 Polyethylene Glycol 3350 Polymers 0.000 description 3
238000010521 absorption reaction Methods 0.000 description 3
229940091181 aconitic acid Drugs 0.000 description 3
238000013019 agitation Methods 0.000 description 3
238000004458 analytical method Methods 0.000 description 3
235000010385 ascorbyl palmitate Nutrition 0.000 description 3
230000009286 beneficial effect Effects 0.000 description 3
239000008280 blood Substances 0.000 description 3
210000004369 blood Anatomy 0.000 description 3
239000001354 calcium citrate Substances 0.000 description 3
229960004256 calcium citrate Drugs 0.000 description 3
159000000007 calcium salts Chemical class 0.000 description 3
GTZCVFVGUGFEME-IWQZZHSRSA-N cis-aconitic acid Chemical compound OC(=O)C\C(C(O)=O)=C\C(O)=O GTZCVFVGUGFEME-IWQZZHSRSA-N 0.000 description 3
230000003628 erosive effect Effects 0.000 description 3
239000004318 erythorbic acid Substances 0.000 description 3
239000012458 free base Substances 0.000 description 3
230000002496 gastric effect Effects 0.000 description 3
238000004128 high performance liquid chromatography Methods 0.000 description 3
HNDVDQJCIGZPNO-UHFFFAOYSA-N histidine Natural products OC(=O)C(N)CC1=CN=CN1 HNDVDQJCIGZPNO-UHFFFAOYSA-N 0.000 description 3
229940026239 isoascorbic acid Drugs 0.000 description 3
239000000787 lecithin Substances 0.000 description 3
235000010445 lecithin Nutrition 0.000 description 3
229940067606 lecithin Drugs 0.000 description 3
235000019359 magnesium stearate Nutrition 0.000 description 3
229920001983 poloxamer Polymers 0.000 description 3
238000004007 reversed phase HPLC Methods 0.000 description 3
238000012216 screening Methods 0.000 description 3
229940035044 sorbitan monolaurate Drugs 0.000 description 3
210000002784 stomach Anatomy 0.000 description 3
239000000725 suspension Substances 0.000 description 3
230000001225 therapeutic effect Effects 0.000 description 3
235000013337 tricalcium citrate Nutrition 0.000 description 3
ZORQXIQZAOLNGE-UHFFFAOYSA-N 1,1-difluorocyclohexane Chemical compound FC1(F)CCCCC1 ZORQXIQZAOLNGE-UHFFFAOYSA-N 0.000 description 2
JAHNSTQSQJOJLO-UHFFFAOYSA-N 2-(3-fluorophenyl)-1h-imidazole Chemical compound FC1=CC=CC(C=2NC=CN=2)=C1 JAHNSTQSQJOJLO-UHFFFAOYSA-N 0.000 description 2
ALYNCZNDIQEVRV-UHFFFAOYSA-N 4-aminobenzoic acid Chemical compound NC1=CC=C(C(O)=O)C=C1 ALYNCZNDIQEVRV-UHFFFAOYSA-N 0.000 description 2
CKLJMWTZIZZHCS-UHFFFAOYSA-N Aspartic acid Chemical compound OC(=O)C(N)CC(O)=O CKLJMWTZIZZHCS-UHFFFAOYSA-N 0.000 description 2
OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 description 2
OUYCCCASQSFEME-QMMMGPOBSA-N L-tyrosine Chemical compound OC(=O)[C@@H](N)CC1=CC=C(O)C=C1 OUYCCCASQSFEME-QMMMGPOBSA-N 0.000 description 2
241000124008 Mammalia Species 0.000 description 2
229920000168 Microcrystalline cellulose Polymers 0.000 description 2
OFOBLEOULBTSOW-UHFFFAOYSA-N Propanedioic acid Natural products OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 2
FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 2
KGUHOFWIXKIURA-VQXBOQCVSA-N [(2r,3s,4s,5r,6r)-6-[(2s,3s,4s,5r)-3,4-dihydroxy-2,5-bis(hydroxymethyl)oxolan-2-yl]oxy-3,4,5-trihydroxyoxan-2-yl]methyl dodecanoate Chemical compound O[C@@H]1[C@@H](O)[C@H](O)[C@@H](COC(=O)CCCCCCCCCCC)O[C@@H]1O[C@@]1(CO)[C@@H](O)[C@H](O)[C@@H](CO)O1 KGUHOFWIXKIURA-VQXBOQCVSA-N 0.000 description 2
229960000583 acetic acid Drugs 0.000 description 2
235000011037 adipic acid Nutrition 0.000 description 2
BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 2
239000007864 aqueous solution Substances 0.000 description 2
230000015572 biosynthetic process Effects 0.000 description 2
239000000872 buffer Substances 0.000 description 2
229960005069 calcium Drugs 0.000 description 2
229910052791 calcium Inorganic materials 0.000 description 2
FNAQSUUGMSOBHW-UHFFFAOYSA-H calcium citrate Chemical compound [Ca+2].[Ca+2].[Ca+2].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O FNAQSUUGMSOBHW-UHFFFAOYSA-H 0.000 description 2
MKJXYGKVIBWPFZ-UHFFFAOYSA-L calcium lactate Chemical compound [Ca+2].CC(O)C([O-])=O.CC(O)C([O-])=O MKJXYGKVIBWPFZ-UHFFFAOYSA-L 0.000 description 2
239000001527 calcium lactate Substances 0.000 description 2
235000011086 calcium lactate Nutrition 0.000 description 2
229960002401 calcium lactate Drugs 0.000 description 2
229920002301 cellulose acetate Polymers 0.000 description 2
238000007796 conventional method Methods 0.000 description 2
230000001079 digestive effect Effects 0.000 description 2
FKRCODPIKNYEAC-UHFFFAOYSA-N ethyl propionate Chemical compound CCOC(=O)CC FKRCODPIKNYEAC-UHFFFAOYSA-N 0.000 description 2
CBOQJANXLMLOSS-UHFFFAOYSA-N ethyl vanillin Chemical compound CCOC1=CC(C=O)=CC=C1O CBOQJANXLMLOSS-UHFFFAOYSA-N 0.000 description 2
238000001914 filtration Methods 0.000 description 2
239000001530 fumaric acid Substances 0.000 description 2
210000001035 gastrointestinal tract Anatomy 0.000 description 2
239000007903 gelatin capsule Substances 0.000 description 2
229940075507 glyceryl monostearate Drugs 0.000 description 2
150000003893 lactate salts Chemical class 0.000 description 2
JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
239000007788 liquid Substances 0.000 description 2
239000012669 liquid formulation Substances 0.000 description 2
239000000314 lubricant Substances 0.000 description 2
239000011976 maleic acid Substances 0.000 description 2
LVHBHZANLOWSRM-UHFFFAOYSA-N methylenebutanedioic acid Natural products OC(=O)CC(=C)C(O)=O LVHBHZANLOWSRM-UHFFFAOYSA-N 0.000 description 2
LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 description 2
239000008108 microcrystalline cellulose Substances 0.000 description 2
229940016286 microcrystalline cellulose Drugs 0.000 description 2
235000019813 microcrystalline cellulose Nutrition 0.000 description 2
239000001788 mono and diglycerides of fatty acids Substances 0.000 description 2
HDKLIZDXVUCLHQ-UHFFFAOYSA-N non-3-en-2-one Chemical compound CCCCCC=CC(C)=O HDKLIZDXVUCLHQ-UHFFFAOYSA-N 0.000 description 2
239000006186 oral dosage form Substances 0.000 description 2
WTJKGGKOPKCXLL-RRHRGVEJSA-N phosphatidylcholine Chemical compound CCCCCCCCCCCCCCCC(=O)OC[C@H](COP([O-])(=O)OCC[N+](C)(C)C)OC(=O)CCCCCCCC=CCCCCCCCC WTJKGGKOPKCXLL-RRHRGVEJSA-N 0.000 description 2
229920000642 polymer Polymers 0.000 description 2
239000000473 propyl gallate Substances 0.000 description 2
235000010388 propyl gallate Nutrition 0.000 description 2
229940075579 propyl gallate Drugs 0.000 description 2
QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 description 2
239000012266 salt solution Substances 0.000 description 2
229940124834 selective serotonin reuptake inhibitor Drugs 0.000 description 2
239000012896 selective serotonin reuptake inhibitor Substances 0.000 description 2
210000000813 small intestine Anatomy 0.000 description 2
239000001593 sorbitan monooleate Substances 0.000 description 2
235000011069 sorbitan monooleate Nutrition 0.000 description 2
229940035049 sorbitan monooleate Drugs 0.000 description 2
KDYFGRWQOYBRFD-UHFFFAOYSA-N succinic acid Chemical compound OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 2
229940032085 sucrose monolaurate Drugs 0.000 description 2
235000000346 sugar Nutrition 0.000 description 2
239000006228 supernatant Substances 0.000 description 2
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- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
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- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/08—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing oxygen, e.g. ethers, acetals, ketones, quinones, aldehydes, peroxides
- A61K47/14—Esters of carboxylic acids, e.g. fatty acid monoglycerides, medium-chain triglycerides, parabens or PEG fatty acid esters
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K47/00—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
- A61K47/06—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite
- A61K47/16—Organic compounds, e.g. natural or synthetic hydrocarbons, polyolefins, mineral oil, petrolatum or ozokerite containing nitrogen, e.g. nitro-, nitroso-, azo-compounds, nitriles, cyanates
- A61K47/18—Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
- A61K47/183—Amino acids, e.g. glycine, EDTA or aspartame

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Chemical & Material Sciences (AREA)
Life Sciences & Earth Sciences (AREA)
Veterinary Medicine (AREA)
Medicinal Chemistry (AREA)
Pharmacology & Pharmacy (AREA)
Animal Behavior & Ethology (AREA)
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Public Health (AREA)
Epidemiology (AREA)
Bioinformatics & Cheminformatics (AREA)
Engineering & Computer Science (AREA)
General Chemical & Material Sciences (AREA)
Biomedical Technology (AREA)
Neurology (AREA)
Neurosurgery (AREA)
Chemical Kinetics & Catalysis (AREA)
Inorganic Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Organic Chemistry (AREA)
Biophysics (AREA)
Molecular Biology (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Medicinal Preparation (AREA)
Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

APAP/P/1998/001280A 1997-07-01 1998-06-25 Solubilized sertraline compositions. AP1192A (en)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
US5141397P	1997-07-01	1997-07-01

Publications (2)

Publication Number	Publication Date
AP9801280A0 AP9801280A0 (en)	1998-06-30
AP1192A true AP1192A (en)	2003-07-23

Family

ID=21971159

Family Applications (1)

Application Number	Title	Priority Date	Filing Date
APAP/P/1998/001280A AP1192A (en)	1997-07-01	1998-06-25	Solubilized sertraline compositions.

Country Status (34)

Country	Link
EP (1)	EP0999829A1 (is)
JP (1)	JP2000514100A (is)
KR (1)	KR100366373B1 (is)
CN (1)	CN1261794A (is)
AP (1)	AP1192A (is)
AR (3)	AR015917A1 (is)
AU (1)	AU742535B2 (is)
BG (1)	BG103918A (is)
BR (1)	BR9810739A (is)
CA (1)	CA2290974C (is)
CO (1)	CO4940495A1 (is)
DZ (1)	DZ2548A1 (is)
EA (1)	EA002481B1 (is)
HN (1)	HN1998000102A (is)
HR (1)	HRP980377A2 (is)
HU (1)	HUP0002236A3 (is)
ID (1)	ID23429A (is)
IL (1)	IL133076A (is)
IS (1)	IS5260A (is)
MA (1)	MA24587A1 (is)
NO (1)	NO996520L (is)
OA (1)	OA11243A (is)
PA (1)	PA8454301A1 (is)
PE (1)	PE97199A1 (is)
PL (1)	PL337804A1 (is)
SK (1)	SK181099A3 (is)
TN (1)	TNSN98124A1 (is)
TR (1)	TR199903297T2 (is)
TW (1)	TW550087B (is)
UA (1)	UA67741C2 (is)
UY (1)	UY25071A1 (is)
WO (1)	WO1999001120A1 (is)
YU (1)	YU68299A (is)
ZA (1)	ZA985708B (is)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
BR0016555A (pt)	1999-12-23	2002-09-17	Pfizer Prod Inc	Composições farmacêuticas que proporcionam concentrações acrescidas de droga
US20030086972A1 (en) *	2000-08-09	2003-05-08	Appel Leah E.	Hydrogel-driven drug dosage form
MXPA03001771A (es)	2000-08-30	2003-06-04	Pfizer Prod Inc	Formulaciones de liberacion sostenida para secretagogos de hormona del crecimiento.
US20040191207A1 (en) *	2003-03-31	2004-09-30	Lipari John M.	Alpha-hydroxy acid ester drug delivery compositions and methods of use
CN101631593B (zh) *	2007-03-12	2014-08-13	帝斯曼知识产权资产管理有限公司	化妆品组合物
TH121482A (th)	2009-08-19	2013-02-28	นางสาวปัณณพัฒน์ เหลืองธาตุทอง	องค์ประกอบทางเภสัชกรรมที่ประกอบด้วยอนุพันธ์ของควิโนลีน
WO2011081118A1 (ja) *	2009-12-29	2011-07-07	興和株式会社	経口投与用医薬組成物
KR20120123289A (ko) *	2009-12-29	2012-11-08	코와 가부시키가이샤	경구 투여용 고형 의약 조성물
CN109908354A (zh) *	2017-12-12	2019-06-21	万特制药(海南)有限公司	盐酸舍曲林口服浓缩液及其制备工艺
CN114894736B (zh) *	2022-05-20	2025-03-21	中化地质矿山总局地质研究院	一种氯化物型卤水中硝酸根的测定方法

Citations (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
EP0415612A2 (en) *	1989-08-30	1991-03-06	Pfizer Inc.	Use of sertraline for the treatment of chemical dependencies

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4803076A (en) *	1986-09-04	1989-02-07	Pfizer Inc.	Controlled release device for an active substance
ZA97976B (en) *	1996-04-05	1997-08-18	Alza Corp	Uniform drug delivery theraphy.

1998
- 1998-06-15 CN CN98806763A patent/CN1261794A/zh active Pending
- 1998-06-15 CA CA002290974A patent/CA2290974C/en not_active Expired - Fee Related
- 1998-06-15 EA EA199900962A patent/EA002481B1/ru unknown
- 1998-06-15 JP JP11506774A patent/JP2000514100A/ja active Pending
- 1998-06-15 WO PCT/IB1998/000933 patent/WO1999001120A1/en not_active Ceased
- 1998-06-15 YU YU68299A patent/YU68299A/sh unknown
- 1998-06-15 BR BR9810739-9A patent/BR9810739A/pt not_active Application Discontinuation
- 1998-06-15 PL PL98337804A patent/PL337804A1/xx unknown
- 1998-06-15 HU HU0002236A patent/HUP0002236A3/hu unknown
- 1998-06-15 IL IL13307698A patent/IL133076A/xx not_active IP Right Cessation
- 1998-06-15 ID IDW991701A patent/ID23429A/id unknown
- 1998-06-15 SK SK1810-99A patent/SK181099A3/sk unknown
- 1998-06-15 KR KR10-1999-7011361A patent/KR100366373B1/ko not_active Expired - Fee Related
- 1998-06-15 EP EP98923019A patent/EP0999829A1/en not_active Withdrawn
- 1998-06-15 AU AU75448/98A patent/AU742535B2/en not_active Ceased
- 1998-06-15 UA UA99116391A patent/UA67741C2/uk unknown
- 1998-06-15 TR TR1999/03297T patent/TR199903297T2/xx unknown
- 1998-06-25 AP APAP/P/1998/001280A patent/AP1192A/en active
- 1998-06-25 TW TW087110267A patent/TW550087B/zh active
- 1998-06-26 PE PE1998000573A patent/PE97199A1/es not_active Application Discontinuation
- 1998-06-29 PA PA19988454301A patent/PA8454301A1/es unknown
- 1998-06-29 AR ARP980103146A patent/AR015917A1/es not_active Application Discontinuation
- 1998-06-29 UY UY25071A patent/UY25071A1/es not_active IP Right Cessation
- 1998-06-30 ZA ZA9805708A patent/ZA985708B/xx unknown
- 1998-06-30 DZ DZ980158A patent/DZ2548A1/xx active
- 1998-06-30 MA MA25146A patent/MA24587A1/fr unknown
- 1998-06-30 TN TNTNSN98124A patent/TNSN98124A1/fr unknown
- 1998-07-01 HR HR60/051,413A patent/HRP980377A2/hr not_active Application Discontinuation
- 1998-07-01 HN HN1998000102A patent/HN1998000102A/es unknown
- 1998-07-01 CO CO98037137A patent/CO4940495A1/es unknown
1999
- 1999-11-19 IS IS5260A patent/IS5260A/is unknown
- 1999-11-23 BG BG103918A patent/BG103918A/xx unknown
- 1999-12-21 OA OA9900301A patent/OA11243A/en unknown
- 1999-12-28 NO NO996520A patent/NO996520L/no not_active Application Discontinuation
2003
- 2003-06-19 AR ARP030102179A patent/AR040279A2/es unknown
- 2003-06-19 AR ARP030102180A patent/AR040280A2/es unknown

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
EP0415612A2 (en) *	1989-08-30	1991-03-06	Pfizer Inc.	Use of sertraline for the treatment of chemical dependencies

Also Published As

Publication number	Publication date
HRP980377A2 (en)	1999-04-30
IS5260A (is)	1999-11-19
EP0999829A1 (en)	2000-05-17
ZA985708B (en)	2000-01-10
BR9810739A (pt)	2000-09-12
AR040280A2 (es)	2005-03-23
EA199900962A1 (ru)	2000-08-28
DZ2548A1 (fr)	2003-02-08
PL337804A1 (en)	2000-09-11
OA11243A (en)	2003-07-24
HUP0002236A3 (en)	2003-12-29
NO996520L (no)	2000-02-29
KR100366373B1 (ko)	2003-01-14
HUP0002236A2 (hu)	2003-08-28
AR015917A1 (es)	2001-05-30
UA67741C2 (uk)	2004-07-15
YU68299A (sh)	2002-06-19
WO1999001120A1 (en)	1999-01-14
HN1998000102A (es)	1999-01-08
UY25071A1 (es)	2000-12-29
CA2290974A1 (en)	1999-01-14
TW550087B (en)	2003-09-01
TR199903297T2 (xx)	2000-07-21
SK181099A3 (en)	2000-07-11
PA8454301A1 (es)	2000-09-29
JP2000514100A (ja)	2000-10-24
BG103918A (en)	2000-07-31
ID23429A (id)	2000-04-20
AU7544898A (en)	1999-01-25
EA002481B1 (ru)	2002-06-27
CO4940495A1 (es)	2000-07-24
CN1261794A (zh)	2000-08-02
CA2290974C (en)	2004-04-27
AU742535B2 (en)	2002-01-03
IL133076A (en)	2003-12-10
TNSN98124A1 (fr)	2005-03-15
MA24587A1 (fr)	1998-12-31
IL133076A0 (en)	2001-03-19
NO996520D0 (no)	1999-12-28
PE97199A1 (es)	1999-10-05
AR040279A2 (es)	2005-03-23
AP9801280A0 (en)	1998-06-30
KR20010013365A (ko)	2001-02-26

Publication	Publication Date	Title
JPH10502390A (ja)	1998-03-03	医薬品用の徐放性マトリックス
EA004443B1 (ru)	2004-04-29	Лекарственная форма для контролируемого высвобождения ципрофлоксацина для приема один раз в день
RU2237480C2 (ru)	2004-10-10	Непосредственно прессуемая матрица для регулируемого высвобождения однократных ежедневных доз кларитромицина
AP1192A (en)	2003-07-23	Solubilized sertraline compositions.
ES2852899T3 (es)	2021-09-14	Formulaciones estabilizadas de molindona
AP1199A (en)	2003-08-28	Delayed-release dosage forms of sertraline.
US7063864B1 (en)	2006-06-20	Morphine sulphate microgranules, method for preparing same and compositions containing same
ES2321908T3 (es)	2009-06-15	Preparaciones farmaceuticas de liberacion prolongada independientemente del ph.
JPH069388A (ja)	1994-01-18	徐放性塩酸オキシブチニン製剤
DE60319983T2 (de)	2009-07-23	Universelle Zusammensetzung zur kontrollierten Wirkstoffabgabe enthaltend Chitosan
JP5105684B2 (ja)	2012-12-26	持続性医薬製剤
JPH0748256A (ja)	1995-02-21	ニセルゴリンを含有する制御放出性の製薬組成物
US20040208926A1 (en)	2004-10-21	Solubilized sertraline compositions
NZ501250A (en)	2003-05-30	Solubilized sertraline compositions
KR20010078703A (ko)	2001-08-21	신규 제약 제제
KR20230067636A (ko)	2023-05-16	듀테트라베나진을 포함하는 다중미립자 제형
CZ464199A3 (cs)	2000-04-12	Solubilizované sertralinové kompozice
BR102018016507A2 (pt)	2019-03-19	Composição líquida de liberação prolongada de guaifenesina
MXPA99012101A (en)	2000-06-01	Solubilized sertraline compositions
KR20260028023A (ko)	2026-03-03	푸다펜신의 서방형 제형
JPWO2016117642A1 (ja)	2017-10-26	フィルム製剤
HK1028881A (en)	2001-03-09	Solubilized sertraline compositions
KR20040044197A (ko)	2004-05-27	약학 제제
MXPA99012082A (en)	2000-09-04	Delayed-release dosage forms of sertraline