IL111116A - Pharmaceutical compositions comprising mycophenolate mofetil or mycophenolic acid and their preparation - Google Patents
Pharmaceutical compositions comprising mycophenolate mofetil or mycophenolic acid and their preparationInfo
- Publication number
- IL111116A IL111116A IL111116A IL11111694A IL111116A IL 111116 A IL111116 A IL 111116A IL 111116 A IL111116 A IL 111116A IL 11111694 A IL11111694 A IL 11111694A IL 111116 A IL111116 A IL 111116A
- Authority
- IL
- Israel
- Prior art keywords
- mycophenolate mofetil
- flavor
- color
- pharmaceutical formulation
- purified water
- Prior art date
Links
- RTGDFNSFWBGLEC-SYZQJQIISA-N mycophenolate mofetil Chemical compound COC1=C(C)C=2COC(=O)C=2C(O)=C1C\C=C(/C)CCC(=O)OCCN1CCOCC1 RTGDFNSFWBGLEC-SYZQJQIISA-N 0.000 title claims abstract description 94
- 229960004866 mycophenolate mofetil Drugs 0.000 title claims abstract description 94
- HPNSFSBZBAHARI-UHFFFAOYSA-N micophenolic acid Natural products OC1=C(CC=C(C)CCC(O)=O)C(OC)=C(C)C2=C1C(=O)OC2 HPNSFSBZBAHARI-UHFFFAOYSA-N 0.000 title claims abstract description 27
- 229960000951 mycophenolic acid Drugs 0.000 title claims abstract description 20
- HPNSFSBZBAHARI-RUDMXATFSA-N mycophenolic acid Chemical compound OC1=C(C\C=C(/C)CCC(O)=O)C(OC)=C(C)C2=C1C(=O)OC2 HPNSFSBZBAHARI-RUDMXATFSA-N 0.000 title claims abstract description 20
- 239000008194 pharmaceutical composition Substances 0.000 title claims description 21
- 238000002360 preparation method Methods 0.000 title claims description 13
- 239000000203 mixture Substances 0.000 claims abstract description 71
- 239000000796 flavoring agent Substances 0.000 claims abstract description 62
- 235000019634 flavors Nutrition 0.000 claims abstract description 62
- 239000000725 suspension Substances 0.000 claims abstract description 34
- 238000007908 dry granulation Methods 0.000 claims abstract description 28
- 239000000872 buffer Substances 0.000 claims abstract description 18
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 18
- 150000001875 compounds Chemical class 0.000 claims abstract description 18
- 235000003599 food sweetener Nutrition 0.000 claims abstract description 16
- 239000003765 sweetening agent Substances 0.000 claims abstract description 16
- 239000004599 antimicrobial Substances 0.000 claims abstract description 12
- 239000000080 wetting agent Substances 0.000 claims abstract description 12
- 235000019264 food flavour enhancer Nutrition 0.000 claims abstract description 10
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 108
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 76
- 239000008213 purified water Substances 0.000 claims description 48
- 239000000230 xanthan gum Substances 0.000 claims description 48
- 229920001285 xanthan gum Polymers 0.000 claims description 48
- 235000010493 xanthan gum Nutrition 0.000 claims description 48
- 229940082509 xanthan gum Drugs 0.000 claims description 48
- 235000010449 maltitol Nutrition 0.000 claims description 47
- 238000009472 formulation Methods 0.000 claims description 46
- 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 claims description 45
- 239000000600 sorbitol Substances 0.000 claims description 45
- 239000004615 ingredient Substances 0.000 claims description 40
- 108010011485 Aspartame Proteins 0.000 claims description 36
- 239000000605 aspartame Substances 0.000 claims description 36
- 235000010357 aspartame Nutrition 0.000 claims description 36
- IAOZJIPTCAWIRG-QWRGUYRKSA-N aspartame Chemical compound OC(=O)C[C@H](N)C(=O)N[C@H](C(=O)OC)CC1=CC=CC=C1 IAOZJIPTCAWIRG-QWRGUYRKSA-N 0.000 claims description 36
- 229960003438 aspartame Drugs 0.000 claims description 36
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 claims description 27
- 229910000397 disodium phosphate Inorganic materials 0.000 claims description 27
- 235000019800 disodium phosphate Nutrition 0.000 claims description 27
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 claims description 27
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 claims description 27
- PZNPLUBHRSSFHT-RRHRGVEJSA-N 1-hexadecanoyl-2-octadecanoyl-sn-glycero-3-phosphocholine Chemical compound CCCCCCCCCCCCCCCCCC(=O)O[C@@H](COP([O-])(=O)OCC[N+](C)(C)C)COC(=O)CCCCCCCCCCCCCCC PZNPLUBHRSSFHT-RRHRGVEJSA-N 0.000 claims description 26
- 235000010268 sodium methyl p-hydroxybenzoate Nutrition 0.000 claims description 26
- 239000008347 soybean phospholipid Substances 0.000 claims description 26
- 229930006000 Sucrose Natural products 0.000 claims description 25
- 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 claims description 25
- 239000005720 sucrose Substances 0.000 claims description 25
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 24
- 239000000845 maltitol Substances 0.000 claims description 24
- PESXGULMKCKJCC-UHFFFAOYSA-M sodium;4-methoxycarbonylphenolate Chemical compound [Na+].COC(=O)C1=CC=C([O-])C=C1 PESXGULMKCKJCC-UHFFFAOYSA-M 0.000 claims description 24
- 229940075614 colloidal silicon dioxide Drugs 0.000 claims description 22
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- 239000008108 microcrystalline cellulose Substances 0.000 claims description 21
- 229920000168 Microcrystalline cellulose Polymers 0.000 claims description 20
- 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 claims description 19
- 239000000787 lecithin Substances 0.000 claims description 19
- 235000010445 lecithin Nutrition 0.000 claims description 19
- 229940067606 lecithin Drugs 0.000 claims description 19
- 235000012745 brilliant blue FCF Nutrition 0.000 claims description 17
- 235000007265 Myrrhis odorata Nutrition 0.000 claims description 16
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- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 16
- GVKCHTBDSMQENH-UHFFFAOYSA-L phloxine B Chemical compound [Na+].[Na+].[O-]C(=O)C1=C(Cl)C(Cl)=C(Cl)C(Cl)=C1C1=C2C=C(Br)C(=O)C(Br)=C2OC2=C(Br)C([O-])=C(Br)C=C21 GVKCHTBDSMQENH-UHFFFAOYSA-L 0.000 claims description 16
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims description 14
- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 claims description 14
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 claims description 14
- 229960002216 methylparaben Drugs 0.000 claims description 14
- 229960003415 propylparaben Drugs 0.000 claims description 14
- SGHZXLIDFTYFHQ-UHFFFAOYSA-L Brilliant Blue Chemical compound [Na+].[Na+].C=1C=C(C(=C2C=CC(C=C2)=[N+](CC)CC=2C=C(C=CC=2)S([O-])(=O)=O)C=2C(=CC=CC=2)S([O-])(=O)=O)C=CC=1N(CC)CC1=CC=CC(S([O-])(=O)=O)=C1 SGHZXLIDFTYFHQ-UHFFFAOYSA-L 0.000 claims description 13
- 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 13
- 201000010099 disease Diseases 0.000 claims description 13
- 235000010232 propyl p-hydroxybenzoate Nutrition 0.000 claims description 13
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- 238000000034 method Methods 0.000 claims description 11
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 claims description 11
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 claims description 11
- 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 10
- 229930195725 Mannitol Natural products 0.000 claims description 10
- CEZCCHQBSQPRMU-UHFFFAOYSA-L chembl174821 Chemical compound [Na+].[Na+].COC1=CC(S([O-])(=O)=O)=C(C)C=C1N=NC1=C(O)C=CC2=CC(S([O-])(=O)=O)=CC=C12 CEZCCHQBSQPRMU-UHFFFAOYSA-L 0.000 claims description 10
- HQPMKSGTIOYHJT-UHFFFAOYSA-N ethane-1,2-diol;propane-1,2-diol Chemical compound OCCO.CC(O)CO HQPMKSGTIOYHJT-UHFFFAOYSA-N 0.000 claims description 10
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- CHHHXKFHOYLYRE-UHFFFAOYSA-M 2,4-Hexadienoic acid, potassium salt (1:1), (2E,4E)- Chemical compound [K+].CC=CC=CC([O-])=O CHHHXKFHOYLYRE-UHFFFAOYSA-M 0.000 claims description 8
- ILRKKHJEINIICQ-OOFFSTKBSA-N Monoammonium glycyrrhizinate Chemical compound N.O([C@@H]1[C@@H](O)[C@H](O)[C@H](O[C@@H]1O[C@H]1CC[C@]2(C)[C@H]3C(=O)C=C4[C@@H]5C[C@](C)(CC[C@@]5(CC[C@@]4(C)[C@]3(C)CC[C@H]2C1(C)C)C)C(O)=O)C(O)=O)[C@@H]1O[C@H](C(O)=O)[C@@H](O)[C@H](O)[C@H]1O ILRKKHJEINIICQ-OOFFSTKBSA-N 0.000 claims description 8
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- 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 description 8
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- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines Containing Material From Animals Or Micro-Organisms (AREA)
- Cosmetics (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
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- Pyridine Compounds (AREA)
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Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US13034393A | 1993-10-01 | 1993-10-01 |
Publications (2)
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| IL111116A0 IL111116A0 (en) | 1994-11-28 |
| IL111116A true IL111116A (en) | 1998-04-05 |
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| IL111116A IL111116A (en) | 1993-10-01 | 1994-09-30 | Pharmaceutical compositions comprising mycophenolate mofetil or mycophenolic acid and their preparation |
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| EP (2) | EP0721335B1 (cs) |
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| RO (1) | RO115412B1 (cs) |
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| TW (1) | TW427914B (cs) |
| UA (1) | UA39962C2 (cs) |
| WO (1) | WO1995009626A1 (cs) |
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| US6436425B1 (en) | 1988-11-16 | 2002-08-20 | Mdv Technologies, Inc. | Method and non-gelling composition for inhibiting post-surgical adhesions |
| US5346703A (en) | 1990-08-07 | 1994-09-13 | Mediventures, Inc. | Body cavity drug delivery with thermo-irreversible polyoxyalkylene and ionic polysaccharide gels |
| US5318780A (en) * | 1991-10-30 | 1994-06-07 | Mediventures Inc. | Medical uses of in situ formed gels |
| US5843470A (en) | 1995-10-06 | 1998-12-01 | Mdv Technologies, Inc. | Method and composition for inhibiting post-surgical adhesions |
| ID18663A (id) | 1996-04-12 | 1998-04-30 | Novartis Ag | Komposisi farmasi berlapis enterik |
| US5759579A (en) * | 1996-12-05 | 1998-06-02 | American Home Products Corporation | Pharmaceutical suspension systems |
| CA2316248A1 (en) * | 1997-12-23 | 1999-07-01 | Alliance Pharmaceutical Corp. | Methods and compositions for the delivery of pharmaceutical agents and/or the prevention of adhesions |
| JP2002524502A (ja) * | 1998-09-14 | 2002-08-06 | バーテックス ファーマシューティカルズ インコーポレイテッド | ウイルス性疾患の処置法 |
| US6410255B1 (en) * | 1999-05-05 | 2002-06-25 | Aurora Biosciences Corporation | Optical probes and assays |
| EP1591437B1 (en) | 1999-05-14 | 2009-11-25 | Nereus Pharmaceuticals, Inc. | Interleukin-1 and tumor necrosis factor-alpha modulators, syntheses of said modulators and methods of using said modulators |
| US6726922B1 (en) | 1999-06-28 | 2004-04-27 | Minu, L.L.C. | Process and composition for temporarily suppressing pain |
| WO2001062919A1 (en) | 2000-02-23 | 2001-08-30 | Aurora Biosciences Corporation | Modified fluorescent proteins |
| AU2002243228B2 (en) * | 2000-11-16 | 2007-08-02 | The Regents Of The University Of California | Marine actinomycete taxon for drug and fermentation product discovery |
| FR2819721B1 (fr) * | 2001-01-19 | 2005-02-04 | L M D | Traitement des escarres avec sucre non metabolisable et un absorbant polymerique |
| ES2243457T3 (es) | 2001-01-23 | 2005-12-01 | Gador S.A. | Composicion que comprende bifosfonatos para la prevencion y/o tratamiento de trastornos metabolicos de huesos, procedimiento de preparacion de dicha composicion y usos de la misma. |
| ES2266084T3 (es) * | 2001-02-14 | 2007-03-01 | Forte Iq B.V. | Composicion farmaceutica que comprende una goma de xantano. |
| ATE243028T1 (de) | 2001-07-11 | 2003-07-15 | Applied Pharma Res | Fettlösliche substanzen enthaltende granulate und verfahren zu ihrer herstellung |
| EP1465620A4 (en) * | 2001-10-02 | 2006-01-25 | Smithkline Beecham Corp | NEW COMPOSITION OF CARVEDILOL |
| GB0124953D0 (en) * | 2001-10-17 | 2001-12-05 | Novartis Ag | Organic Compounds |
| US7176232B2 (en) | 2002-06-24 | 2007-02-13 | The Regents Of The University Of California | Salinosporamides and methods for use thereof |
| AU2003261354A1 (en) * | 2002-08-02 | 2004-02-23 | The Regents Of The University Of California | New uses for inhibitors of inosine monophosphate dehydrogenase |
| US7112581B2 (en) * | 2002-09-27 | 2006-09-26 | Nereus Pharmaceuticals, Inc. | Macrocyclic lactams |
| GB0307553D0 (en) * | 2003-04-01 | 2003-05-07 | Novartis Ag | Organic compounds |
| US20050187170A1 (en) * | 2003-06-16 | 2005-08-25 | Biocryst Pharmaceuticals, Inc. | Enhancing the efficiency of RNA polymerase inhibitors by using inosine monophosphate dehydrogenase inhibitors |
| NZ544588A (en) * | 2003-06-20 | 2010-06-25 | Nereus Pharmaceuticals Inc | Use of salinosporamide A and analogs thereof for the treatment of cancer, inflammation and infectious diseases |
| ZA200600473B (en) * | 2003-06-20 | 2007-04-25 | Univ California | Salinosporamides and methods for use thereof |
| CA2445420A1 (en) | 2003-07-29 | 2005-01-29 | Invitrogen Corporation | Kinase and phosphatase assays |
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1994
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