LT4099B - Oral pharmaceutical compositions, processes for preparation and use thereof - Google Patents
Oral pharmaceutical compositions, processes for preparation and use thereof Download PDFInfo
- Publication number
- LT4099B LT4099B LT96-039A LT96039A LT4099B LT 4099 B LT4099 B LT 4099B LT 96039 A LT96039 A LT 96039A LT 4099 B LT4099 B LT 4099B
- Authority
- LT
- Lithuania
- Prior art keywords
- hydroxybenzoate
- mofetil mycophenolate
- xanthan gum
- pharmaceutical composition
- purified water
- Prior art date
Links
- 238000002360 preparation method Methods 0.000 title claims description 13
- 238000000034 method Methods 0.000 title description 6
- 239000008203 oral pharmaceutical composition Substances 0.000 title 1
- 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 claims abstract description 88
- 239000000725 suspension Substances 0.000 claims abstract description 39
- 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 claims abstract description 35
- 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 claims abstract description 26
- 229960000951 mycophenolic acid Drugs 0.000 claims abstract description 26
- 239000003795 chemical substances by application Substances 0.000 claims abstract description 24
- 239000000872 buffer Substances 0.000 claims abstract description 19
- 239000004599 antimicrobial Substances 0.000 claims abstract description 13
- 235000003599 food sweetener Nutrition 0.000 claims abstract description 13
- 239000003765 sweetening agent Substances 0.000 claims abstract description 13
- 239000000796 flavoring agent Substances 0.000 claims abstract description 9
- 239000000080 wetting agent Substances 0.000 claims abstract description 8
- 235000019264 food flavour enhancer Nutrition 0.000 claims abstract description 7
- 235000019634 flavors Nutrition 0.000 claims abstract description 5
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 98
- 239000000203 mixture Substances 0.000 claims description 89
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Chemical compound O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 claims description 71
- 229920001285 xanthan gum Polymers 0.000 claims description 49
- 239000004615 ingredient Substances 0.000 claims description 48
- 239000000230 xanthan gum Substances 0.000 claims description 47
- 235000010493 xanthan gum Nutrition 0.000 claims description 47
- 229940082509 xanthan gum Drugs 0.000 claims description 47
- 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
- 235000010356 sorbitol Nutrition 0.000 claims description 45
- 239000008213 purified water Substances 0.000 claims description 43
- 108010011485 Aspartame Proteins 0.000 claims description 37
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- 239000000605 aspartame Substances 0.000 claims description 37
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- 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 37
- 239000003973 paint Substances 0.000 claims description 30
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- OWEGMIWEEQEYGQ-UHFFFAOYSA-N 100676-05-9 Natural products OC1C(O)C(O)C(CO)OC1OCC1C(O)C(O)C(O)C(OC2C(OC(O)C(O)C2O)CO)O1 OWEGMIWEEQEYGQ-UHFFFAOYSA-N 0.000 claims description 25
- GUBGYTABKSRVRQ-PICCSMPSSA-N Maltose Natural products O[C@@H]1[C@@H](O)[C@H](O)[C@@H](CO)O[C@@H]1O[C@@H]1[C@@H](CO)OC(O)[C@H](O)[C@H]1O GUBGYTABKSRVRQ-PICCSMPSSA-N 0.000 claims description 25
- 229930006000 Sucrose Natural products 0.000 claims description 24
- 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 24
- 239000005720 sucrose Substances 0.000 claims description 24
- VYPSYNLAJGMNEJ-UHFFFAOYSA-N Silicium dioxide Chemical compound O=[Si]=O VYPSYNLAJGMNEJ-UHFFFAOYSA-N 0.000 claims description 23
- 239000008119 colloidal silica Substances 0.000 claims description 23
- BNIILDVGGAEEIG-UHFFFAOYSA-L disodium hydrogen phosphate Chemical compound [Na+].[Na+].OP([O-])([O-])=O BNIILDVGGAEEIG-UHFFFAOYSA-L 0.000 claims description 23
- 229910000397 disodium phosphate Inorganic materials 0.000 claims description 23
- 235000019800 disodium phosphate Nutrition 0.000 claims description 23
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- 239000001488 sodium phosphate Substances 0.000 claims description 23
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- 235000020357 syrup Nutrition 0.000 claims description 21
- 239000006188 syrup Substances 0.000 claims description 21
- 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 20
- 239000000975 dye Substances 0.000 claims description 20
- KRCMKUNIILUXPF-UHFFFAOYSA-N methyl 4-hydroxybenzoate;sodium Chemical compound [Na].COC(=O)C1=CC=C(O)C=C1 KRCMKUNIILUXPF-UHFFFAOYSA-N 0.000 claims description 19
- 239000008194 pharmaceutical composition Substances 0.000 claims description 19
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- 239000004290 sodium methyl p-hydroxybenzoate Substances 0.000 claims description 19
- 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 18
- 239000000787 lecithin Substances 0.000 claims description 18
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- 229920003088 hydroxypropyl methyl cellulose Polymers 0.000 claims description 17
- 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 17
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- 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
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- 235000010270 methyl p-hydroxybenzoate Nutrition 0.000 claims description 15
- 239000004292 methyl p-hydroxybenzoate Substances 0.000 claims description 15
- 238000011282 treatment Methods 0.000 claims description 14
- LXCFILQKKLGQFO-UHFFFAOYSA-N methylparaben Chemical compound COC(=O)C1=CC=C(O)C=C1 LXCFILQKKLGQFO-UHFFFAOYSA-N 0.000 claims description 13
- QELSKZZBTMNZEB-UHFFFAOYSA-N propylparaben Chemical compound CCCOC(=O)C1=CC=C(O)C=C1 QELSKZZBTMNZEB-UHFFFAOYSA-N 0.000 claims description 13
- 241000167854 Bourreria succulenta Species 0.000 claims description 12
- 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 12
- 235000019693 cherries Nutrition 0.000 claims description 12
- IINNWAYUJNWZRM-UHFFFAOYSA-L erythrosin B Chemical compound [Na+].[Na+].[O-]C(=O)C1=CC=CC=C1C1=C2C=C(I)C(=O)C(I)=C2OC2=C(I)C([O-])=C(I)C=C21 IINNWAYUJNWZRM-UHFFFAOYSA-L 0.000 claims description 12
- 235000012732 erythrosine Nutrition 0.000 claims description 12
- 239000004174 erythrosine Substances 0.000 claims description 12
- 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 11
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- OIQPTROHQCGFEF-UHFFFAOYSA-L chembl1371409 Chemical compound [Na+].[Na+].OC1=CC=C2C=C(S([O-])(=O)=O)C=CC2=C1N=NC1=CC=C(S([O-])(=O)=O)C=C1 OIQPTROHQCGFEF-UHFFFAOYSA-L 0.000 claims description 11
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| US13034393A | 1993-10-01 | 1993-10-01 |
Publications (2)
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| LT96039A LT96039A (en) | 1996-10-25 |
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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 |
| JP2001526246A (ja) * | 1997-12-23 | 2001-12-18 | アライアンス・ファーマスーティカル・コーポレイション | 薬剤送達及び／又は癒着防止のための方法及び組成物 |
| WO2000015210A2 (en) * | 1998-09-14 | 2000-03-23 | Vertex Pharmaceuticals Incorporated | Use of mycophenol acid and its derivatives for the treatment of virus diseases |
| US6410255B1 (en) * | 1999-05-05 | 2002-06-25 | Aurora Biosciences Corporation | Optical probes and assays |
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