NZ723576B2 - Electrolyte purgatives - Google Patents
Electrolyte purgatives Download PDFInfo
- Publication number
- NZ723576B2 NZ723576B2 NZ723576A NZ72357612A NZ723576B2 NZ 723576 B2 NZ723576 B2 NZ 723576B2 NZ 723576 A NZ723576 A NZ 723576A NZ 72357612 A NZ72357612 A NZ 72357612A NZ 723576 B2 NZ723576 B2 NZ 723576B2
- Authority
- NZ
- New Zealand
- Prior art keywords
- composition
- formulation
- water
- soluble
- pharmaceutical composition
- Prior art date
Links
- 239000008141 laxative Substances 0.000 title abstract description 17
- 230000001543 purgative Effects 0.000 title abstract description 16
- 239000003792 electrolyte Substances 0.000 title abstract description 10
- 239000000203 mixture Substances 0.000 claims abstract description 78
- BPKUDUSVDVLOPY-UHFFFAOYSA-N Bisoxatin Chemical compound C1=CC(O)=CC=C1C1(C=2C=CC(O)=CC=2)C(=O)NC2=CC=CC=C2O1 BPKUDUSVDVLOPY-UHFFFAOYSA-N 0.000 claims abstract description 21
- 229960002875 bisoxatin Drugs 0.000 claims abstract description 17
- 159000000001 potassium salts Chemical class 0.000 claims abstract description 14
- 159000000000 sodium salts Chemical class 0.000 claims abstract description 13
- PMZURENOXWZQFD-UHFFFAOYSA-L na2so4 Chemical compound [Na+].[Na+].[O-]S([O-])(=O)=O PMZURENOXWZQFD-UHFFFAOYSA-L 0.000 claims abstract description 12
- 159000000003 magnesium salts Chemical class 0.000 claims abstract description 10
- CSNNHWWHGAXBCP-UHFFFAOYSA-L mgso4 Chemical compound [Mg+2].[O-][S+2]([O-])([O-])[O-] CSNNHWWHGAXBCP-UHFFFAOYSA-L 0.000 claims abstract description 8
- GOZDTZWAMGHLDY-UHFFFAOYSA-L Sodium picosulfate Chemical compound [Na+].[Na+].C1=CC(OS(=O)(=O)[O-])=CC=C1C(C=1N=CC=CC=1)C1=CC=C(OS([O-])(=O)=O)C=C1 GOZDTZWAMGHLDY-UHFFFAOYSA-L 0.000 claims abstract description 7
- ZCBJDQBSLZREAA-UHFFFAOYSA-N [4-[2-(4-acetyloxyphenyl)-3-oxo-4H-1,4-benzoxazin-2-yl]phenyl] acetate Chemical compound C1=CC(OC(=O)C)=CC=C1C1(C=2C=CC(OC(C)=O)=CC=2)C(=O)NC2=CC=CC=C2O1 ZCBJDQBSLZREAA-UHFFFAOYSA-N 0.000 claims abstract description 7
- 229950009290 bisoxatin acetate Drugs 0.000 claims abstract description 7
- 210000001072 Colon Anatomy 0.000 claims abstract description 6
- UNXHWFMMPAWVPI-QWWZWVQMSA-N D-Threitol Natural products OC[C@@H](O)[C@H](O)CO UNXHWFMMPAWVPI-QWWZWVQMSA-N 0.000 claims abstract description 6
- 229940009714 Erythritol Drugs 0.000 claims abstract description 6
- 239000004386 Erythritol Substances 0.000 claims abstract description 6
- UNXHWFMMPAWVPI-ZXZARUISSA-N Erythritol Chemical compound OC[C@H](O)[C@H](O)CO UNXHWFMMPAWVPI-ZXZARUISSA-N 0.000 claims abstract description 6
- 235000019414 erythritol Nutrition 0.000 claims abstract description 6
- 230000001939 inductive effect Effects 0.000 claims abstract description 6
- 229910052938 sodium sulfate Inorganic materials 0.000 claims abstract description 6
- 235000011152 sodium sulphate Nutrition 0.000 claims abstract description 6
- OTYBMLCTZGSZBG-UHFFFAOYSA-L Potassium sulfate Chemical compound [K+].[K+].[O-]S([O-])(=O)=O OTYBMLCTZGSZBG-UHFFFAOYSA-L 0.000 claims abstract description 5
- 229910052939 potassium sulfate Inorganic materials 0.000 claims abstract description 5
- 235000011151 potassium sulphates Nutrition 0.000 claims abstract description 5
- 239000004615 ingredient Substances 0.000 claims abstract description 4
- 229910052943 magnesium sulfate Inorganic materials 0.000 claims abstract description 4
- 235000019341 magnesium sulphate Nutrition 0.000 claims abstract description 4
- 239000011780 sodium chloride Substances 0.000 claims abstract description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims description 60
- 229960005077 Sodium Picosulfate Drugs 0.000 claims description 3
- 239000012530 fluid Substances 0.000 claims description 3
- 238000009472 formulation Methods 0.000 claims description 2
- 229910001425 magnesium ion Inorganic materials 0.000 claims 4
- 229910001415 sodium ion Inorganic materials 0.000 claims 4
- YVPYQUNUQOZFHG-UHFFFAOYSA-N Diatrizoic acid Chemical compound CC(=O)NC1=C(I)C(NC(C)=O)=C(I)C(C(O)=O)=C1I YVPYQUNUQOZFHG-UHFFFAOYSA-N 0.000 claims 3
- 229960005423 diatrizoate Drugs 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-K 2qpq Chemical compound [O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O KRKNYBCHXYNGOX-UHFFFAOYSA-K 0.000 claims 2
- QTBSBXVTEAMEQO-UHFFFAOYSA-M acetate Chemical compound CC([O-])=O QTBSBXVTEAMEQO-UHFFFAOYSA-M 0.000 claims 2
- 239000000654 additive Substances 0.000 claims 2
- OVBPIULPVIDEAO-LBPRGKRZSA-N folic acid Chemical compound C=1N=C2NC(N)=NC(=O)C2=NC=1CNC1=CC=C(C(=O)N[C@@H](CCC(O)=O)C(O)=O)C=C1 OVBPIULPVIDEAO-LBPRGKRZSA-N 0.000 claims 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-M lactate Chemical compound CC(O)C([O-])=O JVTAAEKCZFNVCJ-UHFFFAOYSA-M 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- WCUXLLCKKVVCTQ-UHFFFAOYSA-M potassium chloride Chemical compound [Cl-].[K+] WCUXLLCKKVVCTQ-UHFFFAOYSA-M 0.000 claims 2
- FAPWRFPIFSIZLT-UHFFFAOYSA-M sodium chloride Chemical compound [Na+].[Cl-] FAPWRFPIFSIZLT-UHFFFAOYSA-M 0.000 claims 2
- AOHMFUYIHARAGR-UHFFFAOYSA-N 2-hydroxypropane-1,2,3-tricarboxylic acid;magnesium Chemical compound [Mg].[Mg].[Mg].OC(=O)CC(O)(C(O)=O)CC(O)=O.OC(=O)CC(O)(C(O)=O)CC(O)=O AOHMFUYIHARAGR-UHFFFAOYSA-N 0.000 claims 1
- 229940039231 CONTRAST MEDIA Drugs 0.000 claims 1
- 229960000304 Folic Acid Drugs 0.000 claims 1
- NTHXOOBQLCIOLC-UHFFFAOYSA-N Iohexol Chemical compound OCC(O)CN(C(=O)C)C1=C(I)C(C(=O)NCC(O)CO)=C(I)C(C(=O)NCC(O)CO)=C1I NTHXOOBQLCIOLC-UHFFFAOYSA-N 0.000 claims 1
- 229960004647 Iopamidol Drugs 0.000 claims 1
- UUMLTINZBQPNGF-UHFFFAOYSA-N Ioxilan Chemical compound OCC(O)CN(C(=O)C)C1=C(I)C(C(=O)NCCO)=C(I)C(C(=O)NCC(O)CO)=C1I UUMLTINZBQPNGF-UHFFFAOYSA-N 0.000 claims 1
- GVALZJMUIHGIMD-UHFFFAOYSA-H Magnesium phosphate tribasic Chemical compound [Mg+2].[Mg+2].[Mg+2].[O-]P([O-])([O-])=O.[O-]P([O-])([O-])=O GVALZJMUIHGIMD-UHFFFAOYSA-H 0.000 claims 1
- GGGDNPWHMNJRFN-UHFFFAOYSA-N Metrizoic acid Chemical compound CC(=O)N(C)C1=C(I)C(NC(C)=O)=C(I)C(C(O)=O)=C1I GGGDNPWHMNJRFN-UHFFFAOYSA-N 0.000 claims 1
- AVTYONGGKAJVTE-UHFFFAOYSA-L Potassium tartrate Chemical compound [K+].[K+].[O-]C(=O)C(O)C(O)C([O-])=O AVTYONGGKAJVTE-UHFFFAOYSA-L 0.000 claims 1
- 229940111695 Potassium tartrate Drugs 0.000 claims 1
- UPMFZISCCZSDND-JJKGCWMISA-M Sodium gluconate Chemical compound [Na+].OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O UPMFZISCCZSDND-JJKGCWMISA-M 0.000 claims 1
- 229940005574 Sodium gluconate Drugs 0.000 claims 1
- JZRWCGZRTZMZEH-UHFFFAOYSA-N Thiamine Natural products CC1=C(CCO)SC=[N+]1CC1=CN=C(C)N=C1N JZRWCGZRTZMZEH-UHFFFAOYSA-N 0.000 claims 1
- HRXKRNGNAMMEHJ-UHFFFAOYSA-K Trisodium citrate Chemical compound [Na+].[Na+].[Na+].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O HRXKRNGNAMMEHJ-UHFFFAOYSA-K 0.000 claims 1
- 229940045997 Vitamin A Drugs 0.000 claims 1
- FPIPGXGPPPQFEQ-BOOMUCAASA-N Vitamin A Natural products OC/C=C(/C)\C=C\C=C(\C)/C=C/C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-BOOMUCAASA-N 0.000 claims 1
- 229940046001 Vitamin B Complex Drugs 0.000 claims 1
- 229930003268 Vitamin C Natural products 0.000 claims 1
- 229940046009 Vitamin E Drugs 0.000 claims 1
- 229930003427 Vitamin E Natural products 0.000 claims 1
- 230000000996 additive Effects 0.000 claims 1
- FPIPGXGPPPQFEQ-OVSJKPMPSA-N all-trans-retinol Chemical compound OC\C=C(/C)\C=C\C=C(/C)\C=C\C1=C(C)CCCC1(C)C FPIPGXGPPPQFEQ-OVSJKPMPSA-N 0.000 claims 1
- 125000000129 anionic group Chemical group 0.000 claims 1
- 229910052788 barium Inorganic materials 0.000 claims 1
- DSAJWYNOEDNPEQ-UHFFFAOYSA-N barium(0) Chemical compound [Ba] DSAJWYNOEDNPEQ-UHFFFAOYSA-N 0.000 claims 1
- YBJHBAHKTGYVGT-ZKWXMUAHSA-N biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 claims 1
- 229960002685 biotin Drugs 0.000 claims 1
- 235000020958 biotin Nutrition 0.000 claims 1
- 239000011616 biotin Substances 0.000 claims 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims 1
- 239000011575 calcium Substances 0.000 claims 1
- 229910052791 calcium Inorganic materials 0.000 claims 1
- 239000002775 capsule Substances 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 239000002872 contrast media Substances 0.000 claims 1
- 229960005223 diatrizoic acid Drugs 0.000 claims 1
- 235000016693 dipotassium tartrate Nutrition 0.000 claims 1
- XMXOIHIZTOVVFB-JIZZDEOASA-L disodium;(2S)-2-aminobutanedioate Chemical compound [Na+].[Na+].[O-]C(=O)[C@@H](N)CC([O-])=O XMXOIHIZTOVVFB-JIZZDEOASA-L 0.000 claims 1
- 235000019152 folic acid Nutrition 0.000 claims 1
- 239000011724 folic acid Substances 0.000 claims 1
- 239000007897 gelcap Substances 0.000 claims 1
- PNDPGZBMCMUPRI-UHFFFAOYSA-N iodine Chemical compound II PNDPGZBMCMUPRI-UHFFFAOYSA-N 0.000 claims 1
- 239000011630 iodine Substances 0.000 claims 1
- 229910052740 iodine Inorganic materials 0.000 claims 1
- 229960004359 iodixanol Drugs 0.000 claims 1
- NBQNWMBBSKPBAY-UHFFFAOYSA-N iodixanol Chemical compound IC=1C(C(=O)NCC(O)CO)=C(I)C(C(=O)NCC(O)CO)=C(I)C=1N(C(=O)C)CC(O)CN(C(C)=O)C1=C(I)C(C(=O)NCC(O)CO)=C(I)C(C(=O)NCC(O)CO)=C1I NBQNWMBBSKPBAY-UHFFFAOYSA-N 0.000 claims 1
- 229960001025 iohexol Drugs 0.000 claims 1
- XQZXYNRDCRIARQ-LURJTMIESA-N iopamidol Chemical compound C[C@H](O)C(=O)NC1=C(I)C(C(=O)NC(CO)CO)=C(I)C(C(=O)NC(CO)CO)=C1I XQZXYNRDCRIARQ-LURJTMIESA-N 0.000 claims 1
- 229960002611 ioxilan Drugs 0.000 claims 1
- 239000007788 liquid Substances 0.000 claims 1
- 239000000314 lubricant Substances 0.000 claims 1
- 239000004337 magnesium citrate Substances 0.000 claims 1
- 229960005336 magnesium citrate Drugs 0.000 claims 1
- 235000002538 magnesium citrate Nutrition 0.000 claims 1
- 239000004137 magnesium phosphate Substances 0.000 claims 1
- 229960002261 magnesium phosphate Drugs 0.000 claims 1
- 229910000157 magnesium phosphate Inorganic materials 0.000 claims 1
- 235000010994 magnesium phosphates Nutrition 0.000 claims 1
- 239000003550 marker Substances 0.000 claims 1
- 229960004712 metrizoic acid Drugs 0.000 claims 1
- 235000016709 nutrition Nutrition 0.000 claims 1
- 239000001103 potassium chloride Substances 0.000 claims 1
- 235000011164 potassium chloride Nutrition 0.000 claims 1
- 239000001472 potassium tartrate Substances 0.000 claims 1
- 229960003471 retinol Drugs 0.000 claims 1
- 239000001509 sodium citrate Substances 0.000 claims 1
- 239000000176 sodium gluconate Substances 0.000 claims 1
- 235000012207 sodium gluconate Nutrition 0.000 claims 1
- 235000014347 soups Nutrition 0.000 claims 1
- 239000004094 surface-active agent Substances 0.000 claims 1
- 239000003826 tablet Substances 0.000 claims 1
- 235000019157 thiamine Nutrition 0.000 claims 1
- KYMBYSLLVAOCFI-UHFFFAOYSA-N thiamine Chemical compound CC1=C(CCO)SCN1CC1=CN=C(C)N=C1N KYMBYSLLVAOCFI-UHFFFAOYSA-N 0.000 claims 1
- 229960003495 thiamine Drugs 0.000 claims 1
- 239000011721 thiamine Substances 0.000 claims 1
- 239000011573 trace mineral Substances 0.000 claims 1
- 235000013619 trace mineral Nutrition 0.000 claims 1
- 239000011778 trisodium citrate Substances 0.000 claims 1
- 235000019155 vitamin A Nutrition 0.000 claims 1
- 239000011719 vitamin A Substances 0.000 claims 1
- 235000019156 vitamin B Nutrition 0.000 claims 1
- 239000011720 vitamin B Substances 0.000 claims 1
- 235000019154 vitamin C Nutrition 0.000 claims 1
- 239000011718 vitamin C Substances 0.000 claims 1
- 150000003700 vitamin C derivatives Chemical class 0.000 claims 1
- 235000019165 vitamin E Nutrition 0.000 claims 1
- 239000011709 vitamin E Substances 0.000 claims 1
- 150000003712 vitamin E derivatives Chemical class 0.000 claims 1
- HCHKCACWOHOZIP-UHFFFAOYSA-N zinc Chemical compound [Zn] HCHKCACWOHOZIP-UHFFFAOYSA-N 0.000 claims 1
- 239000011701 zinc Substances 0.000 claims 1
- 229910052725 zinc Inorganic materials 0.000 claims 1
- 235000000346 sugar Nutrition 0.000 abstract description 12
- SRBFZHDQGSBBOR-SQOUGZDYSA-N Xylose Natural products O[C@@H]1CO[C@@H](O)[C@@H](O)[C@@H]1O SRBFZHDQGSBBOR-SQOUGZDYSA-N 0.000 abstract description 8
- 229960003487 Xylose Drugs 0.000 abstract description 4
- 239000001120 potassium sulphate Substances 0.000 abstract description 4
- KEAYESYHFKHZAL-UHFFFAOYSA-N sodium Chemical compound [Na] KEAYESYHFKHZAL-UHFFFAOYSA-N 0.000 abstract description 4
- 239000011734 sodium Substances 0.000 abstract description 4
- 229910052708 sodium Inorganic materials 0.000 abstract description 4
- 239000004902 Softening Agent Substances 0.000 abstract description 3
- 239000003599 detergent Substances 0.000 abstract description 3
- 239000000975 dye Substances 0.000 abstract description 3
- 150000003839 salts Chemical class 0.000 abstract description 3
- 150000008163 sugars Chemical class 0.000 abstract description 3
- FYYHWMGAXLPEAU-UHFFFAOYSA-N magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 abstract 2
- 239000011777 magnesium Substances 0.000 abstract 2
- 229910052749 magnesium Inorganic materials 0.000 abstract 2
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 abstract 2
- 239000011591 potassium Substances 0.000 abstract 2
- 229910052700 potassium Inorganic materials 0.000 abstract 2
- 239000000243 solution Substances 0.000 description 4
- 229920001223 polyethylene glycol Polymers 0.000 description 3
- 208000005577 Gastroenteritis Diseases 0.000 description 2
- 230000000642 iatrogenic Effects 0.000 description 2
- 230000002746 orthostatic Effects 0.000 description 2
- 239000001488 sodium phosphate Substances 0.000 description 2
- 229910000162 sodium phosphate Inorganic materials 0.000 description 2
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 2
- WQZGKKKJIJFFOK-GASJEMHNSA-N D-Glucose Natural products OC[C@H]1OC(O)[C@H](O)[C@@H](O)[C@@H]1O WQZGKKKJIJFFOK-GASJEMHNSA-N 0.000 description 1
- FBPFZTCFMRRESA-KAZBKCHUSA-N D-Mannitol Natural products OC[C@@H](O)[C@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KAZBKCHUSA-N 0.000 description 1
- 206010012735 Diarrhoea Diseases 0.000 description 1
- 206010014418 Electrolyte imbalance Diseases 0.000 description 1
- 102000018711 Facilitative Glucose Transport Proteins Human genes 0.000 description 1
- 108010027279 Facilitative Glucose Transport Proteins Proteins 0.000 description 1
- 229940056944 Golytely Drugs 0.000 description 1
- 239000004705 High-molecular-weight polyethylene Substances 0.000 description 1
- 206010021036 Hyponatraemia Diseases 0.000 description 1
- 210000000936 Intestines Anatomy 0.000 description 1
- FBPFZTCFMRRESA-KVTDHHQDSA-N Mannitol Chemical compound OC[C@@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-KVTDHHQDSA-N 0.000 description 1
- UIIMBOGNXHQVGW-UHFFFAOYSA-M NaHCO3 Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 description 1
- 240000007594 Oryza sativa Species 0.000 description 1
- 235000007164 Oryza sativa Nutrition 0.000 description 1
- 206010047700 Vomiting Diseases 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 230000000112 colonic Effects 0.000 description 1
- 238000002052 colonoscopy Methods 0.000 description 1
- 238000006297 dehydration reaction Methods 0.000 description 1
- 201000008286 diarrhea Diseases 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 235000021255 galacto-oligosaccharides Nutrition 0.000 description 1
- 150000003271 galactooligosaccharides Chemical class 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 230000003284 homeostatic Effects 0.000 description 1
- 239000000815 hypotonic solution Substances 0.000 description 1
- 239000000644 isotonic solution Substances 0.000 description 1
- 239000000594 mannitol Substances 0.000 description 1
- 235000010355 mannitol Nutrition 0.000 description 1
- 229940021222 peritoneal dialysis Isotonic solutions Drugs 0.000 description 1
- 238000002360 preparation method Methods 0.000 description 1
- 235000009566 rice Nutrition 0.000 description 1
- 230000028327 secretion Effects 0.000 description 1
- 231100000486 side effect Toxicity 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
-
- A—HUMAN NECESSITIES
- A23—FOODS OR FOODSTUFFS; TREATMENT THEREOF, NOT COVERED BY OTHER CLASSES
- A23L—FOODS, FOODSTUFFS, OR NON-ALCOHOLIC BEVERAGES, NOT COVERED BY SUBCLASSES A21D OR A23B-A23J; THEIR PREPARATION OR TREATMENT, e.g. COOKING, MODIFICATION OF NUTRITIVE QUALITIES, PHYSICAL TREATMENT; PRESERVATION OF FOODS OR FOODSTUFFS, IN GENERAL
- A23L33/00—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof
- A23L33/10—Modifying nutritive qualities of foods; Dietetic products; Preparation or treatment thereof using additives
- A23L33/16—Inorganic salts, minerals or trace elements
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K2300/00—Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/538—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with carbocyclic ring systems
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
-
- 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
- A61K31/70—Carbohydrates; Sugars; Derivatives thereof
- A61K31/7004—Monosaccharides having only carbon, hydrogen and oxygen atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/06—Aluminium, calcium or magnesium; Compounds thereof, e.g. clay
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K33/00—Medicinal preparations containing inorganic active ingredients
- A61K33/14—Alkali metal chlorides; Alkaline earth metal chlorides
-
- 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
- A61K47/02—Inorganic 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
- A61K47/06—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
- A61K47/10—Alcohols; Phenols; Salts thereof, e.g. glycerol; Polyethylene glycols [PEG]; Poloxamers; PEG/POE alkyl ethers
-
- 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
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
- A61P1/10—Laxatives
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
-
- Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02A—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE
- Y02A50/00—TECHNOLOGIES FOR ADAPTATION TO CLIMATE CHANGE in human health protection, e.g. against extreme weather
- Y02A50/30—Against vector-borne diseases, e.g. mosquito-borne, fly-borne, tick-borne or waterborne diseases whose impact is exacerbated by climate change
Abstract
The disclosure provides compositions for use in purgatives, for use as purgatives, and to methods for inducing purgation of the colon. The composition comprising between 1 and 20 grams of at least one water-soluble sodium salt; between 0.1 and 4.8 grams of at least one water-soluble potassium salt; between 0.1 and 7 grams of at least one water-soluble magnesium salt; erythritol; and a bisoxatin (or 2,2-bis(4-hydroxyphenyl)-2H-benzo[b][1,4]oxazin-3(4H)-one), or bisoxatin acetate, or equivalent. In alternative embodiments, the disclosure provides compositions, e.g., a purgative, comprising: a water-soluble sodium salt (especially sodium sulphate), a water-soluble potassium salt (especially potassium sulphate), and a water-soluble magnesium salt (especially magnesium sulphate); and, compositions further comprising: a bisoxatin, or a detergent stool softening agent (such as sodium picosulphate) and/or a water-soluble sugar (such as xylose or equivalent); or, compositions having these ingredients at different amounts, but at equivalent proportions. In alternative embodiments, the disclosure provides purgative compositions comprising electrolytes, salts, sugars, bisoxatin, dyes and biofilm disruptors. An example of a composition comprises bisoxatin, sodium, potassium and magnesium electrolytes and erythritol. t; between 0.1 and 7 grams of at least one water-soluble magnesium salt; erythritol; and a bisoxatin (or 2,2-bis(4-hydroxyphenyl)-2H-benzo[b][1,4]oxazin-3(4H)-one), or bisoxatin acetate, or equivalent. In alternative embodiments, the disclosure provides compositions, e.g., a purgative, comprising: a water-soluble sodium salt (especially sodium sulphate), a water-soluble potassium salt (especially potassium sulphate), and a water-soluble magnesium salt (especially magnesium sulphate); and, compositions further comprising: a bisoxatin, or a detergent stool softening agent (such as sodium picosulphate) and/or a water-soluble sugar (such as xylose or equivalent); or, compositions having these ingredients at different amounts, but at equivalent proportions. In alternative embodiments, the disclosure provides purgative compositions comprising electrolytes, salts, sugars, bisoxatin, dyes and biofilm disruptors. An example of a composition comprises bisoxatin, sodium, potassium and magnesium electrolytes and erythritol.
Description
ELECTROLYTE PURGATIVES
CROSS-REFERENCE TO RELATED APPLICATIONS
This application is a divisional of New Zealand Patent Application No. 624088 (national
phase of ) claiming priority to USSN 61/552,431 filed 27 October
2011 and to USSN 61/717,599 filed 23 October 2012, the entire contents of each of which
is incorporated herein by reference.
FIELD OF THE INVENTION
The invention provides compositions for use in purgatives, for use as purgatives, and to
methods for inducing purgation of the colon. In alternative embodiments, the invention
provides compositions, e.g., a purgative, comprising: a sodium sulphate, a potassium
sulphate, and a magnesium sulphate; and, compositions further comprising: a bisoxatin, or
a sodium picosulphate and/or a xylose or equivalent; or, compositions having these
ingredients at different amounts, but at equivalent proportions. In alternative embodiments,
the invention provides purgative compositions comprising electrolytes, salts, sugars,
bisoxatin, dyes and biofilm disruptors.
BACKGROUND ART
Colonic orthostatic lavage is an iatrogenic phenomenon related to the administration of a
purgative and therefore is predictable in its action and side effects. It is important to make
the distinction between the use of iatrogenic purgation solutions and fluid/electrolyte
replacement solutions used for treatment of vomiting and diarrhea associated with
gastroenteritis. The use of mainly hypotonic or isotonic solutions such as glucose-based '
Bangladesh' solution and rice-based solutions has been successful in patients with
gastroenteritis and dehydration, a highly unpredictable disease. The physiological principle
of coupled sodium and glucose transport in a 1 : 1 molar ratio in the intestine has been
shown to be safe and effective.
Purgatives developed to date for orthostatic lavage to clean the bowel of faecal matter prior
to colonoscopy have taken the form of either an isotonic, large volume lavage (e.g.
Braintree's Golytely) or more hypertonic lavage products such as Fleet's sodium phosphate
or sodium picosulfate (Picolax) products. The former generally cause little homeostatic
disturbance of intra-vascular sodium and other electrolytes or fluid shifts because of their
isotonic nature, which minimizes electrolyte absorption/secretion by the presence of high
molecular weight polyethylene glycol (PEG mw 3350). However, these preparations have
recently been reported to be associated with hyponatremia (Cohen D. C. et al., Lancet
357(9252): 282-283 (2001)). Products with sodium phosphate and sodium picosulfate are
felt to be better tolerated (Fincher R.K., et al., Am. J. Gastroenterol. 94(8): 2122-7 (1999)).
However, these products have also been associated with a significant hypo-osmolar state
and electrolyte imbalance,
bisoxatin, or between about 100, 110, 120, 130, 140 or 150 mg to about 1, 2, 3, 4, 4.5 or 5
grams (g) or more bisoxatin (e.g., for a constipated patient).
In one aspect of the present invention, there is provided a composition, a pharmaceutical
composition or a formulation, comprising:
between about 1 to about 20 grams of at least one water-soluble sodium salt;
between about 0.1 to about 4.8 grams of at least one water-soluble potassium
salt;
between about 0.1 to about 7 grams of at least one water-soluble magnesium
salt;
erythritol;
and a bisoxatin (or 2,2-bis(4-hydroxyphenyl)-2H-benzo[b][1,4]oxazin-3(4H)-
one), or bisoxatin acetate, or equivalent.
In alternative embodiments, the invention provides compositions, pharmaceutical
compositions or formulations (e.g., as a purgative), comprising
(a) (i) 1 to about 10 gram per unit dose, or between about 1 to 10 gram per unit dose, or
about 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 17.5, 18, 19 or 20
or more gram per unit dose, of at least one water-soluble sodium salt;
(ii) 1 or 2 to about 20 gram per unit dose, or between about 1 to 20 gram per unit
dose, or about 0.5, 1, 2, 3, 4, 5, 6, 7, 8, 9, 10, 11, 12, 13, 14, 15, 16, 17, 18, 19 or
or more gram per unit dose, of at least one water-soluble sugar, or a
water-soluble degradable sugar, or alternatively, a minimally degradable sugar;
(iii) 0.5 to about 5 gram per unit dose, or between about 0.5 to 10 gram per unit dose,
or about 0.1, 0.2, 0.3, 0.4, 0.5, 1.0, 2, 3, 3.1, 3.2, 3.3, 3.4, 3.5, 4, 5, 6, 7, 8, 9, or
or more gram per unit dose, of at least one water-soluble potassium salt;
(iv) 1 to about 10 gram per unit dose, or between about 1 to 10 gram per unit dose, or
about 0.1, 0.2, 0.3, 0.4, 0.5, 0.6, 0.7, 0.8, 0.9, 1.0, 2, 3, 4, 5, 6, 7, 8, 9 or 10 or
more gram per unit dose, of at least one water-soluble magnesium salt; and
(v) a detergent stool softening agent;
wherein the composition is a hypertonic composition, optionally in the form of a unit
dose having a volume of from about 0.2 to about 0.5 liter (L), or dose having a volume of
about 0.1, 0.2, 0.3, 0.4, 0.5, 0.6 or more L,
and wherein optionally the sugar, or the degradable sugar, or the minimally degradable
sugar, comprises a xylose, a xy1otriose, a mannitol, a xylooligosaccharide, a
fructoo1igosaccharide, a fructosan, a galactooligosaccharide, an equivalent degradable
sugar thereof or a mixture thereof;
(b) the composition, pharmaceutical composition, or formulation, of (a), wherein
the composition is a purgative or a purgative composition;
(c) the composition of (a) or (b), wherein the composition comprises:
a sodium sulphate at a per unit dose of about 17.5 gram (g), or between about 2 to about
37 gram,
a potassium sulphate at a per unit dose of about 3.13 g, or between about 0.1 to about
4.8 g, and
WE
Claims (28)
1. A composition, a pharmaceutical composition or a formulation, comprising: between about 1 to about 20 grams of at least one water-soluble sodium salt; between about 0.1 to about 4.8 grams of at least one water-soluble potassium salt; between about 0.1 to about 7 grams of at least one water-soluble magnesium salt; erythritol; and a bisoxatin (or 2,2-bis(4-hydroxyphenyl)-2H-benzo[b][1,4]oxazin-3(4H)- one), or bisoxatin acetate, or equivalent.
2. The composition, pharmaceutical composition or formulation of Claim 1, wherein the composition comprises between about 10 milligrams to about 5 or more grams of bisoxatin, bisoxatin acetate or equivalent.
3. The composition, pharmaceutical composition or formulation of Claim 1, wherein the composition comprises between about 75 milligrams to about 200 milligrams of bisoxatin, bisoxatin acetate or equivalent.
4. The composition, pharmaceutical composition or formulation of Claim 1, wherein the composition comprises between about 100 milligrams to about 5 grams or more of bisoxatin, bisoxatin acetate or equivalent.
5. The composition, pharmaceutical composition or formulation of any one of Claims 1 to 4, wherein the weight of the water-soluble potassium salt in the composition is from about 0.05 to about 1 times the weight of the water-soluble sodium salt in the composition.
6. The composition, pharmaceutical composition or formulation of any one of Claims 1 to 4, wherein the ratio of the water-soluble potassium salt to the water-soluble sodium salt in the composition is from about 1:1 to about 1:8.
7. The composition, pharmaceutical composition or formulation of any one of Claims 1 to 4 or 6, wherein the ratio of the potassium salt to sodium salt in the composition is from about 1:1.5 to about 1:6.
8. The composition, pharmaceutical composition or formulation of any one of Claims 1 to 4 or 6 or 7, wherein the ratio of the potassium salt to sodium salt in the composition is from about 1:2 to about 1:5.
9. The composition, pharmaceutical composition or formulation of any one of Claims 1 to 4 or 6 to 8, wherein the ratio of the potassium salt to sodium salt in the composition is about 1:3.
10. The composition, pharmaceutical composition or formulation of any one of Claims 1 to 9, wherein the at least one water-soluble potassium salt is present in an amount of from about 0.5 gram to 4.8 grams per unit dose.
11. The composition, pharmaceutical composition or formulation of any one of Claims 1 to 10, wherein the at least one potassium salt is present in an amount of from about 1 gram to 4.8 grams per unit dose.
12. The composition, pharmaceutical composition or formulation according to any one of Claims 1 to 11, wherein the weight of magnesium ions to the weight of sodium ions in the composition is from about 1:5 to about 5:1.
13. The composition, pharmaceutical composition or formulation of any one of Claims 1 to 12, wherein the weight of magnesium ions to the weight of sodium ions in the composition is from about 1:3 to about 3:1.
14. The composition, pharmaceutical composition or formulation of any one of Claims 1 to 13, wherein the weight of magnesium ions to the weight of sodium ions in the composition is from about 1:2 to about 2:1.
15. The composition, pharmaceutical composition or formulation of any one of Claims 1 to 14, wherein the weight of magnesium ions to the weight of sodium ions in the composition is about 1:1.
16. The composition, pharmaceutical composition or formulation according to any one of Claims 1 to 15, wherein the at least one water-soluble magnesium salt is present in an amount of from about 1 gram to about 7 grams per unit dose.
17. The composition, pharmaceutical composition or formulation of any one of Claims 1 to 16, wherein the at least one water-soluble magnesium salt is present in an amount of from about 3 grams to 5 grams per unit dose.
18. The composition, pharmaceutical composition or formulation of any one of claims 1 to 17, wherein: the water-soluble sodium salt is selected from the group consisting of a sodium sulphate, a sodium chloride, a sodium gluconate, a sodium citrate, a sodium aspartate and mixtures thereof; the water-soluble potassium salt is selected from the group consisting of a potassium sulfate, a potassium chloride, a potassium tartrate, and mixtures thereof; or the water-soluble magnesium salt is selected from the group consisting of a magnesium sulfate, a magnesium citrate, a magnesium phosphate, and mixtures thereof.
19. The composition, pharmaceutical composition or formulation of any one of claims 1 to 18, wherein the water-soluble sodium salt comprises a sodium picosulfate, a sodium sulphate, or a combination thereof.
20. The composition, pharmaceutical composition or formulation of any one of claims 1 to 19, further comprising at least one composition or additive selected from the group consisting of a flavoring ingredient, citrate, lactate, acetate, a trace element and a nutritional element.
21. The composition, pharmaceutical composition or formulation of any one of claims 1 to 20, further comprising one or more compositions or additives selected from the group consisting of a citrate, a lactate, an acetate, a calcium, a zinc, a Vitamin B complex, a thiamine, a Vitamin A, a Vitamin C, a Vitamin E, a folic acid and a biotin.
22. The composition, pharmaceutical composition or formulation of any one of claims 1 to 21, in the form of, or formulated as a liquid, a fluid, a soup or soup-like composition; or formulated as a sachet or plurality of sachets; or in the form of a plurality of tablets, gel caps, or capsules.
23. The composition, pharmaceutical composition or formulation of any one of claims 1 to 22, further comprising one or more of a contrast media, a barium or an iodine comprising composition or product, a diatrizoate, a metrizoate, an ioxalgate, an iopamidol, an iohexol, an ioxilan, an iopramide, an iodixanol, and/or a diatrizoic acid or its anionic form diatrizoate.
24. The composition, pharmaceutical composition or formulation of any one of claims 1 to 23, further comprising: a dye or vital stain or marker, a surfactant, a lubricant and/ or a biofilm disrupting compound.
25. A composition, pharmaceutical composition or formulation according to any one of claims 1 to 24 for use in inducing purgation of the colon of a patient in need thereof.
26. A composition, pharmaceutical composition or formulation according to any one of claims 1 to 24 for use in inducing pre-surgical lavage of the colon of a patient in need thereof.
27. Use of a composition, pharmaceutical composition or formulation according to any one of claims 1 to 24, for the manufacture of a medicament for use in inducing a pre-surgical lavage of the colon of a patient in need thereof.
28. Use of a composition, pharmaceutical composition or formulation according to any one of claims 1 to 24, for the manufacture of a medicament for use in inducing purgation of the colon of a patient in need thereof. Salix Pharmaceuticals, Inc. By the Attorneys for the Applicant SPRUSON & FERGUSON Per:
Applications Claiming Priority (5)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201161552431P | 2011-10-27 | 2011-10-27 | |
US61/552,431 | 2011-10-27 | ||
US201261717599P | 2012-10-23 | 2012-10-23 | |
US61/717,599 | 2012-10-23 | ||
NZ624088A NZ624088B2 (en) | 2011-10-27 | 2012-10-27 | Electrolyte purgatives |
Publications (2)
Publication Number | Publication Date |
---|---|
NZ723576A NZ723576A (en) | 2018-07-27 |
NZ723576B2 true NZ723576B2 (en) | 2018-10-30 |
Family
ID=
Similar Documents
Publication | Publication Date | Title |
---|---|---|
JP7277396B2 (en) | Compositions containing PEG and ascorbate | |
KR101947720B1 (en) | Gastric and colonic formulations and methods for making and using them | |
AU2016213892B2 (en) | Electrolyte purgatives | |
RU2013138672A (en) | METHOD, COMPOSITION AND KIT FOR CLEANING THE INTESTINES | |
JP2015510491A5 (en) | ||
PT2322190E (en) | Compositions for bowel cleansing and use thereof | |
KR101981069B1 (en) | Bowel cleansing composition | |
US10617761B2 (en) | Compositions and solutions for colon cleansing | |
NZ723576B2 (en) | Electrolyte purgatives | |
KR20150085698A (en) | Laxative composition for colon cleansing | |
IES20130273A2 (en) | Compositions comprising PEG and ascorbate |