DE29910454U1 - Agents for the therapy of hyperphosphataemia - Google Patents
Agents for the therapy of hyperphosphataemiaInfo
- Publication number
- DE29910454U1 DE29910454U1 DE29910454U DE29910454U DE29910454U1 DE 29910454 U1 DE29910454 U1 DE 29910454U1 DE 29910454 U DE29910454 U DE 29910454U DE 29910454 U DE29910454 U DE 29910454U DE 29910454 U1 DE29910454 U1 DE 29910454U1
- Authority
- DE
- Germany
- Prior art keywords
- calcium
- magnesium
- salts
- agent according
- dosage forms
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
- 201000005991 hyperphosphatemia Diseases 0.000 title claims description 7
- 238000002560 therapeutic procedure Methods 0.000 title 1
- 239000011575 calcium Substances 0.000 claims description 27
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims description 26
- 229910052791 calcium Inorganic materials 0.000 claims description 21
- 239000011777 magnesium Substances 0.000 claims description 21
- FYYHWMGAXLPEAU-UHFFFAOYSA-N Magnesium Chemical compound [Mg] FYYHWMGAXLPEAU-UHFFFAOYSA-N 0.000 claims description 19
- 229910052749 magnesium Inorganic materials 0.000 claims description 19
- 229940091250 magnesium supplement Drugs 0.000 claims description 19
- 229960005069 calcium Drugs 0.000 claims description 18
- 239000003795 chemical substances by application Substances 0.000 claims description 14
- 239000002552 dosage form Substances 0.000 claims description 13
- 229910019142 PO4 Inorganic materials 0.000 claims description 10
- NBIIXXVUZAFLBC-UHFFFAOYSA-K phosphate Chemical compound [O-]P([O-])([O-])=O NBIIXXVUZAFLBC-UHFFFAOYSA-K 0.000 claims description 10
- 239000010452 phosphate Substances 0.000 claims description 10
- 150000001413 amino acids Chemical class 0.000 claims description 8
- 229940043430 calcium compound Drugs 0.000 claims description 8
- 210000001035 gastrointestinal tract Anatomy 0.000 claims description 7
- 150000002681 magnesium compounds Chemical class 0.000 claims description 7
- 159000000003 magnesium salts Chemical class 0.000 claims description 7
- 102000006335 Phosphate-Binding Proteins Human genes 0.000 claims description 6
- 108010058514 Phosphate-Binding Proteins Proteins 0.000 claims description 6
- 159000000007 calcium salts Chemical class 0.000 claims description 6
- 239000007941 film coated tablet Substances 0.000 claims description 6
- 239000003826 tablet Substances 0.000 claims description 5
- VTYYLEPIZMXCLO-UHFFFAOYSA-L Calcium carbonate Chemical compound [Ca+2].[O-]C([O-])=O VTYYLEPIZMXCLO-UHFFFAOYSA-L 0.000 claims description 4
- 208000037147 Hypercalcaemia Diseases 0.000 claims description 4
- 206010020669 Hypermagnesaemia Diseases 0.000 claims description 4
- JLVVSXFLKOJNIY-UHFFFAOYSA-N Magnesium ion Chemical compound [Mg+2] JLVVSXFLKOJNIY-UHFFFAOYSA-N 0.000 claims description 4
- 241001465754 Metazoa Species 0.000 claims description 4
- 238000010521 absorption reaction Methods 0.000 claims description 4
- 239000008280 blood Substances 0.000 claims description 4
- 210000004369 blood Anatomy 0.000 claims description 4
- VSGNNIFQASZAOI-UHFFFAOYSA-L calcium acetate Chemical compound [Ca+2].CC([O-])=O.CC([O-])=O VSGNNIFQASZAOI-UHFFFAOYSA-L 0.000 claims description 4
- 239000001639 calcium acetate Substances 0.000 claims description 4
- 235000011092 calcium acetate Nutrition 0.000 claims description 4
- 229960005147 calcium acetate Drugs 0.000 claims description 4
- 229910001424 calcium ion Inorganic materials 0.000 claims description 4
- 230000000148 hypercalcaemia Effects 0.000 claims description 4
- 125000000468 ketone group Chemical group 0.000 claims description 4
- ZLNQQNXFFQJAID-UHFFFAOYSA-L magnesium carbonate Chemical compound [Mg+2].[O-]C([O-])=O ZLNQQNXFFQJAID-UHFFFAOYSA-L 0.000 claims description 4
- 239000001095 magnesium carbonate Substances 0.000 claims description 4
- 229910000021 magnesium carbonate Inorganic materials 0.000 claims description 4
- 235000014380 magnesium carbonate Nutrition 0.000 claims description 4
- 229910001425 magnesium ion Inorganic materials 0.000 claims description 4
- 230000004060 metabolic process Effects 0.000 claims description 4
- 150000007524 organic acids Chemical class 0.000 claims description 4
- 235000005985 organic acids Nutrition 0.000 claims description 4
- 230000004962 physiological condition Effects 0.000 claims description 3
- RWYRUDPAALLKPX-UHFFFAOYSA-N 2,2-difluoro-n-methylethanamine;hydrochloride Chemical compound Cl.CNCC(F)F RWYRUDPAALLKPX-UHFFFAOYSA-N 0.000 claims description 2
- FHVDTGUDJYJELY-UHFFFAOYSA-N 6-{[2-carboxy-4,5-dihydroxy-6-(phosphanyloxy)oxan-3-yl]oxy}-4,5-dihydroxy-3-phosphanyloxane-2-carboxylic acid Chemical compound O1C(C(O)=O)C(P)C(O)C(O)C1OC1C(C(O)=O)OC(OP)C(O)C1O FHVDTGUDJYJELY-UHFFFAOYSA-N 0.000 claims description 2
- 239000001749 Calcium fumarate Substances 0.000 claims description 2
- IWEDUKDKQUXPLH-NFJZTGFVSA-L [Mg++].OP(O)(=O)O[C@H]1[C@@H](OP(O)(O)=O)C(OP(O)([O-])=O)[C@H](OP(O)(O)=O)[C@@H](OP(O)(O)=O)C1OP(O)([O-])=O Chemical compound [Mg++].OP(O)(=O)O[C@H]1[C@@H](OP(O)(O)=O)C(OP(O)([O-])=O)[C@H](OP(O)(O)=O)[C@@H](OP(O)(O)=O)C1OP(O)([O-])=O IWEDUKDKQUXPLH-NFJZTGFVSA-L 0.000 claims description 2
- 229940072056 alginate Drugs 0.000 claims description 2
- 235000010443 alginic acid Nutrition 0.000 claims description 2
- 229920000615 alginic acid Polymers 0.000 claims description 2
- 239000011230 binding agent Substances 0.000 claims description 2
- 235000010410 calcium alginate Nutrition 0.000 claims description 2
- 239000000648 calcium alginate Substances 0.000 claims description 2
- 229960002681 calcium alginate Drugs 0.000 claims description 2
- 229910000019 calcium carbonate Inorganic materials 0.000 claims description 2
- 229960003563 calcium carbonate Drugs 0.000 claims description 2
- 235000010216 calcium carbonate Nutrition 0.000 claims 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 claims description 2
- 239000001354 calcium citrate Substances 0.000 claims description 2
- 229960004256 calcium citrate Drugs 0.000 claims description 2
- 235000013921 calcium diglutamate Nutrition 0.000 claims description 2
- AXCZMVOFGPJBDE-UHFFFAOYSA-L calcium dihydroxide Chemical compound [OH-].[OH-].[Ca+2] AXCZMVOFGPJBDE-UHFFFAOYSA-L 0.000 claims description 2
- 235000019296 calcium fumarate Nutrition 0.000 claims description 2
- 239000004227 calcium gluconate Substances 0.000 claims description 2
- 235000013927 calcium gluconate Nutrition 0.000 claims description 2
- 229960004494 calcium gluconate Drugs 0.000 claims description 2
- 239000000920 calcium hydroxide Substances 0.000 claims description 2
- 229910001861 calcium hydroxide Inorganic materials 0.000 claims description 2
- 235000011116 calcium hydroxide Nutrition 0.000 claims 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 claims description 2
- 239000001527 calcium lactate Substances 0.000 claims description 2
- 235000011086 calcium lactate Nutrition 0.000 claims description 2
- 229960002401 calcium lactate Drugs 0.000 claims description 2
- OLOZVPHKXALCRI-UHFFFAOYSA-L calcium malate Chemical compound [Ca+2].[O-]C(=O)C(O)CC([O-])=O OLOZVPHKXALCRI-UHFFFAOYSA-L 0.000 claims description 2
- 239000001362 calcium malate Substances 0.000 claims description 2
- 229940016114 calcium malate Drugs 0.000 claims description 2
- 235000011038 calcium malates Nutrition 0.000 claims description 2
- UMVAYAXXQSFULN-QHTZZOMLSA-L calcium;(2s)-2-aminopentanedioate;hydron Chemical compound [Ca+2].[O-]C(=O)[C@@H](N)CCC(O)=O.[O-]C(=O)[C@@H](N)CCC(O)=O UMVAYAXXQSFULN-QHTZZOMLSA-L 0.000 claims description 2
- OKHHGHGGPDJQHR-YMOPUZKJSA-L calcium;(2s,3s,4s,5s,6r)-6-[(2r,3s,4r,5s,6r)-2-carboxy-6-[(2r,3s,4r,5s,6r)-2-carboxylato-4,5,6-trihydroxyoxan-3-yl]oxy-4,5-dihydroxyoxan-3-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylate Chemical compound [Ca+2].O[C@@H]1[C@H](O)[C@H](O)O[C@@H](C([O-])=O)[C@H]1O[C@H]1[C@@H](O)[C@@H](O)[C@H](O[C@H]2[C@H]([C@@H](O)[C@H](O)[C@H](O2)C([O-])=O)O)[C@H](C(O)=O)O1 OKHHGHGGPDJQHR-YMOPUZKJSA-L 0.000 claims description 2
- NEEHYRZPVYRGPP-UHFFFAOYSA-L calcium;2,3,4,5,6-pentahydroxyhexanoate Chemical compound [Ca+2].OCC(O)C(O)C(O)C(O)C([O-])=O.OCC(O)C(O)C(O)C(O)C([O-])=O NEEHYRZPVYRGPP-UHFFFAOYSA-L 0.000 claims description 2
- PBUBJNYXWIDFMU-UHFFFAOYSA-L calcium;butanedioate Chemical compound [Ca+2].[O-]C(=O)CCC([O-])=O PBUBJNYXWIDFMU-UHFFFAOYSA-L 0.000 claims description 2
- WPEXVRDUEAJUGY-UHFFFAOYSA-B hexacalcium;(2,3,4,5,6-pentaphosphonatooxycyclohexyl) phosphate Chemical compound [Ca+2].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[Ca+2].[O-]P([O-])(=O)OC1C(OP([O-])([O-])=O)C(OP([O-])([O-])=O)C(OP([O-])([O-])=O)C(OP([O-])([O-])=O)C1OP([O-])([O-])=O WPEXVRDUEAJUGY-UHFFFAOYSA-B 0.000 claims description 2
- UEGPKNKPLBYCNK-UHFFFAOYSA-L magnesium acetate Chemical compound [Mg+2].CC([O-])=O.CC([O-])=O UEGPKNKPLBYCNK-UHFFFAOYSA-L 0.000 claims description 2
- 239000011654 magnesium acetate Substances 0.000 claims description 2
- 229940069446 magnesium acetate Drugs 0.000 claims description 2
- 235000011285 magnesium acetate Nutrition 0.000 claims description 2
- 229960001708 magnesium carbonate Drugs 0.000 claims description 2
- 239000004337 magnesium citrate Substances 0.000 claims description 2
- 229960005336 magnesium citrate Drugs 0.000 claims description 2
- 235000002538 magnesium citrate Nutrition 0.000 claims description 2
- 235000013918 magnesium diglutamate Nutrition 0.000 claims description 2
- VTHJTEIRLNZDEV-UHFFFAOYSA-L magnesium dihydroxide Chemical compound [OH-].[OH-].[Mg+2] VTHJTEIRLNZDEV-UHFFFAOYSA-L 0.000 claims description 2
- 239000001755 magnesium gluconate Substances 0.000 claims description 2
- 229960003035 magnesium gluconate Drugs 0.000 claims description 2
- 235000015778 magnesium gluconate Nutrition 0.000 claims description 2
- 229940063886 magnesium glutamate Drugs 0.000 claims description 2
- 239000000347 magnesium hydroxide Substances 0.000 claims description 2
- 229910001862 magnesium hydroxide Inorganic materials 0.000 claims description 2
- 229960000816 magnesium hydroxide Drugs 0.000 claims description 2
- 235000012254 magnesium hydroxide Nutrition 0.000 claims description 2
- OVGXLJDWSLQDRT-UHFFFAOYSA-L magnesium lactate Chemical compound [Mg+2].CC(O)C([O-])=O.CC(O)C([O-])=O OVGXLJDWSLQDRT-UHFFFAOYSA-L 0.000 claims description 2
- 239000000626 magnesium lactate Substances 0.000 claims description 2
- 235000015229 magnesium lactate Nutrition 0.000 claims description 2
- 229960004658 magnesium lactate Drugs 0.000 claims description 2
- JFQQIWNDAXACSR-UHFFFAOYSA-L magnesium malate Chemical compound [Mg+2].[O-]C(=O)C(O)CC([O-])=O JFQQIWNDAXACSR-UHFFFAOYSA-L 0.000 claims description 2
- 229940096424 magnesium malate Drugs 0.000 claims description 2
- HCWCAKKEBCNQJP-UHFFFAOYSA-N magnesium orthosilicate Chemical compound [Mg+2].[Mg+2].[O-][Si]([O-])([O-])[O-] HCWCAKKEBCNQJP-UHFFFAOYSA-N 0.000 claims description 2
- 239000000391 magnesium silicate Substances 0.000 claims description 2
- 229910052919 magnesium silicate Inorganic materials 0.000 claims description 2
- 235000019792 magnesium silicate Nutrition 0.000 claims description 2
- IAKLPCRFBAZVRW-XRDLMGPZSA-L magnesium;(2r,3s,4r,5r)-2,3,4,5,6-pentahydroxyhexanoate;hydrate Chemical compound O.[Mg+2].OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O.OC[C@@H](O)[C@@H](O)[C@H](O)[C@@H](O)C([O-])=O IAKLPCRFBAZVRW-XRDLMGPZSA-L 0.000 claims description 2
- MYUGVHJLXONYNC-QHTZZOMLSA-J magnesium;(2s)-2-aminopentanedioate Chemical compound [Mg+2].[O-]C(=O)[C@@H](N)CCC([O-])=O.[O-]C(=O)[C@@H](N)CCC([O-])=O MYUGVHJLXONYNC-QHTZZOMLSA-J 0.000 claims description 2
- QUIOHQITLKCGNW-TYYBGVCCSA-L magnesium;(e)-but-2-enedioate Chemical compound [Mg+2].[O-]C(=O)\C=C\C([O-])=O QUIOHQITLKCGNW-TYYBGVCCSA-L 0.000 claims description 2
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- OKUCEQDKBKYEJY-UHFFFAOYSA-N tert-butyl 3-(methylamino)pyrrolidine-1-carboxylate Chemical compound CNC1CCN(C(=O)OC(C)(C)C)C1 OKUCEQDKBKYEJY-UHFFFAOYSA-N 0.000 claims description 2
- 235000013337 tricalcium citrate Nutrition 0.000 claims description 2
- PLSARIKBYIPYPF-UHFFFAOYSA-H trimagnesium dicitrate Chemical compound [Mg+2].[Mg+2].[Mg+2].[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O.[O-]C(=O)CC(O)(CC([O-])=O)C([O-])=O PLSARIKBYIPYPF-UHFFFAOYSA-H 0.000 claims description 2
- ZFXVRMSLJDYJCH-UHFFFAOYSA-N calcium magnesium Chemical compound [Mg].[Ca] ZFXVRMSLJDYJCH-UHFFFAOYSA-N 0.000 claims 2
- 230000015572 biosynthetic process Effects 0.000 claims 1
- 150000001674 calcium compounds Chemical class 0.000 claims 1
- 229940095643 calcium hydroxide Drugs 0.000 claims 1
- 239000000378 calcium silicate Substances 0.000 claims 1
- 229910052918 calcium silicate Inorganic materials 0.000 claims 1
- OYACROKNLOSFPA-UHFFFAOYSA-N calcium;dioxido(oxo)silane Chemical compound [Ca+2].[O-][Si]([O-])=O OYACROKNLOSFPA-UHFFFAOYSA-N 0.000 claims 1
- 238000006243 chemical reaction Methods 0.000 claims 1
- 150000003013 phosphoric acid derivatives Chemical class 0.000 claims 1
- 235000002949 phytic acid Nutrition 0.000 claims 1
- 230000005764 inhibitory process Effects 0.000 description 4
- 230000002496 gastric effect Effects 0.000 description 3
- 230000000694 effects Effects 0.000 description 2
- 230000029142 excretion Effects 0.000 description 2
- 210000003608 fece Anatomy 0.000 description 2
- 210000004051 gastric juice Anatomy 0.000 description 2
- 208000030915 hypercalcemia disease Diseases 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 230000002123 temporal effect Effects 0.000 description 2
- 208000020084 Bone disease Diseases 0.000 description 1
- 108010010803 Gelatin Proteins 0.000 description 1
- 208000001647 Renal Insufficiency Diseases 0.000 description 1
- 208000005770 Secondary Hyperparathyroidism Diseases 0.000 description 1
- 150000001450 anions Chemical class 0.000 description 1
- 235000012241 calcium silicate Nutrition 0.000 description 1
- GUPPESBEIQALOS-UHFFFAOYSA-L calcium tartrate Chemical compound [Ca+2].[O-]C(=O)C(O)C(O)C([O-])=O GUPPESBEIQALOS-UHFFFAOYSA-L 0.000 description 1
- 239000001427 calcium tartrate Substances 0.000 description 1
- 235000011035 calcium tartrate Nutrition 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 239000007910 chewable tablet Substances 0.000 description 1
- 239000011248 coating agent Substances 0.000 description 1
- 238000000576 coating method Methods 0.000 description 1
- 238000000502 dialysis Methods 0.000 description 1
- 239000008298 dragée Substances 0.000 description 1
- 239000006196 drop Substances 0.000 description 1
- 235000011389 fruit/vegetable juice Nutrition 0.000 description 1
- 239000000499 gel Substances 0.000 description 1
- 239000008273 gelatin Substances 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 239000008187 granular material Substances 0.000 description 1
- 150000002500 ions Chemical class 0.000 description 1
- 201000006370 kidney failure Diseases 0.000 description 1
- 239000007937 lozenge Substances 0.000 description 1
- 229940095060 magnesium tartrate Drugs 0.000 description 1
- MUZDLCBWNVUYIR-ZVGUSBNCSA-L magnesium;(2r,3r)-2,3-dihydroxybutanedioate Chemical compound [Mg+2].[O-]C(=O)[C@H](O)[C@@H](O)C([O-])=O MUZDLCBWNVUYIR-ZVGUSBNCSA-L 0.000 description 1
- 239000000463 material Substances 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 235000016709 nutrition Nutrition 0.000 description 1
- 239000006186 oral dosage form Substances 0.000 description 1
- 238000004806 packaging method and process Methods 0.000 description 1
- 239000004033 plastic Substances 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 239000000725 suspension Substances 0.000 description 1
- 238000002626 targeted therapy Methods 0.000 description 1
Classifications
-
- 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
- A61K33/42—Phosphorus; Compounds thereof
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Inorganic Chemistry (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Preparation (AREA)
Description
Vitasyn GmbH 8-2234/99Vitasyn GmbH 8-2234/99
Marburger Str. 3 10. Juni 1999Marburger Str. 3 10 June 1999
10789 Berlin10789 Berlin
Mittel zur Therapie von HyperphosphatämieAgents for the treatment of hyperphosphatemia
BeschreibungDescription
Die Erfindung betrifft ein Mittel zur Senkung der Hy-' percalcamie und der Hypermagnesämie bei der Anwendung calcium- oder magnesiumhaltiger Phosphatbinder zur Therapie von Hyperphosphatämie.The invention relates to an agent for reducing hypercalcemia and hypermagnesemia when using calcium- or magnesium-containing phosphate binders for the treatment of hyperphosphatemia.
Bei- Niereninsuffienz, insbesondere im terminalen, dialysepflichtigen Stadium kommt es im menschlichen Körper zu einer Störung der renalen Phosphatausscheidung. Durch diese Störung der renalen Phosphatausscheidung kann' sich eine Hyperphosphatämie entwickeln, die unbe-· handelt wiederum zu schweren Knochenerkrankungen in Einheit mit einem sekundären Hyperparathyreoidisnius führen kann. Zur Senkung der Blutphosphatwerte werden deshalb Calcium- und Magnesiumverbindungen eingesetzt, die unter physiologischen Bedingungen im Gastrointestinaltrakt dissoziieren und zu einer gastrointestinalen Phosphatbindung führen. Dabei bilden zweiwertige Calcium- bzw. Magnesium-Ionen im Gastrointestinaltrakt mit der resorbierbaren Phosphatmenge nach den Gleichungen .In the case of renal insufficiency, particularly in the terminal stage requiring dialysis, the human body experiences a disruption in renal phosphate excretion. This disruption in renal phosphate excretion can lead to hyperphosphatemia, which, if left untreated, can lead to severe bone diseases in conjunction with secondary hyperparathyroidism. Calcium and magnesium compounds are therefore used to reduce blood phosphate levels. These dissociate in the gastrointestinal tract under physiological conditions and lead to gastrointestinal phosphate binding. In the process, divalent calcium and magnesium ions in the gastrointestinal tract react with the reabsorbable amount of phosphate according to the equations .
'3Ca2++ 2(PO4)3"= Ca3(POJ2 bzw. 3Mg2+ + 2 (PO.,) 3~ = Mg3 (PO.,) 2 '3Ca 2+ + 2(PO 4 ) 3 "= Ca 3 (POJ 2 or 3Mg 2+ + 2 (PO.,) 3 ~ = Mg 3 (PO.,) 2
schwerlösliche Calcium- bzw. Magnesiumverbindungen, die mit den Faeces ausgeschieden werden können. Die resorbierbare Phosphatmenge wird dadurch reduziert und der erhöhte Blutsphosphatspiegel gesenkt.poorly soluble calcium or magnesium compounds that can be excreted in the feces. The amount of reabsorbable phosphate is thereby reduced and the elevated blood phosphate level is lowered.
Durch diese Maßnahmen wird zwar die resorbierbare Phosphatmenge gesenkt und der Blutphosphatspiegel sinkt, gleichzeitig können jedoch als Nebenwirkungen Hypercalcämien bzw. Hypermagnesämien auftreten, da die zur Phosphatbindung erforderlichen Mengen an elementarem Calcium und Magnesium weit über den ernährungsphysiologischen Dosen liegen.Although these measures reduce the amount of absorbable phosphate and the blood phosphate level, side effects such as hypercalcaemia or hypermagnesemia may occur at the same time, since the amounts of elemental calcium and magnesium required for phosphate binding far exceed the nutritional doses.
Aufgabe der vorliegenden Erfindung ist es, ein Mittel zur Therapie der Hyperphosphatämie bei gleichzeitiger Vermeidung der Hypercalcämie und der Hypermagnesämie zu schaffen.The object of the present invention is to provide an agent for the treatment of hyperphosphatemia while simultaneously avoiding hypercalcemia and hypermagnesemia.
Gelöst wird diese Aufgabe durch die Maßnahmen gemäß Anspruch 1, insbesondere durch eine Darreichungsform als teilbare Tabletten zur gleichzeitigen Applikation phosphatbindender, unter physiologischen Bedingungen löslichen Calcium- und Magnesiumverbindungen in einem sich bei der Resorption im Intestinaltrakt wechselseitig behindernden Mol-Verhältnis.This object is achieved by the measures according to claim 1, in particular by a dosage form as divisible tablets for the simultaneous application of phosphate-binding calcium and magnesium compounds which are soluble under physiological conditions in a molar ratio which mutually hinders absorption in the intestinal tract.
Durch diese Maßnahmen wird ein Mittel geschaffen, bei dem sich die an sich bekannte Calciumresorption und die Magnesiumresorption durch die gleichzeitige Anwesenheit des jeweils anderen Ions gegenseitig'behindern. Weitere vorteilhafte Maßnahmen sind in den Unteransprüchen beschrieben. These measures create a means in which the known calcium absorption and the magnesium absorption are mutually hindered by the simultaneous presence of the other ion. Further advantageous measures are described in the subclaims.
Eine vorteilhafte Darreichungsform ist in der einzigen Figur dargestellt. Diese Darreichungsform besteht aus einer brikettförmigen Filmtablette 10, die mitAn advantageous dosage form is shown in the single figure. This dosage form consists of a briquette-shaped film-coated tablet 10, which is
Bruchrillen 11 versehen ist., In diesen Bruchrillen 11 ist die Filmtablette 10. teilbar.is provided with break lines 11. The film-coated tablet 10 can be divided into these break lines 11.
Die Filmtabletten 10 sind bei dem Ausführungsbeispiel zu 250 in-Kunststoffdosen mit Deckel verpackt. Möglich ist■auch jede andere Stückelung und Verpackungsart, so sind weitere Packungsgrößen mit beispielsweise drei Dosen zu je 250 Filmtabletten vorgesehen.In the embodiment, the film-coated tablets 10 are packed in 250-inch plastic containers with lids. Any other denomination and type of packaging is also possible, so other pack sizes with, for example, three containers of 250 film-coated tablets each are provided.
Die Erfindung besteht darin, daß der ernährungsphysiologische, an sich negative Effekt, nämlich die wechselseitige Hemmung der Calcium-, bzw. Magnesiumresorption als gezielte Therapie ausgenutzt wird. Die Hemmung der Calcium- und Magnesiumr.esorption ist zeitlich begrenzt. Durch die gleichzeitige Applikation von Calcium und Magnesium in einer erheblichen Überdosis tritt durch die wechselseitige Hemmung eine zeitliche Verzögerung der Resorptionen auf. Diese zeitliche Verzögerung der Resorptionen reicht aus, um die bei der Phosphatbindung überschüssigen Calcium- und Magnesium-Ionen weitgehend unresorbiert durch den Intestinaltrakt zu fördern, daß sie nahezu vollständig mit den Faeces ausgeschieden werden können.The invention consists in using the nutritional-physiological, in itself negative effect, namely the mutual inhibition of calcium and magnesium resorption, as a targeted therapy. The inhibition of calcium and magnesium resorption is limited in time. The simultaneous application of calcium and magnesium in a significant overdose causes a temporal delay in resorption due to the mutual inhibition. This temporal delay in resorption is sufficient to promote the calcium and magnesium ions that are surplus during phosphate binding through the intestinal tract largely unabsorbed, so that they can be excreted almost completely in the faeces.
Geeignet sind alle Calcium- und/oder Magnesiumverbindungen, die. unter den im menschlichen Gastrointestinaltrakt anzutreffenden Bedingungen Calcium- und/oder Magnesium-Ionen freisetzen. Diese können als Mischungen von Calcium- und Magnesiumsalzen mit gleichen oder unterschiedlichen Anionen eingesetzt werden. Eine Anwendung von Calcium mal Magnesium-Doppelsalzen oder deren Mischungen ist ebenso möglich.All calcium and/or magnesium compounds that release calcium and/or magnesium ions under the conditions found in the human gastrointestinal tract are suitable. These can be used as mixtures of calcium and magnesium salts with the same or different anions. The use of calcium times magnesium double salts or mixtures thereof is also possible.
. Insbesondere sind Calciumacetat, Calciumalginat, Calciumcärbonat, Calciumcitrat, Calciumfumarat, Calciumgluconat, Calciumglutamat, Calciumhydroxid, Calciumlactat,In particular, calcium acetate, calcium alginate, calcium carbonate, calcium citrate, calcium fumarate, calcium gluconate, calcium glutamate, calcium hydroxide, calcium lactate,
Calciummalate, Calciumphytat, Calciumsilicate, Calciumsuc.cinat,-Calciumtartat, die Calciümsalze von Aminosäuren, die Calciümsalze der Ketoanaloga von Aminosäuren oder die Calciümsalze von organischen Säuren, die im pflanzlichen, tierischen und menschlichen Stoffwechsel angetroffen werden, zur Anwendung vorgesehen.Calcium malate, calcium phytate, calcium silicates, calcium succinate, calcium tartrate, calcium salts of amino acids, calcium salts of keto analogues of amino acids or calcium salts of organic acids found in plant, animal and human metabolism are intended for use.
Ebenso sind Magnesiumacetat, Magnesiumalginat, Magnesi- ' umcarbonat, Magnesiumeitrat, Magnesiumfumarat, Magnesiumgluconat, Magnesiumglutamat, Magnesiumhydroxid, Mägnesiumlactat, Magnesiummalate, Magnesiumphytat, Magnesiumsilicate, Magnesiumsuccinat, Magnesiumtartat, die Magnesiumsalze von Aminosäuren, die Magnesiumsalze der Ketoanaloga von Aminosäuren oder die Magnesiumsalze von organischen Säuren, die im pflanzlichen, tierischen und menschlichen Stoffwechsel angetroffen werden, zur Anwendung geeignet.Magnesium acetate, magnesium alginate, magnesium carbonate, magnesium citrate, magnesium fumarate, magnesium gluconate, magnesium glutamate, magnesium hydroxide, magnesium lactate, magnesium malate, magnesium phytate, magnesium silicate, magnesium succinate, magnesium tartrate, the magnesium salts of amino acids, the magnesium salts of the keto analogues of amino acids or the magnesium salts of organic acids found in plant, animal and human metabolism are also suitable for use.
Als besonders geeignet zur erfindungsgemäßen .Erzielung der wechselseitigen Hemmung von Calcium und Magnesium in einer Darreichungsform, hat sich ein molares Verhältnis von Calcium zu Magnesium wie 1. zu 0,2 bis 1 zu . 20 als besonders geeignet erwiesen. Dies bedeutet, daß 1 mmol Calcium mit 0,2 mmol bis 20 mmol Magnesium zusammen appliziert werden kann. In absoluten Maßeinheiten würde das 40,8 mg Calcium zusammen mit 4,86 mg bis 486 mg Magnesium bedeuten.A molar ratio of calcium to magnesium of 1:0.2 to 1:20 has proven to be particularly suitable for achieving the mutual inhibition of calcium and magnesium in a dosage form according to the invention. This means that 1 mmol of calcium can be administered together with 0.2 mmol to 20 mmol of magnesium. In absolute units, this would mean 40.8 mg of calcium together with 4.86 mg to 486 mg of magnesium.
Der absolute Gehalt der Darreichungsformen an Calcium und Magnesium kann so groß sein, daß eine oder mehrere Einheiten täglich eingenommen werden müssen, um die angestrebte Senkung der Hyperphosphatämie zu erreichen.The absolute calcium and magnesium content of the dosage forms may be so high that one or more units must be taken daily to achieve the desired reduction in hyperphosphatemia.
Geeignet sind alle oralen Darreichungsfomen wie. Tabletten, Filmtabletten, Dragees, Kapseln aus Hart- oder Weichgelatine oder sonstigen Umhüllungsstoffen in ma-All oral dosage forms are suitable, such as tablets, film-coated tablets, dragees, capsules made of hard or soft gelatin or other coating materials in ma-
gensaftlöslicher oder magensaftresistenter Form. Ebenfalls sind Lutsch- oder Kautabletten geeignet. Weiterhin können magensaftlösliche und magensaftresistente Granulate, Lösungen, Tropfen, Suspensionen, Säfte oder Gele zur Anwendung gelangen. Diese Darreichungsformen können zusätzlich zu den therapeutisch wirksamen Calcium- und Magnesiumverbindungen weitere galanisch notwendige, pharmazeutischen Regeln entsprechende Hilfsstoffe enthalten.in gastric juice-soluble or gastric juice-resistant form. Lozenges or chewable tablets are also suitable. Gastric juice-soluble and gastric juice-resistant granules, solutions, drops, suspensions, juices or gels can also be used. In addition to the therapeutically effective calcium and magnesium compounds, these dosage forms can contain other necessary galanic excipients that comply with pharmaceutical rules.
Claims (10)
3Ca2+ + 2(PO4)2 = Ca3(PO4)
beziehungsweise
3Mg2+ + 2(PO4)3- = Mg3(PO4)2
enthalten. 5. Agent according to claims 1 to 4, characterized in that the dosage forms ( 10 ) contain blood phosphate-lowering application agents containing divalent calcium and magnesium ions for the formation of poorly soluble phosphate compounds in the gastrointestinal tract after the simultaneous reactions
3Ca 2+ + 2(PO 4 ) 2 = Ca 3 (PO 4 )
or
3Mg 2+ + 2(PO 4 ) 3- = Mg 3 (PO 4 ) 2
contain.
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE29910454U DE29910454U1 (en) | 1999-06-10 | 1999-06-10 | Agents for the therapy of hyperphosphataemia |
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| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DE29910454U DE29910454U1 (en) | 1999-06-10 | 1999-06-10 | Agents for the therapy of hyperphosphataemia |
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| Publication Number | Publication Date |
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| DE29910454U1 true DE29910454U1 (en) | 1999-09-23 |
Family
ID=8074845
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| Application Number | Title | Priority Date | Filing Date |
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| DE29910454U Expired - Lifetime DE29910454U1 (en) | 1999-06-10 | 1999-06-10 | Agents for the therapy of hyperphosphataemia |
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Cited By (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE102008051572A1 (en) * | 2008-09-05 | 2010-03-11 | Maria Clementine Martin Klosterfrau Vertriebsgesellschaft Mbh | Preparation of phosphate binders and phosphate binders prepared in this way |
| WO2010117370A1 (en) * | 2009-04-10 | 2010-10-14 | Cypress Pharmaceuticals, Inc. | Phosphate-binding magnesium salts and uses thereof |
| US8236358B1 (en) | 2009-04-10 | 2012-08-07 | Cypress Pharmaceutical, Inc. | Phosphate-binding magnesium salts and uses thereof |
| WO2014140402A1 (en) * | 2013-03-15 | 2014-09-18 | Laboratoris Sanifit, S. L. | Use of derivatives with c-o-p bonds in patients with renal failure |
| US9394318B2 (en) | 2012-11-30 | 2016-07-19 | Cypress Pharmaceuticals, Inc. | Crystal polymorph of magnesium glycinate dihydrate and process for its preparation |
| EP2324835B1 (en) * | 2008-08-06 | 2016-07-20 | Universitat de les Illes Balears | Composition of dialysis liquid comprising crystallisation inhibitor substances |
| US10010559B2 (en) | 2013-03-15 | 2018-07-03 | Laboratorios Sanifit, S.L. | Use of derivatives containing C-O-P bonds in patients with kidney failure |
| DE102017126255A1 (en) * | 2017-11-09 | 2019-05-09 | Apafit UG (haftungsbeschränkt) | Portioning unit with mineral salts as an additive for water, their use and procedures |
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1999
- 1999-06-10 DE DE29910454U patent/DE29910454U1/en not_active Expired - Lifetime
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2324835B1 (en) * | 2008-08-06 | 2016-07-20 | Universitat de les Illes Balears | Composition of dialysis liquid comprising crystallisation inhibitor substances |
| DE102008051572A1 (en) * | 2008-09-05 | 2010-03-11 | Maria Clementine Martin Klosterfrau Vertriebsgesellschaft Mbh | Preparation of phosphate binders and phosphate binders prepared in this way |
| US9610267B2 (en) | 2009-04-10 | 2017-04-04 | Cypress Pharmaceuticals, Inc. | Phosphate-binding magnesium salts and uses thereof |
| WO2010117370A1 (en) * | 2009-04-10 | 2010-10-14 | Cypress Pharmaceuticals, Inc. | Phosphate-binding magnesium salts and uses thereof |
| US8236358B1 (en) | 2009-04-10 | 2012-08-07 | Cypress Pharmaceutical, Inc. | Phosphate-binding magnesium salts and uses thereof |
| US8247000B2 (en) | 2009-04-10 | 2012-08-21 | Cypress Pharmaceutical, Inc. | Phosphate-binding magnesium salts and uses thereof |
| AU2009344184B2 (en) * | 2009-04-10 | 2016-05-12 | Cypress Pharmaceuticals, Inc. | Phosphate-binding magnesium salts and uses thereof |
| US9339481B2 (en) | 2009-04-10 | 2016-05-17 | Cypress Pharmaceuticals, Inc. | Phosphate-binding magnesium salts and uses thereof |
| US9889157B2 (en) | 2009-04-10 | 2018-02-13 | Cypress Pharmaceuticals, Inc. | Phosphate-binding magnesium salts and uses thereof |
| US10150784B2 (en) | 2012-11-30 | 2018-12-11 | Cypress Pharmaceuticals, Inc. | Crystal polymorph of magnesium glycinate dihydrate and process for its preparation |
| US9394318B2 (en) | 2012-11-30 | 2016-07-19 | Cypress Pharmaceuticals, Inc. | Crystal polymorph of magnesium glycinate dihydrate and process for its preparation |
| WO2014140402A1 (en) * | 2013-03-15 | 2014-09-18 | Laboratoris Sanifit, S. L. | Use of derivatives with c-o-p bonds in patients with renal failure |
| CN105611913A (en) * | 2013-03-15 | 2016-05-25 | 莱博若特瑞斯萨尼菲特有限公司 | Use of derivatives comprising C-O-P bonds in patients with renal failure |
| US10010559B2 (en) | 2013-03-15 | 2018-07-03 | Laboratorios Sanifit, S.L. | Use of derivatives containing C-O-P bonds in patients with kidney failure |
| EP2974714A1 (en) * | 2013-03-15 | 2016-01-20 | Laboratorios Sanifit, S.L. | Use of derivatives with c-o-p bonds in patients with renal failure |
| DE102017126255A1 (en) * | 2017-11-09 | 2019-05-09 | Apafit UG (haftungsbeschränkt) | Portioning unit with mineral salts as an additive for water, their use and procedures |
| US10973838B2 (en) | 2018-10-11 | 2021-04-13 | Sanifit Therapeutics S.A. | IP and IP analogs dosage regimens for the treatment of ectopic calcifications |
| US12070469B2 (en) | 2018-10-11 | 2024-08-27 | Sanifit Therapeutics S.A. | IP and IP analogs dosage regimens for the treatment of ectopic calcifications |
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