DK2531200T3 - Kystalliseringsfremgangsmåde og biotilgængelighed - Google Patents
Kystalliseringsfremgangsmåde og biotilgængelighed Download PDFInfo
- Publication number
- DK2531200T3 DK2531200T3 DK11740284.2T DK11740284T DK2531200T3 DK 2531200 T3 DK2531200 T3 DK 2531200T3 DK 11740284 T DK11740284 T DK 11740284T DK 2531200 T3 DK2531200 T3 DK 2531200T3
- Authority
- DK
- Denmark
- Prior art keywords
- another embodiment
- zoledronic acid
- coformer
- lysine
- unit dose
- Prior art date
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- 239000002594 sorbent Substances 0.000 description 1
- 241000894007 species Species 0.000 description 1
- 238000001228 spectrum Methods 0.000 description 1
- 238000013222 sprague-dawley male rat Methods 0.000 description 1
- 229910001220 stainless steel Inorganic materials 0.000 description 1
- 239000010935 stainless steel Substances 0.000 description 1
- 239000007858 starting material Substances 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 150000005846 sugar alcohols Chemical class 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 230000002459 sustained effect Effects 0.000 description 1
- 208000024891 symptom Diseases 0.000 description 1
- 229920002994 synthetic fiber Polymers 0.000 description 1
- 238000012353 t test Methods 0.000 description 1
- 239000007916 tablet composition Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 229960003080 taurine Drugs 0.000 description 1
- 235000008521 threonine Nutrition 0.000 description 1
- 229960002898 threonine Drugs 0.000 description 1
- 230000000699 topical effect Effects 0.000 description 1
- 239000001069 triethyl citrate Substances 0.000 description 1
- VMYFZRTXGLUXMZ-UHFFFAOYSA-N triethyl citrate Natural products CCOC(=O)C(O)(C(=O)OCC)C(=O)OCC VMYFZRTXGLUXMZ-UHFFFAOYSA-N 0.000 description 1
- 235000013769 triethyl citrate Nutrition 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
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Classifications
-
- 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
- A61K31/66—Phosphorus compounds
- A61K31/675—Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P19/00—Drugs for skeletal disorders
- A61P19/08—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
- A61P19/10—Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/12—Drugs for disorders of the metabolism for electrolyte homeostasis
- A61P3/14—Drugs for disorders of the metabolism for electrolyte homeostasis for calcium homeostasis
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
- A61P35/04—Antineoplastic agents specific for metastasis
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/547—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
- C07F9/645—Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having two nitrogen atoms as the only ring hetero atoms
- C07F9/6503—Five-membered rings
- C07F9/6506—Five-membered rings having the nitrogen atoms in positions 1 and 3
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Physical Education & Sports Medicine (AREA)
- Rheumatology (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Oncology (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Endocrinology (AREA)
- Diabetes (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicinal Preparation (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Claims (14)
1. Farmaceutisk sammensætning omfattende: et krystallinsk molekylært kompleks omfattende zoledronsyre eller et salt deraf og en molekylær kompleks-coformer (ENG: molecular complex coformer) valgt blandt lysin og glycin og et farmaceutisk acceptabelt excipiens; endvidere omfattende en yderligere coformer valgt blandt lysin og/eller glycin, hvor masseforholdet af yderligere coformer til molekylær kompleks-coformer er mellem omkring 2:1 til omkring 5000:1.
2. Farmaceutisk sammensætning ifølge krav 1, hvor coformeren i det molekylære kompleks er lysin.
3. Farmaceutisk sammensætning ifølge krav 1, hvor coformeren i det molekylære kompleks er glycin.
4. Farmaceutisk sammensætning ifølge et hvilket som helst af krav 1 til 3, hvor den molekylære kompleks-coformer og den yderligere coformer er den samme.
5. Farmaceutisk sammensætning ifølge et hvilket som helst af krav 1 til 3, hvor den molekylære kompleks-coformer og den yderligere coformer er forskellige.
6. Farmaceutisk sammensætning ifølge et hvilket som helst af krav 1 til 5, hvor det krystalline molekylære kompleks er valgt fra gruppen bestående af: a. et molekylært kompleks omfattende zoledronsyre, lysin og vand; b. et molekylært kompleks bestående af zoledronsyre, lysin og vand; c. et molekylært kompleks bestående af zoledronsyre, L-lysin og vand; d. et molekylært kompleks bestående af zoledronsyre, DL-lysin og vand; e. et molekylært kompleks bestående af zoledronsyre og lysin; f. et molekylært kompleks bestående af zoledronsyre og L-lysin; g. et molekylært kompleks bestående af zoledronsyre og DL-lysin; h. et molekylært kompleks omfattende zoledronsyre, glycin og vand; i. et molekylært kompleks bestående af zoledronsyre og glycin; j. et molekylært kompleks bestående af zoledronsyre, DL-lysin, ethanol og vand.
7. Farmaceutisk sammensætning ifølge krav 6, hvor det krystalline molekylære kompleks er valgt fra gruppen bestående af: a. et krystallinsk molekylært kompleks af zoledronsyre, L-lysin og vand kendetegnet ved et røntgenpulverdiffraktionsmønster, der omfatter maksima ved omkring 9,0, 14,4, 18,1, 26,0, og 29,6 ±0,2 grader to theta; b. et krystallinsk molekylært kompleks af zoledronsyre, L-lysin og vand kendetegnet ved et røntgenpulverdiffraktionsmønster omfattende maksima ved omkring 9,6, 10,7, 14,3, 21,4, 23,5 ±0,2 grader to theta; c. et krystallinsk molekylært kompleks af zoledronsyre, DL-lysin og vand kendetegnet ved et røntgenpulverdiffraktionsmønster omfattende maksima ved omkring 8,3, 11,8, 12,3, 15,8 og 20,8 ±0,2 grader to theta; d. et krystallinsk molekylært kompleks af DL-lysin og vand kendetegnet ved et røntgenpulverdiffraktionsmønster omfattende maksima ved omkring 9,1, 14,7, 18,0, 21,2, og 26,0 ±0,2 grader to theta e. et krystallinsk molekylært kompleks af zoledronsyre, DL-lysin og vand kendetegnet ved røntgenpulverdiffraktionsmønster omfattende maksima ved omkring 9,7, 10,8, 14,4, 18,9, 21,4 ±0,2 grader to theta; f. et krystallinsk kompleks af zoledronsyre, zoledronsyre, DL-lysin, ethanol and vand kendetegnet ved et røntgenpulverdiffraktionsmønster omfattende maksima ved omkring 8,8, 9,7, 17,6, 23,1 og 26.5 ±0,2 grader to theta; og g. et krystallinsk molekylært kompleks af zoledronsyre og glycin kendetegnet ved et røntgenpulverdiffraktionsmønster omfattende maksima ved omkring 10,2, 17,8, 19,9, 22,9 og 28,1 ±0,2 grader to theta; når røntgenpulverdiffraktionsmønsteret opsamles over et vinkelinterval på 3° til 40° 2Θ ved anvendelse af Cu-Ka-stråling med λ = 1.540562 Å.
8. Farmaceutisk sammensætning af et hvilket som helst af krav 1 til 7, hvor den farmaceutiske sammensætning er en oral dosisform.
9. Farmaceutisk sammensætning ifølge krav 8, hvor sammensætningen er en oral dosisform valgt blandt en tablet, en kapsel, en opløsning eller en suspension.
10. Farmaceutisk sammensætning ifølge krav 8 eller krav 9, hvor den orale dosisform er enterisk overtrukket.
11. Farmaceutisk sammensætning af hvilke som helst af krav 1 til 10, hvor den farmaceutiske sammensætning er i formen af en enhedsdosis, fortrukket hvor enhedsdosis omfatter mellem omkring 1 mg til omkring 500 mg af zoledronsyre.
12. Farmaceutisk sammensætning af hvilke som helst af krav 1 til 11 til anvendelse i behandling eller forebyggelse af en sygdom, hvor zoledronsyre er angivet.
13. Farmaceutisk sammensætning til anvendelse ifølge krav 12, hvor sygdommen er valgt fra gruppen bestående af: osteoporose, hypercalcæmi, cancer-inducerede knoglemetastaser, Pagets sygdom eller adjuverende cancerbehandling og neoadjuverende cancerbehandling.
14. Farmaceutisk sammensætning som defineret i et hvilket som helst af krav 1 til 11 til anvendelse til forøgelse af den orale biotilgængelighed eller permeabilitet af zoledronsyre eller et salt deraf hos en patient, der har behov derfor.
Applications Claiming Priority (12)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US30211010P | 2010-02-06 | 2010-02-06 | |
| US31287910P | 2010-03-11 | 2010-03-11 | |
| US31850310P | 2010-03-29 | 2010-03-29 | |
| US33304110P | 2010-05-10 | 2010-05-10 | |
| US33302810P | 2010-05-10 | 2010-05-10 | |
| US35954410P | 2010-06-29 | 2010-06-29 | |
| PCT/US2010/043916 WO2011014781A1 (en) | 2009-07-31 | 2010-07-30 | Novel oral forms of a phosphonic acid derivative |
| PCT/US2010/043892 WO2011014766A2 (en) | 2009-07-31 | 2010-07-30 | Crystallization method and bioavailability |
| US12/847,568 US8399023B2 (en) | 2009-07-31 | 2010-07-30 | Crystallization method and bioavailability |
| US37981410P | 2010-09-03 | 2010-09-03 | |
| US45577810P | 2010-10-26 | 2010-10-26 | |
| PCT/US2011/023427 WO2011097269A1 (en) | 2010-02-06 | 2011-02-02 | Crystallization method and bioavailability |
Publications (1)
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| DK2531200T3 true DK2531200T3 (da) | 2017-09-11 |
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| AU (2) | AU2012216632B2 (da) |
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| CY (1) | CY1119192T1 (da) |
| DK (1) | DK2531200T3 (da) |
| ES (1) | ES2638072T3 (da) |
| HR (1) | HRP20171201T1 (da) |
| HU (1) | HUE035744T2 (da) |
| IL (1) | IL221306A0 (da) |
| LT (1) | LT2531200T (da) |
| PL (1) | PL2531200T3 (da) |
| PT (1) | PT2531200T (da) |
| SI (1) | SI2531200T1 (da) |
| WO (1) | WO2011097269A1 (da) |
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| US20160016982A1 (en) | 2009-07-31 | 2016-01-21 | Thar Pharmaceuticals, Inc. | Crystallization method and bioavailability |
| AU2010278860B2 (en) | 2009-07-31 | 2016-05-26 | Thar Pharma, Llc | Crystallization method and bioavailability |
| US9169279B2 (en) | 2009-07-31 | 2015-10-27 | Thar Pharmaceuticals, Inc. | Crystallization method and bioavailability |
| WO2011014781A1 (en) | 2009-07-31 | 2011-02-03 | Thar Pharmaceuticals, Inc. | Novel oral forms of a phosphonic acid derivative |
| ES2638072T3 (es) * | 2010-02-06 | 2017-10-18 | Grünenthal GmbH | Método de cristalización y biodisponibilidad |
| US9340565B2 (en) | 2010-11-24 | 2016-05-17 | Thar Pharmaceuticals, Inc. | Crystalline forms |
| CN102268023B (zh) * | 2011-08-15 | 2013-04-17 | 南京丰融化学技术有限公司 | 头孢类衍生物cxd的晶型 |
| US9999629B2 (en) | 2012-05-14 | 2018-06-19 | Antecip Bioventures Ii Llc | Compositions for oral administration of zoledronic acid or related compounds for treating complex regional pain syndrome |
| US10016445B2 (en) | 2012-05-14 | 2018-07-10 | Antecip Bioventures Ii Llc | Compositions for oral administration of zoledronic acid or related compounds for treating complex regional pain syndrome |
| US20140349974A1 (en) * | 2014-08-12 | 2014-11-27 | Antecip Bioventures Ii Llc | Zoledronic acid dosage forms for the treatment of pain |
| US11654152B2 (en) | 2012-05-14 | 2023-05-23 | Antecip Bioventures Ii Llc | Compositions for oral administration of zoledronic acid or related compounds for treating disease |
| US10413561B2 (en) | 2012-05-14 | 2019-09-17 | Antecip Bioventures Ii Llc | Neridronic acid and other bisphosphonates for treating complex regional pain syndrome and other diseases |
| US9956238B2 (en) | 2014-05-15 | 2018-05-01 | Antecip Bioventures Ii Llc | Compositions for administration of zoledronic acid or related compounds for treating low back pain |
| US10413560B2 (en) | 2012-05-14 | 2019-09-17 | Antecip Bioventures Ii Llc | Dosage forms for oral administration of zoledronic acid or related compounds for treating disease |
| US10463682B2 (en) | 2012-05-14 | 2019-11-05 | Antecip Bioventures Ii Llc | Compositions for oral administration of zoledronic acid or related compounds for treating low back pain |
| US10350227B2 (en) | 2012-05-14 | 2019-07-16 | Antecip Bioventures Ii Llc | Neridronic acid for treating complex regional pain syndrome |
| DK2849758T3 (da) * | 2012-05-14 | 2018-05-14 | Antecip Bioventures Ii Llc | Sammensætninger omfattende zoledronsyre eller relaterede forbindelser til at lindre inflammatorisk smerte og relaterede tilstande |
| US10493085B2 (en) | 2012-05-14 | 2019-12-03 | Antecip Bioventures Ii Llc | Neridronic acid and other bisphosphonates for treating complex regional pain syndrome and other diseases |
| US10188617B2 (en) | 2013-03-12 | 2019-01-29 | The Board Of Trustees Of The Leland Stanford Junior University | Modulation of cellular DNA repair activity to intercept malignancy |
| US11406713B2 (en) | 2013-03-15 | 2022-08-09 | Xortx Therapeutics, Inc. | Xanthine oxidase inhibitor formulations |
| AU2014340649C1 (en) * | 2013-10-25 | 2017-05-18 | Antecip Bioventures Ii Llc | Compositions for oral administration of zoledronic acid or related compounds for treating disease |
| CA2997378A1 (en) * | 2015-09-18 | 2017-03-23 | Grunenthal Gmbh | Crystallization method and bioavailability |
| US10195218B2 (en) | 2016-05-31 | 2019-02-05 | Grunenthal Gmbh | Crystallization method and bioavailability |
| KR20180069277A (ko) * | 2016-12-15 | 2018-06-25 | 제이투에이치바이오텍 (주) | 3성분 코크리스탈 |
| GB2571696B (en) | 2017-10-09 | 2020-05-27 | Compass Pathways Ltd | Large scale method for the preparation of Psilocybin and formulations of Psilocybin so produced |
| CA3138008A1 (en) | 2019-04-17 | 2020-10-22 | Compass Pathfinder Limited | Methods of treating neurocognitive disorders, chronic pain and reducing inflammation |
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| US6677320B2 (en) * | 2000-01-20 | 2004-01-13 | Hoffmann-La Roches Inc. | Parenteral bisphosphonate composition with improved local tolerance |
| EP1416919A1 (en) | 2001-07-17 | 2004-05-12 | Teva Pharmaceutical Industries Ltd. | Dosage forms for immediate gastric release of a calcium transport stimulator coupled with delayed gastric release of a bis-phosphonate |
| US20040220264A1 (en) * | 2003-03-17 | 2004-11-04 | Yu Ruey J | Bioavailability and improved delivery of acidic pharmaceutical drugs |
| ES2322592T3 (es) * | 2003-07-03 | 2009-06-23 | Teva Pharmaceutical Industries Ltd. | Formas cristalinas de acido zoledronico, formas cristlinas de la sal sodica de zoledronato, sal sodica de zoledronato amorfa y procedimientos para su preparacion. |
| US20060068010A1 (en) * | 2004-09-30 | 2006-03-30 | Stephen Turner | Method for improving the bioavailability of orally delivered therapeutics |
| JO3006B1 (ar) * | 2005-09-14 | 2016-09-05 | Janssen Pharmaceutica Nv | املاح ليسين مبتكرة من مشتقات حامض 4-((فينوكسي الكيل)ثيو) فينوكسي الخليك |
| AU2010278860B2 (en) * | 2009-07-31 | 2016-05-26 | Thar Pharma, Llc | Crystallization method and bioavailability |
| WO2011014781A1 (en) * | 2009-07-31 | 2011-02-03 | Thar Pharmaceuticals, Inc. | Novel oral forms of a phosphonic acid derivative |
| ES2638072T3 (es) * | 2010-02-06 | 2017-10-18 | Grünenthal GmbH | Método de cristalización y biodisponibilidad |
| US9340565B2 (en) * | 2010-11-24 | 2016-05-17 | Thar Pharmaceuticals, Inc. | Crystalline forms |
| CN102070668B (zh) * | 2010-12-23 | 2013-07-24 | 蚌埠丰原医药科技发展有限公司 | 一种利用相转移催化剂制备唑来膦酸及其钠盐的方法 |
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- 2011-02-02 HU HUE11740284A patent/HUE035744T2/en unknown
- 2011-02-02 WO PCT/US2011/023427 patent/WO2011097269A1/en active Application Filing
- 2011-02-02 PT PT117402842T patent/PT2531200T/pt unknown
- 2011-02-02 DK DK11740284.2T patent/DK2531200T3/da active
- 2011-02-02 CA CA2826548A patent/CA2826548A1/en not_active Abandoned
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2012
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2015
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2016
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2017
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| EP2531200A1 (en) | 2012-12-12 |
| LT2531200T (lt) | 2017-09-25 |
| CA2826548A1 (en) | 2011-08-11 |
| HUE035744T2 (en) | 2018-05-28 |
| PT2531200T (pt) | 2017-08-24 |
| AU2016219653A1 (en) | 2016-09-15 |
| ES2638072T3 (es) | 2017-10-18 |
| WO2011097269A9 (en) | 2012-12-27 |
| JP2013519632A (ja) | 2013-05-30 |
| HRP20171201T1 (hr) | 2017-10-06 |
| EP2531200B1 (en) | 2017-07-12 |
| JP5792748B2 (ja) | 2015-10-14 |
| JP2016006096A (ja) | 2016-01-14 |
| IL221306A0 (en) | 2012-10-31 |
| CY1119192T1 (el) | 2018-02-14 |
| SI2531200T1 (sl) | 2017-12-29 |
| AU2012216632B2 (en) | 2016-05-26 |
| EP2531200A4 (en) | 2014-01-08 |
| AU2016219653B2 (en) | 2018-05-31 |
| PL2531200T3 (pl) | 2017-10-31 |
| WO2011097269A1 (en) | 2011-08-11 |
| JP6190429B2 (ja) | 2017-08-30 |
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