WO2006100527A1 - Comprime effervescent contenant de l’alendronate sodique, utilisation et procede associes - Google Patents
Comprime effervescent contenant de l’alendronate sodique, utilisation et procede associes Download PDFInfo
- Publication number
- WO2006100527A1 WO2006100527A1 PCT/GR2005/000008 GR2005000008W WO2006100527A1 WO 2006100527 A1 WO2006100527 A1 WO 2006100527A1 GR 2005000008 W GR2005000008 W GR 2005000008W WO 2006100527 A1 WO2006100527 A1 WO 2006100527A1
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- sodium
- anhydrous
- composition
- alendronate
- mixing
- Prior art date
Links
- DCSBSVSZJRSITC-UHFFFAOYSA-M alendronate sodium trihydrate Chemical compound O.O.O.[Na+].NCCCC(O)(P(O)(O)=O)P(O)([O-])=O DCSBSVSZJRSITC-UHFFFAOYSA-M 0.000 title claims abstract description 9
- 238000000034 method Methods 0.000 title claims description 11
- 239000007938 effervescent tablet Substances 0.000 title abstract description 10
- 208000001132 Osteoporosis Diseases 0.000 claims abstract description 3
- 239000000203 mixture Substances 0.000 claims description 15
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 claims description 10
- WHNWPMSKXPGLAX-UHFFFAOYSA-N N-Vinyl-2-pyrrolidone Chemical compound C=CN1CCCC1=O WHNWPMSKXPGLAX-UHFFFAOYSA-N 0.000 claims description 7
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 claims description 7
- 229920000036 polyvinylpyrrolidone Polymers 0.000 claims description 7
- 235000005979 Citrus limon Nutrition 0.000 claims description 5
- 244000131522 Citrus pyriformis Species 0.000 claims description 5
- UDIPTWFVPPPURJ-UHFFFAOYSA-M Cyclamate Chemical compound [Na+].[O-]S(=O)(=O)NC1CCCCC1 UDIPTWFVPPPURJ-UHFFFAOYSA-M 0.000 claims description 5
- FBPFZTCFMRRESA-FSIIMWSLSA-N D-Glucitol Natural products OC[C@H](O)[C@H](O)[C@@H](O)[C@H](O)CO FBPFZTCFMRRESA-FSIIMWSLSA-N 0.000 claims description 5
- CDBYLPFSWZWCQE-UHFFFAOYSA-L Sodium Carbonate Chemical compound [Na+].[Na+].[O-]C([O-])=O CDBYLPFSWZWCQE-UHFFFAOYSA-L 0.000 claims description 5
- 229960004543 anhydrous citric acid Drugs 0.000 claims description 5
- 239000000625 cyclamic acid and its Na and Ca salt Substances 0.000 claims description 5
- 239000000796 flavoring agent Substances 0.000 claims description 5
- 239000000843 powder Substances 0.000 claims description 5
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 claims description 5
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 claims description 5
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 claims description 5
- 239000004299 sodium benzoate Substances 0.000 claims description 5
- 235000010234 sodium benzoate Nutrition 0.000 claims description 5
- 229960001462 sodium cyclamate Drugs 0.000 claims description 5
- 239000000600 sorbitol Substances 0.000 claims description 5
- WSVLPVUVIUVCRA-KPKNDVKVSA-N Alpha-lactose monohydrate Chemical compound O.O[C@@H]1[C@@H](O)[C@@H](O)[C@@H](CO)O[C@H]1O[C@@H]1[C@@H](CO)O[C@H](O)[C@H](O)[C@H]1O WSVLPVUVIUVCRA-KPKNDVKVSA-N 0.000 claims description 4
- UIIMBOGNXHQVGW-UHFFFAOYSA-M Sodium bicarbonate Chemical compound [Na+].OC([O-])=O UIIMBOGNXHQVGW-UHFFFAOYSA-M 0.000 claims description 4
- 239000004480 active ingredient Substances 0.000 claims description 4
- 235000019634 flavors Nutrition 0.000 claims description 4
- 239000008187 granular material Substances 0.000 claims description 4
- 229960001021 lactose monohydrate Drugs 0.000 claims description 4
- UIIMBOGNXHQVGW-DEQYMQKBSA-M Sodium bicarbonate-14C Chemical compound [Na+].O[14C]([O-])=O UIIMBOGNXHQVGW-DEQYMQKBSA-M 0.000 claims description 3
- 239000000546 pharmaceutical excipient Substances 0.000 claims description 3
- 229940069328 povidone Drugs 0.000 claims description 3
- OGSPWJRAVKPPFI-UHFFFAOYSA-N Alendronic Acid Chemical compound NCCCC(O)(P(O)(O)=O)P(O)(O)=O OGSPWJRAVKPPFI-UHFFFAOYSA-N 0.000 claims description 2
- 229960004343 alendronic acid Drugs 0.000 claims description 2
- 239000008194 pharmaceutical composition Substances 0.000 claims description 2
- 229910000030 sodium bicarbonate Inorganic materials 0.000 claims description 2
- 235000017557 sodium bicarbonate Nutrition 0.000 claims description 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- CAKRAHQRJGUPIG-UHFFFAOYSA-M sodium;[4-azaniumyl-1-hydroxy-1-[hydroxy(oxido)phosphoryl]butyl]-hydroxyphosphinate Chemical compound [Na+].NCCCC(O)(P(O)(O)=O)P(O)([O-])=O CAKRAHQRJGUPIG-UHFFFAOYSA-M 0.000 claims 2
- FBPFZTCFMRRESA-JGWLITMVSA-N D-glucitol Chemical compound OC[C@H](O)[C@@H](O)[C@H](O)[C@H](O)CO FBPFZTCFMRRESA-JGWLITMVSA-N 0.000 claims 1
- 235000013355 food flavoring agent Nutrition 0.000 claims 1
- 239000002904 solvent Substances 0.000 claims 1
- 239000003826 tablet Substances 0.000 abstract description 6
- 230000009747 swallowing Effects 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 description 3
- 208000018522 Gastrointestinal disease Diseases 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 2
- GUBGYTABKSRVRQ-QKKXKWKRSA-N Lactose Natural products OC[C@H]1O[C@@H](O[C@H]2[C@H](O)[C@@H](O)C(O)O[C@@H]2CO)[C@H](O)[C@@H](O)[C@H]1O GUBGYTABKSRVRQ-QKKXKWKRSA-N 0.000 description 1
- 238000010521 absorption reaction Methods 0.000 description 1
- 239000002253 acid Substances 0.000 description 1
- 210000000988 bone and bone Anatomy 0.000 description 1
- 239000000872 buffer Substances 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 239000008367 deionised water Substances 0.000 description 1
- 229910021641 deionized water Inorganic materials 0.000 description 1
- 201000006549 dyspepsia Diseases 0.000 description 1
- 230000037406 food intake Effects 0.000 description 1
- 210000004051 gastric juice Anatomy 0.000 description 1
- 239000011521 glass Substances 0.000 description 1
- 208000024798 heartburn Diseases 0.000 description 1
- 229960001375 lactose Drugs 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
- -1 monosodium salt Chemical class 0.000 description 1
- 230000001009 osteoporotic effect Effects 0.000 description 1
- 238000010992 reflux Methods 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
Classifications
-
- 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
- A61K9/0002—Galenical forms characterised by the drug release technique; Application systems commanded by energy
- A61K9/0007—Effervescent
-
- 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
-
- 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
- A61K31/662—Phosphorus acids or esters thereof having P—C bonds, e.g. foscarnet, trichlorfon
- A61K31/663—Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid
-
- 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
Definitions
- the present invention relates to the use of effervescent tablet of Sodium Alendronate for an oral osteoporosis treatment in post menopausal women.
- the currently marketed formulation is a tablet and the patient is instructed to take the tablet with a full glass of water.
- Many people suffer from gastrointestinal disorders and particularly from heartburn due to gastro-esophagical reflux.
- the present invention is directed to a new pharmaceutical formulation comprising Sodium Alendronate in the form of effervescent tablet to be taken orally and offering a considerable advantage: avoidance of gastro-intestinal disorders, to the limits of the possible.
- the effervescent tablet of the present invention comprises in addition to the agents producing effervescence a sufficient amount of buffer such that the pH of the obtained aqueous liquid is between approximately 5-7 and particularly 5,9, so that after ingestion the pH of the gastric juice (pH 1,2) raises to a pH of at least 4.
- Another aspect of this invention is that the absorption of the active ingredient is faster when compared to tablet form; consequently an enhanced bioavailability of the active ingredient is probable.
- Method of effervescent tablet preparation Method and process of the preparation of the effervescent tablets are performed in 2 main stages :
- the effervescent tablet of the present invention is prepared by the following process comprising the steps of :
- the effervescent tablet according to the invention has the following composition : Active ingredient
- Lactose monohydrate 31 OOOmg PVP 30 (Povidone) 8,000mg
Landscapes
- Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Physical Education & Sports Medicine (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Orthopedic Medicine & Surgery (AREA)
- Engineering & Computer Science (AREA)
- Rheumatology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Medicinal Preparation (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
La présente invention concerne un comprimé effervescent à usage buccal comprenant de l’alendronate sodique, destiné à traiter et prévenir l’ostéoporose chez les patients ayant du mal à avaler des comprimés classiques.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/GR2005/000008 WO2006100527A1 (fr) | 2005-03-24 | 2005-03-24 | Comprime effervescent contenant de l’alendronate sodique, utilisation et procede associes |
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| PCT/GR2005/000008 WO2006100527A1 (fr) | 2005-03-24 | 2005-03-24 | Comprime effervescent contenant de l’alendronate sodique, utilisation et procede associes |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| WO2006100527A1 true WO2006100527A1 (fr) | 2006-09-28 |
Family
ID=34962994
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/GR2005/000008 WO2006100527A1 (fr) | 2005-03-24 | 2005-03-24 | Comprime effervescent contenant de l’alendronate sodique, utilisation et procede associes |
Country Status (1)
| Country | Link |
|---|---|
| WO (1) | WO2006100527A1 (fr) |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090317460A1 (en) * | 2006-08-24 | 2009-12-24 | Arrow International Limited | Solid dosage form |
| FR2954320A1 (fr) * | 2009-12-17 | 2011-06-24 | Cll Pharma | Composition pharmaceutique orale suprabiodisponible contenant un acide biphosphonique ou un de ses sels |
| CN105796595A (zh) * | 2016-04-06 | 2016-07-27 | 海南师范大学 | 稀土阿伦膦酸盐在制备治疗骨质疏松症药物上的应用 |
Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2153225A (en) * | 1984-01-12 | 1985-08-21 | Gentili Ist Spa | Effervescent preparations containing diphosphonates |
| US5405994A (en) * | 1992-08-05 | 1995-04-11 | Sanofi | Disodium 4-chlorophenylthiomethylenebisphosphonate monohydrate, its preparation and pharmaceutical compositions in which it is present |
| WO1995028936A1 (fr) * | 1994-04-21 | 1995-11-02 | Merck & Co., Inc. | Emploi de biphosphonates inhibant la resorption osseuse consecutive a l'implantation d'une prothese orthopedique |
| WO1997044017A1 (fr) * | 1996-05-17 | 1997-11-27 | Merck & Co., Inc. | Formulation de bisphosphonate efferverscente |
| WO2003086415A1 (fr) * | 2002-04-05 | 2003-10-23 | Merck & Co., Inc. | Procede d'inhibition de resorption osseuse a l'aide d'une formulation a base d'alendronate et de vitamine d |
| WO2004035004A2 (fr) * | 2002-10-17 | 2004-04-29 | Effrx, Inc. | Compositions effervescentes comprenant des bisphosphonates, et procedes correspondants |
-
2005
- 2005-03-24 WO PCT/GR2005/000008 patent/WO2006100527A1/fr not_active Application Discontinuation
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2153225A (en) * | 1984-01-12 | 1985-08-21 | Gentili Ist Spa | Effervescent preparations containing diphosphonates |
| US5405994A (en) * | 1992-08-05 | 1995-04-11 | Sanofi | Disodium 4-chlorophenylthiomethylenebisphosphonate monohydrate, its preparation and pharmaceutical compositions in which it is present |
| WO1995028936A1 (fr) * | 1994-04-21 | 1995-11-02 | Merck & Co., Inc. | Emploi de biphosphonates inhibant la resorption osseuse consecutive a l'implantation d'une prothese orthopedique |
| WO1997044017A1 (fr) * | 1996-05-17 | 1997-11-27 | Merck & Co., Inc. | Formulation de bisphosphonate efferverscente |
| WO2003086415A1 (fr) * | 2002-04-05 | 2003-10-23 | Merck & Co., Inc. | Procede d'inhibition de resorption osseuse a l'aide d'une formulation a base d'alendronate et de vitamine d |
| WO2004035004A2 (fr) * | 2002-10-17 | 2004-04-29 | Effrx, Inc. | Compositions effervescentes comprenant des bisphosphonates, et procedes correspondants |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20090317460A1 (en) * | 2006-08-24 | 2009-12-24 | Arrow International Limited | Solid dosage form |
| US8697124B2 (en) * | 2006-08-24 | 2014-04-15 | Arrow International Limited | Solid dosage form of coated bisphosphonate particles |
| US10420725B2 (en) | 2006-08-24 | 2019-09-24 | Allergan Pharmaceuticals International Limited | Solid dosage form of coated bisphosphonate particles |
| FR2954320A1 (fr) * | 2009-12-17 | 2011-06-24 | Cll Pharma | Composition pharmaceutique orale suprabiodisponible contenant un acide biphosphonique ou un de ses sels |
| WO2011080413A1 (fr) * | 2009-12-17 | 2011-07-07 | Cll Pharma | Composition pharmaceutique orale solide suprabiodisponible contenant un acide biphosphonique ou un de ses sels |
| CN105796595A (zh) * | 2016-04-06 | 2016-07-27 | 海南师范大学 | 稀土阿伦膦酸盐在制备治疗骨质疏松症药物上的应用 |
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