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WO2006100527A1 - Effervescent tablet containing sodium alendronate and related use and process - Google Patents

Effervescent tablet containing sodium alendronate and related use and process Download PDF

Info

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
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.)
Ceased
Application number
PCT/GR2005/000008
Other languages
French (fr)
Inventor
Ioulia Tseti
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Uni Pharma Kleon Tsetis Pharmaceutical Laboratories SA
Original Assignee
Uni Pharma Kleon Tsetis Pharmaceutical Laboratories SA
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Uni Pharma Kleon Tsetis Pharmaceutical Laboratories SA filed Critical Uni Pharma Kleon Tsetis Pharmaceutical Laboratories SA
Priority to PCT/GR2005/000008 priority Critical patent/WO2006100527A1/en
Publication of WO2006100527A1 publication Critical patent/WO2006100527A1/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

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

An effervescent tablet comprising Sodium Alendronate for oral use, in treating and preventing osteoporosis in patients who have difficulty in swallowing conventional tablets.

Description

Effervescent tablet containing Sodium Alendronate and related use and process
DESCRIPTION
Field of the invention The present invention relates to the use of effervescent tablet of Sodium Alendronate for an oral osteoporosis treatment in post menopausal women.
Background of the invention
It is well known that Sodium Alendronate (4-amino-l-hydroxy- butilidene-l,l-bisphosphonic acid monosodium salt) has been approved since many years ago, for the efficacious therapy of patients with bone mass loss and particularly 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. Furthermore, there is a category of patients that cannot or they are fearful to swallow tablets.
In order to overcome this disadvantage of the tablet, it would be desirable to develop a formulation, which would be acceptable of the totality of osteoporotic patients.
Detailed description of the invention
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 :
In detail, the effervescent tablet of the present invention is prepared by the following process comprising the steps of :
(a) Preparing granules of Sodium Alendronate plus Lactose with the aid of a solution consisting of PVP 30 and deionized water already pre-warmed at 70° C.
(b) The granules prepared by the above process are mixed with a mixture consisting of Sorbitol DC and Anhydrous Citric acid.
(c) Mixing of Anhydrous Sodium Bicarbonate, Anhydrous Sodium Carbonate, Sodium Benzoate, Sodium Saccharinate and Sodium Cyclamate.
(d) Mixing of the resulted mixtures of (b) and (c) process and addition Lemon flavor powder.
The effervescent tablet according to the invention has the following composition : Active ingredient
Sodium Alendronate 91 ,350mg*
Excipients
Lactose monohydrate 31 , OOOmg PVP 30 (Povidone) 8,000mg
Anhydrous Citric acid 500, OOOmg
Anhydrous Sodium bicarbonate 550, OOOmg
Anhydrous Sodium carbonate 110, OOOmg
Sorbitol DC 20/60 799,650mg Sodium Saccharinate 15, OOOmg
Sodium benzoate 10, OOOmg
Lemon flavor (powder) 25, OOOmg
Sodium cyclamate 10, OOOmg * corresponds to 70mg Alendronic acid
The invention is defined by the appended claims.

Claims

C L A I M S
1. An effervescent pharmaceutical composition for oral use in the treatment of osteoporosis comprising a therapeutically effective amount of Sodium Alendronate and Lactose Monohydrate, PVP 30 (Povidone), Anhydrous Citric acid, Anhydrous Sodium bicarbonate, Anhydrous Sodium carbonate, Sorbitol DC 20/60, Sodium Saccharinate, Sodium Benzoate, Sodium Cyclamate and Lemon flavor (powder) as excipients.
2. Composition according to claim 1 in form of tablet.
3. An effervescent composition according to claim 2, having the following composition :
Active ingredient
Sodium Alendronate 91 ,350mg* Excipients
Lactose monohydrate 31,000mg
PVP 30 (Povidone) 8,000mg
Anhydrous Citric acid 500,000mg
Anhydrous Sodium bicarbonate 550,000mg Anhydrous Sodium carbonate 110,000mg
Sorbitol DC 20/60 799,650mg
Sodium Saccharinate 15,000mg
Sodium benzoate 10,000mg
Lemon flavor (powder) 25,000mg Sodium cyclamate 10,000mg
* corresponds to 70mg Alendronic acid
4. Process for preparing the effervesent composition of anyone of the claims 1, 2 or 3.
5. Process for making an effervescent composition comprising mixing together Sodium Alendronate and Lactose Monohydrate in a solvent system and forming said mixture into granules.
6. Process of mixing said granules of claim 5 with Sorbitol DC 20/60 and Anhydrous Citric acid.
7. Process of mixing Anhydrous Sodium Bicarbonate, Anhydrous Sodium Carbonate, Sodium Benzoate, Sodium Saccharinate and
Sodium Cyclamate.
8. Process of mixing the blends resulted according to the claims 6 and 7 to the final blend of which the flavoring agent (Lemon powder) is added.
9. Tableting the blend obtained according to claim 8 into tablets.
10. Process for preparing the effervesent composition of anyone of the claims 1, 2 or 3 by the process according to anyone or any combination of claims 5-9.
PCT/GR2005/000008 2005-03-24 2005-03-24 Effervescent tablet containing sodium alendronate and related use and process Ceased WO2006100527A1 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
PCT/GR2005/000008 WO2006100527A1 (en) 2005-03-24 2005-03-24 Effervescent tablet containing sodium alendronate and related use and process

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/GR2005/000008 WO2006100527A1 (en) 2005-03-24 2005-03-24 Effervescent tablet containing sodium alendronate and related use and process

Publications (1)

Publication Number Publication Date
WO2006100527A1 true WO2006100527A1 (en) 2006-09-28

Family

ID=34962994

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/GR2005/000008 Ceased WO2006100527A1 (en) 2005-03-24 2005-03-24 Effervescent tablet containing sodium alendronate and related use and process

Country Status (1)

Country Link
WO (1) WO2006100527A1 (en)

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20090317460A1 (en) * 2006-08-24 2009-12-24 Arrow International Limited Solid dosage form
FR2954320A1 (en) * 2009-12-17 2011-06-24 Cll Pharma SUPPLEMENTALLY AVAILABLE ORAL PHARMACEUTICAL COMPOSITION CONTAINING BIPHOSPHONIC ACID OR ONE OF ITS SALTS
CN105796595A (en) * 2016-04-06 2016-07-27 海南师范大学 Application of rare earth alendronate in preparation of osteoporosis treatment drug

Citations (6)

* Cited by examiner, † Cited by third party
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 (en) * 1994-04-21 1995-11-02 Merck & Co., Inc. Use of bisphophonates for inhibiting bone resorption following implantation of orthopedic prosthesis
WO1997044017A1 (en) * 1996-05-17 1997-11-27 Merck & Co., Inc. Effervescent bisphosphonate formulation
WO2003086415A1 (en) * 2002-04-05 2003-10-23 Merck & Co., Inc. Method for inhibiting bone resorption with an alendronate and vitamin d formulation
WO2004035004A2 (en) * 2002-10-17 2004-04-29 Effrx, Inc. Effervescent compositions comprising bisphosphonates and methods related thereto

Patent Citations (6)

* Cited by examiner, † Cited by third party
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 (en) * 1994-04-21 1995-11-02 Merck & Co., Inc. Use of bisphophonates for inhibiting bone resorption following implantation of orthopedic prosthesis
WO1997044017A1 (en) * 1996-05-17 1997-11-27 Merck & Co., Inc. Effervescent bisphosphonate formulation
WO2003086415A1 (en) * 2002-04-05 2003-10-23 Merck & Co., Inc. Method for inhibiting bone resorption with an alendronate and vitamin d formulation
WO2004035004A2 (en) * 2002-10-17 2004-04-29 Effrx, Inc. Effervescent compositions comprising bisphosphonates and methods related thereto

Cited By (6)

* Cited by examiner, † Cited by third party
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 (en) * 2009-12-17 2011-06-24 Cll Pharma SUPPLEMENTALLY AVAILABLE ORAL PHARMACEUTICAL COMPOSITION CONTAINING BIPHOSPHONIC ACID OR ONE OF ITS SALTS
WO2011080413A1 (en) * 2009-12-17 2011-07-07 Cll Pharma Enhanced bioavailability solid oral pharmaceutical composition containing a biphosphonic acid or one of the salts thereof
CN105796595A (en) * 2016-04-06 2016-07-27 海南师范大学 Application of rare earth alendronate in preparation of osteoporosis treatment drug

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