Liquid alendronate formulations and their use in preventing bone resorption

• Main Authors: NERURKAR, MANEESH J, HUNKE, WILLIAM A, OSTOVICAZEN
• Format: Patent
• Language: English
• Published: 24.11.2000
• Edition: 7
• Subjects: HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

An aqueous liquid pharmaceutical formulation comprising: 1).alendronic acid or a pharmaceutically acceptable salt as an active ingredient; 2).a sufficient amount of a buffer such that: a) the pH of the formulation is between approximately 3.5 and approximately 7.5; and b) 15 ml of the formulation is able to raise the pH of 50 ml 0.1N HCl to a pH of at least 3; and optionally, one or more additional agents selected from the group consisting of preservatives, flavouring agents, colorants, and sweeteners. More particularly, the formulation comprises: (in mg/ml): alendronate monosodium trihydrate 0.2-0.9 (on an alendronic acid basis) sodium benzoate 1.0-2.0 sodium citrate dihydrate 75-125 citric acid, anhydrous 0.340 xylitol 100-640 Also disclosed is the use of alendronic acid as a medicament for inhibiting bone resorption. An aqueous liquid pharmaceutical formulation comprising: 1) alendronic acid or a pharmaceutically acceptable salt as an active ingredient; 2) a sufficient amount of a buffer such that: a) the pH of the formulation is between approximately 3.5 and approximately 7.5; and b) 15 ml of the formulation is able to raise the pH of 50 ml 0.1N HCl to a pH of at least 3; and optionally, one or more additional agents selected from the group consisting of preservatives, flavouring agents, colorants, and sweeteners. More particularly, the formulation comprises: (in mg/ml): alendronate monosodium trihydrate 0.2-0.9 (on an alendronic acid basis) sodium benzoate 1.0-2.0 sodium citrate dihydrate 75-125 citric acid, anhydrous 0.340 xylitol 100-640 Also disclosed is the use of alendronic acid as a medicament for inhibiting bone resorption.